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Selegiline is selective inhibitor of MAO type B inhibits metabolism of dopamine, causing an increase in its concentration in the neurons of the extrapyramidal system. Potentiates and prolongs the therapeutic effect of levodopa.
Selegiline is rapidly absorbed in the digestive tract. Cmax in plasma attained at 30 min after ingestion. Bioavailability is low, on average 10% of unchanged Selegiline enters the systemic circulation (high individual variation). Selegiline is a lipophilic substance with a slightly alkaline reaction, which rapidly penetrates into tissues, including the brain. At therapeutic concentrations, 75-85 % Selegiline binds to plasma proteins. Selegiline is rapidly metabolized, mainly in the liver up dezmetilselegilina, 1- methamphetamine and 1- amphetamine. Average T ? metabolites was 2 hours for desmetilselegilina 17.7 h – for 1 -amphetamine and 20.5 h – 1 for methamphetamine. The total clearance of Selegiline is about 500 l / h Selegiline metabolites found mainly in urine, about 15% – in the feces.
Parkinson’s disease, symptomatic parkinsonism, Alzheimer’s disease, mild to moderate senile dementia of the Alzheimer type.
Before use Selegiline, you should know that the treatment with the medicine requires individual dosage.
Parkinson’s disease – 10 mg / day in 1-2 doses; Alzheimer’s – 10.5 mg / day in 1 or 2 divided doses (every 1-2 hours). Max dose – 10 mg / day (in doses of 30-40 mg / day selectivity of Selegiline against MAO-B is lost).
Hypersensitivity, extrapyramidal disorder, not related to dopamine deficiency (essential tremor, Huntington’s chorea), concomitant use of antidepressants and the period up to 5 weeks after their withdrawal, pregnancy, lactation. Progressive dementia, severe psychosis, tardive dyskinesia, tremor krupnorazmashisty, peptic ulcer gastrointestinal (including history), hyperthyroidism, pheochromocytoma, prostatic hyperplasia (with the presence of residual urine), angle-closure glaucoma, tachycardia, severe angina, diffuse toxic goiter, age 18 years (experience in clinical application is not enough). When combined with levodopa : open-angle glaucoma (chronic), liver and / or kidney failure, melanoma (including history), CNS depression, seizures, asthma, emphysema, myocardial infarction (including history, as well as in combination with atrial, nodal or ventricular arrhythmias), age 12 (safety and efficacy not established).
Adding use Selegiline to levodopa treatment can cause the development of involuntary movements and / or arousal. These side effects disappear at lower doses of levodopa. The dose of levodopa, Selegiline adding the average may be reduced by 30 %. Before use Selegiline, you should know that the drug in the treatment may worsen the condition of patients with peptic ulcer history, labile hypertension, cardiac arrhythmias, severe angina, psychosis.
Selegiline: Side effects
Transient elevation of ALT in the blood plasma, and sleep disorders. Since Selegiline potentiates the clinical effect of levodopa, side effects of levodopa, particularly involuntary movements, nausea, agitation, confusion, hallucinations, headache, postural hypotension, arrhythmia and dizziness may become more pronounced with the addition of Selegiline to the maximum tolerated dose of levodopa. Also during treatment with Selegiline have been described difficulty urinating and skin reactions.
Contraindicated with concomitant use of tricyclic antidepressants. Purpose Selegiline sympathomimetics (ephedrine) and preparations of CNS depressant (including ethanol), can potentiate their effect. Avoid the development of serotonin syndrome, accompanied by mania, hyperhidrosis, fever and hypertension, should not be used simultaneously with fluoxetine Selegiline, it is administered no earlier than 5 weeks after discontinuation of fluoxetine. May cause delirium, stupor, anxiety, agitation, and muscle rigidity, while the appointment of Selegiline and peptidina. The simultaneous use of Selegiline with amantadine and anticholinergic drugs increases the risk of side effects.
Data on clinically significant overdose Selegiline no. Symptoms are similar to those observed with an overdose of non-selective MAO inhibitors. No specific antidote, treatment is symptomatic.