Nisylat 600 mg n20 film-coated tablets

Pharmacodynamics and pharmacokinetics

Pharmacodynamics of amtolmetin guacil

Non-steroidal anti-inflammatory drug, non-selective cyclooxygenase , precursor of tolmetin in the metabolic chain. Suppresses platelet ; blocks cyclooxygenase of the first and second types, changes the metabolism of arachidonic acid , reduces the synthesis of prostaglandins , inhibits the exudative and proliferative phases of the inflammatory process. Impairs capillary ; normalizes lysosomal membranes; slows down the biosynthesis or inactivates inflammatory mediators ( histamine, prostaglandins, bradykinins, complement factors, cytokines ).

Blocks the reaction of bradykinin with tissue receptors, reduces pain in the area of ​​inflammation. Affects the thalamic centers responsible for pain sensitivity; reduces the content of biogenic amines that exhibit algogenic properties. Eliminates the intensity of pain, reduces morning stiffness, increases the range of motion in the joints four days after the start of treatment. The protective effect of amtolmetin guacil on the gastric mucosa is achieved by activating capsaicin in the walls of the digestive tract. This is accompanied by an increase in nitric oxide synthesis and creates a counterbalance to the negative effect of cyclooxygenase .

Pharmacokinetics

Absorption after administration is usually rapid and complete. The drug accumulates in the walls of the digestive tract, where its high concentration is maintained for 2 hours. Metabolized by undergoing hydrolysis blood esterases MED5, guaiacol and tolmetin , which are converted into tolmetin (active metabolite), which has a pharmacological effect in tissues. Binds to plasma proteins by 99%. The half-life is 5 hours. After 24 hours, the drug is completely excreted in the urine (80%) and bile (20%).

Naisilate (600mg)

INSTRUCTIONS for the use of the medicinal product for medical use NAYSILAT

Registration number: LP-001588 Trade name of the drug: Naysylat International nonproprietary name of the drug: amtolmetin guacil. Dosage form: film-coated tablets. Composition Each film-coated tablet contains: Active substance: 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 coating: hypromellose (5 pps) 12.5 mg, titanium dioxide 6.25 mg, macrogol-400 1.25 mg. Description Capsule-shaped tablets, film-coated, white to almost white in color, with a characteristic odor. Pharmacotherapeutic group: non-steroidal anti-inflammatory drug. ATC code: M01AB Pharmacological properties Pharmacodynamics Amtolmetin guacil is a non-steroidal anti-inflammatory drug (NSAID), a non-selective cyclooxygenase (COX) inhibitor. Amtolmetin guacil is a precursor to tolmetin. It has anti-inflammatory, analgesic, antipyretic, desensitizing effects, and 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 at the site 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 impaired microcirculation and reduces pain sensitivity at the site of inflammation. Affects the thalamic centers of pain sensitivity; reduces the concentration of biogenic amines with algogenic properties; increases the pain sensitivity threshold 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 capsaitin receptors, which in turn causes the release of calcitonin gene-encoded peptide (CAGP) and a subsequent increase in nitric oxide (NO) production. Both of these actions counterbalance the negative effect caused by the decrease in prostaglandins due to COX inhibition. Amtolmetin guacil was well tolerated by patients with long-term use (for 6 months). Pharmacokinetics Absorption of amtolmetin guacil after oral administration is rapid and complete. The drug is mainly concentrated in the walls of the stomach and intestines, where its very high concentration is maintained for 2 hours after administration. After absorption, amtolmetin guacil is immediately hydrolyzed by plasma esterases to form three metabolites: MED-5, tolmetin and guacol, which are transformed to the active metabolite tolmetin, which penetrates the tissues, exerting a pharmacological effect. The main metabolic pathway of tolmetin is the oxidation of the methyl group on the benzene ring into a carboxyl group. Time to reach maximum concentration (TCmax) after oral administration is 20-60 minutes. Communication with plasma proteins – 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 for use: Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, articular syndrome with exacerbation of gout, bursitis, tenosynovitis. Pain syndrome (weak and moderate intensity): arthralgia, myalgia, neuralgia, migraine, toothache and headache, algomenorrhea; pain from injuries, burns. Intended for symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease. Contraindications for use 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 a history); erosive and ulcerative changes in the mucous membrane of the stomach and duodenum, active gastrointestinal bleeding; cerebrovascular or other bleeding; inflammatory bowel diseases (Crohn's disease, ulcerative colitis) in the acute phase; hemophilia and other bleeding 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; period after coronary artery bypass surgery; 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. Precautions for use Hyperbilirubinemia, chronic heart failure, coronary heart disease, cerebrovascular diseases, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, chronic renal failure (creatinine clearance 30-60 ml/min), ulcerative lesions of the gastrointestinal tract history, presence of H. pulori infection, long-term use of NSAIDs, alcoholism, severe somatic diseases, old age, simultaneous use of oral glucocorticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel ), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline).

Method of administration and dosage The recommended dose of amtolmetin guacil is 600 mg twice a day. Depending on the degree of control of the symptoms of the disease, the maintenance dose may be reduced to 600 mg once daily. The maximum daily dose is 1800 mg. To maintain the gastroprotective effect of the drug, Naysylat should be taken on an empty stomach. Possible side effects when using the drug The frequency of side effects is classified depending on the frequency of occurrence of the case: often (1-10%), infrequently (0.1-1%), rarely (0.01-0.1%), very rarely (less than 0.01%), including individual messages. From the digestive system: often – nausea; uncommon – 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: increased urea nitrogen in the blood, urinary tract infections From the senses: rarely - tinnitus, visual impairment. From the respiratory system: rarely - bronchospasm, shortness of breath, rhinitis, laryngeal edema. From the central nervous system: often – dizziness, headache, drowsiness; rarely – depression. From the cardiovascular system: often - increased blood pressure. From the hematopoietic organs: rarely - anemia, thrombocytopenia, agranulocytosis, leukopenia. From the skin: uncommon – skin rash (including maculopapular rash), purpura, rare – exfoliative dermatitis (fever with or without chills, redness, thickening or peeling of the skin, swelling and/or tenderness of the tonsils), urticaria, Stevens-Johnson syndrome , Lyell's syndrome. Allergic reactions: rarely - anaphylaxis or anaphylactoid reactions (change in facial skin color, skin rash, urticaria, itching of the skin, tachypnea or dyspnea, swelling of the eyelids, periorbital edema, shortness of breath, difficulty breathing, heaviness in the chest, wheezing). Other: often – weakness; uncommon – swelling (face, legs, ankles, fingers, feet, weight gain); rarely – increased sweating, fever, lymphadenopathy; very rarely - swelling of the tongue. Symptoms of overdose, measures to assist in case of 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 carbon) and symptomatic therapy (maintaining vital body functions). There is no specific antidote. Interaction with other drugs and (or) foods 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 effect of anticoagulants, antiplatelet agents, fibrinolytics, side effects of estrogens, glucocorticosteroids and mineralcorticoids. Antacids and cholestyramine reduce absorption. Increases the concentration of lithium and methotrexate in the blood. In some patients with impaired renal function, co-administration of NSAIDs and angiotensin-converting enzyme (ACE) inhibitors may result in further deterioration of renal function. Myelotoxic drugs increase the manifestations of hematotoxicity of the drug. Special instructions During treatment, it is necessary to monitor the peripheral blood picture and the functional state of the liver and kidneys. Treatment should be stopped 48 hours before determination of 17-ketosteroids. During treatment, you should refrain from engaging in potentially hazardous activities that require increased attention and speed of mental and motor reactions. Release form: Film-coated tablets, 600 mg. 10 tablets per blister made of opaque PVC/PVDC film/aluminum foil. 2 blisters along with instructions for use in a cardboard pack. Storage conditions: In a dry place, protected from light, at a temperature not exceeding 25 °C. Keep out of the reach of children! Shelf life: 2 years. Do not use after the expiration date stated on the packaging. Conditions for dispensing from pharmacies By prescription. Manufacturer Dr. Reddy's Laboratories Ltd. Hyderabad, Andhra Pradesh, India. Address of the place of production Plots 42, 45 and 46, Bachupally Village, Qutbullapur Mandal, Ranga Reddy District, Andhra Pradesh, India.

Send consumer complaints to the following address: Representative office of Dr. Reddy's Laboratories Ltd.: 115035, Moscow, Ovchinnikovskaya embankment, 20, building 1 tel. 783-29-01 fax

Indications for use

• osteoarthritis;
• rheumatoid arthritis;
• ankylosing spondylitis;
• bursitis;
• articular syndrome due to gout;
• tenosynovitis;
• arthralgia;
• pain syndrome;
• myalgia;
• migraine;
• neuralgia;
• headache and toothache;
• algodismenorrhea;
• pain from burns and injuries.

Contraindications

• Allergy to tolmetin, amtolmetin.
• The presence of bronchial asthma , allergy to Aspirin or recurrent polyposis.
• Ulcerative lesions of the mucous membranes of the stomach and duodenum .
• Gastrointestinal bleeding in the active phase.
• Cerebrovascular bleeding.
• Blood clotting disorder.
• Inflammatory bowel diseases ( ulcerative colitis, Crohn's disease ) in the acute phase.
• Heart failure in the stage of decompensation.
• Severe damage to the liver and kidneys.
• Arterial hypertension.
• Postoperative period of coronary artery bypass grafting.
• Lactose intolerance , deficiency , glucose-galactose malabsorption .
• Pregnancy and lactation .
• Age less than 18 years.

Use with caution when:

• hyperbilirubinemia;
• coronary heart disease;
• chronic heart failure;
• cerebrovascular diseases;
• diabetes mellitus;
• lesions of peripheral arteries;
• chronic renal failure;
• in old age.

Buy Nisylat film-coated tablets 600 mg No. 20 in pharmacies

Instructions for use Nizilat Dosage forms tablets 600 mg Synonyms There are no synonyms. Group Nonsteroidal anti-inflammatory drugs International nonproprietary name Amtolmetin guacil Manufacturers Dr. Reddis Laboratories Ltd. (India) Pharmacological action Amtolmetin guacil is a NSAID, a non-selective cyclooxygenase (COX) inhibitor. Amtolmetin guacil is a precursor to tolmetin. It has an anti-inflammatory, analgesic, antipyretic, desensitizing effect, and 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 at the site 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 impaired microcirculation and reduces pain sensitivity at the site of inflammation. Affects the thalamic centers of pain sensitivity; reduces the concentration of biogenic amines with algogenic properties; increases the pain sensitivity threshold 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 calcitonin gene-encoded peptide (CAGP) and a subsequent increase in nitric oxide (NO) production. Both of these actions counterbalance the negative effect caused by the decrease in prostaglandins due to COX inhibition. Amtolmetin guacil was well tolerated by patients with long-term use (for 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 its 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, amtolmetin guacil is immediately hydrolyzed by plasma esterases to form three metabolites: MED5, tolmetin and guacol, which are transformed to the active metabolite tolmetin, which penetrates the tissues, exerting a pharmacological effect. The main metabolic pathway of tolmetin is the oxidation of the methyl group at the benzene ring into a carboxyl group.

Removal

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; articular syndrome during exacerbation of gout; bursitis; Tenosynovitis. Pain syndrome (mild to moderate intensity):

arthralgia; myalgia; neuralgia; migraine; toothache and headache; algodismenorrhea; pain from injuries, burns. Intended for symptomatic therapy, reducing pain and inflammation at the time of use; does not affect the progression of the disease.

Contraindications: hypersensitivity to amtolmetin, tolmetin; complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including a history); erosive and ulcerative changes in the mucous membrane of the stomach and duodenum; active gastrointestinal bleeding; cerebrovascular or other bleeding; inflammatory bowel diseases (Crohn's disease, ulcerative colitis) in the acute phase; hemophilia and other bleeding disorders; decompensated heart failure; liver failure or active liver disease; severe renal failure (creatinine Cl less than 30 ml/min), progressive kidney disease, confirmed hyperkalemia; period after coronary artery bypass surgery; 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 caution: hyperbilirubinemia; chronic heart failure; cardiac ischemia; cerebrovascular diseases; dyslipidemia/hyperlipidemia; diabetes; peripheral arterial disease; smoking; chronic renal failure (Clcreatinine 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 use of oral corticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), SSRIs (including citalopram, fluoxetine, paroxetine, sertraline ).

Special instructions During treatment with Naysilat, monitoring of the peripheral blood picture and the functional state of the liver and kidneys is necessary. Treatment should be stopped 48 hours before determination of 17-ketosteroids. During treatment, you should refrain from engaging in potentially hazardous activities that require increased attention and speed of mental and motor reactions.

Composition Each film-coated tablet contains: Active substance: 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 coating: hypromellose (5 pps) 12.5 mg, titanium dioxide 6.25 mg, macrogol-400 1.25 mg.

Method of administration and dosage The recommended dose of Naysylat is 600 mg twice a day. Depending on the degree of control of the symptoms of the disease, the maintenance dose may be reduced to 600 mg once daily. The maximum daily dose is 1800 mg. To maintain the gastroprotective effect of the drug, Naysylat should be taken on an empty stomach.

Side effects From the digestive system: often - nausea; uncommon - 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: increased urea nitrogen levels in the blood, urinary tract infections.

From the senses: rarely - tinnitus, visual impairment.

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

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

From the cardiovascular system: often - increased blood pressure.

From the hematopoietic organs: rarely - anemia, thrombocytopenia, agranulocytosis, leukopenia.

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

Allergic reactions: rarely - anaphylaxis or anaphylactoid reactions (change in facial skin color, skin rash, urticaria, itching of the skin, tachypnea or dyspnea, swelling of the eyelids, periorbital edema, shortness of breath, difficulty breathing, heaviness in the chest, wheezing).

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

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 effect of anticoagulants, antiplatelet agents, fibrinolytics, side effects of estrogens, glucocorticosteroids and mineralcorticoids. Antacids and cholestyramine reduce absorption. Increases the concentration of lithium and methotrexate in the blood. In some patients with impaired renal function, co-administration of NSAIDs and angiotensin-converting enzyme (ACE) inhibitors may result in further deterioration of renal function. Myelotoxic drugs increase the manifestations of hematotoxicity of the drug. Check the interaction of other drugs with Naisylat

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 carbon) and symptomatic therapy (maintaining vital body functions). There is no specific antidote.

Storage conditions: In a dry place, protected from light, at a temperature not exceeding 25 °C.

Shelf life: 2 years.

Side effects

• From the digestive system: nausea, dyspepsia , diarrhea , vomiting, constipation, peptic ulcer.
• From the genitourinary system: urinary tract infections.
• From the side of vision and hearing: visual impairment, tinnitus.
• From the respiratory system: bronchospasm , rhinitis , shortness of breath, laryngeal edema.
• From the nervous system: dizziness , drowsiness , depression .
• From the circulatory system: increased pressure.
• From the hematopoietic system: anemia, thrombocytopenia, leukopenia.
• Skin: rash, purpura , dermatitis , urticaria , Lyell's syndrome.
• Allergic reactions: anaphylactoid reactions.

Nizilat

Nisylat, film-coated tablets 600 mg, blister 10, cardboard pack 2, No. LP-001588, 2012-03-15 from Dr. Reddy's Laboratories Ltd. (India) Last update of the description by the manufacturer 10/02/2013

•Dosage form and composition •Pharmacological action •Pharmacodynamics •Pharmacokinetics •Indications •Contraindications •Side effects •Interactions •Method of administration and dosage •Overdose •Special instructions •Form of release •Manufacturer •Dispensing conditions from pharmacies

Latin name Niselat Active ingredient Amtolmetin guacil * (Amtolmetin guacil *) ATC M01AB Derivatives of acetic acid and related compounds Pharmacological group • NSAIDs - Derivatives of acetic acid and related compounds Nosological classification (ICD-10) • G43 Migraine • K08.8.0* Toothache • M06. 9 Rheumatoid arthritis, unspecified •M10.9 Gout, unspecified •M19.9 Arthrosis, unspecified •M25.5 Joint pain •M25.9 Joint disease, unspecified •M45 Ankylosing spondylitis •M65 Synovitis and tenosynovitis •M71 Other bursopathies •M79.1 Myalgia •M79 .2 Neuralgia and neuritis, unspecified •N94.6 Dysmenorrhea, unspecified •R51 Headache •R52.2 Other persistent pain •R52.9 Pain, unspecified •T14.9 Trauma, unspecified •T30 Thermal and chemical burns, unspecified Dosage form and composition Tablets, coated film-coated 1 tab. active substance: 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 film shell: hypromellose (5 cps) - 12.5 mg, titanium dioxide - 6.25 mg, macrogol 400 - 1.25 mg Description of the dosage form Tablets: capsule-shaped, coated film coated from white to almost white in color, with a characteristic odor.

Pharmacological action Pharmacological action - desensitizing, gastroprotective, analgesic, antipyretic, anti-inflammatory. Pharmacodynamics Amtolmetin guacil is an NSAID, a non-selective COX inhibitor. Amtolmetin guacil is a precursor to tolmetin. It has anti-inflammatory, analgesic, antipyretic, desensitizing effects, and 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 PG (including at the site of inflammation), suppresses the exudative and proliferative phases of inflammation. Reduces capillary permeability, stabilizes lysosomal membranes, inhibits the synthesis or inactivates inflammatory mediators (PG, histamine, bradykinins, cytokines, complement factors). Blocks the interaction of bradykinin with tissue receptors, restores impaired microcirculation and reduces pain sensitivity at the site of inflammation. It affects the thalamic centers of pain sensitivity, reduces the concentration of biogenic amines that have algogenic properties, and increases the pain sensitivity threshold 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 a peptide encoded by the calcitonin gene and a subsequent increase in nitric oxide (NO) production. Both of these actions counterbalance the negative effect caused by the decrease in PG levels due to COX inhibition. Amtolmetin guacil was well tolerated by patients with long-term use (for 6 months).

Pharmacokinetics Absorption of amtolmetin guacil after oral administration is rapid and complete. The drug is mainly concentrated in the walls of the stomach and intestines, where its very high concentration is maintained for 2 hours after administration. After absorption, amtolmetin guacil immediately undergoes hydrolysis by blood plasma esterases with the formation of three metabolites: MED5, tolmetin and guacol, which are transformed to the active metabolite of tolmetin, which penetrates the tissues, exerting a pharmacological effect. The main metabolic pathway of tolmetin is the oxidation of the methyl group on the benzene ring into a carboxyl group. Tmax after oral administration is 20–60 minutes.

Communication with plasma proteins - 99%. 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 for the drug Naysilat: rheumatoid arthritis,

osteoarthritis, ankylosing spondylitis, articular syndrome with exacerbation of gout, bursitis, tendovaginitis. Pain syndrome (weak and moderate intensity): arthralgia, myalgia, neuralgia, migraine, toothache and headache, algodismenorrhea, pain from injuries, burns.

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

Contraindications: hypersensitivity to amtolmetin, tolmetin,

complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including a 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 bleeding 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 surgery, arterial hypertension, congenital lactase deficiency, lactose intolerance, glucose-galactose malabsorption, glucose-6-phosphate dehydrogenase deficiency, pregnancy, lactation, children under 18 years of age.

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

Side effects Side effects are classified according to the frequency of occurrence: often - 1-10%, infrequently - 0.1-1%, rarely - 0.01-0.1%, very rarely - 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: increased urea nitrogen levels in the blood, urinary tract infections. From the senses: rarely - tinnitus, visual impairment. From the respiratory system: rarely - bronchospasm, shortness of breath, rhinitis, laryngeal edema. From the side of the central nervous system: often - dizziness, headache, drowsiness, rarely - depression. From the cardiovascular system: often - increased blood pressure. From the hematopoietic organs: rarely - anemia, thrombocytopenia, agranulocytosis, leukopenia. From the skin: uncommon - skin rash (including maculopapular rash), purpura, rare - exfoliative dermatitis (fever with or without chills, redness, thickening or peeling of the skin, swelling and/or tenderness of the tonsils), urticaria, Stevens-Johnson syndrome , Lyell's syndrome.

Allergic reactions: rarely - anaphylaxis or anaphylactoid reactions (change in facial skin color, skin rash, urticaria, itching of the skin, tachypnea or dyspnea, swelling of the eyelids, periorbital edema, shortness of breath, difficulty breathing, heaviness in the chest, wheezing).

Other: often - weakness, infrequently - swelling (of the face, legs, 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. Enhances the hypoglycemic effect of sulfonylurea derivatives, the effect of anticoagulants, antiplatelet agents, fibrinolytics, side effects of estrogens, corticosteroids and mineralcorticoids. Antacids and cholestyramine reduce absorption. Increases the concentration of lithium and methotrexate in the blood. In some patients with impaired renal function, co-administration of NSAIDs and ACE inhibitors may lead to further deterioration of renal function. Myelotoxic drugs increase the manifestations of hematotoxicity of the drug.

Directions for use and dosage: Inside. To maintain 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 1 time per day. The maximum daily dose is 1800 mg.

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 carbon) and symptomatic therapy (maintaining vital body functions). There is no specific antidote for the drug.

Special instructions During treatment, it is necessary to monitor the peripheral blood picture and the functional state of the liver and kidneys. Treatment should be stopped 48 hours before determination of 17-ketosteroids.

Impact on the ability to drive vehicles and operate machinery. During treatment, you should refrain from engaging in potentially hazardous activities that require increased attention and speed of mental and motor reactions.

Release form: Film-coated tablets, 600 mg. In a blister of opaque PVC/PVDC film/aluminum foil, 10 pcs. 2 blisters in a cardboard pack.

. Hyderabad, Andhra Pradesh, India.

Address of the place of production: plots 42, 45 and 46, Bachupally Village, Qutbullapur Mandal, Ranga Reddy District, Andhra Pradesh, India. Consumer complaints should be sent to the representative office address: 115035, Moscow, Ovchinnikovskaya embankment, 20, building 1.

Tel., 783-29-01, fax.

Conditions for dispensing from pharmacies By prescription.

Storage conditions for the drug Naisilate: In a dry place, protected from light, at a temperature not exceeding 25 °C. Keep out of the reach of children.

The shelf life of the drug Naysilat is 2 years.

Interaction

The drug reduces the effectiveness of antihypertensives, uricosurics and diuretics .

Nizilat enhances the effect of antiplatelet agents, fibrinolytics, anticoagulants , side effects of estrogens, mineralocorticoids.

Cholestyramine and antacids reduce the absorption of Nisylat.

Myelotoxic drugs enhance the hematotoxic properties of the drug.

Naisilate 600 mg No. 10 tablet p.p.o.

Instructions for medical use of the drug Nayzilat Trade name Nayzilat International nonproprietary name Amtolmetin guacil Dosage form Film-coated tablets, 600 mg Composition One tablet contains the active substance - amtolmetin guacil 600 mg, excipients: lactose monohydrate, hypromellose 15 pps, colloidal silicon dioxide anhydrous, sodium starch glycolate (type A), magnesium stearate, shell composition: hypromellose 5 cps, titanium dioxide E 171, macrogol (PEG 400). Description Caplet-shaped tablets, film-coated, white to almost white, smooth on both sides. Pharmacotherapeutic group Non-steroidal anti-inflammatory drugs. Acetic acid derivatives. ATX code M01AB Pharmacological properties Pharmacokinetics Absorption of amtolmetin guacil after oral administration occurs quickly and completely. Amtolmetin guacil is concentrated mainly in the gastrointestinal wall, where its maximum level is concentrated within 2 hours after taking the drug. Its conversion to active metabolites occurs as soon as it enters the plasma, so amtolmetin guacil as such is barely detectable in plasma and tissues. Amtolmetin guacil is hydrolyzed by plasma esterases into the following metabolites: MED5, tolmetin and guaiacol. MED5 (tolmetin-glycinamide) is the main metabolite in blood plasma. Tolmetin-glycinamide is metabolized to tolmetin and the active metabolite and reaches high concentrations in tissues. Elimination of the drug is almost complete within 24 hours and occurs mainly in the urine (77% of the administered dose) in the form of glucuronides. A small amount is excreted in bile and feces (7.5%). Pharmacodynamics Amtolmetin guacil is a non-steroidal anti-inflammatory drug (NSAID), a prodrug of tolmetin, which has analgesic and anti-inflammatory effects. The main mechanism of action of amtolmetin guacil, like other NSAIDs, is the inhibition of COX and prostaglandin synthesis. Amtolmetin increases the level of antioxidant enzymes in the gastric mucosa, such as superoxide dismutase (SOD), catalase, glutathione, while reducing the level of superoxide anion, peroxide nitrites or peroxide chloride, and malondialdehyde. In addition, when using amtolmetin, the level of nitric oxide (NO) in the stomach increases, which is manifested by the gastroprotective effect of the drug. The antioxidant effect of amtolmetin may be of additional importance in the treatment of patients with osteoarthritis, accompanied by inflammation and pain, in which oxidative stress and free radical damage to cartilage are increased. The reduction in pain with amtolmetin is also associated with a decrease in nitric oxide levels, which helps overcome oxidative stress. These two actions are selective and specific when using amtolmetin. Indications for use: osteoarthritis, rheumatoid arthritis, arthralgia, myalgia, pain after injury. Method of administration and dosage. The drug is taken orally, with a sufficient amount of liquid. Naysylate should be administered on an empty stomach to maintain its gastroprotective effect. Adults 600 mg twice a day. The recommended dose is 600 mg twice a day, the maintenance dose can be reduced to 600 mg. Use in Elderly Patients In elderly patients (over 65 years of age), in whom renal function tends to decline and gastrointestinal tolerance of NSAIDs is reduced, a low dose (600 mg once daily) of amtolmetin guacil is prescribed. The duration of treatment is determined by the doctor depending on the characteristics of the disease and the severity of the condition. Not recommended for long-term treatment. Side effects - lack of appetite, increased appetite, dry mouth, glossitis, stomatitis, oral ulceration, ulcerative stomatitis, bleeding gums, dysphagia, belching, nausea, vomiting, esophagitis, gastritis, gastroenteritis, enteritis, bloating, dyspepsia, pain in abdomen, colitis, rectal bleeding, pain in the gall bladder, peptic ulcer of the stomach and duodenum, diarrhea, tarry stools, constipation, tenesmus, hepatitis, liver dysfunction, pancreatitis, cholestatic jaundice - nasopharyngitis, rhinitis, nosebleeds, bronchitis, pneumonia , shortness of breath, asthma, laryngeal edema - insomnia, drowsiness, anxious dreams, headache, dizziness, paresthesia, hypoesthesia, amnesia, emotional instability, lack of coordination, peripheral neuropathy, torticollis, facial paralysis, hyperkinesia, depression, hypotension - arthralgia, arthritis , cramps in the lower extremities, bursitis, tenosynovitis, tendon rupture, myasthenia gravis, myalgia, muscle contracture, muscle cramps, myositis, myopathy, rhabdomyolysis - itching, contact dermatitis, baldness, dry skin, increased sweating, urticaria, eczema, seborrhea, skin ulcers - urinary tract infections, frequent urination, cystitis, hematuria, dysuria, kidney stones, nocturia, albuminuria, nephritis, urinary incontinence, urinary retention, urge to urinate - epididymitis, impotence, decreased libido, premature ejaculation, fibrocystic mastopathy, vaginal bleeding, acyclic uterine bleeding - chest hypertrophy - amblyopia, dry eyes, refractive error, eye hemorrhage, glaucoma, tinnitus, deafness, parosmia, loss of taste, taste perversion - palpitations, vasodilation, syncope, migraine, orthostatic hypotension, phlebitis , arrhythmia, angina pectoris, arterial hypertension - peripheral edema, hyperglycemia, hypoglycemia, increased creatinine phosphokinase levels, gout, weight gain - bruising, anemia, enlarged lymph nodes, lymphadenopathy, thrombocytopenia, agranulocytosis, leukopenia, petechial hemorrhage - chest pain, pain in back, facial swelling, tongue swelling, fever, neck stiffness, disorientation, increased photosensitivity reaction, generalized edema, anaphylaxis, angioedema, blistering rash (including erythema multiforme, Stevens-Johnson syndrome and toxic epidermal necrolysis, Lyell's syndrome), acute necrosis of skeletal muscles Contraindications - hypersensitivity to any of the components of the drug - intolerance to other non-steroidal anti-inflammatory drugs and patients with a complete or incomplete combination of bronchial asthma, rhinitis, urticaria - erosive and ulcerative lesions of the gastrointestinal tract (peptic ulcer of the stomach and duodenum, inflammatory bowel diseases (ulcerative colitis, Crohn's disease) - decompensated heart failure, edema, arterial hypertension, hemophilia, hypocoagulation - liver failure or active liver disease - chronic renal failure (KK < 30 ml/min), progressive kidney disease - confirmed hyperkalemia - hearing loss, pathology vestibular apparatus - pregnancy and lactation - children under 18 years of age - active gastrointestinal bleeding, cerebrovascular or other bleeding - period after coronary artery bypass grafting - glucose-6-phosphate dehydrogenase deficiency Use with caution in case of hyperbilirubinemia. - chronic heart failure, coronary heart disease, cerebrovascular diseases - dyslipidemia/hyperlipidemia, diabetes mellitus - peripheral arterial disease, smoking - chronic renal failure (creatinine clearance 30-60 ml/min) - history of ulcerative lesions of the gastrointestinal tract, presence of infection H .pylori, long-term use of NSAIDs, alcoholism, severe somatic diseases, old age - simultaneous use of oral glucocorticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline). Drug Interactions H1-histamine blockers are known to interfere with capsaicin receptors. The simultaneous use of amtolmetin guacil with H1 histamine blockers should be avoided. NSAIDs may enhance the effect of anticoagulants such as warfarin, and there may be a risk of gastrointestinal bleeding or ulcers when used together with corticosteroids and antiplatelet agents. NSAIDs may reduce the antihypertensive effect of diuretics, ACE inhibitors and other antihypertensive agents. In some patients with impaired renal function, the concomitant use of NSAIDs and ACE inhibitors may lead to a further deterioration of renal function. These interactions should be taken into account when using amtolmetin guacil in combination with ACE inhibitors. 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 drugs, enhances the hypoglycemic effect of sulfonylurea derivatives. Antacids and cholestyramine reduce the absorption of amtolmetin. Increases the concentration of lithium and methotrexate in the blood. Myelotoxic drugs increase the manifestations of hematotoxicity of the drug. Special instructions In patients with hepatic or renal insufficiency, treatment with amtolmetin guacil should be carried out under clinical monitoring, with periodic monitoring of renal and liver function. If renal and liver function deteriorates, treatment should be suspended. Patients with a history of coagulopathy therapy or anticoagulant treatment should be under close medical supervision. During treatment, monitoring of peripheral blood patterns is necessary. Because ocular changes have been reported in patients receiving other NSAIDs, if visual disturbances develop during treatment with amtolmetin guacil, treatment should be discontinued and an ophthalmologic examination performed. If any allergic reaction occurs, treatment should be stopped immediately. Treatment should be stopped 48 hours before determining 17-ketosteroids. The drug contains lactose monohydrate; therefore, Naysilat is not recommended for patients with hereditary galactose intolerance, Lapp lactase deficiency, or glucose/galactose malabsorption. Use in pregnant or lactating women Safety and effectiveness during pregnancy and lactation have not been established. Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms The drug can cause dizziness and drowsiness, therefore, during the treatment period, patients should not drive a vehicle or potentially dangerous mechanisms. Overdose Symptoms: visual disturbances, tachycardia, dry mouth, nausea, vomiting, increased sweating. Treatment: gastric lavage, taking activated carbon, symptomatic therapy. Release form and packaging 10 tablets are placed in a blister pack made of polyvinyl chloride film and aluminum foil. 1 contour package along with instructions for medical use in the state and Russian languages ​​is placed in a box of cardboard. Storage conditions Store in a dry place, protected from light at a temperature not exceeding 25 ° C. Keep out of the reach of children! Shelf life: 2 years Do not use after expiration date. Conditions for dispensing from pharmacies By prescription Site No: 42,45 and 46, Bachupali Village, Kutubullapur Mandal, Ranga Redi District, Andhra Pradesh, India Name and country of the marketing authorization holder: Dr. Reddy's Laboratories Limited, India Organization Address , which accepts claims from consumers regarding product quality on the territory of the Republic of Kazakhstan: Representative office in the Republic of Kazakhstan, 050057 Almaty, st. 22 line, 45, post office box 7, tel: 8(727)3941688 fax: 8(727)3941294

Analogues of Nizilat

Level 4 ATC code matches:
Voltaren

Rapten

Zerodol

Dickloberl Retard

Dikloberl N 75

Dicloberl

Ketanov

Dolak

Panoxen

Ketorolac

Naklofen Duo

Naklofen

Olfen-100

Olfen-75

Neurodiclovit

Fanigan

Aertal

Methindol retard

Ortofen

The drug was synthesized relatively recently - analogues of Nizilat are not yet produced. Vimovo (a combination of an NSAID and a proton pump inhibitor) is most similar in action to Nisylate.

Nizilat price

In Russia, the price of Naysilat in standard packaging reaches 380 rubles; in Ukraine, the average price of Naysilat 600 mg No. 20 is 63 hryvnia.

• Online pharmacies in RussiaRussia
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• Online pharmacies in KazakhstanKazakhstan

ZdravCity

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Pharmacy24

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• Naysylat tablets Naysylat tablets. 600 mg No. 10 India, Dr. Reddy's
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