Rivastigmin

Chemical name

3-[(1S)-1-(Диметиламино)эт ил]фенилэтилметилкар��амат

Gross

C14-H22-N2-O2

Of drugs

The drugs-antiholinesteraznoe. Selective psevdoobratimy acetylcholinesterase inhibitor brain carbamatnogo type (duration of the blockade acetylcholinesterase is about 9 h). Prevents destroy acetylcholine, selectively increases the acetylcholine in the brain cortex and gippocampe facilitates holinergicescuu transfer improves cognitive processes in Alzheimer's disease. Inhibition cholinesterase can lead to a slowdown of protein fragments beta-predshestvennika amiloida and a amiloidnykh spots (patognomonichnykh for Alzheimer's disease). It absorbed by ingestion, bioavailability of 30-40%. Time to C_max-hour, tying with the plasma protein-40%, the volume of distribution-1,9-2,7 l / kg Easily permeates through GEB. Metabolised primarily by hydrolysis with esterz (biotransformation by the izofermentov zitohroma minimal R450). T_1/2 - 1h. Write mainly kidneys in the form of metabolites, less than 1% from faeces. After 24 h after administration appears more than 90% of the doses. Not Koumouliruet.po studies on animals has teratogenic properties. Safety use during pregnancy in humans and the ability to infiltrate the breast milk are not installed.

Indications

Dementia alzgeimerovsky type (low and moderately expressed in the alleged diagnostirovanna or Alzheimer's disease).

Restrictions on the use of

Ulcers disease stomach and duodenal ulcers, fatigue weakness sinusnogo unit Already, bronchoobstructive syndrome, obstruction of the urinary tract (adenoma gland), convulsions, zakratougolnaya glaucoma.

Pregnancy and lactation

Perhaps if the effect of therapy than the potential risk to the fetus. At the time of treatment should stop breastfeeding.

Contraindications

Гиперчувствительност ь (incl. to carbamoilatino and other derivative carbamata) breastfeeding.

Side-Effects

From the nervous system and sensory organs : increased fatigability, fatigue, dizziness, headache, drowsiness, and the initiation, insomnia, violations orientation, depression, Tremor.so part of the intestine : nausea, vomiting, diarrhoea, pain in the abdomen, anorexia, Dispepcia.prochie : allergic reactions, skin, lower body mass index, infection upper respiratory tract and urinary tract.

Patient interaction

Not recommended simultaneous application with the other holinomimetikami. Do the depoliarizuth miorelaksantov during Narkoza.u Alzheimer patients simultaneous application antatsidov, antiemetics and protivodiabeticakih funds antigipertenziveh preparations central action beta-adrenoblokatorov, blocking calcium channels, digoxin, antianginalnah funds NPVS, estrogen, analgesics, benzodiazepines and antigistaminnah is not accompanied by a change formakokinetiki rivastigmina or risks of side effects. In healthy volunteers has been identified farmakokineticski interaction with digoxinom, varfarinom, diazepam and fluoksetinom.

Overdosing

Symptoms : nausea, vomiting, Diarea.lechenie : Removal of treatment for 24 h, the use of antiemetics, atropine sulfate (with a large overdose in a dose of 0.03 mg / kg / c), and symptomatic therapy. We do not recommend the use of компьютерное as an antidote.

Precautions

Holinergical stimulation could increase the secretion of hydrochloric acid in Jeludke.pobochne effects observed at the time of treatment may be reduced after pass reception of one or more doses of the drug. If side effects persist, the daily dose of the drug should be downgraded to previous well carry the sick. If any of kidney or liver correct dose is not required.

Dosing and Administration

Inside, at the time of delivery. Initial dose-1.5 mg twice a day (with the high degree of sensitivity to holinergicakih to-1 mg twice a day). Good Time in 2 Weeks may increase doses up to 3 mg twice a day and continue at intervals of two weeks to 4.5 and 6 mg / sut. Supporting dose of 1.5-6 mg twice a day. The maximum daily dose of 12 mg / sut. To achieve the best therapeutic effect dose supported to the maximum well perenosimom level.

Literature

Gavrilova SI Pharmacotherapy of Alzheimer's / / RMJ. Modern Psychiatry 1999 .- .- T. 2 .- N 2-3.

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