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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]
6.09999999999999964 nM [Ki]
Target ID: P41146
Gene ID: 4987
Gene Symbol: OPRL1
Target Organism: Homo sapiens (Human)
77.4000000000000057 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

1277856000000
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

1277856000000
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

1277856000000
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

1277856000000
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

1277856000000
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
Other AEs: Respiratory depression...
480 ug 2 times / day multiple, oral
Recommended
Dose: 480 ug, 2 times / day
Route: oral
Route: multiple
Dose: 480 ug, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
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
Health Status: healthy
Age Group: mean age 32.3 years
Sex: M
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Anxiety 0.5%
Disc. AE
480 ug 2 times / day multiple, oral
Recommended
Dose: 480 ug, 2 times / day
Route: oral
Route: multiple
Dose: 480 ug, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
QT interval prolonged 0.5%
Disc. AE
480 ug 2 times / day multiple, oral
Recommended
Dose: 480 ug, 2 times / day
Route: oral
Route: multiple
Dose: 480 ug, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Constipation 0.8%
Disc. AE
480 ug 2 times / day multiple, oral
Recommended
Dose: 480 ug, 2 times / day
Route: oral
Route: multiple
Dose: 480 ug, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Fatigue 0.8%
Disc. AE
480 ug 2 times / day multiple, oral
Recommended
Dose: 480 ug, 2 times / day
Route: oral
Route: multiple
Dose: 480 ug, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Headache 1.1%
Disc. AE
480 ug 2 times / day multiple, oral
Recommended
Dose: 480 ug, 2 times / day
Route: oral
Route: multiple
Dose: 480 ug, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Somnolence 1.1%
Disc. AE
480 ug 2 times / day multiple, oral
Recommended
Dose: 480 ug, 2 times / day
Route: oral
Route: multiple
Dose: 480 ug, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Dizziness 1.4%
Disc. AE
480 ug 2 times / day multiple, oral
Recommended
Dose: 480 ug, 2 times / day
Route: oral
Route: multiple
Dose: 480 ug, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Vomiting 1.6%
Disc. AE
480 ug 2 times / day multiple, oral
Recommended
Dose: 480 ug, 2 times / day
Route: oral
Route: multiple
Dose: 480 ug, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Nausea 4.4%
Disc. AE
480 ug 2 times / day multiple, oral
Recommended
Dose: 480 ug, 2 times / day
Route: oral
Route: multiple
Dose: 480 ug, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
Health Status: unhealthy
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
[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
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
Age-related differences in sensitivity to the antinociceptive effects of opioids in male rats. Influence of nociceptive intensity and intrinsic efficacy at the mu receptor.
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 for opiate addiction: potential economic impact.
2001 Aug 1
[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
Stimulation of guanosine-5'-o-(3-[35S]thio)triphosphate binding in digitonin-permeabilized C6 rat glioma cells: evidence for an organized association of mu-opioid receptors and G protein.
2001 Jul
Response expectancies in placebo analgesia and their clinical relevance.
2001 Jul
Lack of effect of single high doses of buprenorphine on arterial blood gases in the rat.
2001 Jul
Effects of indatraline and buprenorphine on self-administration of speedball combinations of cocaine and heroin by rhesus monkeys.
2001 Jul
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
An exploratory study of buprenorphine use in Bangladesh: a note.
2001 Jun
Epidural analgesia with a combination of bupivacaine and buprenorphine in rats.
2001 Jun
[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
A new era in opioid dependency treatment. Recent law allows qualified physicians to provide care in office setting.
2001 Jun
Examining the limits of the buprenorphine interdosing interval: daily, every-third-day and every-fifth-day dosing regimens.
2001 Jun
Electrically-assisted transdermal delivery of buprenorphine.
2001 Jun 15
The use of analgesic drugs by South African veterinarians.
2001 Mar
SUNCT syndrome: a treatment option with local opioid blockade of the superior cervical ganglion? A case report.
2001 Mar
[Acute hepatitis following intravenous buprenorphine injection as a substitute drug in a drug-addict].
2001 Mar
[Anesthetic management of two patients with essential thrombocythemia].
2001 May
[Review of scientific evidence on alternatives to methadone in the psychopharmacologic treatment of opiate dependence].
2001 May-Jun
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 of buprenorphine maintenance versus methadone maintenance.
2001 Oct
Cost-effectiveness estimates for buprenorphine should factor in crime.
2001 Oct
Comparison of methadone and high dosage buprenorphine users in French care centres.
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
[Continuous epidural administration of droperidol for the prevention of postoperative nausea].
2001 Sep
Preoperative blood pressure and intraoperative hypothermia during lower abdominal surgery.
2001 Sep
Effects of medetomidine and buprenorphine administered for sedation in dogs.
2001 Sep
HS-599: a novel long acting opioid analgesic does not induce place-preference in rats.
2001 Sep
Limits to buprenorphine dosing: a comparison between quintuple and sextuple the maintenance dose every 5 days.
2001 Sep 1
Deaths involving buprenorphine: a compendium of French cases.
2001 Sep 15
Effect of epidural analgesia on postoperative paralytic ileus in chronic schizophrenia.
2001 Sep-Oct
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.
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
Related Record Type Details
METABOLIC ENZYME -> SUBSTRATE
SALT/SOLVATE -> PARENT
TARGET->PARTIAL AGONIST
PARTIAL AGONIST
BINDING
Ki
TARGET -> AGONIST
BINDER->LIGAND
BINDING
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
DERIVATIVE -> PARENT
TARGET -> INHIBITOR
BINDING
Ki
TARGET -> INHIBITOR
BINDING
Ki
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
METABOLITE ACTIVE -> PARENT
receptor binding and pharmacological activity
METABOLITE ACTIVE -> PARENT
FECAL; URINE
METABOLITE -> PARENT
receptor binding and pharmacological activity
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC