Wellbutrin Tablets

Generic Name: bupropion hydrochloride

Dosage Form: tablet, film coated
WELLBUTRIN®

(bupropion hydrochloride)

Tablets

Warning

Suicidality and Antidepressant Drugs

Use in Treating Psychiatric Disorders: Antidepressants increased the risk compared to placebo of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults in short-term studies of major depressive disorder (MDD) and other psychiatric disorders. Anyone considering the use of WELLBUTRIN or any other antidepressant in a child, adolescent, or young adult must balance this risk with the clinical need. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24; there was a reduction in risk with antidepressants compared to placebo in adults aged 65 and older. Depression and certain other psychiatric disorders are themselves associated with increases in the risk of suicide. Patients of all ages who are started on antidepressant therapy should be monitored appropriately and observed closely for clinical worsening, suicidality, or unusual changes in behavior. Families and caregivers should be advised of the need for close observation and communication with the prescriber. WELLBUTRIN is not approved for use in pediatric patients. (See WARNINGS: Clinical Worsening and Suicide Risk in Treating Psychiatric Disorders, PRECAUTIONS: Information for Patients, and PRECAUTIONS: Pediatric Use.)

Use in Smoking Cessation Treatment: WELLBUTRIN®, WELLBUTRIN SR®, and WELLBUTRIN XL® are not approved for smoking cessation treatment, but bupropion under the name ZYBAN® is approved for this use. Serious neuropsychiatric events, including but not limited to depression, suicidal ideation, suicide attempt, and completed suicide have been reported in patients taking bupropion for smoking cessation. Some cases may have been complicated by the symptoms of nicotine withdrawal in patients who stopped smoking. Depressed mood may be a symptom of nicotine withdrawal. Depression, rarely including suicidal ideation, has been reported in smokers undergoing a smoking cessation attempt without medication. However, some of these symptoms have occurred in patients taking bupropion who continued to smoke.

All patients being treated with bupropion for smoking cessation treatment should be observed for neuropsychiatric symptoms including changes in behavior, hostility, agitation, depressed mood, and suicide-related events, including ideation, behavior, and attempted suicide. These symptoms, as well as worsening of pre-existing psychiatric illness and completed suicide have been reported in some patients attempting to quit smoking while taking ZYBAN in the postmarketing experience. When symptoms were reported, most were during treatment with ZYBAN, but some were following discontinuation of treatment with ZYBAN. These events have occurred in patients with and without pre-existing psychiatric disease; some have experienced worsening of their psychiatric illnesses. Patients with serious psychiatric illness such as schizophrenia, bipolar disorder, and major depressive disorder did not participate in the premarketing studies of ZYBAN.

Advise patients and caregivers that the patient using bupropion for smoking cessation should stop taking bupropion and contact a healthcare provider immediately if agitation, hostility, depressed mood, or changes in thinking or behavior that are not typical for the patient are observed, or if the patient develops suicidal ideation or suicidal behavior. In many postmarketing cases, resolution of symptoms after discontinuation of ZYBAN was reported, although in some cases the symptoms persisted; therefore, ongoing monitoring and supportive care should be provided until symptoms resolve.

The risks of using bupropion for smoking cessation should be weighed against the benefits of its use. ZYBAN has been demonstrated to increase the likelihood of abstinence from smoking for as long as 6 months compared to treatment with placebo. The health benefits of quitting smoking are immediate and substantial. (See WARNINGS: Neuropsychiatric Symptoms and Suicide Risk in Smoking Cessation Treatment and PRECAUTIONS: Information for Patients.)

Wellbutrin Tablets Description

WELLBUTRIN (bupropion hydrochloride), an antidepressant of the aminoketone class, is chemically unrelated to tricyclic, tetracyclic, selective serotonin re-uptake inhibitor, or other known antidepressant agents. Its structure closely resembles that of diethylpropion; it is related to phenylethylamines. It is designated as (±)-1-(3-chlorophenyl)-2-[(1,1-dimethylethyl)amino]-1-propanone hydrochloride. The molecular weight is 276.2. The empirical formula is C13H18ClNO•HCl. Bupropion hydrochloride powder is white, crystalline, and highly soluble in water. It has a bitter taste and produces the sensation of local anesthesia on the oral mucosa. The structural formula is:

WELLBUTRIN is supplied for oral administration as 75-mg (yellow-gold) and 100-mg (red) film-coated tablets. Each tablet contains the labeled amount of bupropion hydrochloride and the inactive ingredients: 75-mg tablet − D&C Yellow No. 10 Lake, FD&C Yellow No. 6 Lake, hydroxypropyl cellulose, hypromellose, microcrystalline cellulose, polyethylene glycol, talc, and titanium dioxide; 100-mg tablet − FD&C Red No. 40 Lake, FD&C Yellow No. 6 Lake, hydroxypropyl cellulose, hypromellose, microcrystalline cellulose, polyethylene glycol, talc, and titanium dioxide.

Wellbutrin Tablets - Clinical Pharmacology

Pharmacodynamics

The neurochemical mechanism of the antidepressant effect of bupropion is not known. Bupropion is a relatively weak inhibitor of the neuronal uptake of norepinephrine and dopamine, and does not inhibit monoamine oxidase or the re-uptake of serotonin.

Bupropion produces dose-related central nervous system (CNS) stimulant effects in animals, as evidenced by increased locomotor activity, increased rates of responding in various schedule-controlled operant behavior tasks, and, at high doses, induction of mild stereotyped behavior.

Bupropion causes convulsions in rodents and dogs at doses approximately tenfold the dose recommended as the human antidepressant dose.

Pharmacokinetics

Bupropion is a racemic mixture. The pharmacological activity and pharmacokinetics of the individual enantiomers have not been studied. In humans, following oral administration of WELLBUTRIN, peak plasma bupropion concentrations are usually achieved within 2 hours, followed by a biphasic decline. The terminal phase has a mean half-life of 14 hours, with a range of 8 to 24 hours. The distribution phase has a mean half-life of 3 to 4 hours. The mean elimination half-life (±SD) of bupropion after chronic dosing is 21 (±9) hours, and steady-state plasma concentrations of bupropion are reached within 8 days. Plasma bupropion concentrations are dose-proportional following single doses of 100 to 250 mg; however, it is not known if the proportionality between dose and plasma level is maintained in chronic use.

Absorption:The absolute bioavailability of WELLBUTRIN in humans has not been determined because an intravenous formulation for human use is not available. However, it appears likely that only a small proportion of any orally administered dose reaches the systemic circulation intact.

Distribution: In vitro tests show that bupropion is 84% bound to human plasma protein at concentrations up to 200 mcg/mL. The extent of protein binding of the hydroxybupropion metabolite is similar to that for bupropion, whereas the extent of protein binding of the threohydrobupropion metabolite is about half that seen with bupropion.

Metabolism: Bupropion is extensively metabolized in humans. Three metabolites have been shown to be active: hydroxybupropion, which is formed via hydroxylation of the tert-butyl group of bupropion, and the amino-alcohol isomers threohydrobupropion and erythrohydrobupropion, which are formed via reduction of the carbonyl group. In vitro findings suggest that cytochrome P450IIB6 (CYP2B6) is the principal isoenzyme involved in the formation of hydroxybupropion, while cytochrome P450 isoenzymes are not involved in the formation of threohydrobupropion. Oxidation of the bupropion side chain results in the formation of a glycine conjugate of meta-chlorobenzoic acid, which is then excreted as the major urinary metabolite. The potency and toxicity of the metabolites relative to bupropion have not been fully characterized. However, it has been demonstrated in an antidepressant screening test in mice that hydroxybupropion is one-half as potent as bupropion, while threohydrobupropion and erythrohydrobupropion are 5-fold less potent than bupropion. This may be of clinical importance because their plasma concentrations are as high or higher than those of bupropion.

Because bupropion is extensively metabolized, there is the potential for drug-drug interactions, particularly with those agents that are metabolized by or which inhibit/induce the cytochrome P450IIB6 (CYP2B6) isoenzyme, such as ritonavir or efavirenz. In a healthy volunteer study, ritonavir at a dose of 100 mg twice daily reduced the AUC and Cmax of bupropion by 22% and 21%, respectively. The exposure of the hydroxybupropion metabolite was decreased by 23%, the threohydrobupropion decreased by 38%, and the erythrohydrobupropion decreased by 48%.

In a second healthy volunteer study, ritonavir at a dose of 600 mg twice daily decreased the AUC and the Cmax of bupropion by 66% and 62%, respectively. The exposure of the hydroxybupropion metabolite was decreased by 78%, the threohydrobupropion decreased by 50%, and the erythrohydrobupropion decreased by 68%.

In another healthy volunteer study, KALETRA® (lopinavir 400 mg/ritonavir 100 mg twice daily) decreased bupropion AUC and Cmax by 57%. The AUC and Cmax of hydroxybupropion were decreased by 50% and 31%, respectively (see PRECAUTIONS: Drug Interactions).

In a study in healthy volunteers, efavirenz 600 mg once daily for 2 weeks reduced the AUC and Cmax of bupropion by approximately 55% and 34%, respectively. The AUC of hydroxybupropion was unchanged, whereas Cmax of hydroxybupropion was increased by 50%.

Although bupropion is not metabolized by cytochrome P450IID6 (CYP2D6), there is the potential for drug-drug interactions when bupropion is coadministered with drugs metabolized by this isoenzyme (see PRECAUTIONS: Drug Interactions).

Following a single dose in humans, peak plasma concentrations of hydroxybupropion occur approximately 3 hours after administration of WELLBUTRIN. Peak plasma concentrations of hydroxybupropion are approximately 10 times the peak level of the parent drug at steady state. The elimination half-life of hydroxybupropion is approximately 20 (±5) hours and its AUC at steady state is about 17 times that of bupropion. The times to peak concentrations for the erythrohydrobupropion and threohydrobupropion metabolites are similar to that of the hydroxybupropion metabolite. However, their elimination half-lives are longer, 33 (±10) and 37 (±13) hours, respectively, and steady-state AUCs are 1.5 and 7 times that of bupropion, respectively.

Bupropion and its metabolites exhibit linear kinetics following chronic administration of 300 to 450 mg/day.

Elimination: Following oral administration of 200 mg of 14C-bupropion in humans, 87% and 10% of the radioactive dose were recovered in the urine and feces, respectively. However, the fraction of the oral dose of WELLBUTRIN excreted unchanged was only 0.5%, a finding consistent with the extensive metabolism of bupropion.

Populations Subgroups: Factors or conditions altering metabolic capacity (e.g., liver disease, congestive heart failure [CHF], age, concomitant medications, etc.) or elimination may be expected to influence the degree and extent of accumulation of the active metabolites of bupropion. The elimination of the major metabolites of bupropion may be affected by reduced renal or hepatic function because they are moderately polar compounds and are likely to undergo further metabolism or conjugation in the liver prior to urinary excretion.

Hepatic: The effect of hepatic impairment on the pharmacokinetics of bupropion was characterized in 2 single-dose studies, one in patients with alcoholic liver disease and one in patients with mild-to-severe cirrhosis. The first study showed that the half-life of hydroxybupropion was significantly longer in 8 patients with alcoholic liver disease than in 8 healthy volunteers (32 ± 14 hours versus 21 ± 5 hours, respectively). Although not statistically significant, the AUCs for bupropion and hydroxybupropion were more variable and tended to be greater (by 53% to 57%) in volunteers with alcoholic liver disease. The differences in half-life for bupropion and the other metabolites in the 2 patient groups were minimal.

The second study showed that there were no statistically significant differences in the pharmacokinetics of bupropion and its active metabolites in 9 patients with mild-to-moderate hepatic cirrhosis compared to 8 healthy volunteers. However, more variability was observed in some of the pharmacokinetic parameters for bupropion (AUC, Cmax, and Tmax) and its active metabolites (t½) in patients with mild-to-moderate hepatic cirrhosis. In addition, in patients with severe hepatic cirrhosis, the bupropion Cmax and AUC were substantially increased (mean difference: by approximately 70% and 3-fold, respectively) and more variable when compared to values in healthy volunteers; the mean bupropion half-life was also longer (29 hours in patients with severe hepatic cirrhosis vs. 19 hours in healthy subjects). For the metabolite hydroxybupropion, the mean Cmax was approximately 69% lower. For the combined amino-alcohol isomers threohydrobupropion and erythrohydrobupropion, the mean Cmax was approximately 31% lower. The mean AUC increased by about 1½-fold for hydroxybupropion and about 2½-fold for threo/erythrohydrobupropion. The median Tmax was observed 19 hours later for hydroxybupropion and 31 hours later for threo/erythrohydrobupropion. The mean half-lives for hydroxybupropion and threo/erythrohydrobupropion were increased 5- and 2-fold, respectively, in patients with severe hepatic cirrhosis compared to healthy volunteers (see WARNINGS, PRECAUTIONS, and DOSAGE AND ADMINISTRATION).

Renal: There is limited information on the pharmacokinetics of bupropion in patients with renal impairment. An inter-study comparison between normal subjects and patients with end-stage renal failure demonstrated that the parent drug Cmax and AUC values were comparable in the 2 groups, whereas the hydroxybupropion and threohydrobupropion metabolites had a 2.3– and 2.8–fold increase, respectively, in AUC for patients with end-stage renal failure. A second study, comparing normal subjects and patients with moderate-to-severe renal impairment (GFR 30.9 ± 10.8 mL/min) showed that exposure to a single 150-mg dose of sustained-release bupropion was approximately 2-fold higher in patients with impaired renal function while levels of the hydroxybupropion and threo/erythrohydrobupropion (combined) metabolites were similar in the 2 groups. The elimination of bupropion and/or the major metabolites of bupropion may be reduced by impaired renal function (see PRECAUTIONS: Renal Impairment).

During a chronic dosing study in 14 depressed patients with left ventricular dysfunction (history of CHF or an enlarged heart on x-ray), no apparent effect on the pharmacokinetics of bupropion or its metabolites was revealed, compared to healthy volunteers.

Left Ventricular Dysfunction: The effects of age on the pharmacokinetics of bupropion and its metabolites have not been fully characterized, but an exploration of steady-state bupropion concentrations from several depression efficacy studies involving patients dosed in a range of 300 to 750 mg/day, on a 3 times daily schedule, revealed no relationship between age (18 to 83 years) and plasma concentration of bupropion. A single-dose pharmacokinetic study demonstrated that the disposition of bupropion and its metabolites in elderly subjects was similar to that of younger subjects. These data suggest there is no prominent effect of age on bupropion concentration; however, another pharmacokinetic study, single and multiple dose, has suggested that the elderly are at increased risk for accumulation of bupropion and its metabolites (see PRECAUTIONS: Geriatric Use).

Gender:A single-dose study involving 12 healthy male and 12 healthy female volunteers revealed no sex-related differences in the pharmacokinetic parameters of bupropion.

Smokers: The effects of cigarette smoking on the pharmacokinetics of bupropion were studied in 34 healthy male and female volunteers; 17 were chronic cigarette smokers and 17 were nonsmokers. Following oral administration of a single 150-mg dose of bupropion, there were no statistically significant differences in Cmax, half-life, Tmax, AUC or clearance of bupropion or its active metabolites between smokers and nonsmokers.

Indications and Usage for Wellbutrin Tablets

WELLBUTRIN is indicated for the treatment of major depressive disorder. A physician considering WELLBUTRIN for the management of a patient’s first episode of depression should be aware that the drug may cause generalized seizures in a dose-dependent manner with an approximate incidence of 0.4% (4/1,000). This incidence of seizures may exceed that of other marketed antidepressants by as much as 4-fold. This relative risk is only an approximate estimate because no direct comparative studies have been conducted (see WARNINGS).

The efficacy of WELLBUTRIN has been established in 3 placebo-controlled trials, including 2 of approximately 3 weeks’ duration in depressed inpatients and one of approximately 6 weeks’ duration in depressed outpatients. The depressive disorder of the patients studied corresponds most closely to the Major Depression category of the APA Diagnostic and Statistical Manual III.

Major Depression implies a prominent and relatively persistent depressed or dysphoric mood that usually interferes with daily functioning (nearly every day for at least 2 weeks); it should include at least 4 of the following 8 symptoms: change in appetite, change in sleep, psychomotor agitation or retardation, loss of interest in usual activities or decrease in sexual drive, increased fatigability, feelings of guilt or worthlessness, slowed thinking or impaired concentration, and suicidal ideation or attempts.

Effectiveness of WELLBUTRIN in long-term use, that is, for more than 6 weeks, has not been systematically evaluated in controlled trials. Therefore, the physician who elects to use WELLBUTRIN for extended periods should periodically reevaluate the long-term usefulness of the drug for the individual patient.

Contraindications

WELLBUTRIN is contraindicated in patients with a seizure disorder.

WELLBUTRIN is contraindicated in patients treated with ZYBAN® (bupropion hydrochloride) Sustained-Release Tablets; WELLBUTRIN SR® (bupropion hydrochloride), the sustained-release formulation; WELLBUTRIN XL® (bupropion hydrochloride), the extended-release formulation; or any other medications that contain bupropion because the incidence of seizure is dose dependent.

WELLBUTRIN is contraindicated in patients with a current or prior diagnosis of bulimia or anorexia nervosa because of a higher incidence of seizures noted in such patients treated with WELLBUTRIN.

WELLBUTRIN is contraindicated in patients undergoing abrupt discontinuation of alcohol or sedatives (including benzodiazepines).

The concurrent administration of WELLBUTRIN and a monoamine oxidase (MAO) inhibitor is contraindicated. At least 14 days should elapse between discontinuation of an MAO inhibitor and initiation of treatment with WELLBUTRIN.

WELLBUTRIN is contraindicated in patients who have shown an allergic response to bupropion or the other ingredients that make up WELLBUTRIN.

Warnings

Clinical Worsening and Suicide Risk in Treating Psychiatric Disorders

Patients with major depressive disorder (MDD), both adult and pediatric, may experience worsening of their depression and/or the emergence of suicidal ideation and behavior (suicidality) or unusual changes in behavior, whether or not they are taking antidepressant medications, and this risk may persist until significant remission occurs. Suicide is a known risk of depression and certain other psychiatric disorders, and these disorders themselves are the strongest predictors of suicide. There has been a long-standing concern, however, that antidepressants may have a role in inducing worsening of depression and the emergence of suicidality in certain patients during the early phases of treatment. Pooled analyses of short-term placebo-controlled trials of antidepressant drugs (SSRIs and others) showed that these drugs increase the risk of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults (ages 18-24) with major depressive disorder (MDD) and other psychiatric disorders. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24; there was a reduction with antidepressants compared to placebo in adults aged 65 and older.

The pooled analyses of placebo-controlled trials in children and adolescents with MDD, obsessive compulsive disorder (OCD), or other psychiatric disorders included a total of 24 short-term trials of 9 antidepressant drugs in over 4,400 patients. The pooled analyses of placebo-controlled trials in adults with MDD or other psychiatric disorders included a total of 295 short-term trials (median duration of 2 months) of 11 antidepressant drugs in over 77,000 patients. There was considerable variation in risk of suicidality among drugs, but a tendency toward an increase in the younger patients for almost all drugs studied. There were differences in absolute risk of suicidality across the different indications, with the highest incidence in MDD. The risk differences (drug vs. placebo), however, were relatively stable within age strata and across indications. These risk differences (drug-placebo difference in the number of cases of suicidality per 1,000 patients treated) are provided in Table 1.

Table 1

Age Range	Drug-Placebo Difference in Number of Cases of Suicidality per 1,000 Patients Treated
Increases Compared to Placebo
<18	14 additional cases
18-24	5 additional cases
Decreases Compared to Placebo
25-64	1 fewer case
≥65	6 fewer cases

No suicides occurred in any of the pediatric trials. There were suicides in the adult trials, but the number was not sufficient to reach any conclusion about drug effect on suicide.

It is unknown whether the suicidality risk extends to longer-term use, i.e., beyond several months. However, there is substantial evidence from placebo-controlled maintenance trials in adults with depression that the use of antidepressants can delay the recurrence of depression.

All patients being treated with antidepressants for any indication should be monitored appropriately and observed closely for clinical worsening, suicidality, and unusual changes in behavior, especially during the initial few months of a course of drug therapy, or at times of dose changes, either increases or decreases.

The following symptoms, anxiety, agitation, panic attacks, insomnia, irritability, hostility, aggressiveness, impulsivity, akathisia (psychomotor restlessness), hypomania, and mania, have been reported in adult and pediatric patients being treated with antidepressants for major depressive disorder as well as for other indications, both psychiatric and nonpsychiatric. Although a causal link between the emergence of such symptoms and either the worsening of depression and/or the emergence of suicidal impulses has not been established, there is concern that such symptoms may represent precursors to emerging suicidality.

Consideration should be given to changing the therapeutic regimen, including possibly discontinuing the medication, in patients whose depression is persistently worse, or who are experiencing emergent suicidality or symptoms that might be precursors to worsening depression or suicidality, especially if these symptoms are severe, abrupt in onset, or were not part of the patient's presenting symptoms.

Families and caregivers of patients being treated with antidepressants for major depressive disorder or other indications, both psychiatric and nonpsychiatric, should be alerted about the need to monitor patients for the emergence of agitation, irritability, unusual changes in behavior, and the other symptoms described above, as well as the emergence of suicidality, and to report such symptoms immediately to healthcare providers. Such monitoring should include daily observation by families and caregivers. Prescriptions for WELLBUTRIN should be written for the smallest quantity of tablets consistent with good patient management, in order to reduce the risk of overdose.

Neuropsychiatric Symptoms and Suicide Risk in Smoking Cessation Treatment: WELLBUTRIN, WELLBUTRIN SR, and WELLBUTRIN XL are not approved for smoking cessation treatment, but bupropion under the name ZYBAN is approved for this use. Serious neuropsychiatric symptoms have been reported in patients taking bupropion for smoking cessation (see BOXED WARNING, ADVERSE REACTIONS). These have included changes in mood (including depression and mania), psychosis, hallucinations, paranoia, delusions, homicidal ideation, hostility, agitation, aggression, anxiety, and panic, as well as suicidal ideation, suicide attempt, and completed suicide. Some reported cases may have been complicated by the symptoms of nicotine withdrawal in patients who stopped smoking. Depressed mood may be a symptom of nicotine withdrawal. Depression, rarely including suicidal ideation, has been reported in smokers undergoing a smoking cessation attempt without medication. However, some of these symptoms have occurred in patients taking bupropion who continued to smoke. When symptoms were reported, most were during bupropion treatment, but some were following discontinuation of bupropion therapy.

These events have occurred in patients with and without pre-existing psychiatric disease; some have experienced worsening of their psychiatric illnesses. All patients being treated with bupropion as part of smoking cessation treatment should be observed for neuropsychiatric symptoms or worsening of pre-existing psychiatric illness.

Patients with serious psychiatric illness such as schizophrenia, bipolar disorder, and major depressive disorder did not participate in the pre-marketing studies of ZYBAN.

Advise patients and caregivers that the patient using bupropion for smoking cessation should stop taking bupropion and contact a healthcare provider immediately if agitation, depressed mood, or changes in behavior or thinking that are not typical for the patient are observed, or if the patient develops suicidal ideation or suicidal behavior. In many postmarketing cases, resolution of symptoms after discontinuation of ZYBAN was reported, although in some cases the symptoms persisted, therefore, ongoing monitoring and supportive care should be provided until symptoms resolve.

The risks of using bupropion for smoking cessation should be weighed against the benefits of its use. ZYBAN has been demonstrated to increase the likelihood of abstinence from smoking for as long as six months compared to treatment with placebo. The health benefits of quitting smoking are immediate and substantial.

Screening Patients for Bipolar Disorder

 A major depressive episode may be the initial presentation of bipolar disorder. It is generally believed (though not established in controlled trials) that treating such an episode with an antidepressant alone may increase the likelihood of precipitation of a mixed/manic episode in patients at risk for bipolar disorder. Whether any of the symptoms described above represent such a conversion is unknown. However, prior to initiating treatment with an antidepressant, patients with depressive symptoms should be adequately screened to determine if they are at risk for bipolar disorder; such screening should include a detailed psychiatric history, including a family history of suicide, bipolar disorder, and depression. It should be noted that WELLBUTRIN is not approved for use in treating bipolar depression.

Bupropion-Containing Products

Patients should be made aware that WELLBUTRIN contains the same active ingredient found in ZYBAN, used as an aid to smoking cessation treatment, and that WELLBUTRIN should not be used in combination with ZYBAN, or any other medications that contain bupropion, such as WELLBUTRIN SR (bupropion hydrochloride), the sustained-release formulation or WELLBUTRIN XL (bupropion hydrochloride), the extended-release formulation.

Seizures

Bupropion is associated with seizures in approximately 0.4% (4/1,000) of patients treated at doses up to 450 mg/day. This incidence of seizures may exceed that of other marketed antidepressants by as much as 4-fold. This relative risk is only an approximate estimate because no direct comparative studies have been conducted. The estimated seizure incidence for WELLBUTRIN increases almost tenfold between 450 and 600 mg/day, which is twice the usually required daily dose (300 mg) and one and one-third the maximum recommended daily dose (450 mg). Given the wide variability among individuals and their capacity to metabolize and eliminate drugs this disproportionate increase in seizure incidence with dose incrementation calls for caution in dosing.

During the initial development, 25 among approximately 2,400 patients treated with WELLBUTRIN experienced seizures. At the time of seizure, 7 patients were receiving daily doses of 450 mg or below for an incidence of 0.33% (3/1,000) within the recommended dose range. Twelve patients experienced seizures at 600 mg/day (2.3% incidence); 6 additional patients had seizures at daily doses between 600 and 900 mg (2.8% incidence).

A separate, prospective study was conducted to determine the incidence of seizure during an 8-week treatment exposure in approximately 3,200 additional patients who received daily doses of up to 450 mg. Patients were permitted to continue treatment beyond 8 weeks if clinically indicated. Eight seizures occurred during the initial 8-week treatment period and 5 seizures were reported in patients continuing treatment beyond 8 weeks, resulting in a total seizure incidence of 0.4%.

The risk of seizure appears to be strongly associated with dose. Sudden and large increments in dose may contribute to increased risk. While many seizures occurred early in the course of treatment, some seizures did occur after several weeks at fixed dose. WELLBUTRIN should be discontinued and not restarted in patients who experience a seizure while on treatment.

The risk of seizure is also related to patient factors, clinical situations, and concomitant medications, which must be considered in selection of patients for therapy with WELLBUTRIN.

• Patient factors: Predisposing factors that may increase the risk of seizure with bupropion use include history of head trauma or prior seizure, central nervous system (CNS) tumor, the presence of severe hepatic cirrhosis, and concomitant medications that lower seizure threshold.


• Clinical situations: Circumstances associated with an increased seizure risk include, among others, excessive use of alcohol or sedatives (including benzodiazepines); addiction to opiates, cocaine, or stimulants; use of over-the-counter stimulants and anorectics; and diabetes treated with oral hypoglycemics or insulin.


• Concomitant medications: Many medications (e.g., antipsychotics, antidepressants, theophylline, systemic steroids) are known to lower seizure threshold.

 Recommendations for Reducing the Risk of Seizure: Retrospective analysis of clinical experience gained during the development of WELLBUTRIN suggests that the risk of seizure may be minimized if

• the total daily dose of WELLBUTRIN does not exceed 450 mg,


• the daily dose is administered 3 times daily, with each single dose not to exceed 150 mg to avoid high peak concentrations of bupropion and/or its metabolites, and


• the rate of incrementation of dose is very gradual.

WELLBUTRIN should be administered with extreme caution to patients with a history of seizure, cranial trauma, or other predisposition(s) toward seizure, or patients treated with other agents (e.g., antipsychotics, other antidepressants, theophylline, systemic steroids, etc.) that lower seizure threshold.

Hepatic Impairment

WELLBUTRIN should be used with extreme caution in patients with severe hepatic cirrhosis. In these patients a reduced dose and/or frequency is required, as peak bupropion, as well as AUC, levels are substantially increased and accumulation is likely to occur in such patients to a greater extent than usual. The dose should not exceed 75 mg once a day in these patients (see CLINICAL PHARMACOLOGY, PRECAUTIONS, and DOSAGE AND ADMINISTRATION).

Potential for Hepatotoxicity

In rats receiving large doses of bupropion chronically, there was an increase in incidence of hepatic hyperplastic nodules and hepatocellular hypertrophy. In dogs receiving large doses of bupropion chronically, various histologic changes were seen in the liver, and laboratory tests suggesting mild hepatocellular injury were noted.

Precautions

 General: Agitation and Insomnia: A substantial proportion of patients treated with WELLBUTRIN experience some degree of increased restlessness, agitation, anxiety, and insomnia, especially shortly after initiation of treatment. In clinical studies, these symptoms were sometimes of sufficient magnitude to require treatment with sedative/hypnotic drugs. In approximately 2% of patients, symptoms were sufficiently severe to require discontinuation of treatment with WELLBUTRIN.

Psychosis, Confusion, and Other Neuropsychiatric Phenomena: Depressed patients treated with WELLBUTRIN have been reported to show a variety of neuropsychiatric signs and symptoms including delusions, hallucinations, psychosis, concentration disturbance, paranoia, and confusion. Because of the uncontrolled nature of many studies, it is impossible to provide a precise estimate of the extent of risk imposed by treatment with WELLBUTRIN. In several cases, neuropsychiatric phenomena abated upon dose reduction and/or withdrawal of treatment.

Activation of Psychosis and/or Mania: Antidepressants can precipitate manic episodes in bipolar disorder patients during the depressed phase of their illness and may activate latent psychosis in other susceptible patients. WELLBUTRIN is expected to pose similar risks.

Altered Appetite and Weight: A weight loss of greater than 5 lbs occurred in 28% of patients receiving WELLBUTRIN. This incidence is approximately double that seen in comparable patients treated with tricyclics or placebo. Furthermore, while 35% of patients receiving tricyclic antidepressants gained weight, only 9.4% of patients treated with WELLBUTRIN did. Consequently, if weight loss is a major presenting sign of a patient’s depressive illness, the anorectic and/or weight reducing potential of WELLBUTRIN should be considered.

Allergic Reactions: Anaphylactoid/anaphylactic reactions characterized by symptoms such as pruritus, urticaria, angioedema, and dyspnea requiring medical treatment have been reported in clinical trials with bupropion. In addition, there have been rare spontaneous postmarketing reports of erythema multiforme, Stevens-Johnson syndrome, and anaphylactic shock associated with bupropion. A patient should stop taking WELLBUTRIN and consult a doctor if experiencing allergic or anaphylactoid/anaphylactic reactions (e.g., skin rash, pruritus, hives, chest pain, edema, and shortness of breath) during treatment.

Arthralgia, myalgia, and fever with rash and other symptoms suggestive of delayed hypersensitivity have been reported in association with bupropion. These symptoms may resemble serum sickness.

Cardiovascular Effects: In clinical practice, hypertension, in some cases severe, requiring acute treatment, has been reported in patients receiving bupropion alone and in combination with nicotine replacement therapy. These events have been observed in both patients with and without evidence of preexisting hypertension.

Data from a comparative study of the sustained-release formulation of bupropion (ZYBAN® Sustained-Release Tablets), nicotine transdermal system (NTS), the combination of sustained-release bupropion plus NTS, and placebo as an aid to smoking cessation suggest a higher incidence of treatment-emergent hypertension in patients treated with the combination of sustained-release bupropion and NTS. In this study, 6.1% of patients treated with the combination of sustained-release bupropion and NTS had treatment-emergent hypertension compared to 2.5%, 1.6%, and 3.1% of patients treated with sustained-release bupropion, NTS, and placebo, respectively. The majority of these patients had evidence of preexisting hypertension. Three patients (1.2%) treated with the combination of ZYBAN and NTS and 1 patient (0.4%) treated with NTS had study medication discontinued due to hypertension compared to none of the patients treated with ZYBAN or placebo. Monitoring of blood pressure is recommended in patients who receive the combination of bupropion and nicotine replacement.

There is no clinical experience establishing the safety of WELLBUTRIN in patients with a recent history of myocardial infarction or unstable heart disease. Therefore, care should be exercised if it is used in these groups. Bupropion was well tolerated in depressed patients who had previously developed orthostatic hypotension while receiving tricyclic antidepressants and was also generally well tolerated in a group of 36 depressed inpatients with stable congestive heart failure (CHF). However, bupropion was associated with a rise in supine blood pressure in the study of patients with CHF, resulting in discontinuation of treatment in 2 patients for exacerbation of baseline hypertension.

Hepatic Impairment: WELLBUTRIN should be used with extreme caution in patients with severe hepatic cirrhosis. In these patients, a reduced dose and frequency is required. WELLBUTRIN should be used with caution in patients with hepatic impairment (including mild-to-moderate hepatic cirrhosis) and a reduced frequency and/or dose should be considered in patients with mild-to-moderate hepatic cirrhosis.

All patients with hepatic impairment should be closely monitored for possible adverse effects that could indicate high drug and metabolite levels (see CLINICAL PHARMACOLOGY, WARNINGS, and DOSAGE AND ADMINISTRATION).

Renal Impairment: There is limited information on the pharmacokinetics of bupropion in patients with renal impairment. An inter-study comparison between normal subjects and patients with end-stage renal failure demonstrated that the parent drug Cmax and AUC values were comparable in the 2 groups, whereas the hydroxybupropion and threohydrobupropion metabolites had a 2.3– and 2.8–fold increase, respectively, in AUC for patients with end-stage renal failure. A second study, comparing normal subjects and patients with moderate-to-severe renal impairment (GFR 30.9 ± 10.8 mL/min) showed that exposure to a single 150-mg dose of sustained-release bupropion was approximately 2-fold higher in patients with impaired renal function while levels of the hydroxybupropion and threo/erythrohydrobupropion (combined) metabolites were similar in the 2 groups. Bupropion is extensively metabolized in the liver to active metabolites, which are further metabolized and subsequently excreted by the kidneys. WELLBUTRIN should be used with caution in patients with renal impairment and a reduced frequency and/or dose should be considered as bupropion and the metabolites of bupropion may accumulate in such patients to a greater extent than usual. The patient should be closely monitored for possible adverse effects that could indicate high drug or metabolite levels.

Information for Patients

Prescribers or other health professionals should inform patients, their families, and their caregivers about the benefits and risks associated with treatment with WELLBUTRIN and should counsel them in its appropriate use. A patient Medication Guide about “Antidepressant Medicines, Depression and Other Serious Mental Illnesses, and Suicidal Thoughts or Actions,” “Quitting Smoking, Quit-Smoking Medication, Changes in Thinking and Behavior, Depression, and Suicidal Thoughts or Actions,”and “What Other Important Information Should I Know About WELLBUTRIN?” is available for WELLBUTRIN. The prescriber or health professional should instruct patients, their families, and their caregivers to read the Medication Guide and should assist them in understanding its contents. Patients should be given the opportunity to discuss the contents of the Medication Guide and to obtain answers to any questions they may have. The complete text of the Medication Guide is reprinted at the end of this document.

Patients should be advised of the following issues and asked to alert their prescriber if these occur while taking WELLBUTRIN.

Clinical Worsening and Suicide Risk in Treating Psychiatric Disorders: Patients, their families, and their caregivers should be encouraged to be alert to the emergence of anxiety, agitation, panic attacks, insomnia, irritability, hostility, aggressiveness, impulsivity, akathisia (psychomotor restlessness), hypomania, mania, other unusual changes in behavior, worsening of depression, and suicidal ideation, especially early during antidepressant treatment and when the dose is adjusted up or down. Families and caregivers of patients should be advised to look for the emergence of such symptoms on a day-to-day basis, since changes may be abrupt. Such symptoms should be reported to the patient’s prescriber or health professional, especially if they are severe, abrupt in onset, or were not part of the patient’s presenting symptoms. Symptoms such as these may be associated with an increased risk for suicidal thinking and behavior and indicate a need for very close monitoring and possibly changes in the medication.

Neuropsychiatric Symptoms and Suicide Risk in Smoking Cessation Treatment: Although WELLBUTRIN is not indicated for smoking cessation treatment, it contains the same active ingredient as ZYBAN which is approved for this use. Patients should be informed that quitting smoking, with or without ZYBAN, may be associated with nicotine withdrawal symptoms (including depression or agitation), or exacerbation of pre-existing psychiatric illness. Furthermore, some patients have experienced changes in mood (including depression and mania), psychosis, hallucinations, paranoia, delusions, homicidal ideation aggression, anxiety, and panic, as well as suicidal ideation, suicide attempt, and completed suicide when attempting to quit smoking while taking ZYBAN. If patients develop agitation, hostility, depressed mood, or changes in thinking or behavior that are not typical for them, or if patients develop suicidal ideation or behavior, they should be urged to report these symptoms to their healthcare provider immediately.

Bupropion-Containing Products: Patients should be made aware that WELLBUTRIN contains the same active ingredient found in ZYBAN, used as an aid to smoking cessation, and that WELLBUTRIN should not be used in combination with ZYBAN or any other medications that contain bupropion hydrochloride (such as WELLBUTRIN SR, the sustained-release formulation and WELLBUTRIN XL, the extended-release formulation).

Patients should be instructed to take WELLBUTRIN in equally divided doses 3 or 4 times a day to minimize the risk of seizure.

Patients should be told that WELLBUTRIN should be discontinued and not restarted if they experience a seizure while on treatment.

Patients should be told that any CNS-active drug like WELLBUTRIN may impair their ability to perform tasks requiring judgment or motor and cognitive skills. Consequently, until they are reasonably certain that WELLBUTRIN does not adversely affect their performance, they should refrain from driving an automobile or operating complex, hazardous machinery.

Patients should be told that the excessive use or abrupt discontinuation of alcohol or sedatives (including benzodiazepines) may alter the seizure threshold. Some patients have reported lower alcohol tolerance during treatment with WELLBUTRIN. Patients should be advised that the consumption of alcohol should be minimized or avoided.

Patients should be advised to inform their physicians if they are taking or plan to take any prescription or over-the-counter drugs. Concern is warranted because WELLBUTRIN and other drugs may affect each other’s metabolism.

Patients should be advised to notify their physicians if they become pregnant or intend to become pregnant during therapy.

Laboratory Tests

There are no specific laboratory tests recommended.

Drug Interactions

Because bupropion is extensively metabolized, the coadministration of other drugs may affect its clinical activity. In vitro studies indicate that bupropion is primarily metabolized to hydroxybupropion by the CYP2B6 isoenzyme. Therefore, the potential exists for a drug interaction between WELLBUTRIN and drugs that are substrates of or inhibitors/inducers of the CYP2B6 isoenzyme (e.g., orphenadrine, thiotepa, cyclophosphamide, ticlopidine, and clopidogrel). In addition, in vitro studies suggest that paroxetine, sertraline, norfluoxetine, and fluvoxamine as well as ne

Wellbutrin

Generic Name: bupropion (Oral route)

bue-PROE-pee-on

Oral route(Tablet;Tablet, Extended Release;Tablet, Extended Release, 12 HR;Tablet, Extended Release, 24 HR)

Wellbutrin(R) formulations and Forfivo XL: Antidepressants increased the risk of suicidal thinking and behavior in children, adolescents, and young adults in short-term studies with major depressive disorder (MDD) and other psychiatric disorders. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24, and there was a reduction in risk with antidepressants compared to placebo in adults aged 65 and older. This risk must be balanced with the clinical need. Monitor patients closely for clinical worsening, suicidality, or unusual changes in behavior. Families and caregivers should be advised of the need for close observation and communication with the prescriber. Not approved for use in pediatric patients. Zyban(R): Serious neuropsychiatric events, including depression, suicidal ideation, suicide attempt, and completed suicide, have been reported in patients with and without preexisting psychiatric disease who were taking bupropion for smoking cessation; some experienced worsening of their psychiatric illnesses. All patients should be observed for changes in behavior, hostility, agitation, depressed mood, and suicide-related events, including ideation, behavior, and attempted suicide. The patient should stop taking bupropion and contact a healthcare provider immediately if any neuropsychiatric behavior that is not typical for the patient is observed, or if the patient develops suicidal ideation or suicidal behavior. This risk should be weighed against the benefits of its use .

Oral route(Tablet, Extended Release)

Antidepressants increased the risk of suicidal thinking and behavior in children, adolescents, and young adults in short-term studies with major depressive disorder (MDD) and other psychiatric disorders. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24, and there was a reduction in risk with antidepressants compared to placebo in adults aged 65 and older. This risk must be balanced with the clinical need. Monitor patients closely for clinical worsening, suicidality, or unusual changes in behavior. Families and caregivers should be advised of the need for close observation and communication with the prescriber. Not approved for use in pediatric patients .

Commonly used brand name(s)

In the U.S.

• Aplenzin


• Budeprion SR


• Budeprion XL


• Buproban


• Wellbutrin


• Wellbutrin SR


• Wellbutrin XL


• Zyban

Available Dosage Forms:

• Tablet, Extended Release, 24 HR


• Tablet, Extended Release, 12 HR


• Tablet


• Tablet, Extended Release

Therapeutic Class: Antidepressant

Chemical Class: Aminoketone

Uses For Wellbutrin

Bupropion is used to treat mental depression. It is also used as part of a support program to help people stop smoking. This medicine may also be used to prevent depression in patients with seasonal affective disorder, which is sometimes called winter depression.

Bupropion is sold under different brand names for different uses. If you are already taking medicine for mental depression or to help you stop smoking, discuss this with your doctor before taking bupropion. It is very important that you receive only one prescription for bupropion at a time.

This medicine is available only with your doctor's prescription.

Before Using Wellbutrin

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies have not been performed on the relationship of age to the effects of bupropion in the pediatric population. Studies with other medicines used for depression have shown that some children, teenagers, and young adults think about suicide or attempt suicide when taking these medicines. Because of this toxicity, use in children is not recommended.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of bupropion in the elderly. However, elderly patients may be more sensitive to the effects of this medicine than younger adults, and are more likely to have age-related kidney or liver problems, which may require caution and an adjustment in the dose for patients receiving bupropion.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	C	Animal studies have shown an adverse effect and there are no adequate studies in pregnant women OR no animal studies have been conducted and there are no adequate studies in pregnant women.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

• Clorgyline


• Iproniazid


• Isocarboxazid


• Methylene Blue


• Metoclopramide


• Moclobemide


• Nialamide


• Pargyline


• Phenelzine


• Procarbazine


• Selegiline


• Toloxatone


• Tranylcypromine

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Betamethasone


• Budesonide


• Carbimazole


• Clobetasone


• Corticotropin


• Cortisone


• Cosyntropin


• Danazol


• Deflazacort


• Desonide


• Dexamethasone


• Fludrocortisone


• Flunisolide


• Fluticasone


• Hydrocortisone


• Linezolid


• Methenolone


• Methylprednisolone


• Methyltestosterone


• Nandrolone


• Oxandrolone


• Oxymetholone


• Paramethasone


• Prednisolone


• Prednisone


• Rimexolone


• Stanozolol


• Testosterone


• Theophylline

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Amantadine


• Citalopram


• Desipramine


• Efavirenz


• Flecainide


• Fluoxetine


• Haloperidol


• Levodopa


• Lopinavir


• Metoprolol


• Nortriptyline


• Paroxetine


• Propafenone


• Risperidone


• Ritonavir


• Sertraline


• St John's Wort


• Thioridazine


• Tipranavir


• Zolpidem

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

• Ethanol

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Alcohol use, if stopped suddenly, or


• Eating disorders (e.g., anorexia nervosa, bulimia nervosa), history of or


• Sedative (sleeping medicine) use, if stopped suddenly (e.g., alprazolam [Xanax®], diazepam [Valium®], triazolam [Restoril®]), or


• Seizures or epilepsy, history of—Should not be used in patients with these conditions.

• Bipolar disorder (mood disorder with alternating episodes of mania and depression), or risk of or


• Depression, history of or


• Hypertension (high blood pressure) or


• Psychosis (mental disease that affects emotions and behaviors) or


• Schizophrenia (mental illness)—Use with caution. May make these conditions worse.

• Brain or spine tumor or


• Diabetes or


• Drug or alcohol abuse (e.g., opiates, cocaine, stimulants) or


• Head injury, history of or


• Liver disease (including cirrhosis), severe—The risk of seizures may be increased when bupropion is taken by patients with these conditions.

• Heart attack, recent or


• Heart disease, unstable—The effects of bupropion in patients with these conditions are not known.

• Kidney disease or


• Liver disease—Use with caution. The effects may be increased because of slower removal of the medicine from the body.

• Mania or hypomania, history of—Use of bupropion may activate these conditions.

Proper Use of bupropion

This section provides information on the proper use of a number of products that contain bupropion. It may not be specific to Wellbutrin. Please read with care.

Use bupropion only as directed by your doctor. Do not use more of it, do not use it more often, and do not use it for a longer time than your doctor ordered. To do so, may increase the chance of side effects.

This medicine should come with a Medication Guide. Read and follow these instructions carefully. Ask your doctor if you have any questions.

Use only the brand of this medicine that your doctor prescribed. Different brands may not work the same way.

Swallow the sustained-release tablets whole. Do not break, crush, divide, or chew it.

You may take this medicine with or without food. But, if you have nausea, take this medicine with food.

To lessen stomach upset, this medicine may be taken with food, unless your doctor has told you to take it on an empty stomach.

If you are taking Zyban® tablets to help you stop smoking, you may continue to smoke for about 1 week after you start using this medicine. Then, you should set a target date to quit smoking during your second week of Zyban® treatment. Talk to your doctor if you are having trouble to stop smoking after you have used this medicine for at least 7 weeks.

Do not smoke if you are using a nicotine patch or any other medicine containing nicotine together with Zyban® tablets. To do so, may increase risk for more serious side effects.

This medicine must be taken for several weeks, usually 4 weeks, before you start to feel better. You will probably need to keep taking bupropion for several months to help prevent the return of your depression. Your doctor will check your progress at regular visits, especially during the first few weeks that you take this medicine.

If you have trouble with sleeping (insomnia), do not take this medicine too close to bedtime.

For patients taking the extended-release tablet form of this medicine:

• Take doses at least 24 hours apart to decrease the chance of seizures.


• Swallow the tablets whole. Do not crush, break, or chew them.


• While taking this medicine, part of the tablet may pass into your stools. This is normal and is nothing to worry about.


• If you use this medicine to prevent depression in seasonal affective disorder, take it during the autumn season before your symptoms start. Continue using this medicine through the winter season and until early spring.

To help you remember to use your medicine, take it at the same time each day.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For oral dosage form (extended-release tablets):
  
  • For depression:
    
    • Adults—
      
      • Aplenzin™: At first, 174 milligrams (mg) once a day in the morning. Your doctor may increase your dose as needed and tolerated. However, the dose is usually not more than 522 mg per day.
      
      
      • Forfivo XL®: 450 mg once a day.
      
      
      • Wellbutrin XL®: At first, 150 mg once a day in the morning. Your doctor may increase your dose as needed. However, the dose usually is not more than 450 mg once a day.
      
      
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  
  • For seasonal affective disorder:
    
    • Adults—At first, 150 milligrams (mg) once a day in the morning. Your doctor may increase your dose as needed. However, the dose usually is not more than 300 mg once a day.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  

• For oral dosage form (tablets):
  
  • For depression:
    
    • Adults—At first, 100 milligrams (mg) two times a day. Your doctor may increase your dose as needed. However, the dose is usually not more than 150 mg three times a day. Take doses at least 4 hours apart to decrease the chance of seizures.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  

• For oral dosage form (sustained-release tablets):
  
  • For depression:
    
    • Adults—At first, 150 milligrams (mg) once a day in the morning. Your doctor may increase your dose as needed. However, the dose usually is not more than 200 mg two times a day. Take doses at least 8 hours apart to decrease the chance of seizures.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  
  • To help you stop smoking:
    
    • Adults—At first, 150 milligrams (mg) once a day for the first 3 days. Then, your doctor may increase your dose as needed. However, the dose is usually not more than 300 mg per day. Take doses at least 8 hours apart to decrease the chance of seizures.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  

Missed Dose

If you miss a dose of this medicine, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

If you are taking the extended-release tablets and you miss a dose, skip the missed dose and go back to your regular dosing schedule.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Precautions While Using Wellbutrin

Your doctor will check your progress at regular visits, especially during the first few months that you take this medicine. The amount of bupropion you take may have to be adjusted to meet the needs of your condition and to help avoid unwanted effects.

Do not take bupropion with or within 14 days of taking a drug with monoamine oxidase inhibitor (MAOI) activity (e.g., isocarboxazid [Marplan®], phenelzine [Nardil®], procarbazine [Matulane®], selegiline [Eldepryl®], or tranylcypromine [Parnate®]). Do not take an MAO inhibitor within 14 days of taking bupropion. If you do, you might have convulsions (seizures).

Your blood pressure might get too high while you are using this medicine. This may cause headaches, blurred vision, and other symptoms. You might need to measure your blood pressure at home. If you think your blood pressure is getting too high, call your doctor right away.

Bupropion may cause some people to be agitated, irritable, or display other abnormal behaviors. It may also cause some people to have suicidal thoughts and tendencies or to become more depressed. Make sure the doctor knows if you have trouble sleeping, get upset easily, have a big increase in energy, or start to act reckless. Also tell the doctor if you have sudden or strong feelings, such as feeling nervous, angry, restless, violent, or scared. If you or your caregiver notice any of these side effects, tell your doctor right away.

This medicine may cause a serious type of allergic reaction called anaphylaxis. Anaphylaxis can be life-threatening and requires immediate medical attention. Stop using this medicine and tell your doctor right away if you have a rash; itching; swelling of the face, tongue, and throat; trouble breathing; or chest pain after you take this medicine.

Serious skin reactions can occur with this medicine. Check with your doctor right away if you have blistering, peeling, or loosening of the skin; red skin lesions; severe acne or skin rash; sores or ulcers on the skin; or fever or chills while you are using this medicine.

Drinking alcoholic beverages should be limited or avoided, if possible, while taking bupropion. This will help prevent seizures.

This medicine may cause some people to have a false sense of well-being, or to become drowsy, dizzy, or less alert than they are normally. Make sure you know how you react to this medicine before you drive, use machines, or do anything else that could be dangerous if you are dizzy or not alert and clearheaded.

Do not stop taking this medicine without checking first with your doctor. Your doctor may want you to gradually reduce the amount you are taking before stopping it completely. This is to decrease the chance of having side effects such as agitation, anxiety, dizziness, a feeling of constant movement of self or surroundings, headache, increased sweating, nausea, trembling or shaking, trouble with sleeping or walking, or unusual tiredness when you stop the medicine.

Check with your doctor right away if you have pain or tenderness in the upper stomach; pale stools; dark urine; loss of appetite; nausea; unusual tiredness or weakness; or yellow eyes or skin. These could be symptoms of a serious liver problem.

This medicine may cause changes in your appetite or weight. Your doctor may need to check your weight regularly during treatment with this medicine.

Before you have any medical tests, tell the medical doctor in charge that you are taking this medicine. The results of some tests may be affected by this medicine.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

Wellbutrin Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common

• Anxiety


• dry mouth


• hyperventilation


• irregular heartbeats


• irritability


• nervousness


• restlessness


• shaking


• shortness of breath


• trouble with sleeping

Less common

• Buzzing or ringing in the ears


• headache (severe)


• skin rash, hives, or itching

Rare

• Confusion


• fainting


• false beliefs that cannot be changed by facts


• having extreme distrust of people


• seeing, hearing, or feeling things that are not there


• seizures (convulsions)


• trouble with concentrating

Incidence not known

• Actions that are out of control


• anger


• assaulting others


• attacking others


• being aggressive


• being impulsive


• chest pain or discomfort


• fast or pounding heartbeat


• force


• inability to sit still


• need to keep moving


• sweating


• talking, feeling, or acting with excitement

Get emergency help immediately if any of the following symptoms of overdose occur:

Symptoms of overdose

• Blue lips, fingernails, or skin


• blurred vision


• change in consciousness


• dark-colored urine


• decreased awareness or responsiveness


• difficult or troubled breathing


• dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position


• fever


• irregular, fast or slow, or shallow breathing


• loss of consciousness


• muscle cramps, pain, or spasms


• muscle stiffness or tightness


• nausea


• severe sleepiness


• unusual tiredness or weakness


• vomiting

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

• Abdominal or stomach pain


• constipation


• decrease in appetite


• dizziness


• increased sweating


• trembling


• weight loss (unusual)

Less common

• Blurred vision


• change in sense of taste


• drowsiness


• frequent need to urinate


• sore throat


• unusual feeling of well-being

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

See also: Wellbutrin side effects (in more detail)

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More Wellbutrin resources

• Wellbutrin Side Effects (in more detail)
• Wellbutrin Use in Pregnancy & Breastfeeding
• Drug Images
• Wellbutrin Drug Interactions
• Wellbutrin Support Group
• 128 Reviews for Wellbutrin - Add your own review/rating

• Wellbutrin Prescribing Information (FDA)


• Wellbutrin MedFacts Consumer Leaflet (Wolters Kluwer)


• Wellbutrin Consumer Overview


• Aplenzin Prescribing Information (FDA)


• Aplenzin Consumer Overview


• Aplenzin Extended-Release Tablets MedFacts Consumer Leaflet (Wolters Kluwer)


• Budeprion XL Prescribing Information (FDA)


• Bupropion Prescribing Information (FDA)


• Bupropion Professional Patient Advice (Wolters Kluwer)


• Bupropion Hydrochloride Monograph (AHFS DI)


• Wellbutrin SR Prescribing Information (FDA)


• Wellbutrin SR Sustained-Release Tablets MedFacts Consumer Leaflet (Wolters Kluwer)


• Wellbutrin XL Prescribing Information (FDA)


• Wellbutrin XL Extended-Release Tablets MedFacts Consumer Leaflet (Wolters Kluwer)


• Zyban Prescribing Information (FDA)


• Zyban Consumer Overview


• Zyban Sustained-Release Tablets MedFacts Consumer Leaflet (Wolters Kluwer)

Compare Wellbutrin with other medications

• Depression

Water

Pronunciation: bak-TEER-ee-oh-STAT-ik
Generic Name: Water
Brand Name: Generic only. No brands available.

Water is used for:

Mixing with certain medicines that are given by injection.

Water is a sterile solution used to mix and dilute other medicines.

Do NOT use Water if:

• you are allergic to any ingredient in Water

Contact your doctor or health care provider right away if any of these apply to you.

Before using Water:

Some medical conditions may interact with Water. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

• if you are pregnant, planning to become pregnant, or are breast-feeding


• if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement


• if you have allergies to medicines, foods, or other substances

Some MEDICINES MAY INTERACT with Water. However, no specific interactions with Water are known at this time.

This may not be a complete list of all interactions that may occur. Ask your health care provider if Water may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

How to use Water:

Use Water as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Water is usually administered as an injection at your doctor's office, hospital, or clinic. If you are using Water at home, carefully follow the injection procedures taught to you by your health care provider.


• If you have refrigerated this product, allow it to reach room temperature before using.


• This product is to be mixed with certain medicines just prior to injection. Do not inject this product directly. This product cannot be mixed with all medicines. Use this product to mix only those medicines indicated by your doctor or pharmacist.


• If Water contains particles or is discolored, or if the vial is cracked or damaged in any way, do not use it.


• Keep this product, as well as syringes and needles, out of the reach of children and away from pets. Do not reuse needles, syringes, or other materials. Dispose of properly after use. Ask your doctor or pharmacist to explain local regulations for proper disposal.


• If you miss a dose of Water, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Water.

Important safety information:

• Water is not recommended for use in CHILDREN younger than 4 weeks of age. Safety and effectiveness in this age group have not been confirmed.

Possible side effects of Water:

All medicines may cause side effects, but many people have no, or minor, side effects. When used in small doses, no COMMON side effects have been reported with this product. Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); fever; redness, swelling, or tenderness at injection site.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.

If OVERDOSE is suspected:

Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately.

Proper storage of Water:

Store Water at room temperature, between 68 and 77 degrees F (20 and 25 degrees C). Do not freeze. Store away from heat, moisture, and light. Do not store in the bathroom. Keep Water out of the reach of children and away from pets.

General information:

• If you have any questions about Water, please talk with your doctor, pharmacist, or other health care provider.


• Water is to be used only by the patient for whom it is prescribed. Do not share it with other people.


• If your symptoms do not improve or if they become worse, check with your doctor.


• Check with your pharmacist about how to dispose of unused medicine.

This information is a summary only. It does not contain all information about Water. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.

Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Water resources

• Water Support Group
• 0 Reviews · Be the first to review/rate this drug

Ektebin

Ektebin may be available in the countries listed below.

Ingredient matches for Ektebin

Protionamide

Protionamide is reported as an ingredient of Ektebin in the following countries:

• Germany


• Romania

International Drug Name Search

valrubicin Intravesical

val-ROO-bi-sin

Commonly used brand name(s)

In the U.S.

• Valstar

Available Dosage Forms:

• Solution

Therapeutic Class: Antineoplastic Agent

Chemical Class: Anthracycline

Uses For valrubicin

Valrubicin is used as a solution that is run through a tube (instilled through a catheter) into the bladder to treat bladder cancer.

Valrubicin is to be administered only by or under the immediate supervision of your doctor.

Before Using valrubicin

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For valrubicin, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to valrubicin or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Studies on valrubicin have been done only in adult patients, and there is no specific information comparing use of valrubicin in children with use in other age groups.

Geriatric

Many medicines have not been studied specifically in older people. Therefore, it may not be known whether they work exactly the same way they do in younger adults. Although there is no specific information comparing the use of valrubicin in the elderly with use in other age groups, valrubicin has been used mostly in patients older than 60 years of age and is not expected to cause different side effects or problems in older people than it does in younger adults.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	C	Animal studies have shown an adverse effect and there are no adequate studies in pregnant women OR no animal studies have been conducted and there are no adequate studies in pregnant women.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. Tell your healthcare professional if you are taking any other prescription or nonprescription (over-the-counter [OTC]) medicine.

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of valrubicin. Make sure you tell your doctor if you have any other medical problems, especially:

• Bladder irritation or other bladder problems—Increased risk of unwanted effects

• Small bladder—Possible trouble in being able to hold all of the solution


• Urinary tract infection

Proper Use of valrubicin

Your doctor may ask you to empty your bladder completely before the solution is instilled into it (unless a tube is used to drain the bladder).

Follow your doctor's instructions carefully about how long to hold the solution in your bladder:

• The solution should be held in your bladder for 2 hours. If you think you cannot hold it, tell your health care professional.

It is important that you drink extra fluids after each treatment with valrubicin so that you will pass more urine.

Dosing

The dose of valrubicin will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of valrubicin. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For bladder instillation dosage form (solution):
  
  • For bladder cancer:
    
    • Adults—800 milligrams (mg) (75 milliliters [mL]) instilled into the bladder once a week for six weeks.
    
    
  
  

Precautions While Using valrubicin

Valrubicin commonly causes the urine to turn red for about 24 hours after it is given. This is normal and is no cause for concern. However, tell your doctor if you continue to pass red urine for longer than 24 hours.

valrubicin Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

• Blood in urine


• loss of bladder control


• painful or difficult urination


• red color in urine


• strong urge to urinate


• unusually frequent urination

Less common

• Increased urination at night


• local burning sensation

Rare

• Frequent urge to defecate


• itching


• loss of sense of taste

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

See also: valrubicin Intravesical side effects (in more detail)

The information contained in the Thomson Reuters Micromedex products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you.

The use of the Thomson Reuters Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Reuters Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON REUTERS HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.

More valrubicin Intravesical resources

• Valrubicin Intravesical Side Effects (in more detail)
• Valrubicin Intravesical Use in Pregnancy & Breastfeeding
• Valrubicin Intravesical Drug Interactions
• Valrubicin Intravesical Support Group
• 0 Reviews for Valrubicin Intravesical - Add your own review/rating

Compare valrubicin Intravesical with other medications

• Urinary Tract Tumors

Fortified Procaine Penicillin

Fortified Procaine Penicillin may be available in the countries listed below.

Ingredient matches for Fortified Procaine Penicillin

Benzylpenicillin

Benzylpenicillin procaine (a derivative of Benzylpenicillin) is reported as an ingredient of Fortified Procaine Penicillin in the following countries:

• Ethiopia


• Romania

International Drug Name Search

Soma

Generic Name: carisoprodol (Oral route)

kar-eye-soe-PROE-dol

Commonly used brand name(s)

In the U.S.

• Soma


• Vanadom

Available Dosage Forms:

• Tablet

Therapeutic Class: Skeletal Muscle Relaxant, Centrally Acting

Uses For Soma

Carisoprodol is used to relax certain muscles in your body and relieve the discomfort caused by acute (short-term), painful muscle or bone conditions. However, this medicine does not take the place of rest, exercise, physical therapy, or other treatments that your doctor may recommend for your medical condition.

Carisoprodol is a skeletal muscle relaxant. It acts on the central nervous system (CNS) to relax muscles.

This medicine is available only with your doctor's prescription.

Before Using Soma

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies have not been performed on the relationship of age to the effects of carisoprodol in children below 16 years of age. Safety and efficacy have not been established.

Geriatric

Appropriate studies on the relationship of age to the effects of carisoprodol have not been performed in the geriatric population. Safety and efficacy have not been established.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	C	Animal studies have shown an adverse effect and there are no adequate studies in pregnant women OR no animal studies have been conducted and there are no adequate studies in pregnant women.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Adinazolam


• Alfentanil


• Alprazolam


• Amobarbital


• Anileridine


• Aprobarbital


• Bromazepam


• Brotizolam


• Butabarbital


• Butalbital


• Carisoprodol


• Chloral Hydrate


• Chlordiazepoxide


• Chlorzoxazone


• Clobazam


• Clonazepam


• Clorazepate


• Codeine


• Dantrolene


• Diazepam


• Estazolam


• Ethchlorvynol


• Fentanyl


• Flunitrazepam


• Flurazepam


• Halazepam


• Hydrocodone


• Hydromorphone


• Ketazolam


• Levorphanol


• Lorazepam


• Lormetazepam


• Medazepam


• Meperidine


• Mephenesin


• Mephobarbital


• Meprobamate


• Metaxalone


• Methocarbamol


• Methohexital


• Midazolam


• Morphine


• Morphine Sulfate Liposome


• Nitrazepam


• Nordazepam


• Oxazepam


• Oxycodone


• Oxymorphone


• Pentobarbital


• Phenobarbital


• Prazepam


• Primidone


• Propoxyphene


• Quazepam


• Remifentanil


• Secobarbital


• Sodium Oxybate


• Sufentanil


• Temazepam


• Thiopental


• Triazolam

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Drug abuse or dependence, or history of—Use with caution. Dependence on carisoprodol may develop.

• Kidney disease or


• Liver disease—Use with caution. The effects may be increased because of slower removal of the medicine from the body.

• Porphyria (an enzyme problem), history of—Should not be used in patients with this condition.

• Seizures—Use with caution. May make this condition worse.

Proper Use of carisoprodol

This section provides information on the proper use of a number of products that contain carisoprodol. It may not be specific to Soma. Please read with care.

Take this medicine only as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. If this medicine is taken for a long time, it may become habit-forming (causing mental or physical dependence). This medicine should only be used for 2 to 3 weeks.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For relaxing muscles:
  
  • For oral dosage form (tablets):
    
    • Adults and teenagers 16 years of age and older—250 to 350 milligrams (mg) three times a day and at bedtime.
    
    
    • Children and teenagers younger than 16 years of age—Use and dose must be determined by your child's doctor.
    
    
  
  

Missed Dose

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Precautions While Using Soma

It is very important that your doctor check your progress at regular visits to make sure this medicine is working properly and to check for unwanted effects.

This medicine may cause some people to become dizzy, drowsy, or less alert than they are normally. Avoid driving, using machines, or do anything else that could be dangerous if you are not alert.

This medicine will add to the effects of alcohol and other CNS depressants (medicines that make you drowsy or less alert). Some examples of CNS depressants are antihistamines or medicine for hay fever, allergies, or colds; sedatives, tranquilizers, or sleeping medicine; prescription pain medicine or narcotics; medicine for seizures or barbiturates; or anesthetics, including some dental anesthetics. Check with your medical doctor or dentist before taking any of the above while you are taking this medicine.

Do not stop using this medicine suddenly without first asking your doctor. You may need to slowly decrease your dose before stopping it completely.

If your condition does not improve within two to three weeks, or if it becomes worse, check with your doctor.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

Soma Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

Incidence not known

• Black, tarry stools


• chest pain


• chills


• cold sweats


• confusion


• convulsions


• cough


• dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position


• fast, pounding, or irregular heartbeat or pulse


• fever


• loss of bladder control


• muscle spasm or jerking of all extremities


• painful or difficult urination


• shortness of breath


• sore throat


• sores, ulcers, or white spots on the lips or in the mouth


• sudden loss of consciousness


• swollen glands


• unusual bleeding or bruising


• unusual tiredness or weakness

Get emergency help immediately if any of the following symptoms of overdose occur:

Symptoms of overdose

• Bigger, dilated, or enlarged pupils (black part of the eye)


• blurred vision


• change in consciousness


• confusion as to time, place, or person


• difficult or troubled breathing


• false or unusual sense of well-being


• hallucinations


• headache


• holding false beliefs that cannot be changed by fact


• inability to move the eyes


• increased blinking or spasms of the eyelid


• increased sensitivity of the eyes to light


• irregular, fast or slow, or shallow breathing


• loss of consciousness


• muscle stiffness or tightness


• pale or blue lips, fingernails, or skin


• sticking out of the tongue


• trouble with breathing, speaking, or swallowing


• uncontrolled eye movements


• uncontrolled twisting movements of the neck, trunk, arms, or legs


• unusual excitement, nervousness, or restlessness


• unusual facial expressions


• weakness of the arms and legs

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

• Drowsiness

Incidence not known

• Anxiety


• deep or fast breathing with dizziness


• dry mouth


• face is warm or hot to touch


• fainting feeling of constant movement of self or surroundings


• heartburn


• irritability


• nausea


• nervousness


• numbness of the feet, hands, and around the mouth


• pain or discomfort in the chest, upper stomach, or throat


• redness to face


• restlessness


• sensation of spinning


• shakiness and unsteady walk


• sleeplessness


• trouble sleeping


• unable to sleep


• unsteadiness, trembling, or other problems with muscle control or coordination


• vomiting

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

See also: Soma side effects (in more detail)

The information contained in the Thomson Reuters Micromedex products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you.

The use of the Thomson Reuters Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Reuters Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON REUTERS HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.

More Soma resources

• Soma Side Effects (in more detail)
• Soma Dosage
• Soma Use in Pregnancy & Breastfeeding
• Drug Images
• Soma Drug Interactions
• Soma Support Group
• 71 Reviews for Soma - Add your own review/rating

• Soma Consumer Overview


• Soma MedFacts Consumer Leaflet (Wolters Kluwer)


• Soma Prescribing Information (FDA)


• Carisoprodol Professional Patient Advice (Wolters Kluwer)


• Carisoprodol Monograph (AHFS DI)


• Carisoprodol Prescribing Information (FDA)


• Somatuline Depot Monograph (AHFS DI)


• Somavert Monograph (AHFS DI)

Compare Soma with other medications

• Muscle Spasm
• Nocturnal Leg Cramps