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Identification
NameHydromorphone
Accession NumberDB00327  (APRD01021)
TypeSmall Molecule
GroupsApproved, Illicit
Description

An opioid analgesic derived from morphine and used mainly as an analgesic. It has a shorter duration of action and is more potent than morphine. [PubChem]

Structure
Thumb
Synonyms
(-)-(5R)-4,5-Epoxy-3-hydroxy-9alpha-methylmorphinan-6-one
4,5-Epoxy-3-hydroxy-17-methylmorphinan-6-one
4,5alpha-Epoxy-3-hydroxy-17-methyl-6-morphinanone
6-Deoxy-7,8-dihydro-6-oxomorphine
7,8-Dihydromorphinone
Dihydromorfinon
Dihydromorphinone
Dimorphone
Hidromorfona
Hydromorfona
Hydromorphone
Hydromorphonum
Idromorfone
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Dilaudidliquid5 mg/5mLoralPurdue Pharma LP1956-01-01Not applicableUs
Dilaudidtablet4 mg/1oralLake Erie Medical DBA Quality Care Products LLC1956-01-01Not applicableUs
Dilaudidtablet2 mg/1oralPurdue Pharma LP1956-01-01Not applicableUs
Dilaudidtablet4 mgoralPurdue Pharma1984-12-31Not applicableCanada
Dilaudidtablet2 mgoralPurdue Pharma1984-12-31Not applicableCanada
Dilaudidsuppository3 mgrectalPurdue Pharma1984-12-312010-08-05Canada
Dilaudidinjection, solution4 mg/mLintramuscular; intravenous; subcutaneousPurdue Pharma LP1926-01-01Not applicableUs
Dilaudidliquid1 mgoralPurdue Pharma1989-12-31Not applicableCanada
Dilaudidliquid2 mgintramuscular; intravenous; subcutaneousPurdue Pharma1984-12-31Not applicableCanada
Dilaudidtablet8 mgoralPurdue Pharma1989-12-31Not applicableCanada
Dilaudidinjection, solution2 mg/mLintramuscular; intravenous; subcutaneousPurdue Pharma LP1926-01-01Not applicableUs
Dilaudidinjection, solution1 mg/mLintramuscular; intravenous; subcutaneousPurdue Pharma LP1926-01-01Not applicableUs
Dilaudidtablet1 mgoralPurdue Pharma1986-12-31Not applicableCanada
Dilaudidtablet8 mg/1oralPurdue Pharma LP1956-01-01Not applicableUs
Dilaudidpowder for solution250 mgintramuscular; intravenous; subcutaneousPurdue Pharma1994-12-312013-06-07Canada
Dilaudidtablet4 mg/1oralCardinal Health1926-01-01Not applicableUs
Dilaudidtablet2 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-12-01Not applicableUs
Dilaudidtablet4 mg/1oralPurdue Pharma LP1956-01-01Not applicableUs
Dilaudid Hpinjection, powder, lyophilized, for solution10 mg/mLintramuscular; intravenous; subcutaneousPurdue Pharma LP1984-01-11Not applicableUs
Dilaudid Hpinjection, solution10 mg/mLintramuscular; intravenous; subcutaneousPurdue Pharma LP1984-01-11Not applicableUs
Dilaudid Hpliquid10 mgintramuscular; intravenous; subcutaneousPurdue Pharma1984-12-31Not applicableCanada
Dilaudid-HP-plussolution20 mgintramuscular; intravenous; subcutaneousPurdue Pharma1995-12-312012-08-02Canada
Dilaudid-XPliquid50 mgintramuscular; intravenous; subcutaneousPurdue Pharma1995-12-312012-08-02Canada
Exalgotablet, extended release32 mg/1oralMallinckrodt, Inc2012-08-24Not applicableUs
Exalgotablet, extended release16 mg/1oralMallinckrodt, Inc2011-03-14Not applicableUs
Exalgotablet, extended release12 mg/1oralMallinckrodt, Inc2011-03-14Not applicableUs
Exalgotablet, extended release8 mg/1oralMallinckrodt, Inc2011-03-14Not applicableUs
Exalgotablet, extended release8 mg/1oralSTAT Rx USA LLC2011-03-14Not applicableUs
Exalgotablet, extended release8 mg/1oralLake Erie Medical DBA Quality Care Products LLC2011-03-14Not applicableUs
Exalgotablet, extended release16 mg/1oralLake Erie Medical DBA Quality Care Products LLC2011-03-14Not applicableUs
Exalgotablet, extended release16 mg/1oralPhysicians Total Care, Inc.2012-12-31Not applicableUs
Exalgotablet, extended release12 mg/1oralLake Erie Medical DBA Quality Care Products LLC2011-03-14Not applicableUs
Exalgotablet, extended release8 mg/1oralPhysicians Total Care, Inc.2012-12-31Not applicableUs
Hydromorph Contincapsule (sustained-release)9.0 mgoralPurdue Pharma2011-04-14Not applicableCanada
Hydromorph Contincapsule (sustained-release)4.5 mgoralPurdue Pharma2011-04-14Not applicableCanada
Hydromorph Contin-controlled Release Cap - 12mgcapsule (sustained-release)12 mgoralPurdue Pharma1996-12-31Not applicableCanada
Hydromorph Contin-controlled Release Cap - 18mgcapsule (sustained-release)18 mgoralPurdue Pharma2001-07-03Not applicableCanada
Hydromorph Contin-controlled Release Cap - 24mgcapsule (sustained-release)24 mgoralPurdue Pharma1996-12-31Not applicableCanada
Hydromorph Contin-controlled Release Cap - 30mgcapsule (sustained-release)30 mgoralPurdue Pharma1998-02-16Not applicableCanada
Hydromorph Contin-controlled Release Cap - 3mgcapsule (sustained-release)3 mgoralPurdue Pharma1995-12-31Not applicableCanada
Hydromorph Contin-controlled Release Cap - 6mgcapsule (sustained-release)6 mgoralPurdue Pharma1995-12-31Not applicableCanada
Hydromorph.ir - 2mgtablet2 mgoralPurdue Pharma2002-12-192012-08-02Canada
Hydromorph.ir - 4mgtablet4 mgoralPurdue Pharma2002-12-192012-08-02Canada
Hydromorph.ir - 8mgtablet8 mgoralPurdue Pharma2002-12-192012-08-02Canada
Hydromorphonetablet4 mgoralSorres Pharma Inc2004-04-062014-06-20Canada
Hydromorphonetablet8 mgoralSorres Pharma Inc2004-04-062014-06-20Canada
Hydromorphonetablet1 mgoralSorres Pharma Inc2004-04-062014-06-20Canada
Hydromorphonetablet2 mgoralSorres Pharma Inc2004-04-062014-06-20Canada
Hydromorphone HCl Tab 2mg USPtablet2 mgoralRoxane Labs, Division Of Boehringer Ingelheim1992-12-312001-07-30Canada
Hydromorphone HCl Tab 4mg USPtablet4 mgoralRoxane Labs, Division Of Boehringer Ingelheim1992-12-312001-07-30Canada
Hydromorphone Hp 10solution10 mgintramuscular; intravenous; subcutaneousSandoz Canada Incorporated1995-12-31Not applicableCanada
Hydromorphone Hp 20solution20 mgintramuscular; intravenous; subcutaneousSandoz Canada Incorporated1995-12-31Not applicableCanada
Hydromorphone Hp 50solution50 mgintramuscular; intravenous; subcutaneousSandoz Canada Incorporated1995-12-31Not applicableCanada
Hydromorphone Hp Forte Injectionsolution100 mgintramuscular; intravenous; subcutaneousSandoz Canada Incorporated2001-12-10Not applicableCanada
Hydromorphone Hydrochloridetablet2 mg/1oralAvera Mc Kennan Hospital2015-05-28Not applicableUs
Hydromorphone Hydrochloridesolution5 mg/5mLoralRhodes Pharmaceuticals L.P.2012-07-20Not applicableUs
Hydromorphone Hydrochlorideinjection, solution1 mg/mLintramuscular; intravenous; subcutaneousHospira, Inc.2011-12-01Not applicableUs
Hydromorphone Hydrochloridetablet8 mg/1oralRhodes Pharmaceuticals L.P.2009-11-23Not applicableUs
Hydromorphone Hydrochlorideinjection, solution4 mg/mLintramuscular; intravenous; subcutaneousHospira, Inc.2011-12-01Not applicableUs
Hydromorphone Hydrochloridetablet4 mg/1oralRhodes Pharmaceuticals L.P.2009-11-23Not applicableUs
Hydromorphone Hydrochlorideinjection, solution2 mg/mLintramuscular; intravenous; subcutaneousHospira, Inc.2011-12-01Not applicableUs
Hydromorphone Hydrochloridetablet2 mg/1oralRhodes Pharmaceuticals L.P.2009-11-23Not applicableUs
Hydromorphone Hydrochlorideinjection, solution4 mg/mLintramuscular; intravenous; subcutaneousHospira, Inc.2011-12-01Not applicableUs
Hydromorphone Hydrochlorideinjection, solution1 mg/mLintramuscular; intravenous; subcutaneousHospira, Inc.2011-12-01Not applicableUs
Hydromorphone Hydrochloridetablet2 mg/1oralbryant ranch prepack2009-11-23Not applicableUs
Hydromorphone Hydrochloridetablet8 mg/1oralSTAT Rx USA LLC2009-11-23Not applicableUs
Hydromorphone Hydrochloridetablet4 mg/1oralbryant ranch prepack2009-11-23Not applicableUs
Hydromorphone Hydrochlorideinjection, solution2 mg/mLintramuscular; intravenous; subcutaneousHospira, Inc.2011-12-01Not applicableUs
Hydromorphone Hydrochlorideinjection, solution2 mg/mLintramuscular; intravenous; subcutaneousHospira, Inc.2011-12-01Not applicableUs
Hydromorphone Hydrochloride Extended-releasetablet, extended release8 mg/1oralMallinckrodt, Inc.2014-06-12Not applicableUs
Hydromorphone Hydrochloride Extended-releasetablet, extended release32 mg/1oralMallinckrodt, Inc.2014-06-12Not applicableUs
Hydromorphone Hydrochloride Extended-releasetablet, extended release16 mg/1oralMallinckrodt, Inc.2014-06-12Not applicableUs
Hydromorphone Hydrochloride Extended-releasetablet, extended release12 mg/1oralMallinckrodt, Inc.2014-06-12Not applicableUs
Hydromorphone Hydrochloride Injection USPsolution2 mgintramuscular; intravenous; subcutaneousSandoz Canada Incorporated1995-12-31Not applicableCanada
Hydromorphone Hydrochloride Injection USP Hp 10solution10 mgintramuscular; intravenous; subcutaneousHospira Healthcare Corporation2014-06-11Not applicableCanada
Hydromorphone Hydrochloride Sup 3mgsuppository3 mgrectalSandoz Canada Incorporated1992-12-312012-01-23Canada
Jurnistatablet (extended-release)8 mgoralJanssen Inc2010-03-04Not applicableCanada
Jurnistatablet (extended-release)16 mgoralJanssen Inc2010-03-04Not applicableCanada
Jurnistatablet (extended-release)4 mgoralJanssen Inc2010-03-04Not applicableCanada
Jurnistatablet (extended-release)32 mgoralJanssen Inc2010-03-04Not applicableCanada
Palladone XL - 12mgcapsule (controlled-delivery)12 mgoralPurdue Pharma2002-12-192005-08-05Canada
Palladone XL - 16mgcapsule (controlled-delivery)16 mgoralPurdue Pharma2002-12-192005-08-05Canada
Palladone XL - 24mgcapsule (controlled-delivery)24 mgoralPurdue Pharma2002-12-192005-08-05Canada
PHL-hydromorphonesuppository3 mgrectalPharmel IncNot applicableNot applicableCanada
PHL-hydromorphone -syr 1mg/mlsyrup1 mgoralPharmel IncNot applicableNot applicableCanada
PMS Hydromorphone Sirop 1mg/mlsyrup1 mgoralPharmascience Inc1991-12-31Not applicableCanada
PMS Hydromorphone Suppositoire 3mgsuppository3 mgrectalPharmascience Inc1991-12-31Not applicableCanada
PMS-hydromorphone Tab 1mgtablet1 mgoralPharmascience Inc1991-12-31Not applicableCanada
PMS-hydromorphone Tab 2mgtablet2 mgoralPharmascience Inc1991-12-31Not applicableCanada
PMS-hydromorphone Tab 4mgtablet4 mgoralPharmascience Inc1991-12-31Not applicableCanada
PMS-hydromorphone Tab 8mgtablet8 mgoralPharmascience Inc1991-12-31Not applicableCanada
Teva-hydromorphonetablet8 mgoralTeva Canada Limited2011-11-16Not applicableCanada
Teva-hydromorphonetablet4 mgoralTeva Canada Limited2011-11-16Not applicableCanada
Teva-hydromorphonetablet2 mgoralTeva Canada Limited2011-11-16Not applicableCanada
Teva-hydromorphonetablet1 mgoralTeva Canada Limited2011-11-16Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-hydromorphonetablet1 mgoralApotex Inc2012-12-18Not applicableCanada
Apo-hydromorphonetablet8 mgoralApotex Inc2012-12-18Not applicableCanada
Apo-hydromorphonetablet4 mgoralApotex Inc2012-12-18Not applicableCanada
Apo-hydromorphonetablet2 mgoralApotex Inc2012-12-18Not applicableCanada
Hydromorphone Hydrochloridetablet2 mg/1oralH.J. Harkins Company, Inc.2009-12-09Not applicableUs
Hydromorphone Hydrochloridetablet4 mg/1oralSTAT Rx USA LLC2007-09-19Not applicableUs
Hydromorphone Hydrochlorideinjection, solution10 mg/mLintramuscular; intravenous; subcutaneousTeva Parenteral Medicines, Inc.2011-01-18Not applicableUs
Hydromorphone Hydrochlorideinjection, solution10 mg/mLintramuscular; intravenous; subcutaneousTeva Parenteral Medicines, Inc.2011-01-18Not applicableUs
Hydromorphone Hydrochloridetablet4 mg/1oralLannett Company, Inc.2009-12-09Not applicableUs
Hydromorphone Hydrochloridetablet4 mg/1oralRoxane Laboratories, Inc2009-07-29Not applicableUs
Hydromorphone Hydrochloridetablet, film coated2 mg/1oralPhysicians Total Care, Inc.2004-09-20Not applicableUs
Hydromorphone Hydrochloridetablet8 mg/1oralH.J. Harkins Company, Inc.2009-12-09Not applicableUs
Hydromorphone Hydrochloridetablet2 mg/1oralLake Erie Medical DBA Quality Care Products LLC2009-12-09Not applicableUs
Hydromorphone Hydrochloridetablet, extended release12 mg/1oralWatson Laboratories, Inc.2014-05-21Not applicableUs
Hydromorphone Hydrochloridetablet2 mg/1oralLannett Company, Inc.2009-12-09Not applicableUs
Hydromorphone Hydrochloridetablet4 mg/1oralH.J. Harkins Company, Inc.2009-12-09Not applicableUs
Hydromorphone Hydrochloridetablet4 mg/1oralLake Erie Medical DBA Quality Care Products LLC2009-12-09Not applicableUs
Hydromorphone Hydrochloridetablet, extended release16 mg/1oralWatson Laboratories, Inc.2014-05-21Not applicableUs
Hydromorphone Hydrochlorideinjection, solution10 mg/mLintramuscular; intravenous; subcutaneousHospira, Inc.2008-06-17Not applicableUs
Hydromorphone Hydrochloridetablet8 mg/1oralAmerican Health Packaging2014-08-14Not applicableUs
Hydromorphone Hydrochloridetablet8 mg/1oralTAGI Pharma, Inc.2012-03-09Not applicableUs
Hydromorphone Hydrochloridetablet8 mg/1oralLake Erie Medical DBA Quality Care Products LLC2009-12-09Not applicableUs
Hydromorphone Hydrochloridetablet, extended release8 mg/1oralWatson Laboratories, Inc.2014-05-21Not applicableUs
Hydromorphone Hydrochloridetablet8 mg/1oralMallinckrodt, Inc.2009-05-14Not applicableUs
Hydromorphone Hydrochloridetablet4 mg/1oralAmerican Health Packaging2013-07-17Not applicableUs
Hydromorphone Hydrochloridetablet, extended release16 mg/1oralPaddock Laboratories, LLC2015-05-22Not applicableUs
Hydromorphone Hydrochloridetablet4 mg/1oralMallinckrodt, Inc.2009-05-14Not applicableUs
Hydromorphone Hydrochloridetablet2 mg/1oralAmerican Health Packaging2013-07-17Not applicableUs
Hydromorphone Hydrochloridetablet8 mg/1oralLake Erie Medical DBA Quality Care Products LLC2010-04-26Not applicableUs
Hydromorphone Hydrochloridetablet2 mg/1oralLake Erie Medical DBA Quality Care Products LLC2009-05-14Not applicableUs
Hydromorphone Hydrochloridetablet4 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-11-29Not applicableUs
Hydromorphone Hydrochlorideinjection10 mg/mLparenteralAkorn, Inc.2010-05-15Not applicableUs
Hydromorphone Hydrochloridetablet, extended release12 mg/1oralPaddock Laboratories, LLC2015-05-22Not applicableUs
Hydromorphone Hydrochloridetablet2 mg/1oralMallinckrodt, Inc.2009-05-14Not applicableUs
Hydromorphone Hydrochloridetablet8 mg/1oralbryant ranch prepack2009-07-29Not applicableUs
Hydromorphone Hydrochloridetablet2 mg/1oralPd Rx Pharmaceuticals, Inc.2009-12-09Not applicableUs
Hydromorphone Hydrochloridetablet2 mg/1oralSTAT Rx USA LLC2009-05-14Not applicableUs
Hydromorphone Hydrochloridetablet, extended release8 mg/1oralPaddock Laboratories, LLC2015-05-22Not applicableUs
Hydromorphone Hydrochloridesolution1 mg/mLoralRoxane Laboratories, Inc2012-03-01Not applicableUs
Hydromorphone Hydrochloridetablet, film coated4 mg/1oralPhysicians Total Care, Inc.2004-01-07Not applicableUs
Hydromorphone Hydrochloridetablet2 mg/1oralSTAT Rx USA LLC2007-09-19Not applicableUs
Hydromorphone Hydrochlorideinjection, solution10 mg/mLintramuscular; intravenous; subcutaneousTeva Parenteral Medicines, Inc.2011-01-18Not applicableUs
Hydromorphone Hydrochloridetablet8 mg/1oralLannett Company, Inc.2009-12-09Not applicableUs
Hydromorphone Hydrochloridetablet8 mg/1oralRoxane Laboratories, Inc2009-07-29Not applicableUs
Hydromorphone Hydrochloridetablet, film coated8 mg/1oralPhysicians Total Care, Inc.2002-02-06Not applicableUs
Hyrdomorphone Hydrochloridetablet8 mg/1oralPrecision Dose Inc.2014-02-17Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Hydromorphone HClinjection, solution.4 mg/mLintravenousCantrell Drug Company2014-08-13Not applicableUs
Hydromorphone HClinjection, solution10 mg/mLintravenousCantrell Drug Company2014-08-13Not applicableUs
Hydromorphone HClinjection, solution1 mg/mLintravenousCantrell Drug Company2011-06-30Not applicableUs
Hydromorphone HClinjection, solution.5 mg/mLintramuscular; intravenous; subcutaneousCantrell Drug Company2012-01-18Not applicableUs
Hydromorphone HClinjection, solution.1 mg/mLintravenousCantrell Drug Company2014-08-21Not applicableUs
Hydromorphone HClinjection, solution.2 mg/mLintravenousCantrell Drug Company2010-08-23Not applicableUs
Hydromorphone HClinjection, solution2 mg/mLintravenousCantrell Drug Company2014-08-13Not applicableUs
Hydromorphone Hydrochloridesuppository3 mg/1rectalPaddock Laboratories, LLC1996-01-31Not applicableUs
Hydromorphone Hydrochlorideinjection2 mg/mLintramuscular; intravenous; subcutaneousWest Ward Pharmaceutical Corp.1972-01-01Not applicableUs
Hydromorphone Hydrochlorideinjection2 mg/mLintramuscular; intravenous; subcutaneousWest Ward Pharmaceutical Corp.1972-01-01Not applicableUs
International Brands
NameCompany
PalladoneNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Hydromorphone Hydrochloride
71-68-1
Thumb
  • InChI Key: XHILEZUETWRSHC-NRGUFEMZSA-N
  • Monoisotopic Mass: 321.113171218
  • Average Mass: 321.799
DBSALT000444
Categories
UNIIQ812464R06
CAS number466-99-9
WeightAverage: 285.3377
Monoisotopic: 285.136493479
Chemical FormulaC17H19NO3
InChI KeyInChIKey=WVLOADHCBXTIJK-YNHQPCIGSA-N
InChI
InChI=1S/C17H19NO3/c1-18-7-6-17-10-3-5-13(20)16(17)21-15-12(19)4-2-9(14(15)17)8-11(10)18/h2,4,10-11,16,19H,3,5-8H2,1H3/t10-,11+,16-,17-/m0/s1
IUPAC Name
(1S,5R,13R,17R)-10-hydroxy-4-methyl-12-oxa-4-azapentacyclo[9.6.1.0¹,¹³.0⁵,¹⁷.0⁷,¹⁸]octadeca-7(18),8,10-trien-14-one
SMILES
[H][C@@]12OC3=C(O)C=CC4=C3[C@@]11CCN(C)[C@]([H])(C4)[C@]1([H])CCC2=O
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
  • Isoquinolone
  • Tetralin
  • Benzofuran
  • Aralkylamine
  • Cyclohexanone
  • Alkyl aryl ether
  • Benzenoid
  • Piperidine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Ketone
  • Oxacycle
  • Azacycle
  • Organoheterocyclic compound
  • Ether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the relief of moderate to severe pain such as that due to surgery, cancer, trauma/injury, or burns.
PharmacodynamicsHydromorphone is a hydrogenated ketone derivative of morphine that acts as a narcotic analgesic. It has a shorter duration of action than morphine. Hydromorphone is approximately 8 times more potent on a milligram basis than morphine. In addition, hydromorphone is better absorbed orally than is morphine. In clinical settings, Hydromorphone exerts its principal pharmacological effect on the central nervous system and gastrointestinal tract. Its primary actions of therapeutic value are analgesia and sedation. Hydromorphone appears to increase the patient's tolerance for pain and to decrease discomfort, 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. Opioids also produce respiratory depression by direct action on brain stem respiratory centers.
Mechanism of actionHydromorphone is a narcotic analgesic; its principal therapeutic effect is relief of pain. Hydromorphone interacts predominantly with the opioid mu-receptors. These mu-binding sites are discretely distributed in the human brain, with high densities in the posterior amygdala, hypothalamus, thalamus, nucleus caudatus, putamen, and certain cortical areas. They are also found on the terminal axons of primary afferents within laminae I and II (substantia gelatinosa) of the spinal cord and in the spinal nucleus of the trigeminal nerve. In clinical settings, Hydromorphone exerts its principal pharmacological effect on the central nervous system and gastrointestinal tract. Hydromorphone also binds with kappa-receptors which are thought to mediate spinal analgesia, miosis and sedation.
Related Articles
AbsorptionBetter absorbed orally than morphine
Volume of distributionNot Available
Protein binding20%
Metabolism

Primarily hepatic. After absorption hydromorphone is metabolized by the liver to the glucuronide conjugate which is then excreted in the urine. Hydromorphone is metabolized to the major metabolites hydromorphone-3-glucuronide, hydromorphone-3-glucoside and dihydroisomorphine-6-glucuronide.

SubstrateEnzymesProduct
Hydromorphone
DihydromorphineDetails
Hydromorphone
DihydroisomorphineDetails
Hydromorphone
NorhydromorphoneDetails
Hydromorphone
Hydromorphone 3-beta-O-glucuronideDetails
Hydromorphone
Not Available
Dihydroisomorphine-6-glucuronideDetails
Hydromorphone
Not Available
Hydromorphone-3-glucosideDetails
Hydromorphone
Not Available
Hydromorphone-3-glucuronideDetails
Hydromorphone
Not Available
Hydromorphone-3-sulphateDetails
Dihydromorphine
Dihydromorphine-3-glucuronideDetails
Route of eliminationOnly a small amount of the hydromorphone dose is excreted unchanged in the urine. Most of the dose is excreted as hydromorphone-3-glucuronide along with minor amounts of 6-hydroxy reduction metabolites.
Half life2.6 hours (oral); 18.6 hours for sustained release Palladone
Clearance
  • 1.96 L/min
ToxicityHydromorphone is a schedule II narcotic which can lead to physical dependence or addiction. High doses lead to respiratory depression, nausea, and vomiting. Overdoses lead to extreme somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, and sometimes bradycardia and hypotension. In severe overdosage, apnea, circulatory collapse, cardiac arrest and death may occur.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Hydromorphone Action PathwayDrug actionSMP00410
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9931
Caco-2 permeable+0.8647
P-glycoprotein substrateSubstrate0.8174
P-glycoprotein inhibitor INon-inhibitor0.8497
P-glycoprotein inhibitor IINon-inhibitor0.9641
Renal organic cation transporterInhibitor0.6374
CYP450 2C9 substrateNon-substrate0.7925
CYP450 2D6 substrateSubstrate0.8618
CYP450 3A4 substrateSubstrate0.7571
CYP450 1A2 substrateNon-inhibitor0.6918
CYP450 2C9 inhibitorNon-inhibitor0.9539
CYP450 2D6 inhibitorNon-inhibitor0.5197
CYP450 2C19 inhibitorNon-inhibitor0.8088
CYP450 3A4 inhibitorNon-inhibitor0.8177
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9413
Ames testNon AMES toxic0.7214
CarcinogenicityNon-carcinogens0.9554
BiodegradationNot ready biodegradable0.9815
Rat acute toxicity2.9191 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8906
hERG inhibition (predictor II)Non-inhibitor0.8992
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Purdue pharma lp
  • Purdue pharmaceutical products lp
  • Akorn inc
  • Barr laboratories inc
  • Hospira inc
  • Watson laboratories inc
  • Roxane laboratories inc
  • Mallinckrodt inc
  • Actavis totowa llc
  • Kv pharmaceutical co
  • Lannett holdings inc
  • Tyco healthcare mallinckrodt
Packagers
Dosage forms
FormRouteStrength
Liquidintramuscular; intravenous; subcutaneous2 mg
Liquidoral1 mg
Liquidoral5 mg/5mL
Powder for solutionintramuscular; intravenous; subcutaneous250 mg
Injection, powder, lyophilized, for solutionintramuscular; intravenous; subcutaneous10 mg/mL
Liquidintramuscular; intravenous; subcutaneous10 mg
Liquidintramuscular; intravenous; subcutaneous50 mg
Capsule (sustained-release)oral4.5 mg
Capsule (sustained-release)oral9.0 mg
Capsule (sustained-release)oral12 mg
Capsule (sustained-release)oral18 mg
Capsule (sustained-release)oral24 mg
Capsule (sustained-release)oral30 mg
Capsule (sustained-release)oral3 mg
Capsule (sustained-release)oral6 mg
Injection, solutionintramuscular; intravenous; subcutaneous.5 mg/mL
Injection, solutionintravenous.1 mg/mL
Injection, solutionintravenous.2 mg/mL
Injection, solutionintravenous.4 mg/mL
Injection, solutionintravenous1 mg/mL
Injection, solutionintravenous10 mg/mL
Injection, solutionintravenous2 mg/mL
Solutionintramuscular; intravenous; subcutaneous10 mg
Solutionintramuscular; intravenous; subcutaneous20 mg
Solutionintramuscular; intravenous; subcutaneous50 mg
Solutionintramuscular; intravenous; subcutaneous100 mg
Injectionintramuscular; intravenous; subcutaneous2 mg/mL
Injectionparenteral10 mg/mL
Injection, solutionintramuscular; intravenous; subcutaneous1 mg/mL
Injection, solutionintramuscular; intravenous; subcutaneous10 mg/mL
Injection, solutionintramuscular; intravenous; subcutaneous2 mg/mL
Injection, solutionintramuscular; intravenous; subcutaneous4 mg/mL
Solutionoral1 mg/mL
Solutionoral5 mg/5mL
Suppositoryrectal3 mg/1
Tabletoral2 mg/1
Tabletoral4 mg/1
Tabletoral8 mg/1
Tablet, film coatedoral2 mg/1
Tablet, film coatedoral4 mg/1
Tablet, film coatedoral8 mg/1
Tablet, extended releaseoral12 mg/1
Tablet, extended releaseoral16 mg/1
Tablet, extended releaseoral32 mg/1
Tablet, extended releaseoral8 mg/1
Solutionintramuscular; intravenous; subcutaneous2 mg
Tablet (extended-release)oral16 mg
Tablet (extended-release)oral32 mg
Tablet (extended-release)oral4 mg
Tablet (extended-release)oral8 mg
Capsule (controlled-delivery)oral12 mg
Capsule (controlled-delivery)oral16 mg
Capsule (controlled-delivery)oral24 mg
Syruporal1 mg
Suppositoryrectal3 mg
Tabletoral1 mg
Tabletoral2 mg
Tabletoral4 mg
Tabletoral8 mg
Prices
Unit descriptionCostUnit
Hydromorphone hcl powder166.25USD g
Dilaudid-hp 250 mg vial114.8USD vial
Dilaudid Sterile Powder 250 mg/vial78.99USD vial
HYDROmorphone HCl 6 3 mg Suppository Box54.92USD box
Hydromorphone Hp 50 50 mg/ml13.78USD ml
Dilaudid-Xp 50 mg/ml11.82USD ml
Hydromorphone 3 mg suppository11.11USD suppository
Dilaudid-Hp-Plus 20 mg/ml5.08USD ml
Hydromorphone Hp 20 20 mg/ml4.72USD ml
Hydromorph Contin 30 mg Controlled-Release Capsule4.21USD capsule
Hydromorph Contin 24 mg Controlled-Release Capsule3.52USD capsule
Dilaudid-Hp 10 mg/ml3.14USD ml
Hydromorphone Hp 10 mg/ml2.92USD ml
Hydromorph Contin 18 mg Controlled-Release Capsule2.75USD capsule
Hydromorphone 10 mg/ml ampul2.58USD ml
Pms-Hydromorphone 3 mg Suppository2.42USD suppository
Dilaudid 4 mg/ml ampul2.2USD ml
Dilaudid 8 mg tablet2.19USD tablet
HYDROmorphone HCl 4 mg/ml Solution 1ml Cartridge2.07USD cartridge
Hydromorph Contin 12 mg Controlled-Release Capsule1.91USD capsule
Dilaudid 2 mg/ml ampul1.81USD ml
Dilaudid 1 mg/ml ampul1.64USD ml
Hydromorphone hcl 8 mg tablet1.4USD tablet
Dilaudid 4 mg tablet1.36USD tablet
Hydromorphone 8 mg tablet1.32USD tablet
Dilaudid 2 mg/ml1.28USD ml
Hydromorphone 2 mg/ml1.19USD ml
Hydromorph Contin 6 mg Controlled-Release Capsule1.1USD capsule
Hydromorphone-ns 0.4 mg/ml1.08USD ml
Hydromorphone-ns 0.3 mg/ ml1.05USD ml
Hydromorphone 2 mg/ml vial1.02USD ml
Hydromorphone-ns 25 mg/25 ml1.01USD ml
Dilaudid 2 mg tablet1.0USD tablet
Hydromorphone-ns 2.5 mg/25 ml0.96USD ml
HYDROmorphone HCl 4 mg tablet0.8USD tablet
HYDROmorphone HCl 2 mg tablet0.77USD tablet
Hydromorph Contin 3 mg Controlled-Release Capsule0.73USD capsule
Hydromorphone 4 mg tablet0.72USD tablet
Dilaudid 8 mg Tablet0.55USD tablet
Hydromorphone-ns 0.2 mg/ml0.49USD ml
Hydromorphone 2 mg tablet0.37USD tablet
Pms-Hydromorphone 8 mg Tablet0.37USD tablet
Dilaudid 4 mg Tablet0.35USD tablet
Dilaudid-5 1 mg/ml liquid0.33USD ml
Hydromorphone-ns 5.5 mg/55 ml0.33USD ml
Dilaudid 2 mg Tablet0.23USD tablet
Pms-Hydromorphone 4 mg Tablet0.23USD tablet
Dilaudid 1 mg Tablet0.16USD tablet
Pms-Hydromorphone 2 mg Tablet0.15USD tablet
Pms-Hydromorphone 1 mg Tablet0.1USD tablet
Dilaudid 1 mg/ml Liquid0.09USD ml
Pms-Hydromorphone 1 mg/ml Liquid0.07USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5968551 No1994-12-242011-12-24Us
US6589960 No2000-11-092020-11-09Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point266.5 °CPhysProp
logP0.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility4.39 mg/mLALOGPS
logP1.69ALOGPS
logP1.62ChemAxon
logS-1.8ALOGPS
pKa (Strongest Acidic)10.11ChemAxon
pKa (Strongest Basic)8.59ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area49.77 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity78.26 m3·mol-1ChemAxon
Polarizability30.02 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
MSMass Spectrum (Electron Ionization)splash10-002r-6960000000-9f3d9b17d56e032d76c5View in MoNA
References
Synthesis Reference

Anne M. Hailes, Christopher E. French, Neil C. Bruce, “Morphinone reductase for the preparation of hydromorphone and hydrocodone.” U.S. Patent US5571685, issued November, 1990.

US5571685
General References
  1. Coda BA, Rudy AC, Archer SM, Wermeling DP: Pharmacokinetics and bioavailability of single-dose intranasal hydromorphone hydrochloride in healthy volunteers. Anesth Analg. 2003 Jul;97(1):117-23, table of contents. [PubMed:12818953 ]
  2. Vallner JJ, Stewart JT, Kotzan JA, Kirsten EB, Honigberg IL: Pharmacokinetics and bioavailability of hydromorphone following intravenous and oral administration to human subjects. J Clin Pharmacol. 1981 Apr;21(4):152-6. [PubMed:6165742 ]
External Links
ATC CodesN02AA03N02AG04
AHFS Codes
  • 28:08.08
PDB EntriesNot Available
FDA labelDownload (78.9 KB)
MSDSDownload (48.3 KB)
Interactions
Drug Interactions
Drug
AcepromazineAcepromazine may increase the hypotensive activities of Hydromorphone.
AcetazolamideThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Acetazolamide.
AlvimopanThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Alvimopan.
AmilorideThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Amiloride.
Ammonium chlorideAmmonium chloride may increase the excretion rate of Hydromorphone which could result in a higher serum level.
AmphetamineAmphetamine may increase the analgesic activities of Hydromorphone.
AzelastineHydromorphone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Hydromorphone.
BendroflumethiazideThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Bendroflumethiazide.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Hydromorphone.
BumetanideThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Bumetanide.
ButorphanolButorphanol may decrease the analgesic activities of Hydromorphone.
CathinoneCathinone may increase the analgesic activities of Hydromorphone.
ChlorothiazideThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Chlorothiazide.
ChlorthalidoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Chlorthalidone.
CyclothiazideThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Cyclothiazide.
DesmopressinThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Desmopressin.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Hydromorphone.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Hydromorphone.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Hydromorphone.
EluxadolineHydromorphone may increase the activities of Eluxadoline.
Etacrynic acidThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Ethacrynic acid.
EthanolHydromorphone may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
EthoxzolamideThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Ethoxzolamide.
FurosemideThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Furosemide.
HydrochlorothiazideThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Hydrochlorothiazide.
HydrocodoneHydromorphone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroflumethiazideThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Hydroflumethiazide.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Hydromorphone.
IndapamideThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Indapamide.
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Hydromorphone.
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Hydromorphone.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Hydromorphone.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Hydromorphone.
MethotrimeprazineHydromorphone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MetolazoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Metolazone.
MetyrosineHydromorphone may increase the sedative activities of Metyrosine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Hydromorphone.
MirtazapineHydromorphone may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Hydromorphone.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Hydromorphone.
NaltrexoneThe therapeutic efficacy of Hydromorphone can be decreased when used in combination with Naltrexone.
OrphenadrineHydromorphone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ParaldehydeHydromorphone may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineHydromorphone may increase the serotonergic activities of Paroxetine.
PegvisomantThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Hydromorphone.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Hydromorphone.
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Hydromorphone.
PramipexoleHydromorphone may increase the sedative activities of Pramipexole.
ProcarbazineThe risk or severity of adverse effects can be increased when Procarbazine is combined with Hydromorphone.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Hydromorphone.
RamosetronHydromorphone may increase the activities of Ramosetron.
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Hydromorphone.
RopiniroleHydromorphone may increase the sedative activities of Ropinirole.
RotigotineHydromorphone may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Hydromorphone.
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Hydromorphone.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Hydromorphone.
SpironolactoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Spironolactone.
SuccinylcholineSuccinylcholine may increase the bradycardic activities of Hydromorphone.
SuvorexantHydromorphone may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Hydromorphone.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Tedizolid Phosphate is combined with Hydromorphone.
ThalidomideHydromorphone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TicrynafenThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Ticrynafen.
TorasemideThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Torasemide.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Hydromorphone.
TriamtereneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Triamterene.
TrichlormethiazideThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Trichlormethiazide.
ZolpidemHydromorphone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food Interactions
  • Take without regard to meals. Avoid alcohol.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
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. Quigley C: Hydromorphone for acute and chronic pain. Cochrane Database Syst Rev. 2002;(1):CD003447. [PubMed:11869661 ]
  2. Inturrisi CE: Clinical pharmacology of opioids for pain. Clin J Pain. 2002 Jul-Aug;18(4 Suppl):S3-13. [PubMed:12479250 ]
  3. Sarhill N, Walsh D, Nelson KA: Hydromorphone: pharmacology and clinical applications in cancer patients. Support Care Cancer. 2001 Mar;9(2):84-96. [PubMed:11305075 ]
  4. Kumar P, Sunkaraneni S, Sirohi S, Dighe SV, Walker EA, Yoburn BC: Hydromorphone efficacy and treatment protocol impact on tolerance and mu-opioid receptor regulation. Eur J Pharmacol. 2008 Nov 12;597(1-3):39-45. doi: 10.1016/j.ejphar.2008.08.025. Epub 2008 Aug 30. [PubMed:18789923 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
partial agonist
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. Fang X, Larson DL, Portoghese PS: 7-spirobenzocyclohexyl derivatives of naltrexone, oxymorphone, and hydromorphone as selective opioid receptor ligands. J Med Chem. 1997 Sep 12;40(19):3064-70. [PubMed:9301669 ]
  2. Hennies HH, Friderichs E, Schneider J: Receptor binding, analgesic and antitussive potency of tramadol and other selected opioids. Arzneimittelforschung. 1988 Jul;38(7):877-80. [PubMed:2849950 ]
  3. Jiang Q, Sebastian A, Archer S, Bidlack JM: 5 beta-Methyl-14 beta-(p-nitrocinnamoylamino)-7,8-dihydromorphinone and its corresponding N-cyclopropylmethyl analog, N-cyclopropylmethylnor-5 beta-methyl-14 beta-(p-nitrocinnamoylamino)- 7,8-dihydromorphinone: mu-selective irreversible opioid antagonists. J Pharmacol Exp Ther. 1994 Mar;268(3):1107-13. [PubMed:7511163 ]
  4. Guay DR: Use of oral oxymorphone in the elderly. Consult Pharm. 2007 May;22(5):417-30. [PubMed:17658959 ]
  5. Hartvig P, Neil A, Terenius L, Antoni G, Rimland A, Ulin J, Langstrom B: Brain and plasma kinetics of the opioid 11C-hydromorphone in two macaque species. Pharmacol Toxicol. 1989 Sep;65(3):214-6. [PubMed:2478994 ]
  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
yes
Actions
agonist
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Gharagozlou P, Hashemi E, DeLorey TM, Clark JD, Lameh J: Pharmacological profiles of opioid ligands at kappa opioid receptors. BMC Pharmacol. 2006 Jan 25;6:3. [PubMed:16433932 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 ]
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 ]
  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:
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. 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:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the gener...
Gene Name:
PTGS1
Uniprot ID:
P23219
Molecular Weight:
68685.82 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 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on May 31, 2016 02:11