Nisylate

Nayzilat is a trade name for a drug whose active ingredient is amtolmetin guacil. Amtolmetin guacil is a non-steroidal anti-inflammatory drug (NSAID) used to treat pain syndromes of various etiologies and inflammatory conditions.

Amtolmetin guacil inhibits the activity of cyclooxygenase enzymes (COX-1 and COX-2), which leads to a decrease in the synthesis of prostaglandins - substances that play a key role in the development of inflammation, pain and fever. It has analgesic, anti-inflammatory and antipyretic effects.

Indications Naisilata

1. Rheumatoid Arthritis: Nisilate may help reduce inflammation and pain in rheumatoid arthritis, a chronic inflammatory joint disease.
2. Osteoarthritis: This medication may be used to relieve pain and inflammation in osteoarthritis, a chronic disease characterized by the breakdown of cartilage in the joints.
3. Back Pain: Naysilat can be used to relieve pain from various types of back pain including acute or chronic spondylosis, sciatica and others.
4. Muscle pain: This medication may be used to relieve pain caused by muscle injuries, strains, or sprains.
5. Post-operative pain: After surgical interventions, Nizilat can be used to relieve pain.
6. Other conditions: In some cases, Naysilat may be prescribed to relieve pain from toothache, headache, inflammation, etc.

Release form

Tablets: This is the most common form of Naysilat. Tablets are usually presented as round or oval film-coated tablets. They can have different dosages to suit the needs of different patients.

Pharmacodynamics

The pharmacodynamics of amtolmetin guacil, the main active ingredient in Naysilat, lies in its ability to inhibit the enzyme cyclooxygenase (COX), which results in a decrease in the synthesis of prostaglandins, inflammatory mediators responsible for pain, inflammation and fever.

Amtolmetin guacil is an inhibitor of COX-1 and COX-2. COX-1 is widely present in tissues and is involved in maintaining physiological function such as protecting the gastric mucosa. COX-2, on the other hand, is induced by inflammation and plays a key role in the process of inflammation and pain.

Since amtolmetin guacil inhibits both COX isoforms, it has anti-inflammatory, analgesic and antipyretic effects. This mechanism makes Naysilat an effective agent for reducing inflammation and pain in various conditions such as rheumatoid arthritis, osteoarthritis, muscle pain and others.

Pharmacokinetics

1. Absorption: Amtolmetin guacil is generally well absorbed from the gastrointestinal tract after oral administration. Maximum plasma concentrations are usually reached 1-2 hours after administration.
2. Distribution: Amtolmetin guacil is well distributed in body tissues, including joints and soft tissues. It binds to plasma proteins at a high level.
3. Metabolism: Amtolmetin guacil is metabolized in the liver. The main metabolite is hydroxyamtolmetin, which also has COX inhibitor activity.
4. Excretion: Amtolmetin guacil metabolites and unchanged drug are excreted mainly via the kidneys as glucuronic acid conjugates and unchanged drug. A smaller portion is excreted via the intestines.
5. Half-life: The half-life of amtolmetin guacil in the body is about 3-5 hours, which means that its effects quickly decline after stopping use.

Dosing and administration

Directions for use:

• Oral use: Naysilat is taken by mouth, usually in tablet form.
• Meal: It is recommended to take the tablets after meals to reduce the irritating effect on the stomach.
• Drinking: Tablets should be taken with a sufficient amount of water.

Recommended doses:

1. Adults:

   • Initial dose: The recommended initial dose is 600-1200 mg per day, divided into 2-3 doses.
   • Maintenance dose: Depending on clinical response and tolerability, the dose may be reduced to 600 mg daily.
   • Maximum daily dose: Should not exceed 1800 mg.

2. Elderly patients:

   • For elderly patients, it is recommended to start with the minimum effective dose and gradually increase the dosage if necessary, taking into account possible concomitant diseases and general health condition.

3. Children and teenagers:

   • Nayzilat is not recommended for use in children under 12 years of age. For adolescents over 12 years of age, the dosage is selected individually, usually starting with minimal doses.

Dosage examples:

• For the treatment of pain syndrome:

  • Initial dose: 600 mg (1 tablet) 2 times a day after meals.
  • If necessary, the dose can be increased to 600 mg 3 times a day.

• For the treatment of inflammatory diseases:

  • Initial dose: 600-1200 mg per day, divided into 2-3 doses.
  • Maintenance dose: 600 mg per day.

Duration of treatment:

• The duration of treatment depends on the nature of the disease, the severity of symptoms and the patient's individual response to therapy.
• In acute conditions, the course of treatment may last several days, in chronic conditions - up to several weeks or months, but under the supervision of a doctor.

Special instructions:

• Liver and kidney failure:
  • In patients with impaired liver and kidney function, dosage adjustment and regular monitoring of the function of these organs may be required.
• Status control:
  • With long-term use, regular medical examination is recommended to monitor liver function, kidney function and blood counts.
• Alcohol restriction:
  • Alcohol consumption should be avoided during treatment as it may increase the risk of gastrointestinal side effects.

Use Naisilata during pregnancy

1. Gastroprotective properties: Amtolmetin guacil has a significantly reduced ulcer-forming activity compared to other NSAIDs. This is due to its ability to stimulate the production of nitric oxide, which provides a gastroprotective effect and reduces damage caused by ethanol in the stomach of rats (Coruzzi et al., 2000).
2. Long-term use in rheumatic diseases: Studies show that long-term use of amtolmetin guacil in patients with osteoarthritis, rheumatoid arthritis and ankylosing spondylitis was effective and well tolerated. The incidence of serious side effects was low, and most patients were satisfied with the treatment results (Karateev et al., 2019).
3. Comparative analysis with other NSAIDs: A meta-analysis showed that amtolmetin guacil has better gastrotropic properties compared to other NSAIDs such as diclofenac and indomethacin. The incidence of gastrointestinal side effects and serious ulcers was significantly lower in patients taking amtolmetin guacil (Marcolongo et al., 1999).

Contraindications

1. Gastric or duodenal ulcers: The use of Naysilat may aggravate ulcerative lesions of the gastric or intestinal mucosa and lead to bleeding or perforation.
2. Thrombocytopenia or other blood disorders: Nisilat may increase blood clotting disorders and lead to bleeding.
3. Severe renal or hepatic impairment: Use of Nisilat may worsen these conditions and cause complications.
4. Asthma, rhinitis, nasal polyps: Naisilat may cause an increase in symptoms of bronchial asthma or allergic reactions.
5. Complete or partial closure of the arterial canal in the fetus during the second and third trimesters of pregnancy: Use of Nisilat may result in a risk of complications in the fetus, including premature closure of the arterial canal.
6. Individual intolerance or allergic reaction to amtolmetin guacil or other NSAIDs: Use of the drug may cause allergic reactions in individuals sensitive to this drug.
7. Postoperative condition after coronary artery bypass grafting: The use of Nisilat may increase the risk of cardiac complications and hemorrhagic complications after surgery.

Side effects Naisilata

1. Dyspeptic symptoms: Include abdominal discomfort or pain, nausea, vomiting, diarrhea or constipation.
2. Ulcerative gastrointestinal lesions: Includes gastric or duodenal ulcers, gastrointestinal bleeding, and gastrointestinal perforation.
3. Gastrointestinal bleeding: This may manifest as blood in the stool or through vomit and can be a serious complication.
4. Liver function disorders: Includes increased levels of liver enzymes in the blood (ALT, AST), hepatitis and yellowing of the skin and sclera.
5. Renal dysfunction: May manifest as increased levels of creatinine and urea in the blood, edema and changes in the frequency of urination.
6. Systemic allergic reactions: May include urticaria, itching, angioedema, and even anaphylaxis.
7. Blood disorders: May manifest as thrombocytopenia, agranulocytosis, anemia and other changes in blood composition.
8. Cardiovascular complications: Include increased blood pressure and worsening cardiac function.
9. Central and peripheral nervous systems: May manifest as headache, dizziness, drowsiness, insomnia, or pain in the nerve area.
10. Other side effects: Include alopecia, urticaria, chest pain, sweating, and changes in taste.

Overdose

1. Nausea and vomiting: Excessive consumption may cause nausea and vomiting, which may worsen dehydration and electrolyte imbalances.
2. Abdominal pain: Overdose may cause abdominal pain, which may be due to irritation of the lining of the stomach or intestines.
3. Dizziness and Drowsiness: Excessive use may cause dizziness, drowsiness and central nervous system depression.
4. Hypertension: There may be an increase in blood pressure and associated symptoms such as headache, palpitations, etc.
5. Kidney and liver damage: In case of overdose, kidney and liver damage may occur, which may manifest itself in increased levels of the corresponding indicators in the blood.
6. Other symptoms: May include asthenia, insomnia, hyperventilation, arrhythmia, respiratory arrest, etc.

Interactions with other drugs

1. Other nonsteroidal anti-inflammatory drugs (NSAIDs): Concomitant use of NSAIDs, including aspirin, may increase the risk of gastrointestinal ulcers and bleeding.
2. Acetylsalicylic acid (aspirin): Using Nisilate with aspirin may increase the risk of developing ulcer complications.
3. Glucocorticosteroids: Concomitant use of Nisilat with glucocorticosteroids such as prednisolone or dexamethasone may increase the risk of ulcer complications.
4. Medicines affecting blood coagulation: Nisilat may enhance the effects of anticoagulants (eg, warfarin), platelet antiplatelet agents (eg, cardioprotective dose of aspirin), which may increase the risk of bleeding.
5. Blood pressure medications: Nisilat may decrease the effectiveness of antihypertensive medications such as ACE inhibitors or beta-blockers.
6. Lithium: Using Nisilate with lithium may increase the level of lithium in the blood, which may lead to toxic effects.
7. Methotrexate: Nisilat may increase the toxicity of methotrexate by decreasing its elimination, especially with long-term use.

Storage conditions

It is generally recommended to store the drug in a dry, dark place at room temperature (15 to 30 degrees Celsius). It is important to avoid storing it in places exposed to direct sunlight, humidity or heat.

Tablets or capsules are usually stored in their original package or container, tightly closed to protect them from exposure to moisture and air.

Avoid freezing the medicine as this may change its structure and effectiveness.