Comparative Pharmacology
Head-to-head clinical analysis: NALOXEGOL versus NARCAN.
Peer-Reviewed Evidence
Head-to-head clinical analysis: NALOXEGOL versus NARCAN.
NALOXEGOL vs NARCAN
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Naloxegol is a PEGylated derivative of naloxone, a mu-opioid receptor antagonist. As a peripherally acting mu-opioid receptor antagonist (PAMORA), it binds to and inhibits mu-opioid receptors in the gastrointestinal tract, reducing opioid-induced constipation without crossing the blood-brain barrier to affect central analgesia.
Opioid receptor antagonist; binds competitively to mu, kappa, and delta opioid receptors, reversing opioid effects.
25 mg orally once daily in the morning, with or without food; may increase to 50 mg once daily if tolerated and needed.
Initial dose: 0.4 mg to 2 mg IV, IM, or SC, repeated every 2 to 3 minutes as needed. For opioid-induced respiratory depression, may use 0.1 to 0.2 mg IV increments in patients with opioid dependence to avoid withdrawal.
None Documented
None Documented
Clinical Note
moderateNaloxegol + Digoxin
"The serum concentration of Digoxin can be increased when it is combined with Naloxegol."
Clinical Note
moderateNaloxegol + Levofloxacin
"The serum concentration of Levofloxacin can be increased when it is combined with Naloxegol."
Clinical Note
moderateNaloxegol + Prednisone
"The serum concentration of Prednisone can be increased when it is combined with Naloxegol."
Clinical Note
moderateNaloxegol + Hydrocortisone
Terminal elimination half-life is approximately 11-13 hours in patients with normal renal function; may be prolonged in severe renal impairment.
Approximately 1 hour in adults; context: shorter than most opioids (e.g., morphine 2-4 h), necessitating repeated doses for prolonged opioid effects.
Primarily fecal (approximately 66%) and renal (approximately 33%) as unchanged drug; <1% as metabolites.
Primarily hepatic metabolism (glucuronidation) followed by renal excretion of metabolites; <5% excreted unchanged in urine.
Category C
Category C
Opioid Antagonist
Opioid Antagonist
"The serum concentration of Hydrocortisone can be increased when it is combined with Naloxegol."