Zidovudine
Also known as: AZT
Zidovudine is a synthetic dideoxynucleoside antiviral agent. It was first synthesized as an antineoplastic drug in the 1960s. In 1985, it was found to inhibit the in vitro infectivity of human immunodeficiency virus type-1 (HIV-1), although it was known to possess antiviral activity as early as 1974. Zidovudine is active against other retroviruses and some bacteria, but its sole indication is for the treatment and prevention of HIV infection in adults and children. On a weight basis, Zidovudine is more active than didanosine, but less active than zalcitabine, against HIV-1. It was approved by the FDA in March 1987.
Primary Characteristics
Zidovudine is also known as AZT.
It is of Synthetic origin and belongs to Thymidine.
It belongs to Reverse transcriptase inhibitor pharmacological group on the basis of mechanism of action. It is also classified under Antiviral Agents .
Molecular Weight: 267.2 · pKa: 9.68 · Solubility in Water: 1 in 40 · Solubility in Alcohol: 1 in 14 · Non-proprietary name: Zidovudine.
Pharmacokinetics
Absorption: Zidovudine has an oral bioavailability is 95% (±5%), pre-systemic (first-pass) metabolism accounts for 32.5% (±7.5%).
Distribution: Zidovudine has a volume of distribution is 1.6 l/kg. plasma protein binding is 34 - 38 %.
Elimination: it is metabolised via Hepatic, plasma half-life is 0.78 - 1.93 hr, renal excretion is 18 %.
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Indications
Zidovudine is primarily indicated in conditions like AIDS, HIV infection.
Contraindications
Zidovudine is contraindicated in conditions like Anaemia, Neutropenia.
Dosage
Zidovudine's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 2.857 mg/kg | 2.857 mg/kg | Every 8h | PO | Initial |
| 3.929 mg/kg | 3.929 mg/kg | Every 12h | PO | Maintenance |
| Paediatric Dosage (20kg) | ||||
| 7.75 mg/kg | 7.75 mg/kg | Every 6h | Oral | - |
| Neonatal Dosage (3kg) | ||||
| 8.25 mg/kg | 8.25 mg/kg | Every 6h | Oral | |
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Zidovudine in overdosage may give rise to further complications which include Encephalitis , Polymyositis .
Zidovudine produces potentially life-threatening effects which include Anemia, Neutropenia , Leucopenia . Careful monitoring is needed with proper medical management.
Zidovudine is known to cause more or less tolerable side effects which are usually transient. These include Headache, Insomnia, Nausea.
Warnings / Precautions
Available Brands
Storage Conditions
Drug Classification
- 1.6.5.2 — Antiretroviral drugs