Ksefokam

General characteristics. Structure:

Active agent: to lornoksika — 4 mg or 8 mg.
Excipients: magnesium stearate, povidone (K25), sodium of a kroskarmelloz, cellulose, lactoses monohydrate.
Cover: macrogoal (6000), titanium dioxide, E-171, talc, gipromelloza.

Description: from color, white to white with a yellowish shade, oblong tablets, film coated, with a text impression of "L04" (a dosage of 4 mg) and "L08" (a dosage of 8 mg).

Pharmacological properties:

Pharmacodynamics. Has the expressed anesthetic and antiinflammatory effect.

Lornoksikam possesses the difficult mechanism of action which cornerstone the suppression of synthesis of prostaglandins caused by oppression of activity of isoenzymes of cyclooxygenase is. Besides, to lornoksika release of free radicals of oxygen from the activated leukocytes oppresses.

The analgetic effect of a lornoksikam is not connected with narcotic action.

Drug KSEFOKAM has no opiatopodobny effect on the central nervous system (CNS) and, unlike narcotic analgetics, does not oppress breath, does not cause medicinal dependence.

Pharmacokinetics. Lornoksikam is quickly and almost completely soaked up from the digestive tract (DT) after intake.

At the same time the maximum concentration in plasma are reached approximately in 1-2 h. Meal reduces the maximum concentration (With max) by 30% and raises time of achievement of the maximum concentration (Ttakh) till 2,3 o'clock. Absolute bioavailability of a lornoksikam makes 90-100%. Lornoksikam is present at plasma, generally at not changed look and, to a lesser extent, in the form of a hydroxylated metabolite which has no pharmacological activity. Linkng of a lornoksikam with proteins of plasma, preferential albuminous fraction, makes 99% and does not depend on its concentration. The elimination half-life averages 4 h and does not depend on concentration of drug. Lornoksikam is completely metabolized in a liver. CYP2C9 isoenzyme participates in metabolism. About 1/3 metabolites are brought out of an organism by kidneys and 2/3 - with bile. At elderly people, and also at patients with a renal or liver failure significant changes of pharmacokinetics of a lornoksikam are not revealed.

Indications to use:

Short-term treatment of a pain syndrome of various origin. Symptomatic therapy of rheumatic diseases (a pseudorheumatism, the osteoarthrosis ankylosing a spondylitis, a joint syndrome at an exacerbation of gout, rheumatic defeat of soft tissues).

Route of administration and doses:

For intake: at the expressed pain syndrome the recommended dose of 8-16 mg/days divided into 2-3 receptions. The maximum daily dose makes 16 mg.

At inflammatory and degenerative rheumatic diseases the recommended initial dose makes 12 mg. The standard dose makes 8-16 mg a day, depending on a condition of the patient. Duration of therapy depends on character and the course of a disease. Pill КСЕФОКАМа is taken inside before food, washing down with a glass of water.

At gastrointestinal diseases, the patient with renal failures or a liver, elderly people (65 years are more senior), after extensive operations - the maximum daily dose makes 12 mg, for 3 receptions. For decrease in risk of development of the undesirable phenomena from a GIT it is necessary to use a minimal effective dose minimum possible short course.

Features of use:

The risk of ulcerogenic effect of drug allows to reduce co-administration of inhibitors of a proton pomp and synthetic analogs of prostaglandins. In case of developing of bleeding in a GIT administration of drug it is necessary to stop and take the appropriate urgent measures at once. It is especially attentively necessary to watch a condition of those patients with gastrointestinal pathology who for the first time receive a course of treatment drug KSEFOKAM. As well as other oksikama, drug KSEFOKAM oppresses aggregation of thrombocytes and therefore can increase a bleeding time. At use of this drug it is necessary to watch attentively a condition of the patients needing absolutely normal functioning of system of a blood coagulation (for example, patients, to whom is necessary surgical intervention), having disturbances of system of a blood coagulation or receiving the medicines oppressing coagulation (including heparin in low doses) timely to find symptoms of bleeding. At emergence of signs of damage of a liver (a skin itch, yellowing of integuments, nausea, vomiting, the abdominal pain, urine darkening, increase in level of "hepatic" transaminases) should stop administration of drug and to see the attending physician. It is not necessary to use drug along with other NPVP. Drug can change properties of thrombocytes, however does not replace preventive effect of acetylsalicylic acid at cardiovascular diseases.

The patient with the renal failures caused by big blood loss or heavy dehydration, KSEFOKAM as inhibitor of synthesis of prostaglandins, it is possible to appoint only after elimination of a hypovolemia and the related danger of reduction of perfusion of kidneys. As well as increase in concentration in blood of urea and creatinine, and also a delay of water and sodium, peripheral hypostases, arterial hypertension and other precursory symptoms of a nephropathy can cause other NPVP, KSEFOKAM. Prolonged treatment of such patients with drug KSEFOKAM can lead to the following effects: a glomerulonephritis, a papillary necrosis and a nephrotic syndrome with transition to an acute renal failure. Patients with the expressed depression of function of kidneys cannot appoint drug KSEFOKAM (see. "Contraindications"). At elderly patients, and also at the patients having arterial hypertension and/or obesity it is necessary to control the level of arterial pressure.

It is especially important to carry out monitoring of function of kidneys at elderly patients, and also at patients:
at the same time receiving diuretics;
at the same time receiving drugs which can cause injuries of kidneys.

At prolonged use of drug KSEFOKAM it is necessary to control periodically hematologic parameters, and also function of kidneys and a liver. Use of drug can negatively influence female fertility and is not recommended to the women planning pregnancy.

The patients using drug need to abstain from the types of action requiring special attention bystry mental and motive reactions, alcohol intake.

Side effects:

From a GIT and a liver: dyspepsia, an abdominal pain, dryness in a mouth, stomatitis, nausea, vomiting, heartburn, diarrhea; an esophagitis, gastritis, erosive cankers of a mucous membrane of a stomach and intestines including with perforation and bleeding, a lock, a meteorism, a melena, an abnormal liver function, increase in level of hepatic transaminases; From a nervous system: headache, dizziness, drowsiness, sleep disorders, depression, excitement, tremor, aseptic meningitis, paresthesias;

From integuments and hypodermic and fatty kletchatki:otechny syndrome, ecchymomas, skin rash, itch, small tortoiseshell, alopecia, Stephens-Johnson's syndrome, Lyell's disease, Quincke's disease; From an urinary system: dysuria, decrease in kpubochkovy filtering, intersticial nephrite, glomerulonephritis, papillary necrosis, nephrotic syndrome, peripheral hypostases, acute renal failure;

From sense bodys: sonitus, vision disorder; From cardiovascular system: development or aggravation of heart failure, tachycardia, increase in the arterial pressure (AP);

From bodies of a hemopoiesis and system of a hemostasis: agranulocytosis, leukopenia, anemia, thrombocytopenia, increase in a bleeding time;

From a respiratory organs: pharyngitis, rhinitis, диспноэ, cough, bronchospasm;

Others: anorexia, sweating strengthening, change of body weight, arthralgia, mialgiya.

Interaction with other medicines:

Simultaneous use of drug KSEFOKAM and:
Cimetidinum - increases concentration of a lornoksikam in plasma. Interaction with ranitidine and antiacid drugs is not revealed;
anticoagulants or inhibitors of aggregation of thrombocytes — increase in a bleeding time is possible (the increased risk of bleeding, control of the international normalized relation (MHO) is necessary;
beta adrenoblockers and inhibitors of an angiotensin-converting enzyme can reduce their hypotensive effect;
diuretics — reduces diuretic effect and hypotensive action;
digoxin — reduces renal clearance of digoxin.
hinolonovy antibiotics — increases risk of development of a convulsive syndrome;
other NPVP or glucocorticoids — increases risk of a GIT of bleedings;
methotrexate — increases concentration of a methotrexate in serum;
selective serotonin reuptake inhibitors (for example, to tsitalopra, fluoxetine, пароксетин, сертрапин) the risk of a GIT of bleedings raises.
lithium salts — can cause increase in peak concentration of lithium in plasma and, thereby, strengthen the known side effects of lithium;
cyclosporine — increases nephrotoxicity of cyclosporine.
sulphonylurea derivatives — can strengthen hypoglycemic effect of the last;
alcohol, corticotropin, drugs of potassium increases risk of side effects from a GIT;
the tsefamandola, a tsefoperazona, a tsefotetana, valproyevoy acid increases risk of bleeding.

Contraindications:

The known raised sensitivity/allergy to a lornoksikam or to one of drug components;
full or incomplete combination of bronchial asthma, the nose recuring a polypose or okolonosovy bosoms and intolerance of acetylsalicylic acid and other NPVP (including in the anamnesis);
hemorrhagic diathesis or disturbances of coagulability of blood, and also that who underwent the operations interfaced to risk of bleeding or an incomplete hemostasis;
the period after performing aortocoronary shunting;
erosive and ulcer changes mucous stomach or 12-perstny gut, active gastrointestinal bleeding; cerebrovascular or other bleeding;
recurrent stomach ulcer or repeated bleeding GIT;
Bleeding GIT, NPVP connected with reception in the anamnesis;
inflammatory diseases of intestines (a disease Krone, nonspecific ulcer colitis) in an aggravation phase;
dekompensirovanny heart failure;
the expressed liver failure or active disease of a liver;
the expressed renal failure (level of serumal creatinine more than 300 µmol/l), the progressing diseases of kidneys, the confirmed giperkapiyemiya, a hypovolemia or dehydration;
pregnancy, breastfeeding period;
children's age up to 18 years, due to the lack of clinical data on its use for this age group.

With care:

Erosive cankers and bleedings from a GIT (in the anamnesis), moderately expressed renal failure, states after surgical interventions, age are more senior than 65 years, the coronary heart disease (CHD), the chronic heart failure (CHF), cerebrovascular diseases, дислипидемия / a lipidemia, a diabetes mellitus, diseases of peripheral arteries, smoking, the clearance of creatinine (CC) less than 60 ml/min., GIT cankers in the anamnesis, existence of an infection of Helicobacter pylori, long use NPVP, alcoholism, heavy somatopathies, a concomitant use of peroral glucocorticosteroids (GKS) (including Prednisolonum), anticoagulants (including warfarin), antiagregant (including кпопидогреля), selective serotonin reuptake inhibitors (including a tsitaloprama, fluoxetine, a paroksetin, sertraline).

Overdose:

Symptoms: strengthening of the side effects of KSEFOKAMA described above is possible. Treatment: Symptomatic.

Reception of absorbent carbon right after reception of KSEFOKAMA can promote decrease in absorption of this drug. For prevention of injury of a mucous membrane it is possible to use antiulcerous drugs. Dialysis is inefficient.

Storage conditions:

Period of validity: 5 years. Not to use drug after a period of validity. List B. At a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets film coated 4 mg and 8 mg. On 10 tablets in the blister from aluminum foil and PVC of a film. 1, 2, 3, 5 or 10 blisters with the application instruction place in a cardboard pack.