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ZAROXOLYN ® Metolazone

ZAROXOLYN ® is a drug based on metolazone

THERAPEUTIC GROUP: Diuretics / Diuretics with minor diuretic action, thiazides-like.

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

Directions ZAROXOLYN ® Metolazone

ZAROXOLYN ® is indicated for the treatment of all those oedematous conditions characterized by greater hydro-saline retention and medium-low grade hypertension. In the more severe forms, on the other hand, ZAROXOLYN ® can be combined with other antihypertensive drugs.

Mechanism of action ZAROXOLYN ® Metolazone

ZAROXOLYN ® as a thiazide-like diuretic, is generally taken orally and, once absorbed for about 65% of the total dose, concentrates mainly on the kidney, where it can perform its biological action within an hour of administration. . At this level it is able to inhibit the sodium channels expressed on the apical surface of the cells of the distal tubule and of the ascending tract of the nephron Henle's loop, reducing sodium reabsorption and promoting excretion and the consequent diuretic effect. The antihypertensive action directed towards the arteriolar smooth muscle cells, is observed approximately after 1-2 weeks of treatment, when given the low levels of sodemia there is an increase in the sodium / calcium exchanges, which guarantee a greater reabsorption of sodium and greater excretion of calcium, which reduces the contractile properties of the vascular average layer.

After the therapeutic action, about 80% of the metolazone is excreted in the urine, while the remaining part is removed via the bile.

Studies carried out and clinical efficacy

1 METOLAZONE IN CARDIAC INSUFFICIENCY

Although the literature proposes studies with a very low number of patients enrolled (no more than 250 per study), metolazone is used daily in clinical practice, and often combined with a loop diuretic in the treatment of heart failure. Despite the low sample size, all studies seem to agree on the therapeutic efficacy of metolazone, also used at doses below 5 mg / day, for which many side effects are avoided.

2. METOLAZONE IN THE TREATMENT OF DILATATIVE CARDIOMYOPATHY

This study conducted by the German school of cardiology, shows how in patients suffering from dilated cardiomyopathy, therefore with combined edema and refractory to normal diuretic therapy, the addition of low-dose metolazone (2.5 / 5mg die) ensured an important recovery of diuresis and a significant weight loss.

Adding this drug to standard therapy could lower the dose of furosemide used and thus reduce the incidence of hypokalemia.

3. METOLAZONE IN THE TREATMENT OF HYPERTENSION

The study, dated 1986, is one of the first to show the clinical efficacy of metolazone in the treatment of medium severity hypertension. In fact, the results obtained on 105 patients showed that this active ingredient, even at doses of 0.5 mg, could guarantee a pressure drop of about 10mmHg, in the absence of side effects worthy of clinical note.

Method of use and dosage

ZAROXOLYN ® 5/10 mg metolazone tablets

  1. For the treatment of hypertensive states, dosages of between 2.5 and 5 mg are recommended (half a tablet - 1 tablet) in the morning, prolonged for 3/4 weeks
  2. For the treatment of oedematous conditions due to heart failure, doses of 2.5 to 5 mg per day are suggested, taken in the morning.
  3. For the treatment of edema due to renal failure, doses between 5 and 20 mg a day can be used.

Given the prolonged time of action, once the therapeutic objective is reached, it would be useful to set a maintenance dose, lowering the dosage with respect to the attack action.

The dosages, in any case, must be optimized by the doctor, following a scrupulous evaluation of the physio-pathological state and the severity of the pathology.

Warnings ZAROXOLYN ® Metolazone

As with the other treated diuretics, before taking ZAROXOLYN ® during the whole therapeutic procedure, it would be necessary to constantly monitor some blood parameters, such as sodemia, potassium, azotemia, uricemia and glycaemia, especially in diabetic patients or those undergoing therapy hypoglycemic. In case of alteration of one of these parameters, it would be necessary to review the treatment plan, and report the aforementioned values ​​before continuing with the drug.

Given the hypokalemicizing effect of ZAROXOLYN ® it would be indicated to take potassium-rich foods or specific supplements at the same time as the drug therapy.

Given, on the other hand, the ability to aggravate hyperuricemia, it should be administered cautiously in gouty patients. Although no direct effects of ZAROXOLYN ® are known in altering the normal driving skills and use of machinery, it is necessary to consider that incorrect dosages or unexpected side effects could significantly reduce the normal perceptive and reactive capacities of the patient undergoing therapy.

PREGNANCY AND BREASTFEEDING

Although studies conducted on animals have averted teratogenic effects on the fetus, metolazone, the active ingredient of ZAROXOLYN ® can easily cross the placental barrier, and expose the fetus to the risk of neonatal jaundice, thrombocytopenia and other side effects typical of adults. Furthermore, this active ingredient can be secreted unaltered in breast milk.

In light of these data, the use of ZAROXOLYN ® during the entire period of pregnancy is strongly discouraged, while it is suggested to suspend breastfeeding if taken later.

Interactions

ZAROXOLYN ® may interact with:

  • Loop diuretics, causing an abundant loss of liquids and electrolytes, for which it would be necessary to correct the dosages;
  • Alcohol and barbiturates, with an increased hypotensive effect;
  • Cyclosporine, causing an increase in serum creatinine;
  • Digital, increasing the incidence of arrhythmias and heartbeat disorders associated with hypokalemia;
  • Corticosteroids, and relative risk of hypokalemia;
  • Lithium and curare, enhancing the toxic effect;
  • Anticoagulants, altering their normal biological function;
  • Insulin and oral antidiabetics, with a significant reduction in glucose tolerance.

Contraindications ZAROXOLYN ® Metolazone

ZAROXOLYN ® should not be taken in case of hypersensitivity to the active ingredient of the drug or to one of its compounds, in case of anuria, coma and hepatic pre-coma.

It is not recommended for use in pediatric age.

Undesirable effects - Side effects

The administration of ZAROXOLYN ® could determine the onset of side effects of various kinds, due to the marked biological and metabolic activity of the drug or to hypersensitivity to one of its compounds.

Therefore, among the most common side effects it is possible to find orthostatic hypotension, with difficulty maintaining an upright position, nausea, vomiting, diarrhea, headache, loss of appetite and dry mouth, all symptoms mainly attributable to the diuretic and saluretic action of the drug. To these reactions are added others of hematological interest, determined by the phenomenon of haemoconcentration, such as an increase in glycaemia, azotemia, creatinine, attacks of gout and alteration of the blood count.

In cases of hypersensitivity to the drug, dermatological reactions have been observed, such as hives, exanthema and angiopathies.

In the aforementioned cases, it is necessary to consult your doctor and possibly stop therapy with ZAROXOLYN ®

Note

ZAROXOLYN ® is salable only under medical prescription.

ZAROXOLYN ® should always be used after consulting your doctor.

The indiscriminate use of ZAROXOLYN ® between athletes and non-athletes, in the search for the loss of a few pounds, exposes the body to serious side effects. Furthermore, it is always advisable to reiterate that weight loss is dictated by the elimination of liquids and salts and not by a real weight loss effect, understood as a loss of fat mass.

Therefore ZAROXOLYN ® is classified as a DOPANTI substance.

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