Customization: | Available |
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CAS No.: | 74103-07-4 |
Formula: | C19h24n2o6 |
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Product names | Ketorolac Tromethamine |
CAS No | 74103-07-4 |
Ketorolac tromethamine is an off-white to pale yellow crystalline powder with a pKa of 3.54 in water. It is highly soluble in water, with more than 500 mg dissolving in one mL at room temperature. The commercially available injection form is a clear, slightly yellow solution with a pH of 6.9-7.9.
Medical Uses
Ketorolac tromethamine is a nonsteroidal anti-inflammatory drug (NSAID) that exhibits analgesic, anti-inflammatory, and antipyretic effects. It is primarily used for:
Pain Management: Effective in managing moderate to severe postoperative pain.
Ophthalmic Use: Used in eye drops to treat ocular pain and inflammation, particularly after cataract surgery.
Seasonal Allergic Conjunctivitis: Approved for relieving ocular itching associated with seasonal allergies.
Mechanism of Action
Ketorolac tromethamine inhibits both COX-1 and COX-2 enzymes, preventing the synthesis of prostaglandins, which mediate pain, inflammation, and fever. This dual inhibition provides potent analgesic and anti-inflammatory effects but also increases the risk of gastrointestinal side effects.
Pharmacokinetics
Absorption: Rapidly absorbed after oral administration with a bioavailability of about 80%. Peak plasma levels are reached within 20-60 minutes.
Distribution: Widely distributed throughout the body but does not cross the blood-brain barrier.
Metabolism: Primarily metabolized in the liver via glucuronidation and hydroxylation.
Excretion: Eliminated mainly through urine, with 60% of the drug excreted unchanged.
Half-Life: The S-enantiomer has a half-life of about 2.5 hours, while the R-enantiomer has a half-life of about 5 hours.