VEDIKARDOL

Active material: Karvedilol
When ATH: C07AG02
CCF: Beta₁-,beta₂-adrenoblokator. Alpha₁-adrenoblokator
ICD-10 codes (testimony): I10, i20, I50.0
When CSF: 01.01.01.01.02
Manufacturer: Synthesis of (Russia)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Pills Valium, white or nearly white.

Excipients: lactose, potato starch, low molecular weight polyvinyl Medical (povidone), microcrystalline cellulose, calcium stearate, talc.

10 PC. – packings Valium planimetric (3) – packs cardboard.

Pharmacological action

Alpha- and beta-8th. Carvedilol has a combined non-selective effect, due to β blockade₁-, b₂– и a₁-adrenoreceptorov. The drug does not have its own sympathomimetic activity, has membrane stabilizing properties. Due to the blockade of β-adrenergic receptors of the heart, blood pressure decreases, cardiac output and decreased heart rate.

Carvedilol suppresses the renin-angiotensin-aldosterone system by blocking the β-adrenergic receptors of the kidneys, causing a decrease in Renin activity plasma. Inhibiting α-adrenergic receptor, the drug may cause peripheral vessels, thereby reducing TPR.

The combination of β-adrenergic receptor blockade and vasodilation has the following effects: with hypertension – decrease in blood pressure; at IBS – antianginal action; in patients with left ventricular dysfunction and circulatory failure, it has a beneficial effect on hemodynamic parameters, increases the left ventricular ejection fraction and helps to reduce its size.

Pharmacokinetics

Absorption

Carvedilol is rapidly absorbed from the gastrointestinal tract. High lipophilicity. C_max plasma levels achieved after 1-1.5 no. Bioavailability 24-28%. Eating does not affect the bioavailability of.

Distribution

Plasma protein binding – 95-99%.

Carvedilol penetrates through the placental barrier, excreted in breast milk.

Metabolism

Metabolised in the liver with the formation of a number of active metabolites – 60-75% the absorbed drug is metabolized when “first pass” through the liver. Metabolites have a pronounced anti-oxidant and adrenoblokirutm action.

Deduction

T_1/2 is 6-10 no. Displayed through the intestine.

Pharmacokinetics in special clinical situations

If any of the kidneys carvedilol significantly the pharmacokinetic parameters do not change.

In patients with impaired liver function, the systemic bioavailability of carvedilol increases due to a decrease in metabolism when “first pass” through the liver. In case of serious violations of the liver carvedilol is contraindicated.

Testimony

- Arterial hypertension (as monotherapy and in combination with diuretics);

- CHD: stable angina;

- Congestive heart failure (in a combination therapy).

Dosage regimen

The drug is taken orally, regardless of the meal.

Arterial hypertension

The initial dose is 6.25-12.5 mg 1 times / day for the first 2 days of treatment. Then by 25 mg 1 time / day. In case of insufficient antihypertensive effect through 2 weeks of therapy dose can be increased in 2 times. The maximum recommended daily dose of the drug is 50 mg 1 time / day, it can be divided into 2 admission.

CHD

The initial dose is on 12.5 mg 2 times/day for the first 2 days of treatment. Then by 25 mg 2 times / day. In case of insufficiency antianginalnogo effect through 2 weeks of therapy dose can be increased in 2 times. The maximum recommended daily dose of the drug is 100 mg / day, divided by 2 admission.

Congestive heart failure

Dose picked individually, under close medical supervision. The recommended starting dose is 3.125 mg 2 times / day for 2 weeks. With good endurance dose increase at intervals of not less than 2 weeks before 6.25 mg 2 times / day, then – to 12.5 mg 2 times / day and further – to 25 mg 2 times / day. The dose should be increased to a maximum of, which is well tolerated by patients. In Patients weighing less than 85 kg the target dose of 50 mg / day; in patients weighing more 85 kg target dose – 75-100 mg / day.

Side effect

From the central and peripheral nervous system: dizziness, headache (usually, mild and at the beginning of treatment), loss of consciousness, myasthenia (more often at the beginning of treatment), fatigue, depression, sleep disturbance, paresthesia.

Cardio-vascular system: bradycardia, orthostatic hypotension, AV-blockade II-III degree; rarely – the peripheral blood circulation, progression of heart failure (during the dose increase), edema of the lower extremities, angina, marked reduction in blood pressure, intermittent claudication.

On the part of the digestive tract: dry mouth, nausea, diarrhea or constipation, vomiting, abdominal pain, loss of appetite, increase in liver transaminases.

From the hematopoietic system: rarely – thrombocytopenia, leukopenia.

Metabolism: weight gain, violation of carbohydrate metabolism.

The respiratory system: Dyspnea and bronchospasm (prone patients).

On the part of the organ of vision: blurred vision, decrease in lacrimation.

On the part of the musculoskeletal system: myalgia, arthralgia, pain in the limbs.

From the urinary system: rarely – violation of urination, impairment of renal function.

Allergic reactions: cutaneous manifestations, nasal congestion.

Dermatological reactions: exacerbation of psoriasis.

Other: flu-like symptoms, chikhaniye.

Contraindications

- Acute heart failure;

- Congestive heart failure (decompensated);

- Severe hepatic impairment;

-AV-blokada II degree;

- Vыrazhennaya bradycardia (less 50 u. / min);

- SSS;

- Hypotension (systolic blood pressure less than 85 mm Hg. Art.);

- Cardiogenic shock;

- Chronic obstructive pulmonary disease;

- Up to 18 years (efficacy and safety have not been established);

- Hypersensitivity to the drug.

FROM caution should be used for Prinzmetal angina, thyrotoxicosis, occlusive peripheral vascular disease, pheochromocytoma, psoriaze, renal failure, AV-blockade I degree, for major surgical interventions and general anesthesia, for patients with diabetes, gipoglikemii, depression, myasthenia.

Pregnancy and lactation

Adequate and strictly controlled clinical studies on the safety of Vedicardol^® during pregnancy was conducted, therefore, prescribing the drug during pregnancy is possible only if, when the intended benefits to the mother outweighs the potential risk to the fetus.

Breastfeeding is not recommended during treatment with carvedilol..

Cautions

Therapy should be long and not stop dramatically, especially in patients with CHD, tk. This can lead to poor flow of main disease. If necessary, the dose reduction should be gradual., during 1-2 weeks.

At the beginning of Vedicardol therapy^® or if the dose of the drug in patients, particularly the elderly, There may be an excessive decline ad, mainly to stand up. Dose adjustment is required. In patients with chronic heart failure, when the dose is adjusted, the symptoms of heart failure may increase, the appearance of edema. In this case, you should not increase the dose of Vedicardol.^®, the appointment of large doses of diuretics is recommended until the patient's condition is stabilized.

Continuous monitoring of ECG and blood pressure is recommended with simultaneous administration of Vedicardol^® and blocking slow calcium channels, derived fenilalkilamina (verapamil), benzodiazepine derivatives (diltiazem), and – with class I antiarrhythmics.

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

In case of surgical intervention using general anesthesia, the anesthesiologist should be warned about the previous therapy with Vedicardol.^®.

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

Patients with pheochromocytoma should be prescribed alpha-blockers before starting therapy.

When prescribing to patients, using contact lenses, should be considered, that the drug can cause a decrease in tear production.

Avoid ethanol during treatment.

Effects on ability to drive vehicles and management mechanisms

It is not recommended to drive a car at the beginning of therapy and when increasing the dose of Vedicardol^®. Should refrain from other activities, related to high concentration and psychomotor quick reactions

Overdose

Symptoms: decrease in blood pressure (accompanied by dizziness or fainting), bradycardia. Possibly wheezing due to bronchoconstriction and vomiting. In severe cases there may be cardiogenic shock, respiratory failure, confusion, conduction disorders.

Treatment: it is necessary to monitor and correct vital signs, if necessary – in the intensive care unit (OBE). Symptomatic therapy. Appropriate in/with the introduction of m-holinoblokatorov (atropyn), adrenomimetikov (epinephrine, norepinephrine).

Drug Interactions

Carvedilol may potentiate the effect of other concurrently taken antihypertensive drugs or drugs, which have gipotenzivny effect (nitrates).

When coupled with enalapril and diltiazem can develop violations conductivity heart and hemodynamics.

While receiving carvedilol and digoxin increases the concentration of the latter and may increase time AV-holding.

Carvedilol may potentiate the action of insulin and oral gipoglikemicakih funds, When the symptoms of hypoglycemia (especially the tachycardia) can camouflage, therefore, in patients with diabetes mellitus, it is recommended to carry out regular monitoring of blood sugar levels.

Inhibitors of microsomal oxidation (cimetidine) increase, and its inductors (phenobarbital, rifampicin) weaken gipotenzivny effect of carvedilol.

Preparations, reduced catecholamine (reserpine, MAO inhibitors), increase the risk of arterial hypotension and bradycardia.

While the application of Cyclosporine increases the concentration of the latter (correction is recommended daily dose of Cyclosporine).

Concomitant administration of clonidine may potentiate the antihypertensive effect and the negative chronotropic effect of carvedilol.

General anesthetics are deepening the negative inotropy and hypotensive effects of carvedilol.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored out of reach of children, dry, dark place at a temperature no higher than 25 ° C. Shelf life – 2 year.