Abacavir Sulfate
Pronouncation: (ab-ah-KAV-ear)Class: Antiretroviral, Nucleoside reverse transcriptase inhibitor
Trade Names:
Ziagen
- Tablets 300 mg
- Oral solution 20 mg/mL
Pharmacology
 | |||||||||
Feedback for Abacavir Sulfate
Compare with other drugs.
| |||||||||
Converted by cellular enzymes to carbovir triphosphate, which inhibits HIV-1 reverse transcriptase and interferes with DNA synthesis.
Pharmacokinetics
Absorption
Rapidly and extensively absorbed. Bioavailability is 83% (tablets). C max is approximately 3 mcg/mL and AUC 0-12 is approximately 6.02 mcg•h/mL.
Distribution
Vd after IV administration is approximately 0.86 L/kg. Plasma protein binding is approximately 50%.
Metabolism
Metabolized to inactivate metabolites by alcohol dehydrogenase and glucuronyl transferase.
Elimination
Urine is 1.2% as abacavir, 81% as inactive metabolites; feces is 16% of dose. The t ½ is approximately 1.54 h and Cl is approximately 0.8 L/h/kg (after IV administration).
Special Populations
Hepatic Function ImpairmentMild hepatic function impairment (Child-Pugh score 5 to 6) AUC increased 89% and t ½ increased 58%.
Indications and Usage
Treatment of HIV-1 in combination with other antiretroviral agents.
Contraindications
Moderate or severe hepatic function impairment; hypersensitivity to any component of the product.
Dosage and Administration
AdultsPO 300 mg twice daily in combination with other antiretroviral agents.
Adolescents and Children 3 mo to up to 16 yr of agePO 8 mg/kg twice daily (max, 300 mg twice daily) in combination with other antiretroviral agents.
Hepatic Function ImpairmentPO 200 mg twice daily in patients with mild hepatic function impairment (Child-Pugh score 5 to 6).
Storage/Stability
Store tablets and solution at controlled room temperature (68° to 77°F). Solution may be refrigerated but do not freeze.
Drug Interactions
EthanolIncreases exposure to abacavir by decreasing the elimination and prolonging the t ½ .
MethadonePlasma levels of methadone may be decreased in some patients, reducing the therapeutic effect.
Laboratory Test Interactions
None well documented.
Adverse Reactions
CNS
Insomnia; sleep disorders; headache.
Dermatologic
Skin rashes; Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme (postmarketing).
GI
Nausea; vomiting; diarrhea; loss of appetite; anorexia; pancreatitis.
Metabolic
Elevated blood glucose; elevated triglycerides; redistribution/accumulation of body fat (postmarketing).
Miscellaneous
Hypersensitivity reactions (eg, fever, rash, fatigue, GI symptoms, malaise, lethargy, myalgia, arthralgia, edema, shortness of breath, paresthesia, hypotension, death); fever.
Precautions
WarningsFatal hypersensitivity reactionsAssociated with therapy. Drug should not be restarted after suspected reaction. Lactic acidosis and hepatomegaly reported with steatosis (including fatal cases) reported with the use of nucleoside analogues alone or in combination with other antiretrovirals. |
Pregnancy
Category C .
Lactation
Undetermined; however, HIV-infected mothers should not breast-feed infants.
Children
Safety and efficacy not established in children under 3 mo.
Elderly
Select dose with caution, reflecting greater frequency of decreased hepatic, renal, or cardiac function and comorbidity.
Fat redistribution
Redistribution/accumulation of body fat have been observed (eg, buffalo hump, peripheral/facial wasting, central obesity).
Patient Information
- Advise patient to review Medication Guide before starting therapy and with each refill of the medication.
- Advise patient to review, and carry with them at all times, the Warning Card summarizing the symptoms of abacavir hypersensitivity reaction.
- Instruct patient to take exactly as prescribed and not to change the dose or discontinue therapy unless advised by health care provider.
- Advise patient to take drug twice daily without regard to meals but to take with food if GI upset occurs.
- Advise patient, family, or caregiver to measure prescribed dose of solution using dosing spoon or dosing syringe.
- Instruct patient that if a dose is missed, to take as soon as remembered, take the next dose at the usual scheduled time.
- Instruct patient to continue to take other HIV medications as prescribed by health care provider.
- Instruct patient to discontinue use and notify health care provider immediately if skin rash or 1 or more symptoms from at least 2 of the following groups are noted: fever; nausea, vomiting, diarrhea, abdominal pain; fatigue, muscle aches, malaise; sore throat, shortness of breath, cough.
- Instruct patient to report the following symptoms immediately to health care provider: profound weakness or tiredness; feeling cold, dizzy, or lightheaded; slow or irregular heartbeat; pain or tingling in the hands or feet; muscle or joint pain.
- Inform patient that drug does not completely eliminate HIV virus and, therefore, does not reduce risk of transmitting HIV. Appropriate precautions must still be followed.
- Advise patient that drug is not a cure for HIV infection. Illnesses associated with HIV infection, including opportunistic infections, may continue to be acquired, and patients should remain under a physician's care.
- Inform patient that redistribution or accumulation of body fat may occur.
- Caution breast-feeding mother to discontinue nursing while receiving medication because of potential for adverse reactions from the medication in breast-feeding infants as well as transmission of HIV virus.
 |
Link to Page |  |
Print Page |  |
Email Page |  | Add to List |
HIV Infection, Nonoccupational Exposure
