Comparison of a New Intranasal Naloxone Formulation to Intramuscular Naloxone: Results from Hypothesis-Generating Small Clinical Studies

Abstract

Easy-to-use naloxone formulations are needed to help address the opioid overdose epidemic. The pharmacokinetics of intravenous, intramuscular, and a new intranasal naloxone formulation (2 mg) were compared in six healthy volunteers. Relative to intramuscular naloxone, geometric mean [90% CI] absolute bioavailability of intranasal naloxone was modestly lower (55 [43-70] versus 41 [27-62] %), whereas average (± SE) mean absorption time was substantially shorter (74 ± 8.8 versus 6.7 ± 4.9 min). The opioid-attenuating effects of intranasal naloxone were compared to intramuscular naloxone (2 mg) after administration of oral alfentanil (4 mg) to a separate group of six healthy volunteers pre-treated with 240 ml of water or grapefruit juice. Intramuscular and intranasal naloxone attenuated miosis by similar extents after water (40 ± 15 versus 41 ± 21 h*%) and grapefruit juice (49 ± 18 versus 50 ± 22 h*%) pre-treatment. Results merit further testing of this new naloxone formulation.

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