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ABILIFY / ABILIFY Tablets Aripiprazole

ABILIFY / ABILIFY Tablets Aripiprazole



Packaging, composition and manufactured form:
ABILIFY number 28 15mg tablets are yellow with a facet round shape. On one side labeling - "15", on the other - "A-009. Each tablet contains 15 mg of aripiprazole. Additional components: yellow iron oxide, magnesium stearate, hydroxypropyl cellulose, corn starch, microcrystalline cellulose, lactose monohydrate. The tablets are placed on the 7 pieces in blisters. On 4 packs in one carton box. Registration Number: LS-001812, 07/28/2006.

ABILIFY number 28 5mg tablet blue in color with rounded edges to form a rectangle. On one side labeling - "5", on the other - "A-007.
Each tablet contains 5 mg of aripiprazole. Additional components: the blue lacquer aluminum, magnesium stearate, hydroxypropyl cellulose, corn starch, microcrystalline cellulose, lactose monohydrate. The tablets are placed on the 7 pieces in blisters. On 4 packs in one carton box. Registration Number: LS-001812, 07/28/2006.

ABILIFY number 28 10mg tablets pink with rounded edges to form a rectangle. On one side labeling - "10", on the other - "A-008. Each tablet contains 10 mg of aripiprazole. Additional components: a dye, red iron oxide, magnesium stearate, hydroxypropyl cellulose, corn starch, microcrystalline cellulose, lactose monohydrate. The tablets are placed on the 7 pieces in blisters. On 4 packs in one carton box. Registration Number: LS-001812, 07/28/2006.

The following description is based on instructions edition in 2008 on the use of ABILIFAY, which was approved by the manufacturer.
Farmakovozdeystvie:
Neuroleptic (antipsychotic therapeutic agent). Believe that the effect of aripiprazole in schizophrenia is caused by a combination of a partial agonist of the intensity with respect to the serotonin receptors and 5NT1 and D2 dopamine receptors, as well as antagonistic activity plan in relation to serotonin receptors 5NT2.
Aripiprazole has a high and a moderate in vitro affinity for histamine receptors H1, a1 adrenoreceptors, 5HT7 serotonin receptors and 5HT2c, D4 dopamine receptors.
Aripiprazole in addition has no affinity for muscarinic receptors and affinity (moderate) to the areas of capture (inverse) of serotonin.
In animal experiments, it was noted that aripiprazole reveals for hyperactivity (dopaminergic) and reveals the antagonism against gipoaktivnosti dopaminergic agonism. Part of its clinical effects have the opportunity to explain the reactions with serotonin and dopamine receptors.

Farmakogruppa:
Neuroleptic (antipsychotic therapeutic agent).

Pharmacological kinetics
Suction process
After use, inward absorbed rapidly from the gastrointestinal tract. After a period of 3 to 5 hours in the plasma of fixed C max. Bioavailability is 87 percent. The bioavailability of the drug consumption of food has no effect.
Metabolism and distribution
Css is fixed in two weeks. With repeated use of cumulation is possible to predict the parameters ABILIFAY. The values of the pharmacological kinetics in equilibrium aripiprazole proportional to its dosage. Not recorded changes throughout the day allocation processes as metabolite of aripiprazole degidroaripiprazola, and it directly.
Aripiprazole actively spreading in the tissues. Vd is equal to 4.9 L / kg. When the value of aripiprazole over 99 percent of its observed binding to proteins in the serum (mainly albumin).
It is known that the main metabolite in human plasma degidroaripiprazol, aripiprazole has a similar affinity for the dopamine receptor D2.
ABILIFY subject to presystemic metabolism of the nature of the insignificant level. The liver is metabolized in the following ways: N-dealkylation, hydroxylation, and dehydrogenation. In vitro hydroxylation and dehydrogenation is carried out under the influence of isozymes CYP2D6 and CYP3A4, dealkylation - under the influence of CYP3A4.
ABILIFY intensity of exposure is dependent on the presence of unchanged aripiprazole form. In equilibrium degidroaripiprazol has an indicator in the plasma AUC by about 39 percent of the AUC of aripiprazole.
Processes of elimination
The average T1 / 2 equals 75 hours.
After a single use of 14C-labeled aripiprazole about 60% and 27% of the radioactivity fixed in the feces and urine, respectively. Less than 1 percent of aripiprazole continuing progress in the urine and about 18% of output consumed along with the feces unchanged. Clearance (total) of aripiprazole equals 0.7 ml / min / kg, mainly due to the fact that the liver is derived.
Aripiprazole has no effect on the dynamics of pharmacological and pharmacological kinetics of warfarin (in other words - from its association with blood proteins, aripiprazole does not displace warfarin).
 

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