Apo-Abacavir
Apo-Abacavir Uses, Dosage, Side Effects, Food Interaction and all others data.
Apo-Abacavir (ABC) is a powerful nucleoside analog reverse transcriptase inhibitor (NRTI) used to treat HIV and AIDS. Chemically, it is a synthetic carbocyclic nucleoside and is the enantiomer with 1S, 4R absolute configuration on the cyclopentene ring. In vivo, abacavir sulfate dissociates to its free base, abacavir.
Apo-Abacavir is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Apo-Abacavir is phosphorylated to active metabolites that compete for incorporation into viral DNA. They inhibit the HIV reverse transcriptase enzyme competitively and act as a chain terminator of DNA synthesis. The concentration of drug necessary to effect viral replication by 50 percent (EC50) ranged from 3.7 to 5.8 μM (1 μM = 0.28 mcg/mL) and 0.07 to 1.0 μM against HIV-1IIIB and HIV-1BaL, respectively, and was 0.26 ± 0.18 μM against 8 clinical isolates. Apo-Abacavir had synergistic activity in cell culture in combination with the nucleoside reverse transcriptase inhibitor (NRTI) zidovudine, the non-nucleoside reverse transcriptase inhibitor (NNRTI) nevirapine, and the protease inhibitor (PI) amprenavir; and additive activity in combination with the NRTIs didanosine, emtricitabine, lamivudine, stavudine, tenofovir, and zalcitabine.
| Trade Name | Apo-Abacavir |
| Availability | Prescription only |
| Generic | Abacavir |
| Abacavir Other Names | Abacavir, ABC |
| Related Drugs | Biktarvy, Truvada, tenofovir, ritonavir, zidovudine, emtricitabine, lamivudine, Complera, Atripla, Stribild |
| Type | |
| Formula | C14H18N6O |
| Weight | Average: 286.3323 Monoisotopic: 286.154209228 |
| Protein binding | Moderate (approximately 50%). Binding of abacavir to plasma protein was independent of concentration. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | Canada, United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Apo-Abacavir is an antiviral nucleoside reverse transcriptase inhibitor used in combination with other antiretrovirals for the treatment of HIV.
For the treatment of HIV-1 infection, in combination with other antiretroviral agents.
Apo-Abacavir is also used to associated treatment for these conditions: Human Immunodeficiency Virus Type 1 (HIV-1) Infection
How Apo-Abacavir works
Apo-Abacavir is a carbocyclic synthetic nucleoside analogue and an antiviral agent. Intracellularly, abacavir is converted by cellular enzymes to the active metabolite carbovir triphosphate, an analogue of deoxyguanosine-5'-triphosphate (dGTP). Carbovir triphosphate inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA. Viral DNA growth is terminated because the incorporated nucleotide lacks a 3'-OH group, which is needed to form the 5′ to 3′ phosphodiester linkage essential for DNA chain elongation.
Toxicity
Some myocardial degeneration has been noticed in rats and mice. The most commonly reported adverse reactions of at least moderate intensity (incidence ≥10%) in adult HIV-1 clinical trials were nausea, headache, malaise and fatigue, nausea and vomiting, and dreams/sleep disorders. Serious hypersensitivity reactions have been associated with abacavir which has been strongly linked to the presence of the HLA-B*57:01 allele. This reaction manifests itself in patients within the first 6 weeks of treatment. Patients should be tested for the presence of this allele as recommended by the U.S Food and Drug Administration (FDA).
Food Interaction
- Avoid alcohol. Alcohol increases the systemic exposure to the drug.
- Take with or without food. The absorption is unaffected by food.
Apo-Abacavir Alcohol interaction
[Minor] Consumption of ethanol during treatment with abacavir results in a decrease in elimination of abacavir due to the inhibition of alcohol dehydrogenase.
Coadministration of alcohol 0.7 g/kg (equivalent to 5 drinks) and abacavir resulted in a 41% increase in the area under the time concentration curve and a 26% increase in elimination half life.
The clinical significance of this interaction is unknown.
Apo-Abacavir Cholesterol interaction
[Moderate] Some clinical trials have reported increased risk of myocardial infarction in patients treated with abacavir.
Although some of the findings are inconclusive, as a precaution, the underlying risk of coronary heart disease should be assessed before therapy, and action should be taken to minimize all modifiable risk factors such as hypertension, hyperlipidemia, diabetes mellitus, smoking, etc.
Apo-Abacavir Hypertension interaction
[Moderate] Some clinical trials have reported increased risk of myocardial infarction in patients treated with abacavir.
Although some of the findings are inconclusive, as a precaution, the underlying risk of coronary heart disease should be assessed before therapy, and action should be taken to minimize all modifiable risk factors such as hypertension, hyperlipidemia, diabetes mellitus, smoking, etc.
Apo-Abacavir Drug Interaction
Unknown: aspirin, aspirin, tadalafil, tadalafil, rosuvastatin, rosuvastatin, sodium iodide, sodium iodide, raltegravir, raltegravir, ritonavir, ritonavir, darunavir, darunavir, dolutegravir, dolutegravir, cyanocobalamin, cyanocobalamin, cholecalciferol, cholecalciferol
Apo-Abacavir Disease Interaction
Volume of Distribution
- 0.86 ± 0.15 L/kg [IV administration]
Elimination Route
Rapid and extensive after oral administration (83% bioavailability, tablet). When a 300 mg tablet is given twice daily to subjects, the peak plasma concentration (Cmax) was 3.0 ± 0.89 mcg/mL and the area under the curve (AUC 0-12 hours) was 6.02 ± 1.73 mcg•hr/mL.
Half Life
1.54 ± 0.63 hours
Clearance
- 0.80 ± 0.24 L/hr/kg [asymptomatic, HIV-1-infected adult patients receiving single (IV dose of 150 mg]
Elimination Route
Elimination of abacavir was quantified in a mass balance study following administration of a 600-mg dose of 14C-abacavir: 99% of the radioactivity was recovered, 1.2% was excreted in the urine as abacavir, 30% as the 5′-carboxylic acid metabolite, 36% as the 5′-glucuronide metabolite, and 15% as unidentified minor metabolites in the urine. Fecal elimination accounted for 16% of the dose. Renal excretion of unchanged abacavir is a minor route of elimination in humans.
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