Takrin (tacrine)
TAKRIN (Tacrine).
9-Amino-1, 2,3,4 - tetragidroakridin.
Is reversible cholinesterase inhibitor (butiril- more than acetylcholinesterase) fosters holinergicheskih of acetylcholine neurons; Because of this increased acetylcholine content in tissues, including the nervous. Moderately inhibited MAO-type, as well as the reverse takeover neyronalny noradrenalina, dofamina, serotonin. Membrane blocking potassium channels, lengthens the potential action.
Well-absorbed, bioavailability of approximately 17% (due to the effect "first pass through the liver); With max 1-2 h; The main active metabolite 1-acid takrin called Velnakrin "is also used as a antiholinesteraznogo substance.
Earlier takrin antikurarevoe used as a tool (see Prozerin). In recent years, in connection with violations of roles central holinergicheskih processes with senile dementia, it was used as a tool in the treatment of these diseases.
Accepted inside (to food) is usually in the dose of 0.01 (10 mg) 4 times a day. If necessary, gradually add up to 0.16 g dose (160 mg) a day.
Treatment for the long-term, carefully observing the condition of patients.
In a possible drug side effects associated with its holinomimeticheskoy activity: aetiology, bronchospasm, diarrhea, vomiting and other, as well as dizziness, ataxia, anorexia, jaundice.
Takrin contraindications with bronchial asthma, epilepsy, aetiology, violations of the liver.
Form release: capsules to 0.01; 0.02; 0.03 and 0.04 g (10; 20; 30 and 40 mg).
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