BLOPRESS ® is a drug based on candesartan cilexetil.
THERAPEUTIC GROUP: Antihypertensives - antagonists of the receptor for angiotensin II
Indications BLOPRESS ® Candesartan cilexetil
BLOPRESS® is used in patients with essential hypertension, heart failure and impaired systolic function of the left ventricle. In these latter conditions it can be used in case of intolerance to ACE inhibitors or, when tolerated, in synergy with them, in order to improve their therapeutic properties.
Mechanism of action BLOPRESS ® Candesartan cilexetil
BLOPRESS ® administered orally, is absorbed only in small part, guaranteeing bioavailability values that rarely exceed 14%, determining the beginning of the therapeutic activity 2 hours later, and reaching the maximum plasma peak after 3 and a half hours from his assumption. For BLOPRESS ® to exert its therapeutic action, its active ingredient, candesartan cilexetil, must be transformed into the active metabolite candesartan (through a "hydrolysis that occurs rapidly in the gastro-enteric tract). Once absorbed and bound in largely to plasma proteins, candesartan can thus reach the various target organs and exert its therapeutic action. The biological activity of this molecule is expressed in the antagonist action against angiotensin II on the AT1 receptors. In fact, the angiotensin II-AT1 receptor binding determines a series of effects - such as vasoconstriction, stimulation of aldosterone, induction of cell growth and regulation of hydro-saline homeostasis - which contribute, among other things, to support blood pressure. candesartan, by binding the AT1 receptor in a fairly stable manner, prevents its activation by angiotensin II, significantly reducing vascular contraction and ensuring a significant reduction in blood pressure without potentially dangerous reflex mechanisms for the patient's health.
At the end of the effect, following a half-life of about 9 hours, the active principle is largely eliminated by the urinary route and to a small extent also by the biliary route.
Studies carried out and clinical efficacy
1. CANDESARTAN IN THE TREATMENT OF HYPERTENSION
Arch Mal Coeur Vaiss. 2007 Aug; 100: 679-82.
[Efficacy of candesartan cilexetil in hypertensive patients with or without diabetes]
El Féghali R, Nisse-Durgeat S, Asmar R.
In this study conducted on over 700 patients suffering from hypertension (blood pressure levels above 140/90 mmHg), and in some cases from diabetes, the administration of 8 mg of candesartan cilexetil for 4/6 weeks, guaranteed a reduction in blood pressure levels. of about 20 mmHg, returning these patients to a normal blood pressure range
2. CANDESARTAN AND TREATMENT OF HYPERTENSION IN PATIENTS AT RISK OF HEART.
J Stroke Cerebrovasc Dis. 2010 Aug 10. [Epub ahead of print]
Renin-Angiotensin System Blockade Safely Reduces Blood Pressure in Patients With Minor Ischemic Stroke During the Acute Phase.
Nakamura T, Tsutsumi Y, Shimizu Y, Uchiyama S.
Treatment with candesartan during the acute phase of ischemia, while not determining an immediate "hypotensive action", guarantees in the short term (more precisely in just 14 days of therapy), a drop in blood pressure of about 25 mmHg, reducing the risk future of acute ischemic stroke.
3. CANDESARTAN, THE MOST EFFECTIVE SARTAN
Curr Med Res Opin. 2007 Jul; 23: 1693-705.
Candesartan cilexetil - a review of effects on cardiovascular complications in hypertension and chronic heart failure.
Meredith PA.
A careful re-reading of the international scientific documentation has shown how candesartan is among the antagonists of the receptor for angiotensin II, one of those with greater affinity and with greater therapeutic effect. Among the various advantages deriving from the administration of this drug, it is possible to include the particular antihypertensive efficacy in association with diuretics or other antihypertensives, in the face of a series of side effects of modest clinical entity.
Method of use and dosage
BLOPRESS ® Candesartan cilexetil 8/16/32 mg tablets: the doses foreseen for the treatment of hypertension normally foresee doses between 8 and 16mg per day (1/2 tablets per day). In cases where the patient should be refractory to this dosage, it could reach a maximum of 32 mg / day, or choose an alternative antihypertensive therapy.
In the treatment of heart failure, however, doses of 4 mg of candesartan cinexidil are suggested.
Therapeutic efficacy is generally observed for prolonged administration for at least 4 weeks.
A dosage adjustment must be made in some categories of patients at risk, for which the physician must carefully evaluate the physio-pathological conditions, and choose a dose that can minimize the possible side effects, while preserving the therapeutic functions.
Warnings BLOPRESS ® Candesartan cilexetil
BLOPRESS ® therapy, especially in patients with heart failure, could lead to a significant reduction in renal function; therefore it would be advisable to constantly monitor the plasma levels of potassium and creatinine.
It is important to consider that the concomitant administration of drugs capable of interfering with the renin-angiotensin system, or antihypertensives of various kinds, could lead to hypotensive episodes, even serious ones. Particular attention must be paid in case of simultaneous administration of potassium-sparing diuretics. , due to the risk of hyperkalaemia and consequent alteration of the normal heart rhythm.
Stroke and heart attack may be more frequent in patients with ischemic heart disease or ischemic cardiovascular disease, due to the drug's severe hypotensive effect.
The presence of lactose could cause a series of side effects in patients intolerant to galactose, lactose or suffering from lactase deficiency and glucose and / or galactose malabsorption.
Despite the absence of a direct correlation between administration of BLOPRESS ® reduction of the patient's perceptive and reactive potential, any hypotensive episodes or side effects of various kinds could compromise the ability to drive and use machinery.
PREGNANCY AND BREASTFEEDING
The use of BLOPRESS ® during pregnancy is strictly not recommended, as candesartan could cause an alteration in the blood perfusion of the fetus, seriously compromising its growth and development. On the other hand, preclinical studies conducted on animals have shown a causal link between taking BLOPRESS ® fetal and neonatal malformations.
During breastfeeding, even if not yet ascertained in human milk, the active principle of BLOPRESS ® could be secreted in breast milk; therefore, it is not recommended to take it even during this period.
Interactions
The number of studies evaluating the simultaneous administration of BLOPRESS ® with other drugs appears limited; however it is possible to describe some combinations that alter the normal function of candesartan. More precisely, the simultaneous intake of other drugs with antihypertensive activity, or capable of affecting the renin-angiontensin system, could determine an increase in the hypotensive effect with consequent risk for the patient's health.
Potassium-sparing diuretics, or potassium-sparing diuretics, may increase the risk of hyperkalemia. Non-steroidal anti-inflammatory drugs, on the other hand, could counteract the antihypertensive action of BLOPRESS ®
Contraindications BLOPRESS ® Candesartan cilexetil
We do not recommend the use of BLOPRESS ® during pregnancy and lactation, in case of cholestasis, severe hepatic insufficiency or hypersensitivity to one of its components.
Undesirable Effects - Side Effects
The undesirable effects of BLOPRESS ® are in most cases of mild clinical severity and transient, with involvement of the central nervous system (headache and dizziness), cardiovascular (hypotension), urinary (impaired renal function) and blood (alteration of plasma levels of transaminases, creatinine, potassium and urea).
However, only in a few cases was it necessary to discontinue therapy.
In case of hypersensitivity to one of the components of BLOPRESS ®, dermatological reactions (eruptions, rash) and feverish reactions were mainly observed.
Note
BLOPRESS ® can only be sold under medical prescription
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