OLMETEC ® Olmesartan medoxomil

OLMETEC ® is a drug based on Olmesartan medoxomil

THERAPEUTIC GROUP: Antihypertensives - angiotensin II antagonists

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

Indications OLMETEC ® Olmesartan medoxomil

OLMETEC ® is indicated in the treatment of essential arterial hypertension, in monotherapy or associated with other antihypertensive drugs in case of low responsiveness.

Mechanism of action OLMETEC ® Olmesartan medoxomil

Olmesartan medoxomil, the active ingredient of OLMETEC ® is a pro-drug to be administered orally. Arrived at the intestinal level, it is largely hydrolyzed in its active form, olmesartan, and absorbed reaching maximum plasma concentrations about two hours after intake. At the plasma level it is possible to observe a quantity equal to approximately 25.6% of the dose taken, which shows a relatively low bioavailability. Like the other active ingredients of the same pharmaceutical category, olmesartan acts by antagonizing the biological effect of angiotensin II, through a stable and high-affinity bond with its AT1 receptor. This mechanism results in an increase in the plasma levels of angiontesin I and II, in a decrease in serum aldosterone levels and in a vasodilatory action, which guarantees a drop in blood pressure within 24 hours of its assumption, which stabilizes - optimizing around - the second week of therapy.

After its action, generally after about 15 hours, olmesartan is eliminated intact mainly through the feces and in small part with the urine.

Studies carried out and clinical efficacy

1 OLMESARTAN MEDOXOMIL ON CARDIOVASCULAR HEALTH

It is known that angiotensin II produces - in pathological conditions - an hyperactivation of AT1 receptors, giving rise to a series of events that result in both an increase in arterial pressure, but also in an important pro-inflammatory vascular damage, which exposes the patient at risk of cardiovascular accidents. Olmesartan medoxomil, in addition to being well tolerated and effective in inducing blood pressure reduction, has also proved useful in protecting vessels from inflammatory insult, reducing the diameter of atherosclerotic plaques and increasing the number of endothelial cell progenitors, probably through mechanisms not directly correlated with pressure reduction.

2. SECURITY OF THE OLMESARTAN MEDOXOMIL IN HYPERTESE PATIENTS

J Hypertens. 2010 Nov; 28 (11): 2342-50.

The main application of olmesartan medoxomil remains severe hypertension. Most therapeutic strategies involve combining this active ingredient with other antihypertensive drugs, which act on other metabolic pathways. The study in question not only evaluates the efficacy of the therapy in reducing blood pressure in hypertensive patients, but also their compliance and the safety of treatment. In addition to an average reduction in systolic blood pressure of about 17mmHg and diastolic pressure of 10mmHg, the results show an excellent tolerability of the drug, with very rare and clinically insignificant side effects.

3. THE EFFECTIVENESS OF OLMESARTAN MEDOXOMIL IN COMBINATION IN THE TREATMENT OF HYPERTENSION

The study in question represents only one example of the many studies present in the literature that show the efficacy of the combination olmesartan medoxomil and other antihypertensive drugs, in improving the pressure levels of patients suffering from hypertension. For example, in this study conducted on approximately 1017 patients - with systolic and diastolic arterial pressure averaging more than 140/90 mmHg - the combined eight-week combination therapy with olmesartan medoxomil / amlodipine guaranteed an average reduction of about 17mmHg for systolic and 10 for diastolic.

Method of use and dosage

OLMETEC ® 10/20/40 mg tablets of olmesartan medoxomil: in the treatment of essential arterial hypertension, the initial dosage should be 10 mg daily, taken regardless of the meal. In case of reduced effect, and always under strict medical supervision, the dosage can be increased up to 40mg / day. In some cases, in order to avoid too large an increase in the dose, other antihypertensive drugs such as hydrochlorothiazide can be associated with OLMETEC ®. In any case, the therapeutic protocol must necessarily be described by the doctor after a careful evaluation of the patient's state of health, considering that in some risk categories, as in subjects with impaired hepatic and renal function, the maximum permitted doses are lower than to those previously indicated.

IN ANY CASE, BEFORE TAKING OLMETEC ® Olmesartan medoxomil - THE PRESCRIPTION AND CONTROL OF YOUR OWN DOCTOR IS REQUIRED.

Warnings OLMETEC ® Olmesartan medoxomil

In the event of impaired renal function and mild hepatic function, it would be advisable to constantly monitor the plasma levels of electrolytes, such as sodium and potassium, and of creatinine before and during OLMETEC ® therapy. As anticipated, in these cases the dosages should be reviewed, especially in the maximum dose.

In case of severe kidney or liver disease, the use of this drug is not recommended.

Furthermore, dehydration (frequent in elderly patients), pathologies of the gastro-intestinal tract, renal insufficiency, diabetes, and concomitant use of potassium-sparing diuretic drugs, could - in conjunction with the administration of OLMETEC ® increase the risk of hyperkalemia, with possible effects collateral also of serious entity.

Particular care must be taken in patients suffering from pathologies - such as renal artery stenosis and severe congestive heart failure - in which the vascular tone is strongly dependent on the renin-angiotensin system, so the administration of this drug could cause hypovolaemic crises.

As with the other angiontesin II antagonists, the therapeutic effects of OLMETEC ® appear to be reduced in black patients, probably due to the low levels of renin available.

The presence of lactose as an excipient could cause adverse reactions of varying degrees in patients intolerant to this sugar or galactose, suffering from enzymatic deficits or with malabsorption problems.

Finally, even if there is no evidence that directly correlates the use of olmesartan with the impairment of normal driving skills and use of machinery, it should be considered that some side effects associated with antihypertensive therapy, such as dizziness and drowsiness, could reduce the normal capacity perceptual and reactive of the patient.

PREGNANCY AND BREASTFEEDING

The administration of OLMETEC ® during the entire period of pregnancy is strictly not recommended, given the presence of studies showing the teratogenic effect induced by angiotensin II antagonists, also considering the hemodynamic effects that an antihypertensive drug could determine (reduction of perfusion fetal blood, fetal hypotension, oligohydramnios), with consequent increased risk of anomalies and delays in normal fetal development.

The same indication can be extended to the period of breastfeeding, given the presence of studies (albeit only on laboratory animals) that show how olmesartan is secreted in breast milk.

Interactions

OLMETEC ® its active ingredient may interact with the following drugs:

Potassium-sparing diuretics and potassium supplements, resulting in hyperkalemia;
Antihypertensive drugs, with an enhancement of hypotensive efficacy; this characteristic, if well modulated, could be used for therapeutic purposes, but if poorly managed it could increase the risk of hypotensive crises;
Non-steroidal anti-inflammatory drugs, which, by altering the normal electrolyte balance, could increase the risk of impaired renal function;
Lithium, given the pharmacokinetic alterations, could increase its cytotoxicity.

Contraindications OLMETEC ® Olmesartan medoxomil

OLMETEC ® is contraindicated in case of hypersensitivity to one of its components and metabolites, in case of obstruction of the biliary tract, severe hepatic and renal insufficiency, and during pregnancy and lactation.

Undesirable effects - Side effects

The various clinical trials show a good tolerability of the drug, with clinically little relevant and transient adverse reactions. Among the most complained of symptoms is dizziness, muscle cramps, myalgia, cough and gastro-enteric symptoms.

It is however necessary to remember that, although very rare, some clinically more important adverse reactions can be realized in particular categories of patients at risk or in the case of drug interactions, and determine hyperkalimia, renal failure, changes in liver function and thrombocytopenia.

The drug OLMETEC ® appears to be well tolerated and cases of hypersensitivity are rare, which occur mainly with gastro-intestinal and cutaneous symptoms.