The purpose of this study is to evaluate the relative exposures of lofexidine and its major metabolites in subjects seeking buprenorphine dose reduction.
This is a Phase 1, open-label, inpatient study in male and female subjects seeking at least a 4 mg reduction of their buprenorphine maintenance dose. The purpose of this study is to assess the relative exposures of lofexidine and its 3 major metabolites in subjects tapering from buprenorphine maintenance treatment. Lofexidine is an alpha-2 adrenergic agonist under development for the treatment of acute withdrawal from short-acting opioids.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
10
Unnamed facility
Overland Park, Kansas, United States
Predose and peak metabolite (N-[2- aminoethyl-2-[2,6-dichlorophenoxy] propanamide [LADP], 2-[2,6-dichlorophenoxy] propionic acid [LDPA] and 2,6-Dichlorophenol [2,6-DCP]) plasma concentration to lofexidine (parent) ratios on each day of treatment
Time frame: pre-1 PM dose and 3 hours post-1 PM dose on Days 1-6; pre-8 AM dose and 1, 3, 7, 12, 24, and 34 hours post-8 AM dose on Day 7
Modified Clinical Global Impression - subject and observer
Time frame: 3.5 hours post-8 AM dose on Days 1-7
Visual Analog Scale for Efficacy
Time frame: 3.5 hours post-8 AM dose on Days 1-7
Columbia Suicide Severity Rating Scale (C-SSRS)
Time frame: Baseline: Day -1; 3.5 hours post-first dose on Day 1; Day 8
Holter ECGs
Time frame: Day -1; pre-1 PM dose, 3 and 4 hours post-1 PM dose on Days 1 and 6
Blood pressure and pulse (sitting and standing)
Time frame: screening; Day -1; within 30 minutes before every dose Days 1-8
Laboratory Assessments
Measurements in hematology, chemistry, urinalysis, infectious disease panel. Labs will be done at screening.
Time frame: screening
Oral temperature and respiration
Time frame: screening; Day -1; pre-8 AM dose on Days 1-8
12-Lead ECG
Time frame: screening
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Adverse Events Assessment
Time frame: Day -1; Days 1-8
Urine drug screening
Time frame: Screening; Day -1, Days 1-8
Concomitant medications
Time frame: Screening; Day -1, Days 1-8
Physical exam
Time frame: screening; Day -1; Day 8