ZAROXOLYN ® is a metolazone-based drug
THERAPEUTIC GROUP: Diuretics / Diuretics with minor diuretic action, thiazides-like.
Indications ZAROXOLYN ® Metolazone
ZAROXOLYN ® is indicated in the treatment of all those oedematous conditions characterized by greater hydro-saline retention and in medium-low grade hypertension. In the more severe forms, however, 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 taken, is mainly concentrated in the kidney, where it can carry out its biological action within one "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 loop of Henle of the nephron, reducing the reabsorption of sodium and promoting its excretion and the consequent diuretic effect.The antihypertensive action directed against the smooth arterial muscle cells is observed approximately after 1-2 weeks of treatment, when given the low levels of sodium, there is an increase in sodium / calcium exchanges, which guarantee greater reabsorption of sodium and a greater excretion of calcium, which reduces the contractile properties of the vascular media.
At the end of the therapeutic action, about 80% of metolazone is excreted in the urine, while the remainder is removed via the bile.
Studies carried out and clinical efficacy
1. METOLAZONE IN THE "HEART INSUFFICIENCY
Cardiovasc Drugs Ther. 2005 Aug; 19: 301-6.
Combination therapy with metolazone and loop diuretics in outpatients with refractory heart failure: an observational study and review of the literature.
Rosenberg J, Gustafsson F, Galatius S, Hildebrandt PR.
Although the literature proposes studies with a very low number of enrolled patients (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 DILATIVE CARDIOMYOPATHY
Med Klin (Munich). 1991 Jun 15; 86: 305-8, 332.
[Metolazone in the treatment of advanced therapy-resistant dilated cardiomyopathy]
Kröger N, Szuba J, Frenzel H.
This study, conducted by the German school of cardiology, demonstrates 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 day) ensured an important resumption of diuresis and a significant weight loss.
Adding this drug to standard therapy could result in a lowering of the furosemide dose used and thus reduce the incidence of hypokalaemia.
3. METOLAZONE IN THE TREATMENT OF HYPERTENSION
Clin Ther. 1986; 9: 47-62.
Clinical studies of a new, low-dose formulation of metolazone for the treatment of hypertension.
Curry CL, Janda SM, Harris R, MacKay JH, Nugent CA, Ryan J, Schnaper H, Schoenberger J.
The study, dated 1986, is one of the first to show the clinical efficacy of metolazone in the treatment of hypertension of medium severity. In fact, the results obtained on 105 patients showed how this active principle, already at doses of 0.5 mg, could guarantee a drop in blood pressure of about 10mmHg, in the absence of side effects worthy of clinical note.
Method of use and dosage
ZAROXOLYN ® tablets of 5/10 mg of metolazone
- For the treatment of hypertensive states, dosages between 2.5 and 5 mg (half tablet - 1 tablet) in the morning, prolonged for 3/4 weeks are suggested.
- For the treatment of oedematous conditions due to heart failure, doses between 2.5 and 5 mg per day, taken in the morning, are suggested.
- For the treatment of edema due to renal insufficiency, doses ranging from 5 to 20 mg per day can be used.
Given the prolonged action time, once the therapeutic objective has been reached, it would be useful to set a maintenance dose, lowering the dosage compared 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 for the other diuretics treated, before starting the intake of ZAROXOLYN ® during the whole therapeutic process, it would be necessary to constantly monitor some blood parameters, such as sodium, potassium, azotemia, uricemia and glycemia, especially in diabetic patients or patients undergoing therapy. hypoglycemic. In case of alteration of one of these parameters, it would be necessary to review the therapeutic plan, and bring the aforementioned values back to normal before continuing with the drug intake.
Given the hypokalaemic effect of ZAROXOLYN ® it would be recommended to take foods rich in potassium or specific supplements at the same time as pharmacological therapy.
Given its ability to aggravate hyperuricaemia, it should be administered with caution in gout patients. Although there are no known direct effects of ZAROXOLYN ® in altering normal driving and use of machinery, it is necessary to consider that incorrect dosages or effects unexpected collateral could significantly reduce the normal perceptive and reactive abilities of the patient undergoing therapy.
PREGNANCY AND BREASTFEEDING
Although studies conducted on animals have avoided 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 unchanged in breast milk.
In light of these data, we strongly advise against the use of ZAROXOLYN ® during the whole pregnancy period, while it is suggested to stop 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;
- Ciclosporin, resulting in an increase in serum creatinine;
- Digitalis, increasing the incidence of arrhythmias and heartbeat disturbances associated with hypokalaemia;
- Corticosteroids, and related risk of hypokalaemia;
- Lithium and curaries, enhancing their 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 hepatic anuria, coma and pre-coma.
Its use is not recommended even in children.
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 in 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. these reactions are added to others of haematological interest, determined by the phenomenon of haemoconcentration, such as an increase in blood sugar, 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 urticaria, rashes and angiopathies.
In the aforementioned cases, it is necessary to consult your doctor and, if necessary, discontinue therapy with ZAROXOLYN ®
Note
ZAROXOLYN ® can only be sold under medical prescription.
The use of ZAROXOLYN ® should always be done after consulting your doctor.
The indiscriminate use of ZAROXOLYN ® among athletes and non-athletes, to search for the loss of a few kilos, 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 slimming effect, intended as a loss of fat mass.
Therefore ZAROXOLYN ® is classified among the DOPING substances.
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