Comparative Pharmacology
Head-to-head clinical analysis: NALOXEGOL versus NALOXONE HCL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: NALOXEGOL versus NALOXONE HCL.
NALOXEGOL vs NALOXONE HCL
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-induced respiratory depression and analgesia.
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 mg to 2 mg IV, IM, or subcutaneously, may repeat every 2-3 minutes as needed. For continuous infusion, IV infusion rate of 0.25-6.25 mg/hour.
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.
Terminal elimination half-life is 1.0-1.5 hours in adults. In neonates, half-life is prolonged (3-4 hours) due to immature hepatic function. Clinically, the short half-life necessitates repeated or continuous dosing to reverse opioid effects lasting longer than naloxone's duration.
Primarily fecal (approximately 66%) and renal (approximately 33%) as unchanged drug; <1% as metabolites.
Primarily hepatic metabolism (glucuronidation). Renal excretion accounts for approximately 50% of total clearance, with biliary/fecal elimination contributing 20-30%. Unchanged naloxone in urine is <5%.
Category C
Category A/B
Opioid Antagonist
Opioid Antagonist
"The serum concentration of Hydrocortisone can be increased when it is combined with Naloxegol."