Efavirenz and Ritonavir on Human Brain P-Glycoprotein

Washington University School of Medicine13 enrolled

Overview

To determine the effects of ritonavir and efavirenz on the activity of P-glycoprotein in human brain.

Sequential crossover using tracer 11C-desmethylloperamide, a substrate for brain P-glycoprotein, and positron emission tomography (PET), administered after nothing (control), oral ritonavir (3d), and oral efavirenz (14d) with washout in between

Study Type

INTERVENTIONAL

Allocation

NON_RANDOMIZED

Purpose

OTHER

Masking

NONE

Enrollment

Conditions

Drug Effects

Interventions

[11C] desmethyl-loperamideDRUG

IV administration of 10-14 mCi of \[11C\] desmethyl-loperamide with PET/CT imaging

Control - no pretreatmentOTHER

Session 1: IV administration of 10-14 mCi \[11C\] desmethyl-loperamide (dLop) with PET/CT imaging and brain MRI

Oral ritonavirDRUG

Session 2: Pretreatment with oral ritonavir for 3 days followed by IV administration of 10-14 mCi \[11C\]dLop with PET/CT imaging and brain MRI

Eligibility

Sex: ALLMin age: 18 YearsMax age: 40 YearsHealthy volunteers:

Medical Language ↔ Plain English

Inclusion Criteria: * Male or non-pregnant female, 18-40 yr old * Good general health with no remarkable medical conditions * BMI \< 33 * Provide informed consent Exclusion Criteria: * Known history of liver or kidney disease * History of major medical conditions * HIV seropositive * Fasting blood glucose \> 110 mg/dl * Family history of type 2 diabetes * Use of prescription or non prescription medications, herbals or foods known to be metabolized by or altering P-glycoprotein or CYP3A activity (hormonal birth control medications are acceptable if alternative means of contraception are used) * Females who are pregnant or nursing * Females taking hormonal contraceptives who are unwilling to use alternative means of contraception * Contraindications to MRI * Contraindications to PET scanning

Locations (1)

Washington University School of Medicine

St Louis, Missouri, United States

Outcomes

Primary Outcomes

Cerebral [11C]dLop Distribution Volume

Time frame: 1 day

Data from ClinicalTrials.gov

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