Brands of Ketorolac in Kenya
Dolac®, Cadila Pharmaceuticals (EA) Ltd
Rolac® , Renata Limited
MODE OF ACTION OF KETOROLAC TROMETHAMINE:
The mechanism of action of ketorolac, like that of other NSAIDs, is not completely understood but may be related to prostaglandin synthetase inhibition. The biological activity of ketorolac tromethamine is associated with the S-form.
Acute Pain in Adult Patients
Ketorolac tromethamine is indicated for the short-term (≤5 days) management of moderately severe acute pain that requires analgesia at the opioid level, usually in a postoperative setting. Therapy should always be initiated with IV or IM dosing of ketorolac tromethamine, and oral ketorolac tromethamine is to be used only as continuation treatment, if necessary.
Patients should be switched to alternative analgesics as soon as possible, but ketorolac tromethamine therapy is not to exceed 5 days
- Ketorolac tromethamine is contraindicated in patients with previously demonstrated hypersensitivity to ketorolac tromethamine.
- Ketorolac tromethamine is contraindicated in patients with active peptic ulcer disease, in patients with recent gastrointestinal bleeding or perforation and in patients with a history of peptic ulcer disease or gastrointestinal bleeding.
- Ketorolac tromethamine should not be given to patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs. Severe, rarely fatal, anaphylactic-like reactions to NSAIDs have been reported in such patients.
- Ketorolac tromethamine is contraindicated as prophylactic analgesic before any major surgery.
- Ketorolac tromethamine is contraindicated in the setting of coronary artery bypass graft (CABG) surgery.
- Ketorolac tromethamine is contraindicated in patients with advanced renal impairment or in patients at risk for renal failure due to volume depletion.
- Ketorolac tromethamine is contraindicated in labor and delivery because, through its prostaglandin synthesis inhibitory effect, it may adversely affect fetal circulation and inhibit uterine musculature, thus increasing the risk of uterine hemorrhage.
- Ketorolac tromethamine inhibits platelet function and is, therefore, contraindicated in patients with suspected or confirmed cerebrovascular bleeding, hemorrhagic diathesis, incomplete hemostasis and those at high risk of bleeding.
- Ketorolac tromethamine is contraindicated in patients currently receiving aspirin or NSAIDs because of the cumulative risks of inducing serious NSAID-related adverse events.
- The concomitant use of ketorolac tromethamine and probenecid is contraindicated.
- The concomitant use of ketorolac tromethamine and pentoxifylline is contraindicated.
- Ketorolac tromethamine is contraindicated for neuraxial (epidural or intrathecal) administration due to its alcohol content.
Warfarin, Digoxin, Salicylate, and Heparin
The effects of warfarin and NSAIDs, in general, on GI bleeding are synergistic, such that the users of both drugs together have a risk of serious GI bleeding higher than the users of either drug alone.
When ketorolac tromethamine is administered with aspirin, its protein binding is reduced, although the clearance of free ketorolac tromethamine is not altered. The clinical significance of this interaction is not known; however, as with other NSAIDs, concomitant administration of ketorolac tromethamine and aspirin is not generally recommended because of the potential of increased adverse effects.
Clinical studies, as well as postmarketing observations, have shown that ketorolac tromethamine can reduce the natriuretic effect of furosemide and thiazides in some patients. This response has been attributed to inhibition of renal prostaglandin synthesis. During concomitant therapy with NSAIDs, the patient should be observed closely for signs of renal failure .
Concomitant administration of oral ketorolac tromethamine and probenecid resulted in decreased clearance and volume of distribution of ketorolac and significant increases in ketorolac plasma levels (total AUC increased approximately threefold from 5.4 to 17.8 mcg/h/mL) and terminal half-life increased approximately twofold from 6.6 to 15.1 hours. Therefore, concomitant use of ketorolac tromethamine and probenecid is contraindicated.
NSAIDs have produced an elevation of plasma lithium levels and a reduction in renal lithium clearance. The mean minimum lithium concentration increased 15% and the renal clearance was decreased by approximately 20%. These effects have been attributed to inhibition of renal prostaglandin synthesis by the NSAID. Thus, when NSAIDs and lithium are administered concurrently, subjects should be observed carefully for signs of lithium toxicity.
NSAIDs have been reported to competitively inhibit methotrexate accumulation in rabbit kidney slices. This may indicate that they could enhance the toxicity of methotrexate. Caution should be used when NSAIDs are administered concomitantly with methotrexate.
ACE Inhibitors/Angiotensin II Receptor Antagonists
Concomitant use of ACE inhibitors and/or angiotensin II receptor antagonists may increase the risk of renal impairment, particularly in volume-depleted patients.
Reports suggest that NSAIDs may diminish the antihypertensive effect of ACE inhibitors and/or angiotensin II receptor antagonists. This interaction should be given consideration in patients taking NSAIDs concomitantly with ACE inhibitors and/or angiotensin II receptor antagonists.
Sporadic cases of seizures have been reported during concomitant use of ketorolac tromethamine and antiepileptic drugs (phenytoin, carbamazepine).
Hallucinations have been reported when ketorolac tromethamine was used in patients taking psychoactive drugs (fluoxetine, thiothixene, alprazolam).
When ketorolac tromethamine is administered concurrently with pentoxifylline, there is an increased tendency to bleeding.
Nondepolarizing Muscle Relaxants
In postmarketing experience there have been reports of a possible interaction between ketorolac tromethamine IV/IM and nondepolarizing muscle relaxants that resulted in apnea. The concurrent use of ketorolac tromethamine with muscle relaxants has not been formally studied.
Selective Serotonin Reuptake Inhibitors (SSRIs)
There is an increased risk of gastrointestinal bleeding when selective serotonin reuptake inhibitors (SSRIs) are combined with NSAIDs. Caution should be used when NSAIDs are administered concomitantly with SSRIs.
ADVERSE DRUG REACTIONS:
Body as a Whole: fever, infections, sepsis
Cardiovascular: congestive heart failure, palpitation, pallor, tachycardia, syncope
Dermatologic: alopecia, photosensitivity, urticaria
Gastrointestinal: anorexia, dry mouth, eructation, esophagitis, excessive thirst, gastritis, glossitis, hematemesis, hepatitis, increased appetite, jaundice, melena, rectal bleeding
Hemic and Lymphatic: ecchymosis, eosinophilia, epistaxis, leukopenia, thrombocytopenia
Metabolic and Nutritional: weight change
Nervous System: abnormal dreams, abnormal thinking, anxiety, asthenia, confusion, depression, euphoria, extrapyramidal symptoms, hallucinations, hyperkinesis, inability to concentrate, insomnia, nervousness, paresthesia, somnolence, stupor, tremors, vertigo, malaise
Reproductive, female: infertility
Respiratory: asthma, cough, dyspnea, pulmonary edema, rhinitis
Special Senses: abnormal taste, abnormal vision, blurred vision, hearing loss
Urogenital: cystitis, dysuria, hematuria, increased urinary frequency, interstitial nephritis, oliguria/polyuria, proteinuria, renal failure, urinary retention.
Reporting of suspected adverse reactions
The PPB Department of Pharmacovigilance was set up with a vision to develop, implement and continuously upgrade an appropriate system for detecting, reporting and monitoring adverse drug reactions (ADRs) and other relevant problems with medicines in Kenya. The department strives to ensure the safety and efficacy of pharmaceutical products in Kenya.
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals/ Patients are encouraged to report any suspected adverse reactions via Pharmacovigilance Yellow Form, firstname.lastname@example.org or clicking below button:
Ketorolac in Kenya
Ketorolac in Kenya
Clinical | Pharmacokinetic data
Pregnancy Category: C
Routes of Administration: By mouth, under the tongue, IM, IV, eye drops
Bioavailability: 100% (All routes)
Protein Binding: Greater than 99%
Onset of Action: Not Available
Elimination Half life: 3.5 h to 9.2 h, young adults | 4.7 h to 8.6 h, elderly (mean age 72)
Excretion: Kidney: 91.4% (mean) Biliary: 6.1% (mean)
Legal Status | Dosage forms & Strengths
Prescription only Medicine (POM) , ℞-only
Narcotic Drugs and Psychotropic Substances (Control ) Act Schedule:
This drug is not a controlled substance under Narcotic Drugs and Psychotropic Substances (Control ) Act
Dosage Forms | Strengths:
Tablets | Injectable | Opthalmic formulation
|CompTox Dashboard (EPA)|
- PPB Retention Register
- O’Hara, Dorene A., et al. “Ketorolac tromethamine as compared with morphine sulfate for treatment of postoperative pain.” Clinical Pharmacology & Therapeutics 41.5 (1987): 556-561.
- Brocks, Dion R., and Fakhreddin Jamali. “Clinical pharmacokinetics of ketorolac tromethamine.” Clinical pharmacokinetics 23.6 (1992): 415-427.
- Maloney, P. J., et al. “The analgesic and anti-inflammatory profile of ketorolac and its tromethamine salt.” Drugs under experimental and clinical research 11.8 (1985): 479-492.
- Jung, D., E. Mroszczak, and L. Bynum. “Pharmacokinetics of ketorolac tromethamine in humans after intravenous, intramuscular and oral administration.” European journal of clinical pharmacology 35.4 (1988): 423-425.