Open AccessComparison of a New Intranasal Naloxone Formulation to Intramuscular Naloxone: Results from Hypothesis‐generating Small Clinical Studies
Author(s) -
Gufford BT,
Ainslie GR,
White JR,
Layton ME,
Padowski JM,
Pollack GM,
Paine MF
Publication year - 2017
Publication title -
clinical and translational science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.303
H-Index - 44
eISSN - 1752-8062
pISSN - 1752-8054
DOI - 10.1111/cts.12473
Subject(s) - (+) naloxone , medicine , pharmacokinetics , bioavailability , opioid , anesthesia , pharmacology , narcotic antagonist , alfentanil , morphine , fentanyl , receptor
Easy‐to‐use naloxone formulations are needed to help address the opioid overdose epidemic. The pharmacokinetics of i.v., i.m., and a new i.n. naloxone formulation (2 mg) were compared in six healthy volunteers. Relative to i.m. naloxone, geometric mean (90% confidence interval [CI]) absolute bioavailability of i.n. naloxone was modestly lower (55%; 90% CI, 43–70% vs. 41%; 90% CI, 27–62%), whereas average (±SE) mean absorption time was substantially shorter (74 ± 8.8 vs. 6.7 ± 4.9 min). The opioid‐attenuating effects of i.n. naloxone were compared with i.m. naloxone (2 mg) after administration of oral alfentanil (4 mg) to a separate group of six healthy volunteers pretreated with 240 mL of water or grapefruit juice. The i.m. and i.n. naloxone attenuated miosis by similar extents after water (40 ± 15 vs. 41 ± 21 h*%) and grapefruit juice (49 ± 18 vs. 50 ± 22 h*%) pretreatment. Results merit further testing of this new naloxone formulation .