DICLOREUM ® Diclofenac sodium

DICLOREUM ® 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

Indications DICLOREUM ® Diclofenac sodium

DICLOREUM ® is indicated in the symptomatological treatment of inflammatory and painful states associated with traumatic conditions, rheumatic and musculoskeletal disorders.

Mechanism of action DICLOREUM ® Diclofenac sodium

Diclofenac is today one of the most widely used non-steroidal anti-inflammatory drugs in the treatment of both musculoskeletal and systemic inflammatory states.

The therapeutic efficacy of this active principle is due to its particular biological role, which is able to inhibit certain enzymes known as cyclooxygenases (COX) involved in the metabolism of membrane phospholipids.

More precisely, in the course of traumas and tissue damage, the cells involved in this type of pathology undergo a series of cellular modifications, such as to increase the expression of the aforementioned enzymes, catalysts of the reactions that from arachidonic acid lead to the synthesis of prostaglandins, biologically active molecules capable of increasing vascular permeability, inducing vasodilation and facilitating the development of an inflammatory reaction in place.

Excessive activation of this pathway, inevitably accompanied by a significant increase in prostaglandins with inflammatory activity, results in a typical symptomatology characterized by pain, fever and asthenia, which can fortunately be modulated through the use of non-steroidal anti-inflammatory drugs.

DICLOREUM ® in prolonged-release hard capsules also improves the pharmacokinetic properties of diclofenac, significantly reducing the irritative effect of this active ingredient against gastric mucosa, thereby limiting the onset of gastritis or peptic ulcers that are often associated to NSAID therapy.

Studies carried out and clinical efficacy

1.DICLOFENAC AND OPHTHALMOPATHY OF GRAVES

Arq Bras Endocrinol Metabol. 2011 Dec; 55 (9): 692-5.

In this pilot study, diclofenac has proved effective and safe in the treatment of Graves ophthalmopathy, thus representing a treatment with excellent cost / benefit ratios. However, more significant clinical trials are needed to fully clarify the possibility of including ophthalmopathy among the therapeutic indications of diclofenac.

2. DICLOFENAC AND PANCREATITE POST OPERATORIA

Endoscopy. 2012 Jan; 44 (1): 53-9. Epub 2011 Dec 23.

Work demonstrating that combined therapy between diclofenac and somatostatin may reduce some complications of retrograde cholangiopancreatography such as acute pancreatitis. This property could result in improved prognosis.

3. THE DICLOFENAC AS A FIRST CHOICE DRUG IN THE TREATMENT OF OSTEOARTRITIS

Curr Med Res Opin. 2012 Jan; 28 (1): 163-78.

Despite the marketing of new drugs, diclofenac still remains the drug of choice in the treatment of osteoarthritis, proving to be effective and safe with predictable and controllable side effects.

Method of use and dosage

DICLOREUM ®

150 mg prolonged release hard capsules of diclofenac sodium;

100 mg suppositories of sodium diclofenac;

Vials for intramuscular use from 75mg of diclofenac sodium;

"Retard", 100 mg tablets of diclofenac sodium;

The therapeutic range envisaged for the treatment of inflammatory states with diclofenac fluctuates between 75 mg and 150 mg daily based on the clinical characteristics of the patient and the relevance of his clinical picture.

Treatment should include the use of the minimum effective dose and for the shortest possible time in order to reduce the incidence of side effects associated with therapy with non-steroidal anti-inflammatory drugs.

The need to use higher doses or long-lasting therapies could be established by your doctor due to the presence of particularly resistant inflammatory states.

Warnings DICLOREUM ® Diclofenac sodium

The use of non-steroidal anti-inflammatory drugs should be limited as much as possible to cases of real need, given the different toxic effects described.

For this reason the therapy should include the use of the minimum effective dose for the time strictly necessary to guarantee an appreciable improvement in the symptoms.

All patients undergoing therapy with DICLOREUM ® should be supervised by their doctor, in order to avoid the occurrence of side effects, periodically monitoring the state of renal, hepatic and hematological function.

Particular attention should also be paid to patients suffering from hypertension, cardiac and cerebrovascular diseases given the potential association between diclofenac and aggravation of the clinical course of the aforementioned diseases.

In the case of occurrence of side effects, concentrated above all at the gastrointestinal level, the patient should immediately consult his doctor and eventually evaluate the need to suspend therapy.

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

PREGNANCY AND BREASTFEEDING

Different experimental studies and numerous case reports show how the intake of diclofenac and non-steroidal anti-inflammatory drugs during pregnancy and breastfeeding can determine the appearance of cardiopulmonary toxicity, sometimes lethal renal failure, malformations and premature abortions.

Furthermore, taking diclofenac in the immediate prepared phase could reduce the capacity for uterine contraction and increase the risk of bleeding in women.

Interactions

There are numerous documented drug interactions between diclofenac and other active ingredients.

Among these, the clinically relevant and noteworthy ones are the interactions with ACE inhibitors and angiotensin II antagonists, potentially responsible for increasing the side effects on the kidney, with analgesics, responsible for the alteration of the therapeutic efficacy of diclofenac, with antibiotics and methotrexate, whose simultaneous intake could lead to an increase in the toxicity of these drugs, with oral anticoagulants and antidepressants inhibiting serotonin reuptake, associated with an increased risk of bleeding.

It is also important to avoid the simultaneous use of more anti-inflammatories to reduce the insult to the gastric mucosa.

Contraindications DICLOREUM ® Diclofenac sodium

The intake of DICLOREUM ® 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

Although the formulation in suppositories or in prolonged release tablets may reduce the severity of some side effects associated with diclofenac therapy, it is useful to remember that taking non-steroidal anti-inflammatory drugs may lead to the appearance of nausea, vomiting, abdominal pain, dyspepsia, gastritis, peptic ulcers, hematemesis, melena and allergic reactions also of a dermatological nature.

Different research groups are instead working to characterize the association between chronic administration of NSAIDs and the appearance of heart, renal, hepatic and cerebrovascular insufficiency.