Ksefokam Rapid pills 8mg №12

Ksefokam Rapid

Clinico-pharmacological group

NSAIDs

Mechanism of action

NSAIDs. It has a pronounced analgesic and anti-inflammatory effect. Lornoxicam has a complex mechanism of action, which is based on the suppression of the synthesis of prostaglandins, due to the inhibition of the activity of isoenzymes COX-1 and COX-2 both in the focus of inflammation and in healthy tissues. In addition, lornoxicam inhibits the release of oxygen free radicals from activated leukocytes.

The analgesic effect of lornoxicam is not associated with opioid action. Ksefokam Rapid does not have an opiate-like effect on the central nervous system and, unlike narcotic analgesics, does not inhibit respiration and does not cause drug dependence.

Pharmacokinetics

Suction

Lornoxicam is rapidly and almost completely absorbed from the gastrointestinal tract.

C_max in plasma is achieved within 1-2 hours after ingestion. C_max lornoxicam in the blood plasma when using the drug Ksefokam Rapid is higher than when using the drug Ksefokam pill and is equivalent to C_max for dosage forms of lornoxicam, intended for paranteral administration. Absolute bioavailability for Ksefokam Rapid pills is 90-100% and is equivalent to the bioavailability of the drug Ksefokam tablets.The effect of "first pass" through the liver is not observed.

Simultaneous intake of lornoxicam with food reduces C_max in plasma by 30%. Time to reach C_max increases from 1.5 hours to 2.3 hours. Lornoxicam absorption (calculated by AUC) can be reduced to 20%.

Distribution

The binding of lornoxicam to plasma proteins is 99% and does not depend on its concentration.

Lornoxicam does not accumulate after repeated administration in recommended doses.

Metabolism

In plasma, lornoxicam is found unchanged and in the form of its hydroxylated metabolite. Hydroxylated metabolite does not show pharmacological activity. Lornoxicam is completely metabolized to form a pharmacologically inactive metabolite.

Lornoxicam (like Diclofenac and other oxycam) undergoes metabolism with the participation of the CYP2C9 isoenzyme. As a result of genetic polymorphism, there are persons with slow and intense metabolism, which can be expressed in a noticeable increase in plasma concentration of lornoxicam in individuals with a slow metabolism. Lornoxicam does not induce hepatic enzymes.

Removal

T_1/2 is 3-4 hours

About 2/3 of the dose is excreted through the liver and 1/3 by the kidneys.

Pharmacokinetics in special clinical situations

Simultaneous administration with antacids has no effect on the pharmacokinetics of lornoxicam. In elderly people, systemic clearance is reduced by 30-40%. In patients with impaired liver or kidney function, no significant changes in the pharmacokinetics of lornoxicam are observed.

Indications for use of the drug

- short-term treatment of pain in injuries and after surgical interventions;

- Algomenorrhea;

- lumboischialgia;

- symptomatic therapy of rheumatoid arthritis and osteoarthritis.

Dosage and administration

The pills of the drug Ksefokam Rapid is taken orally with a sufficient amount of liquid.

Special dose selection for elderly patients is not required in the absence of renal impairment or liver function; in the presence of renal or hepatic insufficiency, the daily dose of the drug should be reduced.

For all patients, the dosing regimen should be based on an individual response to treatment.

Ksefokam Rapid should be prescribed in a dose of 8 mg, the maximum daily dose - 16 mg.

Side effect

Frequency of side effects: often (≥1% and <10%), rarely (<1%).

Gastrointestinal: often - abdominal pain, diarrhea, dyspepsia, nausea, vomiting; rarely - constipation, dysphagia, dry mouth, flatulence, gastritis, gastroesophageal reflux, peptic ulcers, Gastrointestinal bleeding, stomatitis, hemorrhoidal bleeding, increased activity of hepatic transaminases and alkaline phosphatase, worsening appetite.

About 16% of patients (in the case of long-term treatment, 20-25% of patients) may experience adverse reactions associated with the gastrointestinal tract.

Hemic and lymphatic: rarely - changes in blood counts, abnormal blood changes, leukopenia, thrombocytopenia, increased bleeding time, anemia, a decrease in the number of red blood cells, hemoglobin and white blood cells.

Cardiovascular: rarely - swelling, increase or decrease in blood pressure, palpitations, tachycardia.

Nervous system: often - dizziness, headache; sometimes - insomnia, indisposition, weakness, hot flashes; rarely - drowsiness, paresthesia, tremor, taste disturbances, agitation, depression.

Respiratory: rarely - shortness of breath, bronchospasm, cough, rhinitis.

Urogenital: rarely, an increase in the urea nitrogen and creatinine levels in the blood, urinary disturbances, interstitial nephritis, glomerulonephritis, tubular necrosis of the kidneys, or nephrotic syndrome.

Musculoskeletal system: rarely - myalgia, cramps of the muscles of the legs.

Special senses: rarely - conjunctivitis, visual disturbances, tinnitus.

Dermatologic: rarely - skin rash, bullous rash, eczema, polymorphic erythema, erythroderma (exfoliative dermatitis), alopecia, photosensitization, purpura.

Allergic reactions: rarely - bronchospasm, urticaria, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), allergic purpura, systemic Anaphylactic reactions (including shock).

Other: rarely a change in body weight.

Contraindications to the use of the drug

- gastrointestinal bleeding;

- hemorrhage in the brain (including suspicion);

- active peptic ulcer or recurrent peptic ulcer in history;

- severe liver failure;

- renal failure severe (serum creatinine level> 700 mcmol / l);

- severe thrombocytopenia;

- severe heart failure and hypovolemia;

- pregnancy;

- lactation period (breastfeeding);

- children's and teenage age up to 18 years (due to insufficient clinical experience);

- hypersensitivity to lornoxicam or other components of the drug;

- hypersensitivity to other NSAIDs, including Acetylsalicylic acid.

Carefully and only after a thorough assessment of the expected benefit of therapy and possible risk should the drug be prescribed with indications of a history of gastrointestinal ulcers and bleeding, renal failure, blood clotting disorders, liver diseases (for example, liver cirrhosis), for a long time (more than months), elderly patients (65 years and older), as well as patients with body weight less than 50 kg and after surgery.

Use of the drug during pregnancy and lactation

The drug is contraindicated in pregnancy and lactation (breastfeeding).

Application for violations of the liver

The drug is contraindicated in severe liver failure. WITH caution and only after a thorough assessment of the expected benefit of therapy and possible risk should the drug be prescribed for indications of a history of liver disease (for example, in liver cirrhosis).

Application for violations of kidney function

The drug is contraindicated in severe renal failure (serum creatinine level> 700 μmol / l). Carefully and only after a thorough assessment of the expected benefits of therapy and possible risk should the drug be prescribed for impaired renal function.

Special notes

Patients with a history of ulcerative lesions of the gastrointestinal tract or bleeding from the gastrointestinal tract during treatment with Ksefokam Rapid are recommended to conduct clinical observation at regular periods of time. If a peptic ulcer and / or gastrointestinal bleeding has developed in a patient during Xefocam Rapid's intake, it is necessary to discontinue the drug and administer the appropriate therapy.

Patients with mild severity of renal insufficiency (serum creatinine level 150-300 mcmol / l) should be examined quarterly, patients with moderately severe renal insufficiency (serum creatinine level 300-700 mcmol / l) should be examined at intervals of 1-2 months. If renal function deteriorates, treatment with Ksefokam Rapid should be discontinued.

When used in patients with coagulation disorders, careful clinical observation and evaluation of laboratory parameters (for example, prothrombin index) is recommended.

In liver diseases (for example, in liver cirrhosis), it is recommended that clinical observation and evaluation of laboratory parameters (for example, liver enzyme activity) be carried out at regular intervals.

With long-term treatment (more than 1 month), it is recommended to regularly assess the blood condition (hemoglobin level), kidney function (serum creatinine level) and liver enzyme activity.

When using the drug in elderly patients (65 years and older), as well as in patients with a body weight less than 50 kg and after surgery, it is recommended to monitor the function of the kidneys and liver.

It is important to monitor renal function in patients who have undergone extensive surgery; in violation of renal function (for example, as a result of significant blood loss or pronounced dehydration of the body); with heart failure; with simultaneous therapy with diuretics, as well as receiving drugs at the same time that are suspected or known to cause kidney damage.

It should be borne in mind that the drug increases the risk of spinal / epidural hematoma during spinal or epidural anesthesia.

The simultaneous appointment of histamine H blockers₂-receptors, Omeprazole, prostaglandins synthetic analogues can reduce the risk of ulcerogenic action of lornoxicam.

If necessary, determine the 17-ketosteroids Ksefokam Rapid should be canceled 48 hours before the study.

During the period of treatment, the patient should refrain from drinking alcohol.

Influence on ability to drive motor transport and control mechanisms

During the period of treatment, patients should refrain from activities that require high concentration of attention and quickness of psychomotor reactions.

Overdose

Symptoms: nausea and vomiting, cerebral symptoms (dizziness, ataxia, passing into a coma and convulsions), impaired liver and kidney function, impaired blood coagulation.

Treatment: With an established or suspected overdose, the drug should be discontinued. Thanks to a small t_1/2 Lornoxicam is rapidly excreted from the body. Lornoxicam is not displayed during dialysis. To date, the specific antidote is not known. It is necessary to provide for the conduct of the usual emergency measures, including gastric lavage. On the basis of general principles, it is possible to use Activated carbon only if it is taken immediately after taking the drug Ksefokam Rapid, which may lead to a decrease in the absorption of lornoxicam.

Drug interaction

At the same time taking the drug Ksefokam Rapid with anticoagulants and inhibitors of platelet aggregation may increase the bleeding time (increased risk of bleeding); with sulfonylurea derivatives - hypoglycemic effect may increase; with other NSAIDs - increased risk of adverse reactions.

At the same time taking Ksefokam Rapid reduces the effectiveness of "loop" diuretics; may reduce the effect of ACE inhibitors.

With simultaneous use with lithium preparations, it is possible to increase the maximum concentration of lithium and, therefore, it is possible to enhance the undesirable effects caused by lithium.

Ksefokam Rapid increases the concentration of Methotrexate and cyclosporine in serum.

When taken simultaneously with cimetidine, an increase in plasma concentration of lornoxicam is observed (no interaction between Ksefokam Rapid and Ranitidine or Ksefokam Rapid and antacids was detected).

Ksefokam Rapid reduces renal clearance of Digoxin.

Inductors of microsomal enzymes (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) reduce plasma concentration of lornoxicam, inhibitors of microsomal enzymes may increase the severity of side effects.

Terms and conditions of storage

The drug should be stored out of the reach of children at a temperature of 18 ° to 30 ° C.