Zalcitabine


Concise Prescribing Info
Indications/Uses
HIV infection combined w/ other antiretrovirals.
Dosage/Direction for Use
Adult : PO 750 mcg 8 hrly.
Dosage Details
Oral
HIV infection
Adult: In combination with other antiretroviral agents: 750 mcg 8 hourly.
Renal Impairment
CrCl Dosage
<10 750 mcg every 24 hr
10-40 750 mcg every 12 hr
Hepatic Impairment
Use with caution.
Administration
Should be taken on an empty stomach.
Contraindications
Hypersensitivity; lactation; peripheral neuropathy or at risk of peripheral neuropathy (CD4 <50 cells/mm3; DM; weight loss).
Special Precautions
History of pancreatitis or raised serum amylase; cardiomyopathy; heart failure. Renal or hepatic impairment. Discontinue if lactic acidosis, hepatic dysfunction, peripheral neuropathy or pancreatitis develops. CBC and biochemical tests to be performed at baseline and regularly. Baseline serum amylase and triglycerides to be performed in patients with previous history of pancreatitis, increased amylase, alcohol abuse or on TPN.
Adverse Reactions
Peripheral neuropathy (numbness, sharp shooting pain), oral and esophageal ulceration; hypersensitivity reactions; cardiomyopathy and heart failure; asthenia; chest pain; fatigue; constipation; diarrhoea; mood changes; fat redistribution and fever; CNS and GI effects; haematologic effects; arthralgia; myalgia; dyspnoea; pharyngitis; alopoecia; pruritus; rashes; hearing, visual and renal disturbances; increased LFT; hyperuricaemia.
Potentially Fatal: Hepatic failure; lactic acidosis; pancreatitis; severe hepatomegaly with steatosis.
Drug Interactions
Decreased absorption with aluminium or magnesium containing antacids and metoclopramide. Increased risk of zalcitabine toxicity with cimetidine, probenecid, amphotericin B, aminoglycosides, foscarnet. Decreased activity of doxorubicin with concurrent use.
Potentially Fatal: Lamivudine antagonises effect of zalcitabine, so concurrent use is not recommended. Increased risk of peripheral neuropathy and pancreatitis with didanosine, stavudine, IV pentamidine. Avoid zalcitabine and zidovudine combination due to higher incidence of adverse reactions and more inferior virological response. Increased risk of peripheral neuropathy with chloramphenicol, dapsone, bortezomib, trimethoprim, ethionamide, metronidazole, nitrofurantoin, ribavarin, vincristine, isoniazid.
Action
Description: Zalcitabine, a synthetic nucleoside analogue of the naturally occuring nucleoside deoxycytidine, is a reverse transcriptase inhibitor with activity against retroviruses including HIV. By inhibiting activity of HIV reverse transcriptase and its incorporation into viral DNA, it terminates viral DNA growth.
Pharmacokinetics:
Absorption: Oral bioavailability: 80%. Rate of absorption decreased by food. Peak plasma concentration (fasting): 1 hr.
Distribution: Crosses blood-brain barrier. Protein binding: Negligible. Plasma elimination half life: 2 hr.
Metabolism: Metabolised intracellularly to active zalcitabine triphosphate. Does not undergo substantial metabolism by liver.
Excretion: Excreted mainly in urine.
Storage
Store at 15-30°C (59-86°F).
MIMS Class
Disclaimer: This information is independently developed by MIMS based on Zalcitabine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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