The elimination half-life of hydroxybupropion is approximately 20 (±5) hours, and its AUC at steady state is about 17 times that of bupropion. 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. The potency and toxicity of the metabolites relative to bupropion have not been fully characterized. 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.
Medical Professionals
- Insomnia can be frustrating and lead to worse treatment outcomes overall.
- These side effects may go away during treatment as your body adjusts to the medicine.
- The threohydrobupropion metabolite of bupropion does not appear to be produced by cytochrome P450 enzymes.
It’s important to understand the risks and benefits of taking antidepressants during pregnancy and while breastfeeding. Other factors may also affect whether this drug is a good treatment option for you. This is especially helpful when you first start taking a new drug or using a combination of treatments. This is a rare but serious adverse drug reaction to certain drugs.
Hypersensitivity Reactions
Your doctor can help you figure out whether your medication, your condition, or both are the cause. Suicidal behaviors can also be a symptom of depression. Wellbutrin is not prescribed for people younger than 18 years old. Children, adolescents, and young adults ages 18 to 24 years had the highest risk compared with older age groups.
Bupropion (Wellbutrin, Zyban, and others) – Uses, Side Effects, and More
Regarding non-life-threatening side effects, always be honest with your healthcare provider. Both tablets should not be chewed or crushed since they are made to release bupropion slowly over time in the body. Wellbutrin SR is specifically approved as an aid in smoking cessation and is prescribed twice each day 12 hours apart. If you experience any symptoms of an allergic reaction, including itching, rash, swelling of the mouth or throat, or trouble breathing, call 911 and get help immediately. Be sure to alert your healthcare provider if you have anatomically narrow angles or any other eye condition.
Clinical Studies
Headaches from bupropion can be mild to painful Wellbutrin side effects and can make concentrating at work or school difficult. However, if a side effect becomes too difficult to manage or you suspect it may be severe, do not hesitate to seek medical help right away or call 911. Keeping side effects at a minimum can help you stay on course with treatment.
- These risk differences (drug-placebo difference in the number of cases of suicidality per 1,000 subjects treated) are provided in Table 1.
- During a chronic dosing trial with bupropion in 14 depressed subjects with left ventricular dysfunction (history of CHF or an enlarged heart on x-ray), there was no apparent effect on the pharmacokinetics of bupropion or its metabolites, compared with healthy volunteers.
- In vitro, bupropion and its metabolites (erythrohydrobupropion, threohydrobupropion, hydroxybupropion) are CYP2D6 inhibitors.
- 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.
- Animal data indicated that bupropion may be an inducer of drug-metabolizing enzymes in humans.
What are the serious side effects of bupropion?
Your doctor will likely stop treatment with Wellbutrin if you experience a seizure. This may help reduce the risk of seizures from Wellbutrin. Headaches were mild to moderate in severity, and most people did not have to stop taking Wellbutrin. If you’ve had a serious allergic reaction to Wellbutrin, your doctor may recommend taking a different medication instead. These symptoms require immediate medical care because they can become life threatening.
Pooled analysis of bupropion pharmacokinetic data from 90 healthy male and 90 healthy female volunteers revealed no sex-related differences in the peak plasma concentrations of bupropion. However, more variability was observed in some of the pharmacokinetic parameters for bupropion (AUC, Cmax, and Tmax) and its active metabolites (t½) in subjects with mild-to-moderate hepatic cirrhosis. WELLBUTRIN should be used with caution in patients with renal impairment and a reduced frequency and/or dose should be considered see Use In Specific Populations. There is limited information on the pharmacokinetics of bupropion in patients with renal impairment. 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. Only 0.5% of the oral dose was excreted as unchanged bupropion.
Starting Wellbutrin on the lowest starting dose possible for treatment may help reduce your risk of suicidal thoughts and behaviors. It’s important to note that the risk of suicidal thoughts and behavior is also a symptom of depression and seasonal affective disorder (SAD). And some people may have an increased risk of mood problems when drinking alcohol during treatment with Wellbutrin. If you use this medicine to prevent depression with seasonal affective disorder, take it during the autumn season before your symptoms start. Your doctor will probably start you on a low dose of bupropion and gradually increase your dose.
Your doctor will weigh the risks and benefits of taking Wellbutrin and determine the best treatment plan for you. Doing so may increase your risk of seizures as a side effect. Your doctor may avoid prescribing Wellbutrin if you are currently taking one of these drugs. Levodopa and amantadine produce the same effect, and if either of these drugs is taken together with Wellbutrin, serious side effects may occur.
During your Wellbutrin treatment, consider taking notes on any side effects you’re having. If your doctor confirms you’ve had a serious allergic reaction to Wellbutrin, they may have you switch to a different treatment. These symptoms could be life threatening and require immediate medical care. If you have mild symptoms of an allergic reaction, such as a mild rash, call your doctor right away. For temporary relief from headache pain when starting Wellbutrin, you can take an OTC pain relief medication.
Keep reading to learn about other possible mild and serious side effects of this drug. Some people may experience mild to serious side effects while taking Wellbutrin. For example, you may only need to take the drug during the winter to help prevent SAD. Throughout this article, the term “Wellbutrin” refers to both forms of the drug. If you notice any other effects, check with your healthcare professional.
The efficacy of WELLBUTRIN in the treatment of a major depressive episode was established in two 4-week controlled inpatient trials and one 6-week controlled outpatient trial of adult subjects with MDD see Clinical Studies. WELLBUTRIN (bupropion hydrochloride) is indicated for the treatment of major depressive disorder (MDD), as defined by the Diagnostic and Statistical Manual (DSM). Wellbutrin (bupropion) is an antidepressant in the aminoketone class used for the management of major depression and seasonal affective disorder. If you have a child taking Wellbutrin or another depression medication, keep a close eye out for signs of self-harm or suicidal thinking. Never take two doses of Wellbutrin at once to make up for a missed dose as this can increase your risk of experiencing a seizure or an accidental overdose.
Allergic Reactions
High doses and/or long-term treatment with Wellbutrin can lower the threshold for seizures to occur; never take more medication than is prescribed to you. Special care should be taken when starting, stopping, or changing the dose of Wellbutrin, as this is often when symptoms of depression worsen. Your healthcare provider will most likely reduce your dose or stop your treatment all together. Your healthcare provider should verify your health history and perform an eye exam if you are at an increased risk.
Improvement of psychological symptoms, such as those related to mood, may take a bit longer—or up to eight weeks. If you are lactating, your healthcare provider can help you weigh your options. Wellbutrin can be present in breast milk, so caution should be used by people who are breastfeeding.
High Blood Pressure
The risk of hypertension is increased if WELLBUTRIN is used concomitantly with MAOIs or other drugs that increase dopaminergic or noradrenergic activity see CONTRAINDICATIONS. WELLBUTRIN is contraindicated in patients with a seizure disorder, current or prior diagnosis of anorexia nervosa or bulimia, or undergoing abrupt discontinuation of alcohol, benzodiazepines, barbiturates, and antiepileptic drugs see CONTRAINDICATIONS, DRUG INTERACTIONS. These risk differences (drug-placebo difference in the number of cases of suicidality per 1,000 subjects treated) are provided in Table 1.
If you have trouble falling asleep or staying asleep, do not take bupropion too close to bedtime. Bupropion comes as a tablet and a sustained-release or extended-release (long-acting) tablet to take by mouth.It is taken 1 to 4 times a day depending on the formulation being used.Follow the directions on your label carefully. Be sure that your family or caregiver knows which symptoms may be serious so they can call the doctor if you are unable to do so. This increase was found in children, teenagers, and young adults (less than 24 years of age).
This condition can be caused by many antidepressant medications, including Wellbutrin. Patients should have their blood pressure assessed prior to treatment and periodically throughout treatment. Review all of your health history with your healthcare provider to ensure safe use. Any abnormal psychiatric symptoms should be treated promptly to avoid worsening symptoms that could lead to self-harm.
