Human Immunodeficiency Virus Book

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ZidovudineAka: Retrovir, ZDV, AZT

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  1. Mechanism
    1. Nucleoside Reverse Transcriptase Inhibitor
    2. Thymidine analogue
    3. Interferes with viral reverse transcriptase
    4. Interferes with elongation of the viral DNA chain
  2. Pharmacokinetics
    1. Well absorbed from the gastrointestinal tract
    2. Glucuronidase added in the liver
    3. Excreted by the kidney
    4. Crosses the blood-brain barrier and the placenta
  3. Efficacy
    1. Delays the progression to AIDS and late HIV
    2. Increases CD4 Counts
    3. Suppresses viral replication in mild HIV (CD4 200-500)
  4. Dosing
    1. Zidovudine 200 mg PO tid ($279/month) OR
    2. Zidovudine 300 mg PO bid
  5. Adverse effects: General
    1. Short term
      1. Headache
      2. Myalgia
      3. Malaise
      4. Fatigue
      5. Insomnia
      6. Nausea or Vomiting
      7. Bloating
      8. Dyspepsia
    2. Long term
      1. Nail pigmentation
      2. Myopathy
  6. Adverse Effects: Major toxicities
    1. Effects
      1. Anemia (Macrocytosis) (7% late, 1.8% early)
      2. Leukopenia (Neutropenia) (37% late, 4% early)
    2. Management of toxicity
      1. Interrupt treatment
        1. Results in reversal of Anemia and Neutropenia
      2. Specific Therapy
        1. Anemia: Give Erythropoietin
        2. Neutropenia: Give growth factors
      3. Persistent Anemia or Neutropenia
        1. Change therapy to Didanosine (ddI)
  7. Monitoring
    1. Advanced disease: Complete Blood Count each month
    2. Early disease: Complete Blood Count every 2-3 months
  8. Resistance
    1. Develops 6 months into therapy

Zidovudine (C0043474)

Definition (MSH)A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.
Definition (CSP)synthetic thymidine analog that inhibits replication of some retroviruses, including human immunodeficiency virus; used in the management of AIDS or HIV infection.
Definition (NCI)A drug that inhibits the human immunodeficiency virus (HIV) that causes AIDS. Also called AZT. It belongs to the family of drugs called systemic antivirals.
Definition (PDQ)A synthetic dideoxynucleoside. After intracellular phosphorylation to its active metabolite, zidovudine inhibits DNA polymerase, resulting in the inhibition of DNA replication and cell death. This agent also decreases levels of available pyrimidines. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=40121&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=40121&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C947" NCI Thesaurus)
Definition (NCI)A synthetic dideoxynucleoside. After intracellular phosphorylation to its active metabolite, zidovudine inhibits DNA polymerase, resulting in the inhibition of DNA replication and cell death. This agent also decreases levels of available pyrimidines. (NCI04)
ConceptsNucleic Acid, Nucleoside, or Nucleotide (T114) , Pharmacologic Substance (T121)
MSHD015215
English3' Azido 3' deoxythymidine, 3'-Azido-3'-deoxythymidine, Antiviral AZT, azidodeoxythymidine, azidothymidine, AZT, AZT - Azidothymidine, AZT Antiviral, ZDV, Zidovudine, ZIDOVUDINE PREPARATION, Zidovudine product
Spanishazidotimidina, zidovudina
Parent ConceptsThymidine (C0040077), 2',3'-Dideoxynucleosides (C0282384), Dideoxynucleosides (C0012136), Reverse Transcriptase Inhibitors (C0282519), Antiviral Agents (C0003451), Zidovudine and derivatives (C1445650), Anti-HIV Agents, Nucleoside and Nucleotide Reverse Transcriptase Inhibitors (C1579421)
SourcesCSP, LNC, MSH, MTH, MTHSPL, NCI, NDFRT, PDQ, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


Retrovir (C0699576)

ConceptsNucleic Acid, Nucleoside, or Nucleotide (T114) , Pharmacologic Substance (T121)
MSHD015215
EnglishRetrovir
SourcesCSP, MSH, NCI, PDQ, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)



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