ChemicalBook > Product Catalog > Biochemical Engineering > Inhibitors > Neuronal Signaling > COX inhibitors > Ketorolac tromethamine
Ketorolac tromethamine Chemical Properties
- Melting point:160-161 C
- storage temp. Hygroscopic, Refrigerator, Under Inert Atmosphere
- solubility H2O: 15 mg/mL stable at least one month at −20 °C., soluble
- form crystalline
- Merck 14,5306
- CAS DataBase Reference74103-07-4(CAS DataBase Reference)
Ketorolac tromethamine Usage And Synthesis
- DescriptionKetorolac tromethamine is a nonsteroidal antiinflammatory agent that exhibits analgesic and antipyretic activity. The compound is effective in the management of moderate to severe postoperative pain. It is, however, the first of this type of agent to be administered parenterally as an analgesic and is specifically indicated for intramuscular injection. Ketorolac represents a useful alternative to the narcotic analgesics due to its lack of abuse potential.
- Chemical PropertiesOff-White to Pale Yellow Solid
- Chemical PropertiesA carboxylic acid derivative nonsteroidal antiinflammatory agent, ketorolac tromethamine occurs as an off-white crystalline powder with a pKa of 3.54 (in water). More than 500 mg are soluble in one mL of water at room temperature. The commercially available injection is a clear, slightly yellow solution with a pH of 6.9 – 7.9. Sodium chloride is added to make the solution isotonic. Ketorolac tromethamine may also be known as RS-37619-00- 31-3; many trade names are available.
- OriginatorSyntex (USA)
- UsesAnalgesic;Cyclooxygenase Inhibitor
- UsesKetorolac is used primarily for its analgesic effects for short-term treatment of mild to moderate pain in dogs and rodents. The duration of analgesic effect in dogs is about 8 – 12 hours, but because of the availability of approved, safer NSAIDs for dogs, its use is questionable.
- UsesCyclo-oxygenase inhibitor; analgesic; anti-inflammatory.
- DefinitionChEBI: An organoammonium salt resulting from the mixture of equimolar amounts of ketorolac and tromethamine (tris). It has potent non-sedating analgesic and moderate anti-inflammatory effects. It is used in the short-term management of post-operative pain, and in eye drops to relieve the ocular itching associated with seasonal allergic conjunctivitis.
- IndicationsKetorolac tromethamine is a pyrrolol-pyrrole nonsteroidal anti- inflammatory agent that inhibits prostaglandin formation. Prostaglandins mediate inflammation within the eye by disrupting the blood-aqueous barrier, inducing vasodilation and increasing intraocular pressure. Prostaglandins may also cause iris sphincter constriction (miosis) independent of cholinergic mechanisms. Ketorolac tromethamine is marketed for use before cataract extraction in human patients (to prevent miosis during surgery) and for control of post surgical inflammation, especially following cataract surgery. It is also approved for management of conjunctivitis associated with seasonal allergy in people. In veterinary medicine, ketorolac tromethamine is primarily used to control surgical or nonsurgical uveitis particularly in cases with concurrent corneal bacterial infection or ulceration when topical corticosteroids are contraindicated. It is also used in diabetic patients, especially smaller patients, adversely affected by systemic uptake of topically applied corticosteroids. Nonsteroidal agents like ketorolac tromethamine can be combined with topical steroids in patients with severe uveal inflammation.
- brand nameAcular (Allergan); Toradol (Roche);Toradol IM.
- PharmacokineticsAfter oral administration, ketorolac is rapidly absorbed; in dogs peak levels occur in about 50 minutes and oral bioavailability is about 50 – 75%.
Ketorolac is distributed marginally through the body. It does not appear to cross the blood-brain barrier and is highly bound to plasma proteins (99%). The volume of distribution in dogs is reported to be about 0.33 – 0.42 L/kg (similar in humans). The drug does cross the placenta.
Ketorolac is primarily metabolized via glucuronidation and hydroxylation. Both unchanged drug and metabolites are excreted mainly in the urine. Patients with diminished renal function will have longer elimination times than normal. In normal dogs, the elimination half-life is between 4 – 8 hours.
- PharmacologyLike other NSAIDs, ketorolac exhibits analgesic, antiinflammatory, and antipyretic activity probably through its inhibition of cyclooxygenase with resultant impediment of prostaglandin synthesis. Ketorolac may exhibit a more potent analgesic effect than some other NSAIDs. It inhibits both COX-1 and COX-2 receptors.
- Side effectsThe manufacturer indicates that ketorolac tromethamine does not enhance the spread of preexisting corneal fungal, viral or bacterial infections in animal models. Ketorolac tromethamine does not in and of itself induce postoperative pressure elevation other then that which frequently follows cataract extraction in people and animals.
- Safety ProfileKetorolac does cross the placenta. In humans, the FDA categorizes this drug as category C for use during the first two trimesters of pregnancy (Animal studies have shown an adverse effect on the fetus, but there are no adequate studies in humans; or there are no animal reproduction studies and no adequate studies in humans.) In humans, all NSAIDs are assigned to category D for use during pregnancy during the third trimester or near delivery (There is evidence of human fetal risk, but the potential benefits from the use of the drug in pregnant women may be acceptable despite its potential risks.) Most NSAIDs are excreted in milk. Ketorolac was detected in human breast milk at a maximum milk:plasma ratio of 0.037. It is unlikely to pose great risk to nursing offspring.
- Veterinary Drugs and TreatmentsKetorolac is used primarily for its analgesic effects for short-term treatment of mild to moderate pain in dogs and rodents. The duration of analgesic effect in dogs is about 8 – 12 hours, but because of the availability of approved, safer NSAIDs for dogs, its use is questionable.
- OverdosageLimited information is available. The oral LD50 is 200 mg/kg in mice. GI effects, including GI ulceration are likely in overdoses in small animals. Metabolic acidosis was reported in one human patient. Consider GI emptying in large overdoses; patients should be monitored for GI bleeding. Treat ulcers with sucralfate; consider giving misoprostol early.
- PrecautionsKetorolac is relatively contraindicated in patients with a history of, or preexisting, hematologic, renal or hepatic disease. It is contraindicated in patients with active GI ulcers or with a history of hypersensitivity to the drug. It should be used cautiously in patients with a history of GI ulcers, or heart failure (may cause fluid retention), and in geriatric patients. Animals suffering from inflammation secondary to concomitant infection, should receive appropriate antimicrobial therapy. Because ketorolac has a tendency to cause gastric erosion and ulcers in dogs, long-term use (>3 days) is not recommended in this species.
- Ketorolac Related Compound B (20 mg) (5-benzoyl-2,3-dihydro-1H-pyrrolizin-1-ol) rac Ketorolac 6-Benzoyl IsoMer Ketorolac EP IMpurity F Ketorolac EP IMpurity I 1-Keto Ketorolac Ketorolac Related Compound A (20 mg) (5-benzoyl-N-(1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl)-2,3-dihydro-1H-pyrrolizine-1-carboxamide) Ketorolac EP IMpurity H Ketorolac EP IMpurity D Ketorolac EP IMpurity G Ketorolac Ammonia TRISTEARIN Ketorolac tromethamine Tris(hydroxymethyl)aminomethane acetate salt 2-Acetyl-1-ethylpyrrole 1-METHYL-PYRROLE-2-ACETIC ACID KETOROLAC 2-Acetyl-1-methylpyrrole
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