Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Antihypertensive agent from the group of alpha and beta-adrenoblockers without internal sympathomimetic activity. Does it block? 1 -,? 1 - and? 2- adrenoreceptors. As a result of the blockade? 1- adrenoreceptors moderately reduces conduction, force and heart rate, without causing a sharp bradycardia. As a result of the blockade? 1-adrenoreceptor causes the dilatation of peripheral vessels. As a result of the blockade? 2- adrenoreceptors may slightly increase the tone of the bronchi, some vessels of the microcirculatory bed, as well as tone and peristalsis of the intestine.
PHARMACOKINETICS
After oral administration, it is quickly and almost completely absorbed from the digestive tract. C max in blood plasma is reached within 1 h. Bioavailability is 25%.
Binding to plasma proteins is 98-99%. V d - about 2 l / kg. Penetrates through the placental barrier, excreted in breast milk. Exposed to the effect of "first passage" through the liver. Metabolites have a pronounced antioxidant and adrenoblocking effect.
T 1/2 - 6-10 hours. The plasma clearance is 590 ml / min. It is excreted mainly with bile.
In patients with impaired liver function, bioavailability can increase to 80%.
INDICATIONS
Arterial hypertension.
IHD: prevention of attacks of stable angina.
Chronic heart failure (as part of combination therapy).
DOSING MODE
Is taken internally. The initial dose is 12.5 mg 1 time / day, then the dose is increased to 25 mg 1 time / day. If necessary, the dose can be increased 1 time in 2 weeks;the maximum dose is 50 mg / day. In elderly patients, an effective dose of 12.5 mg / day may be effective.
SIDE EFFECT
From the side of the cardiovascular system: at the beginning of treatment (the effect of the first dose) and with an increase in the dose, there are episodes of excessive blood pressure lowering (usually these phenomena go by themselves and the patient's condition stabilizes without special correction); with further application of carvedilol, a bradycardia is also possible; less frequent violations of peripheral blood flow, attacks of angina pectoris, AV blockade, episodes of intermittent claudication; in some cases - increased manifestations of heart failure.
From the side of the central nervous system and the peripheral nervous system: weakness, fatigue, headache are possible; in some cases - sleep disorders, mental depression, paresthesia.
On the part of the digestive system: increased tonus and intestinal motility; in some cases - a change in the activity of transaminases in the blood plasma.
Allergic reactions: rarely - allergic exanthema, itching.
Dermatological reactions: urticaria, reactions resembling flat lichen, the appearance of psoriatic plaques or exacerbation of the previously existing psoriatic process.
From the respiratory system: in some cases - nasal congestion.
On the part of the hematopoiesis system: in some cases - thrombocytopenia, leukopenia.
CONTRAINDICATIONS
AV blockade of II and III degree, pronounced bradycardia, heart failure in decompensation stage, shock, bronchial asthma, chronic lung diseases with bronchial obstructive syndrome in the anamnesis, hepatic insufficiency, pregnancy, lactation, hypersensitivity to carvedilol.
PREGNANCY AND LACTATION
Carvedilol is contraindicated in pregnancy and lactation (breastfeeding).
Although there is no direct indication of the embryo or fetotoxic effect of carvedilol, it is known that it penetrates the placental barrier and is excreted in breast milk.Blockade of? - and? -adrenoceptors in a fetus or newborn can induce a perinatal or neonatal distress syndrome manifested by bradycardia, respiratory depression, hypothermia and hypoglycemia.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in liver failure.
APPLICATION FOR CHILDREN
Clinical experience with carvedilol in pediatrics is lacking.
APPLICATION IN ELDERLY PATIENTS
In elderly patients, an effective dose of 12.5 mg / day may be effective.
SPECIAL INSTRUCTIONS
With caution apply in patients with ischemic heart disease and heart failure. Before starting treatment with carvedilol in heart failure, adequate therapy should be used to correct the symptoms of decompensation.
When carvedilol is used in patients with IHD, the need for myocardium in oxygen can be reduced (due to the blockade of? 1- adrenoreceptors). In this regard, the abolition of carvedilol should be carried out gradually to avoid the development of angina attacks.
In patients with endocrine disorders, carvedilol may mask symptoms of hyperthyroidism and early signs of acute hyperglycemia (which should be prevented in patients with insulin-dependent diabetes mellitus).
During the treatment is not recommended the use of alcohol.
Clinical experience with carvedilol in pediatrics is lacking.
Impact on the ability to drive vehicles and manage mechanisms
At the beginning of treatment, as well as increasing the dose of carvedilol during treatment, one should refrain from driving and other activities related to the need for high concentration of attention and rapid psychomotor reactions.
DRUG INTERACTION
With the simultaneous use of antiarrhythmic drugs with carvedilol, anesthetics, antihypertensive drugs, antianginal drugs, other beta-blockers (including in the form of eye drops), there is a risk of unwanted drug interactions.
With the simultaneous use of inhibitors of the isoenzyme CYP2D6, the potentiation of carvedilol is theoretically possible.
With simultaneous application of inducers of the isoenzyme CYP2D6 of the system, a decrease in the action of carvedilol is possible.
With simultaneous use with verapamil, diltiazem for iv introduction, it is possible to develop severe arterial hypotension.
With simultaneous use with digoxin, an increase in the concentration of digoxin in the blood plasma and an increased risk of severe bradycardia and AV conduction disorders are possible.
With the simultaneous use of insulin, oral hypoglycemic drugs may increase the risk of developing hypoglycemia.
With simultaneous application with clonidine possible pronounced bradycardia, arterial hypotension, conduction disorders. In the case of sudden withdrawal of clonidine in patients receiving carvedilol, a sharp increase in blood pressure is possible.
With simultaneous application with reserpine, MAO inhibitors, there is a risk of developing severe arterial hypotension and bradycardia.
With simultaneous use with rifampicin, AUC and C max of carvedilol in blood plasma decrease.
Fluoxetine inhibits the isoenzyme CYP2D6, which leads to inhibition of carvedilol metabolism and its cumulation. It can strengthen cardiodepressive action (including bradycardia). Fluoxetine and, mainly, its metabolites are characterized by a prolonged T 1/2 , so the probability of drug interaction persists even a few days after fluoxetine cancellation.
With simultaneous application with cimetidine, AUC of carvedilol increases without changing its C max in blood plasma.
With simultaneous application with cyclosporine, an increase (from a small to a moderate one) of the concentration of cyclosporine in the blood plasma is possible.
When used simultaneously with ergotamine derivatives, peripheral circulation may worsen.
