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Details

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

SHOW SMILES / InChI
Structure of Buprenorphine

SMILES

CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]4CC5=C6C(O[C@@H]2[C@@]36CCN4CC7CC7)=C(O)C=C5

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

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

2010
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

2010
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

2010
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

2010
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

2010
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:
PubMed

PubMed

TitleDatePubMed
[Treatment of heroin addiction--clinical findings hand-in-hand with evidence].
2001-10-10
Buprenorphine: better late than never.
2001-10-01
Hydrolysis of conjugated metabolites of buprenorphine. I. The quantitative enzymatic hydrolysis of buprenorphine-3-beta-D-glucuronide in human urine.
2001-10
Opioid maintenance: the politics matter.
2001-10
Cost-effectiveness of buprenorphine maintenance versus methadone maintenance.
2001-10
Cost-effectiveness estimates for buprenorphine should factor in crime.
2001-10
Comparison of methadone and high dosage buprenorphine users in French care centres.
2001-10
Effect of epidural analgesia on postoperative paralytic ileus in chronic schizophrenia.
2001-09-19
Deaths involving buprenorphine: a compendium of French cases.
2001-09-15
[Use of a new drug in the treatment of heroin addicts should not be obstructed by political dogmatism].
2001-09-12
Port-site recurrence reproduced in the VX-2 rabbit carcinoma model: an in vivo model comparing laparoscopic port sites and open incisions.
2001-09-11
Limits to buprenorphine dosing: a comparison between quintuple and sextuple the maintenance dose every 5 days.
2001-09-01
The cost-effectiveness of buprenorphine maintenance therapy for opiate addiction in the United States.
2001-09
[Continuous epidural administration of droperidol for the prevention of postoperative nausea].
2001-09
Preoperative blood pressure and intraoperative hypothermia during lower abdominal surgery.
2001-09
Effects of medetomidine and buprenorphine administered for sedation in dogs.
2001-09
HS-599: a novel long acting opioid analgesic does not induce place-preference in rats.
2001-09
[Buprenorphine in pregnancy].
2001-09
[Review of scientific evidence on alternatives to methadone in the psychopharmacologic treatment of opiate dependence].
2001-08-23
[A national model for drug-supported rehabilitation of opiate addicts].
2001-08-20
Buprenorphine for opiate addiction: potential economic impact.
2001-08-01
[The influence of age on hemodynamics and the dose requirements of propofol and buprenorphine in total intravenous anesthesia combined with continuous epidural anesthesia].
2001-08
[The benefit of combining spinal morphine and intravenous buprenorphine for perioperative pain].
2001-08
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.
2001-08
Office-based treatment for opioid dependence: reaching new patient populations.
2001-08
Effect of perinatal buprenorphine exposure on development in the rat.
2001-08
Rapid heroin detoxification using a single high dose of buprenorphine.
2001-07-31
Buprenorphine added to the local anesthetic for brachial plexus block to provide postoperative analgesia in outpatients.
2001-07-21
Opioid chronopharmacology.
2001-07
[The effect of intravenous patient controlled analgesia on activities of daily life and medical expense after thoracotomy].
2001-07
Influence of buprenorphine analgesia on post-operative recovery in two strains of rats.
2001-07
Testing and comparison of non-opioid analgesics in amphibians.
2001-07
The antinociceptive effect of the combination of spinal morphine with systemic morphine or buprenorphine.
2001-07
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.
2001-07
Perceptual and motor effects of morphine and buprenorphine in baboons.
2001-06-23
Electrically-assisted transdermal delivery of buprenorphine.
2001-06-15
An exploratory study of buprenorphine use in Bangladesh: a note.
2001-06
Epidural analgesia with a combination of bupivacaine and buprenorphine in rats.
2001-06
[Usefulness of epidural infusion of ketamine for relief of localized superficial pain].
2001-06
Three-choice discrimination in pigeons is based on relative efficacy differences among opioids.
2001-06
Narcotic analgesia in the acute abdomen--a review of prospective trials.
2001-06
A new era in opioid dependency treatment. Recent law allows qualified physicians to provide care in office setting.
2001-06
[Anesthetic management of two patients with essential thrombocythemia].
2001-05
[Two-year follow-up of an opioid-user cohort treated with high-dose buprenorphine (Subutex)].
2001-04
[Reduction in the number of lethal heroin overdoses in France since 1994. Focus on substitution treatments].
2001-04
The use of analgesic drugs by South African veterinarians.
2001-03
SUNCT syndrome: a treatment option with local opioid blockade of the superior cervical ganglion? A case report.
2001-03
Opioid antagonists for smoking cessation.
2001
[Use of buprenorphine as a substitute treatment for opiate dependence in the Toxicology Clinics--introductory clinical report].
2001
Gradual dose taper following chronic buprenorphine.
2001
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 Mon Mar 31 17:50:57 GMT 2025
Edited
by admin
on Mon Mar 31 17:50:57 GMT 2025
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
PROBUPHINE
Preferred 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
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 Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
NDF-RT N0000175685
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
WHO-ATC N07BC01
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
LIVERTOX NBK548871
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
NDF-RT N0000175689
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
DEA NO. 9064
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
NCI_THESAURUS C1506
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
WHO-ATC N02AE01
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
NCI_THESAURUS C67413
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
FDA ORPHAN DRUG 79093
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
EMA ASSESSMENT REPORTS SUBOXONE (AUTHORIZED: OPIOID-RELATED DISEASES)
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
WHO-ATC N07BC51
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
WHO-VATC QN07BC01
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
WHO-VATC QN02AE01
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
FDA ORPHAN DRUG 541116
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
Code System Code Type Description
PUBCHEM
644073
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
PRIMARY
IUPHAR
1670
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PRIMARY
ChEMBL
CHEMBL511142
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PRIMARY
ECHA (EC/EINECS)
257-950-6
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
PRIMARY
NCI_THESAURUS
C61656
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
PRIMARY
RXCUI
1819
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
PRIMARY RxNorm
MESH
D002047
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
PRIMARY
MERCK INDEX
m2771
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
PRIMARY Merck Index
INN
3403
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
PRIMARY
WIKIPEDIA
BUPRENORPHINE
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
PRIMARY
FDA UNII
40D3SCR4GZ
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
PRIMARY
DRUG CENTRAL
434
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
PRIMARY
LACTMED
Buprenorphine
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
PRIMARY
DAILYMED
40D3SCR4GZ
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
PRIMARY
CAS
52485-79-7
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
PRIMARY
EVMPD
SUB05985MIG
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
PRIMARY
CHEBI
3216
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
PRIMARY
EPA CompTox
DTXSID2022705
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
PRIMARY
SMS_ID
100000085263
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
PRIMARY
DRUG BANK
DB00921
Created by admin on Mon Mar 31 17:50:57 GMT 2025 , Edited by admin on Mon Mar 31 17:50:57 GMT 2025
PRIMARY
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