Ketofril - Instructions For Use, Tablets, Reviews, Price, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Ketofril

Ketofril: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Pharmacokinetics
4. 4. Indications for use
5. 5. Contraindications
6. 6. Method of application and dosage
7. 7. Side effects
8. 8. Overdose
9. 9. Special instructions
10. 10. Application during pregnancy and lactation
11. 11. Use in childhood
12. 12. In case of impaired renal function
13. 13. For violations of liver function
14. 14. Use in the elderly
15. 15. Drug interactions
16. 16. Analogs
17. 17. Terms and conditions of storage
18. 18. Terms of dispensing from pharmacies
19. 19. Reviews
20. 20. Price in pharmacies

Latin name: Ketofreel

ATX code: M01AB15

Active ingredient: ketorolac (Ketorolac)

Manufacturer: Torrent Pharmaceuticals, Ltd. (Torrent Pharmaceuticals, Ltd.) (India)

Description and photo updated: 30.11.2018

Prices in pharmacies: from 83 rubles.

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Ketofril is a non-steroidal anti-inflammatory drug with a pronounced analgesic effect.

Release form and composition

Dosage forms of Ketofril:

• film-coated tablets: round, biconvex, white or almost white (in a cardboard box 1 or 2 strips of 10 tablets);
• solution for intravenous and intramuscular administration: transparent, from pale yellow to colorless (in a cardboard box 1 or 2 blisters containing 5 ampoules of 1 ml).

Each pack also contains instructions for the use of Ketofril.

Composition of 1 tablet:

• active substance: ketorolac trometamol (ketorolac tromethamine) - 10 mg;
• auxiliary components (core): colloidal silicon dioxide, MCC (microcrystalline cellulose), anhydrous lactose, sodium carboxymethyl starch, magnesium stearate;
• shell: colloidal silicon dioxide macrogol, titanium dioxide, hypromellose, talc.

Composition of 1 ml solution:

• active substance: ketorolac trometamol (ketorolac tromethamine) - 30 mg;
• auxiliary components: ethanol, sodium chloride, sodium hydroxide, edetate disodium, water for injection.

Pharmacological properties

Pharmacodynamics

Ketorolac tromethamine - the active substance of Ketofril, has a pronounced analgesic property, also has a moderate antipyretic and anti-inflammatory effect.

The mechanism of its effect is associated with non-selective inhibition of the activity of the enzyme COX-1 and -2 (cyclooxygenase 1 and 2), mainly in peripheral tissues, resulting in inhibition of the biosynthesis of prostaglandins, which are modulators of thermoregulation, pain sensitivity and inflammation. The substance is a racemic mixture of [-] S and [+] R enantiomers, the analgesic effect is due to the [-] S form.

Ketorolac does not affect opioid receptors, does not depress respiration, does not cause drug dependence, does not have a sedative and anxiolytic effect.

In terms of the severity of the analgesic effect, Ketofril is significantly superior to other non-steroidal anti-inflammatory drugs, its effect is comparable to that of morphine.

After oral administration and intramuscular administration, the analgesic effect develops in 30 and 60 minutes, respectively, the maximum effect is achieved in 60-120 minutes.

Pharmacokinetics

Film-coated tablets

When taken orally, ketorolac is well absorbed in the gastrointestinal tract, _Cmax (maximum concentration) in blood plasma is 0.7–1.1 μg / ml, the time to reach this value after taking 10 mg of ketorolac on an empty stomach is 40 minutes. When taken simultaneously with food rich in fats, C _max in the blood decreases, and the time to reach it also slows down by 60 minutes.

99% of the substance binds to plasma proteins; against the background of hypoalbuminemia, an increase in the amount of free substance in the blood is noted.

The biological availability of ketorolac is from 80 to 100%. When administered orally 4 times a day (above the subtherapeutic dose), the time to reach C _ss (equilibrium concentration) is 24 hours. After taking 10 mg of the substance, the C _ss indicator varies in the range from 0.39 to 0.79 μg / ml.

Ketorolac penetrates into breast milk: C _max in milk when taken by the mother at a dose of 10 mg is achieved 2 hours after a single dose and is 7.3 ng / ml, after repeated administration of ketorolac (when using Ketofril 4 times a day) C _max through 2 hours is 7.9 ng / ml.

Solution for intravenous and intramuscular administration

The biological availability of ketorolac is from 80 to 100%. When administered intramuscularly, the absorption of the substance is complete and fast. With _max and the time to reach it with intramuscular injection is (depending on the dose): 30 mg - 1.74-3.1 μg / ml and 15-73 minutes; 60 mg - 3.23-5.77 mcg / ml and 30-60 minutes. With _max with intravenous infusion: 15 mg - 1.96-2.98 mcg / ml; 30 mg - 3.69-5.61 μg / ml.

With parenteral administration 4 times a day (above the subtherapeutic dose), the time to reach C _ss is 24 hours. The value of this indicator (intramuscular / intravenous injection) is: 15 mg - 0.65-1.13 / 0.79-1.39 μg / ml; 30 mg - 1.29-2.47 / 1.68-2.76 mcg / ml.

The total clearance with intramuscular injection of 30 mg of ketorolac is 0.023 l / kg / h; in elderly patients - 0.019 l / kg / h; with renal failure in patients with a plasma concentration of creatinine in the blood from 19 to 50 mg / l - 0.015 l / kg / h. The total clearance for intravenous infusion is 0.03 l / kg / h.

Both dosage forms

50% of the administered dose is metabolized in the liver, with the formation of pharmacologically inactive metabolites, the main of which are glucuronides and p-hydroxyketorolac. Excretion is carried out: by the kidneys - by 91%, through the intestines - 6%.

In patients with no impaired renal function, T _1/2 (half-life) averages 5.3 hours. In elderly patients, the value of this indicator increases, in young patients it decreases. The liver function has no effect on T _1/2. In case of impaired renal function with a plasma concentration of creatinine in the blood of 19-50 mg / l (168-442 μmol / l), the T _1/2 value is in the range from 10.3 to 10.8 hours, if patients have more pronounced renal failure - more than 13.6 hours.

V _d (volume of distribution) ranges from 0.15 to 0.33 l / kg. Against the background of renal failure, the value of this indicator can increase by 2 times, and V _d [+] R-enantiomer of a substance - by 20%.

Ketorolac is not excreted during hemodialysis.

Indications for use

Ketofril is prescribed for pain syndrome of moderate / severe intensity of various etiologies (including in the postoperative period, for oncological diseases, etc.).

Contraindications

Ketofril is not intended for pain relief before / during surgery (associated with a high risk of bleeding), as well as for the treatment of chronic pain.

Absolute:

• a history of rhinitis attacks, bronchial obstruction, urticaria after using acetylsalicylic acid or other non-steroidal anti-inflammatory drug (complete / partial syndrome of acetylsalicylic acid intolerance, manifested by rhinosinusitis, urticaria, nasal mucosa polyps, bronchial asthma);
• hypovolemia (the cause of the disease does not matter);
• angioneurotic edema;
• dehydration;
• intestinal diseases of an inflammatory nature;
• erosive and ulcerative changes in the mucous membrane of the stomach or duodenum, active gastrointestinal bleeding;
• hypocoagulation (including hemophilia);
• active liver disease, severe liver failure;
• progressive kidney disease, severe renal failure (plasma creatinine level above 50 mg / l);
• confirmed hyperkalemia;
• hemorrhagic diathesis, hemorrhagic stroke (suspected or diagnosed);
• violation of hematopoiesis, the presence of a high risk of occurrence / recurrence of bleeding (including after operations);
• period after coronary artery bypass grafting;
• combination therapy with other non-steroidal anti-inflammatory drugs;
• the period of pregnancy and delivery;
• lactation;
• age under 16;
• individual intolerance to the components of the drug.

Relative (Ketofril solution and tablets are prescribed under medical supervision):

• impaired renal function (plasma creatinine level below 50 mg / l);
• active hepatitis;
• cerebrovascular diseases, ischemic heart disease, arterial hypertension;
• bronchial asthma;
• chronic heart failure;
• cholecystitis;
• hyperlipidemia / dyslipidemia;
• diabetes;
• peripheral arterial disease;
• systemic lupus erythematosus;
• cholestasis;
• sepsis;
• polyps of the mucous membrane of the nasopharynx and nose;
• anamnestic data on the development of ulcerative lesions of the gastrointestinal tract;
• presence of Helicobacter pylori infection;
• severe somatic diseases;
• combined treatment with the following means: selective serotonin reuptake inhibitors (sertraline, fluoxetine, citalopram, paroxetine), anticoagulants (warfarin), antiplatelet agents (acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (prednisolone);
• long-term therapy with non-steroidal anti-inflammatory drugs;
• smoking;
• frequent alcohol consumption;
• age over 65.

To minimize the risk of side effects from the gastrointestinal tract, it is necessary to use the lowest effective dose for the minimum possible course duration.

Ketofril, instructions for use: method and dosage

Film-coated tablets

Ketofril tablets are taken orally, depending on the severity of the pain syndrome - once or repeatedly.

Single dose - 10 mg.

Maximum: frequency of application - 4 times a day, daily dose - 40 mg, duration of therapy - 5 days.

Solution for intravenous and intramuscular administration

The dose is selected based on the intensity of the pain syndrome and the patient's response to the drug.

The solution is injected slowly deeply into the muscle (or intravenously) for at least 15 seconds.

If necessary, opioid analgesics may be additionally prescribed in reduced doses.

If Ketofril is used parenterally once, the following doses are shown: patients under 65 years of age - 10-30 mg; patients over 65 years old or patients with impaired renal function - 10-15 mg.

With repeated parenteral administration, Ketofril is prescribed: intramuscularly - every 4–6 hours, intravenously jet - every 6 hours. The initial dose for continuous dosed administration of the solution using an infusion pump is 30 mg, then the infusion rate is 5 mg / hour.

For patients under 65 years of age, the maximum daily dose is 90 mg, for patients over 65 years of age or patients with impaired renal function - 60 mg.

The maximum duration of continuous intravenous infusion is 24 hours.

The duration of the course of treatment for parenteral administration should not exceed 5 days.

The total daily dose of both dosage forms when switching from parenteral administration of Ketofril to oral administration on the day of transfer should not exceed 90 mg in patients under 65 years of age; in patients over 65 years of age or in patients with impaired renal function - 60 mg.

The maximum dose of Ketofril in tablets on the day of transition is 30 mg.

Side effects

Possible adverse reactions (> 3% - often; 1% - infrequently; <1% - rarely):

• urinary system: rarely - hemolytic uremic syndrome (thrombocytopenia, renal failure, hemolytic anemia, purpura), acute renal failure, back pain with / without azotemia and / or hematuria, decrease or increase in urine volume, renal edema, nephritis, frequent urination;
• digestive system: often (in particular, disorders often develop in patients over 65 years of age who have a history of erosive and ulcerative lesions of the gastrointestinal tract) - diarrhea, gastralgia; infrequently - a feeling of fullness in the stomach, constipation, stomatitis, vomiting, flatulence; rarely - nausea, erosive and ulcerative lesions of the gastrointestinal tract (including with bleeding / perforation - melena, heartburn, burning or spasm in the epigastric region, nausea, vomiting like coffee grounds, abdominal pain, etc.), acute pancreatitis, cholestatic jaundice, hepatomegaly, hepatitis;
• cardiovascular system: infrequently - increased blood pressure; rarely - fainting, pulmonary edema;
• nervous system: often - dizziness, headache, drowsiness; rarely - hallucinations, psychosis, aseptic meningitis (convulsions, severe headache, fever, stiff neck and / or back muscles), hyperactivity (anxiety, mood changes), depression;
• respiratory system: rarely - rhinitis, dyspnea or bronchospasm, laryngeal edema (manifested as difficulty breathing, shortness of breath);
• hematopoietic system: rarely - anemia, eosinophilia, leukopenia;
• skin: infrequently - purpura, skin rash (including maculopapular rash); rarely - urticaria, exfoliative dermatitis (in the form of fever with / without chills, redness, peeling or thickening of the skin, tenderness and / or swelling of the palatine tonsils), Lyell and Stevens-Johnson syndromes;
• sensory organs: rarely - ringing in the ears, hearing loss, visual impairment (including blurred visual perception);
• hemostasis system: rarely - rectal or nosebleeds, bleeding from a postoperative wound;
• immune system: rarely - anaphylactoid or anaphylactic reactions (manifested in the form of skin itching, heaviness in the chest, discoloration of the face, skin rash, urticaria, dyspnoea / tachypnea, periorbital edema, edema of the eyelids, shortness of breath, shortness of breath, wheezing);
• others: often - edema (the process may involve the face, legs, ankles, fingers, feet; weight gain); infrequently - increased sweating; rarely - fever, swelling of the tongue.

Overdose

The main symptoms: abdominal pain, vomiting, metabolic acidosis, nausea, impaired renal function, the development of erosive gastritis or peptic ulcer of the stomach.

Therapy: measures aimed at removing the active substance, including gastric lavage and intake of adsorbents (activated carbon), symptomatic treatment (to maintain vital body functions).

With dialysis, ketorolac is not sufficiently excreted.

special instructions

Ketofril ceases to affect platelet aggregation after 24–48 hours.

Do not use the drug in combination with paracetamol for more than 5 days. Against the background of blood coagulation disorders, Ketofril should be prescribed only under constant monitoring of the platelet count (patients need special attention during the postoperative period), which requires careful monitoring of hemostasis.

The risk of adverse reactions from the kidneys on the background of hypovolemia increases. If necessary, Ketofril can be prescribed in combination with narcotic analgesics.

Influence on the ability to drive vehicles and complex mechanisms

You should refrain from driving vehicles during the period of Ketofril therapy, which is associated with a high risk of side effects from the nervous system (in the form of drowsiness, headache, dizziness).

Application during pregnancy and lactation

Ketofril is not prescribed during pregnancy / lactation. Also, the drug can not be used during childbirth and for pain relief in obstetric practice.

Pediatric use

The safety / efficacy profile of Ketofril in patients under 16 years of age has not been studied, therefore, it is contraindicated to prescribe it to this group of patients.

With impaired renal function

• progressive kidney disease, severe renal failure (plasma creatinine level above 50 mg / l): taking the drug is contraindicated;
• impaired renal function (plasma creatinine level below 50 mg / l): Ketofril can be used with caution.

For violations of liver function

• active liver disease, severe hepatic failure: taking the drug is contraindicated;
• active hepatitis: Ketofril may be used with caution.

Use in the elderly

Ketofril therapy in patients over 65 years old should be carried out under medical supervision.

Drug interactions

• acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs, calcium preparations, glucocorticosteroids, ethanol, corticotropin: there is the development of gastrointestinal bleeding and the formation of ulcers of the gastrointestinal tract;
• paracetamol: combined use is accompanied by an increase in nephrotoxicity;
• methotrexate: against the background of simultaneous use, there is an increase in nephro- and hepatotoxicity; combination therapy can be carried out only with the use of low doses of methotrexate under the control of its plasma concentration in the blood;
• drugs that block tubular secretion: there is a decrease in the clearance of ketorolac and an increase in its plasma concentrations in the blood;
• cefoperazone, thrombolytics, indirect anticoagulants, heparin, antiplatelet agents, pentoxifylline, cefotetan: there is an increase in the likelihood of bleeding;
• probenecid: a decrease in plasma clearance and V _{d of} ketorolac, an increase in its plasma concentration in the blood and T _1/2 values;
• methotrexate, lithium preparations: combined use is accompanied by a decrease in clearance and an increase in their toxicity;
• drugs with hypotensive and diuretic action: there is a decrease in their effectiveness (due to a decrease in the synthesis of prostaglandins in the kidneys);
• opioid analgesics: a significant reduction in their dose is possible;
• insulin and oral hypoglycemic agents: simultaneous use leads to an increase in their hypoglycemic action, which requires recalculation of the dose;
• valproic acid: there is a violation of platelet aggregation;
• verapamil, nifedipine: there is an increase in their plasma concentration in the blood;
• other drugs with nephrotoxicity (including gold preparations): against the background of simultaneous use, there is an increase in the likelihood of nephrotoxicity.

Analogs

Analogs of Ketofril are: Ketalgin, Dolomin, Torolak, Dolak, Ketorol, Ketanov, Toradol, Ketolak, Ketorolac, Ketadrop, Ketokam.

Terms and conditions of storage

Store in a place protected from light and moisture at temperatures up to 30 ° C. Keep out of the reach of children.

Shelf life: tablets - 3 years; injection solution - 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Ketofril

Reviews of Ketofril are few. Most often it is noted that it has the claimed therapeutic effect, although some patients indicate an insufficiently strong effect. The cost of the drug is estimated to be affordable.

The price of Ketofril in pharmacies

The approximate price for Ketofril is:

• film-coated tablets (10 mg), 20 pcs. in the package - 82-105 rubles;
• solution for intravenous and intramuscular administration (30 mg / ml, ampoules of 1 ml), 10 pcs. in the package - 101 rubles.

Ketofril: prices in online pharmacies

Drug name Price Pharmacy

Ketofril 10 mg film-coated tablets 20 pcs. 83 rbl. Buy

Ketofril tablets pp 10mg 20 pcs RUB 99 Buy

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!