Zalcitabine

Zalcitabine

Zalcitabine

A synthetic dideoxynucleoside.

Mechanism of action of Zalcitabine

After intracellular phosphorylation to its active metabolite, zalcitabine preferentially inhibits the gamma form of DNA polymerase present in tumor cell mitochondria, resulting in the inhibition of tumor cell mitochondrial DNA replication and tumor cell death.

Indications and use

• Zalcitabine (brand name:HIVID) is indicated in combination with antiretroviral agents for the treatment of HIV infection.
• This indication is based on study results showing a reduction in the rate of disease progression (AIDS-defining events or death) in patients with limited prior antiretroviral therapy who were treated with the combination of HIVID and zidovudine.
• This indication is also based on a study showing a reduction in both mortality and AIDS-defining clinical events for patients who received INVIRASE® (saquinavir mesylate) in combination with HIVID compared to patients who received either HIVID or INVIRASE alone.

Formulation

• HIVID 0.375 mg tablets are oval, beige, film-coated tablets with “HIVID 0.375” imprinted on one side and “ROCHE” on the other side — bottles of 100 (NDC 0004-0220-01).

HIVID 0.750 mg tablets are oval, gray, film-coated tablets with “HIVID 0.750” imprinted on one side and “ROCHE” on the other side — bottles of 100 (NDC 0004-0221-01).

Contraindications

HIVID is contraindicated in patients with clinically significant hypersensitivity to zalcitabine or to any of the excipients contained in the tablets.

Combination therapy

HIVID is indicated in combination with antiretroviral agents for the treatment of HIV infection HIVID is the Hoffmann-La Roche brand of zalcitabine [formerly called 2',3'-dideoxycytidine (ddC)],

Side effects

Systemic side effects

• Fatigue
• Headache
• Fever

Gastrointestinal

• Abdominal Pain
• Oral Lesions/Stomatitis
• Vomiting/Nausea§
• Diarrhea/Constipation

Hepatic

• Abnormal Hepatic Function

Neurological side effects

• Convulsions
• Peripheral Neuropathy

Skin side effects

• Rash/Pruritus/Urticaria

Metabolic and Nutrition

• Pancreatitis

Psychological

• Depression

Musculoskeletal

• Painful/Swollen Joints

Before starting

• HIVID is not a cure for HIV infection
• You may continue to acquire illnesses associated with advanced HIV infection, including opportunistic infections.
• There is currently no data demonstrating that HIVID therapy can reduce the risk of transmitting HIV to others through sexual contact or blood contamination.
• Take HIVID every day as prescribed. Patients should not alter the dose or discontinue therapy without consulting with their physician. If a dose is missed, patients should take the dose as soon as possible and then return to their normal schedule. However, if a dose is skipped, the patient should not double the next dose.
• The major toxicity of HIVID is peripheral neuropathy.
• Pancreatitis and hepatic toxicity are other serious potentially life-threatening toxicities that have been reported in patients treated with HIVID. Early symptoms of these conditions and instructed to promptly report them to their physician. Since the development of peripheral neuropathy appears to be dose-related to HIVID, patients should be advised to follow their physicians’ instructions regarding the prescribed dose.
• Redistribution or accumulation of body fat may occur in patients receiving antiretroviral therapy and that the cause and long-term health effects of these conditions are not known at this time.

Lab tests before start

• Complete blood counts and clinical chemistry tests should be performed prior to initiating HIVID therapy and at appropriate intervals thereafter.
• Baseline testing of serum amylase and triglyceride levels should be performed in individuals with a prior history of
• pancreatitis, increased amylase, those on parenteral nutrition or with a history of ethanol abuse.

Storage

The tablets should be stored in tightly closed bottles at 59° to 86°F (15° to 30°C).

• Dailymed label info on Zalcitabine
• FDA Zalcitabine