Naloxegol

Products

Naloxegol is commercially available in the form of film-coated tablets (Moventig, USA: Movantik). It was approved in many countries in 2015.

Structure and properties

Naloxegol (C34H53NO11, Mr = 651.8 g/mol) is a pegylated derivative of naloxone. It exists as naloxegoloxalate, a white powder that is highly soluble in water.

Effects

Naloxegol (ATC A06AH03) is an antagonist at peripheral μ-opioid receptors, which abolishes the effects of opioids in the intestine to counteract constipation. Due to pegylation, it becomes a substrate of P-glycoprotein. Passive diffusion across membranes is reduced and naloxegol does not cross the bloodbrain barrier into the central nervous system. Thus, naloxegol has no effect on the analgesic effects of concomitantly administered opioids. It has a half-life of 6 to 11 hours.

Indications

For the treatment of constipation caused by opioids.

Dosage

According to the prescribing information. Tablets are taken once daily in the morning on an empty stomach at least 30 minutes before or 2 hours after breakfast.

Contraindications

  • Hypersensitivity
  • Intestinal obstruction
  • Combination with strong CYP3A4 inhibitors.

Additional precautions should be observed in cancer patients. Full details can be found in the drug label.

Interactions

Naloxegol is a substrate of CYP3A4. Strong CYP3A4 inhibitors may lead to a relevant increase in bioavailability and are therefore contraindicated.

Adverse effects

The most common potential adverse effects include abdominal pain, diarrhea, nausea, headache, and flatulence.