Comparative Pharmacology
Head-to-head clinical analysis: NALOXEGOL versus NALTREXONE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: NALOXEGOL versus NALTREXONE.
NALOXEGOL vs NALTREXONE
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.
Naltrexone is a pure opioid antagonist that competitively binds to μ-opioid receptors, blocking the effects of endogenous and exogenous opioids. It also antagonizes κ- and δ-opioid receptors to a lesser extent.
25 mg orally once daily in the morning, with or without food; may increase to 50 mg once daily if tolerated and needed.
Oral: 50 mg once daily for opioid dependence; 25 mg initially for first dose to minimize adverse effects. Intramuscular: 380 mg every 4 weeks for alcohol dependence.
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.
Naltrexone: 3.9–10.3 hours; active metabolite 6β-naltrexol: 12.9 hours. Context: Trough levels of 6β-naltrexol sustain receptor blockade for 24–48 h.
Primarily fecal (approximately 66%) and renal (approximately 33%) as unchanged drug; <1% as metabolites.
Primarily renal (60% as metabolites, including 6β-naltrexol; <2% unchanged) and biliary/fecal (30%).
Category C
Category A/B
Opioid Antagonist
Opioid Antagonist
"The serum concentration of Hydrocortisone can be increased when it is combined with Naloxegol."