Comparative Pharmacology
Head-to-head clinical analysis: NALOXEGOL versus NALOXONE HYDROCHLORIDE AUTOINJECTOR.
Peer-Reviewed Evidence
Head-to-head clinical analysis: NALOXEGOL versus NALOXONE HYDROCHLORIDE AUTOINJECTOR.
NALOXEGOL vs NALOXONE HYDROCHLORIDE (AUTOINJECTOR)
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.
Initial: 0.4 mg or 2 mg intramuscularly (IM) or subcutaneously (SC); may repeat every 2-3 minutes as needed. For autoinjector: 2 mg single dose, administer IM or SC into anterolateral thigh; may repeat every 2-3 minutes with a new device if no response. Max total dose: 10 mg.
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 approximately 1 to 1.5 hours in adults. In neonates, half-life is prolonged (about 3 hours). Clinical context: due to short half-life, repeated doses or continuous infusion may be needed for opioid overdose with long-acting opioids.
Primarily fecal (approximately 66%) and renal (approximately 33%) as unchanged drug; <1% as metabolites.
Primarily hepatic metabolism (glucuronidation) followed by renal excretion of metabolites. Less than 1% excreted unchanged in urine. Fecal excretion minimal (<5%).
Category C
Category A/B
Opioid Antagonist
Opioid Antagonist
"The serum concentration of Hydrocortisone can be increased when it is combined with Naloxegol."