QUPEN FORTE 

INSTRUCTIONS FOR USE

CUPIN FORTE

QUPEN FORTE

Trade name of the drug : Kupin Forte

Active ingredient (INN) : ketorolac

Dosage form : solution for injection

Compound

1 ml of solution for injection contains:

active substance: ketorolac tromethamine – 30 mg.

excipients : monosubstituted potassium phosphate, dibasic sodium phosphate, sodium edetate, sodium hydroxide, propylene glycol, water for injection.

Description : colorless or slightly yellow solution.

Pharmacotherapeutic group : non-steroidal anti-inflammatory drug.

ATX code: M01AV15

Pharmacological properties

Ketorolac is a non-steroidal anti-inflammatory drug, a derivative of pyrrolysine-carboxylic acid. It has a pronounced analgesic effect, and also has anti-inflammatory and moderate antipyretic effects. The mechanism of action is associated with inhibition of the activity of COX, the main enzyme in the metabolism of arachidonic acid, which is a precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever.

Pharmacokinetics

Bioavailability with intravenous and intramuscular administration is 100%. After intramuscular and intravenous administration, it is quickly and completely absorbed. Cmax _is achieved 50 minutes after a single intramuscular injection of 30 mg and is 2.2-3.0 μg/ml. With an intravenous infusion of 10 mg, the highest plasma content (2.4 μg/ml) is determined after 5.4 minutes. Time T _1/2 is 4-6 hours.

The binding of ketorolac to plasma proteins is 99.2%. The degree of binding does not depend on the concentration in the vascular bed. Metabolized in the liver to form conjugated and hydroxylated forms. The main metabolite, hydroxyketorolac, is pharmacologically inactive. Eliminated primarily by the kidneys. In patients with impaired renal function, excretion slows down. Its rate decreases in proportion to the degree of renal dysfunction, with the exception of patients with severe renal failure (plasma clearance is slightly higher than expected for a given degree of renal damage). 92% of the administered dose is found in urine, 6% in feces. With repeated administration, the clearance of ketorolac does not change.

There are reports of the effectiveness of ketorolac tromethamine in migraine attacks.

Indications for use

Indicated for short-term use to relieve moderate to severe pain, such as:

• postoperative pain: after abdominal, gynecological, surgical, orthopedic operations, etc.;
• acute pain syndromes of musculoskeletal origin: acute sprains, dislocations, fractures and soft tissue injuries;
• toothache, including after dental interventions;
• postpartum pain (ketorolac is not indicated during childbirth);
• for short-term pain relief during exacerbations of pain in conditions such as cancer pain, sciatica, fibromyalgia, non-articular pain syndromes in chronic pathology of soft tissues, osteoarthritis and as an adjuvant for renal and hepatic colic.

Directions for use and doses

Injections. Typically, a dose of 10 mg is recommended as an initial dose; 15 to 30 mg IM every 4-6 hours may be prescribed. When administered intravenously, the dose of the drug should be administered over at least 15 seconds. For patients weighing up to 50 kg and the elderly (after 65 years), lower doses are used. Shortening the administration intervals (for example, every 2 hours) is possible, but the daily dose should not exceed 120 mg. With combined parenteral and enteral administration, the daily dose should also not exceed 120 mg. When treating acute severe pain (postoperative period, traumatic and burn shock, etc.), an initial dose of Ketorolac of 10 — 30 mg is administered intravenously, then it is repeated after 10-15 minutes. The next dose of 10 mg is administered intravenously at least 30 minutes later, if necessary. Long-term daily treatment with ketorolac should not exceed 5 days for intramuscular and intravenous administration. After 5 days, the patient can be transferred to the tablet form of Ketorolac. Periodic or single appointment Ketorolac can be used for a long time. Narcotic analgesics can be used in parallel for pain relief, anxiolytic and/or sedative effects. Ketorolac is a peripheral analgesic, so it does not increase respiratory depression and the sedative effects of drugs. When ketorolac is administered together with narcotic analgesics, the daily dose of the latter is significantly reduced.

Children

The recommended dose for children for intramuscular and intravenous administration is 0.5 mg/kg. Possible bolus administration at the rate of 1.0 mg/kg every 6 hours or intravenous infusion of 0.17 mg/kg/hour. The maximum daily dosage is 90 mg, and the maximum duration of treatment is 48 hours. Ketorolac is not recommended for use in children under 1 year of age.

Side effects

From the cardiovascular system : rarely — bradycardia, changes in blood pressure, palpitations, fainting.

From the digestive system : possible nausea, abdominal pain, diarrhea; rarely — constipation, flatulence, feeling of gastrointestinal fullness, vomiting, dry mouth, thirst, stomatitis, gastritis, erosive and ulcerative lesions of the gastrointestinal tract, liver dysfunction.

From the central nervous system and peripheral nervous system : possible anxiety, headache, drowsiness; rarely — paresthesia, depression, euphoria, sleep disturbances, dizziness, changes in taste, visual disturbances, motor disorders.

From the respiratory system : rarely — breathing problems, attacks of suffocation.

From the urinary system : rarely — increased frequency of urination, oliguria, polyuria, proteinuria, hematuria, azotemia, acute renal failure.

From the blood coagulation system : rarely — nosebleeds, anemia, eosinophilia, thrombocytopenia, bleeding from postoperative wounds.

Metabolism : possible increased sweating, swelling; rarely — oliguria, increased levels of creatinine and/or urea in the blood plasma, hypokalemia, hyponatremia.

Allergic reactions : possible skin itching, hemorrhagic rash; in isolated cases — exfoliative dermatitis, urticaria, Lyell’s syndrome, Stevens-Johnson syndrome, anaphylactic shock, bronchospasm, Quincke’s edema, myalgia.

Other : possible fever.

Local reactions : pain at the injection site.

Contraindications

Erosive and ulcerative lesions of the gastrointestinal tract in the acute phase, “aspirin” asthma, severe renal dysfunction (plasma creatinine concentration above 5.0 mg/dl), pregnancy, lactation, early postpartum period, hypersensitivity to ketorolac, aspirin and other non-steroidal anti-inflammatory drugs drugs.

Drug interactions

When ketorolac is used concomitantly with other NSAIDs, additive side effects may develop; with pentoxifylline, anticoagulants (warfarin, heparin in low doses) — the risk of bleeding may increase; with ACE inhibitors — there may be an increased risk of developing renal dysfunction; with probenecid — the plasma concentration of ketorolac and its half-life increase; with lithium preparations — a decrease in the renal clearance of lithium and an increase in its concentration in plasma is possible; with furosemide — reducing its diuretic effect. When using ketoralac, the need for the use of opioid analgesics for pain relief is reduced.

special instructions

Use with caution in patients with impaired liver and kidney function, chronic heart failure, arterial hypertension, in patients with erosive and ulcerative lesions of the gastrointestinal tract and a history of bleeding from the gastrointestinal tract. Ketorolac is not recommended for use as a premedication, maintenance of anesthesia, or for pain relief in obstetric practice.

Ketorolac should be used with caution in the postoperative period in cases where particularly careful hemostasis is required (including after resection of the prostate gland, tonsillectomy, in cosmetic surgery), as well as in elderly patients, because The half-life of ketorolac is prolonged and plasma clearance may be reduced. In this category of patients, it is recommended to use ketorolac in doses close to the lower limit of the therapeutic range. If symptoms of liver damage, skin rash, or eosinophilia appear, ketorolac should be discontinued.

Impact on the ability to drive a car and operate complex machinery

If drowsiness, dizziness, insomnia or depression appear during treatment with ketorolac, special care must be taken when engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions.

The drug should be stored out of the reach of children and not used after the expiration date.

Overdose

Symptoms (with a single dose) : abdominal pain, nausea, vomiting, hyperventilation, peptic ulcers and/or erosive gastritis, impaired renal function.

Release form

1 ml in dark glass ampoules. 5 or 10 ampoules along with instructions for use are placed in cardboard boxes.

Storage conditions

Store in a dry, dark place, at a temperature of 15-25°C.

Best before date

3 years.

Conditions for dispensing from pharmacies

On prescription.

Made in India

“Avison Pharmaceuticals Pvt. Ltd.”, India

Adore Pharmaceuticals Pvt. Ltd.”, India,

(705472) 516 Khokani Ind Complex No. 2

NR, Saibaba Temple, Sativali Vasai (E) – 401208