DEFLAMAT ® Diclofenac sodium

DEFLAMAT ® is a drug based on Diclofenac sodium

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

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

Directions DEFLAMAT ® Diclofenac sodium

DEFLAMAT ® is indicated in the treatment of inflammatory states of rheumatic origin (rheumatoid arthritis, ankylosing spondylitis, arthrosis) and extrareumatic or post-traumatic.

DEFLAMAT ® is also indicated in the treatment of acute gout episodes and in the symptomatic treatment of inflammatory and painful pathologies of the musculoskeletal system.

Mechanism of action DEFLAMAT ® Diclofenac sodium

DEFLAMAT ® is a non-steroidal anti-inflammatory drug based on diclofenac, an active ingredient belonging to the chemical category of acetic acids.

The analgesic and anti-inflammatory activity of these drugs is carried out through the inhibition of an enzymatic class, known as cyclooxygenase (COX), able to catalyze the reaction that leads to the production of prostaglandins starting from membrane phospholipids such as arachidonic acid .

This reaction, which is particularly active following traumatic or damaging events affecting the cell, makes it possible above all through the COX 2 pathway (inducible isoform) to produce a series of molecules with marked pro-inflammatory and algic activity, increasing the vascular permeability and the recall of inflammatory cells with the related biological response.

The persistence of the inflammatory process, the activation of which is physiologically intended as an organic response to harmful agents, is often responsible for the painful symptoms observed in phlogistic states and in the extensive tissue damage that is observed in autoimmune or chronic pathologies.

From the pharmacokinetic point of view however, diclofenac taken orally, is absorbed by the intestinal mucosa and distributed to the various tissues, only after a first-pass metabolism, which significantly reduces its bioavailability.

It is the same liver that catabolizes this active ingredient, guaranteeing its excretion mainly through the kidneys.

Studies carried out and clinical efficacy

1. FANS AND DAMAGE TO MUCOSA

Aliment Pharmacol Ther. 2012 Feb 28.

Endoscopic study that showed how diclofenac can exert damage at the level of gastric mucosa lower than that determined by acetyl salicylic acid but higher than that determined by iboprufene.

2.DICLOFENAC AND MIGRAINE

Cochrane Database Syst Rev. 2012 Feb 15; 2: CD008783.

Work demonstrating the efficacy of diclofenac in the treatment of acute migraine, providing pain relief and associated symptomatology. Only a fraction of the patients did not benefit from this type of therapy.

3. DICLOFENAC AND FETAL HEALTH

Pediatr Nephrol. 2012 Feb 14.

Case reports showing that taking diclofenac during pregnancy can induce renal failure in the newborn, sometimes irreversible, leading to premature death in the first 20 days of life.

Method of use and dosage

DEFLAMAT ®

75 mg or 100 mg capsules of diclofenac sodium;

Vials for intramuscular use of 70 mg of diclofenac sodium:

Intake of a 75 mg daily tablet or 100 mg of diclofenac sodium is generally sufficient to attenuate the pain symptoms expected during musculoskeletal and inflammatory conditions.

During particularly intense pathologies, the doctor may decide to increase the dosage up to the maximum amount of 150 mg daily, preferably divided into two distinct assumptions, given the reduced half-life of the active ingredient.

The intramuscular intake of DEFLAMAT ® should instead be reserved for patients suffering from gastro-intestinal disorders with contextual musculoskeletal pathology.

Warnings DEFLAMAT ® Diclofenac sodium

Taking DEFLAMAT ® should be prescribed by your doctor, after carefully assessing the patient's state of health and the possible presence of potential contraindications,

Treatment with non-steroidal anti-inflammatory drugs should be limited to the shortest possible time necessary to guarantee a remission of the symptoms, in order to avoid the appearance of side effects especially on the gastrointestinal mucosa.

In this regard it is necessary to avoid the concomitant intake of several anti-inflammatories at the same time, immediately reporting to your doctor the possible appearance of abdominal pain, bleeding or symptoms potentially indicative of a gastrointestinal disease, so that you can decide for any suspension of treatment .

All patients undergoing diclofenac therapy should be supervised by their physician, who should in turn periodically monitor the state of renal, hepatic, hematopoietic and coagulative function, in order to avoid the appearance of unpleasant side effects.

The doctor should also carefully evaluate the cost / benefit ratio deriving from the intake of DEFLAMAT ® in patients suffering from hypertension, cardiac and cerebrovascular diseases, known epidemiological data indicative of an increased risk of possible aggravations.

The presence in DEFLAMAT ® vials of benzyl alcohol and other potentially allergenic excipients could increase the risk of hypersensitivity reactions in atopic or particularly predisposed patients.

PREGNANCY AND BREASTFEEDING

The use of DEFLAMAT ® is strongly contraindicated during pregnancy given the effects of the "pathological" absence of prostaglandins on gestation outcomes.

Cardiopulmonary toxicity, renal dysfunction, inhibition of uterine contractions, increased incidence of malformations and abortions are the main risks associated with the use of NSAIDs during pregnancy.

Interactions

Given the hepatic metabolism that distinguishes diclofenac and its particular biological role, various pharmacokinetic studies have tried to better characterize the possible pharmacokinetic interactions expected for diclofenac.

More precisely, the contextual assumption of

ACE inhibitors and angiotensin II antagonists, could increase the risk of kidney failure;
Analgesics, could alter the therapeutic profile of diclofenac;
Antibiotics, given the cytochromial metabolism they face, could be associated with the appearance of side effects linked to the unpredictable increase in blood concentrations of the antibacterials used;
Oral anticoagulants or antidepressants that inhibit serotonin reuptake, would be responsible for an increased risk of bleeding;
Corticosteroids and other NSAIDs could increase the side effects expected for anti-inflammatory therapy, especially for the gastric mucosa;
Methotrexate, would be potentially toxic, due to the increase in blood concentrations of this drug.

Contraindications DEFLAMAT ® Diclofenac sodium

The use of DEFLAMAT ® is contraindicated in patients who are hypersensitive to the active ingredient or to one of its excipients, suffering from gastrointestinal diseases, with a history of gastrointestinal ulcers and bleeding and suffering from haemostasis and coagulation disorders.

Undesirable effects - Side effects

Intake of non-steroidal anti-inflammatory drugs such as diclofenac is often associated with the appearance of side effects with an acute and sometimes chronic course.

Nausea, vomiting, abdominal pain, dyspepsia and rarely hypersensitivity reactions represent the main adverse reactions linked to the administration of the aforementioned active ingredient, although the direct irritative action on the gastric mucosa and the inhibition of prostacicline production with gastroprotective activity could significantly increase the risk of gastritis, peptic ulcers, hematemesis and melena.

On the other hand, prolonged use of NSAIDs may increase the risk of edema, hypertension, heart failure, hematopoietic changes, renal and hepatic failure.