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| Stavudine, d4T (Zerit®) |
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Class:
Nucleoside Reverse Transcriptase Inhibitor
Molecular Weight:
224.2
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Structure
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Summary of Key Pharmacokinetic Parameters
Plasma half life: 1.3-1.4 hours [1]
Cmax : 536±146 ng/ml (40mg bd dosing) [4]
Cmin: 9±8 ng/ml (40mg bd dosing) [4]
AUC: (0-12hr) 1284±227 ng/ml.hr
Bioavailability: Approx 86% [1]
Protein Binding: <5% [2]
Volume of Distribution: 0.66L/kg [1]
CSF:Plasma ratio: 0.39±0.06
Semen:Plasma ratio: >1 [3]
Renal Clearance: Single dose:34±5% , Multiple dose: 40±12%
Renal Impairment: Clearance of stavudine decreases as creatinine clearance decreases; the manufacturers recommend that dosage is adjusted in patients with reduced renal function
Hepatic Impairment: stavudine pharmacokinetics in patients with hepatic impairment were similar to those in patients with normal hepatic function
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Metabolism and Distribution
Metabolised by: Not elucidated in humans
Inducer of: N/A
Inhibitor of: Does NOT inhibit the major cytochrome P450 isoforms CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4
Transported by: Unknown
References
Unless otherwise specified: Zerit® Summary of Product Characteristics, Bristol-Myers Squibb Pharmaceuticals Ltd, updated 29/08/08, accessed 17/09/08
[1] S Khoo, D Back & C Merry. Practical Guidelines in Antiviral Therapy. 2002; Chapter 2: Pharmacology.
[2] B Clotet et al. Guide to Management of HIV resistance and pharmacokinetics of drug therapy. 2000; 94-96.
Antinori A et al. Antiretroviral distribution in cerebrospinal fluid and viral resistance in HIV-infected patients. 9th Conference on Retroviruses and Opportunistic Infections, Seattle, February 2002. Abs 438-W.
[3] Reijers M et al. The concentrations of D4T, 3TC, nelfinavir and saquinavir in plasma, cerebrospinal fluid and semen. 7th Conference on Retroviruses and Opportunistic Infections, San Francisco, February 2000. Abs 316.
[4] Zerit® US Prescribing Information, Bristol-Myers Squibb Pharmaceuticals Ltd, revised July 2008, accessed 17/09/08
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Last reviewed: 6 October 2009
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