Peringatan Keamanan

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).

Abacavir

DB01048

small molecule approved investigational

Deskripsi

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.

Struktur Molekul 2D

Berat 286.3323
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 1.54 ± 0.63 hours
Volume Distribusi * 0.86 ± 0.15 L/kg [IV administration]
Klirens (Clearance) * 0.80 ± 0.24 L/hr/kg [asymptomatic, HIV-1-infected adult patients receiving single (IV dose of 150 mg]

Absorpsi

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.

Metabolisme

Hepatic, by alcohol dehydrogenase and glucuronosyltransferase to a 5′-carboxylic acid metabolite and 5′-glucuronide metabolite, respectively. These metabolites have no antiviral activity. Abacavir is not significantly metabolized by cytochrome P450 enzymes.

Rute Eliminasi

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.

Farmakogenomik

1 Varian
HCP5 (rs2395029)

Patients who carry this SNP are at a higher risk of experiencing a hypersensitivity reaction to abacavir.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Alcohol increases the systemic exposure to the drug.
  • 2. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

779 Data
Ritonavir The serum concentration of Abacavir can be decreased when it is combined with Ritonavir.
Darunavir The serum concentration of Abacavir can be decreased when it is combined with Darunavir.
Lopinavir The serum concentration of Abacavir can be decreased when it is combined with Lopinavir.
Atazanavir The serum concentration of Abacavir can be decreased when it is combined with Atazanavir.
Methadone The therapeutic efficacy of Abacavir can be decreased when used in combination with Methadone.
Ribavirin Ribavirin may increase the hepatotoxic activities of Abacavir.
Nelfinavir The metabolism of Abacavir can be increased when combined with Nelfinavir.
Phenytoin The metabolism of Abacavir can be increased when combined with Phenytoin.
Desogestrel The metabolism of Abacavir can be increased when combined with Desogestrel.
Lamotrigine The metabolism of Abacavir can be increased when combined with Lamotrigine.
Efavirenz The metabolism of Abacavir can be increased when combined with Efavirenz.
Primidone The metabolism of Abacavir can be increased when combined with Primidone.
Tipranavir The metabolism of Abacavir can be increased when combined with Tipranavir.
Ethinylestradiol The metabolism of Abacavir can be increased when combined with Ethinylestradiol.
Rifampin The metabolism of Abacavir can be increased when combined with Rifampicin.
Phenobarbital The metabolism of Abacavir can be increased when combined with Phenobarbital.
Testosterone propionate The metabolism of Abacavir can be increased when combined with Testosterone propionate.
Ganciclovir The risk or severity of cytopenia can be increased when Ganciclovir is combined with Abacavir.
Valganciclovir The risk or severity of cytopenia can be increased when Valganciclovir is combined with Abacavir.
Cyclosporine Cyclosporine may decrease the excretion rate of Abacavir which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Abacavir which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Abacavir which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Abacavir which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Abacavir which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Abacavir which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Abacavir which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Abacavir which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Abacavir which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Abacavir which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Abacavir which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Abacavir which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Abacavir which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Abacavir which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Abacavir which could result in a higher serum level.
Methotrexate Methotrexate may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cephalexin Cephalexin may decrease the excretion rate of Abacavir which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Abacavir which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Abacavir which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Abacavir which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Abacavir which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Abacavir which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Abacavir which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Abacavir which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Abacavir which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Abacavir which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Abacavir which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Abacavir which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Abacavir which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Abacavir which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Abacavir which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Abacavir which could result in a higher serum level.
Meloxicam Meloxicam may decrease the excretion rate of Abacavir which could result in a higher serum level.
Carprofen Carprofen may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Abacavir which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Abacavir which could result in a higher serum level.
Tacrolimus Tacrolimus may decrease the excretion rate of Abacavir which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Abacavir which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Abacavir which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Abacavir which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Abacavir which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Abacavir which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Abacavir which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Abacavir which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Abacavir which could result in a higher serum level.
Ibuprofen Ibuprofen may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Abacavir which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Abacavir which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Abacavir which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Abacavir which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefoperazone Cefoperazone may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefotetan Cefotetan may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefoxitin Cefoxitin may decrease the excretion rate of Abacavir which could result in a higher serum level.
Ceftizoxime Ceftizoxime may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefradine Cefradine may decrease the excretion rate of Abacavir which could result in a higher serum level.
Magnesium salicylate Magnesium salicylate may decrease the excretion rate of Abacavir which could result in a higher serum level.
Salsalate Salsalate may decrease the excretion rate of Abacavir which could result in a higher serum level.
Choline magnesium trisalicylate Choline magnesium trisalicylate may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefepime Cefepime may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefacetrile Cefacetrile may decrease the excretion rate of Abacavir which could result in a higher serum level.
Ceftibuten Ceftibuten may decrease the excretion rate of Abacavir which could result in a higher serum level.
Cefpodoxime Cefpodoxime may decrease the excretion rate of Abacavir which could result in a higher serum level.
Antrafenine Antrafenine may decrease the excretion rate of Abacavir which could result in a higher serum level.
Aminophenazone Aminophenazone may decrease the excretion rate of Abacavir which could result in a higher serum level.
Antipyrine Antipyrine may decrease the excretion rate of Abacavir which could result in a higher serum level.

Target Protein

Reverse transcriptase/RNaseH pol
Gag-Pol polyprotein gag-pol

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17356469
    Zucman D, Truchis Pd, Majerholc C, Stegman S, Caillat-Zucman S: Prospective screening for human leukocyte antigen-B*5701 avoids abacavir hypersensitivity reaction in the ethnically mixed French HIV population. J Acquir Immune Defic Syndr. 2007 May 1;45(1):1-3.

Contoh Produk & Brand

Produk: 90 • International brands: 0
Produk
  • Abacavir
    Solution • 20 mg/1mL • Oral • US • Generic • Approved
  • Abacavir
    Tablet, film coated • 300 mg/1 • Oral • US • Generic • Approved
  • Abacavir
    Tablet, film coated • 300 mg/1 • Oral • US • Generic • Approved
  • Abacavir
    Tablet, film coated • 300 mg/1 • Oral • US • Generic • Approved
  • Abacavir
    Solution • 20 mg/1mL • Oral • US • Generic • Approved
  • Abacavir
    Solution • 20 mg/1mL • Oral • US • Generic • Approved
  • Abacavir
    Tablet, film coated • 300 mg/1 • Oral • US • Generic • Approved
  • Abacavir
    Tablet • 300 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 90 produk.

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