Intravenous Prophylaxis of maternal-fetal HIV transmission during labour and delivery
Adult: 2 mg/kg by infusion over 1 hr, given at the start of labour, then 1 mg/kg/hr by continuous infusion until umbilical cord is clamped. For caesarean section, start infusion 4 hr before the operation.
Intravenous HIV infection
Adult: 1 mg/kg or 2 mg/kg 4 hrly, by infusion over 1 hr. Child: 80-160 mg/m2 6 hrly by infusion.
Intravenous Prophylaxis of HIV infection in neonates
Child: 1.5 mg/kg 6 hrly by infusion over 30 min, starting w/in 12 hr after birth and continuing for 6 wk.
Oral Prophylaxis of HIV infection in neonates
Child: 2 mg/kg 6 hrly, starting w/in 12 hr after birth and continuing for 6 wk.
Oral HIV infection
Adult: 250 mg or 300 mg bid, in combination w/ other antiretroviral agents. Child: As soln: 4 to <9 kg: 12 mg/kg bid; 9 to <30 kg: 9 mg/kg bid; ≥30 kg: 250 mg or 300 mg bid. As cap/tab: 8-13 kg: 100 mg bid; 14-21 kg: 100 mg in the morning, 200 mg in the evening; 22-30 kg: 200 mg bid; ≥30 kg: 250 mg or 300 mg bid. Alternatively (based on BSA), 480 mg/m2 daily in 2-3 divided doses. Doses are given in combination w/ other antiretroviral agents.
Oral Prophylaxis of maternal-fetal HIV transmission
Adult: 100 mg 5 times daily, starting on the 14th wk of gestation until the start of labour.
ESRD maintained on haemodialysis or peritoneal dialysis: 100 mg 6-8 hrly.
100 mg 6-8 hrly.
ESRD maintained on haemodialysis or peritoneal dialysis: 1 mg/kg 6-8 hrly.
1 mg/kg 6-8 hrly.
Dose reduction may be needed.
May be taken with or without food.
W/draw the required dose from the vial and dilute in dextrose 5% soln to provide a final concentration of 2 mg/mL or 4 mg/mL.
Blood products and protein soln.
Hypersensitivity; abnormally low neutrophil counts (<0.75 x 109/L) or Hb levels (<7.5 g/dL or 4.65 mmol/L); newborn infants w/ hyperbilirubinaemia requiring treatment other than phototherapy, or w/ increased transaminase levels >5 times the ULN. Lactation. Concomitant use w/ interferon alfa (w/ or w/o ribavirin) in HIV and hepatitis B or C virus co-infected patients.
Severe renal and hepatic impairment. Childn. Pregnancy.
Monitor viral load, CD4 count; CBC w/ differential, LFT, lipid, glucose. Observe for appearance of opportunistic infection.
Symptoms: Vomiting, CNS effects (e.g. fatigue, dizziness, drowsiness, lethargy, confusion), haematologic effects (e.g. anaemia, decreased Hb). Bone marrow hypoplasia, mild ataxia, tonic-clonic seizure and increased serum concentration of AST and ALT may also occur. Management: Supportive and symptomatic treatment. Induce emesis and admin activated charcoal to prevent further absorption of unrecovered drug.
Decreased plasma concentration w/ rifampicin resulting in partial or total loss of efficacy of zidovudine. Increased risk of anaemia w/ ribavirin in patients co-infected w/ HCV. Antagonistic effect w/ stavudine or doxorubicn. Increased plasma level w/ probenecid, atovaquone, valproic acid, fluconazole, or methadone. May alter phenytoin blood levels. Increased adverse effect w/ potentially nephrotoxic or myelosuppressive drugs (e.g. systemic pentamidine, dapsone, pyrimethamine, co-trimoxazole, amphotericin, flucytosine, ganciclovir, interferon, vincristine, vinblastine, doxorubicin). Reduced absorption w/ clarithromycin. Potentially Fatal: Risk of hepatic decompensation when used concomitantly w/ interferon alfa (w/ or w/o ribavirin) in HIV and HBV/HCV co-infected patients.
Absorption is delayed when given w/ food.
Description: Zidovudine is converted intracellularly to zidovudine triphosphate, which inhibits replication of retroviruses, including HIV, by interfering w/ viral RNA-directed DNA polymerase (reverse transcriptase). Pharmacokinetics: Absorption: Rapidly absorbed from the GI tract. Delayed absorption w/ food. Bioavailability: Approx 60-70%. Time to peak plasma concentration: Approx 1 hr. Distribution: Crosses the blood-brain barrier and placenta, enters breast milk and detected in semen. Volume of distribution: 1-2.2 L/kg. Plasma protein binding: 34-38%. Metabolism: Metabolised intracellularly to the active triphosphate form and undergoes hepatic metabolism, mainly to the inactive glucuronide. Excretion: Via urine, as unchanged drug and metabolite. Plasma half-life: Approx 1 hr.
Store between 15-25°C. Protect from light, heat and moisture. Diluted IV soln: Store at 25°C (stable for 8 hr) or at between 2-8°C (stable for 24 hr).
J05AF01 - zidovudine ; Belongs to the class of nucleoside and nucleotide reverse transcriptase inhibitors. Used in the systemic treatment of viral infections.
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