Abizol (aripiprazole) tablets 10 mg. №28

Pharmacodynamics.

The therapeutic effect of aripiprazole in schizophrenia is due to the combination of partial agonistic activity relative to D ₂2-dofamin and 5HT1 _a -serotonin receptors and antagonistic activity relative to 5HT2 of serotonin receptors.

Arypiprazole has high in vitro affinity to D ₂ – and D ₃3-dofamin receptors, 5HT1 _a – and 5HT2 _a -serotonin receptors and moderate affinity to D ₄ -dofaminic, 5HT2 _c – and 5HT7-serotonin receptors, a ₁ -adrenoreceptors and H ₁ -histamines. Aripiprazole is also characterized by moderate affinity for serotonin re-taking areas and the lack of affinity to muscles. Abizol in animal experiments showed antagonism relative to dopaminergic hyperactivity and agonism relative to dopaminergic hypoactivity. Interaction not only with dopamine and serotonin receptors can explain some of the clinical effects of aripiprazole.  

Pharmacokinetics.

The activity of the drug is due to the active substance – aripiprazole. The average half-life of the drug is approximately 75 hours. The equilibrium concentration is achieved after 14 days. Cumulation of the drug with multiple intake is predictable. Indicators of pharmacokinetics of Abizol in an equilibrium state are proportional to doses. No daily fluctuations in the distribution of aripiprazole and its metabolite dehydroaripiprazole are noted. It has been established that the main metabolite of the drug in human blood plasma, dehydroaripiprazole, has the same affinity to D ₂ -dofaminic receptors as aripiprazole.

The drug is quickly absorbed after taking. The maximum concentration (C _max) of aripiprazole in the blood plasma is achieved after 3-5 hours. The absolute bioavailability of the drug is 87%.

Indications

Adults.

Treatment of schizophrenia.

Treatment of moderate and severe manic episodes of bipolar disorder type I.

Prevention of new manic episodes in patients who have already undergone these episodes and who were treated with Abizol.

Increased sensitivity to aripiprazole or any other component that is part of the drug. Phenylketonuria.