ALDOMET ® Metildopa

ALDOMET ® is a drug based on methyldopa

THERAPEUTIC GROUP: Antihypertensives - antiadrenergic substances with central action

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

Indications ALDOMET ® Metildopa

ALDOMET ® is indicated in the treatment of all forms of moderate or severe arterial hypertension.

Mechanism of action ALDOMET ® Metildopa

ALDOMET ® taken orally, has an unpredictable pharmacokinetics, as its absorption and its bioavailability tend to vary significantly from individual to individual, reaching between 8 and 62%. Its biological action tends to persist for about 24 hours, while elimination is mainly entrusted to the renal route.

The antihypertensive effect is due to the active ingredient contained in ALDOMET ® known as methyldopa, which is able - through different mechanisms - to reduce the sympathetic functionality of the organism. The modalities of action of this active principle foresee an inhibition of the receptors of the vasomotor centers of the central nervous system (effect probably exercised by the alpha-methyl noradrenaline metabolite) and a peripheral antiadrenergic effect impeding the activity of L-dopa-decarboxylase ( which catalyzes the transformation of L-dopa into dopamine, a catecholamine that acts on the sympathetic nervous system causing the acceleration of the heartbeat and the raising of blood pressure).

Studies carried out and clinical efficacy

1 METILDOPA AND HYPERTENSION

Metildopa was - between the 70s and 80s - one of the most used drugs in the treatment of primary hypertension. Its use was then gradually replaced by more effective pharmaceutical classes with fewer side effects. However, this study conducted in meta-analysis on approximately 595 studies has shown the efficacy of methyldopa at doses of 500mg / 2000mg per day in reducing blood pressure. More precisely, the average reduction reached 13mmHg for the maximum and 8mmHg for the minimum.

2. METILDOPA AND HEPATOTOSSICITY IN PREGNANCY

It is known as one of the side effects associated with methyldopa therapy, both liver toxicity. Unfortunately, the literature is rich in cases like these, in which the administration of methyldopa has led to an important reduction in liver function, with alteration of laboratory parameters even in pregnant women. Fortunately, hepatic values and function returned to normal range following discontinuation of therapy.

3. METILDOPA AND ANEMINA

Hemolytic anemia is one of the most risky side effects of methyldopa administration. Although the pathogenic mechanism of this adverse reaction has not yet been elucidated, international literature includes new cases of haemolytic anemia, some of which are very serious.

Method of use and dosage

ALDOMET ® methyldopa 250/500 mg tablets: the attack dose for the treatment of hypertension involves the administration of 2/3 tablets per day of 250 mg in the first 48 hours. Once the effect has been observed, which generally occurs within 12/24 hours after oral administration, it would be necessary to adjust the dose according to the objectives and the first results obtained.

The maximum permitted dose of ALDOMET ® should never exceed 2 grams per day; if this dosage proves to be ineffective, one could resort to the simultaneous administration of thiazide diuretics, which seem particularly effective in assisting the antihypertensive action of methyldopa. In this case - and possibly in other cases of simultaneous administration of antihypertensive drugs - the doctor should adjust the dose of both in order to obtain a good blood pressure control.

IN ANY CASE, BEFORE TAKING ALDOMET ® Metildopa - THE PRESCRIPTION AND CONTROL OF YOUR OWN DOCTOR IS NECESSARY.

Warnings ALDOMET ® Metildopa

The intake of ALDOMET ®, especially in the case of high doses, could be associated with drowsiness and sedation, with a significant increase in these effects in elderly patients or those with renal diseases, given the different metabolism and the reduced excretion of the active ingredient.

During ALDOMET ® therapy, cases of haemolytic anemia of different severity, alteration of hematocrit and laboratory parameters, reduction of liver function and fever were also observed, for which it was necessary to suspend drug therapy. Consequently, in the first weeks of treatment a strict medical monitoring would be necessary, in order to avoid the possible onset of the aforementioned effects dangerous for the patient's health.

ALDOMET ® could also alter the Coombs test.

Generally, the suspension of drug therapy, given also the short half-life of the active principle, determines a return to the pre-therapy pressure levels in 24 hours, without any rebound effect.

Somnolence and decreased attention may occur following the administration of ALDOMET ®, making the driving of vehicles or the use of machinery dangerous.

PREGNANCY AND BREASTFEEDING

The various studies published in the literature seem to agree on the absence of teratogenic effects of ALDOMET ®, however the role of methyldopa on fetal metabolism has not yet been fully clarified. It is in fact known that this active ingredient and its metabolites can easily pass the placental barrier and exercise its biological action also on the fetus. Furthermore, methyldopa is to a small extent secreted into breast milk, therefore it is advisable to stop breast-feeding during ALDOMET ® therapy

Interactions

It is possible to enhance the hypotensive therapeutic action of ALDOMET ® through the concomitant administration of other antihypertensive drugs. The synergy with thiazide diuretics seems particularly effective, in which case a correct dosage adjustment is necessary in order to avoid acute hypotensive episodes.

The partial sedating effect of methyldopa could result in a reduced need for anesthetics in the perioperative phase.

The biological efficacy of ALDOMET ® is instead inhibited by the administration of drugs such as tricyclic antidepressants or non-steroidal anti-inflammatory drugs, capable of determining an increase in water-saline retention.

Contraindications ALDOMET ® Metildopa

Given the potential metabolic effects of methyldopa, the administration of ALDOMET ® is not recommended in patients with hepatic and renal diseases, even previous ones, and in case of hypersensitivity to one of the constituents of the drug.

ALDOMET ® is not effective in the treatment of hypertension in patients with pheochromocytoma.

Undesirable effects - Side effects

The administration of ALDOMET ® especially in the initial phase or following an increase in the dose, could be accompanied by a sedative effect, drowsiness, dizziness, weakness, headache, nausea and abdominal cramps.

Cases in which the intake of ALDOMET ® has led to the onset of haemolytic anemia, alteration of laboratory parameters, including hematocrit, fever, impotence, decreased libido, amenorrhea, gynecomastia and in the most serious cases are also known. also bradycardia.

These effects are generally mild and transient, in fact they tend to rapidly regress once therapy is suspended.

In case of hypersensitivity to one of the components of ALDOMET ®, skin reactions such as rush, eczema and eruptions are generally observed.