Peringatan Keamanan

The most common adverse effects of naldemedine are abdominal pain (11%), diarrhea (7%), nausea (6%), vomiting (3%), and gastroenteritis (3%) FDA Label.

Naldemedine

DB11691

small molecule approved investigational

Deskripsi

Naldemedine is an opioid receptor antagonist FDA Label. It is a modified form of DB00704 to which a side chain has been added to increase molecular weight and polar surface area resulting in restricted transport across the blood brain barrier. Naldemedine was approved in 2017 in both the US and Japan for the treatment of Opioid-induced Constipation.

Struktur Molekul 2D

Berat 570.646
Wujud -

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 is 11 h [FDA Label].
Volume Distribusi The apparent volume of disribution during the terminal phase is 155 L [FDA Label]
Klirens (Clearance) -

Absorpsi

Tmax is 0.75 h FDA Label. Administration with a high-fat meal reduces Cmax by 35% and increases Tmax to 2.5 h.

Metabolisme

Naldemedine is mainly metabolized to nor-naldemedine by CYP3A FDA Label. Some metabolism to naldemedine-3-glucuronide occurs via UGT1A3. Both metabolites are acitive but less potent than naldemedine. The relative exposures of these metabolites are 9-13% and <3% for nor-naldemedine and naldemedine-3-glucuronide respectively. Naldemedine is also cleaved in the intestine to form benzamidine and naldemedine carboxylic acid.

Rute Eliminasi

57% of naldemedine is excreted in the urine with 16-18% as the parent compound and 35% is excreted in the feces FDA Label.

Interaksi Makanan

2 Data
  • 1. Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of naldemedine.
  • 2. Take with or without food.

Interaksi Obat

778 Data
Methylnaltrexone Naldemedine may increase the opioid antagonism activities of Methylnaltrexone.
Naloxegol Naldemedine may increase the opioid antagonism activities of Naloxegol.
Cyclosporine Cyclosporine may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Methotrexate Methotrexate may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cephalexin Cephalexin may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Meloxicam Meloxicam may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Carprofen Carprofen may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Tacrolimus Tacrolimus may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Ibuprofen Ibuprofen may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Atazanavir Atazanavir may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefoperazone Cefoperazone may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefotetan Cefotetan may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefoxitin Cefoxitin may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Ceftizoxime Ceftizoxime may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefradine Cefradine may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Magnesium salicylate Magnesium salicylate may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Salsalate Salsalate may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Choline magnesium trisalicylate Choline magnesium trisalicylate may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefepime Cefepime may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefacetrile Cefacetrile may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Ceftibuten Ceftibuten may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cefpodoxime Cefpodoxime may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Antrafenine Antrafenine may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Aminophenazone Aminophenazone may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Antipyrine Antipyrine may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Tiaprofenic acid Tiaprofenic acid may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Lopinavir Lopinavir may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Etoricoxib Etoricoxib may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Hydrolyzed Cephalothin Hydrolyzed Cephalothin may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cephalothin Group Cephalothin Group may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Oxyphenbutazone Oxyphenbutazone may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Latamoxef Latamoxef may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Nimesulide Nimesulide may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Benoxaprofen Benoxaprofen may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Metamizole Metamizole may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Zomepirac Zomepirac may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Ceftobiprole Ceftobiprole may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Cimicoxib Cimicoxib may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Ceftaroline fosamil Ceftaroline fosamil may decrease the excretion rate of Naldemedine which could result in a higher serum level.

Target Protein

Mu-type opioid receptor OPRM1
Delta-type opioid receptor OPRD1
Kappa-type opioid receptor OPRK1

Referensi & Sumber

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