Raltegravir

DB06817

small molecule approved

Deskripsi

Raltegravir is an antiretroviral drug produced by Merck & Co., used to treat HIV infection. It received approval by the U.S. Food and Drug Administration (FDA) on 12 October 2007, the first of a new class of HIV drugs, the integrase inhibitors, to receive such approval.

Struktur Molekul 2D

Berat 444.4163
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 9 hours
Volume Distribusi Approximately 83% bound to human plasma protein and is minimally distributed into red blood cells (blood-to-plasma partitioning ratio of 0.6).
Klirens (Clearance) The major mechanism of clearance of raltegravir in humans is glucuronidation mediated by UGT1A1, the renal clearance of unchanged drug is a minor pathway of elimination of raltegravir (9% of total dose).

Absorpsi

Absorbed from the gastrointestinal tract.

Metabolisme

Hepatic (UGT1A1)

Rute Eliminasi

Feces and urine

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

238 Data
Pravastatin The risk or severity of myopathy and rhabdomyolysis can be increased when Raltegravir is combined with Pravastatin.
Lovastatin The risk or severity of myopathy and rhabdomyolysis can be increased when Raltegravir is combined with Lovastatin.
Cerivastatin The risk or severity of myopathy and rhabdomyolysis can be increased when Raltegravir is combined with Cerivastatin.
Simvastatin The risk or severity of myopathy and rhabdomyolysis can be increased when Raltegravir is combined with Simvastatin.
Atorvastatin The risk or severity of myopathy and rhabdomyolysis can be increased when Raltegravir is combined with Atorvastatin.
Fluvastatin The risk or severity of myopathy and rhabdomyolysis can be increased when Raltegravir is combined with Fluvastatin.
Rosuvastatin The risk or severity of myopathy and rhabdomyolysis can be increased when Raltegravir is combined with Rosuvastatin.
Mevastatin The risk or severity of myopathy and rhabdomyolysis can be increased when Raltegravir is combined with Mevastatin.
Pitavastatin The risk or severity of myopathy and rhabdomyolysis can be increased when Raltegravir is combined with Pitavastatin.
Pantoprazole Pantoprazole can cause an increase in the absorption of Raltegravir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Omeprazole Omeprazole can cause an increase in the absorption of Raltegravir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Lansoprazole Lansoprazole can cause an increase in the absorption of Raltegravir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Esomeprazole Esomeprazole can cause an increase in the absorption of Raltegravir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Rabeprazole Rabeprazole can cause an increase in the absorption of Raltegravir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Dexlansoprazole Dexlansoprazole can cause an increase in the absorption of Raltegravir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Dexrabeprazole Dexrabeprazole can cause an increase in the absorption of Raltegravir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Ilaprazole Ilaprazole can cause an increase in the absorption of Raltegravir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Vonoprazan Vonoprazan can cause an increase in the absorption of Raltegravir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Rifabutin The serum concentration of Raltegravir can be decreased when it is combined with Rifabutin.
Sucralfate Sucralfate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bentoquatam Bentoquatam can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium sulfate Magnesium sulfate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium salicylate Magnesium salicylate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Kaolin Kaolin can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc Zinc can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc trihydroxide Zinc trihydroxide can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc Substituted Heme C Zinc Substituted Heme C can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Potassium alum Potassium alum can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Polaprezinc Polaprezinc can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc oxide Zinc oxide can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc sulfate Zinc sulfate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium chloride Magnesium chloride can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminum chloride Aluminum chloride can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium citrate Magnesium citrate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc citrate Zinc citrate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc picolinate Zinc picolinate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminum sulfate Aluminum sulfate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc gluconate Zinc gluconate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bentonite Bentonite can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium aspartate Magnesium aspartate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Montmorillonite Montmorillonite can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium gluconate Magnesium gluconate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium orotate Magnesium orotate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Acetylcysteine zinc Acetylcysteine zinc can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc ascorbate Zinc ascorbate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc acetate Zinc acetate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc glycinate Zinc glycinate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium Magnesium can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium levulinate Magnesium levulinate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium lactate Magnesium lactate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc chloride Zinc chloride can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc sulfate, unspecified form Zinc sulfate, unspecified form can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc cation Zinc cation can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Nelfinavir The metabolism of Raltegravir can be increased when combined with Nelfinavir.
Phenytoin The metabolism of Raltegravir can be increased when combined with Phenytoin.
Desogestrel The metabolism of Raltegravir can be increased when combined with Desogestrel.
Zidovudine The metabolism of Raltegravir can be increased when combined with Zidovudine.
Ritonavir The metabolism of Raltegravir can be increased when combined with Ritonavir.
Lamotrigine The metabolism of Raltegravir can be increased when combined with Lamotrigine.
Carbamazepine The metabolism of Raltegravir can be increased when combined with Carbamazepine.
Efavirenz The metabolism of Raltegravir can be increased when combined with Efavirenz.
Primidone The metabolism of Raltegravir can be increased when combined with Primidone.
Tipranavir The metabolism of Raltegravir can be increased when combined with Tipranavir.
Ethinylestradiol The metabolism of Raltegravir can be increased when combined with Ethinylestradiol.
Phenobarbital The metabolism of Raltegravir can be increased when combined with Phenobarbital.
Testosterone propionate The metabolism of Raltegravir can be increased when combined with Testosterone propionate.
Rifampin The serum concentration of Raltegravir can be decreased when it is combined with Rifampicin.
Amprenavir The serum concentration of Raltegravir can be decreased when it is combined with Amprenavir.
Fosamprenavir The serum concentration of Raltegravir can be decreased when it is combined with Fosamprenavir.
Magnesium oxide Magnesium oxide can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sodium bicarbonate The serum concentration of Raltegravir can be decreased when it is combined with Sodium bicarbonate.
Aluminum hydroxide Aluminum hydroxide can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium carbonate The serum concentration of Raltegravir can be decreased when it is combined with Calcium carbonate.
Magaldrate Magaldrate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium hydroxide Magnesium hydroxide can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium trisilicate Magnesium trisilicate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium carbonate Magnesium carbonate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bismuth subnitrate The serum concentration of Raltegravir can be decreased when it is combined with Bismuth subnitrate.
Magnesium silicate Magnesium silicate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium acetoacetate Aluminium acetoacetate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Hydrotalcite Hydrotalcite can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium peroxide Magnesium peroxide can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Almasilate The serum concentration of Raltegravir can be decreased when it is combined with Almasilate.
Aluminium glycinate Aluminium glycinate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aloglutamol Aloglutamol can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium silicate The serum concentration of Raltegravir can be decreased when it is combined with Calcium silicate.
Aluminium phosphate Aluminium phosphate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Leuprolide The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Leuprolide is combined with Raltegravir.
Somatotropin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Somatotropin is combined with Raltegravir.
Infliximab The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Infliximab is combined with Raltegravir.
Daptomycin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Daptomycin is combined with Raltegravir.
Cyclosporine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Cyclosporine is combined with Raltegravir.
Baclofen The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Baclofen is combined with Raltegravir.
Sildenafil The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Sildenafil is combined with Raltegravir.
Cladribine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Cladribine is combined with Raltegravir.
Pamidronic acid The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Pamidronic acid is combined with Raltegravir.
Mefloquine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Mefloquine is combined with Raltegravir.
Tacrine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Tacrine is combined with Raltegravir.
Carbimazole The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Carbimazole is combined with Raltegravir.
Trimethoprim The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Trimethoprim is combined with Raltegravir.

Target Protein

Gag-Pol polyprotein gag-pol
Integrase pol

Referensi & Sumber

Artikel (PubMed)
  • PMID: 24145879
    Nachman S, Zheng N, Acosta EP, Teppler H, Homony B, Graham B, Fenton T, Xu X, Wenning L, Spector SA, Frenkel LM, Alvero C, Worrell C, Handelsman E, Wiznia A: Pharmacokinetics, safety, and 48-week efficacy of oral raltegravir in HIV-1-infected children aged 2 through 18 years. Clin Infect Dis. 2014 Feb;58(3):413-22. doi: 10.1093/cid/cit696. Epub 2013 Oct 21.
  • PMID: 23856784
    Barau C, Furlan V, Yazdanpanah Y, Fagard C, Molina JM, Taburet AM, Barrail-Tran A: Characterization of binding of raltegravir to plasma proteins. Antimicrob Agents Chemother. 2013 Oct;57(10):5147-50. doi: 10.1128/AAC.00625-13. Epub 2013 Jul 15.
  • PMID: 23836466
    Arora R, de Beauchene IC, Polanski J, Laine E, Tchertanov L: Raltegravir flexibility and its impact on recognition by the HIV-1 IN targets. J Mol Recognit. 2013 Sep;26(9):383-401. doi: 10.1002/jmr.2277.
  • PMID: 23664333
    Eron JJ, Cooper DA, Steigbigel RT, Clotet B, Gatell JM, Kumar PN, Rockstroh JK, Schechter M, Markowitz M, Yeni P, Loutfy MR, Lazzarin A, Lennox JL, Strohmaier KM, Wan H, Barnard RJ, Nguyen BY, Teppler H: Efficacy and safety of raltegravir for treatment of HIV for 5 years in the BENCHMRK studies: final results of two randomised, placebo-controlled trials. Lancet Infect Dis. 2013 Jul;13(7):587-96. doi: 10.1016/S1473-3099(13)70093-8. Epub 2013 May 7.
  • PMID: 16863445
    Winston A, Mallon PW, Boffito M: The clinical pharmacology of antiretrovirals in development. Expert Opin Drug Metab Toxicol. 2006 Jun;2(3):447-58.
  • PMID: 17019786
    O'Neal R: MK-0518 and GS-9137: two promising integrase inhibitors in the pipeline. BETA. 2006 Summer;18(4):13-6.
  • PMID: 17096488
    James JS: Integrase inhibitor MK-0518: Merck opens expanded-access program. AIDS Treat News. 2006 Jul-Sep;(419):5.
  • PMID: 17133211
    Markowitz M, Morales-Ramirez JO, Nguyen BY, Kovacs CM, Steigbigel RT, Cooper DA, Liporace R, Schwartz R, Isaacs R, Gilde LR, Wenning L, Zhao J, Teppler H: Antiretroviral activity, pharmacokinetics, and tolerability of MK-0518, a novel inhibitor of HIV-1 integrase, dosed as monotherapy for 10 days in treatment-naive HIV-1-infected individuals. J Acquir Immune Defic Syndr. 2006 Dec 15;43(5):509-15.
Menampilkan 8 dari 13 artikel.

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