Zidovudine (Azt)

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ZIDOVUDINE

zidovudine (Azt) 1

1.       TYPE OF DRUG- ZIDOVUDINE
Zidovudine (ZDV), also known as azidothymidine (AZT), is an antiretroviral medication

 

2.       INDICATIONS (USE)- ZIDOVUDINE
Used in combination with other antiretroviral agents for the treatment of human immunovirus (HIV) infections.

 

3.       MECHANISM OF ACTION (MOA)- ZIDOVUDINE
Zidovudine is phosphorylated to zidovudine-triphosphate, which competes with endogenous nucleotides for incorporation into the viral DNA and once incorporated causes chain termination due to the lack of a 3’ OH group.

 

4.       ROUTES OF ADMINISTRATION- ZIDOVUDINE
tablets, capsules, syrup, injection

 

5.       ONSET OF EFFECT OR ACTION- ZIDOVUDINE
12 to 16 weeks.

 

6. DOSAGE (DOSING INFORMATION)- ZIDOVUDINE
Adults : Initially 200mg 6 times daily.Therefore 500-1500mg daily in 4-5 div. doses .Children > 3 months : 12-22mg/kg/day div.6 hourly .

 

7.       HALF LIFE (DURATION OF ACTION)- ZIDOVUDINE
1.1   hour.

1.2

8.       ADVERSE EFFECTS OR SIDE EFFECTS – ZIDOVUDINE
Nausea, severe headache, myalgia, insomnia, vomiting, anorexia, diarrhoea, asthenia, dizziness, taste perversion, convulsions, myopathy, nail, skin and oral mucosa pigmentation, raised LFT, pancreatitis, fat redistribution.

 

9.       CONTRAINDICATIONS – ZIDOVUDINE
Dose selection for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

 

10.   DRUG INTERACTIONS – ZIDOVUDINE
Decreased zidovudine concentration with tipranavir. Increased risk of peripheral neuropathy with bortezomib. Increased haematological toxicity with IV pentamidine, lamivudine, dapsone, vancomycin flucytosine, amphotericin, ganciclovir, interferon alfa, cyclophosphamide and other bone marrow suppressive or cytotoxic agents Increased risk of zidovudine toxicity with atovaquone, chloramphenicol, fluconazole, valproate. Decreased absorption with clarithromycin, minimise interactions by admin at least 2 hours apart. Increased zidovudine concentration and increased potential for hypersensitivity reactions with probenecid. Increased zidovudine clearance and haematological toxicity with rifampicin. Increased bioavailability of zidovudine with nimodipine. Increased incidences of headache with benzodiazepines. Possible increase in zidovudine concentration with methadone.

 

11. EXCRETION- ZIDOVUDINE
The major route of elimination was by metabolism to GZDV. After intravenous dosing, about 29% of the dose was excreted in the urine unchanged and about 45% of the dose was excreted as GZDV.

 

zidovudine (Azt) 2

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