Index of drugs

Treatment of major depressive episodes.

1 tabl powl. Modified release contains 150 mg or 300 mg of bupropion hydrochloride.

Antidepressant. A selective inhibitor of the neuronal uptake of catecholamines (noradrenaline and dopamine). It has minimal effect on indole amine uptake (serotonin). It does not inhibit MAO activity. The mechanism of action in the treatment of depression is not known, probably associated with a noradrenergic and / or dopaminergic mechanism. After oral administration of 300 mg bupropion hydrochloride in the form of about modifications. The maximum blood concentration occurs after approximately 5 hours. Total bioavailability is unknown, urinary excretion data suggest that at least 87% of the dose is absorbed from the gastrointestinal tract. It is extensively metabolised in the body. The three major metabolites (hydroxybupropion and aminoalcoholic isomers - threhyde and erythrohydrobupropion) show pharmacological activity. The active metabolites are then metabolized into inactive forms and excreted in the urine. Bupropion, hydroxybupropion and threohydrobupropion bind moderately to proteins (84%, 77%, 42%, respectively). researchin vitro show that bupropion is metabolised to the active metabolite - hydroxybupropion primarily by the CYP2B6 isoenzyme, while CYP1A2, 2A6, 2C9, 3A4, 2E1 are involved in the metabolism to a lesser extent. Bupropion and hydroxybupropion are inhibitors of the CYP2D6 isoenzyme. Bupropion is mainly excreted as metabolites: 87% in urine and 10% in faeces, only 0.5% of bupropion is excreted unchanged. Medium T_0,5 in the phase of elimination of bupropion and hydroxybupropion is approx. 20 h, threohydrobupropion - 37 h, erytrohydrobupropion - 33 h.

Hypersensitivity to bupropion or any of the excipients. The use of other preparations containing bupropion, because the occurrence of seizures is dose dependent and to avoid overdose. Seizures presently occurring or in history. Diagnosed tumors o.u.n. Severe cirrhosis. Current or previous bulimia or anorexia nervosa. Concomitant use of MAO inhibitors; the preparation can be used no sooner than 14 days after the end of treatment with irreversible MAO inhibitors, a period of 24 h is sufficient for reversible MAO inhibitors. The preparation is contraindicated in patients who suddenly discontinued alcohol or other medications discontinued during treatment is at risk of a seizure (especially benzodiazepine and benzodiazepine-like agents).

Due to the increased risk of seizure, special care should be taken in patients with one or more factors predisposing to lowering the threshold of convulsive excitability, eg concomitant use of other drugs that lower the threshold of seizures (eg antipsychotic, antidepressant, antimalarial drugs, tramadol , theophylline, systemic steroids, quinolones and antihistamines acting soothingly), alcohol dependence, history of head injury, diabetes mellitus treated with hypoglycemic agents or insulin, use of stimulants or appetite suppressants. Treatment with the preparation should be discontinued and it is not recommended for patients who have experienced seizures during therapy. Depression is associated with an increased risk of suicidal thoughts, self-harm and suicide. This risk persists until there is clear remission. The patient should remain under strict control until improvement occurs and at an early stage of recovery (increased risk of suicide). Patients with a history of suicide related events or those who have shown a significant degree of suicidal ideation prior to commencement of therapy are at increased risk of suicidal thoughts or suicide attempts and should stay under strict treatment (especially in the early stages or after a change in dosage) control, especially patients under 25 years of age. Special care should be taken when changing the dosing schedule, including discontinuation of treatment in patients who develop suicidal thoughts / behaviors, especially if these symptoms are severe, abrupt or not present. Severe episodes of depression may be the initial symptom of bipolar disorder.Treatment of a severe depressive episode with the antidepressant alone may increase the likelihood of a mixed / manic episode being induced in patients at risk for bipolar disorder. Before starting treatment with the antidepressant, patients should be adequately examined to determine the risk of bipolar disorder. Caution should be exercised when treating electroconvulsive therapy in patients co-treated with bupropion, due to limited clinical experience. Treatment with the product should be discontinued immediately if the patient has experienced symptoms of hypersensitivity while taking the drug. Symptoms may develop or recur even after discontinuation of the drug; it is necessary to continue the appropriate symptomatic treatment for a sufficiently long time (at least one week). Caution should be exercised in patients with cardiovascular disease (the drug has been relatively well tolerated in studies on smoking cessation in patients with ischemic heart disease). Baseline blood pressure should be determined when initiating therapy with subsequent monitoring of blood pressure, especially in patients with prior hypertension. Discontinuation of treatment with the preparation should be considered if clinically significant increases in blood pressure are observed. The concomitant use of bupropion and the nicotine transdermal therapeutic system may result in increased blood pressure. The preparation is not indicated for use in children and adolescents under 18 years of age - the safety and efficacy of the drug in this age group have not been established. Treatment with antidepressants is associated with the risk of suicidal thoughts and behaviors in children and adolescents with severe depressive episode and other psychiatric disorders. The preparation should be used with caution in patients with mild to moderate hepatic impairment and with renal impairment (patients in these groups should be closely monitored).

It can only be used during pregnancy if the benefit to the mother outweighs the potential risk to the fetus. Do not use the drug during breast-feeding.

Very often: insomnia, headache, dry mouth, gastrointestinal disorders (nausea, vomiting). Common: agitation, irritability, tremors, dizziness, disturbed taste, blurred vision, tinnitus, increased blood pressure (in some cases significant), redness of the skin, abdominal pain, constipation, loss of appetite, rash, pruritus, sweating, fever , chest pain, weakness, hypersensitivity reactions such as urticaria. Uncommon: depression, confusion, concentration disorders, tachycardia, weight loss. Rare: convulsions (usually generalized tonic-clonic doses, which in some cases may cause post-stroke confusion or memory problems). Very rare: aggression, hostility, irritability, anxiety, hallucinations, abnormal dreams, nightmares, depersonalization, delusions, paranoid thoughts, dystonia, ataxia, Parkinsonism, lack of coordination, memory disorders, paresthesia, fainting, palpitations, vasodilation, orthostatic hypotension, muscle twitching, increased liver enzymes, jaundice, hepatitis, increased urinary frequency and / or urinary retention, erythema multiforme, Stevens-Johnson syndrome, exacerbation of psoriasis, more severe hypersensitivity reactions including angioedema, dyspnoea, bronchospasm, anaphylactic shock; joints, muscles and fever have also been reported in association with rash and other symptoms suggestive of delayed hypersensitivity reactions (these symptoms may resemble serum sickness). Frequency unknown: suicidal thoughts and suicidal behavior.

Orally. Adults: the recommended starting dose is 150 mg once a day. The optimal dose has not been determined in clinical trials. If no improvement is seen after 4 weeks of treatment with 150 mg, the dose may be increased to 300 mg once a day. A 24 h interval should be maintained between each dose. The effect of the drug was observed 14 days after the start of treatment; full antidepressant effect may occur only after several weeks of treatment. Patients with depression should be treated for at least 6 months.
When switching from bupropion to prolonged-release tablets to treatment tablets, the same total daily dose should be used if possible. In patients with mild or moderate hepatic impairment and in patients with renal insufficiency, the recommended dose is 150 mg once a day.
The tablets should be swallowed whole, they should not be broken, crushed or chewed. The preparation can be used regardless of the meal. In order to reduce the occurrence of insomnia, it is recommended to avoid administration of the drug before falling asleep.