Ketofril, 10 mg, film-coated tablets, 20 pcs.

Description of the drug

Ketofril is a non-steroidal anti-inflammatory drug, analgesic, produced on the basis of pyrrolysine carboxylic acid. The active pharmaceutical substance is ketorolac trometamol (ketorolac tromethamine). Additional components depend on the dosage form.

Ketofril is not produced in the form of an ointment.

The medicine is produced in the form:

1. Film-coated tablets. The dragees are disc-shaped, whitish, biconvex.
2. Solution for intravenous and intramuscular injections. The infusion solution is a colorless or pale yellow liquid.

Components of the tablet form in addition to the active pharmaceutical substance:

• Polysorb;

• MCC;
• lactose monohydrate;
• carboxymethylcellulose;
• magnesium salt and stearic acid;
• macrogol;
• titanium dioxide;
• hypromellose;
• talc.

The components of the infusion solution are the following components:

• ethanol;
• sodium chloride;
• sodium hydroxide;
• disodium salt;
• purified water.

The medicine is available only with a doctor's prescription and is stored for 2 years from the date of release. The medication must not be used after the expiration date.

Pharmacodynamic and pharmacokinetic parameters

Ketofril belongs to the non-steroidal anti-inflammatory drugs (NSAIDs). Thanks to the main active ingredient, the medication has a pronounced analgesic effect, reduces fever, and relieves inflammation. The mechanism of action is associated with inhibition of the activity of enzymes involved in the synthesis of prostanoids. These enzymes are precursors of prostaglandins, which cause inflammation, pain and fever.

The effect of Ketofril is very pronounced, superior to the effect of other NSAIDs, comparable to morphine.

Ketorolac does not affect the receptors of the nervous system, is not addictive, and is not an antioxidant. The effect of the medication occurs within 30 to 60 minutes, regardless of what form of release is used. The maximum result is noticeable after 1 - 2 hours.

When administered orally, the medicine is absorbed by the gastrointestinal tract. The maximum concentration of the active substance in the blood serum is visualized after 40 - 50 minutes. Plasma protein binding is 99%. Half-life occurs in 4 - 6 hours. The main part of the medication is absorbed by the kidneys, the rest through the digestive system. In people suffering from renal dysfunction and elderly patients, the rate of elimination of the main pharmaceutical substance slows down.

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Ketofril tablets ppo 10 mg No. 20

Compound

1 tablet contains:
active substance

: ketorolac trometamol (ketorolac tromethamine) 10 mg,

excipients (core):

microcrystalline cellulose, lactose anhydrous, sodium carboxymethyl starch, colloidal silicon dioxide, magnesium stearate,

excipients (shell

): hypromellose, talc, titanium dioxide, macrogol, colloidal silicon dioxide.

Pharmacokinetics

When taken orally, Ketorolac is well absorbed from the gastrointestinal tract - the maximum concentration (Cmax) in the blood plasma (0.7-1.1 mcg/ml) is achieved 40 minutes after taking a dose of 10 mg on an empty stomach. Food rich in fat reduces the maximum concentration of the drug in the blood and delays its achievement by 1 hour.

99% of the drug binds to blood plasma proteins and with hypoalbuminemia the amount of free substance in the blood increases.

Bioavailability - 80-100%. The time to reach equilibrium concentration (Css) with oral administration is 24 hours when administered 4 times a day (above subtherapeutic) and after oral administration of 10 mg is 0.39-0.79 mcg/ml. The volume of distribution is 0.15-0.33 l/kg. In patients with renal failure, the volume of distribution of the drug may increase by 2 times, and the volume of distribution of its R-enantiomer by 20%.

Penetrates into breast milk: when the mother takes 10 mg of ketorolac, Cmax in milk is reached 2 hours after taking the first dose and is 7.3 ng/ml, 2 hours after taking the second dose of ketorolac (when using the drug 4 times a day) it is 7.9 ng/ml.

More than 50% of the administered dose is metabolized in the liver with the formation of pharmacologically inactive metabolites. The main metabolites are glucuronides, which are excreted by the kidneys, and p-hydroxyketorolac. It is excreted 91% by the kidneys, 6% through the intestines.

The half-life (T1/2) in patients with normal renal function averages 5.3 hours. 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 with a plasma creatinine concentration of 19-50 mg/l (168-442 µmol/l), T1/2 is 10.3-10.8 hours, with more severe renal failure - more than 13.6 hours .

Not excreted during hemodialysis.

Indications for use

Pain syndrome of moderate and severe intensity of various origins (including in the postoperative period, with cancer, etc.).

Contraindications

Symptoms

: abdominal pain, nausea, vomiting, the occurrence of peptic ulcers of the stomach or erosive gastritis, impaired renal function, metabolic acidosis.

Treatment

: gastric lavage, administration of adsorbents (activated carbon) and symptomatic therapy (maintaining vital body functions). Not eliminated sufficiently by dialysis.

Directions for use and doses

Ketofril is used orally once or repeatedly depending on the severity of the pain syndrome.

A single dose is 10 mg, when repeated, it is recommended to take 10 mg up to 4 times a day, depending on the severity of pain, the maximum daily dose should not exceed 40 mg.

When taken orally, the duration of the course should not exceed 5 days.

Storage conditions

At a temperature not exceeding 30C, in a dry place, protected from light.

Keep out of the reach of children.

Best before date

3 years.

Do not use after the expiration date stated on the packaging.

special instructions

The effect on platelet aggregation ceases after 24-48 hours.

Hypovolemia increases the risk of developing adverse reactions from the kidneys. If necessary, can be prescribed in combination with narcotic analgesics.

Do not use simultaneously with paracetamol for more than 5 days. Patients with blood coagulation disorders are prescribed the drug only with constant monitoring of the platelet count, which is especially important in the postoperative period, which requires careful monitoring of hemostasis.

Description

Round, biconvex, film-coated tablets, white or almost white.

Conditions for dispensing from pharmacies

On prescription

Dosage form

film-coated tablets

Manufacturer and organization accepting consumer complaints

Torrent Pharmaceuticals Ltd., India

Send quality claims to the following address: Representative office in Russia: Moscow, 117418 st. Novocheremushkinskaya, 61 tel: (495) 232 04 30/31 fax

Pharmacodynamics

Ketorolac has a pronounced analgesic effect and also has anti-inflammatory and moderate antipyretic effects.

The mechanism of action is associated with non-selective inhibition of the activity of the enzyme cyclooxygenase 1 and 2, mainly in peripheral tissues, resulting in inhibition of the biosynthesis of prostaglandins - modulators of pain sensitivity, thermoregulation and inflammation. Ketorolac is a racemic mixture of -S and +R enantiomers, with the analgesic effect due to the -S form.

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

The strength of the analgesic effect is comparable to morphine, significantly superior to other NSAIDs.

After oral administration, the onset of analgesic effect is observed after 1 hour, the maximum effect is achieved after 1-2 hours.

Side effects

Often - more than 3%, less often - 1-3%, rarely - less than 1%.

From the digestive system

: often (especially in elderly patients over 65 years of age with a history of erosive and ulcerative lesions of the gastrointestinal tract) - gastralgia, diarrhea, less often - stomatitis, flatulence, constipation, vomiting, feeling of fullness of the stomach, rarely - nausea, erosive ulcerative lesions of the gastrointestinal tract (including with perforation and/or bleeding - abdominal pain, spasm or burning in the epigastric region, melena, vomiting like coffee grounds, nausea, heartburn, etc.), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.

From
the urinary system
: rarely - acute renal failure, lower back pain with or without hematuria and/or azotemia, hemolytic-uremic syndrome (hemolytic anemia, renal failure, thrombocytopenia, purpura), frequent urination, increased or decreased urine volume, nephritis, edema of renal origin.

From the senses

: rarely - hearing loss, ringing in the ears, visual impairment (including blurred vision).

From the respiratory system

: rarely - bronchospasm or dyspnea, rhinitis, laryngeal edema (shortness of breath, difficulty breathing).

From the side of the central nervous system

: often - headache, dizziness, drowsiness, rarely - aseptic meningitis (fever, severe headache, convulsions, stiffness of the neck and/or back muscles), hyperactivity (mood changes, anxiety), hallucinations, depression, psychosis.

From the cardiovascular system

: less often - increased blood pressure, rarely - pulmonary edema, fainting.

From the hematopoietic organs

: rarely - anemia, eosinophilia, leukopenia.

From the hemostasis system:

rarely - bleeding from a postoperative wound, nosebleeds, rectal bleeding.

From the skin

: less often - skin rash (including maculopapular rash), purpura, rarely - exfoliative dermatitis (fever with or without chills, redness, thickening or peeling of the skin, swelling and/or tenderness of the tonsils), urticaria, Stevens-Johnson syndrome, Lyell's syndrome .

Allergic reactions:

rarely - anaphylaxis or anaphylactoid reactions (change in facial skin color, skin rash, urticaria, skin itching, tachypnea or dyspnea, swelling of the eyelids, periorbital edema, shortness of breath, difficulty breathing, heaviness in the chest, wheezing).

Others

: often - swelling (of the face, legs, ankles, fingers, feet, weight gain), less often - increased sweating, rarely - swelling of the tongue, fever.

Interaction

The simultaneous use of ketorolac with acetylsalicylic acid or other non-steroidal anti-inflammatory drugs, calcium preparations, glucocorticosteroids, ethanol, corticotropin can lead to the formation of ulcers of the gastrointestinal tract and the development of gastrointestinal bleeding.

Co-administration with paracetamol increases nephrotoxicity, and with methotrexate - hepato- and nephrotoxicity. Co-administration of ketorolac and methotrexate is possible only when using low doses of the latter (monitor the concentration of methotrexate in the blood plasma).

Probenecid reduces the plasma clearance and volume of distribution of ketorolac, increases its concentration in the blood plasma and increases its half-life.

With the use of ketorolac, the clearance of methotrexate and lithium may decrease and the toxicity of these substances may increase.

Co-administration with indirect anticoagulants, heparin, thrombolytics, antiplatelet agents, cefoperazone, cefotetan and pentoxifylline increases the risk of bleeding.

Reduces the effect of antihypertensive and diuretic drugs (the synthesis of prostaglandins in the kidneys decreases).

When combined with opioid analgesics, the doses of the latter can be significantly reduced.

Antacids do not affect the complete absorption of the drug.

The hypoglycemic effect of insulin and oral hypoglycemic agents increases (dose recalculation is necessary).

Co-administration with valproic acid causes disruption of platelet aggregation. Increases the plasma concentration of verapamil and nifedipine.

When prescribed with other nephrotoxic drugs (including gold preparations), the risk of developing nephrotoxicity increases. Drugs that block tubular secretion reduce the clearance of ketorolac and increase its concentration in the blood plasma.

Overdose

Symptoms

: abdominal pain, nausea, vomiting, the occurrence of peptic ulcers of the stomach or erosive gastritis, impaired renal function, metabolic acidosis.

Treatment

: gastric lavage, administration of adsorbents (activated carbon) and symptomatic therapy (maintaining vital body functions). Not eliminated sufficiently by dialysis.

Impact on the ability to drive vehicles and operate machinery

Since a significant proportion of patients who are prescribed ketorolac develop side effects from the central nervous system (drowsiness, dizziness, headache), it is recommended to avoid performing work that requires increased attention and quick reaction (driving a vehicle, working with machinery, etc.).

Indications for use of Ketofril

The medication helps relieve moderate to severe pain of various etiologies:

• toothache;
• pain due to injuries, dislocations, sprains;
• pain after childbirth and operations;

• pain due to oncology;
• pain in muscles, joints, nerves;
• radiculopathy;
• rheumatism.

The medication does not prevent the progression of the pathological condition. The drug is also prescribed as an adjuvant for inflammatory diseases and elevated body temperature.

Method of administration and dosage of Ketofril

When using pain medication, you must adhere to the following instructions and dosages:

1. When taking tablets, adults are prescribed 10 mg every 4 to 6 hours. For intense pain, it is allowed to double the dosage and take the medicine 3-4 times a day, but not more than 40 mg.

2. A single dose for intramuscular injection is 10 - 30 mg, the interval between infusions is 4 - 6 hours. The maximum duration of use is no longer than two days. It is prohibited to exceed the dose by more than 60 mg (including oral administration);
3. Intravenous injections should be given at least 15 seconds before.
4. People suffering from renal dysfunction syndrome, or with a body weight of less than 50 kg, are recommended to drink 10 mg as an initial dose, and then in a similar dosage 4 times a day;
5. The maximum daily dose for patients 16 - 64 years old is 90 mg. A thin person weighing less than 50 kg, with kidney dysfunction, elderly people over 65 years old - 60 mg. The duration of therapy should not be longer than 5 days.

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If necessary, opioid analgesics are additionally prescribed in reduced dosages along with Ketofril. Droppers with medication are used for no more than 24 hours per application.

Ketofril, 10 mg, film-coated tablets, 20 pcs.

Hypersensitivity to ketorolac and excipients; anamnestic data on an attack of bronchial obstruction, rhinitis, urticaria after taking acetylsalicylic acid or other NSAIDs (complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs); angioedema; hypovolemia (regardless of the cause that caused it), dehydration; erosive and ulcerative changes in the mucous membrane of the stomach or duodenum, active gastrointestinal bleeding; inflammatory bowel diseases; inflammatory bowel diseases (Crohn's disease, nonspecific colitis) in the acute phase; hypocoagulation (including hemophilia); severe liver failure or active liver disease; severe renal failure (creatinine clearance less than 30 ml/min), progressive kidney disease, confirmed hyperkalemia; acute cerebrovascular accidents (ischemic, hemorrhagic stroke, confirmed or suspected), hemorrhagic diathesis, concomitant use with other NSAIDs, high risk of development or recurrence of bleeding (including after surgery), hematopoietic disorders; decompensated heart failure, the period after coronary artery bypass grafting; lactose intolerance, lactase deficiency or glucose-galactose malabsorption; simultaneous use with probenecid, pentoxifylline, acetylsalicylic acid and other NSAIDs (including cyclooxygenase-2 inhibitors), lithium salts, anticoagulants, including warfarin and heparin; pregnancy, childbirth, breastfeeding; children under 16 years of age (efficacy and safety have not been established). The drug is not used for prophylactic pain relief before and during major surgical interventions due to the high risk of bleeding, as well as for the treatment of chronic pain.

Carefully

- bronchial asthma; cholecystitis; chronic heart failure; coronary heart disease, edema syndrome, cerebrovascular diseases, arterial hypertension; dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, impaired renal function (creatinine clearance less than 30–60 ml/min); cholestasis; active hepatitis; sepsis; systemic lupus erythematosus; old age (over 65 years); anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, the presence of Helicobacter pylori infection, long-term use of NSAIDs, alcohol abuse, severe somatic diseases, concomitant therapy with the following drugs: antiplatelet agents (for example, clopidogrel), oral glucocorticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors ( for example, citalopram, fluoxetine, paroxetine, sertraline).

To reduce the risk of developing adverse events from the gastrointestinal tract, the minimum effective dose should be used for the shortest possible short course.

Contraindications to the use of the medication

Ketofril is not used before or during surgical interventions, and is also not used to relieve pain in chronic pathologies.

There are absolute and relative contraindications to taking an analgesic.

The medicine is contraindicated for treatment during pregnancy and lactation period. Moreover, the drug is prohibited from use during and after labor. Ketofril is also not prescribed for patients under 16 years of age and elderly people.

Also, the medication is prohibited for the following pathological conditions:

• period of exacerbation of erosive and ulcerative lesions of the gastrointestinal tract;

• suspicion or presence of gastrointestinal bleeding syndrome or intracerebral hemorrhage;
• history of poor blood clotting;
• human predisposition to hemorrhages;
• kidney dysfunction;
• bronchial asthma;
• nasal polyposis;
• history of Quincke's edema.

It is dangerous to take the medication if you are hypersensitized to the main active ingredient or additional components, signs of the aspirin triad (aspirin intolerance).

Ketofril

Often - more than 3%, less often - 1-3%, rarely - less than 1%.

From the digestive system: often - gastralgia, diarrhea; less often - stomatitis, flatulence, constipation, vomiting, feeling of fullness in the stomach; rarely - loss of appetite, nausea, erosive and ulcerative lesions of the gastrointestinal tract (including with perforation and/or bleeding - abdominal pain, spasm or burning in the epigastric region, blood in the stool or melena, vomiting with blood or coffee type thick", nausea, heartburn, etc.), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.

From the urinary system: rarely - acute renal failure, lower back pain, hematuria, azotemia, hemolytic-uremic syndrome (hemolytic anemia, renal failure, thrombocytopenia, purpura), increased urination, increased or decreased urine volume, nephritis, edema of renal origin.

From the senses: rarely - hearing loss, ringing in the ears, visual impairment (including blurred visual perception).

From the respiratory system: rarely - bronchospasm or shortness of breath, rhinitis, pulmonary edema, laryngeal edema (shortness of breath, difficulty breathing).

From the side of the central nervous system: often - headache, dizziness, drowsiness; rarely - aseptic meningitis (fever, severe headache, convulsions, stiffness of the neck and/or back muscles), hyperactivity (mood changes, anxiety), hallucinations, depression, psychosis, fainting.

From the cardiovascular system: less often - increased blood pressure.

From the hematopoietic organs: rarely - anemia, eosinophilia, leukopenia.

From the hemostasis system: rarely - bleeding from a postoperative wound, nosebleeds, rectal bleeding.

From the skin: less often - skin rash (including maculopapular rash), purpura, rarely - exfoliative dermatitis (fever with or without chills, flushing, thickening or peeling of the skin, enlargement and/or tenderness of the tonsils), urticaria, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).

Local reactions: less often - burning or pain at the injection site.

Allergic reactions: rarely - anaphylaxis or anaphylactoid reactions (change in facial skin color, skin rash, urticaria, itching of the skin, tachypnea or shortness of breath, swelling of the eyelids, periorbital edema, shortness of breath, difficulty breathing, heaviness in the chest, wheezing).

Other: often - swelling (face, legs, ankles, fingers, feet, weight gain); less often - increased sweating, rarely - swelling of the tongue, fever.

Side effects due to the use of the medicine

Since Ketofril is a strong drug, there are many side effects:

• of cardio-vascular system;

• CNS;
• respiratory organs;
• urinary system;
• hematopoietic organs;
• metabolism.

Allergic reactions often occur as a result of taking non-steroidal medications, so it is important that the dosage is carefully selected taking into account the person’s age and the nature of the pain. Try to avoid overdose - this is fraught with complications.

Ketofril® (Ketofreel®)

Often - more than 3%, less often - 1-3%, rarely - less than 1%.

From the digestive system

: often (especially in elderly patients over 65 years of age with a history of erosive and ulcerative lesions of the gastrointestinal tract) - gastralgia, diarrhea; less often - stomatitis, flatulence, constipation, vomiting, feeling of fullness in the stomach; rarely - nausea, erosive and ulcerative lesions of the gastrointestinal tract (including with perforation and/or bleeding - abdominal pain, spasm or burning in the epigastric region, melena, vomiting like “coffee grounds”, nausea, heartburn, etc. .), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.

From
the urinary system
: rarely - acute renal failure, lower back pain with or without hematuria and/or azotemia, hemolytic-uremic syndrome (hemolytic anemia, renal failure, thrombocytopenia, purpura), frequent urination, increased or decreased urine volume, nephritis, edema of renal origin.

From the senses

: rarely - hearing loss, ringing in the ears, visual impairment (including blurred vision).

From the respiratory system

: rarely - bronchospasm or dyspnea, rhinitis, laryngeal edema (shortness of breath, difficulty breathing).

From the side of the central nervous system

: often - headache, dizziness, drowsiness; rarely - aseptic meningitis (fever, severe headache, convulsions, stiffness of the neck and/or back muscles), hyperactivity (mood changes, anxiety), hallucinations, depression, psychosis.

From the cardiovascular system

: less often - increased blood pressure; rarely - pulmonary edema, fainting.

From the hematopoietic organs

: rarely - anemia, eosinophilia, leukopenia.

From the hemostasis system:

rarely - bleeding from a postoperative wound, nosebleeds, rectal bleeding.

From the skin

: less often - skin rash (including maculopapular rash), purpura; rarely - exfoliative dermatitis (fever with or without chills, redness, thickening or peeling of the skin, swelling and/or tenderness of the tonsils), urticaria, Stevens-Johnson syndrome, Lyell's syndrome.

Allergic reactions:

rarely - anaphylaxis or anaphylactoid reactions (change in facial skin color, skin rash, urticaria, skin itching, tachypnea or dyspnea, swelling of the eyelids, periorbital edema, shortness of breath, difficulty breathing, heaviness in the chest, wheezing).

Others

: often - swelling (face, legs, ankles, fingers, feet, weight gain); less often - increased sweating, rarely - swelling of the tongue, fever.

Analogs of non-steroidal drugs

There are many analogues of Ketofril. Let's pay attention to the table where we compare drugs with similar effects:

All generics have the same indications, contraindications and side effects as Ketofril. There are only minor differences in the set of auxiliary components.