Introduction: This drug was previously known as azidothymidine (AZT). It is a deoxythymidine analog that is well absorbed (63%) and distributed to most body tissues and fluids, including the cerebrospinal fluid, where drug levels are 60–65% of those in serum. Zidovudine was the first antiretroviral agent to be approved and has been well studied. Zidovudine is available in a fixed-dose combination formulation with lamivudine, either alone or in combination with abacavir. The drug has been shown to decrease the rate of clinical disease progression and prolong survival in HIV-infected individuals.
Subclass: Nucleoside Reverse Transcriptase Inhibitor (NRTI).
Pharmacokinetics: Zidovudine is eliminated primarily by renal excretion following glucuronidation in the liver.
Maternal and Child health indications: In pregnancy, a regimen of oral zidovudine beginning between 14 and 34 weeks of gestation, intravenous zidovudine during labor, and zidovudine syrup to the neonate from birth through 6 weeks of age has been shown to reduce the rate of vertical (mother-to-newborn) transmission of HIV by up to 40%.
Side effects: The most common adverse effect of zidovudine is myelosuppression, resulting in macrocytic anemia or neutropenia. Gastrointestinal intolerance, headaches, and insomnia may occur but tend to resolve during therapy. Lipoatrophy appears to be more common in patients receiving zidovudine or other thymidine analogs. Less common toxicities include thrombocytopenia, hyperpigmentation of the nails, and myopathy. High doses can cause anxiety, confusion, and tremulousness.
RELATED;
1. ABACAVIR
2. LAMIVUDINE
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