ASACOL ® Mesalazine

ASACOL ® is a drug based on mesalazine

THERAPEUTIC GROUP: Non-steroidal intestinal anti-inflammatory - Aminosalicylic acid and analogues

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

Indications ASACOL ® Mesalazine

ASACOL® is an intestinal anti-inflammatory drug, used in the treatment of intestinal inflammatory forms such as Crohn's disease and ulcerative colitis.

The various formulations provided allow treatment in the various stages of the disease.

Mechanism of action ASACOL ® Mesalazine

Mesalazine, contained in ASACOL ® is an anti-inflammatory belonging to the broader category of aminosalicylic acids, with selective action against the intestinal mucosa.

This typical characteristic is essentially associated with the pharmacokinetic properties of the active principle, which, taken orally in the form of gastro-resistant tablets, is able to pass undamaged the gastric acid barrier and be released at the ileal level, where it performs its therapeutic action.

In fact topical anti-inflammatory action is possible thanks to the reduced rate of systemic absorption of mesalazine, which, concentrating at the intestinal level, is able to inhibit the production of chemical inflammatory mediators such as arachidonic acid metabolites (prostaglandins, thromboxanes and leukotrienes) ) safeguarding the integrity of the intestinal mucosa.

While the portion of the active drug will subsequently be excreted through the faeces, the very small amount absorbed, following hepatic and intestinal acetylation, will be eliminated mainly through the urine.

Studies carried out and clinical efficacy

1. MESALAZINE IN THE ULCERATIVE COLITIS

Ulcerative colitis is one of those diseases of the intestinal tract for which mesalazine therapy is indicated. In this clinical trial it was noted that the intake of mesalazine at high doses for 2 weeks could provide rapid relief to the main symptoms of the disease, such as rectal bleeding and painful evacuations, which lasted up to 6 weeks in most patients treated.

2. MESALAZINA AND CHRONIC INFLAMMATORY DISEASES: THE STATE OF THE ART

Despite the numerous studies that populate the international literature on the efficacy of mesalazine and of the other active ingredients belonging to the family of aminosalicylic acids in the treatment of inflammatory bowel diseases, from a statistical point of view, it is not yet possible to formulate a single opinion. This evidence therefore suggests the importance of starting new clinical trials, with numerous samples and standardized protocols, which can provide the clinician with an evaluation parameter.

3. MESALAZINA AND PREVENTION

An interesting Italian study that showed how the cyclical intake of mesalazine for 10 days a month, in a 5-year clinical trial, could reduce the incidence of diverticulitis in patients suffering from intestinal problems. However, this study, of little statistical value, assumes particular importance from the clinical point of view, given the preventive action of mesalazine.

Method of use and dosage

ASACOL ® mesalazine 400/800 mg gastro-resistant tablets or mesalazine 400 mg modified-release capsules: useful both in the treatment of active phases and in the prevention of recurrences, it is recommended to take 1 - 2 tablets or 400 capsules mg three times a day.

The intake should be preferred on an empty stomach, and under strict medical supervision.

ASACOL ® suppositories of 500 - 1000 mg of mesalazine : useful in the treatment of inflammatory diseases localized to the rectal level, it is recommended to take a suppository of 1 gr once a day or 2 - 3 suppositories of 500 mg a day.

In any case, in order for the drug to perform its maximum therapeutic action, it is necessary for the suppository to be retained for long periods, such as at night.

ASACOL ® rectal foam of 1 - 2 - 4 gr of mesalazine and rectal suspension of 2 - 4 gr / 50 ml: indicated for the treatment of rectal and sigmoid affections it is recommended to take 1 dose of rectal foam or rectal suspension of 2 gr, Once or twice a day.

The intake should preferably take place in the morning and at bedtime.

All the aforesaid dosages, are purely indicative, as the doctor could vary the dosage and the timing of intake based on the patient's clinical conditions.

Warnings ASACOL ® Mesalazine

Given the partial hepatic and renal metabolism of mesalazine, the intake of ASACOL ® should be done with particular care and under strict medical supervision in patients with reduced liver and kidney function, for which periodic monitoring of these two organs would be necessary.

The same care should be given to patients suffering from changes in the hematological pattern, for which the intake of mesalazine could coincide with severe blood dyscrasias.

The nature of the active ingredient and the presence of easily allergenic excipients can be responsible for allergic reactions, even of a serious nature, in hypersensitive patients, so it would be useful to stop the therapy immediately.

The presence of lactose in ASACOL ® gastro-resistant tablets may be associated with the development of adverse reactions in the gastro-intestinal tract in patients with glucose / galactose malabsorption or lactase enzyme deficiency.

Despite the fact that the drug is not capable of altering the patient's perceptive capacities, some of its side effects, and in particular the headache, could make the use of machinery and driving vehicles dangerous.

PREGNANCY AND BREASTFEEDING

The absence of clinical trials and significant studies regarding the use of Mesalazine during the period of pregnancy and lactation and the relative effects on the health of the fetus and infant, prevent the characterization of the safety profile of ASACOL ®

For this reason, taking this medicine should not be recommended during the period of pregnancy and breastfeeding.

Interactions

Although the low systemic absorption of mesalazine significantly reduces the risk of possible interactions, it is advisable to avoid the simultaneous intake of agents such as lactulose capable of lowering the intestinal lumen pH, delaying the release of mesalazine and drugs from renal metabolism, in order to to reduce the risk of kidney disease.

Concomitant intake of corticosteroids, useful in the acute phases of the disease, could determine a significant increase in the anti-inflammatory potential of mesalazine.

Finally ASACOL ® could interact with active ingredients such as coumarin, methotrexate, probenecid, sulfinpyrazone, spironolactone, furosemide, rifampicin and sulfonylureas with effects not entirely characterized.

Contraindications ASACOL ® Mesalazine

ASACOL ® is contraindicated in patients with known hypersensitivity to the active ingredient or analogues belonging to the salicylate family, and in patients with lesions of the gastric and duodenal mucosa or severe nephropathy.

ASACOL ® is also contraindicated in children under the age of 2 years and in women in the last weeks of pregnancy or during breastfeeding.

Undesirable effects - Side effects

The intake of mesalazine was found to be well tolerated and free of clinically significant side effects.

The most commonly observed adverse reactions involved the gastro-intestinal tract with nausea, diarrhea and abdominal pain and the nervous one with headache.

On several occasions a hypersensitivity symptomatology with skin rash, pruritus, rash and fever was found for which it was necessary to stop the therapy rapidly.

The changes in the hematologic picture and related to renal and hepatic function were decidedly more rare.