Is well absorbed after oral administration, bioavailability of 60-70%. Mean values of maximum concentration at steady state and a minimum concentration at steady stateanadrollplasma when receiving 5 mg / kg every 4 zidovudine hour is 7.1 and 0.4 mol, respectively, (or 1.9 and 0.1 ug / ml). Bioequivalence has been shown that in terms of the area under the curve “concentration-time” (AUC) of zidovudine for oral solution bioequivalent zidovudine capsules. Distribution Binding to plasma proteins is relatively low, is 34-38 %. zidovudine penetrates into cerebrospinal fluid, placenta, amniotic fluid, fetal blood, breast milk and semen.
Metabolism 5′-glucuronide of anadroll is the main metabolite of end determined in plasma and urine and is approximately 50-80% of the dose that excreted by the kidneys. excretion renal clearance of zidovudine greatly exceeds creatinine clearance, indicating that the pre-emptive removal of zidovudine via tubular secretion.Special patient groups children in children over the age of 5-6 months, the pharmacokinetic parameters are similar to those in adults. zidovudine is well absorbed from the gut, bioavailability is 60-74% with a mean of 65%. Reduced clearance and longer half-life recorded in infants younger than 14 days, then the pharmacokinetic parameters are similar to those in adults. Elderly patients The pharmacokinetics of zidovudine in patients has not been studied over 65 years.
Patients with renal impairment In patients with severe renal insufficiency maximum concentration of AZT in the plasma is increased by 50% as compared with that in patients without renal dysfunction. Systemic anadroll exposure increased by 100%, the half-life was not significantly changed. If the kidney function there is a significant accumulation of the main metabolite is 5′-glucuronide of zidovudine, but signs of toxic effects is not detected. Hemodialysis and peritoneal dialysis have no effect on elimination of zidovudine, while elimination of the 5′-glucuronide of zidovudine increases. Patients with hepatic impairmentIn hepatic failure may occur due to decreased accumulation of zidovudine glucuronidation, which requires correction of the dose. Pregnancy pharmacokinetic parameters of zidovudine in pregnancy women do not change, signs of accumulation of zidovudine were observed. the concentration in the plasma of children at birth is the same as that of their mothers during childbirth.
- Treatment infection in combination therapy;
- treatment infection in pregnant women to reduce the incidence of transplacental transmission from mother to fetus.Contraindications
- Hypersensitivity to anadroll, or to any other component of the drug;
- neutropenia (neutrophil count less than 0.75 x 10 9 / L);
- decrease in hemoglobin (less than 75 g / l or 4.65 mmol / l).Carefully
- Elderly patients;
- inhibition of bone marrow hematopoiesis;
- severe hepatic impairment.