ALDOMET ® is a methyldopa-based drug
THERAPEUTIC GROUP: Antihypertensives - antiadrenergic substances with central action
Indications ALDOMET ® Methyldopa
ALDOMET ® is indicated in the treatment of all forms of moderate or severe arterial hypertension.
Mechanism of action ALDOMET ® Methyldopa
ALDOMET ® taken orally, has unpredictable pharmacokinetics, as its absorption and relative bioavailability tend to vary significantly from individual to individual, settling between 8 and 62%. Its biological action tends to persist for about 24 hours, while the elimination is mainly entrusted to the renal route.
The antihypertensive effect is due to the active principle contained in ALDOMET ® known as methyldopa, which is able - through various mechanisms - to reduce the sympathetic functionality of the organism. The modalities of action of this active principle include an inhibition of the receptors of the vasomotor centers of the central nervous system (effect probably exerted by the metabolite alpha-methyl Noradrenaline) and a peripheral antiadrenergic effect of 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 heartbeat to accelerate and blood pressure to rise).
Studies carried out and clinical efficacy
1. METHYLDOPA AND HYPERTENSION
Cochrane Database Syst Rev. 2009 Oct 7;: CD003893.
Methyldopa for primary hypertension.
Mah GT, Tejani AM, Musini VM.
Methyldopa 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 a meta-analysis on about 595 studies it has demonstrated the efficacy of methyldopa at doses of 500mg / 2000mg per day in reducing blood pressure.More precisely, the average reduction stood at values of 13mmHg for the maximum and 8mmHg for the minimum.
2. METHYLDOPA AND HEPATOTOXICITY IN PREGNANCY
J Coll Physicians Surg Pak. 2009 Feb; 19: 125-6.
Alpha-methyldopa hepatotoxicity in pregnancy.
Ali T, Srinivasan N, Le V, Rizvi S.
It is known that one of the side effects associated with methyldopa therapy is hepatic toxicity. Unfortunately, the literature is full of cases like these, in which the administration of methyldopa has determined a "significant reduction in liver function, with alteration of the parameters of laboratory also in pregnant women. Fortunately, liver values and liver function returned to normal after discontinuation of therapy.
3. METHYLDOPA AND ANEMINE
N Z Med J. 2009 Aug 21; 122: 53-6.
Methyldopa-induced autoimmune haemolytic anaemia revisited.
Thomas A, James BR, Graziano SL.
Hemolytic anemia is one of the riskiest side effects associated with the administration of methyldopa. Although the pathogenic mechanism of this adverse reaction has not yet been clarified, the international literature lists new cases of haemolytic anemia every year, some of which are very serious.
Method of use and dosage
ALDOMET ® tablets of 250/500 mg of methyldopa: the attack dose for the treatment of hypertension involves the administration of 2/3 tablets of 250 mg per day in the first 48 hours. Once the effect has been observed, which generally occurs within 12/24 hours of oral administration, it would be necessary to adjust the dose according to the objectives and the first results obtained.
The maximum allowed dose of ALDOMET ® should never exceed 2 grams per day; if this dosage proves 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 good blood pressure control.
IN ANY CASE, BEFORE TAKING ALDOMET ® Methyldopa - YOU NEED THE PRESCRIPTION AND CONTROL OF YOUR DOCTOR.
ALDOMET ® Methyldopa warnings
The intake of ALDOMET ®, especially in the case of high dosages, could be associated with somnolence and sedation, with a significant increase in these effects in elderly patients or patients with kidney problems, given the different metabolism and reduced excretion of the active ingredient.
Cases of haemolytic anemia of varying severity, changes in hematocrit and laboratory parameters, decreased liver function and fever have also been observed during therapy with ALDOMET ®, for which it was necessary to suspend the drug therapy. in the first weeks of treatment, close medical monitoring would be necessary in order to avoid the possible occurrence of the aforementioned dangerous effects on the patient's health.
ALDOMET ® could also determine an "alteration of the Coombs test.
Generally, the suspension of drug therapy, also given the short half-life of the active ingredient, causes a return to pre-therapy blood pressure levels in 24 hours, but without any rebound effect.
Somnolence and decreased attention could occur following the administration of ALDOMET ® making it dangerous to drive or use machines.
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 well known that this active ingredient and its metabolites can easily pass the barrier. placental and exert its biological action also on the fetus. In addition, a small part of methyldopa is secreted in breast milk, therefore it is advisable to stop breastfeeding during therapy with ALDOMET ®.
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 to be 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 lead to 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 causing an increase in hydro-saline retention.
Contraindications ALDOMET ® Methyldopa
Given the potential metabolic effects of methyldopa, the administration of ALDOMET ® is not recommended in patients suffering from liver and kidney 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.
There are also cases in which the intake of ALDOMET ® has determined the onset of haemolytic anemia, alteration of laboratory parameters, including hematocrit, fever, impotence, decreased libido, amenorrhea, gynecomastia and in the most severe cases also bradycardia.
These effects are generally mild and transient, in fact they tend to regress rapidly once therapy is discontinued.
In case of hypersensitivity to one of the components of ALDOMET ®, skin reactions such as rash, eczema and rashes are generally observed.
Note
ALDOMET ® can only be sold under medical prescription.
The information on ALDOMET ® Methyldopa published on this page may be out of date or incomplete. For a correct use of this information, see the Disclaimer and useful information page.
