Bupropion - instructions for use, doses, side effects, contraindications

Clinical and pharmacological group: & nbsp

Included in the formulation

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АТХ:

N.06.A Antidepressants

Pharmacodynamics:Selective inhibition of reuptake of noradrenaline and dopamine, with a slight inhibition of reuptake of serotonin. It also acts as an antagonist of nicotinic choline receptors. Bupropion belongs to the chemical class of psychoanaleptics and is similar in structure to cationic stimulants and diethylpropion, and in general to phenethylamines.

Pharmacokinetics:

After ingestion of bupropion in prolonged-release tablets, the time to reach the maximum plasma concentration was approximately 5 hours.

Eating does not have a significant effect on the absorption of bupropion when taking prolonged-action tablets.

Bupropion moderately bind to blood plasma proteins - 84%.

The metabolism of bupropion is extremely variable: the effective dose of bupropion, assimilated by patients who received the same amount of the drug, can differ by a factor of 5.5 (with a half-life of the drug varies from 3 to 16 hours), and for hydroxybupropion, the difference can be up to 7.5 times half-life = 12 to 38 hours). Based on these data, some researchers insist on the continuous monitoring of bupropion and hydroxybupion in the blood.

Bupropion is metabolized in the liver.

Bupropion clearance for oral administration is approximately 200 liters per hour, half-life is 20 hours.

Indications:Treatment of depression. When an adequate response is achieved, continuation of bupropion therapy for the prevention of exacerbations and relapses of depressive episodes.

ICD-10

V.F30-F39.F33 Recurrent depressive disorder

V.F30-F39.F32 Depressive episode

Contraindications:

Hypersensitivity to bupropion or any other component of the drug, convulsive disorder, abrupt withdrawal of alcohol or sedatives (including benzodiazepines).

Concomitant use of other bupropion-containing drugs (the onset of seizures is a dose-dependent effect), bulimia or anorexia nervosa in the anamnesis (possibly the occurrence of seizures), concomitant use with monoamine oxidase inhibitors.

Do not start therapy with bupropion at least after 2 weeks after the withdrawal of irreversible monoamine oxidase inhibitors.

Age to 18 years.

Carefully: Use in patients with impaired liver function, impaired renal function, cardiovascular disease and reduced threshold convulsive readiness.

Pregnancy and lactation:

Recommendations Food and Drug Administration (US Food and Drug Administration) category - C. The safety of bupropion in pregnant women is not established.

Bupropion can be administered during pregnancy to patients only in cases where the expected benefit from its use exceeds the possible risk.

Bupropion and its metabolites penetrate into breast milk, it is recommended to stop breastfeeding during bupropion therapy.

Dosing and Administration:

Tablets of bupropion prolonged action should be swallowed whole, without chewing, not breaking or chopping, as this can lead to an increased risk of adverse reactions, including convulsive disorders.

The initial dose of bupropion is 150 mg once a day, in the morning.

If an adequate therapeutic response is not achieved, it is recommended to increase the dose to the usual target dose for adults 300 mg once a day.

An increase in the dose to a maximum daily dose of 450 mg once a day is possible for patients who do not experience clinical improvement after several weeks of therapy at a dose of 300 mg per day.

Acute episodes of depression require continuous treatment lasting from 6 months after reaching the initial therapeutic response. The effectiveness of bupropion (300 mg per day) is proven with prolonged therapy (up to 1 year).

The maximum single dose of sustained-release bupropion should be no more than 450 mg. The interval between bupropion should be at least 24 hours after the last dose. Increase the dose should not be more than 100 mg per day for three days.

Side effects:

From the immune system: hypersensitivity reactions such as urticaria, more severe hypersensitivity reactions, including angioedema, dyspnea / bronchospasm and anaphylactic shock, arthralgia, myalgia and fever, accompanied by a rash and other symptoms of a delayed-type hypersensitivity reaction. These symptoms may resemble serum sickness.

On the part of metabolism: anorexia, weight loss, changes in blood glucose concentration.

On the part of the psyche and behavior: insomnia, agitation, anxiety, depression, confusion, aggression, hostility, irritability, anxiety, hallucinations, unusual dreams, depersonalization, illusions, delusions.

From the side of the nervous system: headache, tremor, dizziness, dyspnoea, impaired ability to concentrate, convulsive disorders, dystopia, ataxia, parkinsonism, movement coordination disorders, memory impairment, paresthesia, fainting.

From the cardiovascular system: increased blood pressure, tachycardia, palpitation, vasodilation, orthostatic hypotension.

On the part of the gastrointestinal tract: dry mouth, gastrointestinal disorders, including nausea and vomiting, abdominal pain, constipation, increased activity of hepatic enzymes, jaundice, hepatitis.

Other: visual disturbances, ringing in the ears, rash, itching, sweating, erythema multiforme, Stevens-Johnson syndrome. Fever, chest pain, asthenia, frequent or delayed urination.

Overdose:

Drowsiness, loss of consciousness and changes in the electrocardiogram - conduction disorders (including QRS lengthening) or arrhythmia.It was reported about a case of simultaneous ingestion of bupropion in doses 10 times higher than the maximum therapeutic dose.

Treatment

The specific antidote of bupropion is not known.

In case of an overdose, hospitalization is recommended. It is necessary to monitor the electrocardiogram and indicators of vital functions. It is required to provide airway patency, oxygenation and pulmonary ventilation. Once the bupropion is taken orally, the use of activated carbon is indicated. Further tactics of treatment should be based on the clinical picture and recommendations of the toxicological center.

Interaction:

Drugs affecting the activity of the isoenzyme CYP2B6 (eg, orfenadrine, cyclophosphamide, ifosfamide, ticlopidine, clopidogrel): be careful.

Beta-blockers: treatment should be initiated when the lower dose range of the concomitant drug is reached.

Antiarrhythmics: treatment should be initiated when the lower dose range of the concomitant drug is reached.

Selective serotonin reuptake inhibitors: treatment should be initiated when the lower dose range of the concomitant drug is reached.

Tricyclic antidepressants: treatment should be initiated when the lower dose range of the concomitant drug is reached.

Antipsychotic drugs: treatment should be initiated when the lower dose range of the concomitant drug is reached.

Levodopa: increased incidence of psychoneurological adverse reactions.

Amantadine: an increase in the incidence of psychoneurological adverse reactions.

Transdermal nicotine system: may cause an increase in blood pressure.

Special instructions:

Insomnia is a very common side reaction of a transient nature, if necessary, reduce the dose or frequency of taking the drug. Do not take the drug before bedtime, observing a 24-hour interval between taking the drug.

Unlike many other antidepressants, bupropion does not cause weight gain and sexual dysfunction.

Impact on the ability to drive vehicles and manage mechanisms

Like other drugs that affect the central nervous system, bupropion can adversely affect the ability to perform tasks that require clarity of consciousness,and motor activity and cognitive skills. Patients should be careful when driving and / or other mechanisms.

Instructions

Bupropion (Bupropionum)