← Search & browse all drugs
ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Nucleoside and nucleotide reverse transcriptase inhibitors
zalcitabine
J05AF03
Forms & Strengths
- Oral tablets: 0.375 mg
- Oral tablets: 0.75 mg
Adult Dosing
- 0.75 mg orally every 8 hours administered in combination with antiretroviral agents
- Renal impairment adjustment (CrCl 10-49 mL/min): 0.75 mg every 12 hours
- Renal impairment adjustment (CrCl <10 mL/min): 0.75 mg every 24 hours
Pediatric Dosing
- Safety and efficacy not established in pediatric patients <13 years of age
Indications
- Treatment of HIV-1 infection in combination with other antiretroviral agents (Note: discontinued by manufacturer due to toxicity profile and availability of safer alternatives)
Mechanism of Action
- Synthetic nucleoside analogue of 2'-deoxycytidine
- Inhibits HIV-1 reverse transcriptase by terminating viral DNA chain elongation after intracellular phosphorylation to zalcitabine triphosphate
Contraindications
- Hypersensitivity to zalcitabine or any component of the formulation
- Pre-existing peripheral neuropathy
- Severe hepatic impairment
Adverse Reactions
- Severe peripheral neuropathy (frequently dose-limiting)
- Pancreatitis (potentially fatal)
- Lactic acidosis and severe hepatomegaly with steatosis
- Oral ulcers and stomatitis
- Rash and pruritus
- Elevated liver enzymes
Drug Interactions
- Drugs associated with peripheral neuropathy (e.g., didanosine, stavudine, cisplatin, vincristine) increase the risk of severe neurotoxicity
- Drugs associated with pancreatitis (e.g., didanosine, pentamidine) increase the risk of pancreatic toxicity
- Probenecid and cimetidine reduce renal clearance and increase zalcitabine exposure
Curated Content: Needs Vetting Before Put to Clinical Use