Aponil

Aponil (nimesulide) is a drug used to relieve pain and inflammation. It is an anti-inflammatory drug (NSAID) that also has analgesic (pain-relieving) and antipyretic effects. Nimesulide is often used to relieve symptoms of rheumatic diseases, toothache pain, headaches, muscle pain, and other conditions.

It is important to remember that the use of nimesulide should be carried out in accordance with the instructions and recommendations of the doctor. This drug can have side effects and contraindications, and self-medication with it can be dangerous. Before starting to use nimesulide, it is important to consult a medical specialist.

Indications Aponila

• Rheumatic diseases: Aponil can be used to treat rheumatoid arthritis, osteoarthritis and other inflammatory joint diseases.
• Muscle Pain: It can be used to relieve pain from muscle strains, muscle strains, spasms and other muscle conditions.
• Back pain: Nimesulide can help with back pain, including low back pain and neck pain, caused by a variety of reasons, including muscle tension and inflammation.
• Headache: It can be used to relieve headaches including migraines and brain tension.
• Toothache: Aponil may help with toothache associated with dental caries, gum inflammation, or after dental procedures.
• Cold and Flu Symptoms: It can also be used to reduce fever and relieve common cold and flu symptoms such as fever and headache.

Release form

Tablets are the most common form of nimesulide. Tablets can be of different dosages, which allows you to select the optimal dose for each patient.

Pharmacodynamics

• Cyclooxygenase (COX) inhibition: Nimesulide inhibits the action of COX-1 and COX-2 enzymes, which are involved in the conversion of arachidonic acid to prostaglandins. COX-2 is usually activated in response to inflammatory processes, while COX-1 is present in tissues where it performs physiological functions. By inhibiting COX-2, nimesulide reduces the synthesis of prostaglandins, which leads to a decrease in inflammation, pain and fever.
• Analgesia (pain-relieving effect): By reducing the level of prostaglandins, nimesulide has an analgesic effect, relieving pain in various conditions such as rheumatic diseases, muscle pain and headaches.
• Anti-inflammatory action: Since prostaglandins are key mediators of inflammation, inhibition of their synthesis helps reduce the intensity of inflammatory processes.
• Antipyretic effect: Nimesulide can reduce body temperature by acting on the hypothalamus in the brain, which regulates thermoregulation.

Pharmacokinetics

• Absorption: Nimesulide is usually rapidly and completely absorbed from the gastrointestinal tract after oral administration. Maximum blood concentrations are usually reached 2-4 hours after administration.
• Bioavailability: The bioavailability of nimesulide is about 90%, which means that almost the entire dose taken enters the systemic circulation.
• Metabolism: Nimesulide is metabolized in the liver. The main metabolite is 4-hydroxynimesulide, which also has pharmacological activity.
• Protein binding: Approximately 99% of nimesulide is bound to plasma proteins, mainly albumin.
• Distribution: Nimesulide is evenly distributed in the body and penetrates into various tissues.
• Excretion: Nimesulide and its metabolites are excreted mainly through the kidneys (about 50-60%) and intestines (about 40-50%) as metabolites.
• Half-life: The half-life of nimesulide is about 2-4 hours.

Dosing and administration

• For adults:

  • The usual starting dose is 100 mg (1 tablet or capsule) twice daily after meals.
  • The maximum daily dose usually does not exceed 200 mg.

• For children:

  • Children are recommended to be prescribed a dose of nimesulide depending on their body weight and age. The pediatric dosage is usually determined by the doctor based on the individual characteristics of each child.

• Duration of admission:

  • The duration of treatment with nimesulide is usually limited to short-term use, no more than 15 days.
  • If it is necessary to continue treatment, the duration of the course should be discussed with the doctor.

• Use in elderly patients:

  • For elderly patients, dosage adjustment may be required according to their renal and hepatic function.

• Use in special groups:

  • During pregnancy and lactation, nimesulide is contraindicated or can only be used under strict medical supervision.
  • Patients with gastrointestinal diseases, asthma, kidney and liver diseases should be especially careful when using nimesulide.

Use Aponila during pregnancy

• Risk of congenital anomalies:

  • A study conducted in Italy showed that the use of nimesulide in the first trimester of pregnancy may be associated with an increased risk of congenital urinary tract anomalies in newborns. Women who took nimesulide in the first trimester had a 2.6-fold higher risk of such anomalies compared to those who did not take the drug (Cantarutti et al., 2018).

• Effects on the cardiovascular system of the fetus:

  • In another case, premature stenosis of the ductus arteriosus in the fetus, leading to right ventricular hypertrophy, was reported. This was associated with maternal use of nimesulide in late pregnancy (Sciacca et al., 2005).

• Oligohydramnios:

  • Oligohydramnios (low amniotic fluid) has also been reported in women taking nimesulide during pregnancy, which may lead to various complications in the fetus (Grinceviciene et al., 2016).

• Renal failure in newborns:

  • Newborns exposed to nimesulide during pregnancy may develop acute renal failure. In one case, a child whose mother took nimesulide during the last two weeks of pregnancy developed oliguric renal failure, which gradually resolved after birth (Landau et al., 1999).

Contraindications

• Gastric ulcer and duodenal ulcer: The use of nimesulide may increase the risk of exacerbation of gastric ulcer and gastrointestinal bleeding.
• Conditions associated with an increased risk of bleeding: For example, hemorrhagic diathesis, blood clotting disorders, hemorrhagic diathesis, etc.
• Liver failure: Nimesulide is metabolized in the liver, so its use may be contraindicated in case of dysfunction of this organ.
• Renal failure: Since nimesulide and its metabolites are excreted mainly through the kidneys, if their function is impaired, the drug may accumulate, which increases the risk of side effects.
• Asthma, rhinitis with nasal polyps and rhinitis caused by aspirin and other NSAIDs: In some patients, nimesulide may cause bronchospasm, especially in people with asthma or allergic rhinitis.
• Pregnancy and lactation: The use of nimesulide during pregnancy, especially in the third trimester, may be contraindicated due to the risk to the fetus. In addition, nimesulide can be excreted in breast milk, so its use during lactation may be undesirable.
• Paediatric population: The use of nimesulide in children under 12 years of age may be contraindicated due to the lack of sufficient data on efficacy and safety in this age group.

Side effects Aponila

• Gastrointestinal disorders: Includes dyspepsia (stomach upset), nausea, vomiting, diarrhea, bloating, and abdominal pain.
• Gastrointestinal ulceration: Nimesulide may increase the risk of developing gastric or intestinal ulcers, as well as gastrointestinal bleeding.
• Allergic reactions: Include skin rash, itching, swelling, angioedema, allergic dermatitis and rarely anaphylactic shock.
• Kidney and liver damage: Rarely, nimesulide can cause kidney or liver damage, which is manifested by increased levels of the corresponding indicators in the blood.
• Central nervous system: Headache, dizziness, drowsiness, insomnia, anxiety and irritability may occur.
• Systemic reactions: Include asthenia (weakness), increased body temperature, arterial hypertension (increased blood pressure), peripheral edema.
• Skin and appendage reactions: Urticaria, photodermatitis, skin redness, and hair loss may occur.
• Other reactions: Possible visual impairment, alopecia (hair loss), increased potassium levels in the blood (hyperkalemia), changes in the blood (anemia, thrombocytopenia), anuria (lack of urination), attack of bronchial asthma.

Overdose

Signs of overdose may include nausea, vomiting, abdominal pain, drowsiness, headache, hypertension (high blood pressure), and possible kidney and liver problems.

Interactions with other drugs

• Drugs that increase the risk of ulcer complications: Such as glucocorticoids, anticoagulants (eg, warfarin), antiplatelet agents (eg, acetylsalicylic acid), serticonazole, ketoconazole, erythromycin, cyclosporine, etc.
• Drugs that increase the risk of kidney and liver damage: For example, diuretics, angiotensin-converting enzyme inhibitors (ACEIs), lithium, methotrexate, cyclosporine, etc.
• Drugs that increase the risk of bleeding: For example, anticoagulants, antiplatelet agents, glucocorticoids, selective serotonin reuptake inhibitors (SSRIs), which reduce platelet levels (eg, ticlopidine).
• Drugs that increase the risk of damage to the gastrointestinal mucosa: Such as alcohol, coxibs, glucocorticoids, selective serotonin reuptake inhibitors (SSRIs), anticoagulants, antiplatelet agents, etc.
• Drugs that reduce the effectiveness of nimesulide: For example, aspirin and other NSAIDs, which can compete for the binding site with COX-1 and COX-2.