Brands, Medical Use, Clinical Data
- Anti-HIV Agents
- Nucleoside and Nucleotide Reverse Transcriptase Inhibitors
Brands / Synonyms
D4T; D4T & GM-CSF; Ddethd; Ddetyd; DHT; Estavudina [Inn-Spanish]; Sanilvudine; Stavudine [Usan:Ban:Inn]; Stavudinum [Inn-Latin]; STV; Zerit; Zerit Xr; Zerut Xr
For the treatment of human immunovirus (HIV) infections.
Stavudine is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Stavudine is phosphorylated to active metabolites that compete for incorporation into viral DNA. They inhibit the HIV reverse transcriptase enzyme competitively and act as a chain terminator of DNA synthesis. The lack of a 3'-OH group in the incorporated nucleoside analogue prevents the formation of the 5' to 3' phosphodiester linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated.
Mechanism of Action
Stavudine inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA.
Following oral administration, stavudine is rapidly absorbed (bioavailability is 68-104%).
Side effects include peripheral neuropathy tingling, burning, numbness, or pain in the hands or feet), fatal lactic acidosis has been reported in patients treated with stavudine (ZERIT) in combination with other antiretroviral agents, severe liver enlargement, inflammation (pain and swelling) of the liver, and liver failure.
Biotrnasformation / Drug Metabolism
ZERIT is contraindicated in patients with clinically significant hypersensitivity to stavudine or to
any of the components contained in the formulation.
: Zidovudine competitively inhibits the intracellular phosphorylation of stavudine. Therefore,
use of zidovudine in combination with ZERIT should be avoided.
In vitro data indicate that the phosphorylation of stavudine is also inhibited at relevant
concentrations by doxorubicin and ribavirin. The clinical significance of these in vitro interactions is
unknown; therefore, concomitant use of stavudine with either of these drugs should be undertaken with caution.