Ksefokam

General characteristics. Structure:

Active agent: to lornoksika - 4 mg or 8 mg
Excipients: magnesium stearate, поливидон (To 25), croscarmellose sodium, cellulose, lactose, макроголь (6000), titanium E 171 dioxide, talc, a gipromelloza.

Description
White or yellowish oblong tablets in a film cover with a text impression of "L04" on tablets of 4 mg and "L08" on tablets 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 PG caused by oppression of activity of isoenzymes of TsOG 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.
 The drug Ksefokam® has no opiatopodobny effect on TsNS and, unlike narcotic analgetics, does not oppress breath, does not cause medicinal dependence.

Pharmacokinetics. Lornoksikam is quickly and almost completely soaked up from a GIT after intake. At this Cmax in plasma it is reached approximately in 1–2 h. Meal reduces Cmax by 30% and increases Tmax to 2,3 h. Absolute bioavailability of a lornoksikam makes 90–100%. Lornoksikam is present at plasma generally in 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 (it is preferential with albuminous fraction) makes 99% and does not depend on its concentration.
 
T1/2, on average, makes 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 — 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:

- the moderated and expressed pain syndrome;
- a symptomatic treatment of pain and an inflammation at inflammatory and degenerative rheumatic diseases.

Route of administration and doses:

For intake: at the moderated and 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, or a liver, elderly people (65 years are more senior), the maximum daily dose of 12 mg divided within a day into 3 receptions on 4 mg is recommended to patients with renal failures.

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 PG. 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 the drug Ksefokam®.
 
As well as other oksikama, 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 HP 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 NPVS.
 
Drug can change properties of thrombocytes, however does not replace preventive effect of acetylsalicylic acid at cardiovascular diseases.
 
Patients with the renal failures caused by big blood loss or heavy dehydration, the drug Ksefokam® as inhibitor of synthesis of PG can appoint only after elimination of a hypovolemia and the related danger of reduction of perfusion of kidneys. As well as other NPVS, 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. Prolonged treatment of such patients with the 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 (see. "Contraindications"). At elderly patients, and also at the patients having arterial hypertension and/or obesity it is necessary to control the ABP level.
 
It is especially important to carry out monitoring of function of kidneys at elderly patients, and also at the patients who are at the same time receiving diuretics and HP which can cause injuries of kidneys.
 
At prolonged use of the 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: abdominal pains, diarrhea, dyspepsia, nausea, vomiting; in rare instances - a meteorism, dryness in a mouth, gastritis, an esophagitis, formation of round ulcers and/or bleedings in a GIT (including, rectal bleedings), stomatitis, a glossitis, colitis, a dysphagy, hepatitis, panereatit, abnormal liver functions.
Allergic reakiiya: the skin rashes, hypersensitivity reactions which are followed by short wind, tachycardia, a bronchospasm, Stephens-Johnson's syndrome, exfoliative dermatitis, an angiitis, fever, allergic rhinitis, a lymphadenopathy are possible.
From the central nervous system: seldom - dizziness, a headache, drowsiness, a condition of excitement, a sleep disorder, a sonitus, decrease in hearing, a dysarthtia, hallucinations, migraine, peripheral neuropathy, syncopal states, aseptic meningitis. From the party of sense bodys - a vision disorder, conjunctivitis.
From a picture of peripheral blood and system of coagulation: seldom - a leukopenia, thrombocytopenia.
From a metabolism: seldom - the strengthened sweating, a fever, change of body weight.
From cardiovascular system: seldom - arterial hypertension, tachycardia, peripheral hypostases.
From an urinary system: seldom - a dysuria, in some cases - a glomerulonephritis, a papillary necrosis and a nephrotic syndrome with transition to an acute renal failure, intersticial nephrite, a crystalluria, a polyuria.

Interaction with other medicines:

At simultaneous use of the drug Ksefokam® and Cimetidinum — increase in concentration of a lornoksikam in plasma; ranitidine and antiacid drugs — interaction is not revealed; anticoagulants or inhibitors of aggregation of thrombocytes — increase in a bleeding time is possible (the increased risk of bleeding, MHO control is necessary); beta adrenoblockers and APF inhibitors — decrease in their hypotensive effect is possible; diuretics — decrease in diuretic effect and hypotensive action; digoxin — decrease in renal clearance of digoxin; hinolonovy antibiotics — increase in risk of development of a convulsive syndrome; other NPVS or GKS — increase in risk of gastrointestinal bleedings; a methotrexate — increase in concentration of a methotrexate in serum; SIOZS (for example to tsitalopra, fluoxetine, пароксетин, sertraline) — increase in risk of bleedings from a GIT; lithium salts — increase in peak concentration of lithium in plasma and, thereby, strengthening of the known side effects of lithium is possible; cyclosporine — increase in nephrotoxicity of cyclosporine; sulphonylurea derivatives — strengthening of hypoglycemic effect of the last; alcohol, corticotropin, potassium drugs — increase in risk of development of side effects from a GIT; a tsefamandola, a tsefoperazona, a tsefotetana, valproic acid — increase in risk of developing of bleeding.

Contraindications:

- the known raised sensitivity/allergy to a lornoksikam or to one of drug components;
- instructions in the anamnesis on hypersensitivity to acetylsalicylic acid (aspirin) or other NPVS;
- hemorrhagic diathesis or disturbances of coagulability of blood, and also that who underwent operations,

- the bleedings interfaced to risk or an incomplete hemostasis;
- a peptic ulcer of a stomach and a 12-perstny gut in an aggravation phase;
- nonspecific ulcer colitis;
- the expressed abnormal liver functions;
- moderate or heavy renal failures (level of serumal creatinine> of 300 µmol/l);
- gipovoliyemiya or dehydration;
- the confirmed or estimated hematencephalon;
- bronchial asthma;
- heart failure;
- decrease in hearing;
- deficit dehydrogenase glyukozo-6-phosphate;
- pregnancy and feeding by a breast;
- children's age up to 18 years.

With care to use drug at arterial hypertension and anemia. Patients, with the diseases provided below, drug KSEFOKAM can use "advantage/risk" only after careful assessment of a ratio:

bleedings from a GIT, digestive tract cankers in the anamnesis;
renal failures; and also a diabetes mellitus with reduced function of kidneys;

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 of a GIT purpose of antiulcerous drugs is possible. Dialysis is inefficient.

Storage conditions:

List B. At a temperature of 15 - 25 °C. To store in the place, unavailable to children. Tablets of 4 mg: glass bottles and blisters - 5 years, tablets of 8 mg: glass bottles - 5 years, blisters - 5 years.
Not to use drug after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Bottles of dark glass on 250 tablets. The blister packaging on 10 or 12 tablets, 1,2, 3, 5 or 10 blisters or 1 bottle with the application instruction is located in a cardboard box.