Comparative Pharmacology
Head-to-head clinical analysis: NALOXEGOL versus NALOXONE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: NALOXEGOL versus NALOXONE.
NALOXEGOL vs NALOXONE
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.
Competitive antagonist at 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.
0.4-2 mg IV/IM/SC, may repeat every 2-3 minutes; if no response after 10 mg, reconsider diagnosis.
MODERATE Risk
MODERATE Risk
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.
60-90 minutes in adults; shorter in neonates (3 hours); prolonged in hepatic impairment (up to 2-3 hours).
Primarily fecal (approximately 66%) and renal (approximately 33%) as unchanged drug; <1% as metabolites.
Renal: ~70% as metabolites (naloxone-3-glucuronide, naloxone-3-sulfate) and <2% unchanged; biliary/fecal: ~25% primarily as conjugated metabolites.
Category C
Category A/B
Opioid Antagonist
Opioid Antagonist
"The serum concentration of Hydrocortisone can be increased when it is combined with Naloxegol."