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

Details

Stereochemistry ABSOLUTE
Molecular Formula C29H41NO4
Molecular Weight 467.6412
Optical Activity UNSPECIFIED
Defined Stereocenters 7 / 7
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BUPRENORPHINE

SMILES

CC(C)(C)[C@](C)([C@@]1([H])C[C@]23CC[C@@]1([C@@]4([H])[C@]53CCN(CC6CC6)[C@]2([H])Cc7ccc(c(c75)O4)O)OC)O

InChI

InChIKey=RMRJXGBAOAMLHD-IHFGGWKQSA-N
InChI=1S/C29H41NO4/c1-25(2,3)26(4,32)20-15-27-10-11-29(20,33-5)24-28(27)12-13-30(16-17-6-7-17)21(27)14-18-8-9-19(31)23(34-24)22(18)28/h8-9,17,20-21,24,31-32H,6-7,10-16H2,1-5H3/t20-,21-,24-,26+,27-,28+,29-/m1/s1

HIDE SMILES / InChI

Molecular Formula C29H41NO4
Molecular Weight 467.6412
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 7 / 7
E/Z Centers 0
Optical Activity UNSPECIFIED

Buprenorphine is an opioid analgesic, used to treat opioid addiction, moderate acute pain, and moderate chronic pain. Buprenorphine is a partial agonist at the mµ-opioid receptor and an antagonist at the kappa-opioid receptor. One unusual property of buprenorphine observed in vitro studies is its very slow rate of dissociation from its receptor. This could account for its longer duration of action than morphine, the unpredictability of its reversal by opioid antagonists, and its low level of manifest physical dependence. The principal action of the therapeutic value of buprenorphine is analgesia and is thought to be due to buprenorphine binding with high affinity to opioid receptors on neurons in the brain and spinal cord. Buprenorphine produces respiratory depression by direct action on brain stem respiratory centers. The respiratory depression involves a reduction in the responsiveness of the brain stem respiratory centers to both increases in carbon dioxide tension and electrical stimulation. Buprenorphine causes a reduction in motility associated with an increase in smooth muscle tone in the antrum of the stomach and duodenum. Digestion of food in the small intestine is delayed and propulsive contractions are decreased. Buprenorphine produces peripheral vasodilation, which may result in orthostatic hypotension or syncope. Manifestations of histamine release and/or peripheral vasodilation may include pruritus, flushing, red eyes, sweating, and/or orthostatic hypotension.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
1.5 nM [Ki]
2.5 nM [Ki]
6.1 nM [Ki]
Target ID: P41146
Gene ID: 4987.0
Gene Symbol: OPRL1
Target Organism: Homo sapiens (Human)
77.4 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
BUTRANS

Approved Use

SUBOXONE sublingual film is indicated for maintenance treatment of opioid dependence and should be used as part of a complete treatment plan to include counseling and psychosocial support. Under the Drug Addiction Treatment Act (DATA) codified at 21 U.S.C. 823(g), prescription use of this product in the treatment of opioid dependence is limited to physicians who meet certain qualifying requirements, and who have notified the Secretary of Health and Human Services (HHS) of their intent to prescribe this product for the treatment of opioid dependence and have been assigned a unique identification number that must be included on every prescription. SUBOXONE sublingual film is indicated for maintenance treatment of opioid dependence. Prescription use of this product is limited under the Drug Addiction Treatment Act. (1)

Launch Date

1.27785606E12
Primary
BUTRANS

Approved Use

SUBOXONE sublingual film is indicated for maintenance treatment of opioid dependence and should be used as part of a complete treatment plan to include counseling and psychosocial support. Under the Drug Addiction Treatment Act (DATA) codified at 21 U.S.C. 823(g), prescription use of this product in the treatment of opioid dependence is limited to physicians who meet certain qualifying requirements, and who have notified the Secretary of Health and Human Services (HHS) of their intent to prescribe this product for the treatment of opioid dependence and have been assigned a unique identification number that must be included on every prescription. SUBOXONE sublingual film is indicated for maintenance treatment of opioid dependence. Prescription use of this product is limited under the Drug Addiction Treatment Act. (1)

Launch Date

1.27785606E12
Primary
BUTRANS

Approved Use

SUBOXONE sublingual film is indicated for maintenance treatment of opioid dependence and should be used as part of a complete treatment plan to include counseling and psychosocial support. Under the Drug Addiction Treatment Act (DATA) codified at 21 U.S.C. 823(g), prescription use of this product in the treatment of opioid dependence is limited to physicians who meet certain qualifying requirements, and who have notified the Secretary of Health and Human Services (HHS) of their intent to prescribe this product for the treatment of opioid dependence and have been assigned a unique identification number that must be included on every prescription. SUBOXONE sublingual film is indicated for maintenance treatment of opioid dependence. Prescription use of this product is limited under the Drug Addiction Treatment Act. (1)

Launch Date

1.27785606E12
Primary
BUTRANS

Approved Use

SUBOXONE sublingual film is indicated for maintenance treatment of opioid dependence and should be used as part of a complete treatment plan to include counseling and psychosocial support. Under the Drug Addiction Treatment Act (DATA) codified at 21 U.S.C. 823(g), prescription use of this product in the treatment of opioid dependence is limited to physicians who meet certain qualifying requirements, and who have notified the Secretary of Health and Human Services (HHS) of their intent to prescribe this product for the treatment of opioid dependence and have been assigned a unique identification number that must be included on every prescription. SUBOXONE sublingual film is indicated for maintenance treatment of opioid dependence. Prescription use of this product is limited under the Drug Addiction Treatment Act. (1)

Launch Date

1.27785606E12
Primary
BUTRANS

Approved Use

SUBOXONE sublingual film is indicated for maintenance treatment of opioid dependence and should be used as part of a complete treatment plan to include counseling and psychosocial support. Under the Drug Addiction Treatment Act (DATA) codified at 21 U.S.C. 823(g), prescription use of this product in the treatment of opioid dependence is limited to physicians who meet certain qualifying requirements, and who have notified the Secretary of Health and Human Services (HHS) of their intent to prescribe this product for the treatment of opioid dependence and have been assigned a unique identification number that must be included on every prescription. SUBOXONE sublingual film is indicated for maintenance treatment of opioid dependence. Prescription use of this product is limited under the Drug Addiction Treatment Act. (1)

Launch Date

1.27785606E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
0.17 ng/mL
75 μg single, oral
dose: 75 μg
route of administration: Oral
experiment type: SINGLE
co-administered:
BUPRENORPHINE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
0.63 ng × h/mL
75 μg single, oral
dose: 75 μg
route of administration: Oral
experiment type: SINGLE
co-administered:
BUPRENORPHINE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
3 h
75 μg single, oral
dose: 75 μg
route of administration: Oral
experiment type: SINGLE
co-administered:
BUPRENORPHINE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
4%
75 μg single, oral
dose: 75 μg
route of administration: Oral
experiment type: SINGLE
co-administered:
BUPRENORPHINE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
5.714 ug/kg 1 times / day single, intravenous
Studied dose
Dose: 5.714 ug/kg, 1 times / day
Route: intravenous
Route: single
Dose: 5.714 ug/kg, 1 times / day
Sources:
healthy, 22 to 35 years
n = 5
Health Status: healthy
Age Group: 22 to 35 years
Sex: M
Population Size: 5
Sources:
Other AEs: Respiratory depression...
480 ug 2 times / day multiple, oral (mean)
Recommended
Dose: 480 ug, 2 times / day
Route: oral
Route: multiple
Dose: 480 ug, 2 times / day
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
unhealthy, adult
n = 2127
Health Status: unhealthy
Condition: pain
Age Group: adult
Sex: M+F
Population Size: 2127
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
Disc. AE: Nausea, Vomiting...
AEs leading to
discontinuation/dose reduction:
Nausea (4.4%)
Vomiting (1.6%)
Constipation (0.8%)
Dizziness (1.4%)
Headache (1.1%)
Somnolence (1.1%)
Fatigue (0.8%)
QT interval prolonged (0.5%)
Anxiety (0.5%)
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
32 mg 1 times / day single, oral
Highest studied dose
Dose: 32 mg, 1 times / day
Route: oral
Route: single
Dose: 32 mg, 1 times / day
Sources:
healthy, mean age 32.3 years
n = 4
Health Status: healthy
Age Group: mean age 32.3 years
Sex: M
Population Size: 4
Sources:
0.125 mg 3 times / day multiple, sublingual
Dose: 0.125 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.125 mg, 3 times / day
Sources:
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
Other AEs: Nausea, Vomiting...
Other AEs:
Nausea (below serious, 36 patients)
Vomiting (below serious, 24 patients)
Constipation (below serious, 9 patients)
Dizziness (below serious, 18 patients)
Headache (below serious, 15 patients)
Somnolence (below serious, 6 patients)
Pruritus (below serious, 2 patients)
Hyperhidrosis (below serious, 2 patients)
Oxygen saturation decreased (below serious, 6 patients)
Hot flush (below serious, 2 patients)
Sources:
0.25 mg 3 times / day multiple, sublingual
Dose: 0.25 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.25 mg, 3 times / day
Sources:
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
Other AEs: Nausea, Vomiting...
Other AEs:
Nausea (below serious, 47 patients)
Vomiting (below serious, 33 patients)
Constipation (below serious, 6 patients)
Dizziness (below serious, 26 patients)
Headache (below serious, 23 patients)
Somnolence (below serious, 6 patients)
Pruritus (below serious, 2 patients)
Hyperhidrosis (below serious, 1 patient)
Oxygen saturation decreased (below serious, 8 patients)
Hot flush (below serious, 2 patients)
Sources:
0.5 mg 3 times / day multiple, sublingual
Dose: 0.5 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.5 mg, 3 times / day
Sources:
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
Other AEs: Angioedema, Nausea...
Other AEs:
Angioedema (serious, 1 patient)
Nausea (below serious, 68 patients)
Vomiting (below serious, 59 patients)
Constipation (below serious, 8 patients)
Dizziness (below serious, 44 patients)
Headache (below serious, 13 patients)
Somnolence (below serious, 11 patient)
Pruritus (below serious, 11 patient)
Hyperhidrosis (below serious, 8 patients)
Oxygen saturation decreased (below serious, 7 patients)
Dehydration (below serious, 7 patients)
Hot flush (below serious, 5 patients)
Sources:
AEs

AEs

AESignificanceDosePopulation
Respiratory depression
5.714 ug/kg 1 times / day single, intravenous
Studied dose
Dose: 5.714 ug/kg, 1 times / day
Route: intravenous
Route: single
Dose: 5.714 ug/kg, 1 times / day
Sources:
healthy, 22 to 35 years
n = 5
Health Status: healthy
Age Group: 22 to 35 years
Sex: M
Population Size: 5
Sources:
Anxiety 0.5%
Disc. AE
480 ug 2 times / day multiple, oral (mean)
Recommended
Dose: 480 ug, 2 times / day
Route: oral
Route: multiple
Dose: 480 ug, 2 times / day
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
unhealthy, adult
n = 2127
Health Status: unhealthy
Condition: pain
Age Group: adult
Sex: M+F
Population Size: 2127
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
QT interval prolonged 0.5%
Disc. AE
480 ug 2 times / day multiple, oral (mean)
Recommended
Dose: 480 ug, 2 times / day
Route: oral
Route: multiple
Dose: 480 ug, 2 times / day
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
unhealthy, adult
n = 2127
Health Status: unhealthy
Condition: pain
Age Group: adult
Sex: M+F
Population Size: 2127
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
Constipation 0.8%
Disc. AE
480 ug 2 times / day multiple, oral (mean)
Recommended
Dose: 480 ug, 2 times / day
Route: oral
Route: multiple
Dose: 480 ug, 2 times / day
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
unhealthy, adult
n = 2127
Health Status: unhealthy
Condition: pain
Age Group: adult
Sex: M+F
Population Size: 2127
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
Fatigue 0.8%
Disc. AE
480 ug 2 times / day multiple, oral (mean)
Recommended
Dose: 480 ug, 2 times / day
Route: oral
Route: multiple
Dose: 480 ug, 2 times / day
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
unhealthy, adult
n = 2127
Health Status: unhealthy
Condition: pain
Age Group: adult
Sex: M+F
Population Size: 2127
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
Headache 1.1%
Disc. AE
480 ug 2 times / day multiple, oral (mean)
Recommended
Dose: 480 ug, 2 times / day
Route: oral
Route: multiple
Dose: 480 ug, 2 times / day
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
unhealthy, adult
n = 2127
Health Status: unhealthy
Condition: pain
Age Group: adult
Sex: M+F
Population Size: 2127
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
Somnolence 1.1%
Disc. AE
480 ug 2 times / day multiple, oral (mean)
Recommended
Dose: 480 ug, 2 times / day
Route: oral
Route: multiple
Dose: 480 ug, 2 times / day
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
unhealthy, adult
n = 2127
Health Status: unhealthy
Condition: pain
Age Group: adult
Sex: M+F
Population Size: 2127
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
Dizziness 1.4%
Disc. AE
480 ug 2 times / day multiple, oral (mean)
Recommended
Dose: 480 ug, 2 times / day
Route: oral
Route: multiple
Dose: 480 ug, 2 times / day
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
unhealthy, adult
n = 2127
Health Status: unhealthy
Condition: pain
Age Group: adult
Sex: M+F
Population Size: 2127
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
Vomiting 1.6%
Disc. AE
480 ug 2 times / day multiple, oral (mean)
Recommended
Dose: 480 ug, 2 times / day
Route: oral
Route: multiple
Dose: 480 ug, 2 times / day
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
unhealthy, adult
n = 2127
Health Status: unhealthy
Condition: pain
Age Group: adult
Sex: M+F
Population Size: 2127
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
Nausea 4.4%
Disc. AE
480 ug 2 times / day multiple, oral (mean)
Recommended
Dose: 480 ug, 2 times / day
Route: oral
Route: multiple
Dose: 480 ug, 2 times / day
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
unhealthy, adult
n = 2127
Health Status: unhealthy
Condition: pain
Age Group: adult
Sex: M+F
Population Size: 2127
Sources: Page: nda/2015/207932Orig1s000MedR.pdf - p.53
Headache below serious, 15 patients
0.125 mg 3 times / day multiple, sublingual
Dose: 0.125 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.125 mg, 3 times / day
Sources:
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
Dizziness below serious, 18 patients
0.125 mg 3 times / day multiple, sublingual
Dose: 0.125 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.125 mg, 3 times / day
Sources:
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
Hot flush below serious, 2 patients
0.125 mg 3 times / day multiple, sublingual
Dose: 0.125 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.125 mg, 3 times / day
Sources:
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
Hyperhidrosis below serious, 2 patients
0.125 mg 3 times / day multiple, sublingual
Dose: 0.125 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.125 mg, 3 times / day
Sources:
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
Pruritus below serious, 2 patients
0.125 mg 3 times / day multiple, sublingual
Dose: 0.125 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.125 mg, 3 times / day
Sources:
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
Vomiting below serious, 24 patients
0.125 mg 3 times / day multiple, sublingual
Dose: 0.125 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.125 mg, 3 times / day
Sources:
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
Nausea below serious, 36 patients
0.125 mg 3 times / day multiple, sublingual
Dose: 0.125 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.125 mg, 3 times / day
Sources:
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
Oxygen saturation decreased below serious, 6 patients
0.125 mg 3 times / day multiple, sublingual
Dose: 0.125 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.125 mg, 3 times / day
Sources:
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
Somnolence below serious, 6 patients
0.125 mg 3 times / day multiple, sublingual
Dose: 0.125 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.125 mg, 3 times / day
Sources:
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
Constipation below serious, 9 patients
0.125 mg 3 times / day multiple, sublingual
Dose: 0.125 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.125 mg, 3 times / day
Sources:
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
Hyperhidrosis below serious, 1 patient
0.25 mg 3 times / day multiple, sublingual
Dose: 0.25 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.25 mg, 3 times / day
Sources:
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
Hot flush below serious, 2 patients
0.25 mg 3 times / day multiple, sublingual
Dose: 0.25 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.25 mg, 3 times / day
Sources:
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
Pruritus below serious, 2 patients
0.25 mg 3 times / day multiple, sublingual
Dose: 0.25 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.25 mg, 3 times / day
Sources:
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
Headache below serious, 23 patients
0.25 mg 3 times / day multiple, sublingual
Dose: 0.25 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.25 mg, 3 times / day
Sources:
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
Dizziness below serious, 26 patients
0.25 mg 3 times / day multiple, sublingual
Dose: 0.25 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.25 mg, 3 times / day
Sources:
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
Vomiting below serious, 33 patients
0.25 mg 3 times / day multiple, sublingual
Dose: 0.25 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.25 mg, 3 times / day
Sources:
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
Nausea below serious, 47 patients
0.25 mg 3 times / day multiple, sublingual
Dose: 0.25 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.25 mg, 3 times / day
Sources:
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
Constipation below serious, 6 patients
0.25 mg 3 times / day multiple, sublingual
Dose: 0.25 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.25 mg, 3 times / day
Sources:
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
Somnolence below serious, 6 patients
0.25 mg 3 times / day multiple, sublingual
Dose: 0.25 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.25 mg, 3 times / day
Sources:
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
Oxygen saturation decreased below serious, 8 patients
0.25 mg 3 times / day multiple, sublingual
Dose: 0.25 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.25 mg, 3 times / day
Sources:
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
Pruritus below serious, 11 patient
0.5 mg 3 times / day multiple, sublingual
Dose: 0.5 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.5 mg, 3 times / day
Sources:
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
Somnolence below serious, 11 patient
0.5 mg 3 times / day multiple, sublingual
Dose: 0.5 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.5 mg, 3 times / day
Sources:
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
Headache below serious, 13 patients
0.5 mg 3 times / day multiple, sublingual
Dose: 0.5 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.5 mg, 3 times / day
Sources:
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
Dizziness below serious, 44 patients
0.5 mg 3 times / day multiple, sublingual
Dose: 0.5 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.5 mg, 3 times / day
Sources:
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
Hot flush below serious, 5 patients
0.5 mg 3 times / day multiple, sublingual
Dose: 0.5 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.5 mg, 3 times / day
Sources:
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
Vomiting below serious, 59 patients
0.5 mg 3 times / day multiple, sublingual
Dose: 0.5 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.5 mg, 3 times / day
Sources:
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
Nausea below serious, 68 patients
0.5 mg 3 times / day multiple, sublingual
Dose: 0.5 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.5 mg, 3 times / day
Sources:
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
Dehydration below serious, 7 patients
0.5 mg 3 times / day multiple, sublingual
Dose: 0.5 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.5 mg, 3 times / day
Sources:
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
Oxygen saturation decreased below serious, 7 patients
0.5 mg 3 times / day multiple, sublingual
Dose: 0.5 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.5 mg, 3 times / day
Sources:
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
Constipation below serious, 8 patients
0.5 mg 3 times / day multiple, sublingual
Dose: 0.5 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.5 mg, 3 times / day
Sources:
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
Hyperhidrosis below serious, 8 patients
0.5 mg 3 times / day multiple, sublingual
Dose: 0.5 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.5 mg, 3 times / day
Sources:
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
Angioedema serious, 1 patient
0.5 mg 3 times / day multiple, sublingual
Dose: 0.5 mg, 3 times / day
Route: sublingual
Route: multiple
Dose: 0.5 mg, 3 times / day
Sources:
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
OverviewDrug as perpetrator​Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
yes
yes
yes
yes
yes
yes
yes
yes
yes
Tox targets
PubMed

PubMed

TitleDatePubMed
Opioid antagonists for smoking cessation.
2001
[Use of buprenorphine as a substitute treatment for opiate dependence in the Toxicology Clinics--introductory clinical report].
2001
Buprenorphine treatment of heroin dependence (detoxification and maintenance) in a private practice setting.
2001
Treatment of opioid addiction in physicians' offices: it's about time.
2001
[Two-year follow-up of an opioid-user cohort treated with high-dose buprenorphine (Subutex)].
2001 Apr
[Reduction in the number of lethal heroin overdoses in France since 1994. Focus on substitution treatments].
2001 Apr
Intranasal bioavailability of buprenorphine in rabbit correlated to sheep and man.
2001 Apr 17
Simultaneous determination of buprenorphine, norbuprenorphine, and buprenorphine-glucuronide in plasma by liquid chromatography-tandem mass spectrometry.
2001 Apr 25
Rapid heroin detoxification using a single high dose of buprenorphine.
2001 Apr-Jun
[The influence of age on hemodynamics and the dose requirements of propofol and buprenorphine in total intravenous anesthesia combined with continuous epidural anesthesia].
2001 Aug
Office-based treatment for opioid dependence: reaching new patient populations.
2001 Aug
Effect of perinatal buprenorphine exposure on development in the rat.
2001 Aug
Buprenorphine sublingual tablets: effects on IV heroin self-administration by humans.
2001 Feb
Hepatitis after intravenous buprenorphine misuse in heroin addicts.
2001 Feb
Mechanisms for experimental buprenorphine hepatotoxicity: major role of mitochondrial dysfunction versus metabolic activation.
2001 Feb
Treating opioid dependence.
2001 Feb 15
[The influence of age on hemodynamics and the dose requirements of propofol and buprenorphine in total intravenous anesthesia].
2001 Jan
Agonists determine the pattern of G-protein activation in mu-opioid receptor-mediated supraspinal analgesia.
2001 Jan 15
[The effect of intravenous patient controlled analgesia on activities of daily life and medical expense after thoracotomy].
2001 Jul
Influence of buprenorphine analgesia on post-operative recovery in two strains of rats.
2001 Jul
Testing and comparison of non-opioid analgesics in amphibians.
2001 Jul
The antinociceptive effect of the combination of spinal morphine with systemic morphine or buprenorphine.
2001 Jul
Response expectancies in placebo analgesia and their clinical relevance.
2001 Jul
Effects of indatraline and buprenorphine on self-administration of speedball combinations of cocaine and heroin by rhesus monkeys.
2001 Jul
Pain intolerance in opioid-maintained former opiate addicts: effect of long-acting maintenance agent.
2001 Jul 1
Buprenorphine added to the local anesthetic for brachial plexus block to provide postoperative analgesia in outpatients.
2001 Jul-Aug
Port-site recurrence reproduced in the VX-2 rabbit carcinoma model: an in vivo model comparing laparoscopic port sites and open incisions.
2001 Jul-Sep
[Usefulness of epidural infusion of ketamine for relief of localized superficial pain].
2001 Jun
Three-choice discrimination in pigeons is based on relative efficacy differences among opioids.
2001 Jun
Narcotic analgesia in the acute abdomen--a review of prospective trials.
2001 Jun
Analysis of opioid binding to UDP-glucuronosyltransferase 2B7 fusion proteins using nuclear magnetic resonance spectroscopy.
2001 Jun
Electrically-assisted transdermal delivery of buprenorphine.
2001 Jun 15
SUNCT syndrome: a treatment option with local opioid blockade of the superior cervical ganglion? A case report.
2001 Mar
Observation of psychoactive substance consumption: methods and results of the French OPPIDUM programme.
2001 Mar
[Dose-response study of preincisional buprenorphine on emergence time and postoperative analgesic requirement in patients anesthetized with sevoflurane].
2001 Mar
Development and validation of a sensitive analytical method for the simultaneous determination of buprenorphine and norbuprenorphine in human plasma.
2001 Mar
Perinatal opioids reduce striatal nerve growth factor content in rat striatum.
2001 Mar 2
[Anesthetic management of two patients with essential thrombocythemia].
2001 May
Antinociceptive activity of and clinical experience with buprenorphine in swine.
2001 May
A meta-analysis comparing buprenorphine to methadone for treatment of opiate dependence.
2001 May
The effects of chronic morphine on behavior reinforced by several opioids or by cocaine in rhesus monkeys.
2001 May 1
Perceptual and motor effects of morphine and buprenorphine in baboons.
2001 May-Jun
Hydrolysis of conjugated metabolites of buprenorphine. I. The quantitative enzymatic hydrolysis of buprenorphine-3-beta-D-glucuronide in human urine.
2001 Oct
Opioid maintenance: the politics matter.
2001 Oct
Cost-effectiveness estimates for buprenorphine should factor in crime.
2001 Oct
Buprenorphine: better late than never.
2001 Oct 1
[Treatment of heroin addiction--clinical findings hand-in-hand with evidence].
2001 Oct 10
The cost-effectiveness of buprenorphine maintenance therapy for opiate addiction in the United States.
2001 Sep
Limits to buprenorphine dosing: a comparison between quintuple and sextuple the maintenance dose every 5 days.
2001 Sep 1
Gradual dose taper following chronic buprenorphine.
2001 Spring
Patents

Sample Use Guides

The initial starting dose is 1 mL buprenorphine hydrochloride injection (0.3 mg buprenorphine) given by deep intramuscular or slow (over at least 2 minutes) intravenous injection at up to 6-hour intervals, as needed. Repeat once (up to 0.3 mg) if required, 30 to 60 minutes after initial dosage, giving consideration to previous dose pharmacokinetics, and thereafter only as needed. In high-risk patients (e.g., elderly, debilitated, presence of respiratory disease, etc.) and/or in patients where other CNS depressants are present, such as in the immediate postoperative period, the dose should be limited to the minimum required. Buprenorphine hydrochloride has been used in pediatric patients 2 to 12 years of age at doses between 2 to 6 micrograms/kg of body weight given every 4 to 6 hours. There is insufficient experience to recommend a dose in infants below the age of two years, single doses greater than 6 micrograms/kg of body weight, or the use of a repeat or second dose at 30 to 60 minutes (such as is used in adults).
Route of Administration: Other
Functional activity of μ receptors in intact cells was determined by measuring receptor-induced membrane potential change, which can be directly read by Molecular Devices Membrane Potential Assay Kit (Blue Dye) using the FlexStation 3® microplate reader. CHO cells transfected with human μ-opioid receptors were seeded in a 96-well plate (30 000 cells per well) 1 day prior to the experiments. For agonist assays, after brief washing, the cells were loaded with 225 μL of HBSS assay buffer (HBSS with 20 mM of HEPES, pH 7.4), containing the blue dye, and incubated at 37°C. After 30 min, 25 μL of the Buprenorphine were automatically dispensed into the wells by the FlexStation and receptor stimulation-mediated membrane potential change is recorded every 3 s for 60 s by reading 550–565 nm fluorescence excited at 530 nm wavelength.
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:14:44 UTC 2021
Edited
by admin
on Fri Jun 25 21:14:44 UTC 2021
Record UNII
40D3SCR4GZ
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
BUPRENORPHINE
EMA EPAR   EP   INN   JAN   MART.   MI   ORANGE BOOK   VANDF   WHO-DD  
INN  
Official Name English
SUBLOCADE
Brand Name English
BUPRENORPHINE [JAN]
Common Name English
BUPRENORPHINE [EP]
Common Name English
BUPRENORPHINE [EMA EPAR]
Common Name English
SUBOXONE
Brand Name English
BUPRENORPHINE [VANDF]
Common Name English
BUPRENORPHINE [ORANGE BOOK]
Common Name English
BUPRENORPHINE [EP MONOGRAPH]
Common Name English
BUPRENORPHINE [INN]
Common Name English
BUPRENORPHIN
Common Name English
BUPRENORPHINE [WHO-DD]
Common Name English
BUPRENORPHINE [MI]
Common Name English
BUPRENORPHINE [MART.]
Common Name English
BUTRANS
Brand Name English
PROBUPHINE
Brand Name English
BRIXADI
Brand Name English
ALKS-5461 COMPONENT BUPRENORPHINE
Code English
TEMGESIC
Brand Name English
Classification Tree Code System Code
WHO-VATC QN07BC51
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
NDF-RT N0000175685
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
WHO-ATC N07BC01
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
LIVERTOX 127
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
NDF-RT N0000175689
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
DEA NO. 9064
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
NCI_THESAURUS C1506
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
WHO-ATC N02AE01
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
NCI_THESAURUS C67413
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
FDA ORPHAN DRUG 79093
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
EMA ASSESSMENT REPORTS SUBOXONE (AUTHORIZED: OPIOID-RELATED DISEASES)
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
WHO-ATC N07BC51
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
WHO-VATC QN07BC01
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
WHO-VATC QN02AE01
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
Code System Code Type Description
PUBCHEM
644073
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
PRIMARY
IUPHAR
1670
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
PRIMARY
ChEMBL
CHEMBL511142
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
PRIMARY
ECHA (EC/EINECS)
257-950-6
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
PRIMARY
NCI_THESAURUS
C61656
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
PRIMARY
RXCUI
1819
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
PRIMARY RxNorm
MESH
D002047
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
PRIMARY
MERCK INDEX
M2771
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
PRIMARY Merck Index
INN
3403
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
PRIMARY
WIKIPEDIA
BUPRENORPHINE
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
PRIMARY
FDA UNII
40D3SCR4GZ
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
PRIMARY
DRUG CENTRAL
434
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
PRIMARY
LACTMED
Buprenorphine
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
PRIMARY
CAS
52485-79-7
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
PRIMARY
EVMPD
SUB05985MIG
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
PRIMARY
EPA CompTox
52485-79-7
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
PRIMARY
DRUG BANK
DB00921
Created by admin on Fri Jun 25 21:14:44 UTC 2021 , Edited by admin on Fri Jun 25 21:14:44 UTC 2021
PRIMARY
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SALT/SOLVATE -> PARENT
TARGET->PARTIAL AGONIST
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METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
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