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Nucleoside Reverse Transcriptase Inhibitors:
Zalcitabine
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back to topIntroduction

The information represented on this drug does not necessarily correspond with the information that can be found in the Belgian scientific leaflet.
In 1992, zalcitabine was approved by the FDA for use in HIV-infected patients. This pyrimidine analogue has good in vitro activity, but its in vivo activity is less potent. Like the others NRTIs, zalcitabine must be triphosphorylated to be effective. Zalcitabine should never be given as monotherapy. Although it can be used in individuals who have been receiving  antiretroviral therapy in combination with other drugs, it is most effective when combined with zidovudin.(100,106)

Abbreviation(s): 
Generic name:
Brand name:		 ddC
zalcitabine
Hivid®
USA (FDA)
Adult approval date:
Pediatric approval date:		 June 19, 1992
No pediatric labeling
 		 Roche
Pharmaceutical co.: Hoffmann- La Roche Belgium:
Reimbursable since May 1995
  Active
Ingredient		 Dosage form;
Route		  Strength
Tablets 0,750 mg Zalcitabine Tablet; Oral  0.375MG 
Zalcitabine Tablet; Oral  0.75MG 

back to topPharmacokinetics

It is well absorbed, has a plasma half-life of 1.2 hours, and is excreted largely unchanged by the kidneys. (106)

back to topDosing

The standard dosage of zalcitabine is 0.75 mg every 8 hours. (100,106)

back to topSide effects

The major toxicities associated with zalcitabine treatment are pancreatitis and peripheral neuropathy. The incidence of both side effects appeared to be similar with that of didanosine.(126) Pancreatitis is relatively uncommon, but cases, including fatal ones, have been reported with the use of zalcitabine. The symptoms of patients with zalcitabine-associated peripheral neuropathy typically resolve with prompt discontinuation of the drug, although progressive neuropathic symptoms are possible, despite drug discontinuation. (106)
Rare cases of lactic acidosis in patients receiving zalcitabine have also been reported and patients with hepatic insufficiency appear to be at increased risk. Stomatitis occur commonly in patients receiving zalcitabine. Other potential adverse effects include: esophageal ulceration, congestive cardiomyopathy, arthralgias and dermatologic eruptions. Mild nausea, vomiting, diarrhea, fatigue, rash and elevations in amylase levels have also been reported in a small percentage of patients receiving zalcitabine. A single case of anaphylaxis and several cases of urticaria have also been reported. (106,114)

back to topDrug interactions

Zalcitabine can decrease the AUC of isoniazid by 40%. The mechanism for this interaction is a chemical binding of the excipient of zalcitabine to isoniazid. Dosing of isoniazid and zalcitabine should be separated by at least 1 hour. Zalcitabine can increase the maximum concentration and time to reach maximum concentration of dapsone. This interaction, however, is probably not clinically significant.(114)
 

Interactions with other antiretroviral agents 
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