Identification

Name
Ketorolac
Accession Number
DB00465
Description

Ketorolac is a Non-steroidal anti-inflammatory drug (NSAID) and is commercially available as an oral tablet, injectable, nasal spray and as an ophthalmic solution.910131415

It's analgesic properties make it a useful pain management tool across many settings including postoperative pain, rheumatoid arthritis, osteoarthritis, menstrual disorders, headaches, spinal and soft tissue pain, and ankylosing spondylitis.12 Impressively, ketorolac has a similar efficacy to standard doses of morphine and meperidine making it a useful opioid sparing agent.11

Type
Small Molecule
Groups
Approved
Structure
Thumb
Weight
Average: 255.2686
Monoisotopic: 255.089543287
Chemical Formula
C15H13NO3
Synonyms
  • Ketorolac
  • Kétorolac
  • Ketorolaco
  • Ketorolacum
  • rac-Ketorolac
External IDs
  • BPPC

Pharmacology

Indication

Ketorolac is a Non-steroidal anti-inflammatory drug (NSAID) and has antipyretic, analgesic and anti-inflammatory properties. 2 It is indicated for short term management of acute pain that requires the caliber of pain management offered by opioids. 14 Clinicians may choose to initiate ketorolac to manage post-operative pain, spinal and soft tissue pain, rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, menstrual disorders and headaches among other ailments. 12 Regardless of the etiology of pain, patients should use the lowest possible dose, and avoid using ketorolac for an extended period of time (ideally ≤ 5 days).14,14 A benefit of choosing ketorolac over other analgesics with similar potency is that that there does not appear to be a risk of dependence or tolerance with ketorolac use.2

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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Pharmacodynamics

Ketorolac is a non-selective NSAID and acts by inhibiting both COX-1 and COX-2 enzymes which are normally responsible for converting arachidonic acid to prostaglandins. The COX-1 enzyme is constitutively active and can be found in platelets, gastric mucosa, and vascular endothelium. On the other hand, the COX-2 enzyme is inducible and mediates inflammation, pain and fever.

As a result, inhibition of the COX-1 enzyme is linked to an increased risk of bleeding and risk of gastric ulceration, while the desired anti-inflammatory and analgesic properties are linked to inhibition of the COX-2 enzyme.3 Therefore, despite it's effectiveness in pain management, ketorolac should not be used long-term since this increases the risk of serious adverse effects such as gastrointestinal bleeding, peptic ulcers, and perforations.7

Mechanism of action

Ketorolac inhibits key pathways in prostaglandin synthesis which is crucial to it's mechanism of action.4 Although ketorolac is non-selective and inhibits both COX-1 and COX-2 enzymes, it's clinical efficacy is derived from it's COX-2 inhibition. The COX-2 enzyme is inducible and is responsible for converting arachidonic acid to prostaglandins that mediate inflammation and pain. By blocking this pathway, ketorolac achieves analgesia and reduces inflammation.3 Ketorolac is administered as a racemic mixture; however, the "S" enantiomer is largely responsible for it's pharmacological activity.6

TargetActionsOrganism
AProstaglandin G/H synthase 2
inhibitor
Humans
UProstaglandin G/H synthase 1
inhibitor
Humans
Absorption

Ketorolac is rapidly, and completely absorbed after oral administration with a bioavailability of 80% after oral administration.14,14,144 Cmax is attained 20-60 minutes after administration, and after intramuscular administration, the area under the plasma concentration-time curve (AUC) is proportional to the dose administered.1

After intramuscular administration, ketorolac demonstrates a time to maximal plasma concentration (tmax) of approximately 45-50 minutes, and a tmax of 30-40 minutes after oral administration.4 The rate of absorption may be reduced by food; however, the extent of absorption remains unaffected.4

Volume of distribution

The apparent volume of distribution of ketorolac in healthy human subjects is 0.25 L/kg or less.4

Protein binding

>99% of Ketorolac is plasma protein bound.1

Metabolism

Ketorolac is heavily metabolized via hydroxylation or conjugation in the liver; however, it appears that the key metabolic pathway is glucuronic acid conjugation.14,4 Enzymes involved in phase I metabolism include CYP2C8 and CYP2C9, while phase II metabolism is carried out by UDP-glucuronosyltransferase (UGT) 2B7.8

Hover over products below to view reaction partners

Route of elimination

Ketorolac is primarily renally eliminated and approximately 92% of the dose can be recovered in the urine with 60% of this proportion recovered unchanged, and 40% recovered as metabolites. In addition 6% of a single dose is eliminated in the feces.14

Half-life

Ketorolac tromethamine is administered as a racemic mixture, therefore the half-life of each enantiomer must be considered. The half life of the S-enantiomer is ~2.5 hours, while the half life of the R-enantiomer is ~5 hours. Based on this data, the S enantiomer is cleared about twice as fast as the R enantiomer.14

Clearance

The plasma clearance of ketorolac is 0.021 to 0.037 L/h/kg.4 Further, studies have illustrated that clearance of oral, IM and IV doses of ketorolac are comparable which suggests linear kinetics.14 It should also be noted that clearance in children is about double the clearance found in adults. 5

Adverse Effects
Learn about our commercial Adverse Effects data.
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Toxicity

The rate of adverse effects increases with higher doses of ketorolac. The most frequently observed adverse effects in patients occurring with an incidence of greater than 10% include: abdominal pain, dyspepsia, nausea, and headaches.13 Most adverse effects associated with short term use are mild in nature, related to the gastrointestinal tract and nervous system, and occur in roughly 39% of patients.2 Common symptoms of ketorolac overdose include nausea, vomiting, epigastric pain, gastrointestinal bleeding, lethargy and drowsiness. More rare symptoms of overdose include acute renal failure, hypertension, respiratory depression, and coma.14

Ketorolac is classified as Pregnancy Category C since there is a lack of evidence demonstrating safety in pregnant women.15 NSAIDs including ketorolac increase the risk of premature closure of the fetal ductus arteriosus in the 3rd trimester; therefore, beginning at 30 weeks gestation, pregnant women should avoid ketorolac.15

Ketorolac has been shown to be excreted in breast milk, and although available data has not demonstrated any adverse effects in nursing infants, practitioners should proceed with caution when suggesting ketorolac for nursing mothers.13,14 The benefits should outweigh the risks and the mother should be counselled to monitor the infant closely and to contact the infant's healthcare provider should any adverse effects arise.13,14

Women who are trying to conceive are not advised to take ketorolac since it's effect on prostaglandin synthesis may impair fertility.13,13

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Ketorolac Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbacavirKetorolac may decrease the excretion rate of Abacavir which could result in a higher serum level.
AbataceptThe metabolism of Ketorolac can be increased when combined with Abatacept.
AbciximabThe risk or severity of bleeding and hemorrhage can be increased when Ketorolac is combined with Abciximab.
AbirateroneThe metabolism of Ketorolac can be decreased when combined with Abiraterone.
AcarboseKetorolac may decrease the excretion rate of Acarbose which could result in a higher serum level.
AcebutololKetorolac may decrease the antihypertensive activities of Acebutolol.
AceclofenacThe risk or severity of adverse effects can be increased when Ketorolac is combined with Aceclofenac.
AcemetacinThe risk or severity of adverse effects can be increased when Ketorolac is combined with Acemetacin.
AcenocoumarolThe risk or severity of bleeding and hemorrhage can be increased when Ketorolac is combined with Acenocoumarol.
AcetaminophenThe risk or severity of adverse effects can be increased when Acetaminophen is combined with Ketorolac.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Take with food. Food reduces GI irritation.

Products

Product Ingredients
IngredientUNIICASInChI Key
Ketorolac tromethamine4EVE5946BQ74103-07-4BWHLPLXXIDYSNW-UHFFFAOYSA-N
Product Images
International/Other Brands
Bedoral (Be-Tabs Pharmaceuticals) / Dolten (Pfizer) / Dolten SL (Pfizer) / Dorixina forte NF (Roemmers) / Emodol (Jayson) / Etorac (Incepta) / Ketonic (Eskayef) / Ketora (Medicon) / Lixidol (Roche) / Syndol (Roche) / Taradyl (Roche) / Tarasyn (Roche)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AcularSolution / drops5 mg/1mLOphthalmicAllergan1992-12-01Not applicableUS flag
AcularSolution / drops5 mg/1mLOphthalmicStat Rx USA1992-12-01Not applicableUS flag
AcularSolution5 mg/1mLOphthalmicRebel Distributors1992-11-09Not applicableUS flag
AcularSolution / drops50 mg/1mLOphthalmicPhysicians Total Care, Inc.2002-10-172011-06-30US flag
Acular Liq 0.5%SolutionOphthalmicAllergan1992-12-31Not applicableCanada flag
Acular LsSolution0.4 %OphthalmicAllergan2004-03-08Not applicableCanada flag
Acular LsSolution / drops4 mg/1mLOphthalmicAllergan, Inc.2003-08-19Not applicableUS flag
Acular LsSolution40 mg/1mLOphthalmicPhysicians Total Care, Inc.2003-09-042011-06-30US flag
Acular PFSolution / drops5 mg/1mLOphthalmicAllergan1998-01-082011-06-10US flag
AcuvailSolution / drops4.5 mg/1mLOphthalmicAllergan, Inc.2009-08-01Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Acunivive 15Injection, solution15 mg/1mLIntramuscular; IntravenousIt3 Medical Llc2019-02-01Not applicableUS flag
Acunivive 30Injection, solution30 mg/1mLIntramuscular; IntravenousIt3 Medical Llc2017-03-01Not applicableUS flag
Acunivive 60Injection, solution30 mg/1mLIntramuscularIt3 Medical Llc2017-03-01Not applicableUS flag
Apo-ketorolacTabletOralApotex Corporation1998-07-03Not applicableCanada flag
Apo-ketorolac InjectableSolutionIntramuscularApotex Corporation2001-12-04Not applicableCanada flag
KetorolacTablet, film coated10 mg/1OralStat Rx USA2010-09-15Not applicableUS flag00378 1134 01 nlmimage10 dc3eee57
Ketorolac TromethamineInjection, solution30 mg/1mLIntramuscular; IntravenousFresenius Kabi USA, LLC2015-11-02Not applicableUS flag
Ketorolac TromethamineInjection, solution60 mg/2mLIntramuscularRemedy Repack2018-02-072018-03-08US flag
Ketorolac TromethamineSolution5 mg/1mLOphthalmicNucare Pharmaceuticals,inc.2009-11-05Not applicableUS flag
Ketorolac TromethamineInjection15 mg/1mLIntramuscular; IntravenousWockhardt USA LLC.2007-03-27Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Toradol Tab 10mgTabletOralSyntex Inc.1991-12-311996-09-30Canada flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Acunistat-30Ketorolac tromethamine (30 mg/1mL) + Isopropyl alcohol (0.7 mL/1mL) + Lidocaine hydrochloride (10 mg/1mL)Infiltration; Intramuscular; Intravenous; Perineural; TopicalIt3 Medical Llc2017-03-01Not applicableUS flag
Acunistat-60Ketorolac tromethamine (30 mg/1mL) + Isopropyl alcohol (0.7 mL/1mL) + Lidocaine hydrochloride (10 mg/1mL)Infiltration; Intramuscular; Perineural; TopicalIt3 Medical Llc2017-03-01Not applicableUS flag
Acunivive 90Ketorolac tromethamine (30 mg/1mL) + Ketorolac tromethamine (30 mg/1mL) + Isopropyl alcohol (0.7 mL/1mL)Intramuscular; Intravenous; TopicalIt3 Medical Llc2017-03-01Not applicableUS flag
Acunivive 90Ketorolac tromethamine (30 mg/1mL) + Ketorolac tromethamine (30 mg/1mL) + Isopropyl alcohol (0.7 mL/1mL)Intramuscular; Intravenous; TopicalIt3 Medical Llc2017-03-01Not applicableUS flag
OmidriaKetorolac (2.88 mg/1mL) + Phenylephrine (10.16 mg/1mL)Injection, solution, concentrateIntraocularOmeros Corporation2014-06-13Not applicableUS flag
ReadySharp Anesthetics plus KetorolacKetorolac tromethamine (15 mg/1mL) + Bupivacaine hydrochloride (5 mg/1mL) + Lidocaine hydrochloride (10 mg/1mL)KitIntramuscular; IntravenousTerrain Pharmaceuticals2015-12-29Not applicableUS flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Chi-Myst Resolve TopicalKetorolac tromethamine (0.3 g/100mL) + Bupivacaine hydrochloride (0.3 g/100mL) + Chitosan low molecular weight (20-200 mpa.s) (0.1 g/100mL) + Lidocaine hydrochloride (5 g/100mL)Spray, meteredTopicalPrescription Care Llc2016-06-01Not applicableUS flag
Chi-Myst Resolve TopicalKetorolac tromethamine (0.09 g/30mL) + Bupivacaine hydrochloride (0.09 g/30mL) + Chitosan low molecular weight (20-200 mpa.s) (0.03 g/30mL) + Lidocaine hydrochloride (50 g/30mL)Spray, meteredTopicalPrescription Care Llc2016-06-01Not applicableUS flag
Chi-Myst Synergy TopicalKetorolac tromethamine (0.45 g/30mL) + Bupivacaine hydrochloride (0.09 g/30mL) + Chitosan low molecular weight (20-200 mpa.s) (0.03 g/30mL) + Lidocaine hydrochloride (1.5 g/30mL)Spray, meteredTopicalPrescription Care Llc2016-06-01Not applicableUS flag
Chi-Myst Synergy TopicalKetorolac tromethamine (1.5 g/100mL) + Bupivacaine hydrochloride (0.3 g/100mL) + Chitosan low molecular weight (20-200 mpa.s) (0.1 g/100mL) + Lidocaine hydrochloride (5 g/100mL)Spray, meteredTopicalPrescription Care Llc2016-06-01Not applicableUS flag
Chi-Myst TopicalKetorolac tromethamine (0.3 g/100mL) + Bupivacaine hydrochloride (0.3 g/100mL) + Chitosan low molecular weight (20-200 mpa.s) (0.1 g/100mL)Spray, meteredTopicalPrescription Care Llc2016-08-19Not applicableUS flag
Chi-Myst TopicalKetorolac tromethamine (0.09 g/30mL) + Bupivacaine hydrochloride (0.09 g/30mL) + Chitosan low molecular weight (20-200 mpa.s) (0.03 g/30mL)Spray, meteredTopicalPrescription Care Llc2016-08-19Not applicableUS flag
Dex-Moxi-KetorKetorolac tromethamine (0.4 mg/1mL) + Dexamethasone sodium phosphate (1 mg/1mL) + Moxifloxacin hydrochloride monohydrate (0.5 mg/1mL)Injection, solutionOphthalmicImprimis Njof, Llc2018-01-05Not applicableUS flag
DexMoxiKetor PFKetorolac tromethamine (0.4 mg/1mL) + Dexamethasone sodium phosphate (1 mg/1mL) + Moxifloxacin hydrochloride monohydrate (0.5 mg/1mL)Injection, solutionIntraocularImprimisRx NJ2018-01-01Not applicableUS flag
Ketorocaine L KitKetorolac tromethamine (30 mg/1mL) + Isopropyl alcohol (70 mL/100mL) + Lidocaine hydrochloride (10 mg/1mL) + Povidone-iodine (10 mg/1mL)KitInfiltration; Intramuscular; Intravenous; TopicalAsclemed Usa, Inc.2014-08-15Not applicableUS flag
Ketorocaine LM KitKetorolac tromethamine (30 mg/1mL) + Bupivacaine hydrochloride (2.5 mg/1mL) + Isopropyl alcohol (70 mL/100mL) + Lidocaine hydrochloride (10 mg/1mL) + Povidone-iodine (10 mg/1mL)KitEpidural; Infiltration; Intramuscular; Intravenous; TopicalAsclemed Usa, Inc.2014-08-11Not applicableUS flag

Categories

ATC Codes
M01AB15 — KetorolacS01FB51 — Phenylephrine and ketorolacS01BC05 — Ketorolac
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as aryl-phenylketones. These are aromatic compounds containing a ketone substituted by one aryl group, and a phenyl group.
Kingdom
Organic compounds
Super Class
Organic oxygen compounds
Class
Organooxygen compounds
Sub Class
Carbonyl compounds
Direct Parent
Aryl-phenylketones
Alternative Parents
Pyrrolizines / Benzoyl derivatives / Substituted pyrroles / Heteroaromatic compounds / Monocarboxylic acids and derivatives / Carboxylic acids / Azacyclic compounds / Organopnictogen compounds / Organonitrogen compounds / Organic oxides
show 1 more
Substituents
Aromatic heteropolycyclic compound / Aryl-phenylketone / Azacycle / Benzenoid / Benzoyl / Carboxylic acid / Carboxylic acid derivative / Heteroaromatic compound / Hydrocarbon derivative / Monocarboxylic acid or derivatives
show 9 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
monocarboxylic acid, aromatic ketone, amino acid, pyrrolizines (CHEBI:76223)

Chemical Identifiers

UNII
YZI5105V0L
CAS number
74103-06-3
InChI Key
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

References

Synthesis Reference

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

US6323344
General References
  1. Brocks DR, Jamali F: Clinical pharmacokinetics of ketorolac tromethamine. Clin Pharmacokinet. 1992 Dec;23(6):415-27. doi: 10.2165/00003088-199223060-00003. [PubMed:1458761]
  2. Litvak KM, McEvoy GK: Ketorolac, an injectable nonnarcotic analgesic. Clin Pharm. 1990 Dec;9(12):921-35. [PubMed:2292174]
  3. Macario A, Lipman AG: Ketorolac in the era of cyclo-oxygenase-2 selective nonsteroidal anti-inflammatory drugs: a systematic review of efficacy, side effects, and regulatory issues. Pain Med. 2001 Dec;2(4):336-51. doi: 10.1046/j.1526-4637.2001.01043.x. [PubMed:15102238]
  4. Buckley MM, Brogden RN: Ketorolac. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential. Drugs. 1990 Jan;39(1):86-109. doi: 10.2165/00003495-199039010-00008. [PubMed:2178916]
  5. Kauffman RE, Lieh-Lai MW, Uy HG, Aravind MK: Enantiomer-selective pharmacokinetics and metabolism of ketorolac in children. Clin Pharmacol Ther. 1999 Apr;65(4):382-8. doi: 10.1016/S0009-9236(99)70131-1. [PubMed:10223774]
  6. Hayball PJ, Wrobel J, Tamblyn JG, Nation RL: The pharmacokinetics of ketorolac enantiomers following intramuscular administration of the racemate. Br J Clin Pharmacol. 1994 Jan;37(1):75-8. [PubMed:8148223]
  7. Yarboro TL Sr: Intramuscular Toradol, gastrointestinal bleeding, and peptic ulcer perforation: a case report. J Natl Med Assoc. 1995 Mar;87(3):225-7. [PubMed:7731074]
  8. Valitalo PA, Kemppainen H, Kulo A, Smits A, van Calsteren K, Olkkola KT, de Hoon J, Knibbe CAJ, Allegaert K: Body weight, gender and pregnancy affect enantiomer-specific ketorolac pharmacokinetics. Br J Clin Pharmacol. 2017 Sep;83(9):1966-1975. doi: 10.1111/bcp.13311. Epub 2017 May 14. [PubMed:28429492]
  9. Acular FDA Label [Link]
  10. Ketorolac Tromethamine IV/IM [Link]
  11. Ketorolac: A Reappraisal of its Pharmacodynamic and Pharmacokinetic Properties and Therapeutic Use In Pain Management [Link]
  12. Ketorolac for Pain Management: A Review of the Clinical Evidence) [Link]
  13. FDA Approved Drug Products: Ketorolac tromethamine oral tablets [Link]
  14. FDA Approved Drug Products: Toradol (ketorolac tromethamine) oral tablets [Link]
  15. FDA Approved Drug Products: Sprix (ketorolac tromethamine) nasal spray [Link]
Human Metabolome Database
HMDB0014608
KEGG Compound
C07062
PubChem Compound
3826
PubChem Substance
46507019
ChemSpider
3694
BindingDB
85511
RxNav
35827
ChEBI
76223
ChEMBL
CHEMBL469
Therapeutic Targets Database
DAP000618
PharmGKB
PA450150
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Ketorolac
AHFS Codes
  • 52:08.20 — Nonsteroidal Anti-inflammatory Agents
  • 28:08.04.92 — Other Nonsteroidal Antiimflammatory Agents
MSDS
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Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingSupportive CareHematoma Postoperative1
4CompletedNot AvailableCataract Surgery1
4CompletedNot AvailableCataracts2
4CompletedNot AvailableMacula Thickening1
4CompletedNot AvailableVitrectomy therapy1
4CompletedBasic ScienceInflammatory Reaction1
4CompletedBasic ScienceSecondary Hyperalgesia1
4CompletedOtherHematological Malignancy (Leukemia- Lymphoma)1
4CompletedPreventionCataracts / Inflammatory Reaction1
4CompletedPreventionCesarean Section1

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
  • Akorn Inc.
  • Allergan Inc.
  • Amerisource Health Services Corp.
  • Apotex Inc.
  • Apotheca Inc.
  • Apothecary Shop Wholesale
  • APP Pharmaceuticals
  • A-S Medication Solutions LLC
  • Baxter International Inc.
  • Bedford Labs
  • Ben Venue Laboratories Inc.
  • Bryant Ranch Prepack
  • Cardinal Health
  • Corepharma LLC
  • Cura Pharmaceutical Co. Inc.
  • Direct Dispensing Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Ethex Corp.
  • F Hoffmann-La Roche Ltd.
  • Falcon Pharmaceuticals Ltd.
  • General Injectables and Vaccines Inc.
  • H.J. Harkins Co. Inc.
  • Hospira Inc.
  • Innoviant Pharmacy Inc.
  • Kaiser Foundation Hospital
  • Keltman Pharmaceuticals Inc.
  • Lake Erie Medical and Surgical Supply
  • Mckesson Corp.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Neuman Distributors Inc.
  • Novex Pharma
  • Nucare Pharmaceuticals Inc.
  • Palmetto Pharmaceuticals Inc.
  • PD-Rx Pharmaceuticals Inc.
  • Physicians Total Care Inc.
  • Pliva Inc.
  • Preferred Pharmaceuticals Inc.
  • Prescript Pharmaceuticals
  • Rebel Distributors Corp.
  • Redpharm Drug
  • Resource Optimization and Innovation LLC
  • Southwood Pharmaceuticals
  • Spectrum Pharmaceuticals
  • St Mary's Medical Park Pharmacy
  • Stat Rx Usa
  • Strides Arcolab Limited
  • Sun Pharmaceutical Industries Ltd.
  • Syntex SA
  • Taylor Pharmaceuticals
  • Teva Pharmaceutical Industries Ltd.
  • Wockhardt Ltd.
Dosage Forms
FormRouteStrength
Solution / dropsOphthalmic0.4 %
SolutionOphthalmic5 mg/1mL
Solution / dropsOphthalmic50 mg/1mL
SolutionOphthalmic
SolutionOphthalmic0.4 %
SolutionOphthalmic40 mg/1mL
Solution / dropsOphthalmic5 mg/1mL
SolutionConjunctival; Ophthalmic4 mg
Solution / dropsOphthalmic
SolutionOphthalmic0.45 %
SolutionConjunctival; Ophthalmic4.5 mg
Injection30 mg/ml
Spray, meteredTopical
Injection, solutionOphthalmic
Injection, solutionIntraocular
Injection, solutionParenteral30 MG/ML
Solution / dropsOral20 MG/ML
SolutionConjunctival; Ophthalmic5 mg
SolutionIntracavernous; Intramuscular30 mg
Tablet
Injection, solution30 mg/1mL
KitInfiltration; Intramuscular; Intravenous; Topical
KitEpidural; Infiltration; Intramuscular; Intravenous; Topical
SolutionOphthalmic0.5 %
Solution / dropsOphthalmic5 mg/ml
InjectionIntramuscular30 mg/1mL
InjectionIntramuscular60 mg/2mL
InjectionIntramuscular; Intravenous15 mg/1mL
InjectionIntramuscular; Intravenous30 mg/1mL
InjectionIntramuscular; Intravenous60 mg/1mL
Injection, solutionIntramuscular15 mg/1mL
Injection, solutionIntramuscular30 mg/1mL
Injection, solutionIntramuscular60 mg/2mL
Injection, solutionIntramuscular; Intravenous15 mg/2mL
Injection, solutionIntramuscular; Intravenous15 mg/1mL
Injection, solutionIntramuscular; Intravenous30 mg/1mL
Injection, solutionIntramuscular; Intravenous60 mg/2mL
Injection, solutionIntravenous30 mg/1mL
PowderNot applicable1 g/1g
SolutionOphthalmic0.5 mg/1mL
SolutionOphthalmic4 mg/1mL
SolutionOphthalmic5 mg/1
Solution / dropsOphthalmic4 mg/1mL
Solution / dropsOphthalmic4.5 mg/1mL
TabletOral10 mg/1
Tablet, film coatedOral10 mg/1
LiquidIntramuscular
InjectionIntramuscular; Intravenous30 mg
TabletOral10 mg
Injection, solutionIntramuscular10 mg/mL
Injection, solutionIntramuscular10 mg
Injection, solutionIntramuscular30 mg/mL
Injection, solutionIntramuscular30 mg
SuppositoryRectal30 mg
Tablet, film coatedOral10 mg
Solution / dropsOphthalmic0.5 %
InjectionIntramuscular; Intravenous30 mg/ml
Solution / dropsOphthalmic
TabletSublingual30 mg
Injection, solution, concentrateIntraocular
Solution, concentrateOphthalmic10.2 MG/ML
SolutionOphthalmic; Topical5 mg
KitIntramuscular; Intravenous
Tablet, coatedOral10 mg
Tablet, film coated10 mg
Spray, meteredNasal15.75 mg/1
Injection, solutionParenteral10 MG/ML
Suppository30 MG
Tablet, coated10 MG
SolutionIntramuscular
TabletOral
SolutionIntramuscular; Intravenous15 mg
SolutionIntramuscular; Intravenous30 mg
Tablet, film coatedOral
Injection
Injection, solution30 mg/mL
Solution
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)Region
US5110493No1992-05-052009-11-05US flag
CA1328614No1994-04-192011-04-19Canada flag
US9216127No2015-12-222024-05-28US flag
US8008338Yes2011-08-302027-11-24US flag
US8207215Yes2012-06-262024-11-28US flag
US8377982Yes2013-02-192024-11-28US flag
US8541463Yes2013-09-242024-11-28US flag
US8906950No2014-12-092024-05-28US flag
US9216167No2015-12-222024-05-28US flag
US8946281No2015-02-032024-05-28US flag
US8648107No2014-02-112024-05-28US flag
US6333044No2001-12-252018-12-25US flag
US7842714No2010-11-302029-08-15US flag
US9192571No2015-11-242028-03-07US flag
US8512717No2013-08-202028-03-07US flag
US8992952No2015-03-312024-08-05US flag
US8173707Yes2012-05-082024-01-30US flag
US9278101Yes2016-03-082024-01-30US flag
US8586633Yes2013-11-192024-01-30US flag
US9066856Yes2015-06-302034-04-23US flag
US9399040Yes2016-07-262024-01-30US flag
US9486406Yes2016-11-082034-04-23US flag
US9855246No2018-01-022033-10-23US flag
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)162-165 °C (tromethamine salt)Ketorolac tromethamine MSDS
water solubility200 g/l (tromethamine salt)Ketorolac thromethamine MSDS
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 RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0a4i-0190000000-cc495a56f46ce2f38f4c
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0a4i-0900000000-49260d5fd66684718972
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0a4i-3900000000-cf3a2eedecd98f879db6
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-056r-9500000000-a993ea029f81823db36e
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-004i-9200000000-238f6cde2fac6b0ba421
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4i-1590000000-070501bbf446e4fc9fea

Targets

Kind
Protein
Organism
Humans
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...
Gene Name
PTGS2
Uniprot ID
P35354
Uniprot Name
Prostaglandin G/H synthase 2
Molecular Weight
68995.625 Da
References
  1. 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]
  2. 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]
  3. 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]
  4. 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]
Kind
Protein
Organism
Humans
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 gas...
Gene Name
PTGS1
Uniprot ID
P23219
Uniprot Name
Prostaglandin G/H synthase 1
Molecular Weight
68685.82 Da
References
  1. 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]
  2. Uzan A: The unexpected side effects of new nonsteroidal anti-inflammatory drugs. Expert Opin Emerg Drugs. 2005 Nov;10(4):687-8. [PubMed:16262557]
  3. 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]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Glucuronosyltransferase activity
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.Its unique specificity for 3,4-catechol estrogens and estriol su...
Gene Name
UGT2B7
Uniprot ID
P16662
Uniprot Name
UDP-glucuronosyltransferase 2B7
Molecular Weight
60694.12 Da
References
  1. Kulo A, Smits A, Maleskic S, Van de Velde M, Van Calsteren K, De Hoon J, Verbesselt R, Deprest J, Allegaert K: Enantiomer-specific ketorolac pharmacokinetics in young women, including pregnancy and postpartum period. Bosn J Basic Med Sci. 2017 Feb 21;17(1):54-60. doi: 10.17305/bjbms.2016.1515. [PubMed:27968707]
  2. Valitalo PA, Kemppainen H, Kulo A, Smits A, van Calsteren K, Olkkola KT, de Hoon J, Knibbe CAJ, Allegaert K: Body weight, gender and pregnancy affect enantiomer-specific ketorolac pharmacokinetics. Br J Clin Pharmacol. 2017 Sep;83(9):1966-1975. doi: 10.1111/bcp.13311. Epub 2017 May 14. [PubMed:28429492]
Kind
Protein
Organism
Humans
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 un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Valitalo PA, Kemppainen H, Kulo A, Smits A, van Calsteren K, Olkkola KT, de Hoon J, Knibbe CAJ, Allegaert K: Body weight, gender and pregnancy affect enantiomer-specific ketorolac pharmacokinetics. Br J Clin Pharmacol. 2017 Sep;83(9):1966-1975. doi: 10.1111/bcp.13311. Epub 2017 May 14. [PubMed:28429492]
Kind
Protein
Organism
Humans
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 un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Valitalo PA, Kemppainen H, Kulo A, Smits A, van Calsteren K, Olkkola KT, de Hoon J, Knibbe CAJ, Allegaert K: Body weight, gender and pregnancy affect enantiomer-specific ketorolac pharmacokinetics. Br J Clin Pharmacol. 2017 Sep;83(9):1966-1975. doi: 10.1111/bcp.13311. Epub 2017 May 14. [PubMed:28429492]

Drug created on June 13, 2005 07:24 / Updated on October 29, 2020 19:26

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