Efavirenz

DB00625

small molecule approved investigational

Deskripsi

Efavirenz (brand names Sustiva® and Stocrin®) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and is used as part of highly active antiretroviral therapy (HAART) for the treatment of a human immunodeficiency virus (HIV) type 1.

For HIV infection that has not previously been treated, efavirenz and lamivudine in combination with zidovudine or tenofovir is the preferred NNRTI-based regimen.

Efavirenz is also used in combination with other antiretroviral agents as part of an expanded postexposure prophylaxis regimen to prevent HIV transmission for those exposed to materials associated with a high risk for HIV transmission.

Struktur Molekul 2D

Berat 315.675
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 40-55 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Efavirenz is principally metabolized by the cytochrome P450 system to hydroxylated metabolites with subsequent glucuronidation of these hydroxylated metabolites. These metabolites are essentially inactive against HIV-1.

Rute Eliminasi

Nearly all of the urinary excretion of the radiolabeled drug was in the form of metabolites.

Farmakogenomik

1 Varian
CYP2B6 (rs3745274)

The presence of this polymorphism in CYP2B6 is associated with reduction in efavirenz metabolism.

Interaksi Makanan

2 Data
  • 1. Avoid excessive or chronic alcohol consumption. Alcohol may contribute to additive adverse effects when taken with efavirenz.
  • 2. Take on an empty stomach. Taking efavirenz with food increases efavirenz concentrations and may increase the frequency of adverse reactions. In patients who cannot swallow capsules, the capsule contents can be administered with a small amount of food or infant formula using the capsule sprinkle method of administration.

Interaksi Obat

1710 Data
Ivabradine Ivabradine may increase the QTc-prolonging activities of Efavirenz.
Reserpine Reserpine may decrease the excretion rate of Efavirenz which could result in a higher serum level.
Cimetidine Cimetidine may decrease the excretion rate of Efavirenz which could result in a higher serum level.
Ursodeoxycholic acid Ursodeoxycholic acid may decrease the excretion rate of Efavirenz which could result in a higher serum level.
Cholic Acid Cholic Acid may decrease the excretion rate of Efavirenz which could result in a higher serum level.
Valinomycin Valinomycin may decrease the excretion rate of Efavirenz which could result in a higher serum level.
Olmesartan Olmesartan may decrease the excretion rate of Efavirenz which could result in a higher serum level.
Lenvatinib Lenvatinib may decrease the excretion rate of Efavirenz which could result in a higher serum level.
Cyclosporine The serum concentration of Cyclosporine can be decreased when it is combined with Efavirenz.
Pravastatin The serum concentration of Pravastatin can be decreased when it is combined with Efavirenz.
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Efavirenz.
Peginterferon alfa-2b The serum concentration of Efavirenz can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Efavirenz can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Efavirenz can be decreased when it is combined with Teriflunomide.
Buprenorphine Efavirenz may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Efavirenz.
Dronabinol The serum concentration of Dronabinol can be increased when it is combined with Efavirenz.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Efavirenz.
Magnesium sulfate The therapeutic efficacy of Efavirenz can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Efavirenz may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Efavirenz may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Efavirenz.
Mirtazapine Efavirenz may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Efavirenz.
Orphenadrine Efavirenz may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Efavirenz may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Pramipexole Efavirenz may increase the sedative activities of Pramipexole.
Rotigotine Efavirenz may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Efavirenz.
Sodium oxybate Efavirenz may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Efavirenz may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Efavirenz.
Thalidomide Efavirenz may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Efavirenz may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Citalopram The serum concentration of Citalopram can be increased when it is combined with Efavirenz.
Clopidogrel The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Efavirenz resulting in a loss in efficacy.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Efavirenz.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Efavirenz.
Colchicine The metabolism of Colchicine can be decreased when combined with Efavirenz.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Efavirenz.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Efavirenz.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Efavirenz.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Efavirenz.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Efavirenz.
Indinavir The serum concentration of Indinavir can be decreased when it is combined with Efavirenz.
Lovastatin The serum concentration of Lovastatin can be decreased when it is combined with Efavirenz.
Phenytoin The serum concentration of Efavirenz can be decreased when it is combined with Phenytoin.
Fosphenytoin The serum concentration of Efavirenz can be decreased when it is combined with Fosphenytoin.
Isradipine The serum concentration of Isradipine can be decreased when it is combined with Efavirenz.
Diltiazem The serum concentration of Diltiazem can be decreased when it is combined with Efavirenz.
Trimethadione The serum concentration of Trimethadione can be decreased when it is combined with Efavirenz.
Amlodipine The serum concentration of Amlodipine can be decreased when it is combined with Efavirenz.
Nimodipine The serum concentration of Nimodipine can be decreased when it is combined with Efavirenz.
Nisoldipine The serum concentration of Nisoldipine can be decreased when it is combined with Efavirenz.
Lercanidipine The serum concentration of Lercanidipine can be decreased when it is combined with Efavirenz.
Cinnarizine The serum concentration of Cinnarizine can be decreased when it is combined with Efavirenz.
Ethosuximide The serum concentration of Ethosuximide can be decreased when it is combined with Efavirenz.
Nicardipine The serum concentration of Nicardipine can be decreased when it is combined with Efavirenz.
Verapamil The serum concentration of Verapamil can be decreased when it is combined with Efavirenz.
Loperamide The metabolism of Loperamide can be decreased when combined with Efavirenz.
Zonisamide The serum concentration of Zonisamide can be decreased when it is combined with Efavirenz.
Felodipine The serum concentration of Felodipine can be decreased when it is combined with Efavirenz.
Nitrendipine The serum concentration of Nitrendipine can be decreased when it is combined with Efavirenz.
Perhexiline The serum concentration of Perhexiline can be decreased when it is combined with Efavirenz.
Nifedipine The serum concentration of Nifedipine can be decreased when it is combined with Efavirenz.
Amiodarone The serum concentration of Amiodarone can be decreased when it is combined with Efavirenz.
Carvedilol The serum concentration of Carvedilol can be decreased when it is combined with Efavirenz.
Mibefradil The serum concentration of Mibefradil can be decreased when it is combined with Efavirenz.
Nimesulide The serum concentration of Nimesulide can be decreased when it is combined with Efavirenz.
Prenylamine The serum concentration of Prenylamine can be decreased when it is combined with Efavirenz.
Cyclandelate The serum concentration of Cyclandelate can be decreased when it is combined with Efavirenz.
Flunarizine The serum concentration of Flunarizine can be decreased when it is combined with Efavirenz.
Fluspirilene The serum concentration of Fluspirilene can be decreased when it is combined with Efavirenz.
Clevidipine The serum concentration of Clevidipine can be decreased when it is combined with Efavirenz.
Methsuximide The serum concentration of Methsuximide can be decreased when it is combined with Efavirenz.
Seletracetam The serum concentration of Seletracetam can be decreased when it is combined with Efavirenz.
Nylidrin The serum concentration of Nylidrin can be decreased when it is combined with Efavirenz.
Ziconotide The serum concentration of Ziconotide can be decreased when it is combined with Efavirenz.
Dotarizine The serum concentration of Dotarizine can be decreased when it is combined with Efavirenz.
Xylometazoline The serum concentration of Xylometazoline can be decreased when it is combined with Efavirenz.
Nilvadipine The serum concentration of Nilvadipine can be decreased when it is combined with Efavirenz.
Tranilast The serum concentration of Tranilast can be decreased when it is combined with Efavirenz.
Fasudil The serum concentration of Fasudil can be decreased when it is combined with Efavirenz.
Agmatine The serum concentration of Agmatine can be decreased when it is combined with Efavirenz.
Fendiline The serum concentration of Fendiline can be decreased when it is combined with Efavirenz.
Eperisone The serum concentration of Eperisone can be decreased when it is combined with Efavirenz.
Trimebutine The serum concentration of Trimebutine can be decreased when it is combined with Efavirenz.
Pinaverium The serum concentration of Pinaverium can be decreased when it is combined with Efavirenz.
Aranidipine The serum concentration of Aranidipine can be decreased when it is combined with Efavirenz.
Azelnidipine The serum concentration of Azelnidipine can be decreased when it is combined with Efavirenz.
Benidipine The serum concentration of Benidipine can be decreased when it is combined with Efavirenz.
Cilnidipine The serum concentration of Cilnidipine can be decreased when it is combined with Efavirenz.
Darodipine The serum concentration of Darodipine can be decreased when it is combined with Efavirenz.
Efonidipine The serum concentration of Efonidipine can be decreased when it is combined with Efavirenz.
Lacidipine The serum concentration of Lacidipine can be decreased when it is combined with Efavirenz.
Manidipine The serum concentration of Manidipine can be decreased when it is combined with Efavirenz.
Niguldipine The serum concentration of Niguldipine can be decreased when it is combined with Efavirenz.
Niludipine The serum concentration of Niludipine can be decreased when it is combined with Efavirenz.
Carboxyamidotriazole The serum concentration of Carboxyamidotriazole can be decreased when it is combined with Efavirenz.
Naftopidil The serum concentration of Naftopidil can be decreased when it is combined with Efavirenz.

Target Protein

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

Referensi & Sumber

Synthesis reference: John Doney, "Amorphous efavirenz and the production thereof." U.S. Patent US20070026073, issued February 01, 2007.
Artikel (PubMed)
  • PMID: 12386343
    Ren J, Bird LE, Chamberlain PP, Stewart-Jones GB, Stuart DI, Stammers DK: Structure of HIV-2 reverse transcriptase at 2.35-A resolution and the mechanism of resistance to non-nucleoside inhibitors. Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14410-5. Epub 2002 Oct 17.
  • PMID: 15983905
    Robertson SM, Penzak SR, Lane J, Pau AK, Mican JM: A potentially significant interaction between efavirenz and phenytoin: a case report and review of the literature. Clin Infect Dis. 2005 Jul 15;41(2):e15-8. doi: 10.1086/431208. Epub 2005 Jun 7.
  • PMID: 22318618
    Michaud V, Ogburn E, Thong N, Aregbe AO, Quigg TC, Flockhart DA, Desta Z: Induction of CYP2C19 and CYP3A activity following repeated administration of efavirenz in healthy volunteers. Clin Pharmacol Ther. 2012 Mar;91(3):475-82. doi: 10.1038/clpt.2011.249. Epub 2012 Feb 8.

Contoh Produk & Brand

Produk: 110 • International brands: 7
Produk
  • Apo-efavirenz-emtricitabine-tenofovir
    Tablet • - • Oral • Canada • Generic • Approved
  • Atripla
    Tablet, film coated • - • Oral • US • Approved
  • Atripla
    Tablet, film coated • - • Oral • US • Approved
  • Atripla
    Tablet, film coated • 600 mg/1 • Oral • US • Approved
  • Atripla
    Tablet, film coated • - • Oral • US • Approved
  • Atripla
    Tablet, film coated • - • Oral • US • Approved
  • Atripla
    Tablet, film coated • - • Oral • US • Approved
  • Atripla
    Tablet, film coated • - • Oral • US • Approved
Menampilkan 8 dari 110 produk.
International Brands
  • E.F. — McNeil & Argus
  • Efavir — Cipla
  • Efcure — Emcure Pharmaceuticals
  • Efferven — Ranbaxy Laboratories
  • Estiva — Hetero
  • Evirenz — Alkem Laboratories
  • Viranz — Aurobindo Pharma

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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