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Abacavir/lamivudine Generic Name & Formulations
Legal Class
Rx
General Description
Abacavir (as sulfate) 600mg, lamivudine 300mg; tabs.
Pharmacological Class
Nucleoside analogues (reverse transcriptase inhibitors).
How Supplied
Contact supplier
Manufacturer
Mechanism of Action
Abacavir is converted by cellular enzymes to the active metabolite, carbovir triphosphate (CBV-TP), an analogue of deoxyguanosine-5′-triphosphate (dGTP). CBV-TP inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA. Lamivudine is a synthetic nucleoside analogue. Intracellularly lamivudine is phosphorylated to its active 5′-triphosphate metabolite, lamivudine triphosphate (3TC-TP). The principal mode of action of 3TC-TP is inhibition of RT via DNA chain termination after incorporation of the nucleotide analogue.
Abacavir/lamivudine Indications
Indications
HIV-1 infection, in combination with other antiretroviral agents.
Abacavir/lamivudine Dosage and Administration
Adults and Children
<25kg: use individual components. ≥25kg: 1 tab daily. Mild hepatic or renal impairment (CrCl <30mL/min): not recommended; use individual components.
Abacavir/lamivudine Contraindications
Contraindications
Presence of HLA-B*5701 allele. Prior hypersensitivity reaction to any of the components (see full labeling). Moderate or severe hepatic impairment.
Abacavir/lamivudine Boxed Warnings
Boxed Warning
Hypersensitivity reactions. Exacerbations of hepatitis B.
Abacavir/lamivudine Warnings/Precautions
Warnings/Precautions
Screen for presence of HLA-B*5701 allele prior to starting therapy or reinitiation; if (+), abacavir is contraindicated. Discontinue immediately if hypersensitivity is suspected, regardless of HLA-B*5701 status and even when other diagnoses are possible. If hypersensitivity cannot be ruled out, do not restart. If stopped for reasons other than hypersensitivity, restart only if medical care can be readily accessed. Not for treating chronic HBV infection; closely monitor patients co-infected with HBV and HIV for several months after stopping treatment (discontinuing therapy may exacerbate HBV infection); if appropriate, initiate anti-hepatitis B therapy may be warranted. Suspend if lactic acidosis or pronounced hepatotoxicity (eg, hepatomegaly, steatosis) occurs. Possible risk of MI; minimize risk factors for coronary heart disease (eg, hypertension, hyperlipidemia, diabetes, smoking). Renal impairment (CrCl 30–49mL/min): monitor for hematologic toxicities; if new or worsening neutropenia or anemia develop, adjust lamivudine dose. Women. Obesity. Elderly. Pregnancy. Nursing mothers: not recommended.
Abacavir/lamivudine Pharmacokinetics
Absorption
Oral bioavailability: 86 ± 25% (abacavir); 86 ± 16% (lamivudine).
Distribution
Apparent volume of distribution: 0.86 ± 0.15 L/kg (abacavir); 1.3 ± 0.4 L/kg (lamivudine).
Elimination
Half-life: 1.45 ± 0.32 hours (abacavir); 13–19 hours (lamivudine). Systemic clearance: 0.80 ± 0.24 L/h/kg (abacavir); 0.33 ± 0.06 L/h/kg (lamivudine).
Abacavir/lamivudine Interactions
Interactions
Avoid concomitant sorbitol-containing products. May antagonize methadone. Potentiates riociguat; may need to reduce riociguat dose. Monitor for treatment-associated toxicities (esp. hepatic decompensation) with interferon-alpha with or without ribavirin.
Abacavir/lamivudine Adverse Reactions
Adverse Reactions
Hypersensitivity reactions (may be fatal), insomnia, depression, headache/migraine, fatigue/malaise, dizziness, nausea, diarrhea; rash (may be severe, eg, Stevens-Johnson), pyrexia, immune reconstitution syndrome, lactic acidosis, severe hepatomegaly with steatosis.
Abacavir/lamivudine Clinical Trials
See Literature
Abacavir/lamivudine Note
Notes
Formerly known under the brand name Epzicom. To register pregnant patients exposed to abacavir/lamivudine, call (800) 258-4263.
Abacavir/lamivudine Patient Counseling
See Literature
