Ksefokam Rapid tablets p / o 8mg, No. 12

The drug is taken orally with a sufficient amount of liquid.

For all patients, the appropriate dosing regimen should be based on the individual response to treatment.

The recommended dose of the drug is 8-16 mg / day (1-2 tablets).

On the first day of treatment, the drug is prescribed at an initial dose of 16 mg, 12 hours after its administration - at a dose of 8 mg.

On the following days, the maximum daily dose should not exceed 16 mg.

Special dose selection for elderly patients in the absence of impaired renal or liver function is not required.

In case of impaired renal or liver function, the daily dose should be reduced.

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

Coated tablets from white to light yellow, round, biconvex.

1 tab.

lornoxicam 8 mg

Excipients: calcium stearate - 1.6 mg, hyprolose - 16 mg, sodium bicarbonate - 40 mg, low-substituted hyprolose - 48 mg, microcrystalline cellulose - 96 mg, calcium hydrogen phosphate anhydrous - 110.4 mg.

• Hypersensitivity to lornoxicam or any of the excipients;

• complete or incomplete combination of bronchial asthma,

• recurrent polyposis of the nose or paranasal sinuses,

• rhinitis,

• angioedema,

• urticaria and intolerance to acetylsalicylic acid and other NSAIDs (including a history);

• hemorrhagic diathesis or bleeding disorders;

• surgical intervention associated with the risk of bleeding or incomplete hemostasis (in history);

• decompensated heart failure;

• erosive and ulcerative changes in the mucous membrane of the stomach or duodenum;

• active gastrointestinal bleeding;

• cerebrovascular or other bleeding;

• a history of gastrointestinal bleeding or ulcer perforation associated with NSAIDs;

• a history of active peptic ulcer or recurrent peptic ulcer;

• inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the acute phase;

• severe liver failure;

• severe renal failure (serum creatinine level more than 300 ?mol / l);

• progressive kidney disease;

• confirmed hyperkalemia;

• period after coronary artery bypass grafting;

• pregnancy;

• breastfeeding period;

• age up to 18 years (due to insufficient clinical experience).

Carefully:

impaired renal function mild (serum creatinine 150-300 ?mol / l) and moderate (serum creatinine 300-700 ?mol / l), because maintenance of renal blood flow depends on the level of renal prostaglandins. Lornoxicam should be discontinued if renal function deteriorates during treatment; monitoring of renal function should be carried out in patients who have undergone major surgery, patients with heart failure receiving diuretics, and also, in the case of using drugs with proven or suspected nephrotoxicity; in case of disorders of the blood coagulation system, careful clinical observation and assessment of laboratory parameters, for example, APTT, are recommended;in case of impaired liver function (liver cirrhosis), regular clinical observation and assessment of laboratory parameters should be carried out, because when treating with lornoxicam in a daily dose of 12-16 mg, cumulation of the drug is possible; with long-term treatment (more than 3 months), a regular assessment of laboratory parameters of blood (hemoglobin), renal function (creatinine) and liver enzymes is recommended; in patients over 65 years of age, it is recommended to monitor liver and kidney function. The drug should be used with caution in the elderly in the postoperative period; it is necessary to avoid concomitant use with other NSAIDs, including selective COX-2 inhibitors; gastrointestinal bleeding, ulcer, perforation, which were previously noted with the use of all NSAIDs at any stage of treatment and can be fatal, the presence of Helicobacter pylori;history of gastrointestinal toxicity, in particular in old age; while taking medications such as oral corticosteroids (for example, prednisolone), anticoagulants (for example, warfarin), selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline) and antiplatelet drugs (for example, acetylsalicylic acid, clopidogrel) ). With the simultaneous use of NSAIDs and heparin during spinal and epidural anesthesia, the risk of hematoma increases; a history of gastrointestinal tract pathology (ulcerative colitis, Crohn's disease), because the condition may worsen; history of arterial hypertension and / or heart failure; when using NSAIDs, fluid retention with the development of edema was noted;in the presence of peripheral arterial disease or cerebrovascular diseases, the presence of risk factors for the development of cardiovascular diseases such as arterial hypertension, hyperlipidemia, diabetes mellitus, smoking, lornoxicam should be prescribed only after a careful assessment of the expected benefit of therapy and the possible risk; severe skin reactions leading to death, incl. exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis; the simultaneous use of NSAIDs and tacrolimus can lead to an increased risk of nephrotoxic effects due to inhibition of prostacyclin synthesis in the kidneys; the use of lornoxicam, like any drug that suppresses the synthesis of prostaglandins, can impair the ability to fertilize, therefore it is not recommended for women wishing to become pregnant.the presence of risk factors for the development of cardiovascular diseases such as arterial hypertension, hyperlipidemia, diabetes mellitus, smoking, lornoxicam should be prescribed only after a careful assessment of the expected benefits of therapy and the possible risk; severe skin reactions leading to death, incl. exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis; the simultaneous use of NSAIDs and tacrolimus can lead to an increased risk of nephrotoxic effects due to inhibition of prostacyclin synthesis in the kidneys; the use of lornoxicam, like any drug that suppresses the synthesis of prostaglandins, can impair the ability to fertilize, therefore it is not recommended for women wishing to become pregnant.the presence of risk factors for the development of cardiovascular diseases such as arterial hypertension, hyperlipidemia, diabetes mellitus, smoking, lornoxicam should be prescribed only after a careful assessment of the expected benefits of therapy and the possible risk; severe skin reactions leading to death, incl. exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis; the simultaneous use of NSAIDs and tacrolimus can lead to an increased risk of nephrotoxic effects due to inhibition of prostacyclin synthesis in the kidneys; the use of lornoxicam, like any drug that suppresses the synthesis of prostaglandins, can impair the ability to fertilize, therefore it is not recommended for women wishing to become pregnant.diabetes mellitus, smoking, lornoxicam should be prescribed only after a thorough assessment of the expected benefits of therapy and the possible risk; severe skin reactions leading to death, incl. exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis; the simultaneous use of NSAIDs and tacrolimus can lead to an increased risk of nephrotoxic effects due to inhibition of prostacyclin synthesis in the kidneys; the use of lornoxicam, like any drug that suppresses the synthesis of prostaglandins, can impair the ability to fertilize, therefore it is not recommended for women wishing to become pregnant.diabetes mellitus, smoking, lornoxicam should be prescribed only after a thorough assessment of the expected benefits of therapy and the possible risk; severe skin reactions leading to death, incl. exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis; the simultaneous use of NSAIDs and tacrolimus can lead to an increased risk of nephrotoxic effects due to inhibition of prostacyclin synthesis in the kidneys; the use of lornoxicam, like any drug that suppresses the synthesis of prostaglandins, can impair the ability to fertilize, therefore it is not recommended for women wishing to become pregnant.Stevens-Johnson syndrome and toxic epidermal necrolysis; the simultaneous use of NSAIDs and tacrolimus can lead to an increased risk of nephrotoxic effects due to inhibition of prostacyclin synthesis in the kidneys; the use of lornoxicam, like any drug that suppresses the synthesis of prostaglandins, can impair the ability to fertilize, therefore it is not recommended for women wishing to become pregnant.Stevens-Johnson syndrome and toxic epidermal necrolysis; the simultaneous use of NSAIDs and tacrolimus can lead to an increased risk of nephrotoxic effects due to inhibition of prostacyclin synthesis in the kidneys; the use of lornoxicam, like any drug that suppresses the synthesis of prostaglandins, can impair the ability to fertilize, therefore it is not recommended for women wishing to become pregnant.

pharmachologic effect

NSAIDs, belongs to the class of oxicams. It has a pronounced analgesic and anti-inflammatory effect. The mechanism of action is based on the suppression of prostaglandin synthesis (inhibition of the COX enzyme), leading to a decrease in inflammation. Lornoxicam does not affect the main indicators of the state of the body: body temperature, heart rate, blood pressure, ECG data, spirometry. The analgesic effect of lornoxicam is not drug-related. The drug Ksefokam Rapid does not have an opiate-like effect on the central nervous system and, unlike narcotic analgesics, does not depress respiration, does not cause drug dependence. Due to the presence of a local irritating effect on the gastrointestinal tract and a systemic ulcerogenic effect associated with the suppression of prostaglandin synthesis, complications from the gastrointestinal tract are frequent undesirable effects in the treatment of NSAIDs.

Pharmacokinetics

Absorption and distribution

Lornoxicam is rapidly and almost completely absorbed from the gastrointestinal tract. Cmax in plasma is reached 30 minutes after oral administration. The Cmax of the drug Ksefokam Rapid is higher than the Cmax of the drug Ksefokam tablets and is equivalent to the Cmax for dosage forms of lornoxicam intended for parenteral administration. With the simultaneous administration of lornoxicam with food, a decrease in Cmax and an increase in Tmax, as well as a decrease in the absorption of lornoxicam, can be expected. The absolute bioavailability of Ksefokam Rapid is 90-100% and is equivalent to the bioavailability of Ksefokam tablets. Does not undergo a 'first pass' effect through the liver. The plasma protein binding of lornoxicam is 99% and does not depend on its concentration. Lornoxicam does not accumulate after repeated use at recommended doses.Metabolism and excretion Lornoxicam is completely metabolized in the liver to form inactive 5-hydroxylornoxicam. The isoenzyme CYP2C9 is involved in metabolism. Lornoxicam is present in plasma unchanged and as a hydroxylated metabolite. As a result of genetic polymorphism, there are persons with a slow and intense metabolism, which can be expressed in a noticeable increase in the plasma concentration of lornoxicam in persons with a slow metabolism. Lornoxicam does not induce hepatic enzyme induction. T1 / 2 is 3-4 hours. About 2/3 of the administered dose is excreted in the bile, 1/3 in the urine. Pharmacokinetics in special groups of patients In elderly patients, clearance is reduced by 30-40%. In patients with impaired liver or kidney function, there are no significant changes in the kinetics of lornoxicam,with the exception of cumulation in patients with chronic liver disease after 7 days of treatment at a daily dose of 12 mg or 16 mg.

Side effect

Infections and invasions: rarely - pharyngitis.

From the hematopoietic system: rarely - anemia, thrombocytopenia, leukopenia, increased bleeding time; very rarely - ecchymosis.

From the immune system: rarely - hypersensitivity.

From the side of metabolism: infrequently - anorexia, change in body weight.

Mental disorders: infrequently - sleep disturbance, depression; rarely - confusion, nervousness, agitation.

From the nervous system: often - short-term headaches of mild intensity, dizziness; rarely - somnolence, paresthesias, taste disturbances, tremors, migraines.

From the side of the organ of vision: infrequently - conjunctivitis; rarely - visual disturbances.

On the part of the organ of hearing and vestibular apparatus: infrequently - dizziness, tinnitus.

From the side of the cardiovascular system: infrequently - palpitations, tachycardia, heart failure, rush of blood to the face; rarely - arterial hypertension, flushing, hemorrhage, hematoma.

From the respiratory system: infrequently - rhinitis; rarely - dyspnea, cough, bronchospasm.

From the digestive system: often - nausea, abdominal pain, dyspeptic symptoms, diarrhea, vomiting; infrequently - constipation, flatulence, belching, dry mouth, gastritis, gastric ulcer, epigastric pain, duodenal ulcer, ulceration in the oral cavity, increased ALT or AST activity; rarely - melena, bloody vomiting, stomatitis, esophagitis, gastroesophageal reflux, dysphagia, aphthous stomatitis, glossitis, perforated peptic ulcer, liver dysfunction; very rarely - damage to hepatocytes.

Skin and subcutaneous tissue disorders: infrequently - rash, itching, sweating, erythematous rash, urticaria, alopecia; rarely - dermatitis, purpura; very rarely - edema, bullous reactions, Stevens-Johnson syndrome, toxic epidermal necrolysis.

From the musculoskeletal system: infrequently - arthralgia; rarely - bone pain, muscle spasms, myalgia.

From the urinary system: rarely - nocturia, urinary disorders, increased levels of urea and creatinine in the blood.

General reactions: infrequently - malaise, swelling, swelling of the face; rarely asthenia.

Application during pregnancy and lactation

Due to the lack of data on the use of lornoxicam in pregnant women and during lactation, Xefocam Rapid should not be used during pregnancy and lactation. Suppression of prostaglandin synthesis can have side effects on pregnancy and / or fetal development. The use of inhibitors of prostaglandin synthesis in early pregnancy increases the risk of miscarriage or heart disease. The risk is considered to be proportional to the dose and duration of treatment. The appointment of inhibitors of prostaglandin synthesis in the third trimester of pregnancy can lead to toxic effects on the heart and lungs of the fetus (premature closure of the ductus arteriosus and the development of pulmonary hypertension), as well as impaired renal function and, consequently, a decrease in the amount of amniotic fluid.The use of inhibitors of prostaglandin synthesis in late stages can cause prolongation of bleeding time in the mother and the fetus, as well as suppression of uterine contractile activity, which can delay or lengthen the period of labor.

Application for violations of liver function

Contraindicated in severe hepatic impairment.

With care: in case of impaired liver function (liver cirrhosis). In case of impaired liver function, the daily dose should be reduced.

Application for impaired renal function

Contraindicated in severe renal failure (serum creatinine level more than 300 ?mol / l), progressive kidney disease.

With caution: in case of impaired renal function, mild (serum creatinine 150-300 ?mol / l) and moderate (serum creatinine 300-700 ?mol / l). In case of impaired renal function, the daily dose should be reduced.

Application in children

The use of the drug under the age of 18 is contraindicated.

Use in elderly patients

The drug is prescribed with caution to patients over 65 years of age (monitoring of liver and kidney function is recommended); the elderly in the postoperative period.

special instructions

The drug should not be used concomitantly with other NSAIDs. If signs of liver damage appear (itching, yellowing of the skin, nausea, vomiting, abdominal pain, dark urine, increased activity of hepatic transaminases), stop taking the drug and consult your doctor. The drug can change the properties of platelets, but does not replace the prophylactic effect of acetylsalicylic acid in cardiovascular diseases. Influence on the ability to drive vehicles and control mechanisms Patients who experience dizziness and / or drowsiness during treatment with lornoxicam should refrain from driving and operating equipment.

Overdose

Symptoms: in case of an overdose of Ksefokam Rapid, nausea and vomiting, cerebral symptoms (dizziness, visual disturbances, ataxia, turning into coma and convulsions) may occur; possible changes in liver and kidney function and blood clotting disorders.

Treatment: in case of real or suspected overdose, you should stop taking the drug. Due to its short T1 / 2, lornoxicam is rapidly excreted from the body. Dialysis is ineffective. The specific antidote is currently unknown. It is necessary to carry out urgent measures, including gastric lavage. Based on general principles, the use of activated carbon immediately after taking the drug Ksefokam Rapid can lead to a decrease in the absorption of the drug. For the treatment of gastrointestinal disorders, prostaglandin analogues or ranitidine are used.

Drug interactions

Drug interaction is observed with the simultaneous use of the drug Ksefokam Rapid and the following drugs. Cimetidine - an increase in the concentration of lornoxicam in plasma. Interaction with ranitidine and antacids has not been identified. Anticoagulants or platelet aggregation inhibitors - bleeding time may increase (increased risk of bleeding, MHO monitoring is necessary). Fenprokumon - a decrease in the effectiveness of treatment with phenprokumon. Heparin - NSAIDs increase the risk of spinal / epidural hematoma when used with heparin during spinal or epidural anesthesia. Beta-blockers and ACE inhibitors - it is possible to reduce their hypotensive effect. Diuretics - a decrease in the diuretic effect and the hypotensive effect of loop and thiazide diuretics.Digoxin - decreased renal clearance of digoxin. Antibiotics of the quinolone group - increase the risk of developing convulsive syndrome. Other NSAIDs or glucocorticoids - an increased risk of developing peptic ulcer disease or bleeding from the gastrointestinal tract. Methotrexate - an increase in serum methotrexate concentration. Selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline) - an increased risk of bleeding from the gastrointestinal tract. Lithium salts - it is possible to increase the plasma Cmax of lithium, which enhances the known side effects of lithium. Cyclosporine - an increase in the nephrotoxicity of cyclosporine. Sulfonylurea derivatives - it is possible to enhance the hypoglycemic effect of drugs in this group. Tacrolimus - increased risk of nephrotoxic effect due to inhibition of prostacyclin synthesis in the kidneys.Food intake can reduce the absorption of lornoxicam by 20% and increase the time to reach Cmax in the blood.