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Emsam (Selegiline)

Description

Emsam scope of action - antiparkinsonian agent. Irreversibly inhibits MAO. Preferentially binds MAO B, oxidizing catecholamines (dopamine, norepinephrine, epinephrine, serotonin). It increases the concentration of dopamine in the CNS and eliminates the deficit in the extrapyramidal system. Not potentiates the activity of indirect agonists and serotonin. The drug forms metabolites (amphetamine, methamphetamine), inhibits the reuptake of dopamine in the synapse. The plasma is bound to proteins (94%). When taken orally the medication is metabolized mainly in the liver.

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Indications for use

The medication is designed for Parkinson's disease and symptomatic parkinsonism treatment.

Clinical trials confirm significant improvement in specific cognitive tests (memory tests Sternberg) with Emsam intakes. Statistically significant improvement in global clinical status and behavior/mood are also observed.

Dosing and Administration

Emsam is appointed for perioral administration - 10 mg per day 2 divided into doses of 5 mg at breakfast and lunch. It is typically used in conjunction with combinations of levodopa/carbidopa. During long-term therapy may reduce the dose of levodopa.

Contraindications

The drug course must not be initiated in case of hypersensitivity, extrapyramidal disorders not related to dopamine deficiency (essential tremor, Huntington's chorea); pregnancy, breast-feeding.

Restrictions apply to the following cases: peptic ulcer and duodenal ulcer, uncontrolled hypertension, severe angina pectoris, psychosis, glaucoma, hyperthyroidism, pheochromocytoma, prostatic hyperplasia (with the presence of residual urine), 18+ years old. During pregnancy and breast-feeding the course should be ceased (the medication affects the fetus - C rating assigned by FDA).

Side effects

From the nervous system and sensory organs: anxiety, fatigue, dizziness, headache, drowsiness or insomnia, depression, hallucinations, confusion, speech, gait, supraorbital pain, impaired visual acuity, diplopia. Cardio-vascular system and blood (blood, hemostasis): arrhythmia, orthostatic reactions, increased blood pressure, swelling. From the digestive tract: nausea and vomiting, loss of appetite, dry mouth, indigestion, constipation or diarrhea, exacerbation of peptic ulcer disease, increase in liver transaminases. Other: disorders of sexual function, urinary retention, aggravation of asthma, dysuria, rash, photosensitivity, skin rashes.

However, in clinical trials the proportion of patients who discontinued treatment due to side effects of therapy with placebo was ranging from 0% to 9%. There was a significant increase in the occurrence of disorders of balance and falls into a group of selegiline (22%) versus placebo (5%). Almost all of these patients selegiline combined with vitamin E.

Usage with other drugs

Potentiates the effects of levodopa. The combined use of tricyclic antidepressants, MAO inhibitors and fluoxetine can cause toxic reactions - hyperthermia, rigidity, myoclonus, coma.

Overdose

Symptoms may develop ‘cheese’ syndrome (inhibits all types MAO) as hypertensive reactions and exacerbation of CHD after ingestion of food containing tyramine (cheese, coffee, etc.) stimulation. In case of overdose the following methods can be used: induction vomiting, gastric lavage, administration of activated charcoal; symptomatic therapy.

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