Peringatan Keamanan

LD50 information for darunavir is not readily available in the literature.A191562 One-time doses of up to 3,200 mg of darunavir in an oral solution and up to 1,600 mg of the tablet formulation of darunavir with ritonavir have been given volunteers without significant symptoms.L11988

Information about an overdose with darunavir with ritonavir is limited. No specific antidote exists for this drug. Treatment of In the case of an overdose, employ general supportive measures. Monitor vital signs and clinical status. It is unlikely that darunavir not amenable to removal by dialysis due to its high level of protein binding.L9227

Darunavir

DB01264

small molecule approved

Deskripsi

Darunavir is a protease inhibitor used with other HIV protease inhibitor drugs as well as ritonavir for the effective management of HIV-1 infection.L9227 As a second-generation protease inhibitor, darunavir is designed to combat resistance to standard HIV therapy.A2278,A2281 It was initially approved by the FDA in 2006.L9227

Darunavir is being studied as a possible treatment for SARS-CoV-2, the coronavirus responsible for COVID-19, due to in vitro evidence supporting its ability to combat this infection.A191682 Clinical trials are underway and are expected to conclude in August 2020.L12066

Struktur Molekul 2D

Berat 547.664
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal elimination half-life of darunavir is approximately 15 hours when it is combined with ritonavir.[A2277,L9227]
Volume Distribusi The volume of distribution of darunavir in one pharmacokinetic study in conjunction with ritonavir was 206.5 L (with a range of 161.0–264.9) in healthy young adult volunteers.[A191544] Another pharmacokinetic study revealed a volume of distribution of 220 L.[A191553]
Klirens (Clearance) Darunavir has a low renal clearance.[A191502] After intravenous administration, the clearance darunavir administered alone and with 100 mg ritonavir twice daily, was 32.8 L/h and 5.9 L/h, respectively.[L9227]

Absorpsi

The absolute oral bioavailability of one single 600 mg dose of darunavir alone and with 100 mg of ritonavir twice a day was 37% and 82%, respectively.T762 Exposure to darunavir in boosted patients has been found to be 11 times higher than in unboosted patients.A191502 Tmax is achieved approximately 2.4 to 4 hours after oral administration.T762,L9227 When darunavir is taken with food, the Cmax and AUC of darunavir given with ritonavir increase by 30% when compared to the fasted state.T762

Metabolisme

Darunavir is heavily oxidized and metabolized by hepatic cytochrome enzymes, mainly CYP3A.L9227 Darunavir is extensively metabolized in subjects who do not receive a booster, primarily via carbamate hydrolysis, isobutyl aliphatic hydroxylation, and aniline aromatic hydroxylation, as well as both benzylic aromatic hydroxylation and glucuronidation.A191502

Rute Eliminasi

A mass balance study in healthy volunteers demonstrated that after single dose administration of 400 mg 14C-darunavir, given with 100 mg ritonavir, approximately 79.5% and 13.9% of the administered dose of radiolabeled darunavir was obtained in the feces and urine, respectively. Excretion of unchanged drug accounted for 8.0% of the darunavir dose in volunteers who were unboosted.A191502 In boosted darunavir administration, unchanged darunavir made up 48.8% of the excreted dose in boosted subjects due to inhibition of darunavir metabolism by ritonavir. Unchanged drug in the urine made up 1.2% of the administered dose in volunteers who where unboosted, and 7.7% in boosted volunteers.A191502

Interaksi Makanan

1 Data
  • 1. Take with food. Food increases absorption.

Interaksi Obat

1141 Data
Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Darunavir.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Darunavir.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Darunavir.
Mecamylamine The risk or severity of adverse effects can be increased when Darunavir is combined with Mecamylamine.
Pentolinium The risk or severity of adverse effects can be increased when Darunavir is combined with Pentolinium.
Trimethaphan The risk or severity of adverse effects can be increased when Darunavir is combined with Trimethaphan.
Hexamethonium The risk or severity of adverse effects can be increased when Darunavir is combined with Hexamethonium.
Cyclopentamine The risk or severity of adverse effects can be increased when Darunavir is combined with Cyclopentamine.
Nicotine The risk or severity of adverse effects can be increased when Darunavir is combined with Nicotine.
Abacavir The serum concentration of Abacavir can be decreased when it is combined with Darunavir.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Darunavir.
Cisapride The serum concentration of Cisapride can be increased when it is combined with Darunavir.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Darunavir.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Darunavir.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Darunavir.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Darunavir.
Nevirapine The serum concentration of Nevirapine can be increased when it is combined with Darunavir.
Phenytoin The serum concentration of Phenytoin can be decreased when it is combined with Darunavir.
Tenofovir disoproxil The serum concentration of Darunavir can be increased when it is combined with Tenofovir disoproxil.
Tenofovir The serum concentration of Darunavir can be increased when it is combined with Tenofovir.
Methadone The serum concentration of Methadone can be decreased when it is combined with Darunavir.
Methotrexate The serum concentration of Methotrexate can be increased when it is combined with Darunavir.
Alprazolam The serum concentration of Alprazolam can be increased when it is combined with Darunavir.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Darunavir.
Bosentan The serum concentration of Darunavir can be decreased when it is combined with Bosentan.
Carbamazepine The serum concentration of Carbamazepine can be increased when it is combined with Darunavir.
Voriconazole The serum concentration of Voriconazole can be decreased when it is combined with Darunavir.
Efavirenz The serum concentration of Efavirenz can be increased when it is combined with Darunavir.
Trazodone The serum concentration of Trazodone can be increased when it is combined with Darunavir.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Darunavir.
Paroxetine The serum concentration of Paroxetine can be decreased when it is combined with Darunavir.
Norethisterone The serum concentration of Norethisterone can be decreased when it is combined with Darunavir.
Didanosine The absorption of Didanosine can be decreased when combined with Darunavir.
Ketoconazole The serum concentration of Darunavir can be increased when it is combined with Ketoconazole.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Darunavir.
Sertraline The serum concentration of Sertraline can be decreased when it is combined with Darunavir.
Amiodarone The serum concentration of Amiodarone can be increased when it is combined with Darunavir.
Itraconazole The metabolism of Itraconazole can be decreased when combined with Darunavir.
Saquinavir The serum concentration of Darunavir can be decreased when it is combined with Saquinavir.
Lopinavir The serum concentration of Darunavir can be decreased when it is combined with Lopinavir.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Darunavir.
Garlic Garlic can cause a decrease in the absorption of Darunavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ketoprofen The risk or severity of adverse effects can be increased when Ketoprofen is combined with Darunavir.
Dexketoprofen The risk or severity of adverse effects can be increased when Dexketoprofen is combined with Darunavir.
Insulin glargine The risk or severity of hypoglycemia can be increased when Darunavir is combined with Insulin glargine.
Insulin detemir The risk or severity of hypoglycemia can be increased when Darunavir is combined with Insulin detemir.
Insulin tregopil The risk or severity of hypoglycemia can be increased when Darunavir is combined with Insulin tregopil.
Ipragliflozin The therapeutic efficacy of Ipragliflozin can be decreased when used in combination with Darunavir.
Allicin The therapeutic efficacy of Allicin can be decreased when used in combination with Darunavir.
Tofogliflozin The therapeutic efficacy of Tofogliflozin can be decreased when used in combination with Darunavir.
Remogliflozin etabonate The therapeutic efficacy of Remogliflozin etabonate can be decreased when used in combination with Darunavir.
Tirzepatide The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Darunavir.
Gastric inhibitory polypeptide The therapeutic efficacy of Gastric inhibitory polypeptide can be decreased when used in combination with Darunavir.
Ertugliflozin The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Darunavir.
Troglitazone The therapeutic efficacy of Troglitazone can be decreased when used in combination with Darunavir.
Sulfamethoxazole The therapeutic efficacy of Sulfamethoxazole can be decreased when used in combination with Darunavir.
Rilpivirine The serum concentration of Rilpivirine can be increased when it is combined with Darunavir.
Pitolisant The serum concentration of Darunavir can be decreased when it is combined with Pitolisant.
Elagolix The serum concentration of Darunavir can be increased when it is combined with Elagolix.
Glecaprevir The serum concentration of Darunavir can be increased when it is combined with Glecaprevir.
Fluconazole The metabolism of Darunavir can be decreased when combined with Fluconazole.
Reserpine The serum concentration of Darunavir can be increased when it is combined with Reserpine.
Loxapine The serum concentration of Darunavir can be increased when it is combined with Loxapine.
Clofazimine The serum concentration of Darunavir can be increased when it is combined with Clofazimine.
Arsenic trioxide The serum concentration of Darunavir can be increased when it is combined with Arsenic trioxide.
Biricodar The serum concentration of Darunavir can be increased when it is combined with Biricodar.
Elacridar The serum concentration of Darunavir can be increased when it is combined with Elacridar.
Zosuquidar The serum concentration of Darunavir can be increased when it is combined with Zosuquidar.
Tariquidar The serum concentration of Darunavir can be increased when it is combined with Tariquidar.
Brefeldin A The serum concentration of Darunavir can be increased when it is combined with Brefeldin A.
Carfilzomib The serum concentration of Darunavir can be increased when it is combined with Carfilzomib.
Afatinib The serum concentration of Darunavir can be increased when it is combined with Afatinib.
Ledipasvir The serum concentration of Darunavir can be increased when it is combined with Ledipasvir.
Methylene blue The serum concentration of Darunavir can be increased when it is combined with Methylene blue.
Valspodar The serum concentration of Darunavir can be increased when it is combined with Valspodar.
Sarecycline The serum concentration of Darunavir can be increased when it is combined with Sarecycline.
Favipiravir The serum concentration of Darunavir can be increased when it is combined with Favipiravir.
Laniquidar The serum concentration of Darunavir can be increased when it is combined with Laniquidar.
Pibrentasvir The serum concentration of Darunavir can be increased when it is combined with Pibrentasvir.
ONT-093 The serum concentration of Darunavir can be increased when it is combined with ONT-093.
Umbralisib The serum concentration of Darunavir can be increased when it is combined with Umbralisib.
Diosmin The serum concentration of Darunavir can be increased when it is combined with Diosmin.
Sapropterin The serum concentration of Darunavir can be increased when it is combined with Sapropterin.
Levoketoconazole The metabolism of Levoketoconazole can be decreased when combined with Darunavir.
Boceprevir The serum concentration of Darunavir can be decreased when it is combined with Boceprevir.
Rifabutin The serum concentration of Rifabutin can be increased when it is combined with Darunavir.
Insulin human The risk or severity of hypoglycemia can be increased when Darunavir is combined with Insulin human.
Insulin lispro The risk or severity of hypoglycemia can be increased when Darunavir is combined with Insulin lispro.
Insulin pork The risk or severity of hypoglycemia can be increased when Darunavir is combined with Insulin pork.
Glimepiride The therapeutic efficacy of Glimepiride can be decreased when used in combination with Darunavir.
Sulfisoxazole The therapeutic efficacy of Sulfisoxazole can be decreased when used in combination with Darunavir.
Acarbose The therapeutic efficacy of Acarbose can be decreased when used in combination with Darunavir.
Acetohexamide The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Darunavir.
Miglitol The therapeutic efficacy of Miglitol can be decreased when used in combination with Darunavir.
Chlorpropamide The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Darunavir.
Pentamidine The therapeutic efficacy of Pentamidine can be decreased when used in combination with Darunavir.
Tolazamide The therapeutic efficacy of Tolazamide can be decreased when used in combination with Darunavir.
Phenformin The therapeutic efficacy of Phenformin can be decreased when used in combination with Darunavir.
Gliclazide The therapeutic efficacy of Gliclazide can be decreased when used in combination with Darunavir.
Tolbutamide The therapeutic efficacy of Tolbutamide can be decreased when used in combination with Darunavir.

Target Protein

Pol polyprotein pol
Gag-Pol polyprotein gag-pol

Referensi & Sumber

Synthesis reference: Agarwal Virendra, Kumar Katariya, Lalit Keshav, Upadhyay Ashish, Rameschandra Pada Ranjit Ravatbhai, Ghetiya Renish Mansukhlal ,Tuvar Sabirhusen Ismalbhai. 2016. Google patents: WO2016193481A1
Artikel (PubMed)
  • PMID: 18389894
    Back D, Sekar V, Hoetelmans RM: Darunavir: pharmacokinetics and drug interactions. Antivir Ther. 2008;13(1):1-13.
  • PMID: 19209258
    Tremblay CL: Combating HIV resistance - focus on darunavir. Ther Clin Risk Manag. 2008 Aug;4(4):759-66.
  • PMID: 17635930
    Koh Y, Matsumi S, Das D, Amano M, Davis DA, Li J, Leschenko S, Baldridge A, Shioda T, Yarchoan R, Ghosh AK, Mitsuya H: Potent inhibition of HIV-1 replication by novel non-peptidyl small molecule inhibitors of protease dimerization. J Biol Chem. 2007 Sep 28;282(39):28709-20. Epub 2007 Jul 17.
  • PMID: 16480273
    Kovalevsky AY, Tie Y, Liu F, Boross PI, Wang YF, Leshchenko S, Ghosh AK, Harrison RW, Weber IT: Effectiveness of nonpeptide clinical inhibitor TMC-114 on HIV-1 protease with highly drug resistant mutations D30N, I50V, and L90M. J Med Chem. 2006 Feb 23;49(4):1379-87.
  • PMID: 15917527
    De Meyer S, Azijn H, Surleraux D, Jochmans D, Tahri A, Pauwels R, Wigerinck P, de Bethune MP: TMC114, a novel human immunodeficiency virus type 1 protease inhibitor active against protease inhibitor-resistant viruses, including a broad range of clinical isolates. Antimicrob Agents Chemother. 2005 Jun;49(6):2314-21.
  • PMID: 23143899
    Croteau D, Rossi SS, Best BM, Capparelli E, Ellis RJ, Clifford DB, Collier AC, Gelman BB, Marra CM, McArthur J, McCutchan JA, Morgello S, Simpson DM, Grant I, Letendre S: Darunavir is predominantly unbound to protein in cerebrospinal fluid and concentrations exceed the wild-type HIV-1 median 90% inhibitory concentration. J Antimicrob Chemother. 2013 Mar;68(3):684-9. doi: 10.1093/jac/dks441. Epub 2012 Nov 9.
  • PMID: 19131522
    Vermeir M, Lachau-Durand S, Mannens G, Cuyckens F, van Hoof B, Raoof A: Absorption, metabolism, and excretion of darunavir, a new protease inhibitor, administered alone and with low-dose ritonavir in healthy subjects. Drug Metab Dispos. 2009 Apr;37(4):809-20. doi: 10.1124/dmd.108.024109. Epub 2009 Jan 8.
  • PMID: 29082041
    Balayan T, Horvath H, Rutherford GW: Ritonavir-Boosted Darunavir Plus Two Nucleoside Reverse Transcriptase Inhibitors versus Other Regimens for Initial Antiretroviral Therapy for People with HIV Infection: A Systematic Review. AIDS Res Treat. 2017;2017:2345617. doi: 10.1155/2017/2345617. Epub 2017 Sep 26.
Menampilkan 8 dari 14 artikel.
Textbook
  • Christine J Kubin, Scott M Hammer (2010). Infectious diseases (3rd ed.). Mosby.

Contoh Produk & Brand

Produk: 164 • International brands: 0
Produk
  • Apo-darunavir
    Tablet • 600 mg • Oral • Canada • Generic • Approved
  • Apo-darunavir
    Tablet • 800 mg • Oral • Canada • Generic • Approved
  • Auro-darunavir
    Tablet • 400 mg • Oral • Canada • Generic • Approved
  • Auro-darunavir
    Tablet • 600 mg • Oral • Canada • Generic • Approved
  • Auro-darunavir
    Tablet • 800 mg • Oral • Canada • Generic • Approved
  • Darunavir
    Powder • 1 kg/1kg • Not applicable • US
  • Darunavir
    Tablet • 400 mg • Oral • Canada • Approved
  • Darunavir
    Tablet • 600 mg • Oral • Canada • Approved
Menampilkan 8 dari 164 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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