Ketanov, 10 mg, film-coated tablets, 20 pcs., Terapia SA buy in Moscow at a low price

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

Pharmaceutical group: NSAIDs. Pharmaceutical action: 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 COX-1 and -2, mainly in peripheral tissues, resulting in inhibition of the biosynthesis of PG - modulators of pain sensitivity, thermoregulation and inflammation. Ketorolac is a racemic mixture of [-]S- and [+]R-enantiomers, and the analgesic effect is due to the [-]S form. The drug Ketanov 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 intramuscular administration and oral administration, the onset of analgesic effect is observed after 0.5 and 1 hour, respectively, the maximum effect is achieved after 1–2 hours. Pharmacokinetics: After oral administration, Ketanov® is well absorbed in the gastrointestinal tract - Cmax in blood plasma (0.7 –1.1 mcg/ml) is achieved 40 minutes after taking a 10 mg dose on an empty stomach. Food rich in fat reduces the Cmax 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%. Absorption with intramuscular administration is complete and rapid. After intramuscular administration of 30 mg of the drug, Cmax is 1.74–3.1 μg/ml, 60 mg is 3.23–5.77 μg/ml, Tmax is 15–73 and 30–60 minutes, respectively. The time to reach equilibrium concentration (CSS) for parenteral and oral administration is 24 hours when administered 4 times a day (above subtherapeutic) and is 0.65–1.13 mcg/ml, 30 mg for intramuscular administration at a dose of 15 mg. — 1.29–2.47 μg/ml; after oral administration of 10 mg - 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 its R-enantiomer by 20%. Penetrates into breast milk: after the mother takes the first and second doses of ketorolac (10 mg), Cmax in milk is reached after 2 hours and is 7.3 and 7.9 ng/l, respectively. 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. T1/2 in patients with normal renal function averages 5.3 hours (3.5–9.2 hours after intramuscular administration of 30 mg and 2.4–9 hours after oral administration of 10 mg). T1/2 lengthens in elderly patients and shortens in young ones. 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 The total clearance is 0.023 l/kg/h with intramuscular administration at a dose of 30 mg (0.019 l/kg/h in elderly patients), or 0.025 l/kg/h with oral administration at a dose of 10 mg; in case of renal failure with a plasma creatinine concentration of 19–50 mg/l, with intramuscular administration at a dose of 30 mg - 0.015 l/kg/h, with oral administration of 10 mg - 0.016 l/kg/h. Not excreted during hemodialysis.

Instructions for use of KETANOV

The maximum duration of treatment should not exceed 5 days.

Gastrointestinal bleeding, ulceration and perforation

Gastrointestinal bleeding, ulceration or perforation, which may be fatal, has been reported with the use of NSAIDs at any time during treatment, with or without warning symptoms or in the case of a history of severe gastrointestinal disorders. The risk of severe gastrointestinal bleeding depends on the dosage of the drug. This particularly applies to elderly patients who use ketorolac at an average daily dose of more than 60 mg. For these patients, as well as for patients who are concomitantly using low doses of acetylsalicylic acid or other drugs that may increase gastrointestinal risk, combination treatment with protective agents (eg, misoprostol or proton pump inhibitors) should be considered. Ketanov is used with caution in patients who are concomitantly receiving drugs that may increase the risk of ulceration or bleeding, such as oral corticosteroids, selective serotonin reuptake inhibitors, or antiplatelet agents such as acetylsalicylic acid. If gastrointestinal bleeding or ulceration occurs in patients receiving Ketanov, treatment should be discontinued.

Respiratory dysfunction

Read also: Edarbi® Klo

Caution is required when using the drug in patients with bronchial asthma (or with a history of asthma), since NSAIDs have been reported to accelerate the onset of bronchospasm in such patients.

Effect on kidney function

Prostaglandin biosynthesis inhibitors (including NSAIDs) have been reported to have nephrotoxic effects. The drug should be prescribed with caution to patients with impaired renal, cardiac, or liver function, since the use of NSAIDs may lead to deterioration of renal function. Patients with minor renal impairment are prescribed lower doses of ketorolac (those that do not exceed 60 mg/day IM or IV), and the renal condition of such patients should also be carefully monitored. As with other drugs that inhibit prostaglandin synthesis, increases in serum urea, creatinine and potassium have been reported during use of ketorolac tromethamine, which may occur after a single dose.

Cardiovascular, renal and liver disorders

The drug is prescribed with caution to patients with conditions that lead to a decrease in blood volume and/or a decrease in renal blood flow, when renal prostaglandins play a supporting role in ensuring renal perfusion. In these patients, renal function should be monitored. The volume reduction should be corrected and serum urea and creatinine levels and the volume of urine excreted carefully monitored until the patient becomes normovolemic. In patients on renal dialysis, the clearance of ketorolac was reduced by approximately half the normal rate, and the final T1/2 increased approximately threefold. Patients with impaired liver function due to cirrhosis did not have any clinically significant changes in ketorolac clearance or terminal T1/2. Borderline elevated values on one or more liver function tests may occur. These abnormalities may be temporary, may remain unchanged, or may progress with continued treatment. If clinical signs and symptoms indicate the development of liver disease or if systemic manifestations are observed, Ketanov should be discontinued.

Fluid retention and swelling

Fluid retention and edema have been reported during use of ketorolac, so the drug should be administered with caution to patients with cardiac decompensation, hypertension, or similar conditions.

Cardiovascular and cerebrovascular effects

There is currently insufficient information to assess such a risk for ketorolac tromethamine. Patients with uncontrolled hypertension, congestive heart failure, diagnosed coronary artery disease, peripheral arterial disease and/or cerebrovascular disease should be under medical supervision.

Systemic lupus erythematosus and mixed connective tissue diseases

In patients with systemic lupus erythematosus and various mixed connective tissue diseases, the risk of developing aseptic meningitis increases.

Dermatological reactions

Ketanov should be discontinued at the first signs of a skin rash, damage to the mucous membranes or any other signs of hypersensitivity.

Anaphylactic (anaphylactoid) reactions

As with the use of other NSAIDs, anaphylactic (anaphylactoid) reactions (including anaphylaxis, bronchospasm, flushing, rash, hypotension, laryngeal edema, angioedema) may occur in patients who have no or no history of hypersensitivity reactions to aspirin, other NSAIDs or ketorolac. This set of symptoms may also occur in individuals with a history of bronchospastic reactivity (eg, asthma) and nasal polyps. Anaphylactoid reactions, such as anaphylaxis, can be fatal. Therefore, ketorolac should not be taken by patients with a history of asthma and patients with a complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses, and Quincke's edema. If anaphylactoid reactions occur, seek emergency medical attention.

Hematological effects

Patients with bleeding disorders should not be prescribed Ketanov. Patients receiving anticoagulant therapy may have an increased risk of bleeding if ketorolac is used concomitantly. The condition of patients who are receiving other drugs that can affect the rate of bleeding control should be carefully monitored when prescribing ketorolac. In controlled clinical trials, the incidence of significant postoperative bleeding was less than 1%. Ketorolac inhibits platelet aggregation and prolongs bleeding time. In patients with normal bleeding time, the duration of bleeding increased, but did not go beyond the normal range of 2-11 minutes. In contrast to the long-term effects resulting from the use of acetylsalicylic acid, platelet function returns to normal within 24-48 hours after discontinuation of ketorolac. Ketorolac should not be prescribed to patients who have undergone surgery with a high risk of bleeding or incomplete control of bleeding. Caution should be used if mandatory bleeding control is critical. Ketanov is not an anesthetic agent and does not have sedative or anxiolytic properties; therefore, it is not recommended as a pre-operative sedative to maintain anesthesia.

Use in pediatrics

The drug is not used in children and adolescents under 16 years of age.

Impact on the ability to drive vehicles and operate machinery

Some patients may experience drowsiness, dizziness, vertigo, insomnia, fatigue, blurred vision, or depression when using ketorolac. If the patient experiences the above or other similar side effects, you should not drive or operate machinery.

Ketanov tab ppo 10 mg No. 20

Compound

Active substance: ketorolac trometamol 10 mg.
Excipients: corn starch 44.76 mg, microcrystalline cellulose 122.41 mg, colloidal silicon dioxide 1.83 mg, magnesium stearate 1 mg.

Film coating: hypromellose 2.91 mg, macrogol-400-0.68 mg, purified talc 0.16 mg, titanium dioxide 1.25 mg.

Pharmacokinetics

After oral administration, 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: after the mother takes the first and second doses of ketorolac 10 mg, Cmax in milk is reached after 2 hours and is 7.3 ng/ml and 7.9 g/l, respectively.

More than 50% of the administered dose is metabolized in the liver to form 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 is 2.4-9 hours after oral administration of 10 mg. T1/2 lengthens in elderly patients and shortens in young ones. 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 The total clearance when taken orally is 10 mg - 0.025 l/kg/h; in case of renal failure with a plasma creatinine concentration of 19-50 mg/l when taken orally 10 mg - 0.016 l/kg/h.

Not excreted during hemodialysis.

Indications for use

Pain syndrome of severe and moderate severity: injuries, toothache, pain in the postoperative period, cancer, myalgia, arthralgia, neuralgia, radiculitis, dislocations, sprains, rheumatic diseases.

Intended for symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease.

Contraindications

Complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including a history);
urticaria, rhinitis caused by taking NSAIDs (history);
intolerance to pyrazolone drugs;
dehydration, hypovolemia (regardless of the cause);
bleeding or a high risk of developing it;
condition after coronary artery bypass surgery;
confirmed hyperkalemia;
inflammatory bowel diseases;
erosive and ulcerative lesions of the gastrointestinal tract in the acute stage, peptic ulcers;
hypocoagulation (including hemophilia);
severe renal failure (creatinine clearance less than 30 ml/min);
severe liver failure or active liver disease;
hemorrhagic stroke (confirmed or suspected);
hemorrhagic diathesis;
hematopoietic disorder;
pregnancy;
childbirth;
lactation period (breastfeeding);
children under 16 years of age (efficacy and safety have not been established);
hypersensitivity to ketorolac and other NSAIDs.

Not used as a means for premedication, maintenance of anesthesia, pain relief before and during surgical operations (including in obstetric practice) due to the high risk of bleeding.

Not indicated for the treatment of chronic pain.

With caution: bronchial asthma; cholecystitis; chronic heart failure; arterial hypertension; impaired renal function (plasma creatinine below 50 mg/l); cholestasis; active hepatitis; sepsis; systemic lupus erythematosus; old age (over 65 years); polyps of the nasal and nasopharyngeal mucosa, simultaneous use with other NSAIDs; the presence of factors that increase gastrointestinal toxicity: alcoholism, smoking; postoperative period, edema syndrome, coronary artery disease, cerebrovascular diseases, dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral arterial diseases, creatinine clearance less than 60 ml/min, history of ulcerative lesions of the gastrointestinal tract, presence of Helicobacter pylori infection, long-term use of NSAIDs, severe somatic diseases, simultaneous taking oral corticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline ).

Directions for use and doses

In the form of Ketanov® tablets, they are used orally once or repeatedly, depending on the severity of the pain syndrome.

Single dose - 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

In a dry place, protected from light, at a temperature not exceeding 25°C. Keep out of the reach of children.

Best before date

3 years. Do not use after expiration date.

special instructions

When used together with other NSAIDs, fluid retention, cardiac decompensation, and arterial hypertension may occur.

To reduce the risk of developing NSAID gastropathy, antacids, misoprostol, and omeprazole are prescribed.

The effect on platelet aggregation lasts for 24-48 hours.

Hypovolemia increases the risk of developing adverse reactions from the kidneys.

If necessary, can be prescribed in combination with opioid analgesics.

Do not use simultaneously with paracetamol for more than 5 days.

In patients with blood coagulation disorders, it is used only with constant monitoring of the platelet count, especially in the postoperative period, which requires careful monitoring of hemostasis.

Description

Non-steroidal anti-inflammatory drug (NSAID).

Use in children

Contraindication: children and adolescents under 16 years of age (efficacy and safety have not been established).

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 (COX-1) and cyclooxygenase-2 (COX-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, and the analgesic effect is 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 non-steroidal anti-inflammatory drugs.

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

Side effects

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 - 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, melena, vomiting with blood or coffee grounds, nausea, heartburn), 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), frequent urination, increased or decreased urine volume, nephritis, edema of renal origin.

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

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

Use during pregnancy and breastfeeding

The use of the drug is contraindicated during pregnancy, during childbirth and during breastfeeding.

Interaction

The simultaneous use of ketorolac with acetylsalicylic acid or other NSAIDs, calcium preparations, corticosteroids, ethanol, corticotropin can lead to the formation of gastrointestinal ulcers 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).

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 used simultaneously with opioid analgesics, the doses of the latter can be significantly reduced, because their effect is enhanced.

When used simultaneously, it enhances the hypoglycemic effect of insulin and oral hypoglycemic drugs (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.

Probenecid and drugs that block tubular secretion reduce the clearance of ketorolac and increase its concentration in the blood plasma.

Myelotoxic drugs increase the manifestations of hematotoxicity of the drug.

Pharmaceutically incompatible with tramadol solution and lithium preparations.

Overdose

Symptoms: abdominal pain, nausea, vomiting, peptic ulcers or erosive gastritis, impaired renal function, metabolic acidosis.
Treatment: gastric lavage, administration of adsorbents (activated carbon) and symptomatic therapy (maintaining vital functions in the body).

Not eliminated sufficiently by dialysis.

Impact on the ability to drive vehicles and operate machinery

Since a significant proportion of patients using 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 vehicles, working with machinery).

Ketanov®

According to the World Health Organization (WHO), adverse effects are classified with their frequency of development as follows: very common (1/10), common (1/100 to <1/10), uncommon (1/1000 to <1/100) ), rare (1/10,000 to <1/1000), very rare (1/10,000), frequency unknown (the frequency of events cannot be determined based on available data). The following side effects have been reported in connection with the use of ketorolac:

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; infrequently - stomatitis, flatulence, constipation, vomiting, feeling of fullness of 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 and others), 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 visual perception), impaired taste.

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

From 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: infrequently - increased blood pressure, rarely - pulmonary edema, fainting.

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

From the hemostatic system: rarely - bleeding from a postoperative wound, nosebleeds, rectal bleeding, exacerbation of ulcerative colitis or Crohn's disease.

From the skin: uncommon - skin rash (including maculopapular rash), purpura, rare - 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.

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

Allergic reactions: rarely - anaphylaxis or anaphylactoid reactions (change in facial skin color, skin itching, tachypnea or dyspnea, 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); infrequently - increased sweating; rarely - swelling of the tongue, fever.

If any of the side effects indicated in the instructions get worse, or you notice any other side effects not listed in the instructions, tell your doctor.