MICARDIS ® Telmisartan

MICARDIS ® is a drug based on telmisartan.

THERAPEUTIC GROUP: Antihypertensives - angiotensin II antagonists

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

Indications MICARDIS ® Telmisartan

MICARDIS ® is indicated for the treatment of essential hypertension in adults.

Treatment with MICARDIS ® is also used in the prevention of cardiovascular danger in patients suffering from cardiovascular, atherothrombotic and type II diabetes mellitus diseases.

Mechanism of action MICARDIS ® Telmisartan

Telmisartan, the active ingredient of MICARDIS ®, is absorbed at the level of the gastro-enteric tract with a fairly rapid timing, guaranteeing an absolute bioavailability of 50% compared to the dose taken. Linked to plasma proteins, largely albumin and alpha-1 acid glycoprotein, it reaches the angiotensin II receptor, AT1, expressed in various tissues. By inhibiting the receptor-substrate bond, temisartan reduces the events mediated by this interaction, hindering the vasoconstriction of the smooth muscle, the production of aldosterone and the alteration of the hydro-saline balance (all biological actions involved in the genesis and maintenance of the hypertension).

The antihypertensive action, which generally appears 3 hours after intake and continues throughout the therapy, is not accompanied by potentially dangerous reflex mechanisms, such as an increase in heart rate. These characteristics make this drug a valid protective and preventive against vascular accidents.

After its prolonged action, thanks to a half-life - even more than 20 hours - the telmisartan is partly metabolised in the liver, and eliminated mainly through the faeces.

Studies carried out and clinical efficacy

1 THE LONG-TERM EFFECTS OF TELMISARTAN

The effects of prolonged administration of telmisartan have been evaluated in patients with hypertension. This study has shown that prolonged administration for 12 months at doses between 20 and 60 mg / day, can determine not only a significant drop in blood pressure (from 162/98 to 128/80), but also a significant drop in blood levels of triglycerides. During this period, no clinically relevant side effects were observed.

2. EFFECTIVENESS OF TELMISARTAN IN HYPERTENSION.

This study, conducted on patients suffering from essential hypertension, demonstrates how the administration of 40 mg daily of telmisartan for 12 weeks ensured a significant reduction in blood pressure levels of around 24 mmHg for systolic blood pressure and 14 for diastolic blood pressure. This decrease was greater than that induced by other antihypertensives, such as enalapril, maintaining the same incidence of side effects.

3. TELMISARTAN AND FUTURE PERSPECTIVES

Several studies are focusing on the systemic effects of telmisartan, removing this active ingredient from the sole application in the cardiovascular and hypertensive fields. This study, for example, shows how telmisartan - even if only on experimental models - can guarantee a significant reduction of visceral adipose tissue and prevent adipogenesis, acting on very important cellular mechanisms.

Method of use and dosage

MICARDIS ® Tablets 40 mg of Telmisartan: the dosage generally used most in the treatment of high blood pressure is about 40 mg / day, although sometimes the dose of 20 mg already seems to be quite effective. In case of refractoriness to the normal dosage, it is possible to increase the dose up to a maximum value of 80 mg / day, or to foresee the association with other antihypertensive drugs with an inevitable adjustment of the dosage.

The dosage of 80 mg / day, with close monitoring of blood pressure, can also be used in the prevention of cardiovascular events.

A correction of the treatment plan must be made by the doctor, after a careful evaluation of the patient's physiopathological situation, in the presence of pathologies that could alter the normal pharmacokinetic characteristics of telmisartan.

Warnings MICARDIS ® Telmisartan

Given the hepatic and biliary metabolism of telmisartan, MICARDIS ® should be administered with particular care in patients suffering from mild and moderate hepatic insufficiency, while it is contraindicated in cases of severe hepatic insufficiency or severe renal disorders because it could unexpectedly increase its hypotensive effect.

Hyperkalemia, hypovolemia and hypotensive crises could occur following the concomitant administration of diuretics or drugs acting on the renin-angiotensin system.

Studies show that low levels of renin, typical of black men, can lead to a reduction in the efficacy of the drug, thus hypothesizing a variability of the ethnic-specific drug.

Like other antihypertensive drugs, the possible incidence of hypotensive episodes, drowsiness and dizziness, suggests avoiding the use of MICARDIS ® before driving vehicles or using dangerous machinery.

PREGNANCY AND BREASTFEEDING

The use of MICARDIS ® is strictly contraindicated in pregnancy, given studies conducted in animals showing the teratogenic effects of angiotensin II antagonists. Furthermore, the alteration of fetal blood perfusion could compromise the normal development of the fetus. Therefore, it would be advisable to opt for an alternative antihypertensive therapy, with a greater safety profile for use in pregnancy.

We do not recommend the use of this drug even during breastfeeding, given the absence of safe data concerning the safety of MICARDIS ® in similar circumstances.

Interactions

MICARDIS ® can interact with numerous other compounds, with consequent alteration of the pharmacokinetic and pharmacodynamic properties of its active principle.

The concurrent administration of:

potassium-sparing diuretics, potassium supplements or drugs affecting this element, could increase the risk of hyperkalemia, thus suggesting a constant monitoring of serum mineral levels;
non-steroidal anti-inflammatory drugs and corticosteroids can reduce the hypotensive effects of the drug;
antihypertensives could lead to an increase in the hypotensive effect;
lithium, could cause an increase in the toxicity of this element.

Contraindications MICARDIS ® Telmisartan

MICARDIS ® is contraindicated in case of hypersensitivity to one of its components and metabolites, in case of obstruction of the biliary tract and severe hepatic insufficiency.

Undesirable effects - Side effects

The side effects associated with the administration of MICARDIS ®, although rare, involve various systems and generally result in diarrhea, nausea, depression and insomnia, dizziness, bradycardia, dyspnea, loss of appetite and myalgia, asthenia, hyperkalemia and increased creatinine levels.

Generally these effects do not seem to be dose related, let alone sex or ethnicity related.