TAPAZOLE ® Tiamazolo

TAPAZOLE ® a drug based on Tiamazole

THERAPEUTIC GROUP: Antithyroid

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

Indications TAPAZOLE ® Tiamazolo

TAPAZOLE ® is used in the treatment of hyperthyroidism and in the pharmacological preparation of thyroidectomy.

Treatment with TAPAZOLE ® is also indicated when thyroidectomy is not recommended or inapplicable.

Mechanism of action TAPAZOLE ® Tiamazole

The therapeutic action of tiamazole (also known as methimazole) contained in TAPAZOLE ® allows to restore a good hormonal profile in the hyperthyroid patient, acting selectively on the thyroid level and inhibiting the transformation of inorganic iodine into organic iodine by the enzyme thyroperoxidase.

The absence of the organic substrate therefore prevents the thyrocyte from providing for the incorporation of iodine ions in the thyroglobulin molecule, and for the consequent synthesis of thyroid hormones, without interfering with the biological properties of the already synthesized hormones.

The therapeutic efficacy of TAPAZOLE ® is realized only after 30 minutes from oral intake and persists for about 6- 13 hours after which it is mainly excreted via the kidneys.

Recent studies seem to support the ability of thiamazole in reducing the synthesis of antireceptor TSH and antimicrosomal antibodies, partly involved in the genesis of hyperthyroid pathology.

Studies carried out and clinical efficacy

1. TREATMENT WITH METHYMOZOL AND BONE HEALTH

The reduced bone density observed in hyperthyroid patients was readily reversible following methimazole therapy capable of restoring the correct hormonal balance. This study demonstrates how improving thyroid health may be important in maintaining general health.

2. METIMAZOLE: NOT ONLY AN ANTITHROIDOUS DRUG

Methimazole is historically used for the treatment of Graves' disease and other hyperthyroid diseases. Recent studies like this show how this active ingredient can also present immunosuppressive and immunomodulatory effects, improving the symptoms and clinical evolution of allergic rhinitis.

3. ANTI-THYROID AND AGRANULOCYTOSIS THERAPY

Agranulocytosis is a particularly dangerous disease, characterized by the development of numerous infectious and sometimes lethal diseases. One of the most important side effects associated with methimazole therapy is precisely this condition, whose timely recognition can be important in safeguarding the health of the patient.

Method of use and dosage

TAPAZOLE ® methimazole 5 mg tablets:

the therapeutic range is very wide and ranges from 15 mg to 60 mg daily in severe hyperthyroidism.

Note the half-life of methimazole, equal to about 8 hours, the daily dosage should be divided into 3 administrations, one every 8 hours.

The effective dose must in any case be formulated by your doctor, after a careful evaluation of the physio-pathological and clinical situation of the patient.

Warnings TAPAZOLE ® Tiamazolo

Treatment with TAPAZOLE ® must be preceded and accompanied by continuous monitoring of the hematological and liver function.

At the first signs of alteration of cellularity, with particular reference to agranulocytosis and hypoprothrombinemia, therapy with TAPAZOLE ® should be suspended.

The dosage of TSH and thyroid hormones should be requested as a system to evaluate the efficacy of the therapy and the dosage adjustment.

TAPAZOLE ® tablets contain lactose therefore the administration of this medicine in patients intolerant to glucose / galactose or lactase-deficient enzymes could be associated with the appearance of serious side effects.

Dizziness, drowsiness and other nerve manifestations associated with thiamazole therapy could make the use of machinery and driving vehicles dangerous.

PREGNANCY AND BREASTFEEDING

Treatment of gravidic hyperthyroidism with TAPAZOLE ® due to the ability of its active ingredient to rapidly cross the hematoplacental barrier, can expose the fetus to serious consequences with increased risk of malformations, thyroid goiter and cretinism.

For this reason it is preferred to treat these patients with propylthiouracil (currently not marketed in Italy), which appears to have a higher safety profile than thiamazole.

Interactions

Thiamazole can also cause significant changes in the therapeutic efficacy of various active ingredients. From the pharmacokinetic point of view the most relevant are those with:

Oral anticoagulants, with an enhancement of the biological properties of vitamin K antagonists;
Beta blockers, digitalis glycosidics and theophylline with reduced clearance of the aforementioned products.

It is important to specify how these variations are to be attributed mainly to the effects induced by the restoration of the euthyroid condition and not strictly to the active principle.

Contraindications TAPAZOLE ® Tiamazole

TAPAZOLE ® contraindicated in case of hypersensitivity to the active ingredient or to one of its excipients and during the lactation period.

Undesirable effects - Side effects

Different clinical trials and careful post-marketing monitoring have shown that the administration of tiamazole may be associated with clinically insignificant adverse reactions such as skin rash, hives, nausea, joint pain, hair loss, myalgia, jaundice, edema, headache, vertigo and drowsiness.

Clinically more important side effects, such as haematological changes, autoimmune and nephritis pathologies have been observed only in rare cases