Brand name: Movantik
Generic: Naloxegol, a PEGylated derivative of naloxone and a substrate for P glycoprotein transporter.
Approval status: approved on 16thSeptember 2014
Indication: opioid induced constipation in adults with chronic non cancer pain.
Mechanism of action: it is a peripherally acting mu- opioid receptor antagonist ( PAMORA). It shows its action in tissues like GIT, thereby decreasing the constipating effects produced by opioids.
Dosage: it is supplied in a form of a tablet for oral administration. The recommended dosage is 25mg once daily in the morning. It is to be taken on an empty stomach at 1 hour prior to the first meal of the day, or 2 hours after taking a meal. The tablet is not to be crushed or chewed, and needs to be swallowed whole.
Precaution: Avoidance of consumption of grapefruit or grapefruit juice during treatment with Movantik.
Metabolism : by CYP3A enzyme system.
Half life: in a pharmacological clinical study, the half life of Naloxegol at therapeutic doses ranged from 6-11 hours.
Excretion: Following oral administration of radio-labelled naloxegol, 68% and 16% of total administered dose were recovered in the feces and urine, respectively
Side effects : abdominal pain, diarrhea, nausea, flatulence, headache, vomiting.
The following drug information is obtained from various medical presentations, journals.