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Identification
NameBuprenorphine
Accession NumberDB00921  (APRD00670)
TypeSmall Molecule
GroupsApproved, Illicit, Investigational, Vet Approved
Description

Buprenorphine is a derivative of the opioid alkaloid thebaine that is a more potent (25 – 40 times) and longer lasting analgesic than morphine. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use. [PubChem]

Structure
Thumb
Synonyms
(-)-Buprenorphine
(−)-buprenorphine
17-Cyclopropylmethyl-4,5alpha-epoxy-7alpha-((S)-1-hydroxy-1,2,2-trimethylpropyl)-6-methoxy-6,14-endo-ethanomorphinan-3-ol
2-(N-Cyclopropylmethyl-4,5alpha-epoxy-3-hydroxy-6-methoxy-6,14-endo-ethanomorphinan-6alpha-yl)-3,3-dimethyl-2-butanol
2-[3-Cyclopropylmethyl-11-hydroxy-15-methoxy-(14R)-13-oxa-3-azahexacyclo[13.2.2.12,8.01,6.06,14.07,12]icosa-7,9,11-trien-16-yl]-3,3-dimethyl-2-butanol
21-Cyclopropyl-7alpha-[(S)-1-hydroxy-1,2,2-trimethylpropyl]-6,14-endo-ethano-6,7,8,14-tetrahydrooripavine
Buprenophine
Buprenorfina
Buprenorphinum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Belbucafilm450 ug/1buccalEndo Pharmaceuticals2015-06-01Not applicableUs
Belbucafilm750 ug/1buccalEndo Pharmaceuticals2015-06-01Not applicableUs
Belbucafilm300 ug/1buccalEndo Pharmaceuticals2015-06-01Not applicableUs
Belbucafilm150 ug/1buccalEndo Pharmaceuticals2015-06-01Not applicableUs
Belbucafilm75 ug/1buccalEndo Pharmaceuticals2015-06-01Not applicableUs
Belbucafilm600 ug/1buccalEndo Pharmaceuticals2015-06-01Not applicableUs
Belbucafilm900 ug/1buccalEndo Pharmaceuticals2015-06-01Not applicableUs
Buprenexinjection.3 mg/mLintramuscular; intravenousIndivior Inc.1985-06-30Not applicableUs
Butranspatch, extended release10 ug/htransdermalLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-26Not applicableUs
Butranspatch, extended release10 ug/htransdermalPurdue Pharma LP2011-02-14Not applicableUs
Butranspatch, extended release5 ug/htransdermalPurdue Pharma LP2011-02-14Not applicableUs
Butranspatch, extended release20 ug/htransdermalA S Medication Solutions Llc2011-02-14Not applicableUs
Butranspatch, extended release10 ug/htransdermalA S Medication Solutions Llc2011-02-14Not applicableUs
Butranspatch, extended release15 ug/htransdermalPurdue Pharma LP2011-02-14Not applicableUs
Butranspatch, extended release5 ug/htransdermalLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-26Not applicableUs
Butranspatch, extended release7.5 ug/htransdermalPurdue Pharma LP2011-02-14Not applicableUs
Butranspatch, extended release20 ug/htransdermalLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-26Not applicableUs
Butranspatch, extended release20 ug/htransdermalPurdue Pharma LP2011-02-14Not applicableUs
Butrans 10patch10 mcgtransdermalPurdue Pharma2010-05-26Not applicableCanada
Butrans 15patch15 mcgtransdermalPurdue Pharma2016-06-15Not applicableCanada
Butrans 20patch20 mcgtransdermalPurdue Pharma2010-05-26Not applicableCanada
Butrans 5patch5 mcgtransdermalPurdue Pharma2010-05-26Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Buprenorphinetablet8 mg/1sublingualSun Pharmaceutical Industries Limited2016-02-17Not applicableUs
Buprenorphinetablet2 mg/1sublingualSun Pharmaceutical Industries Limited2016-02-17Not applicableUs
Buprenorphinetablet2 mg/1sublingualActavis Pharma, Inc.2015-03-23Not applicableUs
Buprenorphinetablet8 mg/1sublingualActavis Pharma, Inc.2015-03-23Not applicableUs
Buprenorphinetablet8 mg/1sublingualTeva Pharmaceuticals Usa, Inc.2010-05-25Not applicableUs
Buprenorphinetablet2 mg/1sublingualTeva Pharmaceuticals Usa, Inc.2010-05-25Not applicableUs
Buprenorphine HCltablet2 mg/1sublingualRoxane Laboratories, Inc2009-10-08Not applicableUs
Buprenorphine HCltablet2 mg/1sublingualCardinal Health2009-10-08Not applicableUs
Buprenorphine HCltablet8 mg/1sublingualRoxane Laboratories, Inc2009-10-08Not applicableUs
Buprenorphine Hydrochloridetablet8 mg/1sublingualHi Tech Pharmacal Co., Inc.2010-09-24Not applicableUs
Buprenorphine Hydrochloridetablet2 mg/1sublingualREMEDYREPACK INC.2013-07-25Not applicableUs
Buprenorphine Hydrochlorideinjection, solution.3 mg/mLintramuscular; intravenousHospira, Inc.2010-07-12Not applicableUs
Buprenorphine Hydrochloridetablet8 mg/1sublingualPd Rx Pharmaceuticals, Inc.2010-09-24Not applicableUs
Buprenorphine Hydrochloridetablet2 mg/1sublingualHi Tech Pharmacal Co., Inc.2010-09-24Not applicableUs
Buprenorphine Hydrochloridetablet2 mg/1oralREMEDYREPACK INC.2010-12-07Not applicableUs
Buprenorphine Hydrochloridetablet2 mg/1oralREMEDYREPACK INC.2010-12-07Not applicableUs
Buprenorphine Hydrochloridetablet8 mg/1oralbryant ranch prepack2009-10-09Not applicableUs
Buprenorphine Hydrochlorideinjection.324 mg/mLintramuscular; intravenousPar Pharmaceutical Inc.2015-07-30Not applicableUs
Buprenorphine Hydrochlorideinjection, solution.3 mg/mLintramuscular; intravenousRebel Distributors Corp2010-07-12Not applicableUs
Buprenorphine Hydrochloridetablet8 mg/1sublingualREMEDYREPACK INC.2013-06-24Not applicableUs
Buprenorphine Hydrochloridetablet8 mg/1sublingualA S Medication Solutions Llc2010-09-24Not applicableUs
Buprenorphine Hydrochlorideinjection, solution.324 mg/mLintramuscular; intravenousAmerican Regent, Inc.2010-08-13Not applicableUs
Buprenorphine Hydrochloride Sublingualtablet8 mg/1sublingualMylan Pharmaceuticals Inc.2015-03-06Not applicableUs
Buprenorphine Hydrochloride Sublingualtablet2 mg/1sublingualMylan Pharmaceuticals Inc.2015-03-06Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AddnokRusan Pharma Ltd.
BuprelNot Available
BuprigesicNeon Laboratories
MorgesicSamarth Pharma
NorphinUnichem Laboratories
NorspanNot Available
ProbuphineTitan Pharmaceuticals, Inc.
SubutexNot Available
TemgesicNot Available
TidigesicSun Pharmaceuticals
Brand mixtures
NameLabellerIngredients
Act Buprenorphine/naloxoneActavis Pharma Company
BunavailBio Delivery Sciences International, Inc.
Buprenorphine and NaloxoneTeva Pharmaceuticals USA Inc
Buprenorphine HCl and Naloxone HClMallinckrodt, Inc.
Buprenorphine Hydrochloride and Naloxone Hydrochloride DihydrateRoxane Laboratories, Inc.
Mylan-buprenorphine/naloxoneMylan Pharmaceuticals Ulc
SuboxoneIndivior Inc.
Teva-buprenorphine/naloxoneTeva Canada Limited
ZubsolvOrexo Us, Inc.
Salts
Name/CASStructureProperties
Buprenorphine Hydrochloride
53152-21-9
Thumb
  • InChI Key: UAIXRPCCYXNJMQ-RZIPZOSSSA-N
  • Monoisotopic Mass: 503.280236544
  • Average Mass: 504.101
DBSALT000019
Categories
UNII40D3SCR4GZ
CAS number52485-79-7
WeightAverage: 467.6401
Monoisotopic: 467.303558805
Chemical FormulaC29H41NO4
InChI KeyInChIKey=RMRJXGBAOAMLHD-IHFGGWKQSA-N
InChI
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
IUPAC Name
(1S,2R,6S,14R,15R,16R)-3-(cyclopropylmethyl)-16-[(2S)-2-hydroxy-3,3-dimethylbutan-2-yl]-15-methoxy-13-oxa-3-azahexacyclo[13.2.2.1²,⁸.0¹,⁶.0⁶,¹⁴.0⁷,¹²]icosa-7,9,11-trien-11-ol
SMILES
CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[[email protected]]1CC4=C5C(O[C@@H]2[C@@]35CCN1CC1CC1)=C(O)C=C4
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as morphinans. These are polycyclic compounds with a four-ring skeleton with three condensed six-member rings forming a partially hydrogenated phenanthrene moiety, one of which is aromatic while the two others are alicyclic.
KingdomOrganic compounds
Super ClassAlkaloids and derivatives
ClassMorphinans
Sub ClassNot Available
Direct ParentMorphinans
Alternative Parents
Substituents
  • Morphinan
  • Benzylisoquinoline
  • Phenanthrene
  • Tetralin
  • Azaspirodecane
  • Benzofuran
  • Aralkylamine
  • Alkyl aryl ether
  • Benzenoid
  • Piperidine
  • Tertiary alcohol
  • Tertiary aliphatic amine
  • Tertiary amine
  • Oxacycle
  • Azacycle
  • Organoheterocyclic compound
  • Ether
  • Dialkyl ether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Alcohol
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of moderate to severe pain, peri-operative analgesia, and opioid dependence.
PharmacodynamicsBuprenorphine is a synthetic opioid analgesic and thebaine derivative, with a longer duration of action than morphine. Buprenorphine interacts predominately with the opioid mu-receptor. These mu-binding sites are discretely distributed in the human brain, spinal cord, and other tissues. In clinical settings, buprenorphine exerts its principal pharmacologic effects on the central nervous system. Its primary actions of therapeutic value are analgesia and sedation. Buprenorphine may increase the patient's tolerance for pain and decrease the perception of suffering, although the presence of the pain itself may still be recognized. In addition to analgesia, alterations in mood, euphoria and dysphoria, and drowsiness commonly occur. Buprenorphine depresses the respiratory centers, depresses the cough reflex, and constricts the pupils. Pharmacological effects peaks at 15 minutes and persists for 6 hours or longer when given intramuscularly. When given intravenously, the time to onset and peak effect are shortened.
Mechanism of actionBuprenorphine's analgesic effect is due to partial agonist activity at mu-opioid receptors. Buprenorphine is also a kappa-opioid receptor antagonist. The partial agonist activity means that opioid receptor antagonists (e.g., an antidote such as naloxone) only partially reverse the effects of buprenorphine. The binding to the mu and kappa receptors results in hyperpolarization and reduced neuronal excitability. Furthermore, buprenorphine slowly dissociates from its receptor. This observation would account for the longer duration of action compared to morphine, the unpredictability of its reversal by opioid antagonists, and its low level of manifest physical dependence. Its receptor fixation half life is 40 minutes which is significantly longer than morphine (milliseconds).
Related Articles
Absorption31% bioavailability (sublingual). Sublingual absorption is also dependent on pH. The length of time the tablet is under the tongue has little effect on absorption. Although buprenorphine is rapidly absorbed from the oral mucosa, the absorption into the systemic is slower. The time to reach peak plasma concentration (Tmax) varies between individuals (range of 40 minutes to 3.5 hours). How buprenorphine is formulated does not affect this pharmacokinetic parameter. It also undergoes extensive first-pass metabolism and as a consequence, has very low oral bioavailability. Coadministration with naloxone does not effect the pharmacokinetics of buprenorphine.
Volume of distribution

Buprenorphine is very lipophillic and is thus highly distributed. The estimated volume of distribution is 188 – 335 L when given intravenously. It is able to cross into the placenta and breast milk.

Protein binding96% protein bound to alpha- and beta-globulin.
Metabolism

Hepatic. Buprenorphine undergoes both N-dealkylation to norbuprenorphine and glucuronidation. The N-dealkylation pathway is mediated by cytochrome P-450 3A4 isozyme. Norbuprenorphine, an active metabolite and has one-fifth of the pharmacologic activity of the parent compound, can further undergo glucuronidation.

SubstrateEnzymesProduct
Buprenorphine
NorbuprenorphineDetails
Buprenorphine
HydroxybuprenorphineDetails
Buprenorphine
Buprenorphine glucuronideDetails
Norbuprenorphine
Not Available
HydroxynorbuprenorphineDetails
Hydroxybuprenorphine
Not Available
HydroxynorbuprenorphineDetails
Route of eliminationBuprenorphine, like morphine and other phenolic opioid analgesics, is metabolized by the liver and its clearance is related to hepatic blood flow. It is primarily eliminated via feces (as free forms of buprenorphine and norbuprenorphine) while 10 - 30% of the dose is excreted in urine (as conjugated forms of buprenorphine and norbuprenorphine).
Half lifeIV administration, 0.3 mg = 1.2 - 7.2 hours (mean 2.2 hours); Sublingual administration = 37 hours.
Clearance

Clearance may be higher in children than in adults.
Plasma clearance rate, IV administration, anaesthetized patients = 901.2 ± 39.7 mL/min;
Plasma clearance rate, IV administration, healthy subjects = 1042 – 1280 mL/min.

ToxicityManifestations of acute overdose include pinpoint pupils, sedation, hypotension, respiratory depression and death.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Buprenorphine Action PathwayDrug actionSMP00684
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9055
Blood Brain Barrier+0.9401
Caco-2 permeable+0.6893
P-glycoprotein substrateSubstrate0.9126
P-glycoprotein inhibitor IInhibitor0.5192
P-glycoprotein inhibitor IINon-inhibitor0.6992
Renal organic cation transporterInhibitor0.5797
CYP450 2C9 substrateNon-substrate0.8366
CYP450 2D6 substrateSubstrate0.8919
CYP450 3A4 substrateSubstrate0.8142
CYP450 1A2 substrateNon-inhibitor0.9153
CYP450 2C9 inhibitorNon-inhibitor0.8692
CYP450 2D6 inhibitorNon-inhibitor0.6721
CYP450 2C19 inhibitorNon-inhibitor0.7801
CYP450 3A4 inhibitorNon-inhibitor0.8322
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9212
Ames testNon AMES toxic0.7448
CarcinogenicityNon-carcinogens0.9391
BiodegradationNot ready biodegradable1.0
Rat acute toxicity3.1511 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8366
hERG inhibition (predictor II)Non-inhibitor0.586
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Purdue pharma lp
  • Reckitt benckiser pharmaceuticals inc
  • Bedford laboratories div ben venue laboratories inc
  • Hospira inc
  • Pharmaforce inc
  • Barr laboratories inc
  • Roxane laboratories inc
Packagers
Dosage forms
FormRouteStrength
Filmbuccal150 ug/1
Filmbuccal300 ug/1
Filmbuccal450 ug/1
Filmbuccal600 ug/1
Filmbuccal75 ug/1
Filmbuccal750 ug/1
Filmbuccal900 ug/1
Filmbuccal
Injectionintramuscular; intravenous.3 mg/mL
Tabletsublingual2 mg/1
Tabletsublingual8 mg/1
Injectionintramuscular; intravenous.324 mg/mL
Injection, solutionintramuscular; intravenous.3 mg/mL
Injection, solutionintramuscular; intravenous.324 mg/mL
Tabletoral2 mg/1
Tabletoral8 mg/1
Tabletsublingual
Patch, extended releasetransdermal10 ug/h
Patch, extended releasetransdermal15 ug/h
Patch, extended releasetransdermal20 ug/h
Patch, extended releasetransdermal5 ug/h
Patch, extended releasetransdermal7.5 ug/h
Patchtransdermal10 mcg
Patchtransdermal15 mcg
Patchtransdermal20 mcg
Patchtransdermal5 mcg
Film, solublebuccal; sublingual
Film, solublesublingual
Tabletoral
Tablet, orally disintegratingsublingual
Prices
Unit descriptionCostUnit
Buprenex 0.3 mg/ml Solution (1 Box Contains Five 1ml Box)46.39USD box
Subutex 8 mg Sublingual Tabs10.2USD tab
Subutex 8 mg tablet sl9.4USD tablet
Buprenorphine 8 mg tablet sl7.74USD tablet
Buprenex 0.3 mg/ml ampul6.96USD ml
Subutex 2 mg Sublingual Tabs5.59USD tab
Subutex 2 mg tablet sl5.0USD tablet
Buprenorphine 2 mg tablet sl4.14USD tablet
Buprenorphine 0.3 mg/ml vial2.96USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2030178 No1995-08-152010-11-16Canada
CA2276170 No2007-12-042018-02-24Canada
US5240711 No1993-11-282010-11-28Us
US5968547 No1997-09-292017-09-29Us
US6159498 No1996-10-182016-10-18Us
US6264980 No1995-12-182015-12-18Us
US6344211 No1995-12-182015-12-18Us
US7579019 No2000-01-222020-01-22Us
US8017150 No2003-02-132023-02-13Us
US8147866 No2007-07-232027-07-23Us
US8454996 No1999-09-242019-09-24Us
US8470361 No2010-05-222030-05-22Us
US8475832 No2010-03-262030-03-26Us
US8603514 No2004-04-032024-04-03Us
US8658198 No2007-12-032027-12-03Us
US8703177 No2012-08-202032-08-20Us
US8940330 No2012-09-182032-09-18Us
US9259421 No2012-09-182032-09-18Us
USRE41408 No1997-09-292017-09-29Us
USRE41489 No1997-09-292017-09-29Us
USRE41571 No1997-09-292017-09-29Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP4.98AVDEEF,A ET AL. (1996)
pKa8.31 (at 25 °C)AVDEEF,A ET AL. (1996)
Predicted Properties
PropertyValueSource
Water Solubility0.0168 mg/mLALOGPS
logP4.53ALOGPS
logP3.55ChemAxon
logS-4.4ALOGPS
pKa (Strongest Acidic)7.5ChemAxon
pKa (Strongest Basic)12.54ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area62.16 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity131.76 m3·mol-1ChemAxon
Polarizability53.11 Å3ChemAxon
Number of Rings7ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Kazuhisa Ninomiya, Yasuhiro Fukushima, Mutsuo Okumura, Yuko Hosokawa, “Buprenorphine percutaneous absorption preparation.” U.S. Patent US6090405, issued August, 1992.

US6090405
General References
  1. Huang P, Kehner GB, Cowan A, Liu-Chen LY: Comparison of pharmacological activities of buprenorphine and norbuprenorphine: norbuprenorphine is a potent opioid agonist. J Pharmacol Exp Ther. 2001 May;297(2):688-95. [PubMed:11303059 ]
  2. Bodkin JA, Zornberg GL, Lukas SE, Cole JO: Buprenorphine treatment of refractory depression. J Clin Psychopharmacol. 1995 Feb;15(1):49-57. [PubMed:7714228 ]
  3. Elkader A, Sproule B: Buprenorphine: clinical pharmacokinetics in the treatment of opioid dependence. Clin Pharmacokinet. 2005;44(7):661-80. [PubMed:15966752 ]
External Links
ATC CodesN02AE01N07BC01N07BC51
AHFS Codes
  • 28:08.12
PDB EntriesNot Available
FDA labelDownload (345 KB)
MSDSDownload (196 KB)
Interactions
Drug Interactions
Drug
AcetazolamideThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Acetazolamide.
AlprazolamAlprazolam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
AlvimopanThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Alvimopan.
AmilorideThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Amiloride.
AmitriptylineAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Ammonium chlorideAmmonium chloride may increase the excretion rate of Buprenorphine which could result in a higher serum level.
AmobarbitalAmobarbital may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
AmoxapineAmoxapine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
AmphetamineAmphetamine may increase the analgesic activities of Buprenorphine.
AprepitantThe serum concentration of Buprenorphine can be increased when it is combined with Aprepitant.
AripiprazoleAripiprazole may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
AsenapineAsenapine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
AtazanavirThe serum concentration of Atazanavir can be decreased when it is combined with Buprenorphine.
AzelastineBuprenorphine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenBaclofen may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
BendroflumethiazideThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Bendroflumethiazide.
BexaroteneThe serum concentration of Buprenorphine can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Buprenorphine can be decreased when it is combined with Boceprevir.
BosentanThe serum concentration of Buprenorphine can be decreased when it is combined with Bosentan.
BrexpiprazoleBrexpiprazole may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
BromazepamBromazepam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
BrompheniramineBrompheniramine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
BumetanideThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Bumetanide.
BuspironeBuspirone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ButabarbitalButabarbital may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ButorphanolButorphanol may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
CarbamazepineCarbamazepine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
CarbinoxamineCarbinoxamine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
CarisoprodolCarisoprodol may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
CathinoneCathinone may increase the analgesic activities of Buprenorphine.
CetirizineCetirizine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ChlordiazepoxideChlordiazepoxide may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ChlorothiazideThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Chlorothiazide.
ChlorphenamineChlorphenamine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ChlorpromazineChlorpromazine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ChlorthalidoneThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Chlorthalidone.
ChlorzoxazoneChlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ClemastineClemastine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ClobazamClobazam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ClomipramineClomipramine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ClonazepamClonazepam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ClonidineClonidine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ClorazepateClorazepate may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ClozapineClozapine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
CobicistatThe serum concentration of Buprenorphine can be increased when it is combined with Cobicistat.
ConivaptanThe serum concentration of Buprenorphine can be increased when it is combined with Conivaptan.
CyclizineCyclizine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
CyclobenzaprineCyclobenzaprine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
CyclothiazideThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Cyclothiazide.
CyproheptadineCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
DabrafenibThe serum concentration of Buprenorphine can be decreased when it is combined with Dabrafenib.
DantroleneDantrolene may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
DasatinibThe serum concentration of Buprenorphine can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Buprenorphine can be decreased when it is combined with Deferasirox.
DesfluraneDesflurane may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
DesipramineDesipramine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
DesloratadineDesloratadine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
DesmopressinThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Desmopressin.
Dexchlorpheniramine maleateDexchlorpheniramine maleate may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
DiazepamDiazepam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
DimenhydrinateDimenhydrinate may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
DiphenhydramineDiphenhydramine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
DoxepinDoxepin may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
EfavirenzThe serum concentration of the active metabolites of Buprenorphine can be reduced when Buprenorphine is used in combination with Efavirenz resulting in a loss in efficacy.
EluxadolineBuprenorphine may increase the activities of Eluxadoline.
EntacaponeEntacapone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
EstazolamEstazolam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
EszopicloneEszopiclone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Etacrynic acidThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Ethacrynic acid.
EthanolEthanol may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
EthosuximideEthosuximide may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
EthotoinEthotoin may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
EthoxzolamideThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Ethoxzolamide.
EtravirineThe serum concentration of Buprenorphine can be decreased when it is combined with Etravirine.
EzogabineEzogabine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
FelbamateFelbamate may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
FexofenadineFexofenadine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
FlibanserinFlibanserin may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
FluconazoleThe metabolism of Buprenorphine can be decreased when combined with Fluconazole.
FlunarizineFlunarizine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
FlupentixolFlupentixol may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
FluphenazineFluphenazine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
FlurazepamFlurazepam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
FosaprepitantThe serum concentration of Buprenorphine can be increased when it is combined with Fosaprepitant.
FosphenytoinFosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
FurosemideThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Furosemide.
Fusidic AcidThe serum concentration of Buprenorphine can be increased when it is combined with Fusidic Acid.
GabapentinGabapentin may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
gabapentin enacarbilgabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Gamma Hydroxybutyric AcidGamma Hydroxybutyric Acid may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
GuanfacineGuanfacine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
HaloperidolHaloperidol may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
HydrochlorothiazideThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Hydrochlorothiazide.
HydroflumethiazideThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Hydroflumethiazide.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
IdelalisibThe serum concentration of Buprenorphine can be increased when it is combined with Idelalisib.
IloperidoneIloperidone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ImipramineImipramine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
IndapamideThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Indapamide.
IsocarboxazidThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Isocarboxazid.
IsofluraneIsoflurane may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
IvacaftorThe serum concentration of Buprenorphine can be increased when it is combined with Ivacaftor.
KetamineKetamine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
LamotrigineLamotrigine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
LevetiracetamLevetiracetam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
LevocabastineLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
LevocetirizineLevocetirizine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
LinezolidThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Linezolid.
LoratadineLoratadine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
LorazepamLorazepam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
LoxapineLoxapine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
LuliconazoleThe serum concentration of Buprenorphine can be increased when it is combined with Luliconazole.
LurasidoneLurasidone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
MaprotilineMaprotiline may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
MeclizineMeclizine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
MeprobamateMeprobamate may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
MetaxaloneMetaxalone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
MethocarbamolMethocarbamol may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
MethohexitalMethohexital may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
MethotrimeprazineBuprenorphine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethsuximideMethsuximide may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
MetolazoneThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Metolazone.
MetyrosineBuprenorphine may increase the sedative activities of Metyrosine.
MidazolamMidazolam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
MifepristoneThe serum concentration of Buprenorphine can be increased when it is combined with Mifepristone.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
MirtazapineMirtazapine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
MitotaneThe serum concentration of Buprenorphine can be decreased when it is combined with Mitotane.
MoclobemideThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Moclobemide.
MorphineBuprenorphine may decrease the analgesic activities of Morphine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
NalbuphineNalbuphine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
NaltrexoneThe therapeutic efficacy of Buprenorphine can be decreased when used in combination with Naltrexone.
NelfinavirThe metabolism of Buprenorphine can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Buprenorphine can be increased when it is combined with Netupitant.
NitrazepamNitrazepam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Nitrous oxideNitrous oxide may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
NortriptylineNortriptyline may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
OlanzapineOlanzapine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
OlopatadineOlopatadine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
OrphenadrineBuprenorphine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OxazepamOxazepam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
PalbociclibThe serum concentration of Buprenorphine can be increased when it is combined with Palbociclib.
PaliperidonePaliperidone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ParaldehydeBuprenorphine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineBuprenorphine may increase the serotonergic activities of Paroxetine.
PegvisomantThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Buprenorphine.
PentazocinePentazocine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
PentobarbitalPentobarbital may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
PerphenazinePerphenazine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
PhenelzineThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Phenelzine.
PhenobarbitalPhenobarbital may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
PhenytoinPhenytoin may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
PimozidePimozide may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
PipotiazinePipotiazine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
PizotifenPizotifen may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
PomalidomidePomalidomide may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
PramipexoleBuprenorphine may increase the sedative activities of Pramipexole.
PregabalinPregabalin may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
PrimidonePrimidone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ProcarbazineThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Procarbazine.
ProchlorperazineProchlorperazine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Buprenorphine.
PromazinePromazine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
PromethazinePromethazine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
PropofolPropofol may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ProtriptylineProtriptyline may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
QuazepamQuazepam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
QuetiapineQuetiapine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
RamelteonRamelteon may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
RamosetronBuprenorphine may increase the activities of Ramosetron.
RasagilineThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Rasagiline.
ReserpineReserpine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
RisperidoneRisperidone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
RitonavirThe serum concentration of Buprenorphine can be increased when it is combined with Ritonavir.
RopiniroleBuprenorphine may increase the sedative activities of Ropinirole.
RotigotineBuprenorphine may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Buprenorphine.
ScopolamineScopolamine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Scopolamine butylbromideScopolamine butylbromide may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
SecobarbitalSecobarbital may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
SelegilineThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Selegiline.
SevofluraneSevoflurane may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
SiltuximabThe serum concentration of Buprenorphine can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Buprenorphine can be increased when it is combined with Simeprevir.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
SpironolactoneThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Spironolactone.
St. John's WortThe serum concentration of Buprenorphine can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Buprenorphine can be increased when it is combined with Stiripentol.
SuccinylcholineSuccinylcholine may increase the bradycardic activities of Buprenorphine.
SuvorexantBuprenorphine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TasimelteonTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Tedizolid Phosphate.
TemazepamTemazepam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
TetrabenazineTetrabenazine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ThalidomideBuprenorphine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThioridazineThioridazine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ThiothixeneThiothixene may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
TiagabineTiagabine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
TicrynafenThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Ticrynafen.
TizanidineTizanidine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
TocilizumabThe serum concentration of Buprenorphine can be decreased when it is combined with Tocilizumab.
TolcaponeTolcapone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
TopiramateTopiramate may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
TorasemideThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Torasemide.
TranylcypromineThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Tranylcypromine.
TriamtereneThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Triamterene.
TriazolamTriazolam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
TrichlormethiazideThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Trichlormethiazide.
TrifluoperazineTrifluoperazine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
TrimipramineTrimipramine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
TriprolidineTriprolidine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
VigabatrinVigabatrin may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ZaleplonZaleplon may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ZiconotideZiconotide may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ZiprasidoneZiprasidone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ZolpidemZolpidem may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ZonisamideZonisamide may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ZopicloneZopiclone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ZuclopenthixolZuclopenthixol may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Opioid receptor activity
Specific Function:
G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synthetic opioids and for the psychoactive diterpene salvinorin A. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates th...
Gene Name:
OPRK1
Uniprot ID:
P41145
Molecular Weight:
42644.665 Da
References
  1. Boothby LA, Doering PL: Buprenorphine for the treatment of opioid dependence. Am J Health Syst Pharm. 2007 Feb 1;64(3):266-72. [PubMed:17244875 ]
  2. Robinson SE: Buprenorphine-containing treatments: place in the management of opioid addiction. CNS Drugs. 2006;20(9):697-712. [PubMed:16953647 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
partial agonist
General Function:
Voltage-gated calcium channel activity
Specific Function:
Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone. Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociati...
Gene Name:
OPRM1
Uniprot ID:
P35372
Molecular Weight:
44778.855 Da
References
  1. Kishioka S, Paronis CA, Lewis JW, Woods JH: Buprenorphine and methoclocinnamox: agonist and antagonist effects on respiratory function in rhesus monkeys. Eur J Pharmacol. 2000 Mar 17;391(3):289-97. [PubMed:10729371 ]
  2. Zubieta J, Greenwald MK, Lombardi U, Woods JH, Kilbourn MR, Jewett DM, Koeppe RA, Schuster CR, Johanson CE: Buprenorphine-induced changes in mu-opioid receptor availability in male heroin-dependent volunteers: a preliminary study. Neuropsychopharmacology. 2000 Sep;23(3):326-34. [PubMed:10942856 ]
  3. Sanchez-Blazquez P, Gomez-Serranillos P, Garzon J: Agonists determine the pattern of G-protein activation in mu-opioid receptor-mediated supraspinal analgesia. Brain Res Bull. 2001 Jan 15;54(2):229-35. [PubMed:11275413 ]
  4. Mizoguchi H, Wu HE, Narita M, Hall FS, Sora I, Uhl GR, Nagase H, Tseng LF: Antagonistic property of buprenorphine for putative epsilon-opioid receptor-mediated G-protein activation by beta-endorphin in pons/medulla of the mu-opioid receptor knockout mouse. Neuroscience. 2002;115(3):715-21. [PubMed:12435410 ]
  5. Ide S, Minami M, Satoh M, Uhl GR, Sora I, Ikeda K: Buprenorphine antinociception is abolished, but naloxone-sensitive reward is retained, in mu-opioid receptor knockout mice. Neuropsychopharmacology. 2004 Sep;29(9):1656-63. [PubMed:15100703 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Opioid receptor activity
Specific Function:
G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurot...
Gene Name:
OPRD1
Uniprot ID:
P41143
Molecular Weight:
40368.235 Da
References
  1. Induru RR, Davis MP: Buprenorphine for neuropathic pain--targeting hyperalgesia. Am J Hosp Palliat Care. 2009 Dec-2010 Jan;26(6):470-3. doi: 10.1177/1049909109341868. Epub 2009 Aug 7. [PubMed:19666890 ]
  2. Lester PA, Traynor JR: Comparison of the in vitro efficacy of mu, delta, kappa and ORL1 receptor agonists and non-selective opioid agonists in dog brain membranes. Brain Res. 2006 Feb 16;1073-1074:290-6. Epub 2006 Jan 27. [PubMed:16443205 ]
  3. Megarbane B, Marie N, Pirnay S, Borron SW, Gueye PN, Risede P, Monier C, Noble F, Baud FJ: Buprenorphine is protective against the depressive effects of norbuprenorphine on ventilation. Toxicol Appl Pharmacol. 2006 May 1;212(3):256-67. Epub 2005 Sep 16. [PubMed:16169027 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  3. Kobayashi K, Yamamoto T, Chiba K, Tani M, Shimada N, Ishizaki T, Kuroiwa Y: Human buprenorphine N-dealkylation is catalyzed by cytochrome P450 3A4. Drug Metab Dispos. 1998 Aug;26(8):818-21. [PubMed:9698298 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Retinoic acid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 2 lacks transferase activity but acts as a negative regulator of isoform 1.
Gene Name:
UGT1A9
Uniprot ID:
O60656
Molecular Weight:
59940.495 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP2C18
Uniprot ID:
P33260
Molecular Weight:
55710.075 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity.
Gene Name:
CYP2A6
Uniprot ID:
P11509
Molecular Weight:
56501.005 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Tournier N, Chevillard L, Megarbane B, Pirnay S, Scherrmann JM, Decleves X: Interaction of drugs of abuse and maintenance treatments with human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2). Int J Neuropsychopharmacol. 2010 Aug;13(7):905-15. doi: 10.1017/S1461145709990848. Epub 2009 Nov 4. [PubMed:19887017 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
References
  1. Tournier N, Chevillard L, Megarbane B, Pirnay S, Scherrmann JM, Decleves X: Interaction of drugs of abuse and maintenance treatments with human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2). Int J Neuropsychopharmacol. 2010 Aug;13(7):905-15. doi: 10.1017/S1461145709990848. Epub 2009 Nov 4. [PubMed:19887017 ]
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Drug created on June 13, 2005 07:24 / Updated on July 23, 2016 02:02