AIRTAL ® Aceclofenac

AIRTAL © is a drug based on Aceclofenac

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

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

Indications AIRTAL ® Aceclofenac

AIRTAL® is indicated in the treatment of inflammatory diseases of rheumatic origin such as osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, periarthritis, tendinitis, bursitis and enthesitis.

Aceclofenac, especially in solution for injection, is successfully used in the treatment of acute pain of various kinds (post-operative, colic, gouty).

Mechanism of action AIRTAL ® Aceclofenac

AIRTAL ® is a non-steroidal anti-inflammatory drug based on aceclofenac, an active ingredient belonging to the phenylacetic acid derivative category, such as diclofenac, with which it shares the same mechanism of action.

In fact taken orally, aceclofenac is absorbed by the intestinal mucosa as such and bound in circulation by the plasma proteins, distributed to the various tissues and in particular to the synovias where it concentrates for more than 57% of the total assumed quota.

In these tissues the aceclofenac performs its therapeutic action, inhibiting the cyclooxygenases, enzymes involved, during traumas or harmful stimuli, in the transformation of arachidonic acid into prostaglandins, molecules endowed with a marked pro-inflammatory activity, guaranteed by the vasodilatory action and permeabilizing, able to increase the recruitment and passage of inflammatory cells and mediators.

The modulatory effect on the metabolism of arachidonic acid is also completed with the increased synthesis of lipoxins, chemical mediators able to inhibit both the chemotaxis and the process of leukocyte adhesion, significantly reducing the inflammatory and painful insult exercised towards the tissue injured.

Aceclofenac, after a half-life of about 6-8 hours, is metabolized to the hepatic level and eliminated following glucuronation mainly via the urine.

Studies carried out and clinical efficacy

1. ACECLOFENAC AND NEW RELEASE METHODS

Clin Drug Investig. 2012 Feb 1; 32 (2): 111-9

Important advances are being made in the search for new pharmaceutical formulations capable of optimizing the release of aceclofenac, reducing side effects and increasing therapeutic action instead. In this sense, the study tests some pharmacokinetic characteristics linked to new delivery systems.

2. ACECLOFENAC AND KNEE OSTEOARTRITIS

J Pain. 2011 May; 12 (5): 546-53.

Study showing that the controlled-release intake of aceclofenac has the same therapeutic effects as the conventional one in the treatment of knee osteoarthritis. The advantage deriving from these new formulations is essentially to be sought in the possibility of administering the drug only once a day.

3. THE INFFICACY OF ACECLOFENAC INTRACTING POST-OPERATIVE PAIN

Cochrane Database Syst Rev. 2009 Jul 8; (3): CD007588.

Anti-current study that demonstrates, in light of the numerous studies in the literature, the ineffectiveness of aceclofenac, in the treatment of acute post-operative pain.

Consequently the use of this drug is not justified in the above cases.

Method of use and dosage

AIRTAL ®

100 mg coated tablets of aceclofenac;

powder for oral suspension of 100 mg of aceclofenac:

the therapeutic scheme envisaged for the treatment of inflammatory and painful states, generally involves the intake of 200 mg of aceclofenac daily, taken in two different administrations spaced at least 12 hours apart.

The dosage used may undergo variations for elderly patients or those suffering from kidney and liver disease.

Warnings AIRTAL ® Aceclofenac

Treatment with AIRTAL ® should be limited to cases of real need, and generally for short periods of time, in order to limit the occurrence of serious side effects.

Particular attention should be paid to elderly patients or those suffering from renal, hepatic, gastro-intestinal and cardiovascular diseases, in which the incidence and clinical severity of the possible side effects is more important.

For this reason the doctor should periodically assess the state of renal, hepatic, coagulative and cardiovascular function, suspending therapy in the event of worrying signs and symptoms.

It is also useful to remember that the simultaneous food intake may delay the intestinal absorption of the aceclofenac, reducing however the irritative action on the gastric mucosa, therefore being indicated in patients suffering from gastric pathologies, in which furthermore it should be evaluated the possible need to resort to the use of gastroprotectors.

It is advisable to start treatment with the minimum effective dose, in order to avoid the appearance of side effects.

PREGNANCY AND BREASTFEEDING

The intake of AIRTAL ® is not recommended during pregnancy and in the subsequent period of breastfeeding, given the presence in the literature of studies demonstrating the numerous side effects on the fetus linked to high blood concentrations of non-steroidal anti-inflammatory drugs.

Fetal malformations and unwanted abortions associated with the abuse of non-steroidal anti-inflammatory drugs seem to be linked to the inhibitory action on prostaglandins, which are important in ensuring the correct process of embryonic and fetal development.

The intake of these drugs is also responsible for an increased risk of hemorrhage in the mother at the time of delivery and the reduction, in intensity and frequency, of uterine contractions.

Interactions

There are numerous drug interactions described for non-steroidal anti-inflammatory drugs for oral use, including also aceclofenac.

More precisely, pharmacokinetic studies demonstrate how the contextual intake of

Oral anticoagulants and inhibitors of serotonin reuptake, could increase the risk of bleeding;
Diuretics, ACE inhibitors, angiotensin II antagonists, methotrexate and cyclosporine could exacerbate side effects, and especially those on the kidney level;
Non-steroidal anti-inflammatory drugs and corticosteroids could intensify the action of damage to the varicose vein of the gastric mucosa;
Antibiotics could alter the therapeutic efficacy of both active ingredients;
Sulfonylureas could determine an altered glycemic control, exerted by the hypoglycemic effect of aceclofenac.

Contraindications AIRTAL ® Aceclofenac

Taking AIRTAL ® is contraindicated in patients who are hypersensitive to the active ingredient or to one of its excipients, hypersensitive to acetylsalicylic acid and other analgesics, suffering from asthma, nasal polyposis, liver failure, renal to cardiac, intestinal bleeding, ulcerative colitis, Crohn's disease or previous history for the same conditions.

Undesirable effects - Side effects

The use of non-steroidal anti-inflammatory drugs, including aceclofenac, is generally associated with the onset of side effects, in some cases clinically relevant.

These reactions generally affect:

The gastro-enteric apparatus with nausea, abdominal pain, vomiting, diarrhea and dyspepsia and rarely gastritis and peptic ulcers;
The nervous system with insomnia, headache, drowsiness and vertigo;
The skin, subjected to an increased risk of hives, rash, photosensitivity and bullous reactions.

It is also useful to remember that numerous epidemiological studies associate prolonged administration of non-steroidal anti-inflammatory drugs with the appearance of renal, hepatic, cardio and cerebrovascular diseases.