KETOROL 2% 30-50 g. GEL EXTERNAL APPROX

Active substances of Chlorolac
Country of Originindia Manufacturer Dr. Reddy's Laboratories Ltd
The form of the release gel for external use is 2% -30.0 g - a tube with instructions for use in a cardboard pack.

Keep away from children

Dosage form

Homogeneous transparent or translucent gel with a characteristic odor.

Composition

Each 1 g of gel contains:

Active substance: ketorolac trometamine (ketorolac trometamol) - 20 mg;

Excipients: propylene glycol 300 mg, dimethyl sulfoxide 150 mg, carbomer 974P 20 mg, methylparahydroxybenzoate sodium 1.8 mg, propylparahydroxybenzoate sodium 0.2 mg, trometamine (trometamol) 15 mg, purified water 390 mg, flavor "Dreamon Inde" (triethyl citrate 0.09%, castor seed oil 0.14%, isopropyl myristate 0.3 0%, diethyl phthalate 24.15%) 3 mg, ethanol 50 mg, glycerol 50 mg.

Pharmacotherapeutic group NSAIDs

Storage temperature from 2℃ to 25℃

Special conditions

The drug is recommended to be applied only to undamaged areas of the skin, avoiding contact with open wounds. Avoid contact with the gel in the eyes and other mucous membranes. Do not use the gel under airtight bandages. After applying the gel, wash your hands with soap. Close the tube tightly after using the gel.

Drug interaction

Pharmacokinetic interaction with drugs competing for binding to plasma proteins is not excluded.

Caution should be exercised when using ketorolac with digoxin, phenytoin, lithium preparations, diuretics, cyclosporine, methotrexate, other NSAIDs, hypotensive and antidiabetic agents. Before using the gel, you should consult your doctor if you are using these products or are under the supervision of a doctor.

Pharmacodynamics

Nonsteroidal anti-inflammatory drug (NSAID), has a pronounced analgesic and anti-inflammatory effect. The mechanism of action is associated with non-selective inhibition of the activity of cyclooxygenase (COX) - COX-1 and COX-2, which catalyzes the formation of prostaglandins from arachidonic acid, which play an important role in the pathogenesis of pain, inflammation and fever. Ketorolac is a racemic mixture of [-]S and [+]R enantiomers, while the analgesic effect is due to the [-]S form.
When applied topically, it causes the weakening or disappearance of pain at the place of application of the gel, including joint pain at rest and when moving, reduces morning stiffness and swelling of the joints. Helps to increase the volume of movements.

Pharmacokinetics

Suction

After oral administration, ketorolac is well absorbed from the gastrointestinal tract. Cmax in blood plasma is reached 40 minutes after taking the drug on an empty stomach at a dose of 10 mg and is 0.7-1.1 mcg / ml. Fat-rich foods reduce the Cmax of ketorolac in the blood and delay the time to reach Cmax by 1 hour.
Bioavailability - 80-100%.

After intravenous administration, ketorolac is rapidly and completely absorbed from the injection site into the systemic circulation. After intravenous administration of the drug at a dose of 30 mg Cmax in blood plasma is 1.74-3.1 mcg / ml, at a dose of 60 mg - 3.23-5.77 mcg / ml, the time to reach Cmax, respectively, is 15-73 minutes and 30-60 minutes.

Distribution

Binding to plasma proteins is 99%. With hypoalbuminemia, the amount of free substance in the blood increases.

The time to achieve Css with parenteral and oral administration is 24 hours with the appointment of the drug 4 (higher than subtherapeutic) and is at the intravenous administration of the drug at a dose of 15 mg - 0.65-1.13 mcg / ml, at a dose of 30 mg - 1.29-2.47 mcg / ml; after ingestion of the drug at a dose of 10 mg - 0.39-0.79 mcg / ml. Vd is 0.15-0.33 l/kg.

Penetrates into breast milk. When prescribing the drug at a dose of 10 mg, 4 Cmax in breast milk is reached 2 hours after taking the first dose and is 7.3 ng / ml, 2 hours after taking the second dose, Cmax is 7.9 ng / L.

Metabolism

More than 50% of the administered dose is metabolized in the liver to form pharmacologically inactive metabolites. The main metabolites are glucuronides and p-hydroxyketorolac.

Withdrawal

It is excreted by the kidneys (91%) and through the intestines (6%). Glucuronides are excreted in the urine.

T1 / 2 in patients with normal renal function averages 5.3 hours (3.5-9.2 hours after intravenous administration of the drug at a dose of 30 mg and 2.4-9 hours after oral administration at a dose of 10 mg).

The total clearance is at the intravenous administration of the drug at a dose of 30 mg - 0.023 l / kg / h, when taken orally at a dose of 10 mg - 0.025 l / kg / h.
Pharmacokinetics in special clinical cases

In patients with renal insufficiency, the Vd of ketorolac can increase by 2 times, and the Vd of the R-enantiomer by 20%.
T1/2 is lengthened in elderly patients and shortened in young patients. Liver function has no effect on T1/2. In patients with impaired renal function at a plasma creatinine concentration of 19-50 mg / l (168-442 mmol / L) T1 / 2 is 10.3-10.8 hours, with more severe renal insufficiency - more than 13.6 hours.
Total clearance in patients with renal insufficiency at a plasma creatinine concentration of 19-50 mg / l with intravenous administration of the drug at a dose of 30 mg - 0.015 l / kg / h (0.019 l / kg / h - in elderly patients), when ingested at a dose of 10 mg - 0.016 l / kg / h.
It is not excreted during hemodialysis.

Indications

Topical application for relief of pain syndrome:

• - for injuries (soft tissue contusion, soft tissue inflammation, including post-traumatic origin, ligament damage, bursitis, tendinitis, epicondylitis, synovitis);
• - for pain in muscles (myalgia) and joints (arthralgia), neuralgia, sciatica, rheumatic diseases.

It is intended for symptomatic therapy, reducing the intensity of pain and inflammation at the time of use, does not affect the progression of the disease.

Contraindications

• - Hypersensitivity to ketorolac or other components of the drug;
• - wet dermatoses, eczema, infected or open wounds (at the place of application of the gel);
• - a complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (indications in the anamnesis for bronchospasm, urticaria or rhinitis caused by taking acetylsalicylic acid);
• - pregnancy (III trimester);
• - the period of breastfeeding (lactation);
• - children under the age of 16.

With caution:

Exacerbation of hepatic porphyria, erosive and ulcerative lesions of the gastrointestinal tract, severe renal/ hepatic insufficiency, chronic heart failure, bronchial asthma, old age, pregnancy (I and II trimester).

Overdose

Cases of gel overdose are not described. In case of accidental ingestion of the gel, it is necessary to clear the stomach (by vomiting, taking activated charcoal) and consult a doctor. Further treatment, if necessary, is symptomatic.

Side effects

Local reactions: itching, urticaria, peeling.

If any adverse reactions occur, stop using the drug and consult a doctor.

When applying the gel to large areas of the skin, the development of systemic adverse reactions is not excluded: heartburn, nausea, vomiting, diarrhea, gastralgia, ulceration of the gastrointestinal mucosa, increased activity of "liver" transaminases; headache, dizziness; fluid retention, hematuria; allergic reactions (anaphylactic shock, skin rash); thrombocytopenia, leukopenia, anemia, agranulocytosis, lengthening of time bleeding.

Special storage conditions

At a temperature not exceeding 25 ° C. Do not freeze!