Naisylate tablets 600mg, No. 20

• Rheumatoid arthritis;

• osteoarthritis;

• ankylosing spondylitis;

• articular syndrome with exacerbation of gout;

• bursitis; tenosynovitis.

  Pain syndrome (mild to moderate intensity):

• arthralgia;

• myalgia;

• neuralgia;

• migraine;

• toothache and headache;

• algodismenorrhea;

• pain with injuries, burns.

Designed for symptomatic therapy, reducing pain and inflammation at the time of use; does not affect the progression of the disease.

Inside. To preserve the gastroprotective effect of the drug, amtolmetin guacil should be taken on an empty stomach.

The recommended dose of amtolmetin guacil is 600 mg 2 times a day. 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.

Film-coated tablets from white to almost white, capsule-shaped, with a characteristic odor.

1 tab.

amtolmetin guacil 600 mg

Excipients: lactose monohydrate - 40.1 mg, hypromellose (15 cps) - 6 mg, lactose monohydrate (Flowlac 100) - 120.3 mg, colloidal silicon dioxide - 1.6 mg, sodium carboxymethyl starch (type A) - 24 mg, magnesium stearate - 8 mg ...

• Hypersensitivity to amtolmetin, tolmetin;

• complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including history);

• erosive and ulcerative changes in the mucous membrane of the stomach and duodenum;

• active gastrointestinal bleeding;

• cerebrovascular or other bleeding;

• inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the acute phase;

• hemophilia and other blood clotting disorders;

• decompensated heart failure;

• liver failure or active liver disease;

• severe renal failure (Cl creatinine less than 30 ml / min), progressive kidney disease, confirmed hyperkalemia;

• period after coronary artery bypass grafting;

• arterial hypertension;

• congenital lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

• deficiency of glucose-6-phosphate dehydrogenase;

• pregnancy;

• lactation period;

• children under 18 years of age.

With care: hyperbilirubinemia; chronic heart failure; coronary heart disease; cerebrovascular diseases; dyslipidemia / hyperlipidemia; diabetes; peripheral arterial disease; smoking; chronic renal failure (Cl creatinine 30-60 ml / min); history of ulcerative lesions of the gastrointestinal tract; presence of H. pylori infection; long-term use of NSAIDs; alcoholism; severe somatic diseases; elderly age; simultaneous administration of oral corticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), SSRIs (including citalopram, fluoxetine, paroxetine, sertraline ).

pharmachologic effect

NSAIDs, non-selective COX inhibitor. Amtolmetin guacil is a precursor to tolmetin. Has anti-inflammatory, analgesic, antipyretic, desensitizing effect, has a gastroprotective effect. Suppresses pro-inflammatory factors, reduces platelet aggregation; inhibits COX-1 and COX-2, disrupts the metabolism of arachidonic acid, 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 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.Affects thalamic pain centers; 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 range of motion 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 amtolmetin guacil, it can stimulate capsaicin receptors, which, in turn, causes the release of the peptide encoded by the calcitonin gene (PCGC), and a subsequent increase in the production of nitric oxide (NO). Both of these actions counterbalance the negative effect caused by decreased prostaglandin levels due to COX inhibition. Amtolmetin guacil was well tolerated by patients with prolonged use (within 6 months).

Pharmacokinetics

Absorption and distribution

Absorption of amtolmetin 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 administration. The time to reach Cmax after oral administration is 20-60 minutes.

Plasma protein binding - 99%.

Metabolism

After absorption of amtolmetin, guacil immediately undergoes hydrolysis by blood plasma esterases with the formation of three metabolites: MED5, tolmetin and guiacol, which are transformed to the active metabolite of tolmetin, the latter penetrates into tissues, exerting a pharmacological effect. The main metabolic pathway of tolmetin is the oxidation of the methyl group at the benzene ring to the carboxyl one.

Withdrawal

T1 / 2 in adults - about 5 hours. Within 24 hours, the drug is almost completely excreted from the body in the form of glucuronides (with urine - 80%, with bile - 20%).

Side effect

From the digestive system: often - nausea; infrequently - dyspepsia, discomfort in the stomach and intestines, bloating; rarely - abdominal pain, diarrhea, vomiting, constipation, gastritis; very rarely - peptic ulcer, liver dysfunction.

From the urinary system: the frequency is unknown - an increase in the content of urea nitrogen in the blood, urinary tract infections.

From the side of the organ of vision: rarely - visual impairment.

On the part of the organ of hearing and labyrinth disorders: rarely - tinnitus.

From the respiratory system: rarely - bronchospasm, shortness of breath, rhinitis, laryngeal edema.

From the nervous system: often - dizziness, headache, drowsiness; rarely, depression.

From the side of the cardiovascular system: often - increased blood pressure.

From the side of hematopoiesis: rarely - anemia, thrombocytopenia, agranulocytosis, leukopenia.

From the side of the skin: infrequently - skin rash (including maculopapular rash), purpura; rarely - exfoliative dermatitis (fever with or without chills, redness, thickening or peeling of the skin, swelling and / or soreness of the tonsils), urticaria, Stevens-Johnson syndrome, Lyell's syndrome.

From the immune system: rarely - anaphylaxis or anaphylactoid reactions (discoloration of the face, skin rash, urticaria, itching of the skin, tachypnea or dyspnea, eyelid edema, periorbital edema, shortness of breath, shortness of breath, heaviness in the chest, wheezing).

Others: often - weakness; infrequently - edema (of the face, legs, ankles, fingers, feet, weight gain); rarely - increased sweating, fever, lymphadenopathy; very rarely - swelling of the tongue.

Application during pregnancy and lactation

The safety of using the drug during pregnancy and during breastfeeding has not been established.

The drug is contraindicated during pregnancy and lactation.

Application for violations of liver function

Contraindicated in liver failure or active liver disease.

Application for impaired renal function

Contraindicated in severe renal failure (CC less than 30 ml / min), progressive kidney disease.

Precautions should be taken in chronic renal failure (CC 30-60 ml / min).

Application in children

It is contraindicated for use in children and adolescents under 18 years of age.

Use in elderly patients

The drug should be prescribed with caution to elderly patients.

special instructions

During treatment, it is necessary to control 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.

Influence on the ability to drive vehicles and mechanisms

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

Overdose

Symptoms: abdominal pain, nausea, vomiting, erosive and ulcerative lesions of the gastrointestinal tract, renal dysfunction, metabolic acidosis.

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

Drug interactions

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.

Enhances the hypoglycemic effect of sulfonylurea derivatives, the action of anticoagulants, antiplatelet agents, fibrinolytics, side effects of estrogens, glucocorticoids and mineralocorticoids.

Antacids and cholestyramine reduce absorption.

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

In some patients with impaired renal function, the combined use of NSAIDs and ACE inhibitors can lead to further deterioration of renal function.

Myelotoxic drugs increase the manifestations of the drug's hematotoxicity.