Naizilat
Naizilat: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Prices in pharmacies
Latin name: Niselat
ATX code: M01AB
Active ingredient: amtolmetin guacil (amtolmetin guacil)
Manufacturer: Dr. Reddy's Laboratories Ltd. (India)
Description and photo update: 2018-15-05
Prices in pharmacies: from 437 rubles.
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Naisylate is a non-steroidal anti-inflammatory drug (NSAID).
Release form and composition
The dosage form of Naysilat is film-coated tablets: capsule-shaped, white or almost white, have a characteristic odor (10 pcs. In blisters, in a cardboard box 2 blisters).
Composition for 1 tablet:
- active substance: amtolmetin guatsil - 600 mg;
- auxiliary ingredients: hypromellose (15 cps), lactose monohydrate, lactose monohydrate (Flowlac 100), sodium carboxymethyl starch type A, colloidal silicon dioxide, magnesium stearate;
- film shell: hypromellose (5 cps), titanium dioxide, macrogol 400.
Pharmacological properties
Pharmacodynamics
Amtolmetin guacil - the active component of naysylate - is a non-steroidal anti-inflammatory substance, a non-selective inhibitor of cyclooxygenase (COX), a precursor of tolmetine. It has anti-inflammatory, analgesic, antipyretic, desensitizing and gastroprotective effects. By inhibiting pro-inflammatory factors, amtolmetin guatsil helps to reduce platelet aggregation; it inhibits COX-1 and COX-2, disrupts the metabolism of arachidonic acid, reduces the formation of prostaglandins (including in the focus of inflammation), suppresses proliferative and exudative inflammatory phases, reduces capillary permeability, stabilizes lysosomal membranes, inhibits synthesis or inactivates inflammatory mediators (histamine, prostaglandins, cytokines, bradykinins, complement factors). In the focus of inflammation, it blocks the relationship of bradykinin with tissue receptors, restores microcirculation and reduces pain; affects the centers of pain in the thalamus, reduces the concentration of neurotransmitters (biogenic amines) with algogenic properties, increases the pain sensitivity threshold of the receptor apparatus. Naysilate completely relieves or significantly reduces the intensity of pain, morning swelling and stiffness, increasing the range of motion in the affected joints 4 days after the start of therapy. Naysilate completely relieves or significantly reduces the intensity of pain, morning swelling and stiffness, increasing the range of motion in the affected joints 4 days after the start of therapy. Naysylate completely relieves or significantly reduces the intensity of pain, morning swelling and stiffness, increasing the range of motion in the affected joints 4 days after the start of therapy.
Amtolmetin guacil has a protective effect on the gastric mucosa by stimulating the capsaicin receptors (vanilloid receptors) present in its walls. Due to the presence of the vanillin group in guacil amtolmetin, it is able to stimulate capsaicin receptors, causing the release of a peptide associated with the calcitonin gene (PSGC), and further increase the production of nitric oxide (NO). Both of these processes counterbalance the negative effects caused by the decrease in the amount of prostaglandins due to inhibition of COX.
With prolonged use (up to six months) Amtolmetin guatsil was well tolerated by patients.
Pharmacokinetics
- absorption and distribution: after oral administration, the substance is absorbed quickly and completely; accumulates mainly in the walls of the stomach and intestines and is maintained in a very high concentration for 2 hours after ingestion; the time to reach the maximum concentration (C max) is 20–60 minutes; up to 99% of the taken substance binds to plasma proteins;
- metabolism: immediately after absorption by hydrolysis by blood plasma esterases, amtolmetin guacil is transformed, forming three metabolites: tolmetin, guiacol and MED5, which are then converted into an active metabolite of tolmetin, which penetrates into tissues and has a pharmacological effect; tolmetin is metabolized mainly by oxidation of the methyl group on the benzene ring to the carboxyl one;
- Excretion: the half-life (T1 / 2) for adults is about 5 hours; during the day, the substance is excreted from the body almost completely in the form of glucuronides (by the kidneys - 80%; with bile - 20%).
Indications for use
- ankylosing spondylitis;
- osteoarthritis;
- rheumatoid arthritis;
- articular syndrome due to exacerbation of gout;
- bursitis, tendovaginitis;
- pain syndrome of mild and moderate severity with arthralgia, myalgia, neuralgia, migraine, toothache and headache, algodismenorrhea, pain from injuries, burns, etc.
Naisilat is intended for symptomatic treatment, relieving pain and relieving inflammation at the time of application; taking the drug has no effect on the progression of the disease.
Contraindications
Absolute:
- aspirin triad (complete or partial combination of bronchial asthma with recurrent polyposis of the nose or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs), including a history;
- erosive and ulcerative lesions of the mucous membrane of the stomach and duodenum;
- gastrointestinal bleeding in the active phase;
- cerebrovascular and (or) other bleeding;
- inflammatory bowel disease (ulcerative colitis, Crohn's disease) in the acute phase;
- decompensated heart failure;
- period after coronary artery bypass grafting;
- hemophilia, other blood clotting disorders;
- confirmed hyperkalemia;
- severe liver dysfunction or active liver disease;
- severe renal impairment with creatinine clearance (CC) <30 ml / min;
- progressive kidney disease;
- arterial hypertension;
- lactose intolerance, congenital lactase deficiency, glucose-galactose malabsorption;
- deficiency of G6PD (glucose-6-phosphate dehydrogenase);
- the period of pregnancy and lactation (breastfeeding);
- age up to 18 years;
- increased individual sensitivity to amtolmetin, tolmetin and other components of the drug.
Relative contraindications for which Naysilat should be used with caution are:
- hyperbilirubinemia;
- chronic heart failure;
- ischemic heart disease (CHD);
- cerebrovascular diseases;
- dyslipidemia / hyperlipidemia;
- diabetes;
- peripheral arterial disease;
- chronic renal failure (CC 30-60 ml / min);
- history of ulcerative lesions of the gastrointestinal tract;
- Helicobacter pylori infection;
- severe somatic diseases;
- long-term use of NSAIDs;
- concomitant use of oral glucocorticosteroids (GCS) (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid and clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine);
- alcoholism;
- smoking;
- elderly age.
Instructions for the use of Naizilat: method and dosage
Nizilat 600 mg tablets are taken orally.
Recommended dosage: 600 mg (1 tablet) 2 times a day. Depending on the required level of control of the symptoms of the disease, the maintenance dose may be reduced to 600 mg once a day. The maximum daily dose should not exceed 1800 mg (3 tablets).
To maintain the gastroprotective effect of the drug, Nizilat must be taken on an empty stomach.
Side effects
The frequency of side effects from systems and organs due to the use of Nizilat (according to the scale: often - from 1 to 10%; infrequently - from 0.1 to 1%; rarely - from 0.01 to 0.1%; extremely rare - less than 0.01%, including individual messages):
- digestive system: often - nausea; infrequently - discomfort in the stomach or intestines, dyspepsia, bloating; rarely - diarrhea, vomiting, gastritis, abdominal pain, constipation; extremely rare - hepatic dysfunction, peptic ulcer;
- urinary system: increased blood levels of urea nitrogen, urinary tract infections;
- sense organs: rarely - visual impairment, tinnitus;
- respiratory system: rarely - shortness of breath, bronchospasm, laryngeal edema, rhinitis;
- central and peripheral nervous system: often - headache, dizziness, drowsiness; rarely - depressive disorders;
- cardiovascular system: often - increased blood pressure;
- hematopoietic organs: rarely - anemia, agranulocytosis, thrombocytopenia, leukopenia;
- skin: infrequently - purpura and skin rash, including maculopapular; rarely - urticaria, Lyell's syndrome, Stevens-Johnson syndrome, exfoliative dermatitis, manifested by fever with or without chills, redness, induration or scaling of the skin, swelling and / or tenderness of the tonsils;
- hypersensitivity reactions: rarely - anaphylaxis or anaphylactoid reactions, manifested by a change in complexion, skin rash, urticaria, pruritus, tachypnea or dyspnea, eyelid edema, periorbital edema, shortness of breath, shortness of breath, heaviness in the chest, wheezing;
- other reactions: often - weakness; infrequently - swelling of the face, ankles, legs, fingers, feet; increase in body weight; rarely - hyperhidrosis, lymphadenopathy, fever; extremely rare - swelling of the tongue.
Overdose
Symptoms of an amtolmetine guacil overdose:
- nausea and / or vomiting;
- abdominal pain;
- erosive and ulcerative lesions of the gastrointestinal tract;
- renal failure;
- metabolic acidosis.
For the treatment of the condition, it is necessary to wash the stomach, introduce adsorbents (activated carbon) and then carry out symptomatic therapy to maintain the vital functions of the body. The specific antidote for Naizilat is unknown.
special instructions
In the course of therapy, the peripheral blood picture and the functional state of the liver and kidneys should be monitored.
To obtain reliable test results, taking the drug must be discontinued 48 hours before determining the content of 17-ketosteroids in urine.
Influence on the ability to drive vehicles and complex mechanisms
You should refrain from engaging in activities that require a high concentration of attention and speed of psychomotor reactions during treatment with Nizilat.
Application during pregnancy and lactation
The use of Naizilat is contraindicated for pregnant and lactating women.
Pediatric use
The use of Naizilat is contraindicated in children under the age of 18.
With impaired renal function
Naisylate 600 mg is contraindicated in progressive kidney disease and severe renal failure with CC <30 ml / min.
In chronic renal failure with CC from 30 to 60 ml / min, the drug is prescribed with caution.
For violations of liver function
According to the instructions, Naizilat is contraindicated in liver failure and liver disease in the active phase.
Use in the elderly
Elderly patients should be prescribed Nayzylate with caution.
Drug interactions
- rifampicin, phenylbutazone, ethanol, barbiturates, phenytoin, tricyclic antidepressants (inducers of microsomal oxidation in the liver): potentiate the production of active hydroxylated metabolites;
- uricosuric, antihypertensive drugs and diuretics: amtolmetin guacil reduces their effectiveness;
- sulfonylurea derivatives: their hypoglycemic effect is enhanced;
- anticoagulants, antiplatelet agents, fibrinolytics, estrogen-containing drugs, GCS and mineralocorticoids: their side effects are aggravated;
- antacids and cholestyramine: inhibit the absorption of amtolmetin guacil;
- lithium preparations, methotrexate: their concentration in the blood increases;
- myelotoxic drugs: increase the manifestations of naysylate hematotoxicity;
- ACE inhibitors: in case of impaired renal function, they can lead to further deterioration of renal function.
Analogs
There is no information about Naizilat analogues.
Terms and conditions of storage
Store in a dry, dark place at a temperature not exceeding 25 ° C. Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Naizilat
Patients who took the drug often leave good reviews about Nizilate. As advantages, it is noted that it practically does not affect the gastrointestinal tract, the tablets can be taken for a sufficiently long time and on an empty stomach. The analgesic and anti-inflammatory effect is long lasting.
At the same time, it is indicated that severe pain can only be partially relieved, the smell, taste and aftertaste of the tablets are quite unpleasant, and because of their large size, they are not very easy to swallow.
Price for Naisilat in pharmacies
The approximate price of Naizilat is 490 rubles. for 20 tablets per pack.
Naizilat: prices in online pharmacies
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Drug name Price Pharmacy |
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Naysylate 600 mg film-coated tablets 20 pcs. 437 r Buy |
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Nizylate tablets p.p. 600mg 20 pcs. RUB 528 Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
