ZIROLAC
Therapeutic Indication
Short-term management of moderately severe, acute pain at the opioid level.
Dosage Forms
Soln for inj (amp) 30 mg/mL x 1 mL x 10’s
Bioavailability and Pharmacokinetics
Keterolac trometamol is absorbed after intramuscular or oral doses. At physiological pH, Keterolac trometamol dissociates to form an ionic keterolac molecule which is less hydrophilic than the trometamol salt. The peak plasma concentration of keterolac is reached within 30-60 mins; absorption after intramuscular injection may be slower than after oral doses. Keterolac is highly bound to plasma protein. It does not readily penetrate the blood barrier. Keterolac can cross the placenta and small amounts of drugs are distributed into breast milk. The terminal plasma half life is 4-6hrs, but in adults it is about 6-7hrs and in patients with renal dysfunction it is 9-10hrs. Glucuronic acid conjugation is the major metabolic pathway and there is some parahydroxilation. About 90% of a dose is excreted in urine as unchanged drug and conjugated and hydroxylated metabolites; some are excreted in the feces.
Dosage Range
Adult Initially 10 mg IV/IM. Maintenance: 10-30 mg 4-6 hrly. Childn ≥2 yr 0.5-1 mg/kg as a single dose. May repeat 0.5 mg/kg 6 hrly if necessary & therapy should not exceed 2 days. Elderly, renal failure, patients <50 kg body wt Daily dose should not exceed 60 mg. Max duration: 5 days.
Known Adverse Effects and Toxicities
Nausea, dyspepsia, GI pain, diarrhea; HTN; skin flare; purpura; headache, sweating; mental & sensory changes, aseptic meningitis, hyponatremia, hyperkalemia, nephritic syndrome & flank pain or w/o hematuria.
Special Precautions
History of renal disorder, hepatic & GI disease. Depressed renal function, HTN, cardiac decompensation, CHF, active GI disease, asthma. Hepatic impairment. Concomitant use w/ diuretics. May impair ability to drive or operate machinery. Elderly.
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