Human Immunodeficiency Virus Book

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Stavudine

Aka: Stavudine, d4T, Zerit
  1. See Also
    1. Anti-Retroviral Therapy
    2. Nucleoside Reverse Transcriptase Inhibitor
  2. Mechanism
    1. Nucleoside Reverse Transcriptase Inhibitor
    2. Inhibits HIV replication
  3. Pharmacokinetics
    1. Well absorbed with 83% bioavailability
  4. Efficacy
    1. Increases CD4 Counts and suppresses HIV p24 antigenemia
      1. Doses of 0.1-2.0 mg/day
      2. Dose related response (better at higher doses)
    2. Very little resistance currently
  5. Dosing
    1. Stavudine 40 mg PO bid ($224/month)
  6. Toxicity
    1. Less Bone Marrow toxicity than Zidovudine (AZT)
  7. Adverse Effects
    1. See nRTI for adverse effects attributed to the class
    2. Headache
    3. Nausea, Vomiting
    4. Asthenia, confusion
    5. Serum Aminotransferase elevation
    6. Creatine Kinase elevation
    7. Lipodystrophy
    8. Hyperlipidemia
    9. Glucose intollerance to Diabetes Mellitus
    10. Lactic Acidosis
      1. Potentially lethal
      2. Higher risk when used in combination with Didanosine
    11. Moderate painful sensory Peripheral Neuropathy
      1. Most common serious side effect
      2. Dose related (may not recur if restart at lower dose)
    12. Pancreatitis and hyperamylasemia (rare)
  8. References
    1. (1998) Med Lett Drugs Ther 40(1041):115
    2. (2009) Treat Guidel Med Lett 7(78): 11-22
    3. Reust (2011) Am Fam Physician 83(12): 1443-51

Zerit (C0701312)

Concepts Nucleic Acid, Nucleoside, or Nucleotide (T114) , Pharmacologic Substance (T121)
MSH D018119
German Zerit
English zerit, Zerit, Bristol-Myers Brand of Stavudine, Bristol-Myers Squibb Brand of Stavudine
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Stavudine (C0164662)

Definition (CSP) nucleoside analog; used as an antiviral agent.
Definition (MSH) A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.
Definition (NCI) A synthetic nucleoside, analog of didehydro-3-deoxythymidine with potent antiretroviral activity. In vivo, stavudine is phosphorylated by cellular kinases to the active metabolite stavudine triphosphate; this metabolite inhibits the activity of HIV reverse transcriptase both by competing with the natural substrate deoxythymidine triphosphate and by incorporation into viral DNA causing a termination of DNA chain elongation (due to the lack the essential 3'-OH group). (NCI04)
Definition (NCI) A drug that belongs to the family of drugs called nucleoside analogues. It is used to treat infection caused by viruses.
Definition (PDQ) A synthetic nucleoside, analog of didehydro-3-deoxythymidine with potent antiretroviral activity. In vivo, stavudine is phosphorylated by cellular kinases to the active metabolite stavudine triphosphate; this metabolite inhibits the activity of HIV reverse transcriptase both by competing with the natural substrate deoxythymidine triphosphate and by incorporation into viral DNA causing a termination of DNA chain elongation (due to the lack the essential 3'-OH group). Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41064&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41064&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1428" NCI Thesaurus)
Concepts Nucleic Acid, Nucleoside, or Nucleotide (T114) , Pharmacologic Substance (T121)
MSH D018119
SnomedCT 108690008, 386895008
English D4T, Stavudine, 2',3'-Didehydro-2',3'-dideoxythmidine, 2',3'-Didehydro-3'-deoxythymidine, 2',3' Didehydro 3' deoxythymidine, Thymidine, 2',3'-didehydro-3'-deoxy-, 3'-Deoxy-2'-thymidinene, 1-(2,3-Dideoxy-beta-glycero-pent-2-enofuranosyl)thymine, stavudine, DIDEHYDRODEOXYTHYMIDINE 02 03 03, D A 004 T, Dideoxydidehydrothymidine, 2'3' didehydro 3' deoxythymidine, 2'3' didehydrodeoxythymidine, stavudine (medication), STAVUDINE, Stavudine [Chemical/Ingredient], d4t, Stavudine (product), Stavudine (substance), dideoxydidehydrothymidine, didehydrodeoxythymidine, d4T, Didehydrodeoxythymidine, STAVUDINE (d4T)
German 2,3-Didehydro-3-Desoxythymidin, DIDEHYDRODESOXYTHYMIDIN 02 03 03, D A 004 T, 2',3'-Didehydro-3'-Desoxythymidin, D4T, Stavudin
Swedish Stavudin
Czech stavudin
Finnish Stavudiini
Russian STAVADIN, STAVUDIN, DEGIDRODEZOKSITIMIDIN, 2',3'-DIDEGIDRO-3'-DEZOKSITIMIDIN, D4T, 2',3'-ДИДЕГИДРО-3'-ДЕЗОКСИТИМИДИН, ДЕГИДРОДЕЗОКСИТИМИДИН, СТАВАДИН, СТАВУДИН
Japanese サニルブジン, スタブジン, 2',3'-ジデヒドロ-3'-デオキシチミジン
Polish Stawudyna, D4T
Spanish estavudina (producto), estavudina (sustancia), estavudina, D4T, 2',3'-Didehidro-3'-desoxitimidina, Estavudina
French 2,3'-didehydro-3'-deoxythymidine, d4T, Stavudine
Italian Stavudina
Portuguese D4T, 2',3'-Dideidro-3'-desoxitimidina, Estavudina
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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