Peringatan Keamanan

LD50: 50 mg/kg (primates);
Orthostatic hypotension at plasma levels in excess of 1.400 ng/mL. The most common (>5%) adverse reactions reported with methylnaltrexone bromide are abdominal pain, flatulence, nausea, dizziness, diarrhea and hyperhidrosis.

Methylnaltrexone

DB06800

small molecule approved

Deskripsi

Methylnaltrexone is a pheriphally-acting ?-opioid antagonist that acts on the gastrointestinal tract to decrease opioid-induced constipation without producing analgesic effects or withdrawal symptoms. It is also a weak CYP2D6 inhibitor. FDA approved in 2008.

Struktur Molekul 2D

Berat 356.441
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) terminal: 8.89 ± 2.59 h (intravenous) terminal: 6.14- 8.83 h (subcutaneous)
Volume Distribusi Volume of distribution, steady state = 1.1 L/kg
Klirens (Clearance) 10.5 ± 1.5 ml/min/kg (IV)

Absorpsi

Methylnaltrexone is rapidly absorbed. Tmax (SubQ): 30 minutes (regardless of dose); Cmax, 0.15 mg/kg SubQ dose = 117 ng/mL; AUC24, 0.15 mg/kg SubQ dose = 175 ng·hr/mL;

Metabolisme

60% of the dose is metabolized. Conversion to methyl-6-naltrexol isomers (5% of total dose) and methylnaltrexone sulfate (1.3% of total dose) appear to be the primary pathways of metabolism. N?demethylation of methylnaltrexone to produce naltrexone is not significant.

Rute Eliminasi

Most of the drug is eliminated as unchanged drug (85% of administered radioactivity). Approximately half of the dose is excreted in the urine and somewhat less in feces.

Interaksi Makanan

1 Data
  • 1. Take on an empty stomach. Take methylnaltrexone at least 30 minutes before breakfast.

Interaksi Obat

782 Data
Levallorphan Levallorphan may increase the opioid antagonism activities of Methylnaltrexone.
Butorphanol Butorphanol may increase the opioid antagonism activities of Methylnaltrexone.
Pentazocine Pentazocine may increase the opioid antagonism activities of Methylnaltrexone.
Naltrexone Naltrexone may increase the opioid antagonism activities of Methylnaltrexone.
Nalbuphine Nalbuphine may increase the opioid antagonism activities of Methylnaltrexone.
Buprenorphine Buprenorphine may increase the opioid antagonism activities of Methylnaltrexone.
Naloxone Naloxone may increase the opioid antagonism activities of Methylnaltrexone.
Dezocine Dezocine may increase the opioid antagonism activities of Methylnaltrexone.
Diprenorphine Diprenorphine may increase the opioid antagonism activities of Methylnaltrexone.
Nalmefene Nalmefene may increase the opioid antagonism activities of Methylnaltrexone.
Alvimopan Alvimopan may increase the opioid antagonism activities of Methylnaltrexone.
Naloxegol Naloxegol may increase the opioid antagonism activities of Methylnaltrexone.
Eluxadoline Eluxadoline may increase the opioid antagonism activities of Methylnaltrexone.
Nalorphine Nalorphine may increase the opioid antagonism activities of Methylnaltrexone.
Naldemedine Naldemedine may increase the opioid antagonism activities of Methylnaltrexone.
Axelopran Axelopran may increase the opioid antagonism activities of Methylnaltrexone.
Aticaprant LY-2456302 may increase the opioid antagonism activities of Methylnaltrexone.
Samidorphan Samidorphan may increase the opioid antagonism activities of Methylnaltrexone.
Ondelopran Ondelopran may increase the opioid antagonism activities of Methylnaltrexone.
Meptazinol Meptazinol may increase the opioid antagonism activities of Methylnaltrexone.
Cyclosporine Cyclosporine may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Methotrexate Methotrexate may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cephalexin Cephalexin may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Meloxicam Meloxicam may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Carprofen Carprofen may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Tacrolimus Tacrolimus may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Ibuprofen Ibuprofen may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Atazanavir Atazanavir may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefoperazone Cefoperazone may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefotetan Cefotetan may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefoxitin Cefoxitin may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Ceftizoxime Ceftizoxime may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefradine Cefradine may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Magnesium salicylate Magnesium salicylate may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Salsalate Salsalate may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Choline magnesium trisalicylate Choline magnesium trisalicylate may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefepime Cefepime may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Cefacetrile Cefacetrile may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.
Ceftibuten Ceftibuten may decrease the excretion rate of Methylnaltrexone which could result in a higher serum level.

Target Protein

Mu-type opioid receptor OPRM1
Melanocortin receptor 4 MC4R
Kappa-type opioid receptor OPRK1

Referensi & Sumber

Synthesis reference: Harold Doshan, Julio Perez, "Synthesis of R-N-methylnaltrexone." U.S. Patent US20070099946, issued May 03, 2007.
Artikel (PubMed)
  • PMID: 17981003
    Thomas J: Opioid-induced bowel dysfunction. J Pain Symptom Manage. 2008 Jan;35(1):103-13. Epub 2007 Nov 5.
  • PMID: 21222554
    Rotshteyn Y, Boyd TA, Yuan CS: Methylnaltrexone bromide: research update of pharmacokinetics following parenteral administration. Expert Opin Drug Metab Toxicol. 2011 Feb;7(2):227-35. doi: 10.1517/17425255.2011.549824. Epub 2011 Jan 11.
  • PMID: 20053817
    Chandrasekaran A, Tong Z, Li H, Erve JC, DeMaio W, Goljer I, McConnell O, Rotshteyn Y, Hultin T, Talaat R, Scatina J: Metabolism of intravenous methylnaltrexone in mice, rats, dogs, and humans. Drug Metab Dispos. 2010 Apr;38(4):606-16. doi: 10.1124/dmd.109.031179. Epub 2010 Jan 6.
  • PMID: 21836816
    Bader S, Jaroslawski K, Blum HE, Becker G: Opioid-induced constipation in advanced illness: safety and efficacy of methylnaltrexone bromide. Clin Med Insights Oncol. 2011;5:201-11. doi: 10.4137/CMO.S4867. Epub 2011 Jul 14.

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