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Pharmacokinetic Evaluation of Intranasal and Intramuscular Naloxone in Healthy Volunteers

Phase 1
Completed
Conditions
Drug Overdose
Opioid-Related Disorders
Interventions
Registration Number
NCT02572089
Lead Sponsor
National Institute on Drug Abuse (NIDA)
Brief Summary

To determine the pharmacokinetics of 4 intranasal doses of naloxone compared to a 0.4 mg dose of naloxone administrated intramuscular and to identify an appropriate intranasal dose that could achieve systemic exposure comparable to an approved parenteral dose. To also determine the pharmacokinetics of two different concentrations of intranasal naloxone and finally, to determine the safety of intranasal naloxone with respect to nasal irritation.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
30
Inclusion Criteria
  • Be able to provide written consent
  • Must have a BMI ranging from 18 to 30kg/m2, inclusive
  • Must have adequate venous access
  • Must not have any clinically significant concurrent medical conditions determine by medical history, physical examination, vital signs, and 12-lead electrocardiogram.
  • Must agree to use a reliable double-barrier method of birth control from the start of screening until one week after completing the study. Oral contraceptives are prohibited.
  • Must agree to not ingest alcohol, drinks containing xanthine greater than 500 mg/day (e.g., Coca Cola, coffee, tea, etc.), or grapefruit/grapefruit juice or participate in strenuous exercise 72 hours prior to admission through the last blood draw of the study.
Exclusion Criteria
  • Please contact clinical site directly for more information

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
2mg Intranasal NaloxoneNaloxoneAdminister 0.1mL spray of the 20 mg/mL formulation in one nostril
Intramuscular NaloxoneNaloxoneAdminister 1mL of 0.4mg/mL formulation intramuscularly
4mg(a) Intranasal NaloxoneNaloxoneAdminister 0.1mL spray of the 20 mg/mL formulation in both nostrils
4mg(b) Intranasal NaloxoneNaloxoneAdminister 0.1mL spray of the 40mg/mL formulation in one nostril
8mg Intranasal NaloxoneNaloxoneAdminister 0.1mL spray of the 40mg/mL formulation in both nostrils
Primary Outcome Measures
NameTimeMethod
Maximum Plasma Concentration (Cmax)720 minutes

Measurement of serum naloxone prior to dosing and at times 2.5, 5, 10, 15, 20, 30, 45, 60, 120, 180, 240, 300, 360, 480 and 720 minutes after naloxone administration.

Time at Maximum Plasma Concentration (Tmax)720 minutes

Measurement of serum naloxone prior to dosing and at times 2.5, 5, 10, 15, 20, 30, 45, 60, 120, 180, 240, 300, 360, 480 and 720 minutes after naloxone administration

Area Under the Concentration (AUC 0-t)720 minutes

Time curve from time zero to last measurable concentration. Measurement of serum naloxone prior to dosing and at times 2.5, 5, 10, 15, 20, 30, 45, 60, 120, 180, 240, 300, 360, 480 and 720 minutes after naloxone administration

Area Under Curve (AUC 0-inf)720 minutes

Time curve from time zero to infinity. Measurement of serum naloxone prior to dosing and at times 2.5, 5, 10, 15, 20, 30, 45, 60, 120, 180, 240, 300, 360, 480 and 720 minutes after naloxone administration

Half-life720 minutes

The apparent terminal exponential half-life. Measurement of serum naloxone prior to dosing and at times 2.5, 5, 10, 15, 20, 30, 45, 60, 120, 180, 240, 300, 360, 480 and 720 minutes after naloxone administration

Secondary Outcome Measures
NameTimeMethod
Adverse eventsminimum of 18 days

will be reported from the start of the first session to the follow-up visit

Vital Signs480 minutes

Measured at pre-dose and at times 30 , 60, 120 and 480 minutes after naloxone administration.

12-lead electrocardiogram480 minutes

Measured at pre-dose and at times 60 and 480 minutes after naloxone administration.

Nasal Irritation Scoring24 hours

Measured at pre-dose and at times 5, 30 , 60, 240 minutes and 24 hours after nasal naloxone administration.

Trial Locations

Locations (1)

Vince Associates Clinical Research

🇺🇸

Overland Park, Kansas, United States

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