Document Detail


Zalcitabine. A review of its pharmacology and clinical potential in acquired immunodeficiency syndrome (AIDS).
MedLine Citation:
PMID:  1281077     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Zalcitabine is an analogue of the nucleoside deoxycytidine which, when intracellularly converted to an active triphosphate metabolite, inhibits replication of human immunodeficiency virus (HIV). Zalcitabine is thought to act in the early phase of HIV replication by inhibiting reverse transcriptase and terminating the viral DNA chain. In vitro, zalcitabine is one of the more effective nucleoside analogues currently in clinical use for HIV infection, with 0.5 mumol/L concentrations completely inhibiting HIV replication in human T lymphocyte cell lines. In clinical trials, p24 antigen levels decreased and CD4 cell counts increased in patients with acquired immunodeficiency syndrome (AIDS) receiving zalcitabine > or = 0.03 mg/kg/day as monotherapy. Dose-dependent adverse effects that include peripheral neuropathy, stomatitis and rash, restrict long term use at higher dosages, and it is unclear whether zalcitabine monotherapy is as effective as zidovudine in extending survival in HIV-infected patients. Alternating or concomitant therapy with zalcitabine and zidovudine provides effective inhibition of viral replication and disease progression (as measured by improvements in CD4 cell counts) with lower and less toxic dosage regimens. At present, therefore, zalcitabine has a place in AIDS therapy both in combination with zidovudine, and as monotherapy for patients unable to tolerate zidovudine.
Authors:
R Whittington; R N Brogden
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Publication Detail:
Type:  Clinical Trial; Journal Article; Review    
Journal Detail:
Title:  Drugs     Volume:  44     ISSN:  0012-6667     ISO Abbreviation:  Drugs     Publication Date:  1992 Oct 
Date Detail:
Created Date:  1993-01-08     Completed Date:  1993-01-08     Revised Date:  2005-11-16    
Medline Journal Info:
Nlm Unique ID:  7600076     Medline TA:  Drugs     Country:  NEW ZEALAND    
Other Details:
Languages:  eng     Pagination:  656-83     Citation Subset:  IM; X    
Affiliation:
Adis International Limited, Auckland, New Zealand.
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MeSH Terms
Descriptor/Qualifier:
Acquired Immunodeficiency Syndrome / drug therapy*
CD4-CD8 Ratio / drug effects
Drug Therapy, Combination
Drug Tolerance
HIV / drug effects,  physiology
Humans
Hydrocarbons, Chlorinated / therapeutic use*
Virus Replication / drug effects
Chemical
Reg. No./Substance:
0/Hydrocarbons, Chlorinated; 3575-15-3/1,1-di(4-chlorophenyl)-2,2-dichlorocyclopropane

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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