KARVEA ® Irbesartan

KARVEA ® is a drug based on irbeisartan

THERAPEUTIC GROUP: Antihypertensives - angiotensin II antagonists

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

Indications KARVEA ® Irbesartan

KARVEA ® is indicated for the treatment of essential arterial hypertension or as part of an antihypertensive drug treatment in renal disease of hypertensive patients with type II diabetes mellitus.

Mechanism of action KARVEA ® Irbesartan

Irbesartan, the active ingredient of KARVEA ® taken orally, is rapidly and effectively absorbed, reaching peak plasma levels after 1.5 / 2 hours.

Mainly bound to plasma proteins, with total concentrations ranging between 60 and 80% of the oral intake, it acts downstream of the renin-angiotensin system, inhibiting the activation of the AT1 receptor by angiotensin II. More precisely, this molecule is able to bind the receptor (AT1) with angiotensin II with greater affinity and avidity, preventing its activation and the consequent biological effects, such as vasoconstriction, aldosterone secretion and alteration of the hydro-saline balance . The antihypertensive action - which, given the long half-life of the active principle, occurs on average after 3/6 hours and persists for at least 24 hours - does not generally accompany rebound reactions, such as the increase in heart rate, which in many cases limit the use of these drugs in clinical practice.

After its biological effect, ibersartan, after hepatic metabolism, is mostly eliminated through the faeces, even if a portion of about 20% is found in the urine.

Studies carried out and clinical efficacy

1 IRBESARTAN AND DIABETES

Irbesartan is also known to treat hypertension associated with diabetic nephropathy among its therapeutic indications. Several studies, however, have also stressed the possible efficacy of this active ingredient in the modulation of glycemia, then on insulin-glucose homeostasis. This experimental study, for example, demonstrates how the administration of irbesartan in diabetic guinea pigs can determine a greater efficacy of the insulin action, improving the transport of glucose inside the insulin-sensitive cell.

2. IRBESARTAN AND ERECTILE DYSFUNCTION

Erectile dysfunction is a condition frequently associated with hypertension, endothelial damage and the metabolic syndrome. It is known that irbesartan can guarantee - in addition to a significant drop in blood pressure - a protection against vascular endothelium, with a series of improvements that can also be translated into a revival of erectile function. The detailed study shows that 6-month therapy with this drug can guarantee a marked improvement in erectile function in patients suffering from metabolic syndrome.

3. THE EFFECTIVENESS OF IRBESARTAN / HYDROCHLOROTHIAZIDE IN THE TREATMENT OF HYPERTENSION

This study - conducted on 468 patients suffering from severe hypertension and high cardiovascular risk (obesity) - shows how the treatment for 7 weeks with irbesartan / hydrochlorothiazide, guaranteed a reduction in systolic pressure of about 28/42 mmHg and of diastolic pressure of about 23/27 mmHg, without clinically relevant side effects. These results suggest the good efficacy of irbesartan in the rapid control of hypertension.

Method of use and dosage

KARVEA ® 75 mg tablets of irbesartan: in the treatment of essential arterial hypertension, the most effective therapeutic dose, which guarantees better blood pressure control over a 24-hour period, is 150 mg a day. Given the absence of pharmacokinetic and pharmacodynamic changes, the drug can be taken independently of the simultaneous administration of food.

In elderly or hemodialysed patients, and in other risk groups, therapy should be started with a daily dose of 75 mg.

Your doctor may choose to increase the irbesartarn dose up to 300mg daily in case of a reduced or absent therapeutic response, or prefer concomitant administration with other antihypertensive drugs.

In both cases, the choice of the appropriate dosage must be made by your doctor, based on the patient's health conditions and the severity of his pathology.

KARVEA ® Irbesartan warnings

The administration of an antihypertensive in general, and of an angiotensin II inhibitor in particular, should require - in addition to the evaluation of arterial pressure - also a continuous monitoring of serum levels of some electrolytes (in particular sodium and potassium), and others markers of renal function, such as creatinine. These periodic checks would therefore also be useful to prevent any hyperkalemia, which is more frequent in the case of concomitant therapy with potassium-sparing diuretics.

The vasodilatory action induced by irbesartan could lead to hypotensive crises and related acute diseases in patients suffering from severe heart failure, severe kidney disease and in all those conditions in which vascular tone and renal function are mainly maintained by this system.

In addition, particular attention should be paid to dosages in case of concomitant antihypertensive therapy, in elderly patients and in other risk categories (hemodialysis patients or patients with liver disease).

Although in the literature no direct cases are described in which the intake of KARVEA is correlated with a reduction in driving ability or use of machinery, it is important to consider that some side effects associated with antihypertensive therapy could determine a significant decrease in perceptive and reactive capacities of the patient, inducing for example dizziness and drowsiness.

PREGNANCY AND BREASTFEEDING

It is known from several experimental studies that the administration of ACE inhibitors and antagonists of the renin-angiotensin system may significantly affect correct fetal development, leading to abnormalities, injury and death. Therefore it is strictly not recommended to use KARVEA ® during pregnancy.

Since the possible secretion of irbesartan into breast milk is not known at the moment, it would be advisable to stop breast-feeding during therapy.

Interactions

The antihypertensive activity of KARVEA ® can be increased in case of concomitant administration of other antihypertensive drugs; this property can also be used for therapeutic purposes, in order to increase the effectiveness of the drug, provided that blood pressure and some blood parameters are monitored. Particular attention should be paid in the event that one of the antihypertensive drugs administered belongs to the category of potassium-sparing diuretics, given the possible incidence of hyperkalemia.

Non-steroidal anti-inflammatory drugs and corticosteroids could reduce the therapeutic efficacy of irbesartan.

The pharmacokinetic changes induced by irbesartan on lithium salts could eventually lead to an increase in the cytotoxicity of this compound.

Contraindications KARVEA ® Irbesartan

KARVEA ® is contraindicated in case of hypersensitivity to one of its components and metabolites, in case of obstruction of the biliary tract, severe liver failure, as well as during pregnancy and lactation.

Undesirable effects - Side effects

Several studies seem to agree on the good tolerability of irbesartan, and in this case of KARVEA ® as the side effects found were in most cases of modest clinical and transient significance. Among the adverse reactions, the most observed were those affecting the respiratory system, in particular infections, headache, myalgia, asthenia, diarrhea and nausea. On the other hand, hypersensitivity reactions such as skin rashes or nervous disorders have been more rare.