ZYLORIC ® Allopurinol

ZYLORIC ® is an allopurinol based drug

THERAPEUTIC GROUP: Anti-gout - Xanthine oxidase inhibitors

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

Directions ZYLORIC ® Allopurinol

ZYLORIC ® is indicated in the prophylaxis of gout and the formation of kidney stones containing uric acid and calcium oxalates.

This medicine is also used to prevent hyperuricemia induced by anticancer chemotherapy.

Mechanism of action ZYLORIC ® Allopurinol

Allopurinol, the active ingredient of ZYLORIC ®, is a structurally very similar molecule to hypoxanthine, with which it competes as a substrate of numerous enzymes.

From the therapeutic point of view, the anti-gout efficacy of this active principle is due to its ability to inhibit an enzyme belonging to the oxide reductase family, known as xanthine oxidase, responsible for the conversion of xanthine and hypoxanthine to uric acid, a pathogenic element of gout and uratic lithiasis.

The excess of uric acid, therefore associated with an increased activity of xanthine oxidase, is supported by the increasing concentrations of xanthine, a product derived from the catabolism of purines and hypoxanthine in particular.

However at the base of the pathogenesis of gout, in addition to an increased production of uric acid, fed by diets with high protein content or by particular pharmacological therapies, it is also possible to include alterations in the urinary excretion of this metabolite or congenital deficits that are the basis of syndromes characterized by severe clinical course.

The therapeutic efficacy of allopurinol is also facilitated by the excellent pharmacokinetic properties, which allow the rapid gastrointestinal absorption of this active ingredient and the biotransformation in metabolites endowed with biological activity such as oxyporinol.

Studies carried out and clinical efficacy

1.POLYMORPHISMS AND ADVERSE REACTIONS TO ALLOPURINOL

Br J Dermatol. 2012 Feb 20.

Very interesting study that demonstrates how the presence of a particular polymorphism in the HLA-B gene can significantly increase the risk of developing adverse reactions to allopurinol, with the appearance of skin lesions and related scars.

2. THE CARDIOVASCULAR EFFECTS OF ALLOPURINOL

Cardiol Rev. 2011 Nov-Dec; 19 (6): 265-71.

Experimental study that extends the therapeutic effects of allopurinol also to the treatment of some cardiovascular pathologies.

More precisely, this active ingredient could represent a potential drug for the treatment of ischemia cardiomyopathy and congestive heart failure.

3. ALLOPURINOL: FIRST LINE DRUG IN THE TREATMENT OF THE GOTTA

Clin Pharmacol Ther. 2011 Sep; 90 (3): 363-4.

Study that reaffirms the importance of allopurinol in the treatment of chronic gout.

In fact, despite the introduction into the market of new active ingredients useful in the treatment of gout and urinary lithiasis, allopurinol remains the most effective drug and therefore to be considered as a first-line strategy in urinary-therapy.

Method of use and dosage

ZYLORIC ®

100 mg or 300 mg tablets of allopurinol;

300 mg dispersible granules of allopurinol.

Treatment with allopurinol should be defined by your doctor, based on your blood uric acid level, state of kidney function and the severity of the clinical picture.

Generally, the dosing schedule provides for the start of therapy at low doses (100 mg daily) to be possibly adapted up to the normalization of the uricemia; in this regard the 300 mg of uric acid per day are generally sufficient to rebalance the blood concentrations of this element.

However, the doctor could reserve treatments at even higher doses in patients with severe disorders.

We recommend taking ZYLORIC ® every day at the same time, preferably after meals.

Warnings ZYLORIC ® Allopurinol

All treatment with allopurinol should be supervised by your doctor, in order to avoid the appearance of even serious adverse reactions and at the same time guarantee maximum therapeutic efficacy.

Particular attention should be paid to patients suffering from renal and hepatic insufficiency, for whom the risk of developing side effects is increased.

Furthermore, given the possible appearance of acute gouty articular attacks following the immediate intake of allopurinol, it would be indicated to administer non-steroidal anti-inflammatory drugs or colchicine in the initial phases of the treatment.

It is also advisable to increase the daily intake of water, in order to facilitate both the urinary excretion of uric acid and that of the allopurinol catabolites.

Taking ZYLORIC ® may occasionally cause drowsiness, so the patient should assess their cognitive abilities before driving cars.

The presence of lactose in ZYLORIC ® could be problematic for patients suffering from glucose galactose malabsorption, lactose intolerance or lactase enzyme deficiency.

PREGNANCY AND BREASTFEEDING

The absence of clinical trials and the presence of contradictory experimental studies relating to the potential toxic effects of allopurinol on the health of the fetus and the suckling child, push the experts to advise against the use of ZYLORIC ® during pregnancy and in the subsequent period of breastfeeding at breast, unless it is strictly necessary.

Interactions

Different pharmacokinetic studies have shown the presence of different interactions, some of which are clinically relevant, between allopurinol and different active ingredients.

The most important are those with:

ACE inhibitors, responsible for an increased risk of toxicity especially in the presence of patients suffering from renal failure;
Antibiotics such as amoxicillin and ampicillin, for which an increased risk of developing skin rashes has been observed;
Oral anticoagulants, dangerous due to the increased risk of bleeding;
Antivirals, theophylline, and cyclosporine accompanied by an increase in blood concentrations and the related risk of toxicity;
Cytotoxic, responsible for a potential increase in the toxicity of azathiopyrin and mercaptopurine;
Uricosuric, able to increase the renal clearance of allopurinol and of hypoporinol, reducing its therapeutic effect.

Contraindications ZYLORIC ® Allopurinol

The use of ZYLORIC ® is contraindicated in patients hypersensitive to the active ingredient or to one of its excipients, and as a pharmacological treatment of the acute gout episode.

Undesirable effects - Side effects

Although in most patients the treatment with ZYLORIC ® is well tolerated and at the most accompanied by clinically insignificant side effects, in rare cases, concentrated above all among patients suffering from renal and hepatic insufficiency, the appearance of hypersensitivity reactions has been observed with skin rash, fever, skin exfoliation and vasculitis, gastrointestinal disorders, asthenia, malaise, vertigo, drowsiness, changes in vision and taste, hypertension, alopecia, hepatotoxicity, paresthesia and neuropathies, gynecomastia and haematological disorders.

In all these cases it is of fundamental importance to consult your doctor immediately and if you wish to opt out of treatment.