Naloxegol


Description

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 chr...

Read more

Pharmacology

Indication

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

Pharmacodynamic

Use of opioids induces slowing of gastrointestinal motility and transit. Patients do not develop tol... Read more

Mechanism of action

Naloxegol is an antagonist of opioid binding at the mu-opioid receptor. When administered at the rec... Read more

Absorption

Following oral administration, naloxegol is absorbed with peak concentrations (Cmax) achieved in les... Read more

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

Effect Regions Age Groups Incidences Evidence Type
Gastrointestinal reaction US
  • Kind: experimental
    • Percent: 26-34%
  • Kind: comparator
    • Percent: 39-75%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 12-21%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 6-9%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 7-8%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Flatulence US
  • Kind: experimental
    • Percent: 3-6%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 3-5%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Anxiety US
  • Kind: experimental
    • Percent: 1-3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Irritability US
  • Kind: experimental
    • Percent: 1-3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Yawning US
  • Kind: experimental
    • Percent: 1-3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Hyperhidrosis US
  • Kind: experimental
    • Percent: 0-3%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 1-3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 1-3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Hyperhidrosis US
  • Kind: experimental
    • Percent: 1-3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Chills US
  • Kind: experimental
    • Percent: 1-3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Diarrhea US
    Varying Reports
    Severe abdominal pain US
    Varying Reports
    Gastrointestinal Perforation US
    Varying Reports
    Gastrointestinal Perforation US
    Varying Reports
    Gastrointestinal Perforation US
    Varying Reports
    Gastrointestinal Perforation US
    Varying Reports
    Gastrointestinal Perforation US
    Varying Reports

    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

    • A high-fat meal increased the extent and rate of naloxegol absorption. The Cmax and AUC were increased by approximately 30% and 45%, respectively. In clinical trials, naloxegol was dosed on an empty stomach approximately 1 hour prior to the first meal in the morning.

    Interactions

    Type in a drug name to check for interaction with Naloxegol

    The metabolism of Naloxegol can be decreased when combined with (R)-warfarin.
    The metabolism of Naloxegol can be decreased when combined with (S)-Warfarin.
    The metabolism of Naloxegol can be decreased when combined with 3,5-diiodothyropropionic acid.
    The metabolism of Naloxegol can be decreased when combined with 4-hydroxycoumarin.
    The metabolism of 4-Methoxyamphetamine can be decreased when combined with Naloxegol.
    The metabolism of Naloxegol can be decreased when combined with 5-androstenedione.
    The metabolism of 5-methoxy-N,N-dimethyltryptamine can be decreased when combined with Naloxegol.
    The metabolism of Naloxegol can be decreased when combined with 6-Deoxyerythronolide B.
    The metabolism of Naloxegol can be decreased when combined with 6-O-benzylguanine.
    The metabolism of Naloxegol can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    The metabolism of Naloxegol can be decreased when combined with 9-aminocamptothecin.
    The metabolism of Naloxegol can be increased when combined with Abatacept.
    The serum concentration of Naloxegol can be increased when it is combined with Abemaciclib.
    The metabolism of Naloxegol can be decreased when combined with Abiraterone.
    The metabolism of Naloxegol can be decreased when combined with Acalabrutinib.
    The metabolism of Acebutolol can be decreased when combined with Naloxegol.
    The metabolism of Naloxegol can be decreased when combined with Acenocoumarol.
    The serum concentration of Naloxegol can be increased when it is combined with Acetaminophen.
    The metabolism of Naloxegol can be decreased when combined with Acetazolamide.
    The metabolism of Naloxegol can be increased when combined with Adalimumab.

    References

    • 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 . 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 . 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]

    Recent Questions