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
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
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
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
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:
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Other AEs: Hypotension...
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
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
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
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
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
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
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
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
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Anxiety 2%
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Diarrhea 2%
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Myalgia 2%
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Nausea 2%
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Vomiting 2%
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Dizziness 3%
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Insomnia 3%
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Restlessness <1%
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Somnolence <1%
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Syncope <1%
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Hypotension 1%
Disc. AE
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Orthostatic hypotension 1%
Disc. AE
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Anxiety 2%
Disc. AE
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Diarrhea 2%
Disc. AE
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Myalgia 2%
Disc. AE
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Nausea 2%
Disc. AE
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Vomiting 2%
Disc. AE
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Dizziness 3%
Disc. AE
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Insomnia 3%
Disc. AE
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Restlessness <1%
Disc. AE
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Somnolence <1%
Disc. AE
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Syncope <1%
Disc. AE
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Hypotension 1%
0.54 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Anxiety 1%
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Myalgia 1%
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Restlessness 1%
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Somnolence 1%
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Syncope 1%
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Diarrhea 2%
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Dizziness 2%
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Insomnia 2%
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Orthostatic hypotension 2%
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Pain 2%
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Bradycardia 3%
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Hypotension 3%
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Nausea <1%
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Vomiting <1%
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Anxiety 1%
Disc. AE
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Myalgia 1%
Disc. AE
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Restlessness 1%
Disc. AE
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Somnolence 1%
Disc. AE
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Syncope 1%
Disc. AE
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Diarrhea 2%
Disc. AE
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Dizziness 2%
Disc. AE
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Insomnia 2%
Disc. AE
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Orthostatic hypotension 2%
Disc. AE
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Pain 2%
Disc. AE
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Bradycardia 3%
Disc. AE
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Hypotension 3%
Disc. AE
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Nausea <1%
Disc. AE
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Vomiting <1%
Disc. AE
0.72 mg 4 times / day steady, oral
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)
Health Status: unhealthy
Age Group: 34 years (range: 19-74 years)
Sex: M+F
Sources:
Syncope 0.9%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Syncope 0.9%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Tinnitus 0.9%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Tinnitus 0.9%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Dry mouth 10%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Dry mouth 10%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Somnolence 11%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Somnolence 11%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Sedation 13%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Sedation 13%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Bradycardia 13.5%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Orthostatic hypotension 13.5%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Bradycardia 13.5%
Disc. AE
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Orthostatic hypotension 13.5%
Disc. AE
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Dizziness 19%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Dizziness 19%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Bradycardia 24%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Bradycardia 24%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Orthostatic hypotension 29%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Orthostatic hypotension 29%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Hypotension 30%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Hypotension 30%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Insomnia 51%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Insomnia 51%
0.54 mg 4 times / day steady, oral
Recommended
Dose: 0.54 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.54 mg, 4 times / day
Sources:
unhealthy
Syncope 1.4%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Syncope 1.4%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Dry mouth 11%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Dry mouth 11%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Somnolence 12%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Somnolence 12%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Sedation 13%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Sedation 13%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Hypertension 21%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Hypertension 21%
Disc. AE
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Bradycardia 22%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Orthostatic hypotension 22%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Bradycardia 22%
Disc. AE
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Orthostatic hypotension 22%
Disc. AE
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Dizziness 23%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Dizziness 23%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Tinnitus 3.2%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Tinnitus 3.2%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Hypotension 30%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Hypotension 30%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Bradycardia 32%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Bradycardia 32%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Orthostatic hypotension 42%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Orthostatic hypotension 42%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Insomnia 55%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
Insomnia 55%
0.72 mg 4 times / day steady, oral
Studied dose
Dose: 0.72 mg, 4 times / day
Route: oral
Route: steady
Dose: 0.72 mg, 4 times / day
Sources:
unhealthy
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
[Therapy of tic disorders apparently of organic origin in a multi-morbid 5-year-old patient with lofexidine (Britlofex) and clonidine (Catapressan)].
2001
Two methods of community detoxification from opiates: an open-label comparison of lofexidine and buprenorphine.
2001 Dec 1
Lofexidine in hyperactive and impulsive children with autistic disorder.
2002 Dec
Alpha2-adrenergic agonists in opioid withdrawal.
2002 Jan
Use of qigong therapy in the detoxification of heroin addicts.
2002 Jan-Feb
Prison based detoxification for opioid dependence: a randomised double blind controlled trial of lofexidine and methadone.
2002 Jul 1
Alpha2 adrenergic agonists for the management of opioid withdrawal.
2003
[Clinical observation on effect of modified banxia houpu decoction in treating patients with protracted heroin abstinence syndrome].
2004 Mar
Alpha2 adrenergic agonists for the management of opioid withdrawal.
2004 Oct 18
A comparison of buprenorphine and lofexidine for community opiate detoxification: results from a randomized controlled trial.
2005 Dec
Induction of patients with moderately severe methadone dependence onto buprenorphine.
2005 Jun
Effects of lofexidine on stress-induced and cue-induced opioid craving and opioid abstinence rates: preliminary findings.
2007 Mar
Functional neuroanatomy of the noradrenergic locus coeruleus: its roles in the regulation of arousal and autonomic function part II: physiological and pharmacological manipulations and pathological alterations of locus coeruleus activity in humans.
2008 Sep
The Leeds Evaluation of Efficacy of Detoxification Study (LEEDS) Prisons Project Study: protocol for a randomised controlled trial comparing methadone and buprenorphine for opiate detoxification.
2009 Jul 14
Buprenorphine for the management of opioid withdrawal.
2009 Jul 8
Electrocardiographic effects of lofexidine and methadone coadministration: secondary findings from a safety study.
2009 May
Opioid antagonists with minimal sedation for opioid withdrawal.
2009 Oct 7
A double-blind, randomized, parallel group study to compare the efficacy, safety and tolerability of slow-release oral morphine versus methadone in opioid-dependent in-patients willing to undergo detoxification.
2009 Sep
A case report of inpatient detoxification after kratom (Mitragyna speciosa) dependence.
2010
Lofexidine, an {alpha}2-receptor agonist for opioid detoxification.
2010 Feb
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
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