Following sublingual asenapine is rapidly absorbed and the maximum concentration (the C max ) in plasma is observed trenbolone acetate side effects in 0.5-1.5 h. The absolute bioavailability of asenapine 5 mg for sublingual application is 35%.
The absolute oral bioavailability is low (<2%). Admission of water after 2 or 5 minutes after administration of asenapine led to a decrease in the blood concentration of asenapine (19% and 10% respectively). Therefore within 10 minutes after administration of asenapine should not drink or eat.
Asenapine is rapidly distributed. Large volume of distribution (approximately 1700 l), which indicates the distribution of the active into the extravascular space. Asenapine efficiently (95%) bound to plasma proteins – albumin and α 1 – acid glycoprotein.
In a study in vivo in humans treated with labeled asenapine, preferably in the plasma were determined asenapine N + -glyukuronid and a lesser concentration of other metabolites, including desmetilazenapin N-, N-N-desmetilazenapina carbamoylglucuronide and unmodified asenapine. Drug activity is determined mainly unchanged asenapine.
Asenapine – a weak inhibitor of the isoenzyme. It does not cause induction isoenzymes in cultured human hepatocytes.
Concomitant use of asenapine with known inhibitors, inducers or substrates of these isoenzymes studied in clinical trials of drugs interactions (see. “Interaction with other medicinal products” section).
clearance asenapine high and after intravenous administration of 52 l / h. Most of the radiolabeled dose of asenapine excreted by the kidneys trenbolone acetate side effects (50%) and through the intestine (40%). Only a small part of the dose is excreted through the intestines (5-16%) as unchanged asenapine. After an initial more rapid distribution phase half-life of asenapine is approximately 24 hours.
dose increase from 5 to 10 mg twice a day, leading to a nonlinear increase (1.7 times) the area under the curve “concentration – time” (AUC) and C max . Disproportionate increase in C max and AUC with increasing dose may be due to limits absorption through the oral mucosa after sublingual administration.
Before the drug twice a day equilibrium state is achieved within 3 days. In general, the pharmacokinetics of asenapine in an equilibrium state similar to that following a single dose.
Pharmacokinetics in specific patient populations
Patients with impaired hepatic function
The pharmacokinetics of asenapine is similar in patients with mild (Class A according to Child-Pugh) and moderate (Class B for Child-Pugh) hepatic impairment and patients with normal liver function. In patients with severe hepatic impairment (class C Child-Pugh) showed a 7-fold increase in AUC of asenapine (see. “Dosage and Administration”section).
Patients with impaired renal function
The pharmacokinetics of asenapine following a single dose of 5 mg asenapine were similar in patients with varying degrees of renal impairment and patients with normal renal function.
Elderly patients are
elderly patients asenapine AUC was approximately 30% higher than in younger adults.
pharmacokinetics of asenapine 5 mg twice daily in adolescents aged 12 to 17 years inclusive was similar to that in adults. Adolescents with increasing doses of 5 to 10 mg twice a day did not increase the AUC asenapine.
When a population trenbolone acetate side effects analysis was not revealed according to the pharmacokinetics of the floor.
In a population pharmacokinetic analysis of race has no significant effect on the pharmacokinetics of asenapine.
In a population pharmacokinetic analysis showed that smoking, which causes induction of isoenzyme CYP1A2, has no effect on the clearance of asenapine. In a special study on the background of smoking a single dose of 5 mg sublingual no effect on the pharmacokinetics of asenapine.
Indications for use:
shown to treat acute and maintenance of adult patients with schizophrenia.
Bipolar Affective Disorder
Monotherapy: The s indicated for cupping treatment of manic or mixed episodes associated with bipolar disorder in adults.
Additional therapy: is shown as an adjunct therapy with lithium preparations or valproate for the relief of manic or mixed episodes associated with bipolar affective disorder in adults.
- Hypersensitivity to asenapine or any other component of the formulation;
- Children up to age 18 years (effectiveness and safety have been studied);
of elderly patients with psychosis on dementia
in elderly patients with psychosis on dementia in the treatment of antipsychotic drugs are at increased risk of death. The trenbolone acetate side effects is not recommended for the treatment of patients with psychosis on dementia. rexobol