U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry RACEMIC
Molecular Formula C11H12Cl2N2O
Molecular Weight 259.1321
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LOFEXIDINE

SMILES

CC(C1=NCCN1)Oc2c(cccc2Cl)Cl

InChI

InChIKey=KSMAGQUYOIHWFS-UHFFFAOYSA-N
InChI=1S/C11H12Cl2N2O/c1-7(11-14-5-6-15-11)16-10-8(12)3-2-4-9(10)13/h2-4,7H,5-6H2,1H3,(H,14,15)

HIDE SMILES / InChI
Lofexidine is newly FDA approved in the United States under the brand name LUCEMYRA for the treatment of opioid withdrawal symptoms in adults. Lofexidine acts as an agonist to α2 adrenergic receptors. These receptors inhibit adenylyl cyclase activity, leading to the inhibition of the second messenger, cyclic adenosine monophosphate (cAMP). The inhibition of cAMP leads to potassium efflux through calcium-activated channels, blocking calcium ions from entering the nerve terminal, resulting in suppression of neural firing, inhibition of norepinephrine release. Lofexidine replaces the opioid-driven inhibition of cAMP production and moderating the symptoms of opioid withdrawal.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1755 ng/mL
1.2 mg single, oral
dose: 1.2 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LOFEXIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
2795 ng/mL
2 mg single, oral
dose: 2 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LOFEXIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
6.29 ng/mL
0.6 mg 4 times / day steady-state, oral
dose: 0.6 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LOFEXIDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
31652 ng × h/mL
1.2 mg single, oral
dose: 1.2 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LOFEXIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
54321 ng × h/mL
2 mg single, oral
dose: 2 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LOFEXIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
25.8 ng × h/mL
0.6 mg 4 times / day steady-state, oral
dose: 0.6 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LOFEXIDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
11.16 h
1.2 mg single, oral
dose: 1.2 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LOFEXIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
11.44 h
2 mg single, oral
dose: 2 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LOFEXIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
12 h
0.6 mg 4 times / day steady-state, oral
dose: 0.6 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LOFEXIDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
45%
0.6 mg 4 times / day steady-state, oral
dose: 0.6 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LOFEXIDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Other AEs: Dizziness, Insomnia...
Other AEs:
Dizziness (3%)
Insomnia (3%)
Diarrhea (2%)
Orthostatic hypotension (1%)
Anxiety (2%)
Myalgia (2%)
Syncope (<1%)
Somnolence (<1%)
Restlessness (<1%)
Nausea (2%)
Vomiting (2%)
Sources:
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Other AEs: Hypotension...
0.54 mg 4 times / day steady, oral (starting)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Disc. AE: Hypotension, Dizziness...
AEs leading to
discontinuation/dose reduction:
Hypotension (1%)
Dizziness (3%)
Insomnia (3%)
Diarrhea (2%)
Orthostatic hypotension (1%)
Anxiety (2%)
Myalgia (2%)
Syncope (<1%)
Somnolence (<1%)
Restlessness (<1%)
Nausea (2%)
Vomiting (2%)
Sources:
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Other AEs: Hypotension, Dizziness...
Other AEs:
Hypotension (3%)
Dizziness (2%)
Insomnia (2%)
Diarrhea (2%)
Orthostatic hypotension (2%)
Anxiety (1%)
Myalgia (1%)
Syncope (1%)
Somnolence (1%)
Restlessness (1%)
Nausea (<1%)
Vomiting (<1%)
Bradycardia (3%)
Pain (2%)
Sources:
0.72 mg 4 times / day steady, oral (starting)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Disc. AE: Hypotension, Dizziness...
AEs leading to
discontinuation/dose reduction:
Hypotension (3%)
Dizziness (2%)
Insomnia (2%)
Diarrhea (2%)
Orthostatic hypotension (2%)
Anxiety (1%)
Myalgia (1%)
Syncope (1%)
Somnolence (1%)
Restlessness (1%)
Nausea (<1%)
Vomiting (<1%)
Bradycardia (3%)
Pain (2%)
Sources:
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Disc. AE: Bradycardia, Orthostatic hypotension...
Other AEs: Insomnia, Orthostatic hypotension...
AEs leading to
discontinuation/dose reduction:
Bradycardia (13.5%)
Orthostatic hypotension (13.5%)
Other AEs:
Insomnia (51%)
Orthostatic hypotension (29%)
Bradycardia (24%)
Hypotension (30%)
Dizziness (19%)
Somnolence (11%)
Sedation (13%)
Dry mouth (10%)
Syncope (0.9%)
Tinnitus (0.9%)
Bradycardia (13.5%)
Orthostatic hypotension (13.5%)
Insomnia (51%)
Orthostatic hypotension (29%)
Bradycardia (24%)
Hypotension (30%)
Dizziness (19%)
Somnolence (11%)
Sedation (13%)
Dry mouth (10%)
Syncope (0.9%)
Tinnitus (0.9%)
Sources:
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Disc. AE: Hypertension, Bradycardia...
Other AEs: Insomnia, Orthostatic hypotension...
AEs leading to
discontinuation/dose reduction:
Hypertension (21%)
Bradycardia (22%)
Orthostatic hypotension (22%)
Other AEs:
Insomnia (55%)
Orthostatic hypotension (42%)
Bradycardia (32%)
Hypotension (30%)
Dizziness (23%)
Somnolence (12%)
Sedation (13%)
Dry mouth (11%)
Syncope (1.4%)
Tinnitus (3.2%)
Hypertension (21%)
Bradycardia (22%)
Orthostatic hypotension (22%)
Insomnia (55%)
Orthostatic hypotension (42%)
Bradycardia (32%)
Hypotension (30%)
Dizziness (23%)
Somnolence (12%)
Sedation (13%)
Dry mouth (11%)
Syncope (1.4%)
Tinnitus (3.2%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Orthostatic hypotension 1%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Anxiety 2%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Diarrhea 2%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Myalgia 2%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Nausea 2%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Vomiting 2%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Dizziness 3%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Insomnia 3%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Restlessness <1%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Somnolence <1%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Syncope <1%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Hypotension 1%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Hypotension 1%
Disc. AE
0.54 mg 4 times / day steady, oral (starting)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Orthostatic hypotension 1%
Disc. AE
0.54 mg 4 times / day steady, oral (starting)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Anxiety 2%
Disc. AE
0.54 mg 4 times / day steady, oral (starting)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Diarrhea 2%
Disc. AE
0.54 mg 4 times / day steady, oral (starting)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Myalgia 2%
Disc. AE
0.54 mg 4 times / day steady, oral (starting)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Nausea 2%
Disc. AE
0.54 mg 4 times / day steady, oral (starting)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Vomiting 2%
Disc. AE
0.54 mg 4 times / day steady, oral (starting)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Dizziness 3%
Disc. AE
0.54 mg 4 times / day steady, oral (starting)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Insomnia 3%
Disc. AE
0.54 mg 4 times / day steady, oral (starting)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Restlessness <1%
Disc. AE
0.54 mg 4 times / day steady, oral (starting)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Somnolence <1%
Disc. AE
0.54 mg 4 times / day steady, oral (starting)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Syncope <1%
Disc. AE
0.54 mg 4 times / day steady, oral (starting)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 229
Sources:
Anxiety 1%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Myalgia 1%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Restlessness 1%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Somnolence 1%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Syncope 1%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Diarrhea 2%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Dizziness 2%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Insomnia 2%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Orthostatic hypotension 2%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Pain 2%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Bradycardia 3%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Hypotension 3%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Nausea <1%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Vomiting <1%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Anxiety 1%
Disc. AE
0.72 mg 4 times / day steady, oral (starting)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Myalgia 1%
Disc. AE
0.72 mg 4 times / day steady, oral (starting)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Restlessness 1%
Disc. AE
0.72 mg 4 times / day steady, oral (starting)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Somnolence 1%
Disc. AE
0.72 mg 4 times / day steady, oral (starting)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Syncope 1%
Disc. AE
0.72 mg 4 times / day steady, oral (starting)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Diarrhea 2%
Disc. AE
0.72 mg 4 times / day steady, oral (starting)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Dizziness 2%
Disc. AE
0.72 mg 4 times / day steady, oral (starting)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Insomnia 2%
Disc. AE
0.72 mg 4 times / day steady, oral (starting)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Orthostatic hypotension 2%
Disc. AE
0.72 mg 4 times / day steady, oral (starting)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Pain 2%
Disc. AE
0.72 mg 4 times / day steady, oral (starting)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Bradycardia 3%
Disc. AE
0.72 mg 4 times / day steady, oral (starting)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Hypotension 3%
Disc. AE
0.72 mg 4 times / day steady, oral (starting)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Nausea <1%
Disc. AE
0.72 mg 4 times / day steady, oral (starting)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Vomiting <1%
Disc. AE
0.72 mg 4 times / day steady, oral (starting)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy, 34 years (range: 19-74 years)
n = 390
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Population Size: 390
Sources:
Syncope 0.9%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Syncope 0.9%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Tinnitus 0.9%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Tinnitus 0.9%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Dry mouth 10%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Dry mouth 10%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Somnolence 11%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Somnolence 11%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Sedation 13%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Sedation 13%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Bradycardia 13.5%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Orthostatic hypotension 13.5%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Bradycardia 13.5%
Disc. AE
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Orthostatic hypotension 13.5%
Disc. AE
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Dizziness 19%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Dizziness 19%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Bradycardia 24%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Bradycardia 24%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Orthostatic hypotension 29%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Orthostatic hypotension 29%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Hypotension 30%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Hypotension 30%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Insomnia 51%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Insomnia 51%
0.54 mg 4 times / day steady, oral (max)
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
n = 229
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 229
Sources:
Syncope 1.4%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Syncope 1.4%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Dry mouth 11%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Dry mouth 11%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Somnolence 12%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Somnolence 12%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Sedation 13%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Sedation 13%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Hypertension 21%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Hypertension 21%
Disc. AE
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Bradycardia 22%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Orthostatic hypotension 22%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Bradycardia 22%
Disc. AE
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Orthostatic hypotension 22%
Disc. AE
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Dizziness 23%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Dizziness 23%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Tinnitus 3.2%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Tinnitus 3.2%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Hypotension 30%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Hypotension 30%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Bradycardia 32%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Bradycardia 32%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Orthostatic hypotension 42%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Orthostatic hypotension 42%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Insomnia 55%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
Insomnia 55%
0.72 mg 4 times / day steady, oral (max)
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
n = 222
Health Status: unhealthy
Condition: facilitation of abruption opioid discontinuation
Population Size: 222
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
yes [IC50 4551 uM]
yes [Inhibition 1.1 uM]
Drug as victimTox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Accelerated lofexidine treatment regimen compared with conventional lofexidine and methadone treatment for in-patient opiate detoxification.
1998 May 1
Alpha2 adrenergic agonists for the management of opioid withdrawal.
2001
Randomized placebo controlled trial of lofexidine hydrochloride for chronic pelvic pain in women.
2001 Aug
Two methods of community detoxification from opiates: an open-label comparison of lofexidine and buprenorphine.
2001 Dec 1
Lofexidine versus clonidine in rapid opiate detoxification.
2001 Jul
Repeated lofexidine treatment attenuates stress-induced, but not drug cues-induced reinstatement of a heroin-cocaine mixture (speedball) seeking in rats.
2001 Sep
The Leeds Evaluation of Efficacy of Detoxification Study (LEEDS) project: an open-label pragmatic randomised control trial comparing the efficacy of differing therapeutic agents for primary care detoxification from either street heroin or methadone [ISRCTN07752728].
2004 Apr 29
Alpha2 adrenergic agonists for the management of opioid withdrawal.
2004 Oct 18
Is clonidine useful for treatment of clozapine-induced sialorrhea?
2005 Jul
Induction of patients with moderately severe methadone dependence onto buprenorphine.
2005 Jun
Role of alpha-2 adrenoceptors in stress-induced reinstatement of alcohol seeking and alcohol self-administration in rats.
2005 May
Opiate addiction in China: current situation and treatments.
2006 May
Opioid dependence.
2007 Jun 1
Clinical pharmacokinetics of lofexidine, the alpha 2-adrenergic receptor agonist, in opiate addicts plasma using a highly sensitive liquid chromatography tandem mass spectrometric analysis.
2008
Tai-Kang-Ning, a Chinese herbal medicine formula, alleviates acute heroin withdrawal.
2008
Functional neuroanatomy of the noradrenergic locus coeruleus: its roles in the regulation of arousal and autonomic function part II: physiological and pharmacological manipulations and pathological alterations of locus coeruleus activity in humans.
2008 Sep
A Phase 3 placebo-controlled, double-blind, multi-site trial of the alpha-2-adrenergic agonist, lofexidine, for opioid withdrawal.
2008 Sep 1
Norepinephrine and stimulant addiction.
2009 Apr
Alpha2-adrenergic agonists for the management of opioid withdrawal.
2009 Apr 15
The Leeds Evaluation of Efficacy of Detoxification Study (LEEDS) prisons project: a randomised controlled trial comparing dihydrocodeine and buprenorphine for opiate detoxification.
2009 Feb 5
Electrocardiographic effects of lofexidine and methadone coadministration: secondary findings from a safety study.
2009 May
Clonidine in adults as a sedative agent in the intensive care unit.
2010 Oct
Patents

Patents

Sample Use Guides

The usual LUCEMYRA starting dosage is three 0.18 mg tablets taken orally 4 times daily during the period of peak withdrawal symptoms (generally the first 5 to 7 days following last use of opioid) with dosing guided by symptoms and side effects. There should be 5 to 6 hours between each dose. The total daily dosage of LUCEMYRA should not exceed 2.88 mg (16 tablets) and no single dose should exceed 0.72 mg (4 tablets).
Route of Administration: Oral
In Vitro Use Guide
Unknown
Name Type Language
LOFEXIDINE
INN   MI   VANDF   WHO-DD  
INN  
Official Name English
LOFEXIDINE [VANDF]
Common Name English
LOFEXIDINE [WHO-DD]
Common Name English
LOFEXIDINE [MI]
Common Name English
1H-IMIDAZOLE, 2-(1-(2,6-DICHLOROPHENOXY)ETHYL)-4,5-DIHYDRO-
Systematic Name English
2-(1-(2,6-DICHLOROPHENOXY)ETHYL)-2-IMIDAZOLINE
Systematic Name English
LOFEXIDINE [INN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C29709
Created by admin on Sat Jun 26 09:23:55 UTC 2021 , Edited by admin on Sat Jun 26 09:23:55 UTC 2021
WHO-ATC N07BC04
Created by admin on Sat Jun 26 09:23:55 UTC 2021 , Edited by admin on Sat Jun 26 09:23:55 UTC 2021
WHO-VATC QN07BC04
Created by admin on Sat Jun 26 09:23:55 UTC 2021 , Edited by admin on Sat Jun 26 09:23:55 UTC 2021
Code System Code Type Description
MERCK INDEX
M6885
Created by admin on Sat Jun 26 09:23:55 UTC 2021 , Edited by admin on Sat Jun 26 09:23:55 UTC 2021
PRIMARY Merck Index
EPA CompTox
31036-80-3
Created by admin on Sat Jun 26 09:23:55 UTC 2021 , Edited by admin on Sat Jun 26 09:23:55 UTC 2021
PRIMARY
FDA UNII
UI82K0T627
Created by admin on Sat Jun 26 09:23:55 UTC 2021 , Edited by admin on Sat Jun 26 09:23:55 UTC 2021
PRIMARY
DRUG CENTRAL
1593
Created by admin on Sat Jun 26 09:23:55 UTC 2021 , Edited by admin on Sat Jun 26 09:23:55 UTC 2021
PRIMARY
NCI_THESAURUS
C87578
Created by admin on Sat Jun 26 09:23:55 UTC 2021 , Edited by admin on Sat Jun 26 09:23:55 UTC 2021
PRIMARY
MESH
C025655
Created by admin on Sat Jun 26 09:23:55 UTC 2021 , Edited by admin on Sat Jun 26 09:23:55 UTC 2021
PRIMARY
ChEMBL
CHEMBL17860
Created by admin on Sat Jun 26 09:23:55 UTC 2021 , Edited by admin on Sat Jun 26 09:23:55 UTC 2021
PRIMARY
EVMPD
SUB08558MIG
Created by admin on Sat Jun 26 09:23:55 UTC 2021 , Edited by admin on Sat Jun 26 09:23:55 UTC 2021
PRIMARY
DRUG BANK
DB04948
Created by admin on Sat Jun 26 09:23:55 UTC 2021 , Edited by admin on Sat Jun 26 09:23:55 UTC 2021
PRIMARY
CAS
31036-80-3
Created by admin on Sat Jun 26 09:23:55 UTC 2021 , Edited by admin on Sat Jun 26 09:23:55 UTC 2021
PRIMARY
LACTMED
Lofexidine
Created by admin on Sat Jun 26 09:23:55 UTC 2021 , Edited by admin on Sat Jun 26 09:23:55 UTC 2021
PRIMARY
PUBCHEM
30668
Created by admin on Sat Jun 26 09:23:55 UTC 2021 , Edited by admin on Sat Jun 26 09:23:55 UTC 2021
PRIMARY
INN
3766
Created by admin on Sat Jun 26 09:23:55 UTC 2021 , Edited by admin on Sat Jun 26 09:23:55 UTC 2021
PRIMARY
RXCUI
28863
Created by admin on Sat Jun 26 09:23:55 UTC 2021 , Edited by admin on Sat Jun 26 09:23:55 UTC 2021
PRIMARY RxNorm