Niselat, pills 600 mg 20 pcs.

Composition

Each film-coated tablet contains:Active ingredient: amtolmetin guacil 600 mg; Excipients: lactose monohydrate 40.1 mg, Hypromellose (15 cps) 6.0 mg, lactose monohydrate (Flowlac 100) 120.3 mg, colloidal silicon dioxide 1.6 mg, sodium carboxymethyl starch (Type-A) 24.0 mg, magnesium stearate 8.0 mg; Film coated:Hypromellose (5 cps) 12.5 mg, titanium dioxide 6.25 mg, macrogol-400 1.25 mg

. Pharmacological action

PharmacodynamicAmtolmetin guacil is a non-steroidal anti-inflammatory drug (NSAID), a non-selective cyclooxygenase (COX) inhibitor. Amtolmetin guacil is a precursor to tolmetin. It has an anti-inflammatory, analgesic, antipyretic, desensitizing effect, has a gastroprotective effect. Suppresses pro-inflammatory factors, reduces platelet aggregation; inhibits COX-1 and COX-2, disrupts arachidonic acid metabolism, reduces the formation of prostaglandins (including in the focus of inflammation), suppresses the exudative and proliferative phases of inflammation. Reduces capillary permeability; stabilizes lysosomal membranes; inhibits the synthesis or inactivates inflammatory mediators (prostaglandins, histamine, bradykinins, cytokines, complement factors). Blocks the interaction of bradykinin with tissue receptors, restores disturbed microcirculation and reduces pain sensitivity in the focus of inflammation. It affects the thalamic centers of pain sensitivity; reduces the concentration of biogenic amines with algogenic properties; increases the threshold of pain sensitivity of the receptor apparatus. Eliminates or reduces the intensity of pain, reduces morning stiffness and swelling, increases the amount of movement in the affected joints after 4 days of treatment. The protective effect of amtolmetin guacil on the gastric mucosa is realized by stimulating capsaicin receptors (also called vanilloid receptors) present in the walls of the gastrointestinal tract. Due to the presence of a vanillin group in the composition of amtolmetin guacil, it can stimulate capsaicin receptors, which in turn causes the release of a peptide encoded by the calcitonin gene (PCHA), and the subsequent increase in nitric oxide (NO) production. Both of these actions counterbalance the negative effect caused by a decrease in the number of prostaglandins due to COX inhibition. Amtolmetin guacil was well tolerated by patients with prolonged use (for 6 months). Pharmacokineticsabsorption of amtolmetine guacil after oral administration is rapid and complete. Basically, the drug is concentrated in the walls of the stomach and intestines, where a very high concentration is maintained for 2 hours after ingestion. After absorption, amtolmetin guacil is immediately hydrolyzed by plasma esterases to form three metabolites: MED-5, tolmetin and guiacol, which are transformed to the active metabolite of tolmetin, which penetrates the tissues, having a pharmacological effect. The main route of tolmetin metabolism is the oxidation of the methyl group at the benzene ring to the carboxyl group. The time to reach the maximum concentration (TCmax) after oral administration is 20-60 minutes. Binding to plasma proteins is 99%. The half-life (T1/2) in adults is about 5 hours. Within 24 hours, the drug is almost completely eliminated from the body in the form of glucuronides (with urine-80%, with bile-20%).

Indications

Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, joint syndrome with gout exacerbation, bursitis, tendovaginitis. Pain syndrome (mild to moderate intensity): arthralgia, myalgia, neuralgia, migraine, tooth and headache, algodismenorrhea; pain from injuries, burns. It is intended for symptomatic therapy, reducing pain and inflammation at the time of use, and does not affect the progression of the disease.

Use during pregnancy and lactation

The safety of using the drug during pregnancy or during breastfeeding has not been established. The drug is contraindicated during pregnancy and lactation.

Contraindications

Hypersensitivity to amtolmetin, tolmetin; complete or incomplete combination of bronchial asthma, recurrent nasal or paranasal sinus polyposis and intolerance to acetylsalicylic acid and other NSAIDs (including in the anamnesis); erosive and ulcerative changes in the gastric and duodenal mucosa, active gastrointestinal bleeding; cerebrovascular or other bleeding; inflammatory bowel diseases (Crohn’s disease, ulcerative colitis). colitis) in the acute phase; hemophilia and other blood clotting disorders; decompensated heart failure; liver failure or active liver disease; severe renal failure (creatinine clearance less than 30 ml/min), progressive kidney disease, confirmed hyperkalemia; the period after aorto-coronary bypass surgery; arterial hypertension; congenital lactase deficiency, lactose intolerance, glucose-galactose malabsorption; deficiency of glucose-galactose glucose-6-phosphate dehydrogenase; pregnancy, lactation, children under 18 years of age. With caution:Hyperbilirubinemia, chronic heart failure, ischemic heart disease, cerebrovascular diseases, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial diseases, smoking, chronic renal failure (creatinine clearance 30-60 ml/min), a history of gastrointestinal ulcers, H. pulori infection, long-term use of NSAIDs, alcoholism, severe somatic diseases, old age, concomitant use of the drug oral glucocorticosteroids (including prednisone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline).

Side effects

The frequency of side effects is classified according to the frequency of occurrence of the case: common (1-10%); infrequent (0.1-1%); rare (0.01-0.1%); very rare (less than 0.01%), including individual reports and the frequency is unknown. Gastrointestinal disorders: often – nausea; infrequently-dyspepsia, stomach and intestinal discomfort, bloating; rarely-abdominal pain, diarrhea, vomiting, constipation, gastritis; very rarely-peptic ulcer, liver function disorders. Renal and urinary tract disorders: frequency unknown-increased blood urea nitrogen, urinary tract infections. Visual disturbances: rarely-visual disturbances. Hearing disorders and labyrinth disorders: rarely-tinnitus. Respiratory, thoracic and mediastinal disorders: rarely-bronchospasm, shortness of breath, rhinitis, laryngeal edema. Nervous system disorders: often – dizziness, headache, drowsiness; rarely-depression. Vascular disorders: often-an increase in blood pressure. Disorders of the blood and lymphatic system: rarely-anemia, thrombocytopenia, agranulocytosis, leukopenia. Skin and subcutaneous tissue disorders: infrequently-skin rash (including maculopapular rash), purpura, rarely-exfoliative dermatitis (fever with or without chills, redness, tightness or peeling of the skin, swelling and / or soreness of the palatine tonsils), urticaria, Stevens-Johnson syndrome, Lyell’s syndrome. Immune system disorders: rarely – anaphylaxis or anaphylactoid reactions (discoloration of the skin of the face, skin rash, urticaria, itchy skin, tachypnea or dyspnea, edema of the eyelids, periorbital edema, shortness of breath, difficulty breathing, heaviness in the chest, wheezing). General disorders: often-weakness; infrequently-swelling (face, shins, ankles, fingers, feet, weight gain); rarely – increased sweating, fever, lymphadenopathy; very rarely – swelling of the tongue.

Interaction

Inducers of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites.

Reduces the effectiveness of uricosuric, antihypertensive drugs and diuretics.

Increases the hypoglycemic effect of sulfonylureas, anticoagulants, antiplatelet agents, fibrinolytics, side effects of estrogens, corticosteroids and mineralocorticoids.

Antacids and colestyramine reduce absorption.

Increases the concentration of lithium and methotrexate preparations in the blood.

In some patients with impaired renal function, concomitant use of NSAIDs and ACE inhibitors may lead to further deterioration of renal function.

Myelotoxic drugs increase the manifestations of hematotoxicity of the drug.

How to take it, course of administration and dosage

The recommended dose of amtolmetin guacil is 600 mg twice daily.

Depending on the degree of control of the symptoms of the disease, the maintenance dose can be reduced to 600 mg once a day. The maximum daily dose is 1800 mg.

To preserve the gastroprotective effect of Naizilat®, it should be taken on an empty stomach.

Overdose

Symptoms:

abdominal pain, nausea, vomiting, erosive and ulcerative lesions of the gastrointestinal tract, impaired renal function, metabolic acidosis.

Treatment:

gastric lavage, administration of adsorbents (activated charcoal) and symptomatic therapy (maintenance of vital body functions). There is no specific antidote.

Special instructions

During treatment with Naisilate, it is necessary to monitor the picture of peripheral blood and the functional state of the liver and kidneys.

Treatment should be discontinued 48 hours prior to the determination of 17-ketosteroids.

During treatment, you should refrain from engaging in potentially dangerous activities that require increased attention and speed of mental and motor reactions.

Form of production

Tablets

Storage conditions

At a temperature not exceeding 25 °C. Keep out of reach of children!

Shelf life

2 years

Active ingredient

Amtolmetin guacil

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Osteoarthritis, Lumbago, Arthritis, Sciatica

Weight

Weight: 30 gr.