Nayzilat tabs 600mg #20

Instruction for Nayzilat

You can buy Nayzilat here

Release form and composition Nayzilat

Tablets, film coated from white to almost white color, capsule, with a characteristic smell.
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 .
The composition of the film shell: hypromellose (5 cps) - 12.5 mg, titanium dioxide - 6.25 mg, macrogol 400 - 1.25 mg.

pharmachologic effect

Amtolmetin guacil is a NSAID, 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 prostaglandins (including in the focus 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). 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 (PCHC), 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 number of prostaglandins due to inhibition of COX. Amtolmetin guacil was well tolerated by patients with long-term use (for 6 months).

Pharmacokinetics

Suction and distribution

The absorption of amtolmetin guacil after oral administration is rapid and complete. Basically, Nayzilat 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 ingestion is 20-60 minutes.
Plasma protein binding - 99%.

Metabolism

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 carboxyl.

Removal

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

Indications for use

    rheumatoid arthritis;
    osteoarthritis;
    ankylosing spondylitis;
    articular syndrome with exacerbation of gout;
    bursitis, tendovaginitis;
    pain syndrome of 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, does not affect the progression of the disease.

Dosing regimen

The recommended dose of Nayzilat is 600 mg 2 times / day. Depending on the degree of control of the symptoms of the disease, the maintenance dose may be reduced to 600 mg 1 time / day. The maximum daily dose is 1800 mg.
To preserve the gastroprotective effect of Nayzilat amtolmetin guacil should be taken on an empty stomach.

Side effect of Nayzilat

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.
On the part of 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, abnormal liver function.
On the part of the urinary system: an increase in the content of urea nitrogen in the blood, urinary tract infections.
From the senses: rarely - tinnitus, visual disturbances.
On the part of 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.
Since the cardiovascular system: often - increased blood pressure.
From the side of blood-forming organs: rarely - anemia, thrombocytopenia, agranulocytosis, leukopenia.
On the part of the skin: infrequently - skin rash (including maculo-papular 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, skin itching, tachypnea or dyspnea, eyelid edema, periorbital edema, shortness of breath, difficulty breathing, chest heaviness, wheezing).
Others: often - weakness; infrequently - swelling (face, legs, ankles, fingers, feet, weight gain); rarely, increased 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 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 (CC 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;
    deficiency of glucose-6-phosphate dehydrogenase;
    pregnancy;
    lactation period;
    age up to 18 years;
    Hypersensitivity to amtolmetin, tolmetin.
With caution should be prescribed Nayzilat for hyperbilirubinemia, chronic heart failure, coronary heart disease, cerebrovascular diseases, dyslipidemia / hyperlipidemia, diabetes, peripheral artery disease, chronic renal failure (CK 30-60 ml / min), gastrointestinal ulcers, anamnesis, an infection, and an infection. pylori, severe somatic diseases, prolonged use of NSAIDs, simultaneous administration of oral GCS (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicy oic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), alcoholism, smoking, elderly patients.

Use during pregnancy and lactation

Nayzilat is contraindicated in pregnancy and lactation.

Application for violations of the liver

Contraindicated in liver failure or active liver disease.

Application for violations of renal function

Contraindicated in severe renal failure (CC less than 30 ml / min), progressive kidney disease.
With caution should be prescribed for chronic renal failure (CC 30-60 ml / min).

Use in children

Use in children and adolescents up to 18 years of age is contraindicated.

Use in elderly patients

Precautions should be prescribed Nayzilat to elderly patients.

special instructions

During treatment, control of the pattern of peripheral blood and the functional state of the liver and kidneys is necessary.
Treatment should be discontinued 48 hours before the determination of the 17-ketosteroids.
Influence on ability to drive motor transport and control mechanisms
During treatment, you should refrain from engaging in potentially hazardous activities that require increased attention and speed of mental and motor responses.

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 conducting symptomatic therapy (maintaining the vital functions of the body). There is no specific antidote.

Drug interactions

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 mineralocorticoids.
Antacids and colestyramine reduce absorption.
Increases the blood concentration of drugs lithium, methotrexate.
In some patients with impaired renal function, the combined use of NSAIDs and ACE inhibitors can lead to a further deterioration in renal function.
Myelotoxic drugs increase the hematotoxicity of Nayzilat.

Storage conditions Nayzilat

Nayzilat should be stored in a dry, protected from light, out of reach of children at a temperature not exceeding 25 ° C.
Shelf life - 2 years.

Terms of sell

You can buy Nayzilat without a prescription.