drugs

LIOMETACEN ® Indomethacin

LIOMETACEN ® is a drug based on Indomethacin meglumine

THERAPEUTIC GROUP: Non-steroidal anti-inflammatory and antirheumatic drugs

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Indications LIOMETACEN ® Indomethacin

LIOMETACEN ® is indicated for the treatment of acute pain based on inflammation of the musculoskeletal system.

Mechanism of action LIOMETACEN ® Indomethacin

LIOMETACEN ® is a drug based on indomethacin, the active ingredient derived from arylacetic acid and listed among the non-steroidal anti-inflammatory drugs.

The characteristic efficacy of LIOMETACEN ® in the treatment of acute pain affecting the musculoskeletal system for both rheumatic and post-traumatic pathologies is due to the particular pharmacokinetic properties of this medicine, which allow its active ingredient, once administered for intramuscular way, to reach the plasma peak in just 30 minutes, carrying out a significant therapeutic action immediately.

The latter, as is the case for all other non-steroidal anti-inflammatory drugs, is supported by the ability of indomethacin to inhibit an enzymatic class known as cyclooxygenase, whose activation, which is particularly intense due to various kinds of damaging stimuli, allows the transformation of membrane phospholipids such as arachidonic acid into chemical mediators endowed with vasopermeabilization, chemotactic and algogenic activity, known as prostaglandins.

The possibility of reducing the on-site presence of these molecules therefore translates into a reduction of the inflammatory insult with a harmful and painful nature, which is therefore accompanied by various inflammatory states, both traumatic and rheumatic.

After its action, the indomethacin after hepatic glucuronation is eliminated mainly through the urine.

Studies carried out and clinical efficacy

1. THE EFFECTIVENESS OF INDOMETHACIN IN PREMATURE BORN

Pediatr Int. 2012 Feb 20.

Interesting study that demonstrates how the use of low doses of indomethacin in premature babies, taking advantage of the vasodilatory properties typical of NSAIDs, can favor the normal vascularization of the kidney and intestine, limiting the onset of potential complications.

2. INDOMETHACIN IN THE TREATMENT OF EMICRANIA AND CEFALEA

CNS Drugs. 2011 Apr; 25 (4): 343-58.

Recent study demonstrating that the intake of indomethacin, together with that of prochlorperazine and caffeine, may represent a valid therapeutic option in the treatment of acute migraine and tension-type headache.

3. INDOMETHACIN IN ORTHOPEDIC PRACTICE

Strahlenther Onkol. 2009 Aug; 185 (8): 500-5. Epub 2009 Aug 4.

Study demonstrating that the combined treatment of radiotherapy and indomethacin may be more effective in preventing heterotopic ossification, as a complication of total hip replacement surgery.

Method of use and dosage

LIOMETACEN ®

Powder and solvent for solution for injection of 25 - 50 mg of indomethacin.

The treatment of acute pain states includes a posological scheme consisting of an attack phase characterized by a deep intramuscular administration of 1 or 2 ampoules of LIOMETACEN ® per day, depending on the medical indications and the severity of the pathological picture.

Intramuscular inoculation should preferably take place at the level of the upper-outer quadrant of the buttock.

The use of LIOMETACEN ® intravenously is indicated exclusively in hospital practice.

Warnings LIOMETACEN ® Indomethacin

The use of LIOMETACEN ® must necessarily take place under strict medical supervision, given the numerous side effects associated with systemic therapy with non-steroidal anti-inflammatory drugs.

In order to limit the incidence of possible adverse reactions, it would be indicated to start treatment with the minimum effective dose, limiting the use of the medicine for the shortest possible time.

Particular caution must be reserved to atopic patients, suffering from hepatic, renal, gastro-intestinal and cardiovascular pathologies, given the capacity of the indomethacin to aggravate the clinical course of already present pathological pictures as well as to increase the incidence of new adverse events.

Should unexpected reactions appear or any exacerbations of the pathologies already present, the patient, after having contacted his doctor, should evaluate the possibility of suspending the therapy in progress.

The presence in LIOMETACEN ® of excipients with allergenic power, could increase the incidence of side effects related to hypersensitivity reactions in predisposed subjects, especially during the first month of treatment.

PREGNANCY AND BREASTFEEDING

Different studies show that the intake of non-steroidal anti-inflammatory drugs such as indomethacin during pregnancy, especially in the third trimester, may lead to a significant increase in the risk of fetal malformations, with such significant changes in renal and cardiopulmonary function, as to induce spontaneous abortions.

To the fetal side effects would also be added those to the mother, characterized by an increased risk of hemorrhage and complications at the time of delivery, linked to the reduction in the frequency and intensity of uterine contractions.

Interactions

During indomethacin therapy it is necessary to consider all the possible drug interactions capable of altering the normal pharmacokinetic profile of the active ingredient, varying both its therapeutic efficacy and its safety profile.

For this reason it would be necessary to avoid the simultaneous intake of indomethacin with:

  • Oral anticoagulants and inhibitors of serotonin reuptake, I note the increased risk of bleeding;
  • Diuretics, ACE inhibitors, angiotensin II antagonists, methotrexate and cyclosporine, given the increase in the possible toxic effects of indomethacin mainly on the kidney and liver;
  • Non-steroidal anti-inflammatory drugs and corticosteroids, responsible for significant damage to the gastric mucosa;
  • Antibiotics, whose intake is often linked to a significant variation in the therapeutic profile of both drugs;
  • Sulfonylureas, potentially dangerous for alterations affecting glucose homeostasis.

Contraindications LIOMETACEN ® Indomethacin

The intake of LIOMETACEN ® is contraindicated in case of hypersensitivity to the active substance or to one of its excipients, hypersensitivity to acetylsalicylic acid and other analgesics, nasal polyposis, asthma, bronchospasm, angioedema, peptic ulcer, history of intestinal bleeding, colitis ulcer, Crohn's disease or previous history for the same conditions, cerebrovascular bleeding, bleeding diathesis or concomitant anticoagulant therapy, renal failure and liver failure.

Undesirable effects - Side effects

Indomethacin shares the same side effects with all other non-steroidal anti-inflammatory drugs, which are currently one of the main complications associated with systemic NSAID therapy.

More precisely, the use prolonged over time or carried out at particularly high doses of indomethacin, could determine the appearance of nausea, constipation, diarrhea, epigastric pain, gastritis, ulcers and in severe cases haemorrhages, hepatotoxicity and liver failure, pulmonary edema and dyspnoea, hypertension, vasodilation, increased cerebral and cardiovascular accidents, angioedema, rash, increased sweating, urticaria and bullous reactions, alterations in renal function, headache, dizziness, vertigo, hyperkinesia and taste alterations.

To the aforementioned adverse reactions it is right to add those derived from possible hypersensitivity reactions to the drug or to one of its excipients, given the enteral route of administration.

Note

LIOMETACEN ® is salable only with a medical prescription.