ZYLORIC ® Allopurinol

ZYLORIC ® is an allopurinol-based drug

THERAPEUTIC GROUP: Antigoutoses - Xanthinoxidase inhibitors

Indications 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 in the prevention of hyperuricaemia induced by anticancer chemotherapy.

Mechanism of action ZYLORIC ® Allopurinol

Allopurinol, the active ingredient of ZYLORIC ®, is a molecule structurally very similar to hypoxanthine, with which it competes as a substrate of numerous enzymes.
From the therapeutic point of view, the antigout efficacy of this active ingredient is due to the ability to inhibit an enzyme belonging to the oxide reductase family, known as xanthinoxidase, responsible for the conversion of xanthine and hypoxanthine into 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 of hypoxanthine in particular.
However, at the basis of the pathogenesis of gout, in addition to an increased production of uric acid, fed by diets with a 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 the 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 principle and the biotransformation into metabolites with biological activity such as oxipurinol.

Studies carried out and clinical efficacy

1. POLYMORPHISMS AND ADVERSE REACTIONS TO ALLOPURINOL
Br J Dermatol. 2012 Feb 20.

Association between HLA-B * 58: 01 allele and severe cutaneous adverse reactions with allopurinol in Han Chinese in Hong Kong.

Chiu LS, Hu M, Ng MH, Yeung CK, Chan JC, Chang MM, Cheng SH, Li L, Tomlinson B.


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: 265-71.

Allopurinol as a cardiovascular drug.

Kelkar A, Kuo A, Frishman WH.


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 ischemic cardiomyopathy and congestive heart failure.


3.L "ALLOPURINOL: FIRST-LINE DRUG IN THE TREATMENT OF GOT
Clin Pharmacol Ther. 2011 Sep; 90: 363-4.

Improving the use of allopurinol in chronic gout: monitoring oxypurinol levels to guide therapy.

Keith MP, Gilliland WR.


Study that reaffirms the importance of allopurinol in the treatment of chronic gout.
In fact, despite the marketing of new active ingredients useful in the treatment of gout and uratic lithiasis, allopurinol remains the most effective drug and for this reason to be considered as a first-line strategy in urato-therapy.

Method of use and dosage

ZYLORIC ®
Tablets of 100 mg or 300 mg of allopurinol;
Allopurinol 300 mg dispersible granules.
Treatment with allopurinol should be defined by your physician based on the blood uric acid level, the state of renal function and the severity of the clinical picture.
Generally, the dosage schedule provides for the initiation of therapy at low doses (100 mg per day) to be adjusted, if necessary, until the uricemia is normalized; in this regard, 300 mg per day of uric acid are generally sufficient to rebalance the blood concentrations of this element.
However, the doctor could reserve treatments at even higher doses in patients characterized by severe imbalances.
It is recommended to take ZYLORIC ® at the same time every day, preferably after meals.

Warnings ZYLORIC ® Allopurinol

All treatment with allopurinol should be supervised by your doctor, in order to avoid the occurrence of even serious adverse reactions and at the same time ensure 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 onset of acute joint gouty attacks following the immediate intake of allopurinol, it would be indicated to administer prophylactically, non-steroidal anti-inflammatory drugs or colchicine in the initial stages of treatment.
It is also advisable to increase the daily water intake, in order to facilitate both the urinary excretion of uric acid and that of the allopurinol catabolites.
Taking ZYLORIC ® may occasionally cause drowsiness, therefore the patient should evaluate their cognitive abilities before driving a car.
The presence of lactose in ZYLORIC ® could be problematic for patients suffering from glucose-galactose malabsorption, lactose intolerance or enzyme deficiency of lactase.


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 infant, lead experts to advise against the use of ZYLORIC ® during pregnancy and in the subsequent lactation period. breasts, unless strictly necessary.

Interactions

Different pharmacokinetic studies have demonstrated 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 with renal insufficiency;
  • Antibiotics such as amoxicillin and ampicillin, for which an increased risk of developing skin rash has been observed;
  • Oral anticoagulants, dangerous for 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 azathiopirine and mercaptopurine;
  • Uricosurics, capable of increasing the renal clearance of allopurinol and oxipurinol, reducing their therapeutic effect.

Contraindications ZYLORIC ® Allopurinol

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

Undesirable Effects - Side Effects

Although treatment with ZYLORIC ® is well tolerated in most patients and at most accompanied by clinically insignificant side effects, in rare cases, mainly concentrated among patients with renal and hepatic insufficiency, hypersensitivity reactions have been observed. with skin rash, fever, skin exfoliation and vasculitis, gastrointestinal disturbances, asthenia, malaise, dizziness, somnolence, visual and taste disturbances, hypertension, alopecia, hepatotoxicity, paraesthesia and neuropathies, gynecomastia and haematological disorders.
In all these cases it is of fundamental importance to consult your doctor immediately and, if necessary, to opt for the suspension of the treatment.

Note

ZYLORIC ® can only be sold with a medical prescription.


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