Top Gene Interactions
- Metabolism: Hepatic. Metabolized by glucuronide conjugation to major, inactive metabolite, 3′-azido-3′-deoxy-5′- O-beta-D-glucopyranuronosylthymidine (GZDV). UGT2B7 is the primary UGT isoform that is responsible for glucuronidation. Compared to zidovudine, GZDV's area under the curve is approximately 3-fold greater. The cytochrome P450 isozymes are responsible for the reduction of the azido moiety to form 3'-amino-3'- deoxythymidine (AMT). Route of Elimination: As in adult patients, 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. Half Life: Elimination half life, HIV-infected patients, IV administration = 1.1 hours (range of 0.5 - 2.9 hours)
- Uses/Sources: Used in combination with other antiretroviral agents for the treatment of human immunovirus (HIV) infections.
- Symptoms: Symptoms of overdose include fatigue, headache, nausea, and vomiting.
- Route of Exposure: Rapid and nearly complete absorption from the gastrointestinal tract following oral administration; however, because of first-pass metabolism, systemic bioavailability of zidovudine capsules and solution is approximately 65% (range, 52 to 75%). Bioavailability in neonates up to 14 days of age is approximately 89%, and it decreases to approximately 61% and 65% in neonates over 14 days of age and children 3 months to 12 years, respectively. Administration with a high-fat meal may decrease the rate and extent of absorption.
- Carcinogenicity: 2B, possibly carcinogenic to humans. (L135)
- Toxicity: LD<sub>50</sub> is 3084 mg/kg (orally in mice).
Mechanism of Action
|Target Name||Mechanism of Action||References|
|Telomerase reverse transcriptase||