Adult: In combination with other antiretroviral agents: 0.75 mg 8 hourly. Dose reduction, dosing interruption, or discontinuation may be required according to individual safety and tolerability (refer to detailed product guideline).
Renal Impairment
CrCl (mL/min)
Dosage
<10
0.75 mg 24 hourly.
10-40
0.75 mg 12 hourly.
Administration
Should be taken on an empty stomach.
Contraindications
Hypersensitivity. Moderate or severe peripheral neuropathy. Lactation.
Special Precautions
Patient with mild neuropathy or at risk of developing peripheral neuropathy (e.g. CD4 >50 cells/mm3, diabetes, weight loss); history of pancreatitis or known risk factors for the development of pancreatitis; history of CHF or cardiomyopathy, and alcohol abuse. Renal and hepatic impairment. Pregnancy.
Adverse Reactions
Significant: Peripheral neuropathy (sensorimotor neuropathy), severe oral ulcers, oesophageal ulcers, cardiomyopathy, CHF, hypersensitivity reaction (including anaphylactic reaction or urticaria without other signs of anaphylaxis). Blood and lymphatic system disorders: Anaemia, leucopenia, eosinophilia, neutropenia, thrombocytopenia. Gastrointestinal disorders: Abdominal pain. General disorders and administration site conditions: Fatigue, fever. Hepatobiliary disorders: Abnormal hepatic function. Nervous system disorders: Headache, convulsion. Skin and subcutaneous tissue disorders: Rash, pruritus. Potentially Fatal: Pancreatitis; lactic acidosis and severe hepatomegaly with steatosis. Rarely, hepatic failure.
Monitoring Parameters
Obtain CBC and clinical chemistry test at baseline and as necessary thereafter. Monitor for signs and symptoms of peripheral neuropathy.
Drug Interactions
Increased plasma concentrations with cimetidine, probenecid, trimethoprim. Reduced absorption with Al- or Mg- containing antacids. Increased risk of peripheral neuropathy with other nucleoside reverse transcriptase inhibitors, chloramphenicol, dapsone, ethionamide, isoniazid, metronidazole, nitrofurantoin, ribavirin, vincristine, didanosine. May reduce clearance with amphotericin B, aminoglycosides, foscarnet Na. Potentially Fatal: Increased risk of pancreatitis with IV pentamidine. Concomitant use with lamivudine may antagonise the therapeutic effect of zalcitabine.
Action
Description: Zalcitabine is a synthetic nucleoside analogue of the naturally occurring nucleoside deoxycytidine which is converted into the active metabolite, dideoxycytidine 5'-triphosphate (ddCTP). The active metabolite competes for the ulitisation of the natural substrate (deoxycytidine 5'-triphosphate [dCTP]) and incorporates into viral DNA thus inhibiting the activity of the HIV-reverse transcriptase which results in the termination of viral DNA growth. Pharmacokinetics: Absorption: Absorbed from the gastrointestinal tract. Decreased rate of absorption with food. Bioavailability: >80%. Time to peak plasma concentration: Within 1 hour (fasting state). Distribution: Crosses the blood-brain barrier. Metabolism: Metabolised intracellularly to the active metabolite ddCTP. Excretion: Mainly via urine. Elimination half-life: Approx 2 hours.
Chemical Structure
Zalcitabine Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 24066, Zalcitabine. https://pubchem.ncbi.nlm.nih.gov/compound/Zalcitabine. Accessed Oct. 26, 2022.
J05AF03 - zalcitabine ; Belongs to the class of nucleoside and nucleotide reverse transcriptase inhibitors. Used in the systemic treatment of viral infections.
References
Buckingham R (ed). Zalcitabine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/10/2022.Hivid Tablets (Roche Laboratories Inc.). U.S. FDA. https://www.fda.gov. Accessed 05/10/2022.
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