Human Immunodeficiency Virus Book

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Zidovudine

Aka: Zidovudine, Retrovir, ZDV, AZT
  1. See Also
    1. Anti-Retroviral Therapy
    2. Nucleoside Reverse Transcriptase Inhibitor
  2. Mechanism
    1. Nucleoside Reverse Transcriptase Inhibitor
    2. Thymidine analogue
    3. Interferes with viral reverse transcriptase
    4. Interferes with elongation of the viral DNA chain
  3. 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
  4. Efficacy
    1. Delays the progression to AIDS and late HIV
    2. Increases CD4 Counts
    3. Suppresses viral replication in mild HIV (CD4 200-500)
  5. Dosing
    1. Zidovudine 200 mg PO tid ($279/month) OR
    2. Zidovudine 300 mg PO bid
  6. 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
  7. 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
  8. Monitoring
    1. Advanced disease: Complete Blood Count each month
    2. Early disease: Complete Blood Count every 2-3 months
  9. Resistance
    1. Develops 6 months into therapy
  10. 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

Retrovir (C0699576)

Concepts Nucleic Acid, Nucleoside, or Nucleotide (T114) , Pharmacologic Substance (T121)
MSH D015215
German Retrovir
English retrovir, Retrovir
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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) A drug that inhibits the human immunodeficiency virus (HIV) that causes AIDS. It is a type of systemic antiviral.
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 (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 (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
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, 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
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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