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Identification
NameKetorolac
Accession NumberDB00465  (APRD01060)
TypeSmall Molecule
GroupsApproved
Description

A pyrrolizine carboxylic acid derivative structurally related to indomethacin. It is an NSAID and is used principally for its analgesic activity. (From Martindale The Extra Pharmacopoeia, 31st ed)

Structure
Thumb
Synonyms
(+-)-5-Benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid
(+-)-Ketorolac
Ketorolac
Kétorolac
Ketorolaco
Ketorolacum
rac-Ketorolac
External Identifiers
  • BPPC
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Acularsolution/ drops5 mg/mLophthalmicAllergan, Inc.1992-12-01Not applicableUs
Acularsolution5 mg/mLophthalmicRebel Distributors Corp.1992-11-09Not applicableUs
Acularsolution/ drops5 mg/mLophthalmicSTAT Rx USA LLC1992-12-01Not applicableUs
Acular Liq 0.5%solution0.5 %ophthalmicAllergan Inc1992-12-31Not applicableCanada
Acular Lssolution0.4 %ophthalmicAllergan Inc2004-03-08Not applicableCanada
Acular Lssolution/ drops4 mg/mLophthalmicAllergan, Inc.2003-08-19Not applicableUs
Acuvailsolution0.45 %ophthalmicAllergan Inc2012-01-10Not applicableCanada
Acuvailsolution/ drops4.5 mg/mLophthalmicAllergan, Inc.2009-08-01Not applicableUs
Ketorolacsolution0.5 %ophthalmicAa Pharma Inc2002-12-06Not applicableCanada
Ketorolactablet10 mgoralAa Pharma Inc1998-07-03Not applicableCanada
Ketorolac Tromethaminesolution/ drops4 mg/mLophthalmicPhysicians Total Care, Inc.2014-03-28Not applicableUs
Ketorolac Tromethaminesolution/ drops4 mg/mLophthalmicPacific Pharma, Inc.2013-11-21Not applicableUs
Ketorolac Tromethamine Injection USPliquid30 mgintramuscularSandoz Canada Incorporated1999-05-21Not applicableCanada
Ketorolac Tromethamine Injection USPliquid10 mgintramuscularSabex IncNot applicableNot applicableCanada
Ketorolac Tromethamine Injection, USPliquid30 mgintramuscularFresenius Kabi Canada Ltd2002-05-23Not applicableCanada
Ketorolac Tromethamine Injection, USPsolution30 mgintramuscularMda Inc.Not applicableNot applicableCanada
Ketorolac Tromethamine Injection, USPsolution30 mgintramuscularHospira Healthcare Corporation2014-05-29Not applicableCanada
Novo-ketorolac - Tab 10mgtablet10 mgoralNovopharm Limited1998-06-022015-10-26Canada
Nu-ketorolactablet10 mgoralNu Pharm Inc1998-10-202012-09-04Canada
Nu-ketorolac Ophthalmic Solutionsolution0.5 %ophthalmicNu Pharm IncNot applicableNot applicableCanada
Ratio-ketorolacsolution0.5 %ophthalmicRatiopharm Inc Division Of Teva Canada Limited2003-07-142014-09-19Canada
Riva-ketorolac 10 mgtablet10 mgoralLaboratoire Riva IncNot applicableNot applicableCanada
Sprixspray, metered15.75 mg/1nasalPhysicians Total Care, Inc.2011-07-20Not applicableUs
Sprixspray, metered15.75 mg/1nasalMedsource Pharmaceuticals2011-04-262016-02-25Us
Sprixspray, metered15.75 mg/1nasalH.J. Harkins Company, Inc.2011-04-26Not applicableUs
Sprixspray, metered15.75 mg/1nasalAmerican Regent, Inc.2011-04-262016-01-16Us
Sprixspray, metered15.75 mg/1nasalEgalet Us Inc.2011-04-26Not applicableUs
Toradoltablet10 mgoralAtnahs Pharma Uk Limited1995-12-31Not applicableCanada
Toradol Imsolution10 mgintramuscularAtnahs Pharma Uk Limited1996-10-16Not applicableCanada
Toradol Im 30mg/mlliquid30 mgintramuscularHoffmann La Roche Limited1996-12-312011-01-04Canada
Toradol Inj 10mg/mlliquid10 mgintramuscularSyntex Inc.1993-12-311997-08-26Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-ketorolac Injectablesolution30 mgintramuscularApotex Inc2001-12-04Not applicableCanada
Ketorolactablet, film coated10 mg/1oralSTAT Rx USA LLC2010-09-15Not applicableUs
Ketorolac Tromethaminesolution/ drops5 mg/mLophthalmicSun Pharma Global FZE2014-12-15Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2010-04-20Not applicableUs
Ketorolac Tromethaminesolution5 mg/mLophthalmicAkorn Inc.2009-11-05Not applicableUs
Ketorolac Tromethaminesolution4 mg/mLophthalmicAkorn Inc.2009-11-05Not applicableUs
Ketorolac Tromethaminesolution5 mg/mLophthalmicPhysicians Total Care, Inc.2010-11-03Not applicableUs
Ketorolac Tromethamineinjection15 mg/mLintramuscular; intravenousWest Ward Pharmaceutical Corp.2004-07-21Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralNorthwind Pharmaceuticals, LLC2014-07-15Not applicableUs
Ketorolac Tromethaminesolution/ drops5 mg/mLophthalmicApotex Corp.2009-12-07Not applicableUs
Ketorolac Tromethamineinjection15 mg/mLintramuscular; intravenousPfizer Laboratories Div Pfizer Inc2011-05-112016-04-13Us
Ketorolac Tromethaminesolution/ drops5 mg/mLophthalmicSun Pharma Global FZE2014-12-15Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralCardinal Health2010-04-20Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralKeltman Pharmaceuticals Inc.2010-04-20Not applicableUs
Ketorolac Tromethamineinjection, solution30 mg/mLintramuscular; intravenousCardinal Health2011-07-27Not applicableUs
Ketorolac Tromethamineinjection, solution15 mg/mLintramuscular; intravenousFresenius Kabi USA, LLC2001-09-05Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralA S Medication Solutions1998-06-17Not applicableUs
Ketorolac Tromethaminesolution4 mg/mLophthalmicSandoz Inc2009-11-05Not applicableUs
Ketorolac Tromethamineinjection60 mg/2mLintramuscularAGILA SPECIALTIES PRIVATE LIMITED2014-08-05Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralPreferred Pharmaceuticals, Inc.2015-01-21Not applicableUs
Ketorolac Tromethaminesolution/ drops5 mg/mLophthalmicSun Pharma Global FZE2014-12-15Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralAidarex Pharmaceuticals LLC1998-06-17Not applicableUs
Ketorolac Tromethaminesolution/ drops4.5 mg/mLophthalmicAkorn2014-02-10Not applicableUs
Ketorolac Tromethamineinjection30 mg/mLintramuscular; intravenousPhysicians Total Care, Inc.2000-11-03Not applicableUs
Ketorolac Tromethamineinjection, solution60 mg/2mLintramuscularHospira, Inc.1997-06-05Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralUnit Dose Services2010-04-20Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralClinical Solutions Wholesale1998-06-17Not applicableUs
Ketorolac Tromethamineinjection, solution15 mg/mLintramuscular; intravenousCardinal Health2011-07-27Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralCarilion Materials Management1998-06-17Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralProficient Rx LP1998-06-17Not applicableUs
Ketorolac Tromethamineinjection, solution15 mg/mLintramuscularREMEDYREPACK INC.2016-03-08Not applicableUs
Ketorolac Tromethamineinjection30 mg/mLintramuscular; intravenousAGILA SPECIALTIES PRIVATE LIMITED2014-08-05Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralPd Rx Pharmaceuticals, Inc.2010-09-15Not applicableUs
Ketorolac Tromethamineinjection, solution30 mg/mLintramuscular; intravenousSagent Pharmaceuticals2014-09-05Not applicableUs
Ketorolac Tromethaminesolution5 mg/mLophthalmicSTAT Rx USA LLC2009-11-05Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralPhysicians Total Care, Inc.2001-01-10Not applicableUs
Ketorolac Tromethamineinjection, solution30 mg/mLintramuscular; intravenousHospira, Inc.1997-06-05Not applicableUs
Ketorolac Tromethaminesolution5 mg/mLophthalmicUnit Dose Services2009-11-05Not applicableUs
Ketorolac Tromethamineinjection30 mg/mLintramuscular; intravenousWockhardt Limited2007-03-27Not applicableUs
Ketorolac Tromethamineinjection, solution60 mg/2mLintramuscularCardinal Health2011-07-27Not applicableUs
Ketorolac Tromethamineinjection30 mg/mLintramuscular; intravenousWOCKHARDT USA LLC2007-03-27Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralDIRECT RX2014-01-01Not applicableUs
Ketorolac Tromethamineinjection30 mg/mLintramuscularREMEDYREPACK INC.2013-06-12Not applicableUs
Ketorolac Tromethamineinjection15 mg/mLintramuscular; intravenousAGILA SPECIALTIES PRIVATE LIMITED2014-08-05Not applicableUs
Ketorolac Tromethamineinjection, solution15 mg/mLintramuscular; intravenousSagent Pharmaceuticals2014-09-05Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralH.J. Harkins Company, Inc.2010-04-20Not applicableUs
Ketorolac Tromethamineinjection, solution15 mg/mLintramuscular; intravenousHospira, Inc.1997-06-05Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralLake Erie Medical DBA Quality Care Products LLC2010-11-17Not applicableUs
Ketorolac Tromethamineinjection15 mg/mLintramuscular; intravenousWockhardt Limited2007-03-27Not applicableUs
Ketorolac Tromethamineinjection, solution60 mg/2mLintramuscular; intravenousCardinal Health1999-04-26Not applicableUs
Ketorolac Tromethamineinjection15 mg/mLintramuscular; intravenousWOCKHARDT USA LLC2007-03-27Not applicableUs
Ketorolac Tromethamineinjection, solution30 mg/mLintravenousREMEDYREPACK INC.2015-07-15Not applicableUs
Ketorolac Tromethamineinjection, solution30 mg/mLintramuscular; intravenousHospira, Inc.1999-01-27Not applicableUs
Ketorolac Tromethamineinjection, solution15 mg/mLintramuscular; intravenousBd Rx, Inc.2015-11-02Not applicableUs
Ketorolac Tromethaminesolution5 mg/mLophthalmicSun Pharma Global Inc.2009-11-06Not applicableUs
Ketorolac Tromethaminesolution4 mg/mLophthalmicRebel Distributors Corp2009-11-05Not applicableUs
Ketorolac Tromethaminetablet10 mg/1oralApotheca, Inc2005-10-25Not applicableUs
Ketorolac Tromethamineinjection, solution30 mg/mLintramuscular; intravenousGeneral Injectables & Vaccines, Inc2012-04-10Not applicableUs
Ketorolac Tromethamineinjection, solution15 mg/mLintramuscular; intravenousHospira, Inc.1999-01-27Not applicableUs
Ketorolac Tromethamineinjection30 mg/mLintramuscularREMEDYREPACK INC.2013-06-14Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralPd Rx Pharmaceuticals, Inc.2010-09-15Not applicableUs
Ketorolac Tromethamineinjection, solution15 mg/mLintramuscular; intravenousCardinal Health1999-04-26Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralReady Meds2013-05-16Not applicableUs
Ketorolac Tromethamineinjection, solution30 mg/mLintramuscularREMEDYREPACK INC.2015-03-25Not applicableUs
Ketorolac Tromethamineinjection, solution30 mg/mLintramuscularCardinal Health2000-10-18Not applicableUs
Ketorolac Tromethamineinjection, solution60 mg/2mLintramuscularBd Rx, Inc.2015-11-02Not applicableUs
Ketorolac Tromethaminesolution4 mg/mLophthalmicRebel Distributors Corp2009-11-05Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralBlenheim Pharmacal, Inc.2011-07-15Not applicableUs
Ketorolac Tromethamineinjection, solution30 mg/mLintramuscular; intravenousGeneral Injectables & Vaccines, Inc2012-04-10Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralMylan Pharmaceuticals Inc.2013-05-16Not applicableUs
Ketorolac Tromethamineinjection30 mg/mLintramuscularREMEDYREPACK INC.2013-06-14Not applicableUs
Ketorolac Tromethamineinjection, solution60 mg/2mLintramuscularCardinal Health2000-10-18Not applicableUs
Ketorolac Tromethamineinjection, solution60 mg/2mLintramuscularCardinal Health2011-07-27Not applicableUs
Ketorolac Tromethamineinjection, solution30 mg/mLintramuscularMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2010-05-03Not applicableUs
Ketorolac Tromethamineinjection, solution60 mg/2mLintramuscularREMEDYREPACK INC.2014-10-29Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralCentral Texas Community Health Centers1998-06-17Not applicableUs
Ketorolac Tromethamineinjection, solution30 mg/mLintramuscular; intravenousBd Rx, Inc.2015-11-02Not applicableUs
Ketorolac Tromethaminesolution5 mg/mLophthalmicSun Pharma Global Inc.2009-11-06Not applicableUs
Ketorolac Tromethamineinjection, solution30 mg/mLintramuscularCardinal Health2000-10-18Not applicableUs
Ketorolac Tromethamineinjection, solution15 mg/mLintramuscular; intravenousCardinal Health2011-07-27Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralbryant ranch prepack2010-04-20Not applicableUs
Ketorolac Tromethamineinjection, solution30 mg/mLintramuscularREMEDYREPACK INC.2015-11-12Not applicableUs
Ketorolac Tromethaminesolution5 mg/mLophthalmicProficient Rx LP2009-11-05Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralAvera Mc Kennan Hospital2015-04-27Not applicableUs
Ketorolac Tromethaminesolution5 mg/mLophthalmicSun Pharma Global Inc.2009-11-06Not applicableUs
Ketorolac Tromethamineinjection, solution30 mg/mLintramuscular; intravenousRebel Distributors Corp1999-01-27Not applicableUs
Ketorolac Tromethamineinjection30 mg/mLintramuscularWest Ward Pharmaceutical Corp.2004-07-21Not applicableUs
Ketorolac Tromethamineinjection30 mg/mLintramuscularREMEDYREPACK INC.2013-06-10Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralTeva Pharmaceuticals USA Inc1998-06-17Not applicableUs
Ketorolac Tromethaminetablet10 mg/1oralREMEDYREPACK INC.2011-12-28Not applicableUs
Ketorolac Tromethaminesolution5 mg/mLophthalmicPreferred Pharmaceuticals, Inc.2015-04-13Not applicableUs
Ketorolac Tromethaminesolution5 mg/mLophthalmicLake Erie Medical DBA Quality Care Products LLC2009-11-05Not applicableUs
Ketorolac Tromethaminetablet, film coated10 mg/1oralRebel Distributors Corp2010-04-20Not applicableUs
Ketorolac Tromethamineinjection30 mg/mLintramuscular; intravenousWest Ward Pharmaceutical Corp.2004-07-21Not applicableUs
Ketorolac Tromethaminesolution5 mg/1ophthalmicREMEDYREPACK INC.2013-04-15Not applicableUs
Ketorolac Tromethamineinjection30 mg/mLintramuscular; intravenousPfizer Laboratories Div Pfizer Inc2011-05-112016-04-13Us
Ketorolac Tromethaminetablet10 mg/1oralREMEDYREPACK INC.2010-12-06Not applicableUs
Ketorolac Tromethamineinjection, solution15 mg/mLintramuscularCardinal Health2001-09-05Not applicableUs
Ketorolac Tromethamineinjection, solution30 mg/mLintramuscular; intravenousCardinal Health2011-07-27Not applicableUs
Ketorolac Tromethamineinjection, solution30 mg/mLintramuscularFresenius Kabi USA, LLC2000-10-18Not applicableUs
Ketorolac Tromethaminesolution5 mg/mLophthalmicFalcon Pharmaceuticals, Ltd.2009-11-05Not applicableUs
Ketotolac Tromethaminetablet, film coated10 mg/1oralSTAT Rx USA LLC2010-09-15Not applicableUs
Approved Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Toradol Tab 10mgtablet10 mgoralSyntex Inc.1991-12-311996-09-30Canada
Unapproved/Other Products Not Available
International Brands
NameCompany
BedoralBe-Tabs Pharmaceuticals
DoltenPfizer
Dolten SLPfizer
Dorixina forte NFRoemmers
EmodolJayson
EtoracIncepta
KetonicEskayef
KetoraMedicon
LixidolRoche
SyndolRoche
TaradylRoche
TarasynRoche
ToradolRoche
Brand mixtures
NameLabellerIngredients
OmidriaOmeros Corporation
Salts
Name/CASStructureProperties
Ketorolac tromethamine
74103-07-4
Thumb
  • InChI Key: BWHLPLXXIDYSNW-UHFFFAOYSA-N
  • Monoisotopic Mass: 376.163436501
  • Average Mass: 376.409
DBSALT001045
Categories
UNIIYZI5105V0L
CAS number74103-06-3
WeightAverage: 255.2686
Monoisotopic: 255.089543287
Chemical FormulaC15H13NO3
InChI KeyInChIKey=OZWKMVRBQXNZKK-UHFFFAOYSA-N
InChI
InChI=1S/C15H13NO3/c17-14(10-4-2-1-3-5-10)13-7-6-12-11(15(18)19)8-9-16(12)13/h1-7,11H,8-9H2,(H,18,19)
IUPAC Name
5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid
SMILES
OC(=O)C1CCN2C1=CC=C2C(=O)C1=CC=CC=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as acetophenones. These are organic compounds containing the acetophenone structure.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassAcetophenones
Direct ParentAcetophenones
Alternative Parents
Substituents
  • Acetophenone
  • Aryl ketone
  • Pyrrolizine
  • Benzoyl
  • Substituted pyrrole
  • Heteroaromatic compound
  • Pyrrole
  • Ketone
  • Azacycle
  • Organoheterocyclic compound
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the short-term (~5 days) management of moderately severe acute pain that requires analgesia at the opioid level, usually in a postoperative setting.
PharmacodynamicsKetorolac, an antiinflammatory agent with analgesic and antipyretic properties, is used to treat osteoarthritis and control acute pain. It is a peripherally acting analgesic. The biological activity of ketorolac tromethamine is associated with the S-form. Ketorolac tromethamine possesses no sedative or anxiolytic properties.
Mechanism of actionKetorolac is a nonsteroidal anti-inflammatory drug (NSAID) chemically related to indomethacin and tolmetin. Ketorolac tromethamine is a racemic mixture of [-]S- and [+]R-enantiomeric forms, with the S-form having analgesic activity. Its antiinflammatory effects are believed to be due to inhibition of both cylooxygenase-1 (COX-1) and cylooxygenase-2 (COX-2) which leads to the inhibition of prostaglandin synthesis leading to decreased formation of precursors of prostaglandins and thromboxanes from arachidonic acid. The resultant reduction in prostaglandin synthesis and activity may be at least partially responsible for many of the adverse, as well as the therapeutic, effects of these medications. Analgesia is probably produced via a peripheral action in which blockade of pain impulse generation results from decreased prostaglandin activity. However, inhibition of the synthesis or actions of other substances that sensitize pain receptors to mechanical or chemical stimulation may also contribute to the analgesic effect. In terms of the ophthalmic applications of ketorolac - ocular administration of ketorolac reduces prostaglandin E2 levels in aqueous humor, secondary to inhibition of prostaglandin biosynthesis.
Related Articles
AbsorptionRapidly and completely absorbed after oral administration
Volume of distribution
  • 0.26 ± 0.08 L/kg [children 4 to 8 years old]
Protein binding99%
Metabolism

Primarily hepatic. Less than 50% of a dose is metabolized. The major metabolites are a glucuronide conjugate, which may also be formed in the kidney, and p-hydroxy ketorolac. Neither metabolite has significant analgesic activity.

SubstrateEnzymesProduct
Ketorolac
Not Available
4-hydroxy ketorolacDetails
Route of eliminationThe principal route of elimination of ketorolac and its metabolites is renal. Approximately 6% of a dose is excreted in the feces.
Half life2.5 hours for the S-enantiomer compared with 5 hours for the R-enantiomer
Clearance
  • 0.042 +/- 0.01 L/hr/kg [Pediatric Patients]
  • 0.02 L/h/kg [Normal Subjects IM]
  • 0.03 L/h/kg [Normal Subjects oral]
  • 0.02 L/h/kg [Healthy Elderly Subjects IM]
  • 0.02 L/h/kg [Healthy Elderly Subjects oral]
  • 0.03 L/h/kg [Patients with Hepatic Dysfunction IM]
  • 0.03 L/h/kg [Patients with Hepatic Dysfunction oral]
  • 0.02 L/h/kg [Patients with Renal Impairment IM]
  • 0.02 L/h/kg [Patients with Renal Impairment oral]
  • 0.02 L/h/kg [Renal Dialysis Patients IM]
ToxicityLD50 = 189 mg/kg (rat, oral).
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Ketorolac Action PathwayDrug actionSMP00098
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9919
Blood Brain Barrier+0.7918
Caco-2 permeable-0.8957
P-glycoprotein substrateNon-substrate0.7127
P-glycoprotein inhibitor INon-inhibitor0.9624
P-glycoprotein inhibitor IINon-inhibitor0.8684
Renal organic cation transporterNon-inhibitor0.6042
CYP450 2C9 substrateNon-substrate0.7845
CYP450 2D6 substrateNon-substrate0.7046
CYP450 3A4 substrateNon-substrate0.6338
CYP450 1A2 substrateInhibitor0.5483
CYP450 2C9 inhibitorNon-inhibitor0.9081
CYP450 2D6 inhibitorNon-inhibitor0.9333
CYP450 2C19 inhibitorNon-inhibitor0.9225
CYP450 3A4 inhibitorNon-inhibitor0.9621
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9467
Ames testNon AMES toxic0.7615
CarcinogenicityNon-carcinogens0.9592
BiodegradationNot ready biodegradable0.5254
Rat acute toxicity2.5902 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9478
hERG inhibition (predictor II)Non-inhibitor0.9298
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Akorn strides llc
  • Amphastar pharmaceutical inc
  • Apotex inc richmond hill
  • Apothecon inc div bristol myers squibb
  • App pharmaceuticals llc
  • Baxter healthcare corp anesthesia and critical care
  • Baxter healthcare corp anesthesia critical care
  • Bedford laboratories div ben venue laboratories inc
  • Claris lifesciences ltd
  • Gland pharma ltd
  • Hospira inc
  • Luitpold pharmaceuticals inc
  • Sandoz canada inc
  • Sun pharma global inc
  • Wockhardt ltd
  • Roche palo alto llc
  • Allergan inc
  • Allergan
  • Akorn inc
  • Alcon inc
  • Roxro pharma inc
  • Mylan pharmaceuticals inc
  • Pliva inc
  • Roxane laboratories inc
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
Packagers
Dosage forms
FormRouteStrength
Solution/ dropsophthalmic5 mg/mL
Solutionophthalmic0.5 %
Solutionophthalmic0.4 %
Solution/ dropsophthalmic4 mg/mL
Solutionophthalmic0.45 %
Solution/ dropsophthalmic4.5 mg/mL
Solutionintramuscular30 mg
Tabletoral10 mg
Injectionintramuscular30 mg/mL
Injectionintramuscular60 mg/2mL
Injectionintramuscular; intravenous15 mg/mL
Injectionintramuscular; intravenous30 mg/mL
Injection, solutionintramuscular15 mg/mL
Injection, solutionintramuscular30 mg/mL
Injection, solutionintramuscular60 mg/2mL
Injection, solutionintramuscular; intravenous15 mg/mL
Injection, solutionintramuscular; intravenous30 mg/mL
Injection, solutionintramuscular; intravenous60 mg/2mL
Injection, solutionintravenous30 mg/mL
Solutionophthalmic4 mg/mL
Solutionophthalmic5 mg/1
Solutionophthalmic5 mg/mL
Tabletoral10 mg/1
Tablet, film coatedoral10 mg/1
Liquidintramuscular30 mg
Injection, solution, concentrateintraocular
Spray, meterednasal15.75 mg/1
Solutionintramuscular10 mg
Liquidintramuscular10 mg
Prices
Unit descriptionCostUnit
Acular 0.5% Solution 10ml Bottle254.39USD bottle
Acular 0.5% Solution 5ml Bottle122.36USD bottle
Ketorolac Tromethamine 0.4% Solution 5ml Bottle109.72USD bottle
Ketorolac tromethamine powder71.05USD g
Acular 0.5% Solution 3ml Bottle59.34USD bottle
Acular ls 0.4% ophth sol24.46USD ml
Acular 0.5% eye drops18.68USD ml
Ketorolac 30 mg/ml syringe8.77USD ml
Ketorolac 15 mg/ml syringe8.39USD ml
Acuvail 0.45% ophth solution4.17USD each
Ketorolac Tromethamine 30 mg/ml3.9USD ml
Acular 0.5 % Solution3.78USD ml
Toradol 10 mg/ml2.52USD ml
Ketorolac im 30 mg/ml syring2.11USD ml
Apo-Ketorolac 0.5 % Solution2.11USD ml
Ratio-Ketorolac 0.5 % Solution2.11USD ml
Toradol 10 mg tablet1.53USD tablet
Ketorolac Tromethamine 10 mg tablet1.06USD tablet
Ketorolac 10 mg tablet0.93USD tablet
Toradol 10 mg Tablet0.76USD tablet
Apo-Ketorolac 10 mg Tablet0.43USD tablet
Novo-Ketorolac 10 mg Tablet0.43USD tablet
Nu-Ketorolac 10 mg Tablet0.43USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1328614 No1994-04-192011-04-19Canada
US5110493 No1992-11-052009-11-05Us
US6333044 No1998-12-252018-12-25Us
US7842714 No2009-08-152029-08-15Us
US8008338 Yes2007-11-242027-11-24Us
US8173707 No2003-07-302023-07-30Us
US8207215 Yes2004-11-282024-11-28Us
US8377982 Yes2004-11-282024-11-28Us
US8512717 No2008-03-072028-03-07Us
US8541463 Yes2004-11-282024-11-28Us
US8586633 No2003-07-302023-07-30Us
US8648107 No2004-05-282024-05-28Us
US8906950 No2004-05-282024-05-28Us
US8946281 No2004-05-282024-05-28Us
US8992952 No2004-08-052024-08-05Us
US9066856 No2013-10-232033-10-23Us
US9192571 No2008-03-072028-03-07Us
US9216127 No2004-05-282024-05-28Us
US9216167 No2004-05-282024-05-28Us
US9278101 No2003-07-302023-07-30Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point165-167 °C (tromethamine salt)Not Available
water solubility25 mg/mL (tromethamine salt)Not Available
logP2.1Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.513 mg/mLALOGPS
logP2.66ALOGPS
logP2.28ChemAxon
logS-2.7ALOGPS
pKa (Strongest Acidic)3.84ChemAxon
pKa (Strongest Basic)-7.8ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area59.3 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity70.19 m3·mol-1ChemAxon
Polarizability26.67 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Peter J. Harrington, Hiralal N. Khatri, George C. Schloemer, “Preparation of ketorolac.” U.S. Patent US6323344, issued October, 1989.

US6323344
General ReferencesNot Available
External Links
ATC CodesM01AB15S01BC05
AHFS Codes
  • 28:08.04.92
  • 52:08.20
PDB EntriesNot Available
FDA labelDownload (138 KB)
MSDSDownload (76.4 KB)
Interactions
Drug Interactions
Drug
AbciximabKetorolac may increase the anticoagulant activities of Abciximab.
AcenocoumarolKetorolac may increase the anticoagulant activities of Acenocoumarol.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Ketorolac is combined with Acetylsalicylic acid.
AliskirenKetorolac may decrease the antihypertensive activities of Aliskiren.
AlteplaseKetorolac may increase the anticoagulant activities of Alteplase.
AmikacinKetorolac may decrease the excretion rate of Amikacin which could result in a lower serum level and potentially a reduction in efficacy.
AmitriptylineAmitriptyline may increase the antiplatelet activities of Ketorolac.
AnistreplaseKetorolac may increase the anticoagulant activities of Anistreplase.
ApixabanThe risk or severity of adverse effects can be increased when Ketorolac is combined with Apixaban.
ArbekacinKetorolac may decrease the excretion rate of Arbekacin which could result in a lower serum level and potentially a reduction in efficacy.
Atracurium besylateThe risk or severity of adverse effects can be increased when Ketorolac is combined with Atracurium besylate.
BalsalazideKetorolac may increase the nephrotoxic activities of Balsalazide.
CaffeineThe risk or severity of adverse effects can be increased when Ketorolac is combined with Caffeine.
CelecoxibThe risk or severity of adverse effects can be increased when Ketorolac is combined with Celecoxib.
Cisatracurium besylateThe risk or severity of adverse effects can be increased when Ketorolac is combined with Cisatracurium besylate.
Citric AcidKetorolac may increase the anticoagulant activities of Citric Acid.
ColesevelamColesevelam can cause a decrease in the absorption of Ketorolac resulting in a reduced serum concentration and potentially a decrease in efficacy.
CollagenaseThe risk or severity of adverse effects can be increased when Ketorolac is combined with Collagenase.
CyclosporineKetorolac may increase the nephrotoxic activities of Cyclosporine.
Dabigatran etexilateKetorolac may increase the anticoagulant activities of Dabigatran etexilate.
DalteparinKetorolac may increase the anticoagulant activities of Dalteparin.
DasatinibDasatinib may increase the anticoagulant activities of Ketorolac.
DeferasiroxThe risk or severity of adverse effects can be increased when Ketorolac is combined with Deferasirox.
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Ketorolac is combined with Deoxycholic Acid.
DesmopressinThe risk or severity of adverse effects can be increased when Ketorolac is combined with Desmopressin.
DexketoprofenThe risk or severity of adverse effects can be increased when Dexketoprofen is combined with Ketorolac.
DiclofenacThe risk or severity of adverse effects can be increased when Ketorolac is combined with Diclofenac.
DicoumarolKetorolac may increase the anticoagulant activities of Dicoumarol.
DiflunisalThe risk or severity of adverse effects can be increased when Ketorolac is combined with Diflunisal.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Ketorolac.
DihydrocodeineThe risk or severity of adverse effects can be increased when Ketorolac is combined with Dihydrocodeine.
DrospirenoneKetorolac may increase the hyperkalemic activities of Drospirenone.
Edetic AcidKetorolac may increase the anticoagulant activities of Edetic Acid.
EnoxaparinKetorolac may increase the anticoagulant activities of Enoxaparin.
EplerenoneKetorolac may decrease the antihypertensive activities of Eplerenone.
Ethyl biscoumacetateKetorolac may increase the anticoagulant activities of Ethyl biscoumacetate.
EtodolacThe risk or severity of adverse effects can be increased when Ketorolac is combined with Etodolac.
FenoprofenThe risk or severity of adverse effects can be increased when Ketorolac is combined with Fenoprofen.
FloctafenineThe risk or severity of adverse effects can be increased when Floctafenine is combined with Ketorolac.
FludrocortisoneThe risk or severity of adverse effects can be increased when Fludrocortisone is combined with Ketorolac.
FlurbiprofenThe risk or severity of adverse effects can be increased when Ketorolac is combined with Flurbiprofen.
Fondaparinux sodiumKetorolac may increase the anticoagulant activities of Fondaparinux sodium.
FramycetinKetorolac may decrease the excretion rate of Framycetin which could result in a lower serum level and potentially a reduction in efficacy.
GentamicinKetorolac may decrease the excretion rate of Gentamicin which could result in a lower serum level and potentially a reduction in efficacy.
GlucosamineGlucosamine may increase the antiplatelet activities of Ketorolac.
HaloperidolThe risk or severity of adverse effects can be increased when Ketorolac is combined with Haloperidol.
HeparinKetorolac may increase the anticoagulant activities of Heparin.
HomoharringtonineThe risk or severity of adverse effects can be increased when Ketorolac is combined with Homoharringtonine.
HydralazineKetorolac may decrease the antihypertensive activities of Hydralazine.
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Ketorolac is combined with Ibritumomab.
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Ketorolac.
IbuprofenThe risk or severity of adverse effects can be increased when Ketorolac is combined with Ibuprofen.
IndomethacinThe risk or severity of adverse effects can be increased when Ketorolac is combined with Indomethacin.
InfliximabThe risk or severity of adverse effects can be increased when Ketorolac is combined with Infliximab.
KanamycinKetorolac may decrease the excretion rate of Kanamycin which could result in a lower serum level and potentially a reduction in efficacy.
KetoprofenThe risk or severity of adverse effects can be increased when Ketorolac is combined with Ketoprofen.
LimaprostLimaprost may increase the antiplatelet activities of Ketorolac.
LithiumThe serum concentration of Lithium can be increased when it is combined with Ketorolac.
Mefenamic acidThe risk or severity of adverse effects can be increased when Ketorolac is combined with Mefenamic acid.
MeloxicamThe risk or severity of adverse effects can be increased when Ketorolac is combined with Meloxicam.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Ketorolac.
MorniflumateThe risk or severity of adverse effects can be increased when Morniflumate is combined with Ketorolac.
NabumetoneThe risk or severity of adverse effects can be increased when Ketorolac is combined with Nabumetone.
NadololKetorolac may decrease the antihypertensive activities of Nadolol.
NaproxenThe risk or severity of adverse effects can be increased when Ketorolac is combined with Naproxen.
NeomycinKetorolac may decrease the excretion rate of Neomycin which could result in a lower serum level and potentially a reduction in efficacy.
NetilmicinKetorolac may decrease the excretion rate of Netilmicin which could result in a lower serum level and potentially a reduction in efficacy.
ObinutuzumabThe risk or severity of adverse effects can be increased when Ketorolac is combined with Obinutuzumab.
Omega-3 fatty acidsOmega-3 fatty acids may increase the antiplatelet activities of Ketorolac.
OxaprozinThe risk or severity of adverse effects can be increased when Ketorolac is combined with Oxaprozin.
PamidronateThe risk or severity of adverse effects can be increased when Ketorolac is combined with Pamidronate.
PancuroniumThe risk or severity of adverse effects can be increased when Ketorolac is combined with Pancuronium.
ParoxetineParoxetine may increase the antiplatelet activities of Ketorolac.
PemetrexedThe serum concentration of Pemetrexed can be increased when it is combined with Ketorolac.
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Ketorolac.
PentoxifyllineThe risk or severity of adverse effects can be increased when Ketorolac is combined with Pentoxifylline.
PerindoprilThe risk or severity of adverse effects can be increased when Perindopril is combined with Ketorolac.
PhenindioneKetorolac may increase the anticoagulant activities of Phenindione.
PhenprocoumonKetorolac may increase the anticoagulant activities of Phenprocoumon.
PiroxicamThe risk or severity of adverse effects can be increased when Ketorolac is combined with Piroxicam.
PorfimerKetorolac may increase the photosensitizing activities of Porfimer.
PralatrexateThe serum concentration of Pralatrexate can be increased when it is combined with Ketorolac.
ProbenecidThe serum concentration of Ketorolac can be increased when it is combined with Probenecid.
ReteplaseKetorolac may increase the anticoagulant activities of Reteplase.
RibostamycinKetorolac may decrease the excretion rate of Ribostamycin which could result in a lower serum level and potentially a reduction in efficacy.
RidogrelKetorolac may increase the anticoagulant activities of Ridogrel.
RivaroxabanKetorolac may increase the anticoagulant activities of Rivaroxaban.
RocuroniumThe risk or severity of adverse effects can be increased when Ketorolac is combined with Rocuronium.
SparfloxacinKetorolac may increase the neuroexcitatory activities of Sparfloxacin.
SpectinomycinKetorolac may decrease the excretion rate of Spectinomycin which could result in a lower serum level and potentially a reduction in efficacy.
StreptokinaseKetorolac may increase the anticoagulant activities of Streptokinase.
StreptomycinKetorolac may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
SulindacThe risk or severity of adverse effects can be increased when Ketorolac is combined with Sulindac.
SulodexideKetorolac may increase the anticoagulant activities of Sulodexide.
TacrolimusKetorolac may increase the nephrotoxic activities of Tacrolimus.
TalniflumateThe risk or severity of adverse effects can be increased when Talniflumate is combined with Ketorolac.
TenecteplaseKetorolac may increase the anticoagulant activities of Tenecteplase.
TenofovirThe risk or severity of adverse effects can be increased when Ketorolac is combined with Tenofovir.
Tiaprofenic acidThe risk or severity of adverse effects can be increased when Ketorolac is combined with Tiaprofenic acid.
TipranavirTipranavir may increase the antiplatelet activities of Ketorolac.
TobramycinKetorolac may decrease the excretion rate of Tobramycin which could result in a lower serum level and potentially a reduction in efficacy.
TolmetinThe risk or severity of adverse effects can be increased when Ketorolac is combined with Tolmetin.
TorasemideKetorolac may decrease the diuretic activities of Torasemide.
TositumomabThe risk or severity of adverse effects can be increased when Ketorolac is combined with Tositumomab.
TreprostinilThe risk or severity of adverse effects can be increased when Treprostinil is combined with Ketorolac.
TriamtereneKetorolac may decrease the antihypertensive activities of Triamterene.
TrichlormethiazideThe therapeutic efficacy of Trichlormethiazide can be decreased when used in combination with Ketorolac.
UnoprostoneThe therapeutic efficacy of Unoprostone can be decreased when used in combination with Ketorolac.
UrokinaseKetorolac may increase the anticoagulant activities of Urokinase.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Ketorolac.
VancomycinThe serum concentration of Vancomycin can be increased when it is combined with Ketorolac.
VecuroniumThe risk or severity of adverse effects can be increased when Ketorolac is combined with Vecuronium.
VenlafaxineVenlafaxine may increase the antiplatelet activities of Ketorolac.
VerteporfinKetorolac may increase the photosensitizing activities of Verteporfin.
Vitamin EVitamin E may increase the antiplatelet activities of Ketorolac.
WarfarinKetorolac may increase the anticoagulant activities of Warfarin.
Food Interactions
  • Take with food to reduce GI irritation

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Constitutively expressed in some tissues in physiological conditions, such as the endothelium, kidney and brain, and in pathological conditions, such as in cancer. PTGS2 is responsible for production of inflammatory prostaglandins. Up-regulation of PTGS2 is also associated with increased cell adhesion, p...
Gene Name:
PTGS2
Uniprot ID:
P35354
Molecular Weight:
68995.625 Da
References
  1. Hocherl K, Kammerl MC, Schumacher K, Endemann D, Grobecker HF, Kurtz A: Role of prostanoids in regulation of the renin-angiotensin-aldosterone system by salt intake. Am J Physiol Renal Physiol. 2002 Aug;283(2):F294-301. [PubMed:12110513 ]
  2. Blais V, Zhang J, Rivest S: In altering the release of glucocorticoids, ketorolac exacerbates the effects of systemic immune stimuli on expression of proinflammatory genes in the brain. Endocrinology. 2002 Dec;143(12):4820-7. [PubMed:12446609 ]
  3. Ma W, Eisenach JC: Intraplantar injection of a cyclooxygenase inhibitor ketorolac reduces immunoreactivities of substance P, calcitonin gene-related peptide, and dynorphin in the dorsal horn of rats with nerve injury or inflammation. Neuroscience. 2003;121(3):681-90. [PubMed:14568028 ]
  4. Ma W, Eisenach JC: Cyclooxygenase 2 in infiltrating inflammatory cells in injured nerve is universally up-regulated following various types of peripheral nerve injury. Neuroscience. 2003;121(3):691-704. [PubMed:14568029 ]
  5. Padi SS, Jain NK, Singh S, Kulkarni SK: Pharmacological profile of parecoxib: a novel, potent injectable selective cyclooxygenase-2 inhibitor. Eur J Pharmacol. 2004 Apr 26;491(1):69-76. [PubMed:15102535 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. Bosch-Marce M, Claria J, Titos E, Masferrer JL, Altuna R, Poo JL, Jimenez W, Arroyo V, Rivera F, Rodes J: Selective inhibition of cyclooxygenase 2 spares renal function and prostaglandin synthesis in cirrhotic rats with ascites. Gastroenterology. 1999 May;116(5):1167-75. [PubMed:10220509 ]
  2. Lashbrook JM, Ossipov MH, Hunter JC, Raffa RB, Tallarida RJ, Porreca F: Synergistic antiallodynic effects of spinal morphine with ketorolac and selective COX1- and COX2-inhibitors in nerve-injured rats. Pain. 1999 Jul;82(1):65-72. [PubMed:10422661 ]
  3. Dionne RA, Khan AA, Gordon SM: Analgesia and COX-2 inhibition. Clin Exp Rheumatol. 2001 Nov-Dec;19(6 Suppl 25):S63-70. [PubMed:11695255 ]
  4. Uzan A: The unexpected side effects of new nonsteroidal anti-inflammatory drugs. Expert Opin Emerg Drugs. 2005 Nov;10(4):687-8. [PubMed:16262557 ]
  5. Blais V, Turrin NP, Rivest S: Cyclooxygenase 2 (COX-2) inhibition increases the inflammatory response in the brain during systemic immune stimuli. J Neurochem. 2005 Dec;95(6):1563-74. Epub 2005 Nov 8. [PubMed:16277613 ]
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Drug created on June 13, 2005 07:24 / Updated on May 24, 2016 03:10