Bupropion is an aminoketone antidepressant that is widely used in therapy of depression and smoking cessation. Bupropion therapy can be associated with transient, usually asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury.This agent does not inhibit monoamine oxidase and, compared to classical tricyclic antidepressants, is a weak blocker of the neuronal uptake of serotonin and norepinephrine. Buproprion also weakly inhibits the neuronal reuptake of dopamine.
Bupropion is a medication primarily used as an antidepressant and smoking cessation aid. It is one of the most frequently prescribed antidepressants in the United States and Canada, although in many countries this is an off-label use. It is an effective antidepressant on its own but is also popular as an add-on medication in cases of incomplete response to first-line SSRI antidepressants. Bupropion is taken in tablet form and is available only by prescription in most countries.
Mechanism of action of Bupropion
Bupropion selectively inhibits the neuronal reuptake of dopamine, norepinephrine, and serotonin; actions on dopaminergic systems are more significant than imipramine or amitriptyline whereas the blockade of norepinephrine and serotonin reuptake at the neuronal membrane is weaker for bupropion than for tricyclic antidepressants. The increase in norepinephrine may attenuate nicotine withdrawal symptoms and the increase in dopamine at neuronal sites may reduce nicotine cravings and the urge to smoke. Bupropion exhibits moderate anticholinergic effects.
Indications of Bupropion
-
Indicated as an aid to smoking cessation in combination with motivational support in nicotine-dependent patients
- Treatment of depression and as an aid to smoking cessation.
- Anxiety
- Seasonal affective disorder
- Depression, bipolar
- Major depressive disorder
- Seasonal affective disorder
- Bipolar disorder
- Major depressive disorder
- Depression
- Migraine prevention
- Obesity
- Panic disorder
- Persistent depressive disorder
- Postural orthostatic tachycardia syndrome
- Premenstrual dysphoric disorder
- Sexual dysfunction, SSRI induced
Contra-Indications of Bupropion
- Spread of cancer to the brain
- Tumor of the brain or spinal cord
- Symptoms from alcohol withdrawal
- Mild degree of Mania
- Manic-depression
- Mental disorder with loss of normal personality & reality
- Having thoughts of suicide
- Alcoholism
- Narcotic addiction
- Anorexia nervosa
- Bulimia
- Feeling anger toward something
- Lower seizure threshold
- Closed angle glaucoma
- high blood pressure
- Heart attack
- Severe liver disease
- Seizures
- Weight loss
- Seizure caused by sudden withdrawal of benzodiazepine
- Stimulant drug dependence
- Sedative drug dependence
- risk of angle-closure glaucoma due to narrow angle of anterior chamber of eye
Dosage of Bupropion
Strengths: 75 mg; 100 mg; 150 mg; 200 mg ;300mg; 400mg; 450mg.
Smoking Cessation
Sustained-release tablets
- Initial dose: 150 mg orally once a day for 3 days, increased to 150 mg orally twice a day
- Maintenance dose: 150 mg orally twice a day
- Maximum dose: 300 mg/day; maximum single dose should not exceed 150 mg
- Duration of therapy: 7 to 12 weeks
Depression
Immediate-release tablets
- Initial dose: 100 mg orally twice a day, increase if necessary after 3 days to 100 mg orally three times a day.
- Maintenance dose: 100 mg orally three times a day
- Maximum dose: 450 mg/day in up to 4 divided doses; single doses should not exceed 150 mg
Sustained-release tablets
- Initial dose: 150 mg orally once a day in the morning, increase if necessary after 3 days to 150 mg orally twice a days
- Maintenance dose: 150 mg orally twice a day
- Maximum dose: 400 mg/day; maximum single dose should not exceed 200 mg
Extended-release tablets
- Initial dose: 150 mg orally once a day in the morning, increase if necessary after 4 days to 300 mg orally once a day.
- Maintenance dose: 300 mg orally once a day
- Maximum dose: 450 mg/day
Seasonal Affective Disorder
Extended-release tablets
- Initial dose: 150 mg orally once a day in the morning, increased if necessary after 7 days to 300 mg orally once a day
- Maintenance dose: 150 to 300 mg orally once a day
- Maximum dose: 300 mg/day
Side Effects of Bupropion
The most common
- dry mouth
- hyperventilation
- irregular heartbeats
- irritability
- Nausea and vomiting
- Severe stomach ache
- epigastric pain
- diarrhoea,
- anorexia,,
- headache,
- dizziness,
- fainting, fast or pounding heartbeats;
- confusion, hallucinations;
Common
- Agitation
- Dry mouth
- Constipation
- Headache/migraine
- Dizziness
- Excessive sweating
- Insomnia
- Blurred vision
- Nausea and vomiting
- Severe stomach ache
- Severe diarrhea
- Mouth sores
- Vaginal thrush
- Skin rash
- Headache
- Ringing or buzzing in the ears
- Decreased appetite
Rare
- Buzzing or ringing in the ears
- headache (severe)
- skin rash, hives, or itching
- Confusion
- false beliefs that cannot be changed by facts
- having extreme distrust of people
- seeing, hearing, or feeling things that are not there
- seizures
- trouble concentrating
Drug Interactions of Bupropion
Bupropion may interacts with following drugs, supplyments & may change the efficacy of drugs
- MAO inhibitors (phenelzine , selegiline , tranylcypromine)
- beta blockers such as atenolol metoprolol
- insulin or oral medications for diabetes
- medications for irregular heartbeat such as flecainide and propafenone
- medications for mental illness such as haloperidol risperidone , and thioridazine
- medications for seizures such as carbamazepine , phenobarbital and phenytoin
- levodopa
- oral steroids such as dexamethasone
- methylprednisolone and prednisone
- other antidepressants such as desipramine , fluoxetine, imipramine nortriptyline , paroxetine and sertraline
- theophylline
This is not a complete list of all drug interactions of bupropion. Ask your doctor for more information.
Pregnancy & Lactation of Bupropion
FDA Pregnancy Catagory C
Pregnancy
This medication falls into category C. In animal studies, pregnant animals were given this medication and had some babies born with problems. No well-controlled studies have been done in humans. Therefore, this medication may be used if the potential benefits to the mother outweigh the potential risks to the unborn child.
Lactation
Limited information indicates that maternal bupropion doses of up to 300 mg daily produce low levels in breast milk and would not be expected to cause any adverse effects in breastfed infants. However, there is little-reported use in breastfed newborn infants and case reports of a possible seizure in partially breastfed 6-month-old. If bupropion is required by a nursing mother.
References
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