Description

Simple

A medication used to treat constipation caused by narcotic painkillers.

Clinical

A peripherally-selective opioid antagonist used to treat opioid-induced constipation (OIC) in adult patients with chronic non-cancer pain.

Overview

Naloxegol, for "PEGylated naloxol" is a peripherally-selective opioid antagonist developed by AstraZeneca. It was approved by the FDA in September 2014 and is indicated for the treatment of opioid-induced constipation (OIC) in adult patients with chronic non‑cancer pain. The advantage of naloxegol over the opioid antagonist naloxone is that its PEGylated structure allows for high selectivity for peripheral opioid receptors and lack of entry into the central nervous system through the blood-brain barrier.

Pharmacology

Indication

Indicated for the treatment of opioid-induced constipation (OIC) in adult patients with chronic non-cancer pain.

Pharmacodynamic

Use of opioids induces slowing of gastrointestinal motility and transit. Patients do not develop tolerance to these effects, unlike many other opioid side effects. Naloxegol antagonizes mu, delta, and kappa opioid receptors, having the highest affinity for mu. Antagonism of gastrointestinal mu-opioi... Read more

Mechanism of action

Naloxegol is an antagonist of opioid binding at the mu-opioid receptor. When administered at the recommended dose levels, naloxegol functions as a peripherally-acting mu-opioid receptor antagonist in tissues such as the gastrointestinal tract, thereby decreasing the constipating effects of opioids.... Read more

Absorption

Following oral administration, naloxegol is absorbed with peak concentrations (Cmax) achieved in less than 2 hours.

Protein binding

~4.2%

Volume of distribution

968 to 2140 L.

Clearance

Feces (68%), urine (16%).

Half life

6-11 hours.

Route of elimination

Feces: 68% after oral administration.
Urine: 16% after oral administration.

Toxicity

Information currently not available.

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Gastrointestinal obstruction
      • Drugbank Id: DBCOND0010786
  • Regions: US
  • With Categories Coadmin:
      • Name: Cytochrome P-450 CYP3A4 Inhibitors
      • Drugbank Id: DBCAT003232
      • Mesh Id: D065692

Food Interactions

  • Take on an empty stomach. High-fat food increases drug absorption. Take naloxegol at least 1 hour prior to the first meal of the day or 2 hours after the meal.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The metabolism of (R)-warfarin can be decreased when combined with Naloxegol.
(S)-Warfarin
The metabolism of (S)-Warfarin can be decreased when combined with Naloxegol.
4-Methoxyamphetamine
The metabolism of 4-Methoxyamphetamine can be decreased when combined with Naloxegol.
5-methoxy-N,N-dimethyltryptamine
The metabolism of 5-methoxy-N,N-dimethyltryptamine can be decreased when combined with Naloxegol.
6-Deoxyerythronolide B
The metabolism of Naloxegol can be decreased when combined with 6-Deoxyerythronolide B.
7-ethyl-10-hydroxycamptothecin
The metabolism of Naloxegol can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
9-aminocamptothecin
The metabolism of Naloxegol can be decreased when combined with 9-aminocamptothecin.
Abatacept
The metabolism of Naloxegol can be increased when combined with Abatacept.
Abemaciclib
The serum concentration of Naloxegol can be increased when it is combined with Abemaciclib.
Acalabrutinib
The metabolism of Naloxegol can be decreased when combined with Acalabrutinib.
Acebutolol
The metabolism of Acebutolol can be decreased when combined with Naloxegol.
Acenocoumarol
The metabolism of Acenocoumarol can be decreased when combined with Naloxegol.
Acetaminophen
The serum concentration of Naloxegol can be increased when it is combined with Acetaminophen.
Acetazolamide
The metabolism of Naloxegol can be decreased when combined with Acetazolamide.
Adalimumab
The metabolism of Naloxegol can be increased when combined with Adalimumab.
Afatinib
The serum concentration of Naloxegol can be increased when it is combined with Afatinib.
Afelimomab
The metabolism of Naloxegol can be increased when combined with Afelimomab.
Albendazole
The serum concentration of Naloxegol can be increased when it is combined with Albendazole.
Aldesleukin
The metabolism of Naloxegol can be decreased when combined with Aldesleukin.
Alectinib
The serum concentration of Naloxegol can be increased when it is combined with Alectinib.
3 References
  1. 1 . Leonard J, Baker DE: Naloxegol: treatment for opioid-induced constipation in chronic non-cancer pain. Ann Pharmacother. 2015 Mar;49(3):360-5. doi: 10.1177/1060028014560191. Epub 2014 Dec 3.PubMed: 25471070
  2. 2 . Anantharamu T, Sharma S, Gupta AK, Dahiya N, Singh Brashier DB, Sharma AK: Naloxegol: First oral peripherally acting mu opioid receptor antagonists for opioid-induced constipation. J Pharmacol Pharmacother. 2015 Jul-Sep;6(3):188-92. doi: 10.4103/0976-500X.162015.PubMed: 26312011
  3. 3 . Jones R, Prommer E, Backstedt D: Naloxegol: A Novel Therapy in the Management of Opioid-Induced Constipation. Am J Hosp Palliat Care. 2015 Jul 6. pii: 1049909115593937.PubMed: 26150678