KETOROLAC TROMETHAMINE INJECTION 30mg/ML FOR INTRAVENOUS, INTRAMUSCULAR USE

Product Information

Registration Status: Active

KETOROLAC TROMETHAMINE INJECTION 30mg/ML is approved to be sold in Singapore with effective from 2000-06-16. It is marketed by HOSPIRA SINGAPORE PTE LTD, with the registration number of SIN11340P.

This product contains Ketorolac 30mg/ml in the form of INJECTION. It is approved for INTRAVENOUS, INTRAMUSCULAR use.

This product is manufactured by HOSPIRA INC in UNITED STATES.

It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Description

A pyrrolizine carboxylic acid derivative structurally related to indomethacin. It is an NSAID and is used principally for its analgesic activity. (From Martindale The Extra Pharmacopoeia, 31st ed)

Indication

For the short-term (~5 days) management of moderately severe acute pain that requires analgesia at the opioid level, usually in a postoperative setting.

Mechanism of Action

Ketorolac is a nonsteroidal anti-inflammatory drug (NSAID) chemically related to indomethacin and tolmetin. 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 medications. Analgesia is probably produced via a peripheral action in which blockade of pain impulse generation results from decreased prostaglandin activity. However, inhibition of the synthesis or actions of other substances that sensitize pain receptors to mechanical or chemical stimulation may also contribute to the analgesic effect. In terms of the ophthalmic applications of ketorolac - ocular administration of ketorolac reduces prostaglandin E2 levels in aqueous humor, secondary to inhibition of prostaglandin biosynthesis.

Pharmacokinetics

Absorption: Rapidly and completely absorbed after oral administration
Distribution: * 0.26 ± 0.08 L/kg [children 4 to 8 years old]
Metabolism: Primarily hepatic. Less than 50% of a dose is metabolized. The major metabolites are a glucuronide conjugate, which may also be formed in the kidney, and p-hydroxy ketorolac. Neither metabolite has significant analgesic activity.
Elimination

Clearance

* 0.042 +/- 0.01 L/hr/kg [Pediatric Patients] * 0.02 L/h/kg [Normal Subjects IM] * 0.03 L/h/kg [Normal Subjects oral] * 0.02 L/h/kg [Healthy Elderly Subjects IM] * 0.02 L/h/kg [Healthy Elderly Subjects oral] * 0.03 L/h/kg [Patients with Hepatic Dysfunction IM] * 0.03 L/h/kg [Patients with Hepatic Dysfunction oral] * 0.02 L/h/kg [Patients with Renal Impairment IM] * 0.02 L/h/kg [Patients with Renal Impairment oral] * 0.02 L/h/kg [Renal Dialysis Patients IM]

Toxicity

LD₅₀ = 189 mg/kg (rat, oral).

Active Ingredient/Synonyms

Source of information: Drugbank (External Link). Last updated on: 3^rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.