MODURETIC ® is a drug based on amiloride hydrochloride + hydrochlorothiazide
THERAPEUTIC GROUP: diuretics / thiazide diuretics in association with potassium sparing agents
IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects
Indications MODURETIC ® Amiloride + hydrochlorothiazide
MODURETIC ® is used in the treatment of oedematous situations due to cardiac and hepatic diseases.
MODURETIC ® is also used successfully in antihypertensive therapy.
Mode of action MODURETIC ® Amiloride + hydrochlorothiazide
MODURETIC ® taken orally, has a good absorption profile, with a maximum plasma peak of both active ingredients (amiloride and hydrochlorothiazide) between the fourth and sixth hours. The beginning of the diuretic action is already observed around the second hour, when the biological effect of the two active ingredients begins to be fulfilled. The first, belonging to the category of thiazide diuretics, guarantees an inhibition of the sodium / chlorine transporter on the apical surface of the cells of the distal convoluted tubule of the nephron, increasing the urinary excretion of water, sodium and chlorine (and subsequently also of potassium and magnesium ), with an important diuretic effect.
Amiloride, on the other hand, is able to inhibit the dependent sodium / potassium ATP transporter expressed on the surface of the cells of the distal tubule, while ensuring a reduction in sodium reabsorption and an inhibition of active potassium excretion.
This combination is very important, not only to enhance the modest diuretic effects of amiloride, but above all to combine the marked saluretic and diuretic action of hydrochlorothiazide, a saving action on the excretion of potassium. It is in fact known that most of the side effects related to the use of diuretics are related to the symptoms associated with hypokalemia, which is significantly reduced thanks to the simultaneous presence of amiloride.
The effect of the drug is prolonged on average between 9 and 12 hours, following which begins the unchanged urinary excretion of both the active principles of MODURETIC ®
Studies carried out and clinical efficacy
1 HYDROCHLOROTHYZIDE / AMYLORIDE IN PRESSURE CONTROL
The concomitant administration of amiloride and hydrochlorothiazide was tested in 82 patients suffering from hypertension, with blood pressure above 140/90 mmHg. The data reported in this study show that the addition between 2.5 and 5 mg / day of amiloride to 25 mg of hydrochlorothiazide, guaranteed a further drop in blood pressure values of about 2 mmHg. Despite the positivity of this combination, the combination of hydrochlorothiazide with enalapril seems to be even more effective.
2. AMYLORIDE / HYDROCHLOROTHYZIDE AND FIBRINOLYSIS.
This study conducted on 28 hypertensive patients, shows how therapy with hydrochlorothiazide at 50 mg + 5 mg amiloride, although it can guarantee a significant decrease in blood pressure, does not guarantee the reduction of fibrinolytic effects (potentially dangerous for the hypertensive patient), such as observed instead in the combination hydrochlorothiazide - spironolactone.
3. AMYLORIDE / HYDROCHLOROTHYZIDE AND DOPING
Study dated 1975, which shows how the administration of amiloride and hydrochlorothiazide at high doses (15 mg - 150 mg / day), therefore potentially dangerous, in 10 normal subjects, guaranteed a reduction in body weight of about 1.9 kg, preserving the levels muscle intracellular calcium and magnesium, and resulting in an increase in blood pH. Despite this effect, it is necessary to remember that the use, indeed the abuse of the drug in normal subjects, is potentially dangerous, especially when used at high doses, as well as illegal.
Method of use and dosage
MODURETIC ® 5mg tablets of amiloride + 50mg of hydrochlorothiazide: it is generally recommended to take one or 2 tablets a day, taking into account that the maximum permitted dose should never exceed 4 tablets per day. It should be remembered that taking MODURETIC ® must be under strict medical supervision, and that the dosage may undergo variations based on the patient's physiopathological conditions and the severity of the pathology.
Furthermore, in the case of prolonged therapies, it is recommended to use lower maintenance dosages, which still allow for adequate diuresis.
IN ANY CASE, BEFORE TAKING MODURETIC ® Amiloride + hydrochlorothiazide - THE REQUIREMENT AND CHECK OF YOUR DOCTOR IS NECESSARY.
Warnings MODURETIC ® Amiloride + hydrochlorothiazide
Plasma levels of electrolytes should be carefully evaluated before the administration of MODURETIC ® in order to avoid potentially dangerous water-saline decompensations for the patient's health. These controls must be even more stringent in subjects with a manifest risk of alteration of the electrolyte balance, suffering from cirrhosis, cardiopulmonary diseases, old age or hospitalized patients. In this case, frequent checks are not only useful to detect hyponatremia episodes, but also to avoid the possibility of hyperkalaemia, particularly evident in diabetic patients.
The use of thiazide diuretics exposes the diabetic patient to potential hyperglycaemia, for which an adjustment of hypoglycemic therapy may be necessary, while in hyperuremic patients gouty episodes may become more frequent.
MODURETIC ® could cause an increase in plasma calcium levels, altering the results of any tests on parathyroid function.
Although there are no known direct effects of the drug in altering the normal driving skills and use of machinery, it should be considered that electrolyte imbalances, potentially verifiable in the case of taking MODURETIC ®, could cause a decrease in the patient's normal perceptive and reactive capacities .
PREGNANCY AND BREASTFEEDING
The use of MODURETIC ® during the entire pregnancy is not recommended. In fact it is known that amiloride can easily cross the placental barrier and reach the fetal blood, with consequent fetal jaundice or side effects typical of diuretics. Furthermore, the hemodynamic action of diuretics on maternal blood could result in impairment of the normal haemrophic supply of organs important for fetal development, compromising growth.
Since both the active ingredients of MODURETIC ® have been found intact in breast milk, it is advisable to stop breast-feeding during drug therapy.
Interactions
The simultaneous administration of other diuretics and antihypertensives could increase the hypotensive effect of MODURETIC ® with the consequent appearance of the related side effects.
Furthermore, the effects of MODURETIC ® could be exacerbated by the concomitant administration of alcohol, barbiturates and narcotics of various kinds.
The toxicity of lithium and the biological action of curare derivatives may increase if administered concomitantly with hydrochlorothiazide and amiloride, while the risk of an electrolyte alteration in the case of concomitant intake of corticosteroids and ACTH may increase.
Contraindications MODURETIC ® Amiloride + hydrochlorothiazide
MODURETIC ® should not be taken in case of hyperkalemia or concomitant administration of other potassium-sparing diuretics, in case of reduced or impaired hepatic and renal function with anuria, in diabetic patients with relative nephropathy, hyperuremic or with elevated plasma levels of nitrogen and creatinine .
Naturally the drug is strictly not recommended in case of hypersensitivity to one of its components.
Undesirable effects - Side effects
The synergy between amiloride and hydrochlorothiazide, present in MODURETIC ® seems to be well tolerated by patients undergoing drug therapy, with the absence of clinically relevant side effects and mostly characterized by gastro-intestinal effects such as thirst, nausea, vomiting, lack of appetite, accompanied in the most serious cases by dizziness, drowsiness, nervousness, general malaise.
In patients suffering from hyperuricemia it is possible to find an increase in gouty episodes, probably due to the phenomenon of haemoconcentration which is accompanied by therapy with MODURETIC ®, whereas in diabetic patients the episodes of hyperglycemia for which a therapy adjustment is often used are quite frequent hypoglycemic.
Of course, to the side effects typical of the drug are added all those due to hypersensitivity to one of its components, which include dermatological phenomena such as skin rashes and hives, systemic and respiratory.
Note
MODURETIC ® is salable only under medical prescription.
The use of MODURETIC ® should always take place after consulting your doctor.
The indiscriminate use of MODURETIC ® 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 it is classified as a DOUBLE substance.
