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
Double-blind randomised controlled trial of lofexidine versus clonidine in the treatment of heroin withdrawal.
1997 Nov 25
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
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
Opioid dependence.
2007 Jun 1
A comparative clinical study of the effects of the traditional Chinese medicine Jinniu capsules and lofexidine on acute heroin withdrawal symptoms.
2008
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
Pharmacokinetics of lofexidine hydrochloride in healthy volunteers.
2009 Jan
A comparison of methadone, buprenorphine and alpha(2) adrenergic agonists for opioid detoxification: a mixed treatment comparison meta-analysis.
2010 Apr 1
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