NISELAT 600MG PILLS

Composition

Description of the dosage form

Pills: capsular, film-coated from white to almost white color, with a characteristic smell.

Mechanism of action

pharmachologic effect - desensitizing, gastroprotective, analgesic, antipyretic, anti-inflammatory.

Pharmacodynamics

Amtolmetin guacil - NPVS, non-selective inhibitor of COX. Amtolmetin guacil is a precursor of tolmetin. It has anti-inflammatory, analgesic, antipyretic, desensitizing effect, has a gastroprotective effect. Suppresses pro-inflammatory factors, reduces platelet aggregation; inhibits COX-1 and COX-2, violates the metabolism of arachidonic acid, reduces the formation of PG (including in the 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). It blocks the interaction of bradykinin with tissue receptors, restores impaired microcirculation and reduces pain sensitivity in the inflammatory focus. 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 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 the Capsaicin receptors (also called vanilloid receptors) present in the walls of the gastrointestinal tract. Due to the fact that amtolmetin guacil contains a vanillin group, it can stimulate capsaicin receptors, which in turn causes the release of the peptide encoded by the calcitonin gene and the subsequent increase in nitric oxide production (NO). Both of these actions create a counterbalance to the negative effect caused by a decrease in the number of PGs due to inhibition of COX. Amtolmetin guacil was well tolerated by patients with long-term use (for 6 months).

Pharmacokinetics

The absorption of amtolmetin guacil after oral administration is fast 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 of amtolmetin, guacil is immediately hydrolyzed by plasma esterases to form three metabolites: MED5, tolmetin and guviacol, which are transformed to the active metabolite of tolmetin, which penetrates into tissues, exerting a pharmacological effect. The main metabolic pathway of tolmetin is the oxidation of the methyl group on the benzene ring to the carboxyl. Tmax after ingestion - 20–60 minutes.

Communication with plasma proteins - 99%. T1/2 in adults, about 5 hours. Within 24 hours, the drug is almost completely excreted from the body in the form of glucuronides (80% with urine, 20% with bile).

Indications and usage

rheumatoid arthritis;

osteoarthritis;

ankylosing spondylitis;

articular syndrome with exacerbation of gout;

bursitis;

tendovaginitis.

Pain syndrome (low and medium intensity):

arthralgia;

myalgia;

neuralgia;

migraine;

toothache and headache;

algomenorrhea;

pain with injuries, burns.

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

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 of);

erosive and ulcerative changes of 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;

the period after coronary artery bypass surgery;

arterial hypertension;

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

glucose-6-phosphate dehydrogenase deficiency;

pregnancy;

lactation period;

children's age up to 18 years.

Carefully: 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); ulcerative lesions of the gastrointestinal tract in history; infection N. pylori; prolonged use of NSAIDs; alcoholism; severe somatic diseases; elderly age; simultaneous administration of oral GCS (including prednisolone), anticoagulants (including warfarin), antiaggregants (including acetylsalicylic acid, clopidogrel), SSRIs (including citalopram, Fluoxetine, paroxetine, sertraline ).

Side effects

Side effects are classified according to the frequency of occurrence of a case: often 1–10%; infrequently - 0.1–1%; rarely, 0.01–0.1%; very rarely - <0.01%, including individual messages.

Gastrointestinal: often nausea; infrequently - dyspepsia, discomfort in the stomach and intestines, bloating; rarely - abdominal pain, diarrhea, vomiting, constipation, gastritis; very rarely - peptic ulcer, abnormal liver function.

Urogenital: increased urea nitrogen in the blood, urinary tract infections.

Special senses: rarely - tinnitus, visual disturbances.

Respiratory: rarely - bronchospasm, shortness of breath, rhinitis, laryngeal edema.

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

From the CCC: often - the rise of blood pressure.

From the side of blood-forming organs: rarely - anemia, thrombocytopenia, agranulocytosis, leukopenia.

From the skin: infrequently - skin rash (including maculopapular rash), purpura; rarely - exfoliative dermatitis (fever with or without chills, redness, hardening 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 (discoloration of the skin, skin rash, urticaria, itchy skin, tachypnea or dyspnea, eyelid edema, periorbital edema, shortness of breath, difficulty breathing, chest pain, wheezing).

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

Interaction

Inductors 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, fibrinolitikov, side effects of estrogen, GCS and mineralcorticoids.

Antacids and colestyramine reduce absorption.

Increases the blood concentration of drugs lithium, Methotrexate .

In some patients with impaired renal function, co-administration of NSAIDs and ACE inhibitors may lead to a further deterioration in the functioning of the kidneys.

Myelotoxic drugs increase the hematotoxicity of the drug.

Dosage and administration

Inside To preserve the gastroprotective action 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 may be reduced to 600 mg once a 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, the introduction of adsorbents (activated carbon) and symptomatic therapy (maintaining the vital functions of the body). The specific antidote of the drug does not exist.

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 before the determination of the 17-ketosteroids.

Influence on ability to drive vehicles and work with mechanisms. During treatment, you should refrain from engaging in potentially hazardous activities that require increased attention and speed of mental and motor responses.

Release form

Tablets, film coated, 600 mg. In a blister of opaque PVC / PVDX film / aluminum foil in 10 pcs. 2 blisters in a carton box.