Comparative Pharmacology
Head-to-head clinical analysis: NALMEFENE HYDROCHLORIDE versus NALOXEGOL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: NALMEFENE HYDROCHLORIDE versus NALOXEGOL.
NALMEFENE HYDROCHLORIDE vs NALOXEGOL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Nalmefene is an opioid receptor antagonist with high affinity for mu, kappa, and delta receptors, and partial agonist activity at kappa receptors.
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.
18 mcg intranasally once, repeated after 2-3 minutes if needed; maximum 2 doses (36 mcg) per episode. Alternatively, 0.5 mg subcutaneously or intramuscularly once, repeated after 2-3 minutes if needed; maximum 1.5 mg per episode.
25 mg orally once daily in the morning, with or without food; may increase to 50 mg once daily if tolerated and needed.
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: ~10.8 hours (range 8–13 hours); clinically supports twice-daily dosing or use in alcohol use disorder
Terminal elimination half-life is approximately 11-13 hours in patients with normal renal function; may be prolonged in severe renal impairment.
Primarily renal (approximately 50% unchanged drug); biliary/fecal excretion accounts for ~20%
Primarily fecal (approximately 66%) and renal (approximately 33%) as unchanged drug; <1% as metabolites.
Category C
Category C
Opioid Antagonist
Opioid Antagonist
"The serum concentration of Hydrocortisone can be increased when it is combined with Naloxegol."