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Communication Aripiprazole drug receptors - in vitro.

Abilify possesses high in vitro affinity for D2 and D3 receptors, 5HT1a, santoninovym 5HT2a receptors and moderate affinity for dopamine D4. Abilify is characterized by moderate affinity for serotonin reuptake sites and the lack of affinity for muscarinic receptors. Abilify - showed antagonism of dopaminergic hyperactivity and agonism at dopamine hypoactivity.

Activity Abilify-Aripiprazole.

The activity is mainly due to the presence of starting material. The average half-life of Abilify is approximately 75 hours. The equilibrium concentration is reached after 14 days. Drug accumulation after repeated admission predictable. Indicators pharmacokinetics of Abilify in the equilibrium state is proportional to the dose. There was no daily fluctuations in the distribution of Aripiprazole and its metabolite, dehydro-Abilify. It is found that the major metabolite of the drug in human plasma, dehydro-Abilify, has the same affinity for dopamine D2 receptors as Aripiprazole.

Abilify is rapidly absorbed after oral administration with Cmax in plasma drug attained within 3-5 hours. The absolute bioavailability of tablets Aripiprazole is 87%. Eating on Abilify does not affect the bioavailability.

The action of the drug.

Aripiprazole intensively distributed in tissues. At therapeutic concentrations greater than 99% - Abilify bound to serum proteins. It does not affect the pharmacokinetics and pharmacodynamics of warfarin - does not displace warfarin from its association with blood proteins. Treated first-pass metabolism only minimally. It is metabolized in the liver in three ways: dehydrogenation, hydroxylation, N-dealkylation.

According to the experiments in vitro, dehydrogenation and hydroxylation Abilify occurs under the action of enzymes CYP3A4 and CYP2D6 - catalyzed dealkylation of N CYP3A4 enzyme. Aripiprazole is a major component of the drug in the blood. At the equilibrium state AUC dehydro Aripiprazole, or approximately 39% of the AUC in the plasma Abilify.

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Withdrawal Aripiprazole.

Less than 1% Abilify constant determined in urine. Approximately 18% of the dose in unchanged form Aripiprazole is excreted in the feces. The total clearance of Abilify was 0,7ml and minute per 1 kg, mainly due to the elimination by the liver.

Treatment Aripiprazole (Abilify).

  • Acute attacks of schizophrenia (treatment and supportive therapy).
  • Acute manic episodes of bipolar I disorder.
  • For patients with bipolar I disorder who have recently had manic or mixed episode (maintenance therapy).

It prohibited for use in patients.

  • With hypersensitivity to Abilify, or any other components that make up the drug.
  • Patients whose age has not reached 18 years of age.

With care, under the supervision of a physician.

  1. Prescribed to patients with cardiovascular diseases.
  2. In patients with cerebrovascular diseases and conditions predisposing to hypotension.
  3. Patients with seizures.
  4. Patients with an increased risk of hyperthermia.
  5. Patients with an increased risk of aspiration pneumonia.
  6. Patients suffering from obesity and the presence of diabetes.
  7. Pregnancy or breast-feeding.

Attention!
There are no adequate and well-controlled studies of Abilify for pregnant women have been conducted.
Abilify for sale can be taken during pregnancy only if the potential benefit outweighs the potential application risk to the fetus - is strictly under medical supervision!

Data on the penetration of Abilify in human milk is not. Breastfeeding when using the drug is not recommended.

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