Freim tablets 15 mg. №30

Description

Freim tablets Storage:

active substance: aripiprazole;

1 tablet contains aripiprazole 5 mg or 10 mg, or 15 mg, or 30 mg;

Freim tablets excipients:

5 mg tablets: lactose monohydrate; microcrystalline cellulose; croscarmellose sodium; colloidal anhydrous silica; magnesium stearate; indigo carmine (E 132); vanilla flavor (contains propylene glycol and benzyl alcohol); aspartame (E 951);

10 mg tablets: lactose monohydrate; microcrystalline cellulose; croscarmellose sodium; colloidal anhydrous silica; magnesium stearate; iron oxide red (E 172); vanilla flavor (contains propylene glycol and benzyl alcohol); aspartame (E 951);

15 mg tablets: lactose monohydrate; microcrystalline cellulose; croscarmellose sodium; colloidal anhydrous silica; magnesium stearate; iron oxide yellow (E 172); vanilla flavor (contains propylene glycol and benzyl alcohol); aspartame (E 951);

30 mg tablets: lactose monohydrate; microcrystalline cellulose; croscarmellose sodium; colloidal anhydrous silica; magnesium stearate; iron oxide red (E 172); vanilla flavor (contains propylene glycol and benzyl alcohol); aspartame (E 951).

Freim tablets Dosage form.

Tablets.

Basic physical and chemical properties:

5 mg tablets – blue, rectangular, biconvex tablets, smooth on both sides;

10 mg tablets – pink, rectangular, biconvex tablets, smooth on both sides;

15 mg tablets – yellow, round, flat tablets, smooth on both sides;

30 mg tablets – pink, round, flat tablets, smooth on both sides.

Pharmacotherapeutic group. Antipsychotics (neuroleptics).

ATX code N05A X12.

Pharmacological properties.

Pharmacodynamics.

The therapeutic effect of aripiprazole in schizophrenia is due to a combination of partial agonist activity against D2-dopamine and 5HT1a-serotonin receptors and antagonistic activity against 5HT2-serotonin receptors.

Aripiprazole has high in vitro affinity for D2- and D3-dopamine receptors, 5HT1a- and 5HT2a-serotonin receptors and moderate affinity for D4-dopamine, 5HT2c- and 5HT7-serotonin receptors, α1-adrenoceptors and H1. Aripiprazole is also characterized by moderate affinity for serotonin reuptake sites and lack of affinity for muscarinic receptors. Aripiprazole in animal experiments showed antagonism against dopaminergic hyperactivity and agonism against dopaminergic hypoactivity. Some clinical effects of aripiprazole may be explained by interactions not only with dopamine and serotonin receptors.

Pharmacokinetics.

The activity of the drug is due to the active substance – aripiprazole. The mean half-life of aripiprazole is approximately 75 hours. Equilibrium concentration is reached after 14 days. Accumulation of the drug with repeated administration is expected. The steady-state pharmacokinetics of aripiprazole are dose proportional. No daily fluctuations in the distribution of aripiprazole and its metabolite dehydroaripiprazole were observed.

Aripiprazole is rapidly absorbed after ingestion. The maximum concentration (Cmax) of aripiprazole in blood plasma is reached in 3-5 hours. The absolute bioavailability of the drug is 87%. Food intake does not affect the bioavailability of aripiprazole.

At therapeutic concentrations, more than 99% of aripiprazole is bound to serum proteins, mainly albumin. Aripiprazole is only minimally amenable to presystemic metabolism. Aripiprazole is metabolized in the liver in three ways: dehydrogenation, hydroxylation, and N-dealkylation. According to in vitro experiments, dehydrogenation and hydroxylation of aripiprazole occurs under the action of enzymes CYP3A4 and CYP2D6, and N ‑ dealkylation is catalyzed by the enzyme CYP3A4. Aripiprazole is a major component of the drug in the blood. At steady state, the area under the concentration-time curve (AUC) of dehydroaripiprazole in plasma is about 39% of the AUC of aripiprazole.

After a single dose of [14C] -labeled aripiprazole, approximately 27% and 60% of the radioactivity were detected in urine and feces, respectively. Less than 1% of unchanged aripiprazole is detected in the urine and approximately 18% of the administered dose is excreted unchanged in the feces. The total clearance of aripiprazole is 0.7 ml / min / kg, mainly due to hepatic excretion.

Clinical characteristics.

Indication.

Adults

Treatment of schizophrenia.

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

Prevention of new manic episodes in patients who have already experienced these episodes and who have been treated with aripiprazole.

Contraindication.

Hypersensitivity to aripiprazole or to any other component of the drug.