Atazanavir

DB01072

small molecule approved investigational

Deskripsi

Atazanavir (formerly known as BMS-232632) is an antiretroviral drug of the protease inhibitor (PI) class. Like other antiretrovirals, it is used to treat infection of human immunodeficiency virus (HIV). Atazanavir is distinguished from other PIs in that it can be given once daily (rather than requiring multiple doses per day) and has lesser effects on the patient's lipid profile (the amounts of cholesterol and other fatty substances in the blood). Like other protease inhibitors, it is used only in combination with other HIV medications. The U.S. Food and Drug Administration (FDA) approved atazanavir on June 20, 2003.

Struktur Molekul 2D

Berat 704.8555
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean elimination half-life of atazanavir in healthy subjects (n=214) and adult subjects with HIV-1 infection (n=13) was approximately 7 hours at steady state following a dose of 400 mg daily with a light meal. Elimination half-life in hepatically impaired is 12.1 hours (following a single 400 mg dose).[L48636]
Volume Distribusi In patients with HIV infection, the volume of distribution of atazanavir was estimated to be 88.3 L.[A261971]
Klirens (Clearance) In patients with HIV infection, the clearance of atazanavir was estimated to be 12.9 L/hr.[A261971]

Absorpsi

Atazanavir is rapidly absorbed with a Tmax of approximately 2.5 hours. Atazanavir demonstrates nonlinear pharmacokinetics with greater than dose-proportional increases in AUC and Cmax values over the dose range of 200 to 800 mg once daily. A steady state is achieved between Days 4 and 8, with an accumulation of approximately 2.3-fold.L48636 Administration of atazanavir with food enhances bioavailability and reduces pharmacokinetic variability. Administration of a single 400-mg dose of atazanavir with a light meal (357 kcal, 8.2 g fat, 10.6 g protein) resulted in a 70% increase in AUC and 57% increase in Cmax relative to the fasting state. Administration of a single 400-mg dose of atazanavir with a high-fat meal (721 kcal, 37.3 g fat, 29.4 g protein) resulted in a mean increase in AUC of 35% with no change in Cmax relative to the fasting state. Administration of atazanavir with either a light or high-fat meal decreased the coefficient of variation of AUC and Cmax by approximately one-half compared to the fasting state.L48636 Coadministration of a single 300-mg dose of atazanavir and a 100-mg dose of ritonavir with a light meal (336 kcal, 5.1 g fat, 9.3 g protein) resulted in a 33% increase in the AUC and a 40% increase in both the Cmax and the 24-hour concentration of atazanavir relative to the fasting state. Coadministration with a high-fat meal (951 kcal, 54.7 g fat, 35.9 g protein) did not affect the AUC of atazanavir relative to fasting conditions and the Cmax was within 11% of fasting values. The 24-hour concentration following a high-fat meal was increased by approximately 33% due to delayed absorption; the median Tmax increased from 2.0 to 5.0 hours. Coadministration of atazanavir with ritonavir with either a light or a high-fat meal decreased the coefficient of variation of AUC and Cmax by approximately 25% compared to the fasting state.L48636

Metabolisme

Atazanavir is extensively metabolized in humans. The major biotransformation pathways of atazanavir in humans consisted of monooxygenation and dioxygenation. Other minor biotransformation pathways for atazanavir or its metabolites consisted of glucuronidation, N-dealkylation, hydrolysis, and oxygenation with dehydrogenation. Two minor metabolites of atazanavir in plasma have been characterized. Neither metabolite demonstrated in vitro antiviral activity. In vitro studies using human liver microsomes suggested that atazanavir is metabolized by CYP3A.L48636

Rute Eliminasi

Following a single 400-mg dose of 14C-atazanavir, 79% and 13% of the total radioactivity was recovered in the feces and urine, respectively. Unchanged drugs accounted for approximately 20% and 7% of the administered dose in the feces and urine, respectively.L48636

Farmakogenomik

3 Varian
UGT1A1 (rs3064744)

The presence of this genotype in UGT1A1 may indicate an increased risk of hyperbilirubinemia from atazanavir treatment.

UGT1A1 (rs8175347)

The presence of this genotype in UGT1A1 may indicate an increased risk of hyperbilirubinemia from atazanavir treatment.

UGT1A1 (rs887829)

The presence of this genotype in UGT1A1 may indicate an increased risk of hyperbilirubinemia from atazanavir treatment.

Interaksi Makanan

1 Data
  • 1. Take with food. Food increases product absorption and reduces pharmacokinetic variability.

Interaksi Obat

1846 Data
Reserpine Reserpine may decrease the excretion rate of Atazanavir which could result in a higher serum level.
Ursodeoxycholic acid Ursodeoxycholic acid may decrease the excretion rate of Atazanavir which could result in a higher serum level.
Cholic Acid Cholic Acid may decrease the excretion rate of Atazanavir which could result in a higher serum level.
Valinomycin Valinomycin may decrease the excretion rate of Atazanavir which could result in a higher serum level.
Olmesartan Olmesartan may decrease the excretion rate of Atazanavir which could result in a higher serum level.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Atazanavir.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Atazanavir.
Cimetidine Cimetidine can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Nizatidine Nizatidine can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ranitidine Ranitidine can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Famotidine Famotidine can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methantheline Methantheline can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium oxide Magnesium oxide can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sodium bicarbonate Sodium bicarbonate can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminum hydroxide Aluminum hydroxide can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium carbonate Calcium carbonate can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Metiamide Metiamide can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Roxatidine acetate Roxatidine acetate can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magaldrate Magaldrate can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium hydroxide Magnesium hydroxide can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium trisilicate Magnesium trisilicate can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium carbonate Magnesium carbonate can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lafutidine Lafutidine can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lavoltidine Lavoltidine can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bismuth subnitrate Bismuth subnitrate can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium silicate Magnesium silicate can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium acetoacetate Aluminium acetoacetate can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Hydrotalcite Hydrotalcite can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium peroxide Magnesium peroxide can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Almasilate Almasilate can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium glycinate Aluminium glycinate can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aloglutamol Aloglutamol can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Niperotidine Niperotidine can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium silicate Calcium silicate can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium phosphate Aluminium phosphate can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Omeprazole Omeprazole can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Esomeprazole Esomeprazole can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Rabeprazole Rabeprazole can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dexlansoprazole Dexlansoprazole can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dexrabeprazole Dexrabeprazole can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sodium zirconium cyclosilicate Sodium zirconium cyclosilicate can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Vonoprazan Vonoprazan can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Abacavir The serum concentration of Abacavir can be decreased when it is combined with Atazanavir.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Atazanavir.
Cisapride The serum concentration of Cisapride can be increased when it is combined with Atazanavir.
Clarithromycin The serum concentration of Clarithromycin can be increased when it is combined with Atazanavir.
Cyclophosphamide The serum concentration of the active metabolites of Cyclophosphamide can be increased when Cyclophosphamide is used in combination with Atazanavir.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Atazanavir.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Atazanavir.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Atazanavir.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Atazanavir.
Desogestrel The serum concentration of Desogestrel can be increased when it is combined with Atazanavir.
Megestrol acetate The serum concentration of Megestrol acetate can be increased when it is combined with Atazanavir.
Levonorgestrel The serum concentration of Levonorgestrel can be increased when it is combined with Atazanavir.
Medroxyprogesterone acetate The serum concentration of Medroxyprogesterone acetate can be increased when it is combined with Atazanavir.
Norethisterone The serum concentration of Norethisterone can be increased when it is combined with Atazanavir.
Ethynodiol diacetate The serum concentration of Ethynodiol diacetate can be increased when it is combined with Atazanavir.
Norgestimate The serum concentration of Norgestimate can be increased when it is combined with Atazanavir.
Drospirenone The serum concentration of Drospirenone can be increased when it is combined with Atazanavir.
Cyproterone acetate The serum concentration of Cyproterone acetate can be increased when it is combined with Atazanavir.
Gestodene The serum concentration of Gestodene can be increased when it is combined with Atazanavir.
Hydroxyprogesterone caproate The serum concentration of Hydroxyprogesterone caproate can be increased when it is combined with Atazanavir.
Dienogest The serum concentration of Dienogest can be increased when it is combined with Atazanavir.
Norethynodrel The serum concentration of Norethynodrel can be increased when it is combined with Atazanavir.
Norgestrel The serum concentration of Norgestrel can be increased when it is combined with Atazanavir.
Gestrinone The serum concentration of Gestrinone can be increased when it is combined with Atazanavir.
Lynestrenol The serum concentration of Lynestrenol can be increased when it is combined with Atazanavir.
Chlormadinone The serum concentration of Chlormadinone can be increased when it is combined with Atazanavir.
Norgestrienone The serum concentration of Norgestrienone can be increased when it is combined with Atazanavir.
Quingestanol The serum concentration of Quingestanol can be increased when it is combined with Atazanavir.
Demegestone The serum concentration of Demegestone can be increased when it is combined with Atazanavir.
Nomegestrol acetate The serum concentration of Nomegestrol acetate can be increased when it is combined with Atazanavir.
Tenofovir disoproxil The serum concentration of Atazanavir can be decreased when it is combined with Tenofovir disoproxil.
Tenofovir alafenamide The serum concentration of Atazanavir can be decreased when it is combined with Tenofovir alafenamide.
Tenofovir The serum concentration of Atazanavir can be decreased when it is combined with Tenofovir.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Atazanavir.
Alprazolam The serum concentration of Alprazolam can be increased when it is combined with Atazanavir.
Foscarnet The risk or severity of nephrotoxicity can be increased when Atazanavir is combined with Foscarnet.
Mannitol The risk or severity of nephrotoxicity can be increased when Mannitol is combined with Atazanavir.
Olanzapine Olanzapine can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Promethazine Promethazine can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Doxepin Doxepin can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Asenapine Asenapine can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Epinastine Epinastine can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lamotrigine The serum concentration of Lamotrigine can be decreased when it is combined with Atazanavir.
Bosentan The serum concentration of Atazanavir can be decreased when it is combined with Bosentan.
Rifabutin The serum concentration of 25-O-Desacetylrifabutin, an active metabolite of Rifabutin, can be increased when used in combination with Atazanavir.
Efavirenz The serum concentration of Atazanavir can be decreased when it is combined with Efavirenz.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Atazanavir.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Atazanavir.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Atazanavir.
Disulfiram The therapeutic efficacy of Disulfiram can be decreased when used in combination with Atazanavir.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Atazanavir.
Didanosine The serum concentration of Atazanavir can be decreased when it is combined with Didanosine.
Minocycline The serum concentration of Atazanavir can be decreased when it is combined with Minocycline.
Elvitegravir The serum concentration of Elvitegravir can be increased when it is combined with Atazanavir.
Etravirine The serum concentration of Etravirine can be increased when it is combined with Atazanavir.
Pitavastatin The serum concentration of Pitavastatin can be increased when it is combined with Atazanavir.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Atazanavir.
Garlic Garlic can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.

Target Protein

Pol polyprotein pol
Gag-Pol polyprotein gag-pol

Referensi & Sumber

Artikel (PubMed)
  • PMID: 19496633
    Croom KF, Dhillon S, Keam SJ: Atazanavir: a review of its use in the management of HIV-1 infection. Drugs. 2009 May 29;69(8):1107-40. doi: 10.2165/00003495-200969080-00009.
  • PMID: 18389089
    von Hentig N: Atazanavir/ritonavir: a review of its use in HIV therapy. Drugs Today (Barc). 2008 Feb;44(2):103-32. doi: 10.1358/dot.2008.44.2.1137107.
  • PMID: 16266202
    Swainston Harrison T, Scott LJ: Atazanavir: a review of its use in the management of HIV infection. Drugs. 2005;65(16):2309-36.
  • PMID: 16176117
    Le Tiec C, Barrail A, Goujard C, Taburet AM: Clinical pharmacokinetics and summary of efficacy and tolerability of atazanavir. Clin Pharmacokinet. 2005;44(10):1035-50.
  • PMID: 20116610
    Lopez-Cortes LF: Pharmacology, pharmacokinetic features and interactions of atazanavir. Enferm Infecc Microbiol Clin. 2008 Dec;26 Suppl 17:2-8. doi: 10.1016/S0213-005X(08)76613-8.
  • PMID: 15585441
    Busti AJ, Hall RG, Margolis DM: Atazanavir for the treatment of human immunodeficiency virus infection. Pharmacotherapy. 2004 Dec;24(12):1732-47.
  • PMID: 16940065
    Colombo S, Buclin T, Cavassini M, Decosterd LA, Telenti A, Biollaz J, Csajka C: Population pharmacokinetics of atazanavir in patients with human immunodeficiency virus infection. Antimicrob Agents Chemother. 2006 Nov;50(11):3801-8. doi: 10.1128/AAC.00098-06. Epub 2006 Aug 28.

Contoh Produk & Brand

Produk: 115 • International brands: 2
Produk
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    Capsule • 150 mg • Oral • Canada • Generic • Approved
  • Apo-atazanavir
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  • Apo-atazanavir
    Capsule • 300 mg • Oral • Canada • Generic • Approved
  • Atazanavir
    Capsule, gelatin coated • 150 mg/1 • Oral • US • Generic • Approved
  • Atazanavir
    Capsule, gelatin coated • 200 mg/1 • Oral • US • Generic • Approved
  • Atazanavir
    Capsule, gelatin coated • 300 mg/1 • Oral • US • Generic • Approved
  • Atazanavir
    Capsule, gelatin coated • 100 mg/1 • Oral • US • Generic • Approved
  • Atazanavir
    Capsule, gelatin coated • 150 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 115 produk.
International Brands
  • Latazanavir
  • Zrivada

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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