Peringatan Keamanan

In the event of an overdose, contact a poison control centre.L7069 Patients should be treated with symptomatic and supportive measures, including monitoring of the QT interval.L7069 Dialysis is not expected to remove significant amounts of the drug from plasma as it is highly bound to albumin.L7069

Rilpivirine

DB08864

small molecule approved

Deskripsi

Rilpivirine is non-nucleoside reverse transcriptase inhibitor (NNRTI) which is used for the treatment of HIV-1 infections in treatment-naive patients.A31328 It is a diarylpyrimidine derivative.A31329 The internal conformational flexibility of rilpivirine and the plasticity of it interacting binding site gives it a very high potency and reduces the chance of resistance compared to other NNRTI's.A31331 Rilpivirine was developed by Tilbotec, Inc. and FDA approved on May 20, 2011.L1030 On November 21, 2017, Rilpivirine, in combination with dolutegravir, was approved as part of the first complete treatment regimen with only two drugs for the treatment of adults with HIV-1 named Juluca.L1031 Rilpivirine in combination with cabotegravir was granted FDA approval on 21 January 2021.L31193 While previously administered once-monthly only, this combination product was granted FDA approval for dosing every two months on February 01, 2022 L40084 and without the need for an oral lead-in period prior.L31193

Struktur Molekul 2D

Berat 366.4185
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Rilpivirine has a terminal half-life of 34-55 hours.[A31331]
Volume Distribusi In HIV-1 patients, the apparent volume of distribution in the central compartment was 152-173 L.[L1032]
Klirens (Clearance) In HIV-1 patients, the apparent total clearance is estimated to be 6.89-8.66 L/h.[L1032]

Absorpsi

Rilpivirine has a Tmax of 3-4 hours and has a mean AUC of 2235 ± 851 ng\*h/mL.A31331,L7069 A 25mg dose reaches a Cmax of 247 ng/mL in healthy subjects and 138.6 ng/mL in patients with HIV-1.L1032

Metabolisme

Rilpivirine is predominantly metabolized by CYP3A4 and CYP3A5 to the hydroxylated metabolites M1, M2, M3, and M4.A31336,L7069 UGT1A1 glucuronidates the M2 metabolite to form M6, UGT1A4 glucuronidates rilpivirine to form M5, and an unknown UGT glucuronidates the M4 metabolite to form M7.A31336

Rute Eliminasi

Rilpivirine is 85% eliminated in the feces and 6.1% eliminated in the urine.L7069 25% of a dose is recovered in the feces as the unchanged parent drug, while <1% of a dose is recovered in the urine as the unchanged parent drug.L7069

Interaksi Makanan

2 Data
  • 1. Avoid St. John's Wort. St.John's Wort will decrease levels of this medication.
  • 2. Take with food. Absorption is increased by 40% if taken with food.

Interaksi Obat

1131 Data
Lomitapide The metabolism of Lomitapide can be decreased when combined with Rilpivirine.
Dabrafenib The serum concentration of Rilpivirine can be decreased when it is combined with Dabrafenib.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Rilpivirine.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Rilpivirine.
Erythromycin The serum concentration of Rilpivirine can be increased when it is combined with Erythromycin.
Telithromycin The serum concentration of Rilpivirine can be increased when it is combined with Telithromycin.
Clarithromycin The serum concentration of Rilpivirine can be increased when it is combined with Clarithromycin.
Troleandomycin The serum concentration of Rilpivirine can be increased when it is combined with Troleandomycin.
Omeprazole Omeprazole can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lansoprazole Lansoprazole can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Esomeprazole Esomeprazole can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Rabeprazole Rabeprazole can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dexlansoprazole The serum concentration of Rilpivirine can be decreased when it is combined with Dexlansoprazole.
Dexrabeprazole Dexrabeprazole can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ilaprazole Ilaprazole can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Luliconazole The serum concentration of Rilpivirine can be increased when it is combined with Luliconazole.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Rilpivirine.
Colchicine The metabolism of Colchicine can be decreased when combined with Rilpivirine.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Rilpivirine.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Rilpivirine.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Rilpivirine.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Rilpivirine.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Rilpivirine.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Rilpivirine.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Rilpivirine.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Rilpivirine.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Rilpivirine.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Rilpivirine.
Olanzapine Olanzapine can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cimetidine Cimetidine can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Nizatidine Nizatidine can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ranitidine Ranitidine can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Famotidine Famotidine can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methantheline Methantheline can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Promethazine Promethazine can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Doxepin Doxepin can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Asenapine Asenapine can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Metiamide Metiamide can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Roxatidine acetate Roxatidine acetate can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lafutidine Lafutidine can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lavoltidine Lavoltidine can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Niperotidine Niperotidine can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Epinastine Epinastine can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Rilpivirine.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Rilpivirine.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Rilpivirine.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Rilpivirine.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Rilpivirine.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Rilpivirine.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Rilpivirine.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Rilpivirine.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Rilpivirine.
Lumacaftor The serum concentration of Rilpivirine can be decreased when it is combined with Lumacaftor.
Goserelin The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Goserelin.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Moxifloxacin.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Sulfisoxazole.
Sulpiride The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Sulpiride.
Droperidol The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Droperidol.
Perflutren The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Perflutren.
Atropine The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Atropine.
Adenosine The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Adenosine.
Pentamidine The metabolism of Pentamidine can be decreased when combined with Rilpivirine.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Gadobenic acid.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Nalidixic acid.
Cinoxacin The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Cinoxacin.
Levosimendan The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Levosimendan.
Mesoridazine The metabolism of Mesoridazine can be decreased when combined with Rilpivirine.
Desloratadine The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Desloratadine.
Lomefloxacin The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Lomefloxacin.
Dimenhydrinate The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Dimenhydrinate.
Papaverine The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Papaverine.
Gemifloxacin The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Gemifloxacin.
Ofloxacin The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Ofloxacin.
Probucol The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Probucol.
Aceprometazine The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Aceprometazine.
Terlipressin The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Terlipressin.
Azimilide The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Azimilide.
Pracinostat The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Pracinostat.
Technetium Tc-99m ciprofloxacin The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Technetium Tc-99m ciprofloxacin.
Garenoxacin The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Garenoxacin.
Tedisamil The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Tedisamil.
Tucidinostat The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Tucidinostat.
Telavancin The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Telavancin.
Nemonoxacin The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Nemonoxacin.
Antazoline The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Antazoline.
Butriptyline The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Butriptyline.
Melperone The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Melperone.
Amifampridine The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Amifampridine.
Mocetinostat The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Mocetinostat.
Entinostat The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Entinostat.
CUDC-101 The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with CUDC-101.
Simendan The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Simendan.
Ricolinostat The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Ricolinostat.
Mizolastine The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Mizolastine.
Abexinostat The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Abexinostat.
Oxatomide The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Oxatomide.
Sitafloxacin The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Sitafloxacin.
Sultopride The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Sultopride.
Nizofenone The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Nizofenone.
Bunaftine The risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Bunaftine.

Target Protein

Reverse transcriptase/RNaseH pol
Sodium channel protein type 10 subunit alpha SCN10A
Gag-Pol polyprotein gag-pol
Nuclear receptor subfamily 1 group I member 2 NR1I2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 24068877
    Putcharoen O, Kerr SJ, Ruxrungtham K: An update on clinical utility of rilpivirine in the management of HIV infection in treatment-naive patients. HIV AIDS (Auckl). 2013 Sep 16;5:231-41. doi: 10.2147/HIV.S25712.
  • PMID: 24008177
    Usach I, Melis V, Peris JE: Non-nucleoside reverse transcriptase inhibitors: a review on pharmacokinetics, pharmacodynamics, safety and tolerability. J Int AIDS Soc. 2013 Sep 4;16:1-14. doi: 10.7448/IAS.16.1.18567.
  • PMID: 22096405
    Ford N, Lee J, Andrieux-Meyer I, Calmy A: Safety, efficacy, and pharmacokinetics of rilpivirine: systematic review with an emphasis on resource-limited settings. HIV AIDS (Auckl). 2011;3:35-44. doi: 10.2147/HIV.S14559. Epub 2011 Apr 28.
  • PMID: 19933797
    Azijn H, Tirry I, Vingerhoets J, de Bethune MP, Kraus G, Boven K, Jochmans D, Van Craenenbroeck E, Picchio G, Rimsky LT: TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. Antimicrob Agents Chemother. 2010 Feb;54(2):718-27. doi: 10.1128/AAC.00986-09. Epub 2009 Nov 23.
  • PMID: 23917319
    Lade JM, Avery LB, Bumpus NN: Human biotransformation of the nonnucleoside reverse transcriptase inhibitor rilpivirine and a cross-species metabolism comparison. Antimicrob Agents Chemother. 2013 Oct;57(10):5067-79. doi: 10.1128/AAC.01401-13. Epub 2013 Aug 5.

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