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ketorolac 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
anti-inflammatory agents, ibufenac derivatives	1529	74103-06-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: ketorolac ketorolac tromethamine ketorolac trometamol trometamol ketorolac (+/-)-Ketorolac keromin	A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is a non-steroidal anti-inflammatory agent used for analgesia for postoperative pain and inhibits cyclooxygenase activity. Molecular weight: 255.27 Formula: C15H13NO3 CLOGP: 1.62 LIPINSKI: 0 HAC: 4 HDO: 1 TPSA: 59.30 ALOGS: -2.70 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

ketorolac
ketorolac tromethamine
ketorolac trometamol
trometamol ketorolac
(+/-)-Ketorolac
keromin

A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is a non-steroidal anti-inflammatory agent used for analgesia for postoperative pain and inhibits cyclooxygenase activity.

Molecular weight: 255.27
Formula: C15H13NO3
CLOGP: 1.62
LIPINSKI: 0
HAC: 4
HDO: 1
TPSA: 59.30
ALOGS: -2.70
ROTB: 3

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
30	mg	O
30	mg	P

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	99 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	9.79 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	58 %	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	5.10 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	200 mg/mL	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	0.35 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.11 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.01 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Nov. 30, 1989	FDA

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug hypersensitivity	450.07	12.60	479	16408	310208	63161927
Punctate keratitis	85.80	12.60	22	16865	599	63471536
Ulcerative keratitis	78.89	12.60	29	16858	2681	63469454
Corneal epithelium defect	76.76	12.60	18	16869	334	63471801
Skin papilloma	74.53	12.60	33	16854	4936	63467199
Spinal epidural haematoma	72.82	12.60	22	16865	1105	63471030
Tendon disorder	63.37	12.60	31	16856	5812	63466323
Concussion	55.18	12.60	33	16854	9211	63462924
Renal infarct	51.61	12.60	18	16869	1429	63470706
Torsade de pointes	50.97	12.60	36	16851	13315	63458820

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Sedation	162.25	16.86	84	7841	20922	34928084
Nightmare	157.45	16.86	73	7852	14318	34934688
Respiratory depression	137.15	16.86	69	7856	16176	34932830
Nephrolithiasis	130.97	16.86	83	7842	30250	34918756
Victim of child abuse	129.09	16.86	32	7893	895	34948111
Drug dependence	126.89	16.86	75	7850	24142	34924864
Epidural lipomatosis	105.67	16.86	28	7897	1026	34947980
Product used for unknown indication	98.01	16.86	26	7899	957	34948049
Product prescribing error	97.10	16.86	62	7863	22865	34926141
Juvenile idiopathic arthritis	89.41	16.86	28	7897	1869	34947137

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug hypersensitivity	346.11	12.67	407	20397	298509	79425075
Respiratory depression	134.56	12.67	86	20718	27544	79696040
Victim of child abuse	123.72	12.67	32	20772	921	79722663
Nightmare	122.24	12.67	79	20725	25782	79697802
Nephrolithiasis	105.50	12.67	97	20707	53194	79670390
Punctate keratitis	98.92	12.67	27	20777	959	79722625
Epidural lipomatosis	97.51	12.67	28	20776	1200	79722384
Drug dependence	88.16	12.67	78	20726	40691	79682893
Sedation	82.98	12.67	84	20720	51811	79671773
Anaphylactic reaction	81.85	12.67	105	20699	83638	79639946

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	M01AB15	MUSCULO-SKELETAL SYSTEM ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS Acetic acid derivatives and related substances
ATC	S01BC05	SENSORY ORGANS OPHTHALMOLOGICALS ANTIINFLAMMATORY AGENTS Antiinflammatory agents, non-steroids
ATC	S01FB51	SENSORY ORGANS OPHTHALMOLOGICALS MYDRIATICS AND CYCLOPLEGICS Sympathomimetics excl. antiglaucoma preparations
CHEBI has role	CHEBI:35475	non-steroidal anti-inflammatory agent
CHEBI has role	CHEBI:50629	COX-2 inhibitor
CHEBI has role	CHEBI:50630	COX-1 inhibitor
FDA CS	M0001335	Anti-Inflammatory Agents, Non-Steroidal
FDA EPC	N0000175722	Nonsteroidal Anti-inflammatory Drug
FDA EPC	N0000175939	Cyclooxygenase Inhibitor
FDA MoA	N0000000160	Cyclooxygenase Inhibitors

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Severe pain	indication	76948002
Allergic conjunctivitis	indication	473460002	DOID:11204
Acute postoperative pain	indication	107401000119105
Postoperative Ocular Pain	indication
Post-Op Ocular Inflammation	indication
Post-Op Photophobia	indication
Renal colic	off-label use	7093002
Peptic ulcer	contraindication	13200003	DOID:750
Disorder of cornea	contraindication	15250008	DOID:10124
Acute gastric ulcer with perforation	contraindication	19850005

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.47	acidic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
0.4%	ACULAR LS	ABBVIE	N021528	May 30, 2003	RX	SOLUTION/DROPS	OPHTHALMIC	8207215	May 28, 2024	A METHOD OF CONTROLLING POSTOPERATIVE OCULAR PAIN AND BURNING/STINGING IN A PATIENT
0.4%	ACULAR LS	ABBVIE	N021528	May 30, 2003	RX	SOLUTION/DROPS	OPHTHALMIC	8377982	May 28, 2024	A METHOD OF TREATING OR PREVENTING OCULAR PAIN AND BURNING/STINGING FOLLOWING CORNEAL SURGERY
0.4%	ACULAR LS	ABBVIE	N021528	May 30, 2003	RX	SOLUTION/DROPS	OPHTHALMIC	8541463	May 28, 2024	A METHOD OF TREATING OR REDUCING OCULAR PAIN AND BURNING/STINGING
0.4%	ACULAR LS	ABBVIE	N021528	May 30, 2003	RX	SOLUTION/DROPS	OPHTHALMIC	8906950	May 28, 2024	A METHOD OF TREATING OR PREVENTING OCULAR PAIN AND BURNING
0.4%	ACULAR LS	ABBVIE	N021528	May 30, 2003	RX	SOLUTION/DROPS	OPHTHALMIC	8946281	May 28, 2024	A METHOD OF TREATING OCULAR PAIN
0.4%	ACULAR LS	ABBVIE	N021528	May 30, 2003	RX	SOLUTION/DROPS	OPHTHALMIC	9216167	May 28, 2024	A METHOD OF TREATING OCULAR PAIN AND/OR ENHANCING OCULAR COMFORT
0.4%	ACULAR LS	ABBVIE	N021528	May 30, 2003	RX	SOLUTION/DROPS	OPHTHALMIC	8008338	May 24, 2027	A METHOD OF TREATING OR PREVENTING OCULAR PAIN IN A PATIENT
EQ 0.3% BASE;EQ 1% BASE	OMIDRIA	RAYNER SURGICAL	N205388	May 30, 2014	RX	SOLUTION	IRRIGATION	8173707	July 30, 2023	MAINTAINING PUPIL SIZE BY PREVENTING INTRAOPERATIVE MIOSIS AND REDUCING POSTOPERATIVE OCULAR PAIN
EQ 0.3% BASE;EQ 1% BASE	OMIDRIA	RAYNER SURGICAL	N205388	May 30, 2014	RX	SOLUTION	IRRIGATION	9278101	July 30, 2023	MAINTAINING PUPIL SIZE BY PREVENTING INTRAOPERATIVE MIOSIS AND REDUCING POSTOPERATIVE OCULAR PAIN

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Prostaglandin G/H synthase 2	Enzyme	P35354	PGH2_HUMAN	INHIBITOR	IC50	6.90	WOMBAT-PK	CHEMBL
Prostaglandin G/H synthase 1	Enzyme	P23219	PGH1_HUMAN	INHIBITOR	IC50	9.72	WOMBAT-PK	CHEMBL
Serine/threonine-protein kinase PAK 1	Kinase	Q13153	PAK1_HUMAN		IC50	4.44	CHEMBL
Fatty acid-binding protein, liver	Unclassified		FABPL_RAT		Ki	4.94	CHEMBL
Aldose reductase	Enzyme		ALDR_RAT		IC50	5.21	DRUG MATRIX
Prostaglandin-H2 D-isomerase	Enzyme		PTGDS_MOUSE		IC50	6.64	CHEMBL

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External reference:

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ID	Source
KTR	PDB_CHEM_ID
003539	NDDF
004812	NDDF
108512006	SNOMEDCT_US
108513001	SNOMEDCT_US
28200	RXNORM
30341	MMSL
372501008	SNOMEDCT_US
3826	PUBCHEM_CID
39892	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Acular	HUMAN PRESCRIPTION DRUG LABEL	1	0023-2181	SOLUTION/ DROPS	5 mg	OPHTHALMIC	NDA	23 sections
Acular	HUMAN PRESCRIPTION DRUG LABEL	1	0023-2181	SOLUTION/ DROPS	5 mg	OPHTHALMIC	NDA	23 sections
ACULAR LS	HUMAN PRESCRIPTION DRUG LABEL	1	0023-9277	SOLUTION/ DROPS	4 mg	OPHTHALMIC	NDA	22 sections
ACULAR LS	HUMAN PRESCRIPTION DRUG LABEL	1	0023-9277	SOLUTION/ DROPS	4 mg	OPHTHALMIC	NDA	22 sections
ACUVAIL	HUMAN PRESCRIPTION DRUG LABEL	1	0023-3507	SOLUTION/ DROPS	4.50 mg	OPHTHALMIC	NDA	23 sections
ACUVAIL	HUMAN PRESCRIPTION DRUG LABEL	1	0023-3507	SOLUTION/ DROPS	4.50 mg	OPHTHALMIC	NDA	23 sections
ACUVAIL	HUMAN PRESCRIPTION DRUG LABEL	1	0023-3507	SOLUTION/ DROPS	4.50 mg	OPHTHALMIC	NDA	23 sections
Ketorolac Tromethamine	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0314	TABLET, FILM COATED	10 mg	ORAL	ANDA	27 sections
Ketorolac Tromethamine	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0314	TABLET, FILM COATED	10 mg	ORAL	ANDA	27 sections
Ketorolac Tromethamine	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0314	TABLET, FILM COATED	10 mg	ORAL	ANDA	27 sections

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