Alvimopan

DB06274

small molecule approved investigational

Deskripsi

Alvimopan is a peripherally acting ? opioid antagonist. It is used to avoid postoperative ileus following small or large bowel resection and accelerates the gastrointestinal recovery period.

Struktur Molekul 2D

Berat 424.5326
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 10 to 17 hours (gut metabolite: 10 to 18 hours)
Volume Distribusi * 30±10 L
Klirens (Clearance) * 402 ± 89 mL/min

Absorpsi

Alvimopan's high affinity for the peripheral mu-receptor leads to slower absorption dependent on dissociation from the receptor and subsequently low oral bioavailability of less than 7%.

Metabolisme

Alvimopan is primarily metabolized by intestinal flora to an active metabolite although it has no clinically significant contribution to the effects of the drug.

Rute Eliminasi

Biliary secretion was considered the primary pathway for alvimopan elimination. Unabsorbed drug and unchanged alvimopan resulting from biliary excretion were then hydrolyzed to its ‘metabolite’ by gut microflora. Feces (via biliary excretion) & urine (35%)

Interaksi Makanan

1 Data
  • 1. Take with or without food. High-fat meals may reduce the Cmax and AUC by 38% and 21%, respectively; however, the clinical significance of this is unknown.

Interaksi Obat

54 Data
Tramadol The therapeutic efficacy of Tramadol can be decreased when used in combination with Alvimopan.
Morphine The risk or severity of adverse effects can be increased when Morphine is combined with Alvimopan.
Codeine The risk or severity of adverse effects can be increased when Codeine is combined with Alvimopan.
Hydromorphone The risk or severity of adverse effects can be increased when Hydromorphone is combined with Alvimopan.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Alvimopan.
Meperidine The risk or severity of adverse effects can be increased when Meperidine is combined with Alvimopan.
Oxycodone The therapeutic efficacy of Oxycodone can be decreased when used in combination with Alvimopan.
Butorphanol The risk or severity of adverse effects can be increased when Butorphanol is combined with Alvimopan.
Dextropropoxyphene The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Alvimopan.
Pentazocine The risk or severity of adverse effects can be increased when Pentazocine is combined with Alvimopan.
Naltrexone The risk or severity of adverse effects can be increased when Naltrexone is combined with Alvimopan.
Sufentanil The risk or severity of adverse effects can be increased when Sufentanil is combined with Alvimopan.
Alfentanil The risk or severity of adverse effects can be increased when Alfentanil is combined with Alvimopan.
Fentanyl The risk or severity of adverse effects can be increased when Fentanyl is combined with Alvimopan.
Nalbuphine The risk or severity of adverse effects can be increased when Nalbuphine is combined with Alvimopan.
Levorphanol The risk or severity of adverse effects can be increased when Levorphanol is combined with Alvimopan.
Remifentanil The risk or severity of adverse effects can be increased when Remifentanil is combined with Alvimopan.
Buprenorphine The risk or severity of adverse effects can be increased when Buprenorphine is combined with Alvimopan.
Hydrocodone The risk or severity of adverse effects can be increased when Hydrocodone is combined with Alvimopan.
Diphenoxylate The risk or severity of adverse effects can be increased when Diphenoxylate is combined with Alvimopan.
Oxymorphone The risk or severity of adverse effects can be increased when Oxymorphone is combined with Alvimopan.
Dezocine The risk or severity of adverse effects can be increased when Dezocine is combined with Alvimopan.
Levacetylmethadol The risk or severity of adverse effects can be increased when Levacetylmethadol is combined with Alvimopan.
Methadyl acetate The risk or severity of adverse effects can be increased when Methadyl acetate is combined with Alvimopan.
Dihydroetorphine The risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Alvimopan.
Diamorphine The risk or severity of adverse effects can be increased when Diamorphine is combined with Alvimopan.
Bezitramide The risk or severity of adverse effects can be increased when Bezitramide is combined with Alvimopan.
Ethylmorphine The risk or severity of adverse effects can be increased when Ethylmorphine is combined with Alvimopan.
Etorphine The risk or severity of adverse effects can be increased when Etorphine is combined with Alvimopan.
Dextromoramide The risk or severity of adverse effects can be increased when Dextromoramide is combined with Alvimopan.
Desomorphine The risk or severity of adverse effects can be increased when Desomorphine is combined with Alvimopan.
Carfentanil The risk or severity of adverse effects can be increased when Carfentanil is combined with Alvimopan.
Dihydrocodeine The risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Alvimopan.
Alphacetylmethadol The risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Alvimopan.
Dihydromorphine The risk or severity of adverse effects can be increased when Dihydromorphine is combined with Alvimopan.
Tapentadol The risk or severity of adverse effects can be increased when Tapentadol is combined with Alvimopan.
Ketobemidone The risk or severity of adverse effects can be increased when Ketobemidone is combined with Alvimopan.
DPDPE The risk or severity of adverse effects can be increased when DPDPE is combined with Alvimopan.
Lofentanil The risk or severity of adverse effects can be increased when Lofentanil is combined with Alvimopan.
Eluxadoline The risk or severity of adverse effects can be increased when Eluxadoline is combined with Alvimopan.
Opium The risk or severity of adverse effects can be increased when Opium is combined with Alvimopan.
Normethadone The risk or severity of adverse effects can be increased when Normethadone is combined with Alvimopan.
Piritramide The risk or severity of adverse effects can be increased when Piritramide is combined with Alvimopan.
Alphaprodine The risk or severity of adverse effects can be increased when Alphaprodine is combined with Alvimopan.
Nicomorphine The risk or severity of adverse effects can be increased when Nicomorphine is combined with Alvimopan.
Meptazinol The risk or severity of adverse effects can be increased when Meptazinol is combined with Alvimopan.
Phenoperidine The risk or severity of adverse effects can be increased when Phenoperidine is combined with Alvimopan.
Phenazocine The risk or severity of adverse effects can be increased when Phenazocine is combined with Alvimopan.
Tilidine The risk or severity of adverse effects can be increased when Tilidine is combined with Alvimopan.
Carfentanil, C-11 The risk or severity of adverse effects can be increased when Carfentanil, C-11 is combined with Alvimopan.
Benzhydrocodone The risk or severity of adverse effects can be increased when Benzhydrocodone is combined with Alvimopan.
Oliceridine The risk or severity of adverse effects can be increased when Oliceridine is combined with Alvimopan.
Methylnaltrexone Alvimopan may increase the opioid antagonism activities of Methylnaltrexone.
Naloxegol Alvimopan may increase the opioid antagonism activities of Naloxegol.

Target Protein

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

Referensi & Sumber

Artikel (PubMed)
  • PMID: 23066346
    Wang S, Shah N, Philip J, Caraccio T, Feuerman M, Malone B: Role of alvimopan (entereg) in gastrointestinal recovery and hospital length of stay after bowel resection. P T. 2012 Sep;37(9):518-25.
  • PMID: 19086236
    Buchler MW, Seiler CM, Monson JR, Flamant Y, Thompson-Fawcett MW, Byrne MM, Mortensen ER, Altman JF, Williamson R: Clinical trial: alvimopan for the management of post-operative ileus after abdominal surgery: results of an international randomized, double-blind, multicentre, placebo-controlled clinical study. Aliment Pharmacol Ther. 2008 Aug 1;28(3):312-25.

Contoh Produk & Brand

Produk: 6 • International brands: 0
Produk
  • Alvimopan
    Capsule • 12 mg/1 • Oral • US • Generic • Approved
  • Alvimopan
    Capsule • 12 mg/1 • Oral • US • Generic • Approved
  • Alvimopan
    Capsule • 12 mg/1 • Oral • US • Generic • Approved
  • Alvimopan
    Capsule • 12 mg/1 • Oral • US • Generic • Approved
  • Entereg
    Capsule • 12 mg/1 • Oral • US • Approved
  • Entereg
    Capsule • 12 mg/1 • Oral • US • Approved

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