Human Immunodeficiency Virus Book

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Zalcitabine

Aka: Zalcitabine, ddC, Hivid
  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 (87% oral bioavailability)
  4. Efficacy
    1. Combination treatment Zalcitabine and Zidovudine (AZT)
      1. Late HIV without prior Anti-Retroviral Therapy
      2. Large and sustained CD4 Count increase
      3. Improves survival in patients with late HIV disease
  5. Dosing
    1. Zalcitabine 0.75 mg PO tid ($207/month)
  6. Adverse Effects
    1. See nRTI for adverse effects attributed to the class
    2. Common symptoms during the first several weeks
      1. Effects
        1. Maculovesicular cutaneous eruptions
        2. Mucosal Ulcers
        3. Fevers
      2. Symptoms often resolve without stopping medication
      3. Consider Symptomatic therapy
        1. Tylenol
        2. Antihistamines
        3. NSAIDS
      4. Symptoms less frequent at a dose of 2.25 mg/day
    3. Painful Sensorimotor leg Peripheral Neuropathy (10-25%)
      1. Major dose limiting toxicity
      2. Discontinue drug at first signs of Neuropathy!
      3. Symptoms usually resolve over a few weeks
    4. Pancreatitis (<1%)
  7. References
    1. (1998) Med Lett Drugs Ther 40(1041):115 [PubMed]
    2. (2009) Treat Guidel Med Lett 7(78): 11-22 [PubMed]
    3. Reust (2011) Am Fam Physician 83(12): 1443-51 [PubMed]

Zalcitabine (C0012132)

Definition (NCI) A synthetic dideoxynucleoside. After intracellular phosphorylation to its active metabolite, zalcitabine preferentially inhibits the gamma form of DNA polymerase present in tumor cell mitochondria, resulting in the inhibition of tumor cell mitochondrial DNA replication and tumor cell death. (NCI04)
Definition (CSP) cytidine analog which inhibits reverse transcriptase and has potential efficacy against AIDS.
Definition (MSH) A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. 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 at low concentrations, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal toxic side effect is axonal degeneration resulting in peripheral neuropathy.
Definition (PDQ) A synthetic dideoxynucleoside. After intracellular phosphorylation to its active metabolite, zalcitabine preferentially inhibits the gamma form of DNA polymerase present in tumor cell mitochondria, resulting in the inhibition of tumor cell mitochondrial DNA replication and tumor cell death. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=40349&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=40349&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C430" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Nucleic Acid, Nucleoside, or Nucleotide (T114)
MSH D016047
SnomedCT 34693000, 387187000
LNC LP21316-2, MTHU013857
English 2',3' Dideoxycytidine, 2',3'-Dideoxycytidine, ddC (Antiviral), Dideoxycytidine, 2'3' dideoxycytidine, Cytidine, 2',3'-dideoxy-, zalcitabine, Zalcitabine, DDC, DIDEOXYCYTIDINE 002 003, ZALCITABINE, zalcitabine (medication), Zalcitabine [Chemical/Ingredient], ddc, Zalcitabine (product), Zalcitabine (substance), dideoxycytidine, ddC, ZALCITABINE (DIDEOXYCYTIDINE,ddC)
German ddC (antiviral), DDC, DIDESOXYCYTIDIN 002 003, 2',3'-Didesoxycytidin, Didesoxycytidin, Zalcitabin, ddC (Antivirusmittel)
Swedish Zalcitabin
Czech dideoxycytidin
Finnish Tsalsitabiini
Russian 2',3'-DIDEZOKSITSITIDIN, DIDEZOKSITSITIDIN, DDTS (PROTIVOVIRUSNYI), ZALTSITABIN, 2',3'-ДИДЕЗОКСИЦИТИДИН, ДДЦ (ПРОТИВОВИРУСНЫЙ), ДИДЕЗОКСИЦИТИДИН, ЗАЛЦИТАБИН
Japanese ザルシタビン, ジデオキシシチジン, 2',3'-ジデオキシシチジン
Polish Zalcytabina, Dideoksycytydyna
Spanish zalcitabina (producto), zalcitabina (sustancia), zalcitabina, 2',3'-Didesoxicitidina, ddC (Antiviral), Didesoxicitidina, Zalcitabina
French Didéoxycytidine
Italian Zalcitabina
Portuguese 2',3'-Didesoxicitidina, ddC (Antiviral), Didesoxicitidina, Zalcitabina
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Hivid (C0678123)

Concepts Pharmacologic Substance (T121) , Nucleic Acid, Nucleoside, or Nucleotide (T114)
MSH D016047
German HIVID Roche, Hivid
English hivid, Hivid, HIVID Roche, Hoffman-La Roche Brand of Zalcitabine, Roche Brand of Zalcitabine
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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