Remopain

Each mL contains: Ketorolac trometamol 30 mg.

Pharmacology: Pharmacodynamics: Ketorolac trometamol is a non-steroidal anti-inflammatory drug (NSAID). It acts on cyclooxygenase route, inhibits prostaglandin 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, musculoskeletal pain, post minor or major operative, renal cholic & pain in cancer at adult or children. Ketorolac has analgesic efficacy equivalent to morphine or pethidine. 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.
Pharmacokinetics: 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 metabolized in the liver, and excreted renally. The metabolites do not have significant analgesic activity. The elimination terminal half-life of ketorolac (t¹/₂β) is ± 5 hours.
In geriatric patients, absorption of ketorolac and plasma protein binding is not affected substantially, but the plasma clearance is decreased (CL) (t¹/₂β= 6-7 hours). In patients with renal impairment the plasma clearance is decreased, it prolongs t¹/₂β (9-10 hours).
Patients with alcoholic cirrhosis show a little increase of t¹/₂β and T_max.

It is used in short-term management of moderate to severe post-operative pain.

Long-term treatment of ketorolac IV and IM should not exceed 5 days.
Hypovolemia should be corrected prior to the administration of ketorolac trometamol.
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 trometamol. 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 trometamol 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 post-operative pain. For those with severe pain, a 90 mg dose should be given. (See Table 1.)

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Patients with known hypersensitivity to ketorolac trometamol or in patients 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 contractions, 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.
Absolute contraindication: Not to be given to those patients who have history of: Stroke, cerebrovascular accident, CVA; Heart attack, myocardial infarction, MI; Coronary artery bypass graft, CABG; Congestive heart failure (CHF) NYHA II-IV.

Contraindication in patients with history of hypersensitivity to ASA or any other NSAIDs.
NSAIDs are contraindicated in patients with previous or active peptic ulceration.
Use with cautions in patients with cardiac, liver and renal disease.
Dose adjustments like using the lowest effective dose and monitoring of renal and liver functions should be instituted.
Should be used cautiously in patients receiving anticoagulant therapy and patients with hemophilia.
Hematological effects: ketorolac inhibits thrombocyte aggregation and prolongs bleeding time. Because of that ketorolac should not be used before surgery and use with caution if there are hemostasis disturbances.
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 trometamol is not recommended for children under 16 years (safety and efficacy have not been established).

Side effect incidence increases proportionally with increasing dose of ketorolac. Severe complications are caused by ketorolac therapy eg, ulcer, bleeding and gastrointestinal perforation, postoperative bleeding, acute renal failure, anaphylactic and anaphylactoid reactions and hepatic failure must be kept on guard. Complications of NSAIDs may be serious, especially if administration of ketorolac is not in the recommended dose.
The adverse reactions listed as follows are reported as probably related to ketorolac in clinical trials: Incidence >1%: Percentage incidence was reported in ≥3% patients: Body as a Whole: Edema (4%).
Cardiovascular: Hypertension.
Dermatologic: Pruritus, rash.
Gastrointestinal: Nausea (12%), dyspepsia (12%), gastrointestinal pain (13%), diarrhea (7%), constipation, flatulence, gastrointestinal fullness, vomiting and stomatitis.
Hematologic and Lymphatic: Purpura.
Central Nervous System: Cephalgia (17%), drowsiness (6%), dizziness (7%), swelling.
Pain on injection sites was reported by 2% of patients studied with multiple doses.
Incidence ≤1%: Body as a Whole: Increased weight, fever, infections, asthenia.
Cardiovascular: Palpitations, not for cardiovascular effects.
Dermatological: Urticaria.
Gastrointestinal: Gastritis, rectal bleeding, belch, anorexia, and/or increased appetite.
Hematologic and Lymphatic: Epistaxis, anemia, eosinophilia. Nervous System: Tremor, abnormal dreams, hallucinations, euphoria, extrapyramidal symptoms, vertigo, paresthesia, depression, insomnia, nervousness, excessive thirst, dry mouth, abnormal vision, difficulty to concentrate, hyperkinesis, stupor.
Respiratory: Dyspnea, lung edema, rhinitis, cough.
Sensory: Abnormal taste, abnormal or blurred vision, tinnitus, deafness. Urogenital: Hematuria, proteinuria, oliguria, urine retention, polyuria, increased urinary frequency.

Side effects 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 of NSAID may be serious, especially if administration of ketorolac is out of recommended dose. The adverse reactions listed below are reported as probably related to ketorolac in clinical trials.
Incidence >1%: Percentage incidence was reported in 3% or more patients.
Body as a whole: edema (4%).
Cardiovascular effect: hypertension.
Dermatologic: pruritus, rash.
Gastrointestinal: nausea (12%), dyspepsia (12%), gastrointestinal pain (13%), diarrhea (7%), constipation, flatulence, gastrointestinal fullness, vomiting and stomatitis.
Hematologic and lymphatic: purpura.
Central nervous system: cephalgia (17%), drowsiness (6%), dizziness (7%), swelling.
Pain on injection site was reported by 2% patients at study with multiple dose.
Incidence <1%: Body as a whole: increasing in weight, fever, infections, asthenia.
Cardiovascular: palpitations, not for cardiovascular effects.
Dermatologic: urticaria.
Gastrointestinal: gastritis, rectal bleeding, belch, anorexia and or increase in appetite.
Hematologic and lymphatic: epistaxis, anemia, and eosinophilia.
Nervous system: tremor, abnormal dream, hallucinations, euphoria, extrapyramidal symptoms, vertigo, paresthesia, depression, insomnia, nervousness, excessive thirst, dry mouth, abnormal thinking, difficult to concentrate, hyperkinesis, stupor.
Respiratory: dyspnea, lung edema, rhinitis, cough.
Five senses: abnormal taste, abnormal vision, blurred vision, tinnitus, deafness.
Urogenital: hematuria, proteinuria, oliguria, urine retention, polyuria, increased urinary frequency.

Should be used with caution in patients undergoing anticoagulant therapy and use must be strictly monitored. Combination of ketorolac trometamol and other NSAIDs is not recommended, because it would increase the risk of side effects. (See Table 2.)

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Store at temperatures not exceeding 30°C.

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)

M01AB15 - ketorolac ; Belongs to the class of acetic acid derivatives and related substances of non-steroidal antiinflammatory and antirheumatic products.

Rx