KARVEA ® Irbesartan

KARVEA ® is an irbeisartan-based drug

THERAPEUTIC GROUP: Antihypertensives - angiotensin II antagonists

Indications KARVEA ® Irbesartan

KARVEA ® is indicated in 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 plasma peak after 1.5 / 2 hours.
Predominantly bound to plasma proteins, with total concentrations ranging between 60 and 80% of the amount taken orally, 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 greater affinity and avidity than angiotensin II, 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 ingredient occurs on average after 3/6 hours and persists for at least 24 hours - is generally not accompanied by rebound reactions, such as an increase in heart rate, which in many cases limit the "use of these drugs in clinical practice.
Once its biological effect is terminated, ibersartan, following hepatic metabolism, is mainly eliminated through the faeces, even if about 20% is recovered in the urine.

Studies carried out and clinical efficacy

1. IRBESARTAN AND DIABETES

Eur J Pharmacol. 2010 Sep 6. [Epub ahead of print]

Irbesartan enhances GLUT4 translocation and glucose transport in skeletal muscle cells.

Kobayashi T, Akiyama Y, Akiyama N, Katoh H, Yamamoto S, Funatsuki K, Yanagimoto T, Notoya M, Asakura K, Shinosaki T, Hanasaki K.

It is known that irbesartan also includes the treatment of hypertension associated with diabetic nephropathy among its therapeutic indications. Several studies, however, have also emphasized the possible efficacy of this active ingredient in modulating blood glucose, therefore on the " insulin-glucose homeostasis. This experimental study, for example, demonstrates how the administration of irbesartan in diabetic guinea pigs can determine a greater efficacy of insulin action, improving the transport of glucose within the insulin-sensitive cell.

2. IRBESARTAN AND ERECTILE DYSFUNCTION

Int J Impot Res. 2008 Sep-Oct; 20: 493-500. Epub 2008 Jul 3.

Effect of irbesartan on erectile function in patients with hypertension and metabolic syndrome.

Baumhäkel M, Schlimmer N, Böhm M; DO-IT Investigators.

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

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

J Clin Hypertens (Greenwich). 2010 Jul 1; 12: 487-94.

Efficacy and safety of irbesartan / HCTZ in severe hypertension according to cardiometabolic factors.

Franklin SS, Neutel JM.

This study - conducted on 468 patients with severe hypertension and high cardiovascular risk (obesity) - shows how treatment for 7 weeks with irbesartan / hydrochlorothiazide, guaranteed a reduction in systolic blood pressure of about 28/42 mmHg and in diastolic blood pressure of about 23/27 mmHg, with no clinically relevant side effects. These results suggest the good efficacy of irbesartan in the rapid control of hypertension.

Method of use and dosage

KARVEA ® irbesartan 75 mg tablets: in the treatment of essential arterial hypertension, the most effective therapeutic dose, which guarantees better blood pressure control over 24 hours, is that of 150 mg per day. Given the absence of pharmacokinetic and pharmacodynamic variations, the drug can be taken independently of the simultaneous administration of food.
In elderly or hemodialysis patients, and in other risk categories, therapy should be initiated with a daily dosage of 75 mg.
The physician may choose to increase the dose of irbesartarn up to 300mg daily in case of 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.

Warnings KARVEA ® Irbesartan

The administration of an antihypertensive in general, and of an angiotensin II inhibitor in particular, should require - in addition to the evaluation of blood pressure - also a continuous monitoring of the serum levels of some electrolytes (in particular sodium and potassium), and of others renal function markers, such as creatinine. These periodic checks would therefore also be useful in avoiding any hyperkalaemia, more frequent in case of concomitant therapy with potassium-sparing diuretics.
The vasodilating action induced by irbesartan could cause hypotensive crises and related acute diseases in patients with severe heart failure, severe renal diseases 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 therapy with antihypertensives, in elderly patients and in other categories at risk (patients on hemodialysis or with liver disease).
Although no direct cases have been described in the literature in which the intake of KARVEA is correlated with a reduction in the ability to drive or use machines, it is important to consider that some side effects associated with antihypertensive therapy could lead to a significant decrease in perceptive and reactive abilities. of the patient, for example inducing 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 can significantly affect the correct development of the fetus, resulting in abnormalities, injury and death. Therefore it is strictly not recommended to use KARVEA ® during pregnancy.
As the possible secretion of irbesartan in breast milk is not known at this time, breastfeeding should be discontinued 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 efficacy of the drug, provided that blood pressure and some blood parameters are monitored. Particular attention should be paid if one of the antihypertensive drugs administered belongs to the category of potassium-sparing diuretics, given the possible incidence of hyperkalaemia.
Non-steroidal anti-inflammatory drugs and corticosteroids may reduce the therapeutic efficacy of irbesartan.
The pharmacokinetic variations induced by irbesartan on lithium salts could eventually determine 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 biliary tract obstruction, severe hepatic insufficiency, as well as in 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 observed were in most cases of modest clinical relevance and transient. Among the adverse reactions, the most observed were those affecting the respiratory system, in particular infections, headache, myalgia, asthenia, diarrhea and nausea. Hypersensitivity reactions such as skin or nervous rash were rarer.

Note

KARVEA ® can only be sold under medical prescription.

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