Each ampoule (1 mL) contains : Ketorolac tromethamine 10 mgEach ampoule (1 mL) contains : Ketorolac tromethamine 30 mg
Ketorolac tromethamine is a nonsteroidal anti-inflammatory drug (NSAID). It acts on cyclooxigenase route, inhibits prostaglandins synthesis and may be considered a strong analgesic, both peripherally and centrally, besides having anti-inflammatory and antipyretic effects. Ketorolac reduce the mild to severe pain at emergency cases, musculosceletal pain, post minor or major operative, renal cholic & pain in cancer at adults or children. Ketorolac has analgesic efficacy equivalent to morphine or pethidin. Initial analgesic effects of ketorolac may be slower, but the duration longer than opioid. Combination therapy of ketorolac and opioid may reduce 25-50% of opioid needs. And for some patients, this case is accompanied by decreasing side effects which is induced by opioid, faster normalization of gastrointestinal tract function and shorter hospital stay.
Bioavailability has been reported to range from 80-100% following oral administration. T max occurs within 30-60 minutes after oral or parenteral administration. Food decreases the absorption rate, but not the extent of oral absorption. 99% of the ketorolac in plasma is protein-bound, volume distribution (Vd) < 0.3 L/kg. Ketorolac is metabolised in liver, and excreted through renal. The metabolites doesn't have significant analgesic activity. The elimination terminal half-life of ketorolac (t �b) is � 5 hours In geriatric patients, absorption of ketorolac and plasma protein bound does not affect substantially, but the plasma clearance is decreased (CL) (t �b= 6-7 hours).In patients with renal impairment the plasma clearance is decreased, it prolongs t�b (9-10 hours).Patients with alcoholic cirrhosis shows a little increase of t�b and T max.
Ketorolac is indicated for the short-term (≤ 5 days) management of moderate and severe acute pain that requires analgesia at the opioid level.
Patients with known hypersensitivity to Ketorolac tromethamine or in patients in whom aspirin or other NSAIDS induce serious allergic manifestations.Patients with acute peptic ulcer, patients with recent gastrointestinal bleeding or perforation and in patients with a history of peptic ulcer disease or gastrointestinal bleeding.Patients with severe renal impairment or patients at high risk of renal failure.In labor and delivery, it may adversely affect fetal circulation and inhibit uterine contraindications, thus increasing the risk of uterine hemorrhage.Nursing mother because of the potential adverse effects of prostaglandin inhibiting drugs on neonates.Hemostasis disorders.Patients with suspected or confirmed cerebrovascular bleeding, hemorrhagic diathesis, incomplete hemostasis and those at high risk of bleeding.Patients in concomitant use of other NSAIDs and probenecid. Ketorolac is contraindicated for neuraxial (epidural or intrathecal) administration.
DOSAGE and ADMINISTRATION
Longterm treatment of ketorolac IV and IM should not exceed 5 days.Hypovolemia should be corrected prior to the administration of ketorolac tromethamine.The IV bolus must be given over no less than 15 seconds.The IM administration should be given deeply and slowly into the muscle.The analgesic effect begins in 30 minutes with maximum effect occurring in 1-2 hours after dosing IV or IM. The duration of analgesic effect is usually 4-6 hours.For breakthrough pain, do not increase the dose or the frequency of ketorolac tromethamine. Consideration should be given to supplementing these regiments with low doses of opioids unless otherwise contraindicated.For the short-term management of pain, an initial IM ketorolac tromethamine loading dose is recommended of 30 mg or 60 mg, and if necessary therapy is then continued with 15 mg or 30 mg administered every 6 hours. The maximum daily dose is 120 mg, but if needed, the dose can be increased up to 150 mg in the first day of treatment. A 30 mg (IM) dose is optimal dose for relieving moderate postoperative pain. For those with severe pain, a 90 mg dose should be given.
WARNINGS and PRECAUTIONS
Should be used cautiously in patients receiving anticoagulant therapy and patients with hemophilia.
Haematological effects : Ketorolac inhibits thrombocyte aggregation and prolong bleeding time. Because of that ketorolac should not be used before surgery and use with caution if there is hemostasis disturbances.
Should be used with caution in patients with cardiac decompensation, acute renal failure, hypertension or other conditions associated with fluid retention.
Ketorolac tromethamine should be used with caution in patients with impaired hepatic function or patients with history of hepatic desease.
Hepatic effects : Ketorolac therapy increases hepatic enzymes and in hepatic disease patients, severe hepatic risk reaction may occur. Administration of ketorolac should be discontinued if abnormality of hepatic function test occurs after ketorolac administration.
Ketorolac tromethamine is not recommended for children under 16 years (Safety and efficacy have not been established).
:: SIDE EFFECTS ::
Side effect incidence increases proportionally with increasing dose of ketorolac. Severe complications are caused by ketorolac therapy like ulcer, bleeding and gastrointestinal perforation, post operative bleeding, acute renal failure, anaphylactic and anaphylactoid reactions and hepatic failure must be keep on guard. Complications NSAID may be serious, especially if administration of ketorolac out of recommended dose.The adverse reactions listed below are reported as probably related to ketorolac in clinical trials.
INCIDENCE > 1%
Percentage incidence were reported in 3% or more patients.
Body as a whole : Edema (4%)
Cardiovascular effects: Hypertension
Dermatologic : pruritus, rash
Gastrointestinal : Nausea (12%), dyspepsia (12%), gastrointestinal pain (13%), diarrhoea (7%), constipation, flatulence, gastrointestinal fullness, vomiting, stomatitis.
Hemic and lymphatic : purpura
Central Nervous system : Cephalgia (17%), drowsiness (6%), dizziness(7%), swelling.
Pain on injection site were reported by 2% patients at study with multiple doses.
:: INCIDENCE ≤ 1% ::
Body as a whole: Increasing in weight, fever, infections, asthenia.
Cardiovascular : Palpitations, pale, syncope.
Dermatologic : Urticaria.
Gastrointestinal : Gastritis, rectal bleeding, belch, anorexia, appetite increasing.
Hemic and lymphatic : Epistaxis, anemia, eosinophilia.
Nervous system : Tremor, abnormal dream, hallucinations, euphoria, extrapyramidal symptoms, vertigo, paresthesia, depression, insomnia, nervousness, excessive thirst, dry mouth, abnormal vision, difficult to concentrate, hyperkinesis, stupor.
Respiratory : Dyspnea, lung oedema, rhinitis, cough.
Five senses : abnormal taste, abnormal vision, blurred vision, tinnitus, deaf.
Urogenital : Hematuria, proteinuria, oliguria, urine retention, polyuria, increased urinary frequency.
There are no significant interactions between ketorolac and warfarin or heparin. Should be used with cautiously and strictly monitored if administration of ketorolac for patients with anticoagulant therapy.Combination of ketorolac tromethamine and other NSAIDs is not recommended, because it would increase side effects potency.
PRESENTATION and REGISTRATION NUMBER
Remopain injection : Box, 5 ampoules 10 mg/mL @ 1 mL; Reg.No. DKL0305032943A1Remopain injection : Box, 5 ampoules 30 mg/mL @ 1 mL; Reg.No. DKL0305032943B1
ON MEDICAL PRESCRIPTION ONLY
STORE AT ROOM TEMPERATURE (25-30) Degree C, PROTECT FROM LIGHT