COLVER ® is a carvedilol drug
THERAPEUTIC GROUP: Beta-blockers
Indications COLVER ® Carvedilol
COLVER ® is indicated in the treatment of essential arterial hypertension and angina pectoris.
The hypotensive effects of COLVER ® can be enhanced by the combination with antihypertensive drugs, such as diuretics.
Mechanism of action COLVER ® Carvedilol
The carvedilol contained in COLVER ® taken orally, is absorbed very quickly at the gastrointestinal level, reaching maximum plasma concentrations already after one "hour from" intake. Despite the good absorption profile, the bioavailability of this active ingredient never exceeds 25% of the total dose taken, given the presence of a very evident first pass metabolism.
Due to its lipophilic nature, the drug is bound to plasma proteins in the bloodstream, which act as transporters.
Carvedilol acts as a non-selective beta blocker. The important hypotensive effect, in fact, is also due to the inhibitory action exerted on the alpha 1 adrenergic receptors, expressed on the surface of the smooth muscle fiber cells of the small vessels (responsible for peripheral vasodilation); moreover, carvedilol carries out a "beta blocking activity on cardiac adrenergic receptors, necessary to reduce the work of the heart through modulation of the ventricular pre and post load.
Studies ascribe to carvedilol also an "antioxidant action, exerted through the detoxification of oxygen free radicals and probably involved in vascular protection.
Following a significantly longer half-life (6/10 hours) compared to its beta blocker relatives, the active principle is eliminated mainly through the faeces, following hepatic glucuroconjugation.
Studies carried out and clinical efficacy
COPERNICUS STUDY: THE "USE OF CARVEDILOL IN" HEART INSUFFICIENCY
Circulation. 2002 Oct 22; 106: 2194-9.
Effect of carvedilol on the morbidity of patients with severe chronic heart failure: results of the carvedilol prospective randomized cumulative survival (COPERNICUS) study.
Packer M, Fowler MB, Roecker EB, Coats AJ, Katus HA, Krum H, Mohacsi P, Rouleau JL, Tendera M, Staiger C, Holcslaw TL, Amann-Zalan I, DeMets DL; Carvedilol Prospective Randomized Cumulative Survival (COPERNICUS) Study Group.
This important study, conducted on approximately 2300 patients, has shown how the administration of carvedilol, in patients with mild or moderate heart failure, can reduce the risk of death and hospitalization related to cardiovascular events by 27% compared to control, and as much as 31% for heart failure. These data show how carvedilol can have a protective action on heart health, hindering the worsening of heart failure.
2. THE ANTIOXIDANT EFFECTS OF CARVEDILOL
J Hypertens. 2007 Apr; 25: 731-41.
Antioxidant activity of carvedilol in cardiovascular disease.
Dandona P, Ghanim H, Brooks DP.
Unlike cardioselective beta blockers used in the treatment of cardiovascular diseases, carvedilol seems to have a strong antioxidant action. Recent studies show how this active ingredient can intervene both in the detoxification of oxygen free radicals and in the suppression of the production of these reactive species, guaranteeing an improvement in the patient's clinical condition.
3.CARVEDILOL IN METABOLIC SYNDROME
Int Heart J. 2006 May; 47: 421-30.
The effect of carvedilol on metabolic parameters in patients with metabolic syndrome.
Uzunlulu M, Oguz A, Yorulmaz E.
The direct involvement of carvedilol in numerous metabolic pathways has prompted researchers to study the effects of this active ingredient in patients with metabolic syndrome. The data, somewhat encouraging, have shown how - unlike other beta blockers - the administration of carvedilol can cause a decrease in blood pressure while maintaining the biochemical and metabolic parameters, thus reducing cardiovascular risk.
Method of use and dosage
COLVER ® 6.25 / 25 mg carvedilol tablets: the standard treatment for hypertension involves the administration of 12.5 mg of carvedilol in the first two days, followed by the maintenance dose of 25 mg daily in a single dose. In case of reduced therapeutic response, it is possible to increase the dosage up to a maximum of 50 mg, possibly taken in two different daily doses; alternatively, COLVER ® can be combined with an antihypertensive drug of another nature.
The same therapeutic protocol should also be used for the treatment of angina pectoris, while in the case of heart failure it is advisable to formulate the dosage based on the severity of the disease.
Dosage adjustment, more precisely a dose reduction, is advisable in the case of patients undergoing therapy with digitalis, diuretics and ACE inhibitors, to subsequently provide for an increase in the dose based on the therapeutic effects observed and in any case not before two weeks (time interval needed to maximize effects).
IN ANY CASE, BEFORE TAKING COLVER ® Carvedilol - THE PRESCRIPTION AND CONTROL OF YOUR DOCTOR IS NECESSARY.
Warnings COLVER ® Carvedilol
The warnings and precautions necessary to minimize the side effects of carvedilol are multiple and justified by the numerous biological reactions in which this active ingredient is involved.
Diabetic patients undergoing hypoglycemic therapy, for example, should constantly monitor glycemic levels to prevent the action of carvedilol on glucose metabolism from causing glycemic decompensation, while patients suffering from ischemic heart disease, vascular disease, heart failure, even treated, should monitor the renal function parameters, in order to reduce the risk of renal failure.
Ventilatory capacities should be monitored by a physician during carvedilol therapy in patients with bronchospasms and breathing difficulties. In case of worsening of this functionality, it is necessary to suspend the therapy through a phase of gradual reduction of the dosage used.
In case of surgical interventions, it is advisable to notify the anesthetist in due time, in order to avoid the use of anesthetics with marked negative inotropic activity and thus reduce side effects, such as severe bradycardia and hypotension.
In hypersensitive patients, carvedilol, like all other beta-blockers, could increase the sensitization phenomena to allergens, with a consequent risk of anaphylactic reactions.
Pheochromocytoma, Prinzmetal's angina and other particular pathological conditions could lead to an increase in the side effects of carvedilol.
The presence of some side effects such as headache and dizziness could reduce the patient's normal perceptive abilities, making the use of machinery and driving cars dangerous.
PREGNANCY AND BREASTFEEDING
Although there are no studies in the literature concerning the use of carvedilol in pregnancy, the haemodynamic (reduced placental perfusion) and metabolic (hypoglycemia) effects associated with the use of COLVER ® could harm the fetus and compromise its normal growth. Furthermore, given the presence of the active ingredient in breast milk, it is not recommended to take this drug both during pregnancy and during breastfeeding.
Interactions
Carvedilol, given its important antihypertensive effect, could easily interact with other drugs with hypotensive effect, such as diuretics or calcium antagonists, resulting in an enhancement of this activity. In this case, it is advisable to adjust the dosage in order to optimize the "therapeutic efficacy and minimize the onset of side effects.
In heart failure patients receiving digoxin therapy, concomitant administration of carvedilol may result in increased plasma digoxin concentrations, requiring monitoring of digoxin levels.
Furthermore, given the masking effect of the typical symptoms of hypoglycemia, it may be necessary to adjust the dose of hypoglycemic agents used.
The concomitant administration of rifampicin and mixed function oxidase inhibitors could result in an increase in plasma levels of carvedilol, with unpredictable biological effects.
Carvedilol could eventually interact with anesthetics with negative inotropic activity, enhancing their effect and increasing the patient's health risk.
Contraindications COLVER ® Carvedilol
COLVER ® is contraindicated in case of severe or inadequately treated heart failure, in case of bronchopneumopathy with bronchospasm, liver function abnormalities, asthma, cardiogenic shock, severe bradycardia, accentuated hypotension and in case of hypersensitivity to one of the its components.
Undesirable Effects - Side Effects
The undesirable effects described for COLVER ® appear to be generally transient and not clinically relevant. Among the most common adverse reactions it is possible to describe: dizziness, bradycardia, edema, nausea, diarrhea, vomiting, visual changes, headache and hyperglycemia.
The onset of asthma, dyspnoea, hypercholesterolemia, thrombocytopenia, mood alterations, decreased cardiac function and skin reactions in case of hypersensitivity has also been observed in predisposed patients.
Despite the numerous side effects described, only in a few cases it was necessary to discontinue the therapy.
Note
COLVER ® is sold only under medical prescription.
The use of COLVER ® in athletes, in the absence of therapeutic need, to reduce the physiological response to stress and the related symptoms (tremor of the limbs, increase in blood pressure, increase in emotional tension, etc.), constitutes a DOPANTE practice.
The information on COLVER ® Carvedilol published on this page may be out of date or incomplete. For a correct use of this information, see the Disclaimer and useful information page.
