The most zealous

Naisylate is the trade name of a drug whose active substance is amtolmetin guacil. Amtolmetin guacil is a nonsteroidal anti-inflammatory drug (NSAID) that is 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. Has analgesic, anti-inflammatory and antipyretic effects.

Indications The crowbar

1. Rheumatoid Arthritis: Nisylate may help reduce inflammation and pain in rheumatoid arthritis, a chronic inflammatory joint disease.
2. Osteoarthritis: This drug may be used to relieve pain and inflammation from osteoarthritis, a chronic disease characterized by the breakdown of cartilage in joints.
3. Back pain: Naysilate 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, sprains, or strains.
5. Postoperative pain: After surgical interventions, Naysilat can be used to relieve pain.
6. Other conditions: In some cases, Naysilat may be prescribed to relieve pain from toothache, headache, inflammatory processes, etc.

Release form

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

Pharmacodynamics

The pharmacodynamics of amtolmetin guacil, the main active ingredient in Naysylat, is its ability to inhibit the enzyme cycloxygenase (COX), resulting 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 functions such as protecting the gastric mucosa. COX-2, on the other hand, is inflammation-induced and plays a key role in the process of inflammation and pain.

Since amtolmetin guacil inhibits both isoforms of COX, it has anti-inflammatory, analgesic and antipyretic effects. This mechanism makes Naisilate effective in 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 into 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: The amtolmetin guacil metabolites and unchanged drug are excreted primarily via the kidneys as glucuronic acid conjugates and unchanged drug. A smaller portion is excreted in the intestines.
5. Half-life: The half-life of amtolmetin guacil in the body is about 3-5 hours, meaning that its effects decline rapidly after stopping administration.

Dosing and administration

Method of application:

• Oral administration: Nisylat is taken orally, usually in tablet form.
• Eating: It is recommended to take the tablets after meals to reduce irritation to the stomach.
• Washing down: 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 can be reduced to 600 mg per day.
   • 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.

3. Children and teenagers:

   • Nysylate 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 the minimum doses.

Dosage examples:

• For the treatment of pain:

  • 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 can 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:
  • Patients with impaired liver and kidney function may require dose adjustment and regular monitoring of the function of these organs.
• Condition monitoring:
  • With long-term use, regular examination by a doctor is recommended to monitor liver function, kidney function and blood counts.
• Alcohol limit:
  • Alcohol should be avoided during treatment as this may increase the risk of gastrointestinal side effects.

Use The crowbar during pregnancy

1. Gastroprotective properties: Amtolmetin guacil has significantly reduced ulcer-forming activity compared to other NSAIDs. This is due to its ability to stimulate nitric oxide production, which provides gastroprotective effects and reduces the 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 gastrotropism 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. Peptic ulcer of the stomach or duodenum: The use of Naisilate may aggravate ulcerative lesions of the gastric or intestinal mucosa and lead to bleeding or perforation.
2. Thrombocytopenia or other blood disorders: Nisylat may increase bleeding disorders and lead to bleeding.
3. Severe renal or hepatic impairment: Use of Nisylat may aggravate these conditions and cause complications.
4. Asthma, rhinitis, nasal polyps: Naisylate may cause increased symptoms of asthma or allergic reactions.
5. Complete or partial closure of the arterial canal in the fetus in the second and third trimesters of pregnancy: The use of Naysilat may lead to 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: The use of the drug may cause allergic reactions in persons sensitive to this drug.
7. Postoperative condition after coronary artery bypass grafting: The use of Naisilate may increase the risk of cardiac complications and hemorrhagic complications after surgery.

Side effects The crowbar

1. Dyspeptic symptoms: Include abdominal discomfort or pain, nausea, vomiting, diarrhea, or constipation.
2. Gastrointestinal ulcers: Includes gastric or duodenal ulcers, gastrointestinal bleeding, and gastrointestinal perforation.
3. Gastrointestinal bleeding: May occur through blood in the stool or vomit and can be a serious complication.
4. Liver dysfunction: Includes increased levels of liver enzymes in the blood (ALT, AST), hepatitis and jaundice of the skin and sclera.
5. Kidney dysfunction: May manifest itself through increased creatinine and urea levels in the blood, swelling and changes in urinary frequency.
6. Systemic allergic reactions: May include urticaria, pruritus, angioedema, and even anaphylaxis.
7. Blood disorders: May manifest through thrombocytopenia, agranulocytosis, anemia and other changes in blood composition.
8. Cardiovascular complications: Include increased blood pressure and deterioration of cardiac function.
9. Central and peripheral nervous systems: May manifest through headache, dizziness, drowsiness, insomnia, or nerve pain.
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 imbalance.
2. Stomach pain: Overdose may cause abdominal pain, which may be due to irritation of the stomach or intestinal mucosa.
3. Dizziness and drowsiness: Excessive consumption may cause dizziness, drowsiness and central nervous system depression.
4. Hypertension: Possible increased blood pressure and associated symptoms such as headache, palpitations, etc.
5. Kidney and liver damage: In case of overdose, damage to the kidneys and liver is possible, which may be manifested by increased blood levels.
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 ulcers and gastrointestinal bleeding.
2. Acetylsalicylic acid (aspirin): Using Nisylate with aspirin may increase the risk of developing ulcerative complications.
3. Glucocorticosteroids: Concomitant use of Naysylate with glucocorticosteroids, such as prednisolone or dexamethasone, may increase the risk of ulcerative complications.
4. Drugs that affect blood clotting: Nisylat may enhance the effects of anticoagulants (for example, warfarin), platelet antiplatelet agents (for example, a cardioprotective dose of aspirin), which may increase the risk of bleeding.
5. Drugs that increase blood pressure: Naisylate may reduce the effectiveness of antihypertensive drugs such as ACE inhibitors or beta blockers.
6. Lithium: Using Nisylate with lithium may increase lithium levels in the blood, which may result in toxic effects.
7. Methotrexate: Nisylate may increase the toxicity of methotrexate by decreasing its elimination, especially with long-term use.

Storage conditions

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

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

Avoid freezing the drug, as this may change its structure and potency.