Trade Names:Hivid- Tablets 0.375 mg- Tablets 0.75 mg
Inhibits replication of DNA in HIV.
Oral bioavailability is about 80%. Absorption rate of a 1.5 mg oral dose was reduced with food. C max is 25.2 ng/mL. T max is 0.8 h. AUC is 72 ng•h/mL.
Vd is 0.534 L/kg. Less than 4% protein bound. Drug interaction involved in binding site is unlikely.
Major metabolite is dideoxyuridine.
Renal elimination is the primary route of elimination. The t ½ is about 2 h.
Prolonged elimination may be expected.Children
Mean bioavailability is 54%.
For the treatment of selected patients with advanced HIV infection.
PO 0.75 mg (coadministered with other antiviral agents) every 8 h (total daily dose 2.25 mg zalcitabine).
Store at room temperature in tight containers.
May increase risk of peripheral neuropathy and other zalcitabine toxicities caused by decreased clearance of zalcitabine.Chloramphenicol, cisplatin, dapsone, disulfiram, ethionamide, glutethimide, gold, hydralazine, iodoquinol, isoniazid, metronidazole, nitrofurantoin, phenytoin, ribavirin, vincristine
May increase risk of peripheral neuropathy.Drugs associated with pancreatitis (eg, pentamidine)
Fatal pancreatitis has occurred, possibly related to zalcitabine and IV pentamidine given concurrently.
None well documented.
Chest pain; cardiomyopathy; CHF.
Headache; dizziness; confusion; impaired concentration; peripheral neuropathy.
Rash; pruritus; dermatitis.
Pancreatitis; oral ulcers; nausea; dysphagia; anorexia; abdominal pain; vomiting; diarrhea; dry mouth; esophageal ulcers; dyspepsia; glossitis.
Weight decrease; weight gain; increased amylase; hyperglycemia; hyponatremia; hypoglycemia; loss of appetite.
Nasal discharge; cough; respiratory distress.
Myalgia; arthralgia; foot pain; fatigue; anaphylactoid reaction; abnormal GGT.
Hepatic failure and death, possibly related to underlying hepatitis B and zalcitabine, have been reported.Lactic acidosis and hepatomegaly
Have been reported with steatosis (including fatal cases) reported with the use of nucleoside analogues alone or in combination with other antiretrovirals.Neuropathy
Severe peripheral neuropathy, use with extreme caution in patients with preexisting neuropathy.Pancreatitis
Rarely occurs; monitor.
Category C .
Undetermined. It is recommended that HIV-positive women do not breast-feed.
Safety and efficacy in children less than 13 yr not established.
Patients with renal impairment (CrCl less than 55 mL/min) may be at greater risk of toxicity because of decreased drug clearance. Dosage reduction may be needed.
In patients with history of liver disease or alcoholism, zalcitabine may exacerbate hepatic dysfunction. Dosage reduction or interruption of therapy may be needed.
Anaphylactoid reaction has occurred. Urticaria has occurred without other signs of anaphylaxis.
Cardiomyopathy/CHF may develop. Use drug with caution in patients with history of cardiomyopathy or CHF.
Esophageal ulcers have occurred.
Patients receiving zalcitabine or any other antiretroviral therapy may continue to develop opportunistic infections and other complications of HIV infection.
Rash, fever, peripheral neuropathy.
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