Universal reference book for medicines
Name of the preparation: NISYLATE (NISELAT)

Active substance: amtolmetin guacil

Type: NSAIDs

Manufacturer: DR.
REDDY`S LABORATORIES (India)
Composition, form of production and packaging

Tablets covered with a film coat from white to almost white, capsular, with a characteristic odor.

1 tab.

amtolmethine guacyl 600 mg

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

The composition of the film membrane: hypromellose (5 cps) - 12.5 mg, titanium dioxide - 6.25 mg, macrogol 400 - 1.25 mg.

10 pieces.
- blisters (2) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2017.

PHARMACHOLOGIC EFFECT

Amtolmethine guacyl is an NSAID, a non-selective COX inhibitor.
Amtolmethine guacyl is a precursor of tolmetine. Has anti-inflammatory, analgesic, antipyretic, desensitizing effect, has a gastroprotective effect. Suppresses inflammatory factors, reduces platelet aggregation; oppresses 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 the permeability of capillaries; stabilizes the lysosomal membranes; inhibits synthesis or inactivates mediators of inflammation (prostaglandins, histamine, bradykinins, cytokines, complement factors). It blocks the interaction of bradykinin with tissue receptors, restores disturbed microcirculation, and reduces pain sensitivity in the inflammatory focus. Affects 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 syndrome, reduces morning stiffness and swelling, increases the amount of movement in the affected joints after 4 days of treatment.
The protective effect of amtolmethine guacyl on the gastric mucosa is realized by stimulating capsaicin receptors (also called vanilloid receptors) present in the gastrointestinal wall.
Due to the presence of the vanillin group in amtolmetin guacyl, it can stimulate capsaicin receptors, which in turn causes the release of the peptide encoded by the calcitonin gene (PCHA) and the subsequent increase in the production of nitric oxide (NO). Both of these actions create a counterbalance to the negative effect caused by a decrease in the amount of prostaglandins due to inhibition of COX. Amtolmethine guacil was well tolerated by patients with prolonged use (within 6 months).
PHARMACOKINETICS

Suction and distribution

Absorption of amotolmetine guacyl 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. The time to reach C max after ingestion is 20-60 min.
Binding to plasma proteins - 99%.

Metabolism

After absorption of amtolmethine, guacyl is immediately subjected to hydrolysis by plasma esterases with the formation of three metabolites: MED5, tolmetine and guiacaul, which are transformed to the active metabolite of tolmetin, which penetrates into tissues, providing pharmacological action.
The main way of metabolism of tolmetine is the oxidation of the methyl group in the benzene ring to the carboxyl group.
Excretion

T 1/2 in adults - 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;

- osteoarthrosis;

ankylosing spondylitis;

- articular syndrome with exacerbation of gout;

- bursitis, tendovaginitis;

- pain syndrome of mild and moderate intensity (arthralgia, myalgia, neuralgia, migraine, dental and headache, algodismenorea, pain with injuries, burns).

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

DOSING MODE

The recommended dose of the drug is 600 mg 2 times / day.
Depending on the degree of control of the symptoms of the disease, the maintenance dose can be reduced to 600 mg 1 time / day. The maximum daily dose is 1800 mg.
To maintain the gastroprotective effect of the drug amtolmethine guacyl should be taken on an empty stomach.

SIDE EFFECT

The frequency of side effects is classified according to the incidence of the case: often (1-10%), infrequently (0.1-1%), rarely (0.01-0.1%), very rarely (less than 0.01%), including individual reports.

From the digestive system: often - nausea;
infrequently - dyspepsia, discomfort in the stomach and intestines, bloating; rarely - abdominal pain, diarrhea, vomiting, constipation, gastritis; very rarely - a peptic ulcer, a violation of the liver.
From the urinary system: an increase in the content of urea nitrogen in the blood, urinary tract infection.

From the senses: rarely - noise in the ears, visual disturbances.

From the respiratory system: rarely - bronchospasm, dyspnea, 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 hemopoiesis: rarely - anemia, thrombocytopenia, agranulocytosis, leukopenia.

On the part of the skin: infrequent - skin rash (including maculopapular rash), purpura;
rarely - exfoliative dermatitis (fever with chills or without, redness, densification or flaking of the skin, swelling and / or tenderness of the tonsils), hives, Stevens-Johnson syndrome, Lyell's syndrome.
Allergic reactions: rarely anaphylaxis or anaphylactoid reactions (skin discoloration, skin rash, hives, skin itch, tachypnea or dyspnea, edema of the eyelids, periorbital edema, shortness of breath, shortness of breath, chest pain, wheezing).

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

- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including in the anamnesis);

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

- active gastrointestinal hemorrhage;

- cerebrovascular or other bleeding;

- Inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the phase of exacerbation;

- hemophilia and other disorders of blood coagulability;

Decompensated heart failure;

- liver failure or active liver disease;

- marked renal failure (CC less than 30 ml / min);

progressive kidney disease;

- confirmed hyperkalemia;

- period after aortocoronary shunting;

- arterial hypertension;

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

- deficiency of glucose-6-phosphate dehydrogenase;

- Pregnancy;

- lactation period;

- age up to 18 years;

- hypersensitivity to amtolmethine, tolmetin.

With caution should prescribe the drug for hyperbilirubinemia, chronic heart failure, coronary heart disease, cerebrovascular diseases, dyslipidemia / hyperlipidemia, diabetes, peripheral arterial disease, chronic kidney failure (KK 30-60 ml / min), ulcerative gastrointestinal lesions in history, the presence of infection of Helicobacter pylori, severe somatic diseases, prolonged use of NSAIDs, simultaneous intake of oral GCS (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicycium
oic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), alcoholism, smoking, elderly patients.
PREGNANCY AND LACTATION

The drug is contraindicated in pregnancy and lactation.

APPLICATION FOR FUNCTIONS OF THE LIVER

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

With caution should be prescribed for chronic kidney failure (KK 30-60 ml / min).

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Contraindicated in hepatic insufficiency or active liver disease.

APPLICATION FOR CHILDREN

Contraindicated in children and adolescents under 18 years.

APPLICATION IN ELDERLY PATIENTS

Caution should be given to elderly patients.

SPECIAL INSTRUCTIONS

During treatment, 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 before the determination of 17-ketosteroids.

Impact on the ability to drive vehicles and manage mechanisms

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

OVERDOSE

Symptoms: abdominal pain, nausea, vomiting, erosive-ulcerative gastrointestinal lesion, impaired renal function, metabolic acidosis.

Treatment: gastric lavage, the introduction of adsorbents (activated charcoal) and the conduct of symptomatic therapy (maintenance of vital body functions).
There is no specific antidote.
DRUG 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, hypotensive drugs and diuretics.

Strengthens the hypoglycemic effect of derivatives of sulfonylurea, the effect of anticoagulants, antiaggregants, fibrinolytic agents, side effects of estrogens, GCS and mineralocorticoids.

Antacids and colestyramine 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 may lead to further impairment of renal function.

Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored in a dry, protected from light, out of reach of children at a temperature of no higher than 25 ° C.
Shelf life - 2 years.
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