Stavudine drug data and news

Stavudine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name

Stavudine

Brand Names/Synonyms

D4T; D4T & GM-CSF; DHT; DRG-0043; Ddethd; Ddetyd; Estavudina [Inn-Spanish]; STAVUDINE; STV; Sanilvudine; Stavudine; Stavudine [Usan:Ban:Inn]; Stavudinum [Inn-Latin]; Zerit; Zerit Xr; Zerut Xr

Indication

For the treatment of human immunovirus (HIV) infections

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Description

Not Available

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.

Stavudine News
(When available)

Treatment simplification appears clinically safe in children with ... May 11, 2006
The most commonly used nucleoside combinations were 3TC (lamivudine, Epivir) with AZT (zidovudine, Retrovir) or 3TC with d4T (stavudine, Zerit). ... - Aidsmap,

HIV Pharmacology Workshop: The dangers of breaking up tablets for ... Apr 30, 2006
Triomune (a fixed dose combination of stavudine (d4T), lamuvdine (3TC) and nevirapine) is the cheapest regimen available in much of sub-Saharan Africa, and is ... - Aidsmap,

South Africa: Indian First-Line ARV Registered Apr 27, 2006
Triomune contains lamivudine, nevirapine and stavudine, which currently form part of first-line ARVs recommended by the South African Department of Health, and ... - AllAfrica.com,

Zimbabwe: Fake ARVs on sale Apr 23, 2006
The ARVs are administered in triple-therapy comprising Stavudine, Lamivudine and Nevirapine — commonly abbreviated to Stalanev. ... - African News Dimension,

Enaleni unveils 3-in-1 Aids drug Apr 24, 2006
The drug contains lamivudine, nevirapine and stavudine - three different anti-HIV/Aids medicines in one tablet, reducing the daily pill burden from six or more ... - News24,

Anti-Aids drug registered in SA Apr 24, 2006
...and the Wellcome Foundation Ltd.); nevirapine (under licence from the Boehringer Ingelheim group of companies) and stavudine, currently form part of the first ... - Sunday Times,

First-Line Antiretroviral Drug Triomune Registered in South Africa Apr 25, 2006
According to iafrica.com , Triomune is composed of lamivudine, nevirapine and stavudine, all of which are part of the first-line treatment regimen recommended ... - Kaiser network.org,

HIV Pharmacology Workshop: Are drug levels affected by racial ... Apr 30, 2006
...once a day (QD) plus two nucleoside reverse transcriptase inhibitors (NRTI) comprising 3TC (lamivudine, Epivir), ddI-EC (VidexEC)or d4T (stavudine, Zerit) to ... - Aidsmap,

Dosage Forms

CAPSULE

Drug_Category

Anti-HIV Agents; Antimetabolites; Nucleoside and Nucleotide Reverse Transcriptase Inhibitors; ATC:J05AF04

Absorption

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

Interactions

-->Interactions for Stavudine:

: 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.

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,

Organisms Affected

Human immunodeficiency virus

Chemical IUPAC Name

1-[5-(hydroxymethyl)-2,5-dihydrofuran-2-yl]-5-methyl-1H-pyrimidine-2,4-dione

Chemical Formula

C10H12N2O4

Molecular Weight

224.213 g/mol

Smiles String

CC1=CN(C(=O)NC1=O)C2C=CC(O2)CO

Melting Point

159 - 160 oC

Water Solubility

5-10 g/100 mL at 21 °C

State

Solid

LogP/Hphobicity

-0.992

Isoelectric Point

Not Available

Biotransformation

Not Available

Half Life

0.8-1.5 hours (in adults)

Protein Binding [%]

Negligible

RxList Link

RXlist

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Drug Reference

http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/zer1496.shtml
http://www.drugs.com/cons/Stavudine.html
http://www.rxlist.com/cgi/generic/stavudin.htm

Drug Type

Approved Drug

Accession No

APRD00440

CAS Registry Number

3056-17-5

KEGG Compound ID

C07312

PubChem ID

SID:9520

PharmGKB ID

PA451494

SwissProt ID

Not Available

GenBank ID

Not Available

Drug ID Number [DIN]

2216094