Ketorolac
Mechanism :
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 anti-inflammatory 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.
Indication :
Contraindications :
Hypersensitivity to drug/class/component
ASA or NSAID-induced asthma or urticaria, Aspirin triad, GI bleeding or PUD history, Cerebrovascular hemorrhage, Coagulation disorder, Active bleeding, CABG surgery periop use, Major surgery preop use, Epidural or intrathecal use, Renal impairment severe, Volume depletion.
Caution in elderly or debilitated patients, inflammatory bowel disease, coagulation disorder, alcohol use or smoker, asthma, hepatic impairment, mild-moderate renal impairment, CHF or HTN, cardiovascular disease or cardiac disease risk.
Dosing :
Under 2 years: Safety and efficacy not established.
IV/IM
2-16 years:
0.5 mg/kg IM/IV every 6 hourly for 5 days. Max: 15 mg/day.
>16 years but <50 kg:
15 mg IV/IM every 6 hourly. Max: 60 mg/day.
>16 years and >50 kg:
30 mg IV/IM every 6 hourly. Max: 120 mg/day.
Oral:In children >16 years
>50 kg or more:
20 mg orally once followed by 10 mg every 4 to 6 hours. Maximum dose: 40 mg/day.
<50 kg:
10 mg orally once followed by 10 mg every 4 to 6 hours. Maximum dose: 40 mg/day.
Adverse Effect :
Common Reactions: dyspepsia, headache, nausea, abdominal pain, somnolence, diarrhea, rash, dizziness, constipation, tinnitus, edema, ALT and AST elevated, fluid retention, injection site pain, hypertension, pruritus, flatulence, diaphoresis, ecchymosis, photosensitivity.
Serious reaction: GI bleeding, GI perforation/ulcer, ulcerative stomatitis, bleeding, congestive heart failure, hypertension, stroke, myocardial infarction, Stevens-Johnson syndrome, anaphylactoid reaction, nephrotoxicity, renal papillary necrosis, hepatotoxicity, thromboembolism, bronchospasm, exfoliative dermatitis, blood dyscrasias, toxic epidermal necrolysis, anemia, inflammatory bowel disease exacerbation.
Interaction :
Contraindicated:
Aspirin, celecoxib, cidofovir, pentoxifylline, probenecid.
Avoid/Use Alternative:
Acebutolol, Atenolol, Betaxolol, Bisoprolol, Carvedilol, Dalteparin, Danshen, Diclofenac, Diclofenac Topical, Diflunisal, Drotrecogin Alfa, Enoxaparin, Esmolol, Ethanol, Etodolac, Fenoprofen, Flurbiprofen, Fondaparinux, Heparin, Ibritumomab Tiuxetan, Ibuprofen, Ibuprofen Lysine, Indomethacin, Ketoprofen, Ketorolac, Labetalol, Meclofenamate, Mefenamic Acid, Meloxicam, Methotrexate, Metoprolol, Mycophenolate Mofetil, Mycophenolic Acid, Nabumetone, Nadolol, Naproxen, Nebivolol, Omacetaxine Mepesuccinate, Oxaprozin, Pemetrexed, Penbutolol, Pentosan Polysulfate Sodium, Pindolol, Piroxicam, Propranolol, Sirolimus, Sulindac, Tacrolimus, Timolol, Tinzaparin, Tolmetin, Tositumomab, Warfarin.
Monitor/Modify Treatment:
Adefovir Dipivoxil, Aliskiren, Amiloride, Azilsartan Medoxomil, Benazepril, Canagliflozin, Candesartan Cilexetil, Captopril, Carbamazepine, Chamomile-German, Citalopram, Cyclosporine, Dapagliflozin, Desmopressin, Desvenlafaxine, Drospirenone (Hormone Replacement), Duloxetine, Enalapril, Enalaprilat, Eplerenone, Eprosartan, Escitalopram, Exenatide, Fluoxetine, Fluvoxamine, Fosinopril, Hydralazine, Ibrutinib, Irbesartan, Levomilnacipran, Liraglutide, Lisinopril, Lithium, Losartan, Magnesium Citrate, Milnacipran, Moexipril, Olmesartan Medoxomil, Pamidronate, Paroxetine, Perindopril, Polyethylene Glycol/Electrolytes, Quinapril, Ramipril, Red Clover, Sertraline, Sodium Phosphate (Bowel Prep), Sodium Phosphate Rectal, Spironolactone, Sulfate Bowel Prep, Telavancin, Telmisartan, Trandolapril, Trazodone, Triamterene, Valsartan, Venlafaxine, Vilazodone, Vortioxetine, Zoledronic Acid.
Caution Advised:
Abciximab, Aldesleukin, Alendronate, Alteplase, Anagrelide, Antithrombin, Apixaban, Argatroban, Bendroflumethiazide, Betamethasone, Black Cohosh, Bromfenac Ophthalmic, Budesonide, Bumetanide, Capsicum, Chlorothiazide, Chlorthalidone, Chondroitin, Cilostazol, Ciprofloxacin, Clopidogrel, Collagenase Clostridium Histolyticum, Cortisone, Creatine, Dabigatran Etexilate, Darunavir, Dasatinib, Deferasirox, Desirudin, Dexamethasone, Diclofenac Ophthalmic, Dipyridamole, Donepezil, Dong Quai, Eptifibatide, Erlotinib, Ethacrynic Acid, Etidronate, Evening Primrose Oil, Fenugreek, Feverfew, Fish Oils, Flaxseed, Flurbiprofen Ophthalmic, Furosemide, Galantamine, Garlic, Gemifloxacin, Ginger, Ginkgo, Ginseng, Asian, Ginseng, Siberian, Glucosamine, Green Tea, Horse Chestnut Seed, Hydrochlorothiazide, Hydrocortisone, Ibandronate, Icosapent Ethyl, Iloprost Inhaled, Indapamide, Kava, Ketorolac Ophthalmic, Lepirudin, Levofloxacin, Licorice, Methyclothiazide, Methylprednisolone, Metolazone, Moxifloxacin, Neostigmine, Nepafenac Ophthalmic, Norfloxacin, Ofloxacin, Omega-3-Acid, Porfimer, Pralatrexate, Prasugrel, Prednisolone, Prednisone, Pyridostigmine, Reteplase, Risedronate, Rivaroxaban, Rivastigmine, Sibutramine, Tacrine, Tenecteplase, Ticagrelor, Ticlopidine, Tiludronate, Tipranavir, Tirofiban, Torsemide, Treprostinil, Treprostinil Inhaled, Triamcinolone, Valproic Acid, Willow Bark.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
20-50 | Maximum 60 mg daily |
10-20 | Avoid if possible. Use small doses and monitor closely |
<10 | Avoid if possible. Use small doses and monitor closely |
Dose in Patients undergoing Renal Replacement Therapies
CAPD | Unlikely to be dialysed. Dose as in GFR<10 mL/min |
HD | Unlikely to be dialysed. Dose as in GFR<10 mL/min |
HDF/High flux | Unknown dialysability. Dose as in GFR<10 mL/min |
CAV/VVHD | Unknown dialysability. Dose as in GFR=10–20 mL/min |
Hepatic Dose :
No dose adjustments are recommended.