II. Mechanism

  1. Nucleoside Reverse Transcriptase Inhibitor
  2. Thymidine analogue
  3. Interferes with viral reverse transcriptase
  4. Interferes with elongation of the viral DNA chain

III. 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

IV. Efficacy

  1. Delays the progression to AIDS and late HIV
  2. Increases CD4 Counts
  3. Suppresses viral replication in mild HIV (CD4 200-500)

V. Dosing

  1. Zidovudine 200 mg PO tid ($279/month) OR
  2. Zidovudine 300 mg PO bid

VI. Adverse effects: General

  1. See nRTI for adverse effects attributed to the class
  2. Short term
    1. Headache
    2. Myalgia
    3. Malaise
    4. Fatigue
    5. Insomnia
    6. Nausea or Vomiting
    7. Bloating
    8. Dyspepsia
  3. Long term
    1. Nail and Oral Mucosa Hyperpigmentation
    2. Myopathy

VII. Adverse Effects: Major toxicities

  1. Effects
    1. Anemia (Macrocytosis) (7% late, 1.8% early)
    2. Leukopenia (Neutropenia) (37% late, 4% early)
    3. Hepatitis
  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

VIII. Monitoring

  1. Advanced disease: Complete Blood Count each month
  2. Early disease: Complete Blood Count every 2-3 months

IX. Resistance

  1. Develops 6 months into therapy

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Cost: Medications

zidovudine (on 8/17/2016 at Medicaid.Gov Survey of pharmacy drug pricing)
ZIDOVUDINE 300 MG TABLET Generic $0.37 each

Ontology: Zidovudine (C0043474)

Definition (CHV) an antiviral drug used in the treatment of AIDS
Definition (CHV) an antiviral drug used in the treatment of AIDS
Definition (CHV) an antiviral drug used in the treatment of AIDS
Definition (CHV) an antiviral drug used in the treatment of AIDS
Definition (CHV) an antiviral drug used in the treatment of AIDS
Definition (CHV) an antiviral drug used in the treatment of AIDS
Definition (CHV) an antiviral drug used in the treatment of AIDS
Definition (NCI_NCI-GLOSS) A drug that inhibits the human immunodeficiency virus (HIV) that causes AIDS. It is a type of systemic antiviral.
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)
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 (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)
Concepts Nucleic Acid, Nucleoside, or Nucleotide (T114) , Pharmacologic Substance (T121)
MSH D015215
SnomedCT 27479000, 387151007
LNC LP16744-2, MTHU013874
English 3' Azido 2',3' Dideoxythymidine, 3'-Azido-2',3'-Dideoxythymidine, Antiviral AZT, Azidothymidine, AZT (Antiviral), AZT Antiviral, AZT, Antiviral, Zidovudine, zidovudine, Thymidine, 3'-azido-3'-deoxy-, 3' Azido 3' deoxythymidine, 3'-Azido-3'-deoxythymidine, 3'-azido-3'-deoxythymidine, azidodeoxythymidine, ZIDOVUDINE, azidothymidine (AZT) (medication), azidothymidine (AZT), Zidovudine [Chemical/Ingredient], azt, zdv, compound s, zidovudine (AZT), s compound, Compound S, 1-(3-Azido-2,3-dideoxy-beta-D-ribofuranosyl)-5-methylpyrimidine-2,4-(1H,3H)-dione, antiviral zidovudine, zidovudine (medication), AZT, AZT - Azidothymidine, Zidovudine product, Zidovudine (product), Zidovudine (substance), azidothymidine, ZDV
German Azidothymidin, 3-Azido-2,3-Dideoxythymidin, 3'-Azido-2',3'-Dideoxythymidin, AZT (Antiviral), AZT, antiviral, 3'-Azido-3'-Deoxythymidin, AZT (Antivirusmittel), 3-Azido-3-Deoxythymidin, Zidovudin
Swedish Zidovudin
Czech azidothymidin, zidovudin
Finnish Tsidovudiini
Russian AZIDOTIMIDIN, ZIDOVUDIN, AZT (ANTIVIRUSNYI), AZT (АНТИВИРУСНЫЙ), АЗИДОТИМИДИН, ЗИДОВУДИН
Japanese アジドチミジン, アジドデオキシチミジン, レトロビル, ジドブジン, 3'-アジド-3'-デオキシチミジン
Polish Azydotymidyna, Zidowudine, Zydowudyna, AZT przeciwwirusowa, AZT
Spanish azidotimidina, zidovudina (producto), zidovudina (sustancia), zidovudina, AZT, Azidotimidina, AZT (Antiviral), Zidovudina
French AZT, Azidothymidine, Zidovudine
Italian Zidovudina
Portuguese Azidotimidina, AZT (Antiviral), Zidovudina

Ontology: Retrovir (C0699576)

Concepts Pharmacologic Substance (T121) , Nucleic Acid, Nucleoside, or Nucleotide (T114)
MSH D015215
German Retrovir
English retrovir, Retrovir