Action and Spectrum

Actions and Spectrum:

naloxegol works by blocking the mu-opioid receptors in the digestive system, which oversee sluggish bowel motions and constipation. naloxegol can improve bowel motility and encourage more frequent bowel motions by inhibiting these receptors.

The range of diseases or symptoms that the medication is successful in addressing is referred to as the naloxegol spectrum. In this situation, the treatment of opioid-induced constipation in people with advanced disease or persistent non-cancer pain who regularly take opioid pain drugs is especially approved for naloxegol.

Drug Interaction

Adverse Reaction

Frequency defined

1-10%

Diarrhea (6-9%)

Vomiting (3-5%)

headache (4%)

Opioid withdrawal (1-3%)

Hyperhidrosis (<1-3%)

Flatulence (3-6%)

Nausea (7-8%)

Post marketing reports

Angioedema, urticaria and rash

Gastrointestinal perforation

Severe abdominal pain and diarrhea

>10%

Abdominal pain (12-21%)

GI effects

12.5 mg/day of naloxegol: 39% (methadone) against 26% (other opioid)

25 mg/day of naloxegol: 75% (methadone) against 34% (other opioid)

Black Box Warning

Black Box Warning

naloxegol should only be used in people with opioid-induced constipation who have not responded to other laxatives, according to the black box warning, as it might produce severe opioid withdrawal symptoms if used in those who are physically dependent on opioids. naloxegol should not be administered to people who need to take opioid painkillers for cancer-related, postoperative, or acute pain.

Additionally, the warning mentions that there have been cases of severe gastrointestinal perforation in patients taking naloxegol, particularly in those who have a history of bowel obstruction, inflammatory bowel disease, or other conditions that may raise the risk of gastrointestinal perforation.

Contraindication / Caution

Contraindication/Caution:

Contraindication:

• history of hypersensitivity to naloxegol or any of the formulation’s constituents
• Bowel blockage or a history of bowel obstruction in the gastrointestinal tract
• gastrointestinal perforation that is present, suspected, or has a history of perforation

Caution:

• Patients who have a history of cardiovascular illness, such as heart failure, bradycardia, or conduction problems, should use this medication with caution.
• Use with care in individuals receiving pharmaceuticals such some antiarrhythmic meds or antipsychotic medications that lengthen the QT interval.

Patients having a history of seizures or ailments that might reduce the seizure threshold should use with caution.

Pregnancy / Lactation

Pregnancy warnings:   

Pregnancy category: N/A

Lactation: Excretion into human milk is unknown

Pregnancy Categories:     

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology

As a peripherally acting mu-opioid receptor antagonist, naloxegol lowers the constipating effects of opioids without impairing their analgesic characteristics by specifically inhibiting the mu-opioid receptors in the gastrointestinal tract.

Pharmacodynamics

naloxegol is a peripherally acting mu-opioid receptor antagonist, which implies that it has no effect on the analgesic abilities of opioids in the central nervous system since it does not pass the blood-brain barrier.

naloxegol can improve bowel motility and encourage more frequent bowel motions by inhibiting these receptors.

Pharmacokinetics

Absorption

After oral treatment, naloxegol is quickly absorbed, reaching its peak plasma concentrations in one to two hours. The medication must be taken on an empty stomach at least one hour before the first meal of the day.

Distribution

At therapeutic dosages, naloxegol is strongly bound to plasma proteins roughly 97% bound. naloxegol is widely dispersed throughout the body since its volume of distribution is around 1600 liters.

Metabolism

The liver metabolizes naloxegol largely through the cytochrome P450 3A4 (CYP3A4) enzyme system. naloxegol’s two main metabolites are M5 (produced by hydrolysis) and M3. (produced by oxidative metabolism). The metabolites are quickly excreted from the body and have less potency than the original molecule.

Elimination and excretion

Only a tiny portion of naloxegol and its metabolites are excreted in the urine, with the majority being removed through the feces. naloxegol has a half-life of around 11 hours, and a once daily dosage takes 3 to 4 days to reach steady-state concentrations.

Adminstartion

Administration:

One dose of the prescription drug naloxegol should be taken orally each day. 25 mg once day, given on an empty stomach at least one hour before the first meal of the day, is the suggested starting dose.

naloxegol should not be chewed, crushed, or broken; it should be eaten whole. For constant blood levels of the medication throughout the day, it should be given at the same time each day.

Patient Information Leaflet

Patient information leaflet

Generic Name: naloxegol

Why do we use naloxegol?

naloxegol is a drug used to treat opioid-induced constipation in adult patients with advanced disease or persistent non-cancer pain who regularly take opioid painkillers.

naloxegol lowers the constipating effects of opioid painkillers without altering their analgesic characteristics by inhibiting the mu-opioid receptors in the gastrointestinal system.