Selegiline

Chemical name

(R)-N,альфа-Диметил-N-2-пр опинилбензолэтанамин (as hydrochloride)

Gross

C13-H17-N

Characteristics

White or almost white crystalline powder dissolves easily in water, chloroform, methanol.

Of drugs

The drugs - противопаркинсоничес кое. Ingibiruet irreversible MAO. Mostly links MAO B, patents kateholamin (dofamin, noradrenalin, adrenaline, serotonin). Increases in the CNS dopamine concentration and eliminates the deficit ekstrapiramidna system. Not potenziruet activity proximity adrenomimetikov and Serotonin.obrazuet metabolites (amphetamine, methamphetamine), a person's return hostage release in neurotransmission. The plasma is associated with the protein (94%). In oral metabolised mainly in the liver education is N-desmetilselegilina (ingibiruet MAO), and small quantities of L-amfetamina and L-metamfetamina. N-desmetilselegilina concentration in plasma exceeds the selegilina in 4-20 times. T_1/2 variabelen, ranging from 2 to 10 hours Metabolites derived from urine.

Indications

Parkinson's disease, symptomatic parkinsonism; Integrated treatment of Alzheimer's and endogenous depression.

Contraindications

Hypersensitivity, pregnancy, breast-feeding (at the time of treatment to a breast-feeding).

Side-Effects

Anxiety, fatigue, drowsiness or insomnia, depression, hallucinations, sputannosti consciousness, the speech, gait, migraine, supraorbitale pain, diplopia, disorders of sexual function Already, orthostatic reaction gipotenzia, oedema, dry mouth, neuralgia, the worsening ulcers, increasing transaminaz, aggravation of asthma dizuria, rash, photosensitization, skin rashes.

Patient interaction

Potenziruet effects of levodopa. The combined use of tricyclic antidepressants, MAO inhibitors and fluoksetinom can cause toxic reaction, gipertermiu, rigidity, mioclonus, coma.

Overdosing

Symptoms : Evolution "sarnogo" syndrome (ingibiruet all types MAO) in the form of gipertenziveh reactions, and the exacerbation of disease after eating food containing tiramin (cheese, coffee, etc.), the institution.

Precautions

Be wary designate of renal failure, pathology circulatory system, ulcers stomach and duodenal ulcers, glaucome, Thyroid diseases and napochechnikov. Reduces the speed of reaction and attention, as it is necessary to inform drivers and working with potentially dangerous machinery. It should be borne in mind long posleactie preparation for the MAO-up to 5-7 days in the appointment adrenomimetikov. Selegilin may be nominated in five weeks after fluoksetina (prozaka).

Dosing and Administration

Inside, 10 mg / day in 2 admission to 5 mg for breakfast and lunch. Typically, the association with combinations levodopa / carbidopa. In the long-term therapy may reduce the dose of levodopa.

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