Composition, form of production and packaging
The tablets covered with a film cover from white to white with a yellowish shade of color, oblong, with an inscription "LO4".
1 tab.
lornoxicam 4 mg
Excipients: magnesium stearate, povidone K25, sodium croscarmellose, cellulose, lactose monohydrate.
Sheath composition: macrogol 6000, titanium dioxide (E171), talc, hypromellose.
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.
The tablets covered with a film cover from white to white with a yellowish shade of color, oblong, with an inscription "LO8".
1 tab.
lornoxicam 8 mg
Excipients: magnesium stearate, povidone K25, sodium croscarmellose, cellulose, lactose monohydrate.
Sheath composition: macrogol 6000, titanium dioxide (E171), talc, hypromellose.
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.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
PHARMACHOLOGIC EFFECT
NSAIDs. Has a pronounced analgesic and anti-inflammatory effect. Lornoxicam has a complex mechanism of action, which is based on suppression of the synthesis of prostaglandins, due to inhibition of the activity of COX isoenzymes. In addition, lornoxicam is inhibited by the release of free oxygen radicals from activated leukocytes.
The analgesic effect of lornoxicam is not associated with narcotic effects.
The drug Xefokam 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.
PHARMACOKINETICS
Suction and distribution
Once ingested, lornoxicam is rapidly and almost completely absorbed from the digestive tract. At the same time, Cmax in plasma is reached after approximately 1-2 hours. Food intake reduces C max by 30% and increases T max to 2.3 h. The absolute bioavailability of lornoxicam is 90-100%. The binding of lornoxicam to plasma proteins, mainly with the albumin fraction, is 99% and does not depend on its concentration.
Metabolism and excretion
Lornoxicam is completely metabolized in the liver. The isozyme CYP2C9 is involved in the metabolism. Lornoxicam is present in the plasma, mostly unchanged and, to a lesser extent, in the form of hydroxylated metabolite, which does not possess pharmacological activity.
T 1/2 on the average is 4 hours and does not depend on the concentration of the drug. Approximately 1/3 of the metabolites is excreted from the body by the kidneys and 2/3 - with bile.
Pharmacokinetics in specific patient groups
In elderly patients, as well as in patients with renal or hepatic insufficiency, no significant changes in the pharmacokinetics of lornoxicam were detected.
INDICATIONS
- short-term treatment of pain syndrome of different origin;
- symptomatic therapy of rheumatic diseases (rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, articular syndrome with exacerbation of gout, rheumatic soft tissue damage).
DOSING MODE
The drug is taken by mouth before eating, with a glass of water.
At the expressed painful syndrome the recommended dose of 8-16 mg / sut, divided into 2-3 admission. The maximum daily dose is 16 mg.
In inflammatory and degenerative rheumatic diseases, the recommended initial dose is 12 mg. The standard 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.
With gastrointestinal diseases, patients with impaired renal or hepatic function , elderly patients (over 65 years) , after extensive operations - the maximum daily dose is 12 mg for 3 doses.
To reduce the risk of developing adverse events from the gastrointestinal tract, the minimum effective dose should be used as little as possible with a short course.
SIDE EFFECT
On the part of the digestive system: dyspepsia, abdominal pain, dry mouth, stomatitis, nausea, vomiting, heartburn, diarrhea; esophagitis, gastritis, erosive-ulcerative lesions of the mucous membrane of the stomach and intestines, including. with perforation and bleeding, constipation, flatulence, melena, impaired liver function, increased level of hepatic transaminases.
From the side of the nervous system: headache, dizziness, drowsiness, sleep disturbances, depression, agitation, tremor, aseptic meningitis, paresthesia.
From the senses: tinnitus, impaired vision.
From the cardiovascular system: the development or worsening of heart failure, tachycardia, increased blood pressure.
On the part of the respiratory organs: pharyngitis, rhinitis, dyspnoea, cough, bronchospasm.
From the urinary system: dysuria, decreased glomerular filtration, interstitial nephritis, glomerulonephritis, papillary necrosis, nephrotic syndrome, peripheral edema, acute renal failure.
From the skin and subcutaneous fat: edematous syndrome, ecchymosis, skin rash, itching, urticaria, alopecia, Stevens-Johnson syndrome, Lyell syndrome, angioedema.
On the part of the hematopoiesis and hemostasis system: agranulocytosis, leukopenia, anemia, thrombocytopenia, increased bleeding time.
Other: anorexia, increased sweating, weight change, arthralgia, myalgia.
CONTRAINDICATIONS
- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including in the anamnesis);
- hemorrhagic diathesis or bleeding disorders;
- recent surgery, associated with a risk of bleeding or incomplete hemostasis;
- period after aortocoronary shunting;
- erosive and ulcerative changes in the mucosa of the stomach or duodenum, active gastrointestinal bleeding;
- cerebrovascular or other bleeding;
- recurrent gastric ulcer or repeated gastrointestinal bleeding;
- Gastrointestinal bleeding associated with taking an NSAID in an anamnesis;
- Inflammatory bowel disease (Crohn's disease, ulcerative colitis) during the exacerbation phase;
Decompensated heart failure;
- severe hepatic impairment or active liver disease;
- severe renal failure (serum creatinine level more than 300 Ојmol / l), progressive kidney disease;
- confirmed hyperkalemia;
- hypovolemia or dehydration;
- Pregnancy;
- the period of lactation (breastfeeding);
- Children's and adolescence under 18 (due to the lack of clinical data on its use in this age group);
- hypersensitivity / allergy to lornoxicam or to one of the components of the drug.
With caution: erosive and ulcerative lesions and bleeding from the digestive tract (in history); moderately expressed renal failure, CC less than 60 ml / min; condition after surgery; IHD, chronic heart failure; cerebrovascular diseases; dyslipidemia / hyperlipidemia; diabetes; diseases of peripheral arteries; presence of Helicobacter pylori infection; long-term use of NSAIDs; severe physical illness; simultaneous use of oral GCS (including prednisolone), anticoagulants (including warfarin), antiaggregants (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline); smoking, alcoholism; age over 65 years.
PREGNANCY AND LACTATION
The use of the drug is contraindicated in pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
Patients with impaired renal function - the maximum daily dose is 12 mg, for 3 doses.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Patients with impaired liver function - the maximum daily dose is 12 mg, for 3 doses.
APPLICATION FOR CHILDREN
Contraindication: age to 18 years (due to the lack of clinical data on its use in this age group).
APPLICATION IN ELDERLY PATIENTS
Patients older (over 65 years) - the maximum daily dose is 12 mg, for 3 admission.
SPECIAL INSTRUCTIONS
The risk of ulcerogenic action of the drug reduces the simultaneous administration of inhibitors of the proton pump and synthetic analogues of prostaglandins. In case of bleeding in the gastrointestinal tract, the drug should be stopped immediately and appropriate emergency measures taken. It is especially necessary to monitor the condition of those patients with gastrointestinal pathology, who for the first time receive a course of treatment with Xefokam.
Like other oxicams, the drug Xefokam inhibits platelet aggregation and therefore may increase the time of bleeding. When using this drug, it is necessary to closely monitor the condition of patients who need the absolutely normal functioning of the blood coagulation system (for example, patients who are undergoing surgery) who have disorders of the blood clotting system or who receive medications that depress coagulation (including heparin at low doses) , in order to timely detect signs of bleeding.
If there are signs of liver damage (skin itching, yellowing of the skin, nausea, vomiting, abdominal pain, darkening of the urine, increased liver transaminases), the patient should stop taking the drug and consult a doctor.
Do not use the drug simultaneously with other NSAIDs.
The drug can change the properties of platelets, but does not replace the preventive effect of acetylsalicylic acid in cardiovascular diseases.
Patients with impaired renal function caused by large blood loss or severe dehydration, Xefokam, as an inhibitor of the synthesis of prostaglandins, can be prescribed only after the elimination of hypovolemia and the associated danger of reducing renal perfusion. Like other NSAIDs, Xefokam can cause an increase in the concentration of urea and creatinine in the blood, as well as water and sodium retention, peripheral edema, arterial hypertension and other early signs of nephropathy.Long-term treatment of such patients with the drug Xefokam can lead to the following consequences: glomerulonephritis, papillary necrosis and nephrotic syndrome with transition to acute renal failure. Patients with a marked decrease in renal function should not be prescribed Xefokam. In elderly patients, as well as in patients suffering from hypertension and / or obesity, it is necessary to monitor blood pressure.
It is especially important to monitor kidney function in elderly patients, as well as in patients:
- concomitantly receiving diuretics;
- concurrently receiving drugs that can cause kidney damage.
With prolonged use of the drug, Xefokam should periodically monitor hematological parameters, as well as kidney and liver function.
The use of the drug may adversely affect female fertility and is not recommended for women planning pregnancy.
Patients who use the drug should refrain from drinking alcohol.
Impact on the ability to drive vehicles and manage mechanisms
Patients using the drug should refrain from work requiring increased attention and speed of psychomotor reactions.
OVERDOSE
Symptoms: The side effects of the drug described above may be increased.
Treatment: symptomatic therapy. Taking activated charcoal right after taking Xefokam can help reduce absorption of the drug. To prevent damage to the mucosa, you can use antiulcer drugs. Dialysis is ineffective.
DRUG INTERACTION
Simultaneous use of the drug Xefokam and:
cimetidine - increases the concentration of lornoxicam in plasma; interactions with ranitidine and antacids have not been identified;
anticoagulants or platelet aggregation inhibitors - bleeding time may be increased (increased risk of bleeding, MHO control required;
beta-blockers and ACE inhibitors - can reduce their hypotensive effect;
diuretics - reduces the diuretic effect and hypotensive effect;
digoxin - reduces renal clearance of digoxin;
quinolone antibiotics - increases the risk of convulsive syndrome;
other NSAIDs or GCS - increases the risk of gastrointestinal bleeding;
methotrexate - increases the concentration of methotrexate in the serum;
selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline) - increases the risk of gastrointestinal bleeding;
lithium salts - can cause an increase in peak lithium concentrations in the plasma and, thereby, enhance the known side effects of lithium;
cyclosporine - increases the nephrotoxicity of cyclosporine.
derivatives of sulfonylurea - may enhance the hypoglycemic effect of the latter;
ethanol, corticotropin, potassium preparations - increases the risk of GI tract side effects;
cefamandole, cefoperazone, cefotetan, valproic acid - increases the risk of bleeding.
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 25 В° C. Shelf life - 5 years.
