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Home / Drugs / Starting with Z / Zalcitabine

A dideoxynucleoside compound in which the 3'-hydroxyl group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of 5' to 3' phosphodiester linkages, which are needed for the elongation of DNA chains, thus resulting in the termination of viral DNA growth. 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. [PubChem]
CategoriesAnti-HIV Agents
Nucleoside and Nucleotide Reverse Transcriptase Inhibitors
Reverse Transcriptase Inhibitors
ManufacturersHoffmann la roche inc
PackagersMurfreesboro Pharmaceutical Nursing Supply
Pharmaceutical Utilization Management Program VA Inc.
Physicians Total Care Inc.


For the treatment of Human immunovirus (HIV) infections in conjunction with other antivirals.


Zalcitabine is an analog of 2'-deoxycytidine that is pharmacologically related to but structurally different from other nucleotide reverse transcriptase inhibitors (NRTIs). Zalcitabine inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA.

mechanism of action

Zalcitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Within cells, zalcitabine is converted to its active metabolite, dideoxycytidine 5'-triphosphate (ddCTP), by the sequential action of cellular enzymes. ddCTP interferes with viral RNA-directed DNA polymerase (reverse transcriptase) by competing for utilization of the natural substrate deoxycytidine 5'-triphosphate (dCTP), as well as incorpating into viral DNA. Due to it's lack of a 3'-OH group, the formation of a 5' to 3' phosphodiester linkage that is necessary for DNA chain elongation is inhibited, thus leading to the termination of viral DNA growth.


Acute overdose: Inadvertent pediatric overdoses have occurred with doses up to 1.5 mg/kg zalcitabine. Chronic overdose: in an initial dose-finding study in which zalcitabine was administered at doses 25 times (0.25 mg/kg every 8 hours) the currently recommended dose, one patient discontinued zalcitabine after 1½ weeks of treatment subsequent to the development of a rash and fever.




Bioavailability is over 80% following oral administration.

half life

2 hours

route of elimination

Renal excretion of unchanged drug appears to be the primary route of elimination, accounting for approximately 80% of an intravenous dose and 60% of an orally administered dose within 24 hours after dosing (n=19). Renal clearance exceeds glomerular filtration rate suggesting renal tubular secretion contributes to the elimination of zalcitabine by the kidneys.

drug interactions

Didanosine: Additive toxicities (peripheral neuropathy)

Lamivudine: Lamivudine may reduce the efficacy of zalcitabine. Combination therapy is not recommended.

Pentamidine: Additive risk of pancreatitis. Concomitant therapy should be avoided.

Ribavirin: Ribavirin may increase the hepatotoxicity of zalcitabine. May cause lactic acidosis. MOnitor for lactic acidosis during concomitant therapy.