Karvenal - instructions for use, dose, side effects, contraindications

Carvedilol has a combined non-selective β₁-, β₂and α₁-blocking action. The drug does not have its own sympathomimetic activity, it has membrane-stabilizing properties. Thanks to blockade of β-adrenergic receptors of the heart, blood pressure, cardiac output and heart rate can be reduced. Carvedilol suppresses the renin-angiotensin-aldosterone system through blockade of β-adrenergic receptors of the kidney, causing a decrease in plasma renin activity. Blocking α-adrenoreceptors, the drug can cause the expansion of peripheral vessels, thereby reducing systemic vascular resistance.The combination of blockade of β-adrenergic receptors and vasodilation has the following effects: in patients with arterial hypertension - lowering blood pressure; in patients with ischemic heart disease - anti-ischemic and antianginal action; in patients with left ventricular dysfunction and circulatory failure - favorably affects hemodynamic parameters, increases the fraction of the left ventricular ejection and reduces its size.

Pharmacokinetics:

Carvedilol is rapidly absorbed from the gastrointestinal tract. Has high lipophilicity. The maximum concentration in the blood is reached after 1-1,5 hours. The half-life is 6-10 hours. It binds to blood plasma proteins by 95-99%. Bioavailability of the drug is 24-28%. Eating does not affect bioavailability. Metabolized in the liver with the formation of a number of active metabolites - 60-75% of the adsorbed drug is metabolized at the first "passage" through the liver. Metabolites have a pronounced antioxidant and adrenoblocking effect. Removal of the drug from the body occurs through the gastrointestinal tract.

When the renal function is impaired, the pharmacokinetic parameters of carvedilol do not change significantly.

In patients with impaired liver function, the systemic bioavailability of carvedilol increases due to a decrease in metabolism during the first "passage" through the liver. With serious violations of liver function, carvedilol is contraindicated.

Carvedilol penetrates the placental barrier, excreted in breast milk.

Indications:

Arterial hypertension (in monotherapy and combination with diuretics).

Chronic heart failure (as part of combination therapy).

Ischemic heart disease: stable angina.

Contraindications:

Hypersensitivity to carvedilol or other components of the drug; acute and decompensated chronic heart failure, requiring intravenous inotropic drugs; severe hepatic insufficiency, atrioventricular block II-III (less than 50 beats per minute), sinus node weakness syndrome, arterial hypotension (systolic blood pressure less than 85 mm Hg), cardiogenic shock, chronic obstructive pulmonary disease, age under 18 years (efficacy and safety not established ).

Carefully:

Stenocardia of Prinzmetal, thyrotoxicosis, occlusive diseases of peripheral vessels, pheochromocytoma, psoriasis, renal failure, atrioventricular blockade of the 1st degree, extensive surgical interventions and general anesthesia, diabetes mellitus, hypoglycemia, depression, myasthenia gravis.

Pregnancy and lactation:

Controlled studies of the use of carvedilol in pregnant women have not been carried out, so the prescription of this category of patients is possible only in cases where the benefit to the mother exceeds the potential risk to the fetus.

Not recommended breastfeeding during treatment with carvedilol.

Dosing and Administration:

For oral administration, regardless of food intake.

For the therapy of essential hypertension, it is necessary to use CARVENAL in dosages: 6.25 mg (1/4 tablet) and 12.5 mg (1/2 tablet).

Arterial hypertension

The initial dose is 6.25 - 12.5 mg once a day for the first two days of treatment. Then 25 mg once a day. If the antihypertensive effect is inadequate after 2 weeks of therapy, the dose can be increased 2-fold. The maximum recommended daily dose of the drug is 50 mg 1 time per day (possibly divided into 2 doses).

Cardiac ischemia

For the therapy of ischemic disease, it is necessary to use CARVENAL in dosages: 12.5 mg (1/2 tablet); 25 mg.

The initial dose is 12.5 mg twice a day in the first two days of treatment. Then 25 mg twice a day. If the antianginal effect is inadequate after 2 weeks of therapy, the dose may be increased 2-fold. The maximum recommended daily dose of the drug is 100 mg per day, divided by 2 reception.

Chronic heart failure

For the therapy of chronic heart failure, it is necessary to use CARVENAL in dosages: 3,125 mg (1/8 tablet), 6.25 mg (1/4 tablet); 12.5 mg (1/2 tablet).

The dose is selected individually, under the careful supervision of the doctor. The recommended initial dose is 3,125 mg 2 times a day for 2 weeks. With good tolerability, the dose is increased at intervals of at least 2 weeks to 6.25 mg twice a day, then to 12.5 mg twice a day, then to 25 mg twice a day. The dose should be increased to the maximum dose, which is well tolerated by the patient. In patients with a body weight of less than 85 kg, the target dose is 50 mg per day; in patients with a body weight of more than 85 kg, the target dose of 75-100 mg per day.

Side effects:

From the central nervous system: dizziness, headache (usually not severe pain and early treatment), loss of consciousness, myasthenia gravis (often at the beginning of treatment), increased fatigue, depression, sleep disturbance, paresthesia.

From the side of the cardiovascular system: bradycardia, orthostatic hypotension, atrioventricular block II-III s, rarely - violation of peripheral circulation, progression of heart failure (in the period of increasing doses), swelling of the lower extremities, angina, marked decrease in blood pressure.

From the side of the digestive tract: dry mouth, nausea, diarrhea or constipation, vomiting, abdominal pain, loss of appetite, increased activity of "liver" transaminases.

On the part of the hematopoiesis system: rarely - thrombocytopenia, leukopenia.

From the side of metabolism: weight gain, violation of carbohydrate metabolism.

Allergic reactions: skin allergic reactions, exacerbation of psoriasis, nasal congestion.

From the respiratory system: dyspnea and bronchospasm (in predisposed patients).

Other: impaired vision, reduced tearing, flu-like syndrome, sneezing, myalgia, arthralgia, pain in the limbs, "intermittent" lameness, rarely - urination disorder, renal dysfunction.

Overdose:

Symptoms: lowering blood pressure (accompanied by dizziness or fainting), bradycardia. There may be shortness of breath due to bronchospasm and vomiting. In severe cases, cardiogenic shock, respiratory failure, confusion, conduction disorders are possible.

Treatment: it is necessary to monitor and correct vital signs, if necessary - in the intensive care unit. Treatment is symptomatic. It is expedient to use intravenous m-holinoblokatorov (atropine), adrenomimetics (epinephrine, norepinephrine).

Interaction:

CARVENAL may potentiate the action of other concurrently taken antihypertensive drugs or drugs that have an antihypertensive effect (nitrates).

With the joint application of CARVENAL and diltiazem may develop violations of cardiac conduction and hemodynamic disorders.

With the simultaneous reception of CARVENAL and digoxin the concentration of the latter increases and the time of atrioventricular conduction may increase.

CARVENAL can potentiate the action insulin and oral hypoglycemic agents, while the symptoms of hypoglycemia (especially tachycardia) can be masked, so patients with diabetes recommended regular monitoring of blood sugar levels.

Inhibitors of microsomal oxidation (cimetidine) strengthen, and inducers (phenobarbital, rifampicin) weaken the hypotensive effect of CARVENAL.

Drugs that reduce the content of catecholamines (reserpine, monoamine oxidase inhibitors), increase the risk of arterial hypotension and severe bradycardia.

With simultaneous application cyclosporine the concentration of the latter increases (a correction of the daily dose of cyclosporine is recommended).

Simultaneous appointment clonidine can potentiate antihypertensive and heart rhythm-reducing effects of CARVENAL.

General anesthetics intensify the negative inotropic and hypotensive effect of CARVENAL.

Special instructions:

Therapy should be carried out for a long time and should not abruptly cease, especially in patients with coronary heart disease, since this can lead to a worsening of the course of the underlying disease. If necessary, the dose reduction should be gradual, within 1-2 weeks.

At the beginning of therapy with CARVENAL or with increasing the dose of the drug in patients, especially the elderly, there may be an excessive decrease in blood pressure, mainly on rising. A dose adjustment is necessary. In patients with chronic heart failure, the choice of a dose may increase the symptoms of heart failure, the appearance of edema. In this case, do not increase the dose of CARVENAL, recommended the appointment of large doses of diuretics until the stabilization of the patient.

It is recommended to monitor the electrocardiogram and blood pressure continuously while simultaneously prescribing CARVENAL and blockers of "slow" calcium channels, phenylalkylamine derivatives (verapamil) and benzodiazepine (diltiazem), and also with antiarrhythmic drugs of the first class.

It is recommended to monitor kidney function in patients with chronic renal failure, arterial hypotension and chronic heart failure.

In the case of a surgical procedure using general anesthesia, an anesthesiologist should be warned about the previous therapy with CARVENAL.

KARVENAL does not affect the concentration of glucose in the blood and does not cause changes in the glucose tolerance test in patients with non-insulin dependent diabetes mellitus.

During treatment avoid the use of ethanol.

Patients with pheochromocytoma prior to initiation of therapy should be assigned alpha-adrenoblock locators.

Patients wearing contact lenses should note that the drug can cause a decrease in tearing.

Effect on the ability to drive transp. cf. and fur:It is not recommended to drive at the beginning of therapy and with increasing doses of CARVENAL. It is necessary to refrain from other activities associated with the need for high concentration of attention and rapid psychomotor reactions.

Form release / dosage:

Tablets, 25 mg.

Packaging:

10 tablets in a blister of aluminum foil.

10 blisters together with instructions for use are placed in a cardboard box.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-003244/07

Date of registration:16.10.2007

Expiration Date:Unlimited

The owner of the registration certificate:Shin Pung Pharmaceutical Co., Ltd.Shin Pung Pharmaceutical Co., Ltd. The Republic of Korea

Manufacturer: & nbsp

SHIN POONG PHARMACEUTICAL, Co. Ltd. The Republic of Korea

Representation: & nbspPharmInform Ltd.PharmInform Ltd.Russia

Information update date: & nbsp10.12.2017

Illustrated instructions

Instructions

Carvénal (Carvenal)