KSEFOKAM PILLS 8MG

Ksefokam tab

Clinico-pharmacological group

NSAIDs

Mechanism of action

NSAIDs, belongs to the class oxycam. It has a pronounced analgesic and anti-inflammatory effect.

The basis of the mechanism of action of lornoxicam is the suppression of the synthesis of prostaglandins, due to the inhibition of the activity of COX isoenzymes. In addition, lornoxicam inhibits the release of oxygen radicals from activated leukocytes.

Ksefokam does not have an opiate-like effect on the central nervous system, does not inhibit respiration, does not cause drug dependence.

Pharmacokinetics

Suction

Lornoxicam is rapidly and completely absorbed from the gastrointestinal tract after oral administration. Cmax in plasma is reached in about 1-2 hours. The absolute bioavailability of lornoxicam is 90-100%.

Eating reduces Cmax by 30% and increases Tmax up to 2.3 h

Distribution

The binding of lornoxicam with plasma proteins, mainly with the albumin fraction, is 99% and does not depend on its concentration.

Metabolism

Lornoxicam is present in plasma mainly unchanged and, to a lesser extent, in the form of a hydroxylated metabolite that does not possess pharmacological activity. Lornoxicam is completely metabolized in the liver with the participation of the CYP2C9 isoenzyme.

Removal

T1/2 the average is 4 hours and does not depend on the concentration of lornoxicam. Approximately 1/3 of its metabolites excreted by the kidneys and 2/3 with bile.

Pharmacokinetics in special clinical situations

In the elderly, as well as in patients with renal or hepatic insufficiency, no significant changes in the pharmacokinetic parameters of lornoxicam were found.

Indications for use of the drug

- short-term treatment of pain syndrome of various origins;

- symptomatic therapy of rheumatic diseases (rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, articular syndrome with exacerbation of gout, rheumatic soft tissue damage).

Dosage and administration

At severe pain syndrome The recommended dose is 8-16 mg / day in 2-3 doses. The maximum daily dose is 16 mg.

At inflammatory and degenerative rheumatic diseases The recommended starting dose is 12 mg / day. The average dose is 8-16 mg / day, depending on the patient's condition.

The duration of therapy depends on the nature and course of the disease.

Tablets are taken orally before meals with a glass of water.

Patients with gastrointestinal diseases, impaired renal function or the liver to patients elderly (over 65), after extensive operations, the maximum dose is 12 mg / day in 3 doses.

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

Side effect

From the digestive system: dyspepsia, abdominal pain, dry mouth, stomatitis, anorexia, nausea, vomiting, heartburn, diarrhea, esophagitis, gastritis, erosive and ulcerative lesions of the mucous membrane of the stomach and intestines (including perforation and bleeding), constipation, meteorism, melena, abnormal liver function, increased levels of liver transaminases.

Nervous system: headache, dizziness, drowsiness, sleep disorders, depression, agitation, tremor, aseptic meningitis, paresthesias.

Dermatologic: edematous syndrome, ecchymosis, skin rash, pruritus, alopecia, Stevens-Johnson syndrome, Lyell's syndrome.

Allergic reactions: urticaria, angioedema.

Urogenital: dysuria, reduction of glomerular filtration, interstitial nephritis, glomerulonephritis, papillary necrosis, nephrotic syndrome, peripheral edema, acute renal failure.

Special senses: tinnitus, blurred vision.

Cardiovascular: development or aggravation of heart failure, tachycardia, increased blood pressure.

From the hemopoietic system: agranulocytosis, leukopenia, anemia, thrombocytopenia.

From the blood coagulation system: increase bleeding time.

On the part of the respiratory system: pharyngitis, rhinitis, dyspnea, cough, bronchospasm.

Other: increased sweating, changes in body weight, arthralgia, myalgia.

Contraindications to the use of the drug

- A complete or incomplete combination of asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to Acetylsalicylic acid and other NSAIDs (including a history of);

- hemorrhagic diathesis or bleeding disorders, as well as those who have undergone surgery, with the risk of bleeding or incomplete hemostasis;

- the period after coronary artery bypass surgery;

- erosive and ulcerative changes of the gastric or duodenal mucosa;

- active Gastrointestinal bleeding, cerebrovascular or other bleeding;

- recurrent gastric ulcer or repeated bleeding from the gastrointestinal tract;

- bleeding from the gastrointestinal tract associated with taking NSAIDs in history;

- inflammatory bowel disease (Crohn's disease, UC) in the acute phase;

- decompensated heart failure;

- severe liver failure or active liver disease;

- severe renal failure (serum creatinine level more than 300 mcmol / l);

- progressive kidney disease;

- confirmed hyperkalemia;

- hypovolemia or dehydration;

- pregnancy;

- lactation period (breastfeeding);

- children's age up to 18 years (there are no clinical data on the use of this age group);

- hypersensitivity to the drug.

WITH caution the drug should be used for erosive and ulcerative lesions and bleeding from the gastrointestinal tract (in history), moderate renal failure, conditions after surgery, ischemic heart disease, chronic heart failure, cerebrovascular diseases, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral artery disease, CC less than 60 ml / min, ulcerative lesions of the gastrointestinal tract in history, Helicobacter pyloriori infection with long-term use of NSAIDs, severe somatic diseases, simultaneously with oral administration of GCS (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, Fluoxetine, paroxetine, sertraline), in patients over 65 years old, while smoking, alcoholism.

Use of the drug during pregnancy and lactation

Ksefokam is contraindicated for use during pregnancy and lactation (breastfeeding).

The use of the drug may adversely affect female fertility.

Application for violations of the liver

The drug is contraindicated in marked disorders of the liver.

Application for violations of kidney function

The drug is contraindicated in case of moderate or severe renal dysfunction (serum creatinine level> 300 mcmol / l).

Special notes

The risk of an ulcerogenic effect of the drug can be reduced by the simultaneous administration of proton pump inhibitors. In the event of bleeding in the gastrointestinal tract, taking the drug should be immediately stopped and appropriate emergency measures should be taken.Especially carefully it is necessary to monitor the condition of those patients with gastrointestinal pathology, who for the first time receive a course of treatment with the drug Ksefokam.

Like other oxycams, Ksefokam inhibits platelet aggregation, so an increase in bleeding time is possible. When using the drug, it is necessary to strictly control the condition of patients in need of an absolutely normal functioning of the blood coagulation system (for example, patients who are to undergo surgery) who have a disruption of the blood coagulation system or who are receiving drugs that suppress coagulation (including low doses of heparin). timely detect signs of bleeding.

If there are signs of liver damage (skin itching, jaundice of the skin, nausea, vomiting, abdominal pain, dark urine, increased liver transaminases), stop taking the drug and consult your doctor.

Do not use the drug at the same time as other NSAIDs.

The drug can change the properties of platelets, but does not replace the prophylactic action of acetylsalicylic acid in cardiovascular diseases.

Patients with impaired renal function caused by large blood loss or severe dehydration, Ksefokam, as an inhibitor of prostaglandin synthesis, can be appointed only after the elimination of hypovolemia and the associated risk of reducing renal perfusion.

Xefocam (like other NSAIDs) can cause an increase in urea and creatinine concentrations in the blood, as well as water retention, sodium, peripheral edema, hypertension and other early signs of nephropathy. Long-term treatment of such patients with Ksefokam can lead to the following consequences: glomerulonephritis, papillary necrosis and nephrotic syndrome with a transition to acute renal failure.

In elderly patients, as well as in patients suffering from hypertension and / or obesity, it is necessary to control the level of blood pressure.

It is especially important to monitor kidney function in elderly patients, as well as in patients receiving diuretics at the same time; simultaneously receiving medications that can cause kidney damage.

With prolonged use of the drug Ksefokam need to periodically monitor hematological parameters, as well as the function of the kidneys and liver.

Influence on ability to drive motor transport and control mechanisms

Patients using the drug should refrain from types of action that require increased attention, quick mental and motor reactions, alcohol consumption.

Overdose

Symptoms: may increase the described side effects of Xefocam.

Treatment: conduct symptomatic therapy. To reduce the absorption, it is advisable to use Activated carbon immediately after taking Xefocam, to prevent lesions of the gastrointestinal mucosa, anti-ulcer drugs can be used. Dialysis is ineffective.

Drug interaction

With simultaneous use of the drug Ksefokam with cimetidine increases the concentration of lornoxicam in the plasma. Interaction with Ranitidine and antacid drugs was not detected.

With simultaneous use of the drug Ksefokam with anticoagulants or inhibitors of platelet aggregation may increase bleeding time and increase the risk of bleeding (need to control MHO).

Ksefokam can reduce the hypotensive effects of beta-blockers and ACE inhibitors.

Ksefokam reduces the diuretic effect and the hypotensive effect of diuretics.

Ksefokam reduces renal clearance of Digoxin.

The simultaneous use of quinolone antibiotics increases the risk of convulsive syndrome.

With simultaneous use with other NSAIDs or GCS increases the risk of bleeding from the gastrointestinal tract.

Ksefokam increases serum Methotrexate concentration.

When used simultaneously with selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline) increases the risk of bleeding from the gastrointestinal tract.

Ksefokam can cause an increase in Cmax lithium in the plasma and, thereby, enhance the known side effects of lithium.

Ksefokam increases nephrotoxicity of cyclosporine.

Ksefokam able to enhance the hypoglycemic effect of sulfonylurea derivatives.

With simultaneous use of Xefocam with corticotropin, potassium preparations, alcohol increases the risk of side effects from the gastrointestinal tract.

With the simultaneous use of Xefocam with cefamandol, cefoperazone, cefotetan, valproic acid increases the risk of bleeding.

Pharmacy sales terms

The drug is available on prescription.

Terms and conditions of storage

List B. The drug should be kept out of the reach of children at a temperature not exceeding 25 ° C.