Pharmacokinetic Evaluation of Intranasal and Intramuscular Naloxone in Healthy Volunteers

National Institutes of Health (NIH)

Status and phase: Completed; Phase 1

Conditions: Opioid-Related Disorders; Drug Overdose

Treatments: Drug: Naloxone

Study type: Interventional

Funder types: Other; NIH

Identifiers

NCT02572089

Naloxone-Phase1a-002

Details and patient eligibility

About

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.

Enrollment: 30 patients

Sex: All

Ages: 18 to 55 years old

Volunteers: Accepts Healthy Volunteers

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

Trial design

Primary purpose: Treatment

Allocation: Randomized

Interventional model: Crossover Assignment

Masking: None (Open label)

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30 participants in 5 patient groups

2mg Intranasal Naloxone

Experimental group

Description:

Administer 0.1mL spray of the 20 mg/mL formulation in one nostril

Treatment:

Drug: Naloxone

4mg(a) Intranasal Naloxone

Experimental group

Description:

Administer 0.1mL spray of the 20 mg/mL formulation in both nostrils

Treatment:

Drug: Naloxone

4mg(b) Intranasal Naloxone

Experimental group

Description:

Administer 0.1mL spray of the 40mg/mL formulation in one nostril

Treatment:

Drug: Naloxone

8mg Intranasal Naloxone

Experimental group

Description:

Administer 0.1mL spray of the 40mg/mL formulation in both nostrils

Treatment:

Drug: Naloxone

Intramuscular Naloxone

Experimental group

Description:

Administer 1mL of 0.4mg/mL formulation intramuscularly

Treatment:

Drug: Naloxone