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Details

Stereochemistry RACEMIC
Molecular Formula C15H13NO3.C4H11NO3
Molecular Weight 376.4037
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of KETOROLAC TROMETHAMINE

SMILES

NC(CO)(CO)CO.OC(=O)C1CCN2C1=CC=C2C(=O)C3=CC=CC=C3

InChI

InChIKey=BWHLPLXXIDYSNW-UHFFFAOYSA-N
InChI=1S/C15H13NO3.C4H11NO3/c17-14(10-4-2-1-3-5-10)13-7-6-12-11(15(18)19)8-9-16(12)13;5-4(1-6,2-7)3-8/h1-7,11H,8-9H2,(H,18,19);6-8H,1-3,5H2

HIDE SMILES / InChI
Molecular Formula C4H11NO3
Molecular Weight 121.135
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
Molecular Formula C15H13NO3
Molecular Weight 255.2686
Charge 0
Count
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Description

Ketorolac is a pyrrolizine carboxylic acid derivative structurally related to indomethacin. It is an NSAID and is used principally for its analgesic activity and has been shown to decrease opioid requirements in post-operative patients. It does not affect consciousness or respiration but does have effects on gastric mucosa, renal perfusion, and platelet function. Ketorolac tromethamine ophthalmic solution is sold under brand name acular LS and is indicated for the reduction of ocular pain and burning/stinging following corneal refractive surgery. 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 medication. Analgesia is probably produced via a peripheral action in which blockade of pain impulse generation results from decreased prostaglandin activity.

CNS Activity

Originator

Approval Year

1989
115
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
ACULAR LS

Approved Use

ACULAR LS ophthalmic solution is indicated for the reduction of ocular pain and burning/stinging following corneal refractive surgery.

Launch Date

2003
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2382.2 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/022382s000lbl.pdf
30 mg single, intramuscular
dose: 30 mg
route of administration: Intramuscular
experiment type: SINGLE
co-administered:
KETOROLAC plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
1805.8 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/022382s000lbl.pdf
31.5 mg single, nasal
dose: 31.5 mg
route of administration: Nasal
experiment type: SINGLE
co-administered:
KETOROLAC plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
11152.8 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/022382s000lbl.pdf
30 mg single, intramuscular
dose: 30 mg
route of administration: Intramuscular
experiment type: SINGLE
co-administered:
KETOROLAC plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
7477.3 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/022382s000lbl.pdf
31.5 mg single, nasal
dose: 31.5 mg
route of administration: Nasal
experiment type: SINGLE
co-administered:
KETOROLAC plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
4.8 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/022382s000lbl.pdf
30 mg single, intramuscular
dose: 30 mg
route of administration: Intramuscular
experiment type: SINGLE
co-administered:
KETOROLAC plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
5.24 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/022382s000lbl.pdf
31.5 mg single, nasal
dose: 31.5 mg
route of administration: Nasal
experiment type: SINGLE
co-administered:
KETOROLAC plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
2 mg single, intrathecal
Highest studied dose
Dose: 2 mg
Route: intrathecal
Route: single
Dose: 2 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/12406536/
healthy, 18-50
n = 5
Health Status: healthy
Age Group: 18-50
Sex: M+F
Population Size: 5
Sources:
https://pubmed.ncbi.nlm.nih.gov/12406536/
Sources:
https://pubmed.ncbi.nlm.nih.gov/12406536/
30 mg single, intramuscular
Highest studied dose
Dose: 30 mg
Route: intramuscular
Route: single
Dose: 30 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/17192497/
healthy, 19-45
n = 15
Health Status: healthy
Age Group: 19-45
Sex: M+F
Population Size: 15
Sources:
https://pubmed.ncbi.nlm.nih.gov/17192497/
Sources:
https://pubmed.ncbi.nlm.nih.gov/17192497/
30 mg single, intranasal
Highest studied dose
Dose: 30 mg
Route: intranasal
Route: single
Dose: 30 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/17192497/
healthy, 19-45
n = 15
Health Status: healthy
Age Group: 19-45
Sex: M+F
Population Size: 15
Sources:
https://pubmed.ncbi.nlm.nih.gov/17192497/
Sources:
https://pubmed.ncbi.nlm.nih.gov/17192497/
31.5 mg 3 times / day multiple, intranasal
Recommended
Dose: 31.5 mg, 3 times / day
Route: intranasal
Route: multiple
Dose: 31.5 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
unhealthy, 51.7
n = 199
Health Status: unhealthy
Condition: pain
Age Group: 51.7
Sex: M+F
Population Size: 199
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
Other AEs: Nausea, Constipation...
Other AEs:
Nausea (58%)
Constipation (29%)
Vomiting (28%)
Nasal passage irritation (24%)
Headache (24%)
Flatulence (23%)
Anemia (19%)
Tachycardia (14%)
Pruritis (11%)
Dizziness (6%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
90 mg single, intravenous
Dose: 90 mg
Route: intravenous
Route: single
Dose: 90 mg
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765128
unhealthy
n = 8
Health Status: unhealthy
Condition: Percutaneous Nephrolithotomy operation
Population Size: 8
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765128
Other AEs: Anaemia, Thrombocytopenia...
Other AEs:
Anaemia (below serious, 7 patients)
Thrombocytopenia (below serious, 3 patients)
Hyponatraemia (below serious, 3 patients)
Hypokalaemia (below serious, 2 patients)
Leucopenia (below serious, 1 patient)
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765128
90 mg single, intravenous
Dose: 90 mg
Route: intravenous
Route: single
Dose: 90 mg
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765232
unhealthy
n = 57
Health Status: unhealthy
Condition: Laparoscopic Donor Nephrectomy
Population Size: 57
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765232
Other AEs: Hypercapnia, Thrombocytopenia...
Other AEs:
Hypercapnia (below serious, 12 patients)
Thrombocytopenia (below serious, 12 patients)
Leukocytosis (below serious, 38 patients)
Hypokalaemia (below serious, 20 patients)
Hyperkalaemia (below serious, 3 patients)
Hyponatraemia (below serious, 10 patients)
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765232
AEs

AEs

AESignificanceDosePopulation
Pruritis 11%
31.5 mg 3 times / day multiple, intranasal
Recommended
Dose: 31.5 mg, 3 times / day
Route: intranasal
Route: multiple
Dose: 31.5 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
unhealthy, 51.7
n = 199
Health Status: unhealthy
Condition: pain
Age Group: 51.7
Sex: M+F
Population Size: 199
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
Tachycardia 14%
31.5 mg 3 times / day multiple, intranasal
Recommended
Dose: 31.5 mg, 3 times / day
Route: intranasal
Route: multiple
Dose: 31.5 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
unhealthy, 51.7
n = 199
Health Status: unhealthy
Condition: pain
Age Group: 51.7
Sex: M+F
Population Size: 199
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
Anemia 19%
31.5 mg 3 times / day multiple, intranasal
Recommended
Dose: 31.5 mg, 3 times / day
Route: intranasal
Route: multiple
Dose: 31.5 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
unhealthy, 51.7
n = 199
Health Status: unhealthy
Condition: pain
Age Group: 51.7
Sex: M+F
Population Size: 199
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
Flatulence 23%
31.5 mg 3 times / day multiple, intranasal
Recommended
Dose: 31.5 mg, 3 times / day
Route: intranasal
Route: multiple
Dose: 31.5 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
unhealthy, 51.7
n = 199
Health Status: unhealthy
Condition: pain
Age Group: 51.7
Sex: M+F
Population Size: 199
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
Headache 24%
31.5 mg 3 times / day multiple, intranasal
Recommended
Dose: 31.5 mg, 3 times / day
Route: intranasal
Route: multiple
Dose: 31.5 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
unhealthy, 51.7
n = 199
Health Status: unhealthy
Condition: pain
Age Group: 51.7
Sex: M+F
Population Size: 199
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
Nasal passage irritation 24%
31.5 mg 3 times / day multiple, intranasal
Recommended
Dose: 31.5 mg, 3 times / day
Route: intranasal
Route: multiple
Dose: 31.5 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
unhealthy, 51.7
n = 199
Health Status: unhealthy
Condition: pain
Age Group: 51.7
Sex: M+F
Population Size: 199
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
Vomiting 28%
31.5 mg 3 times / day multiple, intranasal
Recommended
Dose: 31.5 mg, 3 times / day
Route: intranasal
Route: multiple
Dose: 31.5 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
unhealthy, 51.7
n = 199
Health Status: unhealthy
Condition: pain
Age Group: 51.7
Sex: M+F
Population Size: 199
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
Constipation 29%
31.5 mg 3 times / day multiple, intranasal
Recommended
Dose: 31.5 mg, 3 times / day
Route: intranasal
Route: multiple
Dose: 31.5 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
unhealthy, 51.7
n = 199
Health Status: unhealthy
Condition: pain
Age Group: 51.7
Sex: M+F
Population Size: 199
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
Nausea 58%
31.5 mg 3 times / day multiple, intranasal
Recommended
Dose: 31.5 mg, 3 times / day
Route: intranasal
Route: multiple
Dose: 31.5 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
unhealthy, 51.7
n = 199
Health Status: unhealthy
Condition: pain
Age Group: 51.7
Sex: M+F
Population Size: 199
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
Dizziness 6%
31.5 mg 3 times / day multiple, intranasal
Recommended
Dose: 31.5 mg, 3 times / day
Route: intranasal
Route: multiple
Dose: 31.5 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
unhealthy, 51.7
n = 199
Health Status: unhealthy
Condition: pain
Age Group: 51.7
Sex: M+F
Population Size: 199
Sources:
https://pubmed.ncbi.nlm.nih.gov/19594851/
Leucopenia below serious, 1 patient
90 mg single, intravenous
Dose: 90 mg
Route: intravenous
Route: single
Dose: 90 mg
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765128
unhealthy
n = 8
Health Status: unhealthy
Condition: Percutaneous Nephrolithotomy operation
Population Size: 8
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765128
Hypokalaemia below serious, 2 patients
90 mg single, intravenous
Dose: 90 mg
Route: intravenous
Route: single
Dose: 90 mg
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765128
unhealthy
n = 8
Health Status: unhealthy
Condition: Percutaneous Nephrolithotomy operation
Population Size: 8
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765128
Hyponatraemia below serious, 3 patients
90 mg single, intravenous
Dose: 90 mg
Route: intravenous
Route: single
Dose: 90 mg
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765128
unhealthy
n = 8
Health Status: unhealthy
Condition: Percutaneous Nephrolithotomy operation
Population Size: 8
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765128
Thrombocytopenia below serious, 3 patients
90 mg single, intravenous
Dose: 90 mg
Route: intravenous
Route: single
Dose: 90 mg
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765128
unhealthy
n = 8
Health Status: unhealthy
Condition: Percutaneous Nephrolithotomy operation
Population Size: 8
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765128
Anaemia below serious, 7 patients
90 mg single, intravenous
Dose: 90 mg
Route: intravenous
Route: single
Dose: 90 mg
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765128
unhealthy
n = 8
Health Status: unhealthy
Condition: Percutaneous Nephrolithotomy operation
Population Size: 8
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765128
Hyponatraemia below serious, 10 patients
90 mg single, intravenous
Dose: 90 mg
Route: intravenous
Route: single
Dose: 90 mg
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765232
unhealthy
n = 57
Health Status: unhealthy
Condition: Laparoscopic Donor Nephrectomy
Population Size: 57
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765232
Hypercapnia below serious, 12 patients
90 mg single, intravenous
Dose: 90 mg
Route: intravenous
Route: single
Dose: 90 mg
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765232
unhealthy
n = 57
Health Status: unhealthy
Condition: Laparoscopic Donor Nephrectomy
Population Size: 57
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765232
Thrombocytopenia below serious, 12 patients
90 mg single, intravenous
Dose: 90 mg
Route: intravenous
Route: single
Dose: 90 mg
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765232
unhealthy
n = 57
Health Status: unhealthy
Condition: Laparoscopic Donor Nephrectomy
Population Size: 57
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765232
Hypokalaemia below serious, 20 patients
90 mg single, intravenous
Dose: 90 mg
Route: intravenous
Route: single
Dose: 90 mg
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765232
unhealthy
n = 57
Health Status: unhealthy
Condition: Laparoscopic Donor Nephrectomy
Population Size: 57
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765232
Hyperkalaemia below serious, 3 patients
90 mg single, intravenous
Dose: 90 mg
Route: intravenous
Route: single
Dose: 90 mg
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765232
unhealthy
n = 57
Health Status: unhealthy
Condition: Laparoscopic Donor Nephrectomy
Population Size: 57
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765232
Leukocytosis below serious, 38 patients
90 mg single, intravenous
Dose: 90 mg
Route: intravenous
Route: single
Dose: 90 mg
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765232
unhealthy
n = 57
Health Status: unhealthy
Condition: Laparoscopic Donor Nephrectomy
Population Size: 57
Sources:
https://clinicaltrials.gov/ct2/show/NCT00765232
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer
OAT1
599

OAT3
642

OCTN2
66

UGT2B7
146
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
UGT2B7
157
 no [IC50 >1000 uM]
OAT1
603
 strong [IC50 0.653 uM]
OAT3
644
 strong
OCTN2
71
 weak [Ki 1530 uM]
PubMed

PubMed

TitleDatePubMed
Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: a full in vitro analysis.
1999 Jun 22
Ketorolac entrapped in polymeric micelles: preparation, characterisation and ocular anti-inflammatory studies.
2000 Nov 19
Parecoxib (parecoxib sodium).
2001
Analgesic efficacy of ketorolac and morphine in neonatal rats.
2001 Apr
Corneal complications associated with topical ophthalmic use of nonsteroidal antiinflammatory drugs.
2001 Apr
New advances in the treatment of sickle cell disease: focus on perioperative significance.
2001 Aug
Prohemorrhagic potential of dipyrone, ibuprofen, ketorolac, and aspirin: mechanisms associated with blood flow and erythrocyte deformability.
2001 Aug
Treatment of vinorelbine-associated tumor pain.
2001 Aug
Delayed diffuse lamellar keratitis after laser in situ keratomileusis.
2001 Dec
Topical ketorolac after cataract surgery.
2001 Dec
Incidence of hematoma associated with ketorolac after TRAM flap breast reconstruction.
2001 Feb
Ketorolac reduces postoperative narcotic requirements.
2001 Jan
Using evidence from different sources: an example using paracetamol 1000 mg plus codeine 60 mg.
2001 Jan 10
A double-blind, randomized comparison of intramuscularly and intravenously administered parecoxib sodium versus ketorolac and placebo in a post-oral surgery pain model.
2001 Jul
Testing and comparison of non-opioid analgesics in amphibians.
2001 Jul
In vitro effects of NSAIDS and paracetamol on oxidative stress-related parameters of human erythrocytes.
2001 Jun
Prospective double-blind study of effect of ketorolac administration after laparoscopic urologic surgery.
2001 Mar
In vitro based index of topical anti-inflammatory activity to compare a series of NSAIDs.
2001 Mar
Postoperative narcotic requirement after microscopic lumbar discectomy is not affected by intraoperative ketorolac or bupivacaine.
2001 Mar 15
Children's use of PCA following spinal fusion.
2001 Mar-Apr
Effect of preemptive multimodal analgesia for arthroscopic knee ligament repair.
2001 Mar-Apr
Precipitation in Manchester: ketorolac/cyclizine.
2001 May
Pain control after knee arthroplasty: intraarticular versus epidural anesthesia.
2001 Nov
Safety of ketorolac in the pediatric population after ureteroneocystostomy.
2001 Nov
Analgesia and COX-2 inhibition.
2001 Nov-Dec
Upper gastrointestinal safety evaluation of parecoxib sodium, a new parenteral cyclooxygenase-2-specific inhibitor, compared with ketorolac, naproxen, and placebo.
2001 Sep
Effect of 10 pharmacologic probes on mRNA levels of inducible nitric oxide synthetase and selected inflammatory cytokines in a rat model of acute otitis media.
2002 Apr
Drug-induced extrapyramidal reactions.
2002 Feb
A systematic review of adjuncts for intravenous regional anesthesia for surgical procedures.
2002 Jan
Opioid-free analgesia following total knee arthroplasty--a multimodal approach using continuous lumbar plexus (psoas compartment) block, acetaminophen, and ketorolac.
2002 Jan-Feb
Effect of ketorolac on renal function after donor nephrectomy.
2002 Jun
The influence of timing and route of administration of intravenous ketorolac on analgesia after hand surgery.
2002 Jun
Intra-muscular ketorolac administered as a supplemental analgesic for removal of impacted third molar teeth: a prospective study.
2002 Mar
Parenteral ketorolac and risk of myocardial infarction.
2002 Mar
Effect of topical diclofenac and ketorolac on patient discomfort and corneal sensitivity.
2002 Mar-Apr
Pain reduction after laser in situ keratomileusis with ketorolac tromethamine ophthalmic solution 0.5%: a randomized, double-masked, placebo-controlled trial.
2002 Mar-Apr
Comparison of the morphine-sparing effects of diclofenac sodium and ketorolac tromethamine after major orthopedic surgery.
2002 May
Role for both spinal cord COX-1 and COX-2 in maintenance of mechanical hypersensitivity following peripheral nerve injury.
2002 May 24
Patents

Patents

04089969
3
JP2002528495A
37
JP2003507415A
33
JP2006500085A
2
JP2009525778A
32
JP2011524366A
2
JP2966094B2
2
JP4756823B2
22

Sample Use Guides

In Vivo Use Guide
The recommended dose of ACULAR LS (ketorolac tromethamine ophthalmic solution) is one drop four times a day in the operated eye as needed for pain and burning/stinging for up to 4 days following corneal refractive surgery. Ketorolac tromethamine ophthalmic solution has been safely administered in conjunction with other ophthalmic medications such as antibiotics, beta blockers, carbonic anhydrase inhibitors, cycloplegics, and mydriatics.
Route of Administration: Other
In Vitro Use Guide
It was discovered, that ketorolac inhibition of stretch-induced ureteral contractility was concentration-dependent between 1 nM and 1 microM. Local administration of ketorolac at these doses may be useful during the management of stones while at the same time limiting the risk for adverse effects. Porcine ureter strips attached to force displacement transducers were suspended in organ tissue baths that contained aerated Krebs buffer. Tissues equilibrated for 1 hour, and a spontaneous contractility rate was established. Tissues were incubated with a concentration-response curve of ketorolac (0.1 nM-10 microM) for 90 minutes and compared with indomethacin (1 muM) and dimethyl sulfoxide (DMSO) 0.1%. Contractility rates were recorded on a polygraph and analyzed for changes over exposure time
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:36:52 GMT 2023
Edited
by admin
on Fri Dec 15 15:36:52 GMT 2023
Record UNII
4EVE5946BQ
Record Status Validated (UNII)
Record Version
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Name Type Language
KETOROLAC TROMETHAMINE
ORANGE BOOK   USAN   USP   USP-RS   VANDF   WHO-DD  
USAN  
Official Name English
OMIDRIA COMPONENT KETOROLAC TROMETHAMINE
Brand Name English
(±)-5-BENZOYL-2,3-DIHYDRO-1H-PYRROLIZINE-1-CARBOXYLIC ACID, COMPOUND WITH 2-AMINO-2-(HYDROXYMETHYL)-1,3-PROPANEDIOL (1:1)
Common Name English
LIXIDOL
Brand Name English
KETOROLAC TROMETAMOL [JAN]
Common Name English
KETOROLAC TROMETHAMINE [USP MONOGRAPH]
Common Name English
ACULAR
Brand Name English
KETOROLAC TROMETHAMINE COMPONENT OF OMIDRIA
Brand Name English
KETOROLAC TROMETAMOL
EP   MART.  
Common Name English
ACUVAIL
Brand Name English
TARASYN
Brand Name English
2-AMINO-2-(HYDROXYMETHYL)PROPANE-1,3-DIOL (1RS)-5-BENZOYL-2,3-DIHYDRO-1H-PYRROLIZINE-1-CARBOXYLATE
Systematic Name English
NSC-758637
Code English
KETOROLAC TROMETHAMINE [USP-RS]
Common Name English
1H-PYRROLIZINE-1-1H-PYRROLIZINE-1-CARBOXYLIC ACID, 5-BENZOYL-2,3-DIHYDRO, (±)-, COMPOUND WITH 2-AMINO-2-(HYDROXYMETHYL)-1,3-PROPANEDIOL (1:1)
Common Name English
Ketorolac tromethamine [WHO-DD]
Common Name English
KETOROLAC TROMETHAMINE [USAN]
Common Name English
DOLAC
Brand Name English
KETOROLAC (±)-FORM TROMETHAMINE SALT [MI]
Common Name English
KETOROLAC TROMETHAMINE [VANDF]
Common Name English
TORADOL
Brand Name English
KETOROLAC TROMETHAMINE [ORANGE BOOK]
Common Name English
SPRIX
Brand Name English
KETOROLAC TROMETAMOL [EP MONOGRAPH]
Common Name English
KETOROLAC TROMETAMOL [MART.]
Common Name English
2-AMINO-2-(HYDROXYMETHYL)PROPANE-1,3-DIOL; 5-BENZOYL-2,3-DIHYDRO-1H-PYRROLIZINE-1-CARBOXYLIC ACID
Systematic Name English
Classification Tree Code System Code
NCI_THESAURUS C1323
Created by admin on Fri Dec 15 15:36:52 GMT 2023 , Edited by admin on Fri Dec 15 15:36:52 GMT 2023
Code System Code Type Description
NCI_THESAURUS
C61798
Created by admin on Fri Dec 15 15:36:52 GMT 2023 , Edited by admin on Fri Dec 15 15:36:52 GMT 2023
PRIMARY
EVMPD
SUB02835MIG
Created by admin on Fri Dec 15 15:36:52 GMT 2023 , Edited by admin on Fri Dec 15 15:36:52 GMT 2023
PRIMARY
PUBCHEM
84003
Created by admin on Fri Dec 15 15:36:52 GMT 2023 , Edited by admin on Fri Dec 15 15:36:52 GMT 2023
PRIMARY
FDA UNII
4EVE5946BQ
Created by admin on Fri Dec 15 15:36:52 GMT 2023 , Edited by admin on Fri Dec 15 15:36:52 GMT 2023
PRIMARY
ChEMBL
CHEMBL469
Created by admin on Fri Dec 15 15:36:52 GMT 2023 , Edited by admin on Fri Dec 15 15:36:52 GMT 2023
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EPA CompTox
DTXSID0045597
Created by admin on Fri Dec 15 15:36:52 GMT 2023 , Edited by admin on Fri Dec 15 15:36:52 GMT 2023
PRIMARY
USAN
T-104
Created by admin on Fri Dec 15 15:36:52 GMT 2023 , Edited by admin on Fri Dec 15 15:36:52 GMT 2023
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RS_ITEM_NUM
1356665
Created by admin on Fri Dec 15 15:36:52 GMT 2023 , Edited by admin on Fri Dec 15 15:36:52 GMT 2023
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CHEBI
6130
Created by admin on Fri Dec 15 15:36:52 GMT 2023 , Edited by admin on Fri Dec 15 15:36:52 GMT 2023
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DRUG BANK
DBSALT001045
Created by admin on Fri Dec 15 15:36:52 GMT 2023 , Edited by admin on Fri Dec 15 15:36:52 GMT 2023
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CAS
74103-07-4
Created by admin on Fri Dec 15 15:36:52 GMT 2023 , Edited by admin on Fri Dec 15 15:36:52 GMT 2023
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SMS_ID
100000091653
Created by admin on Fri Dec 15 15:36:52 GMT 2023 , Edited by admin on Fri Dec 15 15:36:52 GMT 2023
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RXCUI
28200
Created by admin on Fri Dec 15 15:36:52 GMT 2023 , Edited by admin on Fri Dec 15 15:36:52 GMT 2023
PRIMARY RxNorm
MESH
D020911
Created by admin on Fri Dec 15 15:36:52 GMT 2023 , Edited by admin on Fri Dec 15 15:36:52 GMT 2023
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DAILYMED
4EVE5946BQ
Created by admin on Fri Dec 15 15:36:52 GMT 2023 , Edited by admin on Fri Dec 15 15:36:52 GMT 2023
PRIMARY
MERCK INDEX
m6623
Created by admin on Fri Dec 15 15:36:52 GMT 2023 , Edited by admin on Fri Dec 15 15:36:52 GMT 2023
PRIMARY Merck Index
NSC
758637
Created by admin on Fri Dec 15 15:36:52 GMT 2023 , Edited by admin on Fri Dec 15 15:36:52 GMT 2023
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Related Record Type Details
Structure of KETOROLAC
PARENT -> SALT/SOLVATE
Structure of KETOROLAC TROMETHAMINE, (R)-
ENANTIOMER -> RACEMATE
Structure of KETOROLAC TROMETHAMINE
BASIS OF STRENGTH->SUBSTANCE
ASSAY (TITRATION)
EP
Structure of KETOROLAC TROMETHAMINE
BASIS OF STRENGTH->SUBSTANCE
ASSAY (HPLC)
USP
Structure of KETOROLAC TROMETHAMINE, (S)-
ENANTIOMER -> RACEMATE
Related Record Type Details
Structure of 5-BENZOYL-2,3-DIHYDRO-1H-PYRROLIZIN-1-ONE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of 5-BENZOYL-2,3-DIHYDRO-1H-PYRROLIZIN-1-OL, (±)-
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of 1H-PYRROLIZINE-1-CARBOXAMIDE, 5-BENZOYL-2,3-DIHYDRO-N-(2-HYDROXY-1,1-BIS(HYDROXYMETHYL)ETHYL)-, (±)-
IMPURITY -> PARENT
Structure of KETOROLAC ETHYL ESTER
IMPURITY -> PARENT
unspecified
UNKNOWN
EP
Structure of 5-BENZOYL-1-METHOXY-2,3-DIHYDRO-1H-PYRROLIZINE-1-CARBOXYLIC ACID, (±)-
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
Structure of METHYL 5-BENZOYL-1-HYDROXY2,3-DIHYDRO-1H-PYRROLIZINE-1-CARBOXYLATE, (±)-
IMPURITY -> PARENT
unspecified
UNKNOWN
EP
Structure of 5-BENZOYL-2,3-DIHYDRO-1H-PYRROLIZIN-1-OL, (±)-
IMPURITY -> PARENT
For the calculation of contents, multiply the peak areas by 0.67
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
Structure of 5-BENZOYL-2,3-DIHYDRO-1H-PYRROLIZIN-1-ONE
IMPURITY -> PARENT
For the calculation of contents, multiply the peak areas by 0.52
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
Structure of 6-BENZOYL-2,3-DIHYDRO-1H-PYRROLIZINE-1-CARBOXYLIC ACID, (±)-
IMPURITY -> PARENT
For the calculation of contents, multiply the peak areas by 2.2
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
Structure of 7-BENZOYL-2,3-DIHYDRO-1H-PYRROLIZINE-1-CARBOXYLIC ACID, (±)-
IMPURITY -> PARENT
unspecified
UNKNOWN
EP
Structure of PHENYL(2,3-DIHYDRO-1H-PYRROLIZIN-5-YL)METHANONE
IMPURITY -> PARENT
unspecified
UNKNOWN
EP
Structure of KETOROLAC METHYL ESTER
IMPURITY -> PARENT
unspecified
UNKNOWN
EP
Related Record Type Details
Structure of KETOROLAC
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