The purpose of this study is to determine the pharmacodynamics (change in minute ventilation) of nalmefene when given as an autoinjector intramuscularly (IM; into the thigh) compared to naloxone when given intranasally (IN; into the nose) to healthy subjects with prior opioid exposure under steady state fentanyl concentrations (opioid agonism).
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
24
Nalmefene Hydrochloride injection 1.5 mg for intramuscular (IM) administration
Naloxone 4 mg for intranasal (IN) administration
Ohio Clinical Trials
Columbus, Ohio, United States
Change in Minute Ventilation 5 Minutes From Opioid Induced Nadir
To assess the change in minute ventilation at 5 minutes of intramuscular nalmefene and intranasal naloxone reversal from the opioid induced nadir.
Time frame: 5 minutes after opioid antagonist administration
Change in Minute Ventilation at 2.5, 5, 10, 15, 20, 30, and 90 Minutes From Opioid Induced Nadir
To assess the time course of changes in minute ventilation of intramuscular nalmefene and intranasal naloxone reversal from the opioid induced nadir.
Time frame: Baseline, 2.5, 5, 10, 15, 20, 30, and 90 minutes after opioid antagonist administration
Maximum Plasma Concentration (Cmax)
Maximum plasma concentration of nalmefene and naloxone.
Time frame: up to 24 hours post-dose
Area Under the Curve (AUC0-2.5)
Area under the plasma concentration-time curve from time zero to 2.5 minutes
Time frame: 2.5 minutes post-dose
Area Under the Curve (AUC0-5)
Area under the plasma concentration-time curve from time zero to 5 minutes
Time frame: 5 minutes post-dose
Area Under the Curve (AUC0-10)
Area under the plasma concentration-time curve from time zero to 10 minutes
Time frame: 10 minutes post-dose
Area Under the Curve (AUC0-15)
Area under the plasma concentration-time curve from time zero to 15 minutes
Time frame: 15 minutes post-dose
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Area Under the Curve (AUC0-20)
Area under the plasma concentration-time curve from time zero to 20 minutes
Time frame: 20 minutes post-dose
Area Under the Curve (AUCt)
Area under the plasma concentration-time curve from time zero to the time of last measurable concentration.
Time frame: up to 24 hours post-dose
Area Under the Curve (AUCinf)
Area under the plasma concentration-time curve from time zero to infinity.
Time frame: up to 24 hours post-dose
Time to Maximum Plasma Concentration (Tmax)
Time to maximum plasma concentration of nalmefene and naloxone.
Time frame: up to 24 hours post-dose
Time to First Measurable Plasma Concentration (Tlag)
Time to first measurable plasma concentration of nalmefene and naloxone.
Time frame: up to 24 hours post-dose
Half-life (T1/2)
Half life of nalmefene and naloxone.
Time frame: up to 24 hours post-dose