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

Molecular Formula C11H12Cl2N2O
Molecular Weight 259.1321
Charge 0
Count
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

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
Alpha-2 adrenergic receptor agonists block stress-induced reinstatement of cocaine seeking.
2000 Aug
[Therapy of tic disorders apparently of organic origin in a multi-morbid 5-year-old patient with lofexidine (Britlofex) and clonidine (Catapressan)].
2001
Alpha2 adrenergic agonists for the management of opioid withdrawal.
2001
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
A double-blind randomized placebo-controlled trial of lofexidine in alcohol withdrawal: lofexidine is not a useful adjunct to chlordiazepoxide.
2001 Sep-Oct
Acceptability and availability of pharmacological interventions for substance misuse by British NHS treatment services.
2002 Jan
Prescribing to drug misusers in practice--often effective, but rarely straightforward.
2002 Jul
Prison based detoxification for opioid dependence: a randomised double blind controlled trial of lofexidine and methadone.
2002 Jul 1
A review of chemical agents in the pharmacotherapy of addiction.
2002 Oct
Alpha2 adrenergic agonists for the management of opioid withdrawal.
2003
The effectiveness of combined naloxone/lofexidine in opiate detoxification: results from a double-blind randomized and placebo-controlled trial.
2003 Jul-Sep
Major disruptions of sleep during treatment of the opiate withdrawal syndrome: differences between methadone and lofexidine detoxification treatments.
2003 Mar
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
A placebo-controlled study of lofexidine in the treatment of children with tic disorders and attention deficit hyperactivity disorder.
2004 Jun
[Clinical observation on effect of modified banxia houpu decoction in treating patients with protracted heroin abstinence syndrome].
2004 Mar
Evidence-based addiction medicine: the use of lofexidine for opioid detoxification.
2004 Nov
QT interval increased after single dose of lofexidine.
2004 Nov 6
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
Cognitive function during early abstinence from opioid dependence: a comparison to age, gender, and verbal intelligence matched controls.
2006 Feb 24
Opioid antagonists with minimal sedation for opioid withdrawal.
2006 Jan 25
Opiate addiction in China: current situation and treatments.
2006 May
The place of detoxification in treatment of opioid dependence.
2006 May
Buprenorphine versus dihydrocodeine for opiate detoxification in primary care: a randomised controlled trial.
2007 Jan 8
A comparative clinical study of the effects of the traditional Chinese medicine Jinniu capsules and lofexidine on acute heroin withdrawal symptoms.
2008
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
Agenda for specialty section in addiction medicine.
2008 Oct
Pharmacotherapy for cannabis dependence: how close are we?
2009
Norepinephrine and stimulant addiction.
2009 Apr
Alpha2-adrenergic agonists for the management of opioid withdrawal.
2009 Apr 15
Pharmacokinetics of lofexidine hydrochloride in healthy volunteers.
2009 Jan
Buprenorphine for the management of opioid withdrawal.
2009 Jul 8
A case report of inpatient detoxification after kratom (Mitragyna speciosa) dependence.
2010
The pharmacological treatment of opioid addiction--a clinical perspective.
2010 Jun
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
Substance Class Chemical
Created
by admin
on Sat Jun 26 09:23:54 UTC 2021
Edited
by admin
on Sat Jun 26 09:23:54 UTC 2021
Record UNII
UI82K0T627
Record Status Validated (UNII)
Record Version
  • Download
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
Related Record Type Details
TARGET -> AGONIST
SHORT-ACTING
SALT/SOLVATE -> PARENT
METABOLIC ENZYME -> SUBSTRATE
MINOR
METABOLIC ENZYME -> SUBSTRATE
Lofexidine exposures were approximately 30% greater with co-administration of paroxetine a strong inhibitor of CYP2D6.
MAJOR
METABOLIC ENZYME -> SUBSTRATE
MINOR
METABOLIC ENZYME -> INHIBITOR
Interaction with CYP2D6 substrates is not expected to be clinically significant.
MINOR
IC50
BINDER->LIGAND
BINDING
EXCRETED UNCHANGED
The primary route of elimination of lofexidine and its metabolites was via the kidney.
URINE
Related Record Type Details
METABOLITE INACTIVE -> PARENT
MAJOR
METABOLITE INACTIVE -> PARENT
MAJOR
METABOLITE INACTIVE -> PARENT
MAJOR
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC