Buprenorphine Disposition and CYP3A

Washington University School of Medicine21 enrolled

Overview

To evaluate role of CYP3A in buprenorphine disposition and effect

Subjects will be studied during a maximum of seven occasions. Study drugs are intravenous buprenorphine (0.025-0.2 mg infused over 1 hr) and sublingual buprenorphine (2-4 mg), with 1-3 week washout between sessions. Sessions 1\&2: Control (no pretreatment) - intravenous and sublingual buprenorphine. Some subjects will only undergo session 1 (IV) Sessions 3\&4: Liver and gut CYP3A induction (rifampin 600 mg daily), intravenous and sublingual buprenorphine Session 5: Gut only CYP3A inhibition (grapefruit juice the night before), sublingual buprenorphine Sessions 6\&7: Liver and gut CYP3A inhibition (ketoconazole 400 mg daily), intravenous and sublingual buprenorphine

Study Type

INTERVENTIONAL

Purpose

OTHER

Masking

NONE

Enrollment

Conditions

Healthy

Interventions

Buprenorphine ControlDRUG

Control (no pretreatment) - intravenous and sublingual buprenorphine. Some subjects will only undergo session 1 (IV)

Buprenorphine + RifampinDRUG

Liver and gut CYP3A induction (rifampin 600 mg daily), intravenous and sublingual buprenorphine

Buprenorphine + Grapefruit juiceDRUG

Gut only CYP3A inhibition (grapefruit juice the night before), sublingual buprenorphine

Eligibility

Sex: ALLMin age: 18 YearsMax age: 50 YearsHealthy volunteers:

Medical Language ↔ Plain English

Inclusion Criteria: Each subject must meet all of the following criteria: 1. Male or non-pregnant female volunteer, 18-50 yr old 2. Good general health with no known major medical conditions 3. BMI \< 33 4. Provide informed consent Exclusion Criteria: Subjects will not be enrolled if any of the following criteria exist: 1. Known history of liver or kidney disease 2. Use of prescription or non-prescription medications, herbals or foods known to be metabolized by or affect CYP3A activity (this includes the use of oral contraceptives). 3. Females who are pregnant or nursing 4. Known history of drug or alcohol addiction (prior or present addiction or addiction treatment) 5. Direct physical access to and routine handling of addicting drugs in the regular course of duty (this is a routine exclusion from studies of drugs with addiction potential)

Locations (1)

Washington University School of Medicine

St Louis, Missouri, United States

Outcomes

Primary Outcomes

Plasma Cmax of Buprenorphine

Time frame: 96 hr

Data from ClinicalTrials.gov

This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.