Details
Stereochemistry | RACEMIC |
Molecular Formula | C11H12Cl2N2O |
Molecular Weight | 259.132 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(OC1=C(Cl)C=CC=C1Cl)C2=NCCN2
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)
Molecular Formula | C11H12Cl2N2O |
Molecular Weight | 259.132 |
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
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Palliative | LUCEMYRA Approved UseLUCEMYRA is a central alpha-2 adrenergic agonist indicated for mitigation of opioid withdrawal symptoms to facilitate abrupt opioid discontinuation in adults Launch Date2018 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1755 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18393298/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18393298/ |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
31652 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18393298/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18393298/ |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
11.16 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18393298/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18393298/ |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Dose | Population | Adverse 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%) Sources: Insomnia (3%) Diarrhea (2%) Orthostatic hypotension (1%) Anxiety (2%) Myalgia (2%) Syncope (<1%) Somnolence (<1%) Restlessness (<1%) Nausea (2%) 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: |
Other AEs: Hypotension... Other AEs: Hypotension (1%) Sources: |
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%) Sources: Dizziness (3%) Insomnia (3%) Diarrhea (2%) Orthostatic hypotension (1%) Anxiety (2%) Myalgia (2%) Syncope (<1%) Somnolence (<1%) Restlessness (<1%) Nausea (2%) Vomiting (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: |
Other AEs: Hypotension, Dizziness... Other AEs: Hypotension (3%) Sources: 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%) |
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%) Sources: 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%) |
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%) Other AEs:Orthostatic hypotension (13.5%) Insomnia (51%) Sources: 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%) |
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%) Other AEs:Bradycardia (22%) Orthostatic hypotension (22%) Insomnia (55%) Sources: 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%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
major | no (co-administration study) Comment: Paroxetine did not affect mean lofexidine Cmax values and slightly increased mean AUC values by approximately 30%. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209229Orig1s000MultidisciplineR.pdf#page=28 Page: 28.0 |
|||
no | ||||
yes | ||||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
Animal experiments on the safety pharmacology of lofexidine. | 1982 |
|
Alcohol withdrawal syndromes: clinical management with lofexidine. | 1985 Mar-Apr |
|
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 |
|
A placebo-controlled study of lofexidine in the treatment of children with tic disorders and attention deficit hyperactivity disorder. | 2004 Jun |
|
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 |
|
A comparison of buprenorphine and lofexidine for community opiate detoxification: results from a randomized controlled trial. | 2005 Dec |
|
Lofexidine for opioid detoxification. | 2005 Jan |
|
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 |
|
Pharmacologic treatments for opioid dependence: detoxification and maintenance options. | 2007 |
|
In-patient detoxification procedures, treatment retention, and post-treatment opiate use: comparison of lofexidine + naloxone, lofexidine + placebo, and methadone. | 2007 Apr 17 |
|
Hemodynamic and cognitive effects of lofexidine and methadone coadministration: a pilot study. | 2007 Aug |
|
The Leeds Evaluation of Efficacy of Detoxification Study (LEEDS) prisons project pilot study: protocol for a randomised controlled trial comparing dihydrocodeine and buprenorphine for opiate detoxification. | 2007 Jan 8 |
|
Buprenorphine versus dihydrocodeine for opiate detoxification in primary care: a randomised controlled trial. | 2007 Jan 8 |
|
Opioid dependence. | 2007 Jun 1 |
|
Effects of lofexidine on stress-induced and cue-induced opioid craving and opioid abstinence rates: preliminary findings. | 2007 Mar |
|
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 |
|
Effects of THC and lofexidine in a human laboratory model of marijuana withdrawal and relapse. | 2008 Mar |
|
Agenda for specialty section in addiction medicine. | 2008 Oct |
|
Functional neuroanatomy of the noradrenergic locus coeruleus: its roles in the regulation of arousal and autonomic function part II: physiological and pharmacological manipulations and pathological alterations of locus coeruleus activity in humans. | 2008 Sep |
|
A Phase 3 placebo-controlled, double-blind, multi-site trial of the alpha-2-adrenergic agonist, lofexidine, for opioid withdrawal. | 2008 Sep 1 |
|
A study on Fu-Yuan Pellet, a traditional chinese medicine formula for detoxification of heroin addictions. | 2009 |
|
Urine and plasma pharmacokinetics of lofexidine after oral delivery in opiate-dependent patients. | 2009 |
|
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 |
|
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 |
|
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 |
|
Opioid dependence. | 2009 Jul 24 |
|
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 |
|
Alpha2-receptor agonists for treatment and prevention of iatrogenic opioid abstinence syndrome in critically ill patients. | 2009 Sep |
|
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 |
|
A comparison of methadone, buprenorphine and alpha(2) adrenergic agonists for opioid detoxification: a mixed treatment comparison meta-analysis. | 2010 Apr 1 |
|
Lofexidine, an {alpha}2-receptor agonist for opioid detoxification. | 2010 Feb |
|
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
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/6890366
Unknown
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 17:20:12 GMT 2023
by
admin
on
Sat Dec 16 17:20:12 GMT 2023
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Record UNII |
UI82K0T627
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C29709
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WHO-ATC |
N07BC04
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WHO-VATC |
QN07BC04
Created by
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m6885
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PRIMARY | Merck Index | ||
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DTXSID7023221
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UI82K0T627
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1593
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C87578
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C025655
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CHEMBL17860
Created by
admin on Sat Dec 16 17:20:13 GMT 2023 , Edited by admin on Sat Dec 16 17:20:13 GMT 2023
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SUB08558MIG
Created by
admin on Sat Dec 16 17:20:13 GMT 2023 , Edited by admin on Sat Dec 16 17:20:13 GMT 2023
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DB04948
Created by
admin on Sat Dec 16 17:20:13 GMT 2023 , Edited by admin on Sat Dec 16 17:20:13 GMT 2023
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31036-80-3
Created by
admin on Sat Dec 16 17:20:13 GMT 2023 , Edited by admin on Sat Dec 16 17:20:13 GMT 2023
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Lofexidine
Created by
admin on Sat Dec 16 17:20:13 GMT 2023 , Edited by admin on Sat Dec 16 17:20:13 GMT 2023
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Lofexidine
Created by
admin on Sat Dec 16 17:20:13 GMT 2023 , Edited by admin on Sat Dec 16 17:20:13 GMT 2023
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51368
Created by
admin on Sat Dec 16 17:20:13 GMT 2023 , Edited by admin on Sat Dec 16 17:20:13 GMT 2023
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30668
Created by
admin on Sat Dec 16 17:20:13 GMT 2023 , Edited by admin on Sat Dec 16 17:20:13 GMT 2023
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100000082020
Created by
admin on Sat Dec 16 17:20:13 GMT 2023 , Edited by admin on Sat Dec 16 17:20:13 GMT 2023
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3766
Created by
admin on Sat Dec 16 17:20:13 GMT 2023 , Edited by admin on Sat Dec 16 17:20:13 GMT 2023
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28863
Created by
admin on Sat Dec 16 17:20:13 GMT 2023 , Edited by admin on Sat Dec 16 17:20:13 GMT 2023
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UI82K0T627
Created by
admin on Sat Dec 16 17:20:13 GMT 2023 , Edited by admin on Sat Dec 16 17:20:13 GMT 2023
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Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT | |||
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TARGET -> AGONIST |
SHORT-ACTING
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METABOLIC ENZYME -> SUBSTRATE |
MINOR
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METABOLIC ENZYME -> SUBSTRATE |
Lofexidine exposures were approximately 30% greater with co-administration of paroxetine a strong inhibitor of CYP2D6.
MAJOR
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METABOLIC ENZYME -> SUBSTRATE |
MINOR
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METABOLIC ENZYME -> INHIBITOR |
Interaction with CYP2D6 substrates is not expected to be clinically significant.
MINOR
IC50
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BINDER->LIGAND |
BINDING
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EXCRETED UNCHANGED |
The primary route of elimination of lofexidine and its metabolites was via the kidney.
URINE
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Related Record | Type | Details | ||
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METABOLITE INACTIVE -> PARENT |
MAJOR
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METABOLITE INACTIVE -> PARENT |
MAJOR
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METABOLITE INACTIVE -> PARENT |
MAJOR
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Tmax | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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Volume of Distribution | PHARMACOKINETIC |
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