Composition, form of production and packaging
Lyophilizate for the preparation of a solution for intravenous and / or injections in the form of a dense mass of yellow color.
lornoxicam 8 mg
Excipients: mannitol (E421) - 100 mg, trometamol - 12 mg, disodium edetate - 0.2 mg.
Bottles of dark glass (5) - packs of cardboard.
Vials of dark glass (5) - plastic pallets (1) - cardboard packs.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
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. Inhibition of COX leads to desensitization of peripheral pain receptors and, accordingly, to inhibition of inflammation. In addition, lornoxicam is inhibited by the release of free oxygen radicals from activated leukocytes. The analgesic effect of lornoxicam is not associated with an opiate-like effect on the central nervous system and, unlike narcotic analgesics, lornoxicam does not inhibit respiration, it does not cause drug dependence.
Lornoxicam does not affect vital signs: body temperature, respiratory rate, heart rate, blood pressure, ECG parameters, spirometry.
With the / m introduction of Cmax lornoxicam in plasma is achieved after about 0.4 h. Absolute bioavailability (calculated from the value of AUC) after the / m introduction is 97%.
The binding with plasma proteins is 99% and does not depend on concentration.
Metabolism and excretion
Lornoxicam is present in plasma unchanged, as well as in the form of hydroxylated metabolite, which does not possess pharmacological activity.
T 1/2 is an average of 3-4 hours. Lornoxicam is completely metabolized, about 1/3 of the metabolites is excreted by the kidneys and 2/3 by metabolism in the liver.
Pharmacokinetics in special clinical cases
In elderly patients and patients with impaired liver and kidney function, no significant changes in the pharmacokinetics of lornoxicam were found.
- short-term therapy of acute pain from mild to moderately strong.
The drug is used parenterally.
With postoperative pain, the drug is given in / m or / in, with an acute attack of lumbago / ishalgia - in / m.
The initial dose may be 8 mg or 16 mg. With an insufficient analgesic effect of the drug at a dose of 8 mg, you can also add the same dose.
Maintenance therapy: 8 mg 2 times / day.
The maximum daily dose is 16 mg.
The drug should be applied at the lowest effective dose with the minimum possible short course.
The injection solution is prepared immediately before use by dissolving the contents of one vial (8 mg Xefokam powder) with water for injection (2 ml). After the solution is prepared, the needle is replaced.
In / m injections make a long needle.
The solution thus prepared is administered iv or I / m. The duration of IV administration of the solution should be at least 15 seconds, v / m - not less than 5 seconds.
In the treatment of NSAIDs, the most frequent adverse reactions from the gastrointestinal tract; there may be edema, arterial hypertension and heart failure. The use of such drugs may be associated with a slight increase in the risk of arterial thrombotic events.
With Xefokam, the following side effects may occur.
Infections and parasitic diseases : rarely - pharyngitis.
From the hemopoietic system: rarely - anemia, thrombocytopenia, leukopenia.
From the coagulation system: rarely - an increase in bleeding time; very rarely - a hemorrhagic rash.
From the immune system : rarely - hypersensitivity.
From the metabolism: sometimes - anorexia, weight change.
From the side of the psyche: sometimes - insomnia, depression; rarely confusion, nervousness, excitement.
From the nervous system: often - light and transient headaches, dizziness; rarely - drowsiness, paresthesia, taste disorder, distortion of taste perception, tremor, migraine.
From the side of the organ of vision: sometimes - conjunctivitis; rarely - a vision disorder.
From the side of the organ of hearing and the labyrinth: sometimes - dizziness, noise in the ears.
From the cardiovascular system: sometimes - palpitations, tachycardia, edema, heart failure, hot flashes, swelling; rarely - arterial hypertension, bleeding, hematoma.
From the respiratory tract: sometimes - rhinitis; rarely - shortness of breath, cough, bronchospasm.
On the part of the digestive system: often (? 1% and <10%) - abdominal pain, diarrhea, nausea, vomiting, indigestion; sometimes - constipation, flatulence, belching, dry mouth, gastritis, stomach ulcer, pain in the epigastric region, duodenal ulcer, ulceration of the oral cavity; rarely (<1%) - dysphagia, esophagitis, stomatitis, tarry stool, bloody vomiting, reflux, aphthous stomatitis, glossitis, peptic ulcer with perforation.
From the liver and gallbladder: sometimes - an increase in liver function; rarely - violations of the liver function; very rarely - hepatocellular disorders.
From the skin and subcutaneous tissue: sometimes - skin rash, itching, hyperhidrosis, erythematous rash, hives, alopecia; rarely - dermatitis, hemorrhagic rash; Very rarely (<1/10 000) - edema and bullous reactions, Stevens-Johnson syndrome, toxic epidermal necrolysis.
From the musculoskeletal system: sometimes - arthralgia; rarely - pain in the bones, muscle spasms, myalgia.
From the side of the urinary system: rarely - nocturia, violation of urination, an increase in the blood urea nitrogen and creatinine levels.
General reactions: sometimes - malaise, swelling of the face; rarely - asthenia.
Local reactions: hyperemia, tenderness at the injection site.
- 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, as well as after operations involving 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 bleeding from the gastrointestinal tract;
- data on previous bleeding from the gastrointestinal tract associated with the intake of NSAIDs;
- Inflammatory bowel diseases (Crohn's disease, NJC) in the phase of exacerbation;
- heart failure in the stage of decompensation;
- liver failure or active liver disease;
- severe renal failure (serum creatinine content more than 300 Ојmol / l), progressive kidney disease, confirmed hyperkalemia, hypovolemia or dehydration;
- the period of breastfeeding;
- Children's and adolescence under 18 years (due to the lack of clinical data on the use of the drug in this age group);
- hypersensitivity / allergy to the components of the drug.
Erosion-ulcerative lesions and bleeding from the gastrointestinal tract (in the anamnesis), moderately pronounced renal failure, conditions after surgery, age over 65 years, arterial hypertension, coronary heart disease, chronic heart failure, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes, peripheral arterial disease , smoking, CC less than 60 ml / min, ulcerative lesions of the gastrointestinal tract in history, presence of Helicobacter pylori infection, prolonged use of NSAIDs, alcoholism, severe physical illnesses; simultaneous administration of oral GCS (including prednisolone), anticoagulants (including warfarin), antiaggregants (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), diuretics, drugs with known or suspected nephrotoxic effects.
Simultaneous treatment with NSAIDs and tacrolimus may increase the risk of nephrotoxicity.
The simultaneous use of NSAIDs and heparin in combination with spinal or epidural anesthesia increases the risk of spinal / epidural hematomas.
PREGNANCY AND LACTATION
Xefokam is contraindicated for use in pregnancy and lactation (breastfeeding).
The use of the drug may adversely affect female fertility and is not recommended for women planning pregnancy.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindications: marked renal failure (serum creatinine content more than 300 Ојmol / L), progressive kidney disease, confirmed hyperkalemia, hypovolymia, or dehydration.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindications: liver failure or active liver disease.
APPLICATION FOR CHILDREN
Contraindicated in children and adolescents under 18 years.
APPLICATION IN ELDERLY PATIENTS
With caution: age over 65 years.
The risk of ulcerogenic action of the drug can be reduced by simultaneous administration of proton pump inhibitors and synthetic analogues of prostaglandins. In case of bleeding from the gastrointestinal tract, the drug should be stopped immediately and appropriate emergency measures taken. Especially it is necessary to observe 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 the aggregation of platelets, so it is possible to increase the time of bleeding. When using the drug, it is necessary to strictly monitor the condition of patients who need absolutely normal functioning of the blood coagulation system (for example, patients who are undergoing surgery) who have disorders of the blood coagulation system or who receive drugs depressing coagulation (including heparin at low doses), for in time to detect signs of bleeding.
If there are signs of liver damage (itchy skin, icterus of skin, nausea, vomiting, abdominal pain, darkening of urine, increased level of liver transaminases), stop taking the drug and consult a doctor.
Do not use the drug simultaneously with other NSAIDs.
The drug is able to 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.
Xephoxam (as well as other NSAIDs) can cause an increase in the concentration of urea and creatinine in the blood, as well as water retention, sodium, 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.
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 receiving diuretics simultaneously; simultaneously receiving medicines that can cause kidney damage.
With prolonged use of the drug, Xefokam should periodically monitor hematological parameters, as well as kidney and liver function.
Impact on the ability to drive vehicles and manage mechanisms
Patients receiving the drug should refrain from types of action that require increased attention, rapid mental and motor reactions, alcohol consumption.
Currently, there is no evidence of Xefokam overdose, which would allow to determine its consequences or to propose specific measures for their elimination.
Symptoms: more frequent and severe side effects from the gastrointestinal tract, central nervous system and signs of kidney failure are expected. Serious symptoms are ataxia, convulsions, liver and kidney damage, possibly a coagulation disorder.
Treatment: for suspected overdose, Xefokam administration should be discontinued. Due to the fact that T 1/2 lornoxicam is about 4 hours, it is rapidly excreted from the body. Lornoxicam can not be removed from the body by dialysis. At present, there is no specific antidote. You should use usual emergency measures and perform symptomatic treatment.
With the simultaneous use of the drug Xefokam with cimetidine, the concentration of lornoxicam in plasma increases. Interaction with ranitidine and antacids was not revealed.
With the simultaneous use of Xsefokam with anticoagulants or platelet aggregation inhibitors, bleeding time and an increased risk of bleeding may be increased (MHO control is necessary).
Simultaneous use with fenprokumonom reduces its effectiveness.
With the simultaneous use of NSAIDs and heparin in combination with spinal / epidural anesthesia, the risk of spinal or epidural hematomas increases.
With the simultaneous use of Xefokam, the hypotensive effect of beta-adrenoblockers and ACE inhibitors decreases.
Xefokam reduces the diuretic effect and the hypotensive effect of diuretics.
Xefokam reduces renal clearance of digoxin.
At simultaneous application with antibiotics of group of quinolones the risk of development of a convulsive syndrome increases.
When used simultaneously with other NSAIDs or GCS, the risk of bleeding from the gastrointestinal tract increases.
Xefokam increases the concentration of methotrexate in the serum.
When used simultaneously with selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline), the risk of bleeding from the gastrointestinal tract increases.
Xefokam is able to cause an increase in Cmax of lithium in plasma and, thereby, enhance the known side effects of lithium.
Xefokam increases the nephrotoxicity of cyclosporine.
Xefokam is able to enhance the hypoglycemic effect of sulfonylurea derivatives.
With the simultaneous use of Xephocam with corticotropin, potassium preparations, alcohol, the risk of GIT side effects increases.
With the simultaneous use of Xephocam with cefamandole, cefoperazone, cefotetan, valproic acid, the risk of bleeding increases.
With simultaneous application with tacrolimus, the risk of nephrotoxicity increases.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of the reach of children, protected from light at a temperature of no higher than 25 В° C. Shelf life of the lyophilisate is 5 years, the solvent (water for injection) is 5 years.
The prepared solution should be used within 24 hours.