Novell Pharma




Genemax Healthcare
Full Prescribing Info
Ketorolac tromethamine.
Name and dose of active substance: Ketorolac tromethamine 30 mg.
Pharmaceutical form: Injection.
Appearance: Sterile odorless and colorless until pale yellow solution.
Route of administration: Intramuscular or Intravenous Injection.
Pharmacology: Pharmacodynamics: Ketorolac tromethamine is a non-steroidal anti-inflammatory drug. It has anti-inflammatory, analgesic and antipyretic activity.
Ketorolac tromethamine may inhibit the synthesis of prostaglandins in tissues by inhibiting cyclooxygenase, an enzyme that catalyzes the formation of prostaglandins from arachidonic acid.
Pharmacokinetics: Ketorolac tromethamine is absorbed after intramuscular or oral doses. At physiological pH ketorolac tromethamine dissociates to form an anionic ketorolac molecule which is less hydrophilic than the tromethamine salt. The peak plasma concentration of ketorolac is reached within about 30 to 60 minutes; absorption after intramuscular injection maybe slower than that after oral doses in some individuals. Ketorolac is over 99% bound to plasma proteins. It does not readily penetrate the blood brain barrier. Ketorolac crosses the placenta and small amounts of drug are distributed into breast milk. The terminal plasma half-life is about 4 to 6 hours, but is about 6 to 7 hours in the elderly and 9 to 10 hours in patients with renal dysfunction. The major metabolic pathway is glucuronic acid conjugation; there is some para-hydroxylation. About 90% of a dose is excreted in urine as unchanged drug and conjugated and hydroxylated metabolites, the remainder are excreted in the feces.
Ketorolac is indicated for short-term treatment/therapy of moderate to severe acute post-operative pain.
Ketorolac is not recommended for use as an obstetrical pre-operative medication or for obstetrical analgesic because it inhibits prostaglandin synthesis, which may affect uterine contraction and fetal circulation.
Dosage/Direction for Use
Recommended Dose: Single dose: IM: Adult: 60 mg.
Patient ≥65 years, renally impaired &/or <50 kg body weight: 30 mg.
To be given slowly & deeply into the muscle.
IV: Adult: 30 mg.
Patient ≥65 years, renally impaired &/or <50 kg body weight: 15 mg.
IV bolus to be given over no <15 seconds.
For children a maximum dose for IM is 30 mg (single dose), a maximum dose for IV is 15 mg (single dose).
Multiple dose: IV/IM: Adult: 30 mg 6 hourly. Max: 120 mg/day.
Patient ≥65 years, renally impaired &/or <50 kg body weight: 15 mg 6 hourly.
Max: 60 mg/day.
Mode of Administration: Administer IV, IM in adults; administer IV or IM in children 2-16 years of age.
Initiate therapy in adults with parenteral (IV or IM) ketorolac; oral formulation is used as continuation therapy, as required.
Administer IV or IM as a single dose or every 6 hours. In children 2-16 years of age, administer as a single IV or IM dose.
Switch patients to alternate analgesic therapy as soon as clinically possible.
IV: Administer over ≥15 seconds.
IM: Administer IM slowly and deeply into the muscle.
Onset: IM administration: Onset in 10 minutes, with peak analgesia at 75-150 minutes.
Duration: IM administration: 6-8 hours
Signs and Symptoms: Single overdoses of ketorolac have been variously associated with abdominal pain, nausea, vomiting, hyperventilation, peptic ulcers and/or erosive gastritis and renal dysfunction which have resolved after discontinuation of dosing. Gastrointestinal bleeding may occur.
Hypertension, acute renal failure, respiratory depression and coma may occur after the ingestion of NSAIDs but are rare. Headache, epigastric pain, disorientation, excitation, drowsiness, dizziness, tinnitus and fainting have also been observed. Rare cases of diarrhea and occasional convulsions have been reported. Anaphylactoid reactions have been reported with therapeutic ingestion of NSAIDs and may occur following an overdose.
Treatment: Patients should be managed by symptomatic and supportive care following NSAIDs overdose.
There are no specific antidotes. Dialysis does not significantly clear ketorolac from the blood stream. Within one hour of ingestion of a potentially toxic amount, activated charcoal should be considered. Alternatively, in adults, gastric lavage should be considered within one hour of ingestion of a potentially life threatening overdose.
Good urine output should be ensured. Renal and liver function should be closely monitored. Patients should be observed for at least 4 hours after ingestion of potentially toxic amounts. Frequent or prolonged convulsions should be treated with intravenous diazepam. Other measures may be indicated by the patient's clinical condition.
Contraindicated in patients with hypersensitivity to ketorolac, any of its excipients, orother NSAIDs.
Contraindicated in patients with nasal polyp, angioedema or bronchospasm.
Contraindicated in patients with moderate or severe renal impairment or at risk of renal failure due to volume depletion.
Contraindicated in patients with severe heart failure.
Contraindicated in pregnancy, labour, delivery or lactation.
Contraindicated in patients with suspected or confirmed cerebrovascular bleeding, hemorrhagic diathesis, incomplete hemostasis or high risk of bleeding.
Ketorolac is contraindicated as prophylactic analgesic before surgery or intra-operatively because of the increased risk of bleeding.
Ketorolac is contraindicated for the treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery.
Ketorolac is contraindicated for neuraxial (epidural or intrathecal) administration due to its alcohol content.
The concomitant use of ketorolac and probenecid, lithium salts, aspirin, other NSAIDs, or anticoagulants (warfarin, heparin) is contraindicated.
Warning according to Thai FDA Notification: Contraindicated in patients with history of asthma, urticaria or acute rhinitis that cause from aspirin or NSAIDs.
Pregnancy in the last quarter should avoid to use ketorolac, except the doctor prescribe.
Contraindicated in patients with GI bleeding or perforation.
Contraindicated in patients with severe hepatic failure, renal failure.
Contraindicated in patients with Dengue fever.
Ketorolac may increase risk of bleeding or ulceration on GI tract.
Ketorolac may increase risk of brain vascular and cardiovascular narrowing, especially for long term use with high dosage.
Ketorolac may cause undesirable effect of edema, therefore it should be used with caution in patients with cardiac and renal dysfunction.
Use with caution in hypertension or elderly.
Ketorolac inhibits platelet aggregation. Therefore it should be avoided to use in patients with suspected dengue fever or other platelet disorders.
Special Precautions
Ketorolac does not possess sedative or anxiolytic properties. Therefore, it is not recommended as a pre-operative medication for the support of anesthesia.
Use in Children: Safety and efficacy not established in children <2 years of age.
Use In Pregnancy & Lactation
Pregnancy: Reproduction studies in rabbits and rats receiving oral ketorolac tromethamine dosages of 3.6 and 10 mg/kg daily, respectively (about 1.8 and 5 times the maximum recommended human parenteral dosage, respectively), during the period of organogenesis have not revealed evidence of harm to the fetus; however, oral dosages exceeding the maximum recommended human parenteral dosage in rats produced delayed parturition and dystocia, probably secondary to inhibition of prostaglandin synthesis. There are no adequate and controlled studies to date using ketorolac tromethamine in pregnant women. Therefore ketorolac tromethamine is not recommended for use during pregnancy and should be used only when the potential benefits justify the possible risks to the fetus. Ketorolac tromethamine should not be used during late pregnancy or during labor or delivery, since inhibitors of prostaglandin synthesis may have adverse effects on the fetal cardiovascular system (e.g., premature closure of the ductus arteriosus) and on uterine contraction.
Lactation: Because ketorolac is distributed into milk, and because of the potential adverse effects of prostaglandin-inhibiting drugs in neonates, the drug should not be used in nursing women.
Adverse Reactions
Cardiovascular system: edema, hypertension.
Gastrointestinal tract: dyspepsia, nausea, GI pain (most common); diarrhea, constipation, flatulence, vomiting, stomatitis, peptic ulcer, GI bleeding.
Nervous system: headache, somnolence or drowsiness, dizziness.
Local and dermatologic: IM; pain at injection site (2-4%), ecchymosis, bruising, hematoma, pruritus, sweating and tingling at the injection site (reported rarely).
Ophthalmologic: blurred vision have been observed with NSAIDs.
Hepatic: borderline elevations of one or more liver function tests results (15% of patients).
Renal: elevations of serum urea, creatinine and potassium.
Drug Interactions
Ketorolac may slightly decrease protein binding of warfarin (from 99.5% to 99.3%).
However, because ketorolac can inhibit platelet function, concomitant use with anticoagulants (warfarin, heparin) may increase risk of bleeding complications.
Concomitant use with ACE inhibitors may increase the risk of renal impairment, especially in patients who are hypovolemic.
Concomitant use with diuretics may increase risk of developing renal failure and natriuretic effects may be reduced.
Seizures have been reported rarely with concomitant use of anticonvulsant drugs e.g. phenytoin, carbamazepine.
Hallucinations have been reported with concomitant use of psychoactive drugs e.g. fluoxetine, thiothixene, alprazolam.
Concomitant use with methotrexate has been reported to reduce the clearance of methotrexate and enhancing the toxicity of methotrexate.
Concomitant use with probenecid resulted in decreased clearance and increased plasma level to ketorolac.
NSAIDs appear to decrease renal lithium clearance leading to an increase in plasma lithium concentration, with associated symptoms of lithium toxicity (e.g. nausea, vomiting,neurological effects) have been reported.
Store below 30°C, protect from light.
MIMS Class
Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)
ATC Classification
M01AB15 - ketorolac ; Belongs to the class of acetic acid derivatives and related substances of non-steroidal antiinflammatory and antirheumatic products.
Xevolac inj 30 mg/mL
6 × 1's
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