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

Details

Stereochemistry ABSOLUTE
Molecular Formula C29H41NO4
Molecular Weight 467.6401
Optical Activity UNSPECIFIED
Defined Stereocenters 7 / 7
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BUPRENORPHINE

SMILES

[H][C@@]12OC3=C4C(C[C@H]5N(CC6CC6)CC[C@@]14[C@@]57CC[C@@]2(OC)[C@]([H])(C7)[C@](C)(O)C(C)(C)C)=CC=C3O

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 467.6401
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 7 / 7
E/Z Centers 0
Optical Activity UNSPECIFIED

Description

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.

CNS Activity

Originator

Approval Year

1981
137
Targets

Targets

Primary TargetPharmacologyConditionPotency
Partial Agonist
283
 1.5 nM [Ki]
Antagonist
2737
 2.5 nM [Ki]
Antagonist
2737
 6.1 nM [Ki]
Nociceptin receptor
14
Target ID: P41146
Gene ID: 4987.0
Gene Symbol: OPRL1
Target Organism: Homo sapiens (Human)
Partial Agonist
283
 77.4 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8307
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
Approved
8307
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
Phase IV
63
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
Phase IV
63
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
Phase IV
63
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
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/207932s012lbl.pdf
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
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/207932s012lbl.pdf
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
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/207932s012lbl.pdf
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%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/207932s012lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207932s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/16547090/
healthy, 22 to 35 years
n = 5
Health Status: healthy
Age Group: 22 to 35 years
Sex: M
Population Size: 5
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207932s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/16547090/
Other AEs: Respiratory depression...
Other AEs:
Respiratory depression
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207932s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/16547090/
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://pubmed.ncbi.nlm.nih.gov/8181201/
healthy, mean age 32.3 years
n = 4
Health Status: healthy
Age Group: mean age 32.3 years
Sex: M
Population Size: 4
Sources:
https://pubmed.ncbi.nlm.nih.gov/8181201/
Sources:
https://pubmed.ncbi.nlm.nih.gov/8181201/
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207932s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/16547090/
healthy, 22 to 35 years
n = 5
Health Status: healthy
Age Group: 22 to 35 years
Sex: M
Population Size: 5
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207932s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/16547090/
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207932Orig1s000MedR.pdf
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 82
Health Status: unhealthy
Condition: postoperative pain
Population Size: 82
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 80
Health Status: unhealthy
Condition: postoperative pain
Population Size: 80
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
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:
https://clinicaltrials.gov/ct2/show/NCT02634788
unhealthy
n = 81
Health Status: unhealthy
Condition: postoperative pain
Population Size: 81
Sources:
https://clinicaltrials.gov/ct2/show/NCT02634788
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1670

inhibitor
1532
substrate
985
substrate
1168

inhibitor
1789
inhibitor
1570

OverviewOther

Other InhibitorOther SubstrateOther Inducer
Nav1.7
36

Cav1.2
45

Nav1.5
95

P-gp
1401

BCRP
678

CYP1A
71

CYP2B6
770

CYP2C19
1410

CYP2C8/9
43

CYP2E1
846
P-gp
1491

CYP1A1
344

CYP1A2
1013

CYP2A6
510

CYP2B6
648

CYP2C8
670

CYP2C18
138

CYP2C19
955

CYP2E1
633

CYP3A5
383

CYP3A7
110

UGT1A1
417

UGT1A3
421

UGT1A4
345

UGT1A6
306

UGT1A9
378

UGT2B7
387

UGT2B17
212
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP3A4
1857
 strong [Ki 14.7 uM]
CYP2D6
1826
 strong [Ki 21.4 uM]
CYP1A
119
 weak [Ki 132 uM]
CYP2B6
946
 weak [Ki 133 uM]
CYP2C19
1484
 weak [Ki 146 uM]
CYP2C8/9
43
 weak [Ki >300 uM]
CYP2E1
929
 weak [Ki >300 uM]
Nav1.7
36
 yes [IC50 47 uM]
BCRP
751
 yes
P-gp
1588
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP1A1
344
 no
CYP1A2
1013
 no
CYP2A6
510
 no
CYP2B6
648
 no
CYP2C18
138
 no
CYP2C19
955
 no
CYP2C9
985
 no
CYP2E1
633
 no
P-gp
1491
 no
UGT1A4
345
 no
UGT1A6
306
 no
UGT1A9
378
 no
CYP2C8
670
 yes
CYP2D6
1168
 yes
CYP3A4
1670
 yes
CYP3A5
383
 yes
CYP3A7
110
 yes
UGT1A1
417
 yes
UGT1A3
421
 yes
UGT2B17
212
 yes
UGT2B7
387
 yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
Cav1.2
49
Nav1.5
98
hERG
1603
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:3216
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:3216
ZINC
ZINC000001319780
http://zinc15.docking.org/substances/ZINC000001319780
PubMed

PubMed

TitleDatePubMed
Agonistic effects of the opioid buprenorphine on the nociceptin/OFQ receptor.
2000 Jul
Disulfiram and buprenorphine for treating cocaine addiction.
2000 Jul
Thrice-weekly versus daily buprenorphine maintenance.
2000 Jun 15
Relationship between cocaine-induced hepatotoxic neurobehavioral & biochemical changes in mice: the antidotal effects of buprenorphine.
2000 May 26
A comparison of levomethadyl acetate, buprenorphine, and methadone for opioid dependence.
2000 Nov 2
Dilated bile duct in patients receiving narcotic substitution: an early report.
2000 Sep
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
Simultaneous determination of buprenorphine, norbuprenorphine, and buprenorphine-glucuronide in plasma by liquid chromatography-tandem mass spectrometry.
2001 Apr 25
[The benefit of combining spinal morphine and intravenous buprenorphine for perioperative pain].
2001 Aug
Effect of perinatal buprenorphine exposure on development in the rat.
2001 Aug
Treating opioid dependence.
2001 Feb 15
Buprenorphine substitution ameliorates spontaneous withdrawal in fentanyl-dependent rat pups.
2001 Jan
Thrice-weekly supervised dosing with the combination buprenorphine-naloxone tablet is preferred to daily supervised dosing by opioid-dependent humans.
2001 Jan 1
Deaths attributable to methadone vs buprenorphine in France.
2001 Jan 3
Testing and comparison of non-opioid analgesics in amphibians.
2001 Jul
[Usefulness of epidural infusion of ketamine for relief of localized superficial pain].
2001 Jun
Narcotic analgesia in the acute abdomen--a review of prospective trials.
2001 Jun
The use of analgesic drugs by South African veterinarians.
2001 Mar
Effects of buprenorphine/naloxone in opioid-dependent humans.
2001 Mar
Inefficacy of buprrenorphine in rats.
2001 Mar
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
[Continuous epidural administration of droperidol for the prevention of postoperative nausea].
2001 Sep
Effect of epidural analgesia on postoperative paralytic ileus in chronic schizophrenia.
2001 Sep-Oct
Patents

Patents

JP2003515526A
454
JP2004534002A
17
JP2004536811A
35
JP2009242415A
4
JP2013543488A
4
JP4790219B2
12
JPH03163014A
4

Sample Use Guides

In Vivo Use Guide
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
In Vitro Use Guide
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 Dec 16 16:33:27 UTC 2022
Edited
by admin
on Fri Dec 16 16:33:27 UTC 2022
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 [EMA EPAR]
Common Name English
SUBOXONE
Brand Name English
Buprenorphine [WHO-DD]
Common 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 [MI]
Common Name English
BUPRENORPHINE [MART.]
Common Name English
BUTRANS
Brand Name English
PROBUPHINE
Brand Name English
BRIXADI
Brand Name English
BUPRENORPHINE [EP IMPURITY]
Common 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 Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
NDF-RT N0000175685
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
WHO-ATC N07BC01
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
LIVERTOX NBK548871
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
NDF-RT N0000175689
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
DEA NO. 9064
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
NCI_THESAURUS C1506
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
WHO-ATC N02AE01
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
NCI_THESAURUS C67413
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
FDA ORPHAN DRUG 79093
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
EMA ASSESSMENT REPORTS SUBOXONE (AUTHORIZED: OPIOID-RELATED DISEASES)
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
WHO-ATC N07BC51
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
WHO-VATC QN07BC01
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
WHO-VATC QN02AE01
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
FDA ORPHAN DRUG 541116
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
Code System Code Type Description
PUBCHEM
644073
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
PRIMARY
IUPHAR
1670
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
PRIMARY
ChEMBL
CHEMBL511142
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
PRIMARY
ECHA (EC/EINECS)
257-950-6
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
PRIMARY
NCI_THESAURUS
C61656
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
PRIMARY
RXCUI
1819
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
PRIMARY RxNorm
MESH
D002047
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
PRIMARY
MERCK INDEX
M2771
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
PRIMARY Merck Index
INN
3403
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
PRIMARY
WIKIPEDIA
BUPRENORPHINE
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
PRIMARY
FDA UNII
40D3SCR4GZ
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
PRIMARY
DRUG CENTRAL
434
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
PRIMARY
LACTMED
Buprenorphine
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
PRIMARY
DAILYMED
40D3SCR4GZ
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
PRIMARY
CAS
52485-79-7
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
PRIMARY
EVMPD
SUB05985MIG
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
PRIMARY
CHEBI
3216
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
PRIMARY
EPA CompTox
DTXSID2022705
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
PRIMARY
DRUG BANK
DB00921
Created by admin on Fri Dec 16 16:33:27 UTC 2022 , Edited by admin on Fri Dec 16 16:33:27 UTC 2022
PRIMARY
Related Record Type Details
CYTOCHROME P450 2C8
METABOLIC ENZYME -> SUBSTRATE
Structure of BUPRENORPHINE HYDROCHLORIDE
SALT/SOLVATE -> PARENT
MU-TYPE OPIOID RECEPTOR
TARGET->PARTIAL AGONIST
PARTIAL AGONIST
BINDING
Ki
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
CYTOCHROME P450 3A7
METABOLIC ENZYME -> SUBSTRATE
Structure of BUPRENORPHINE 3-HEXANOATE
DERIVATIVE -> PARENT
DELTA-TYPE OPIOID RECEPTOR
TARGET -> INHIBITOR
BINDING
Ki
KAPPA-TYPE OPIOID RECEPTOR
TARGET -> INHIBITOR
BINDING
Ki
CYTOCHROME P450 3A5
METABOLIC ENZYME -> SUBSTRATE
DELTA-TYPE OPIOID RECEPTOR
TARGET -> AGONIST
Related Record Type Details
Structure of BUPRENORPHINE 3-GLUCURONIDE
METABOLITE ACTIVE -> PARENT
receptor binding and pharmacological activity
Structure of NORBUPRENORPHINE
METABOLITE ACTIVE -> PARENT
FECAL; URINE
Structure of NORBUPRENORPHINE 3-GLUCURONIDE
METABOLITE -> PARENT
receptor binding and pharmacological activity
Related Record Type Details
Structure of BUPRENORPHINE
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
For language access assistance, contact the NCATS Public Information Officer
National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966