Composition, form of production and packaging
The tablets covered with a cover from white up to light yellow color, round, biconcave.
lornoxicam 8 mg
Excipients: calcium stearate - 1.6 mg, giprolose - 16 mg, sodium hydrogen carbonate - 40 mg, low-substituted giprolose - 48 mg, microcrystalline cellulose - 96 mg, calcium hydrophosphate anhydrous - 110.4 mg.
The composition of the shell: propylene glycol - about 1.1 mg, talc - about 3.6 mg, titanium dioxide - about 3.6 mg, hypromellose - about 5.7 mg.
6 pcs. - blisters (1) - packs of cardboard.
6 pcs. - blisters (2) - packs of cardboard.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (3) - packs of cardboard.
10 pieces. - blisters (5) - packs of cardboard.
10 pieces. - blisters (10) - packs of cardboard.
10 pieces. - blisters (25) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2017.
NSAIDs belong to the class of oxycomas. Has a pronounced analgesic and anti-inflammatory effect.
The mechanism of action is based on suppression of the synthesis of prostaglandins (inhibition of the enzyme COX), leading to a reduction in inflammation.
Lornoxicam does not affect the main indicators of the body: body temperature, heart rate, blood pressure, ECG data, spirometry.
The analgesic effect of lornoxicam is not related to the narcotic effect. The drug Xefokam Rapid does not have an opiate-like effect on the central nervous system and, unlike narcotic analgesics, does not depress respiration, it does not cause drug dependence.
Due to the presence of locally irritating effect on the gastrointestinal tract and systemic ulcerogenic effect associated with the suppression of the synthesis of prostaglandins, complications from the gastrointestinal tract are frequent undesirable effects in the treatment of NSAIDs.
Suction and distribution
Lornoxicam is quickly and almost completely absorbed from the digestive tract. C max in plasma is achieved 30 minutes after ingestion. C max of the drug Xefokam Rapid is higher than the C max drug Xefokam tablets and is equivalent to C max for dosage forms of lornoxicam intended for parenteral administration. When taking lornoxicam with food at the same time, you can expect a decrease in C max and an increase in T max , as well as a decrease in suction of lornoxicam. Absolute bioavailability of the drug Xefokam Rapid is 90-100% and is equivalent to the bioavailability of the drug Xefokam tablets. Not exposed to the effect of "first passage" through the liver.
The binding of lornoxicam with plasma proteins is 99% and does not depend on its concentration. Lornoxicam does not cumulate after repeated use at recommended doses.
Metabolism and excretion
Lornoxicam is completely metabolized in the liver with the formation of inactive 5-hydroxylornoxicam. The isozyme CYP2C9 is involved in the metabolism.Lornoxicam is present in the plasma in unchanged form and in the form of hydroxylated metabolite. As a result of genetic polymorphism, there are individuals with slowed and intensive metabolism, which can be expressed by a marked increase in the concentration of lornoxicam in plasma in persons with delayed metabolism.Lornoxicam does not induce the induction of hepatic enzymes.
T 1/2 is 3-4 hours. About 2/3 of the administered dose is excreted with bile, 1/3 - with urine.
Pharmacokinetics in specific patient groups
In elderly patients, the clearance is reduced by 30-40%.
In patients with impaired hepatic or renal function, no significant changes in the lornoxicam kinetics are observed, except for cumulation in patients with chronic liver disease after 7 days of treatment at a daily dose of 12 mg or 16 mg.
- short-term treatment of pain syndrome from mild to moderate intensity.
The drug is taken orally by washing with a sufficient amount of liquid.
For all patients, the appropriate dosing regimen should be based on an 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 in an initial dose of 16 mg, 12 hours after its administration, at a dose of 8 mg. In the following days, the maximum daily dose should not exceed 16 mg.
Special dose selection for elderly patients in the absence of violations of kidney or liver function is not required. In the case of a violation of kidney or liver function, the daily dose should be reduced.
To reduce the risk of developing adverse events from the gastrointestinal tract, use a minimally effective dose with the minimum possible short course.
In the application of NSAIDs, the most frequent adverse reactions from the digestive system: peptic ulcer, perforation or gastrointestinal bleeding are possible. There were also nausea, vomiting, diarrhea, flatulence, constipation, dyspeptic phenomena, abdominal pain, melena, bloody vomiting, ulcerative stomatitis, exacerbation of colitis or Crohn's disease; in more rare cases - gastritis.
Approximately 20% of patients receiving lornoxicam may develop adverse reactions. Most often - nausea, vomiting and diarrhea, dyspeptic phenomena, indigestion, stomach pain.
In each particular category, side effects are grouped according to the system-organ class and are presented in descending order of frequency: very often (> 10%), often (> 1% and 10%), infrequently (> 0.1% and <1%), rarely > 0.01% and 0.1%), very rarely (<0.01%), the frequency is unknown (it is impossible to determine based on available data).
Infections and infestations: rarely - pharyngitis.
From the hemopoietic 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, anxiety.
From the nervous system: often - short-term headaches of low intensity, dizziness; rarely - somnolentia, paresthesia, taste disorder, tremor, migraine.
From the side of the organ of vision: infrequently - conjunctivitis; rarely - vision disorders.
From the side of the organ of hearing and the vestibular apparatus: infrequently - dizziness, noise in the ears.
From the cardiovascular system: infrequently - palpitation, tachycardia, heart failure, rush of blood to the face; rarely - arterial hypertension, hot flushes, hemorrhage, hematoma.
From the respiratory system: infrequently - rhinitis; rarely - dyspnea, cough, bronchospasm.
On the part of the digestive system: often - nausea, abdominal pain, dyspepsia, diarrhea, vomiting; infrequent - constipation, flatulence, belching, dry mouth, gastritis, peptic 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, impaired liver function; very rarely - damage to hepatocytes.
From the skin and subcutaneous tissues: infrequently - rash, itching, sweating, erythematous rash, hives, alopecia; rarely - dermatitis, purpura; very rarely - edema, bullous reactions, Stevens-Johnson syndrome, toxic epidermal necrolysis.
From the musculoskeletal system: infrequently - arthralgia; rarely - pain in the bones, muscle spasms, myalgia.
From the urinary system: rarely - nocturia, urination disorders, increased levels of urea and creatinine in the blood.
General reactions: infrequent - malaise, swelling, swelling of the face; rarely - asthenia.
- hypersensitivity to lornoxicam or any of the excipients;
- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses, rhinitis, angioedema, urticaria and intolerance of acetylsalicylic acid and other NSAIDs (including in the anamnesis);
- hemorrhagic diathesis or bleeding disorders;
- surgical intervention, associated with a 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 hemorrhage;
- cerebrovascular or other bleeding;
- gastrointestinal bleeding or perforation of an ulcer in anamnesis associated with taking NSAIDs;
- active peptic ulcer or recurrent peptic ulcer in history;
- Inflammatory bowel disease (Crohn's disease, ulcerative colitis) during the exacerbation phase;
severe hepatic impairment;
- marked renal failure (serum creatinine level more than 300 Ојmol / l);
progressive kidney disease;
- confirmed hyperkalemia;
- period after aortocoronary shunting;
- the period of breastfeeding;
- age to 18 years (due to lack of clinical experience).
- impaired renal function of the lung (serum creatinine 150-300 Ојmol / l) and moderate degree (serum creatinine 300-700 Ојmol / l), t. maintenance of renal blood flow depends on the level of renal prostaglandins. The use of lornoxicam should be discontinued if the kidney function worsens during treatment;
- Renal function monitoring should be performed in patients who underwent extensive surgery, patients with heart failure receiving diuretics, and also in cases of drugs with proven or suspected nephrotoxicity;
- with violations from the coagulation system recommended thorough clinical observation and evaluation of laboratory indicators, for example, APTTV;
- for violations of liver function (cirrhosis of the liver), regular clinical observation and evaluation of laboratory parameters should be carried out. when treatment with lornoxicam in a daily dose of 12-16 mg, cumulation of the drug is possible;
- In case of long-term treatment (more than 3 months), regular evaluation of laboratory blood counts (hemoglobin), kidney function (creatinine) and liver enzymes is recommended;
- in patients older than 65 years, it is recommended to monitor the function of the liver and kidneys. Use the drug with caution in the elderly in the postoperative period;
- simultaneous administration with other NSAIDs, including selective COX-2 inhibitors, should be avoided;
- gastrointestinal bleeding, ulceration, perforation, which were previously observed with all NSAIDs at any stage of treatment and can lead to death, the presence of Helicobacter pylori;
- the phenomenon of gastrointestinal toxicity in the history, in particular, in the elderly;
(eg, prednisone), anticoagulants (eg, warfarin), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline) and antiplatelet drugs (eg, acetylsalicylic acid, clopidogrel). With the simultaneous use of NSAIDs and heparin in spinal and epidural anesthesia, the risk of developing a hematoma increases;
- Gastrointestinal pathology in the anamnesis (ulcerative colitis, Crohn's disease), because the condition may deteriorate;
- arterial hypertension and / or heart failure in history, tk. when using NSAIDs, fluid retention with edema development was noted;
- In the presence of diseases of peripheral arteries or cerebrovascular diseases, the presence of risk factors for the development of cardiovascular diseases such as hypertension, hyperlipidemia, diabetes, smoking, should be prescribed lornoxicam only after a thorough assessment of the expected benefit of therapy and possible risk;
- severe skin reactions leading to death, incl. exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis;
- simultaneous use of NSAIDs and tacrolimus may lead to an increased risk of nephrotoxicity due to oppression of prostacyclin synthesis in the kidneys;
- The use of lornoxicam, like any drug that suppresses the synthesis of prostaglandins, can impair fertility, so it is not recommended for women who want to become pregnant.
PREGNANCY AND LACTATION
Because of the lack of data on the use of lornoxicam in pregnant women and during breastfeeding, Xephocam Rapid should not be used during pregnancy and lactation.
Suppressing the synthesis of prostaglandins can have a side effect on pregnancy and / or fetal development.
The use of inhibitors of prostaglandin synthesis in early pregnancy increases the risk of miscarriage or the development of heart disease. It is believed that the risk is 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 arterial duct 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 later periods may cause prolongation of bleeding time in the mother and fetus, as well as suppression of contractile activity of the uterus, which may delay or prolong the period of labor.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe renal failure (serum creatinine level more than 300 Ојmol / l), progressive kidney disease.
With caution: if the kidney function is mild (serum creatinine 150-300 Ојmol / L) and moderate (serum creatinine 300-700 Ојmol / L).
In case of renal dysfunction, the daily dose should be reduced.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe hepatic insufficiency.
With caution: with a violation of the liver (cirrhosis of the liver).
In the case of a violation of liver function, the daily dose should be reduced.
APPLICATION FOR CHILDREN
Contraindicated in the use of drugs under the age of 18 years.
APPLICATION IN ELDERLY PATIENTS
With caution appoint the drug to patients over 65 years of age (recommended control of liver and kidney function); elderly persons in the postoperative period.
Do not use the drug simultaneously with other NSAIDs.
If signs of liver damage (itchy skin, yellowing of the skin, nausea, vomiting, abdominal pain, darkening of the urine, increased activity of liver transaminases), stop taking the drug and consult a doctor.
The drug can change the properties of platelets, but does not replace the preventive effect of acetylsalicylic acid in cardiovascular diseases.
Impact on the ability to drive vehicles and manage mechanisms
Patients who are dizzy and / or drowsy during treatment with lornoxicam should refrain from driving the car and managing the technique.
Symptoms: in case of an overdose of Xephocam Rapid, there may be nausea and vomiting, cerebral symptoms (dizziness, visual disturbance, ataxia, coma and seizures); changes in the function of the liver and kidneys and blood clotting disorders are possible.
Treatment: with a real or suspected overdose, stop taking the drug. Thanks to a short T 1/2 , lornoxicam is rapidly excreted from the body. Dialysis is ineffective. At present, the specific antidote is 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 Xefokam Rapid may lead to a decrease in absorption of the drug. To treat gastrointestinal disorders, prostaglandin or ranitidine analogues are used.
Drug interaction is observed with the simultaneous use of the drug Xefokam Rapid and the following medicines.
Cimetidine - increased concentration of lornoxicam in plasma. Interaction with ranitidine and antacids was not revealed.
Anticoagulants or inhibitors of platelet aggregation - it is possible to increase the time of bleeding (increased risk of bleeding, MHO control is needed).
Fenprokumone - a decrease in the effectiveness of treatment with fenprocumone.
Heparin - NSAIDs increase the risk of developing a spinal / epidural hematoma with concomitant use with heparin in spinal or epidural anesthesia.
Beta-adrenoblockers and ACE inhibitors - possibly reducing their hypotensive effect.
Diuretics - a decrease in the diuretic effect and hypotensive effect of "loop" and thiazide diuretics.
Digoxin - decreased renal clearance of digoxin.
Antibiotics of the quinolone group - increased risk of developing convulsive syndrome.
Other NSAIDs or glucocorticoids are an increased risk of developing a peptic ulcer or bleeding from the digestive tract.
Methotrexate - increased serum concentrations of methotrexate.
Selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline) increase the risk of bleeding from the gastrointestinal tract.
Lithium salts - it is possible to increase Cmax of lithium in plasma, which enhances the known side effects of lithium.
Cyclosporine - increased nephrotoxicity of cyclosporine.
Derivatives of sulfonylureas - possibly increasing the hypoglycemic effect of drugs in this group.
Tacrolimus - increased risk of nephrotoxic effect due to oppression of prostacyclin synthesis in the kidneys.
Eating can reduce suction of lornoxicam by 20% and increase the time to reach Cmax in the blood.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of no higher than 30 В° C. Shelf life - 2 years.