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Active ingredient: Stavudine - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Anti-HIV Agents
  • Antimetabolites
  • Nucleoside and Nucleotide Reverse Transcriptase Inhibitors

Dosage Forms

  • Capsule

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

Indications

For the treatment of human immunovirus (HIV) infections.

Pharmacology

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.

Absorption

Following oral administration, stavudine is rapidly absorbed (bioavailability is 68-104%).

Toxicity

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

Not Available

Contraindications

ZERIT is contraindicated in patients with clinically significant hypersensitivity to stavudine or to any of the components contained in the formulation.

Drug Interactions

: 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.

 

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