The pharmacokinetic properties of atazanavir were evaluated in healthy volunteers and HIV-infected patients. Absorption: chronic administration of the drug Reyataz 400 mg once daily at the same time taking an easily digestible food bayer primobolan depot maximum equilibrium concentration of atazanavir in plasma is established in about 2.7 hours after administration . Stable equilibrium concentration of atazanavir achieved between the 4th and 8th days of receipt. The effect of food: the use of the drug with food enhances bioavailability and reduces pharmacokinetic variability. The use of a combination ritonavir with food enhances the bioavailability of atazanavir. Distribution: atazanavir by 86% bound to serum proteins, the degree of protein binding is independent of concentration. In a similar degree atazanavir binds alpha-1 acid glycoprotein and albumin. Atazanavir is determined in the cerebrospinal and seminal fluid. Metabolism: atazanavir is metabolized primarily by isozyme to oxygenated metabolites. Metabolites are excreted in bile in free form or in form of conjugates with glucuronic acid. A small part of atazanavir is metabolised by N-dealkylation and hydrolysis.
Excretion: After a single administration of 14C-atazanavir (400 mg) in the feces and urine was determined, respectively, 79% and 13% of the total radioactivity. Ratio atazanavir unchanged in the feces and urine was, respectively, 20% and 7% of the administered dose. The average half-life of atazanavir in healthy volunteers and HIV-infected adults was around 7:00 when taking 400 mg per day, easily digestible food.
Indications for use:
HIV-1 infection in combination with other drugs antiretrovirusnshi, in patients previously treated or not treated with antiretroviral therapy.
- Hypersensitivity to atazanavir or any drugomukomponentu drug;
- Severe liver failure in any dosing regimen;
- The combination of Reyataz / ritonavir in patients with hepatic impairment;
- Lactase deficiency, bayer primobolan depot lactose intolerance, glucose-galactose malabsorption
- Reyataz in combination with astemizole, terfenadine, cisapride, pimozide, bepridilom, quinidine, triazolam, midazolam (oral), ergot alkaloids (especially ergotamine, dihydroergotamine, ergometrine, metilergometrina), drugs St. John’s wort, simvastatin, lovastatin, indinavir, irinotecan, rifampin;
- The combination of Reyataz / ritonavir together with quinidine;
- Children under 18 years old.
Precautions: diabetes mellitus, hyperglycemia, dyslipidemia, hyperbilirubinemia, nefrolptiaz, viral hepatitis, liver disease, hemophilia A and B, the syndrome of congenital prolongation of the interval PR, syndrome of congenital lengthening the interval QT, gastric hyperacidity, joint application with nevirapine, efavirenz, glucocorticoids .
Pregnancy and lactation
There are no adequate and well-controlled studies in pregnant women have not been conducted. Reyataz should be used during pregnancy only if the potential benefits of the use of the mother outweighs the potential risk to the fetus. It is unknown whether atazanavir into breast milk. In connection with the possibility of transmission of HIV from mother to child with milk, and because of the risk of serious side effects in children, should not breastfeed when using the drug.
Dosage and administration:
The drug is taken orally in combination therapy.
The decision to start therapy takes a doctor with experience in the treatment of HIV infection. The dosage regimen for patients who have not previously received antiretroviral therapy:
- Reyataz 400 mg once daily with food;
- Reyataz 300 mg and rntonavir 100 mg once daily with a meal. The dosage regimen for patients who have received prior antiretroviral therapy:
- . Reyataz 300 mg and ritonavir 100 mg once daily with food
use of the drug Reyataz without ritonavir is not recommended for patients with a poor virological outcome of earlier antiretroviral therapy. Patients with renal impairment: dose adjustment is required for patients not on dialysis. For hemodialysis patients previously untreated antnretrovirusnoy therapy, it is recommended to use the drug Reyataz 300 mg with ritonavir 100 mg. The drug should not be used in patients on dialysis previously treated with antiretroviral therapy. Patients with hepatic insufficiency: Caution should be exercised in the appointment of the drug Reyataz without ritonavpra patients with hepatic impairment or mild to moderate severity. When the average degree of liver failure, it is recommended to decrease bayer primobolan depot the dose of 300 mg once a day. Modes at any dosage; should not be used with severe hepatic insufficiency. The use of the drug in combination with ritonavir has not been studied in patients with hepatic failure patients, so this combination should not be used in these patients.
- Elderly patients: clinical trials of the drug did not include sufficient numbers of patients aged 65 years and . older based on pharmacokinetic data, the dose adjustment based on age is not required. combination therapy : didanosine: didanosine should be taken on an empty stomach, and Reyataz during meals, so combination therapy is recommended to take didanosine 2 hours after taking the drug Reyataz with food. Tenofovir: it recommends the use of a combination of Reyataz 300 mg and 100 mg ritonavnr together with tenofovir 300 mg (all drugs should be taken once daily with a meal). Application of medication Reyataz (without ritonavpra) together with tenofovir is not recommended.