Universal reference book for medicines
Product name: CARVEDILOL (CARVEDILOL)

Active ingredient: carvedilol

Type: Beta 1 -, beta 2 -adrenergic blocker.
Alpha 1- adrenoblocker
Manufacturer: MAKIZ-PHARMA (Russia)
Composition, form of production and packaging
Tablets are
flat-cylindrical, white, with a facet and a risk.

1 tab.

carvedilol 12.5 mg

- "- 25 mg

Excipients: lactose, sucrose, polyvidon K25, crospovidone, methylcellulose, sodium croscarmellose.

10 pieces.
- packings cellular planimetric (3) - packs cardboard.
30 pcs.
- packings of cellular contour (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

The description of the drug was approved by the manufacturer for the 2006 print edition.

PHARMACHOLOGIC EFFECT

Alpha- and beta-adrenoblocker without internal sympathomimetic activity.

Does it block?
1 -,? 1 and? 2- adrenoreceptors. Has vasodilating, antianginal and antiarrhythmic action.
The vasodilating effect is associated mainly with blockade?
1- adrenoreceptors. Thanks to vasodilation reduces OPSS. It has membrane-stabilizing properties. The combination of vasodilation and blockade of ОІ-adrenoreceptors leads to the following effects: in patients with arterial hypertension, a decrease in blood pressure is not accompanied by an increase in OPSS, peripheral blood flow (in contrast to beta-blockers) does not decrease. The heart rate decreases slightly.
In patients with IHD, it has an antianginal effect.
Reduces pre- and postnagruzku on the heart. It has no pronounced effect on the lipid metabolism and the content of potassium, sodium, and magnesium in the blood plasma. In patients with impaired left ventricular function or circulatory failure, it has a beneficial effect on hemodynamic parameters and improves the ejection fraction and the size of the left ventricle. It has an antioxidant effect, eliminating free oxygen radicals.
PHARMACOKINETICS

Suction

After ingestion, carvedilol is rapidly and almost completely absorbed from the digestive tract.
Bioavailability is 25% (due to the high degree of metabolism in the liver). Concentration in the blood plasma is proportional to the dose taken. C max in blood plasma is achieved after 1 hour. The intake of food slows the absorption of carvedilol, without affecting its bioavailability.
Distribution

Binding to plasma proteins is almost complete - 98-99%.
Penetrates through the placental barrier, excreted in breast milk.
Metabolism

Metabolized with the formation of metabolites that have a high ability to block ОІ-adrenoreceptors.

Excretion

T 1/2 - 6-10 h. It is excreted mainly with bile.

Pharmacokinetics in special clinical cases

In elderly patients, the carvedilol concentration in the blood plasma is approximately 50% higher than in young patients.

In patients with impaired liver function, bioavailability can increase to 80%.

INDICATIONS

- arterial hypertension (as a mono or combination therapy);

- stable angina pectoris;

- chronic heart failure (as part of combination therapy).

DOSING MODE

The dosage regimen is set individually.

The drug is taken orally, regardless of food intake.

With hypertension for the first 7-14 days, the recommended initial dose is 12.5 mg / day (1 tab.) In the morning after breakfast.
The dose can be divided into 2 divided doses of 6.25 mg of Carvedilol (1/2 tablets of 12.5 mg). Next, the drug is prescribed in a dose of 25 mg (1 table, 25 mg) in 1 morning, or divided into 2 divided doses of 12.5 mg (1 table 12.5 mg). If necessary, after 14 days, it is possible to increase the dose once more.
With stable angina, the initial dose of Carvedilol is 12.5 mg (1 table 12.5 mg) 2 times / day.
After 7-14 days the dose can be increased to 25 mg (1 table 25 mg) 2 times / day. With insufficient effectiveness and good tolerability after 14 days and the dose of Carvedilol can be further increased. The daily dose of Carvedilol in angina pectoris should not exceed 50 mg (2 tablets of 25 mg), prescribed 2 times / day.
For patients over the age of 70, the daily dose of Carvedilol should not exceed 25 mg (1 table 25 mg) 2 times / day.

If the drug is withdrawn, the dose reduction should be carried out gradually within 1-2 weeks.

If you miss a regular dose, the drug should be taken as soon as possible.
However, if it's time for the next appointment, then you need to take only one single dose (without doubling).
At a break in taking the drug for more than 2 weeks, it is necessary to resume treatment with the lowest doses of Carvedilol.

Tablets are taken after meals, washed down with a small amount of water.

With chronic heart failure, the dose is selected individually, under the careful supervision of a doctor.
The recommended initial dose is 3.125 mg 2 times / day for 2 weeks. With good tolerability, the dose is increased at intervals of at least 2 weeks to 6.25 mg 2 times / day, then 12.5 mg 2 times / day and then to 25 mg 2 times / day. The dose should be increased to the maximum, which is well tolerated by the patient. In patients with a body weight of less than 85 kg, the target dose is 50 mg / day, in patients with a body weight of more than 85 kg, the target dose is 75-100 mg / day. If treatment is interrupted for more than 2 weeks, then its resumption begins with a dose of 3.125 mg 2 times / day, followed by an increase in the dose.
SIDE EFFECT

From the side of the central nervous system and peripheral nervous system: headache, dizziness, syncopal conditions, muscle weakness (often at the beginning of treatment), sleep disorders, depression, paresthesia.

From the cardiovascular system: bradycardia, orthostatic hypotension, angina pectoris, AV blockade;
rarely - violations of peripheral circulation, intermittent claudication, progression of heart failure.
On the part of the digestive system: dry mouth, nausea, abdominal pain, diarrhea, constipation, vomiting, increased activity of hepatic transaminases.

From the hemopoietic system: thrombocytopenia, leukopenia.

From the urinary system: severe renal dysfunction, edema.

Allergic reactions: skin reactions (exanthema, urticaria, pruritus, rash), exacerbation of psoriasis, sneezing, nasal congestion, bronchospasm, dyspnea (in predisposed patients).

Other: influenza-like syndrome, pain in the extremities, reduction of teardrop, weight gain.

CONTRAINDICATIONS

severe hepatic impairment;

- pronounced bradycardia (heart rate less than 50 beats per minute);

- SSSU;

- AV blockade II and III degree (except for patients with an artificial pacemaker);

- chronic heart failure in the stage of decompensation;

- acute heart failure;

- cardiogenic shock;

- arterial hypotension (systolic blood pressure less than 85 mm Hg);

- Pregnancy;

- lactation (breastfeeding);

- children and adolescence under 18;

- hypersensitivity to carvedilol and other components of the drug.

With caution appoint the drug with angina Prinzmetal, thyrotoxicosis, occlusive diseases of peripheral vessels, pheochromocytoma, psoriasis, renal insufficiency, AV-blockade I degree, extensive surgical interventions and general anesthesia, diabetes mellitus, hypoglycemia, depression, myasthenia gravis.

PREGNANCY AND LACTATION

The drug is contraindicated for use in pregnancy and lactation (breastfeeding).

APPLICATION FOR FUNCTIONS OF THE LIVER

With caution appoint a drug for kidney failure.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Contraindicated in severe hepatic insufficiency.

APPLICATION FOR CHILDREN

The drug is contraindicated in children and adolescents under 18 years.

APPLICATION IN ELDERLY PATIENTS

For patients over the age of 70, the daily dose of Carvedilol should not exceed 25 mg (1 table 25 mg) 2 times / day.

SPECIAL INSTRUCTIONS

Caution should be given to patients with bronchospastic syndrome, chronic bronchitis, emphysema.

At the beginning of treatment with Carvedilol and with increasing the dose of the drug, a sharp decrease in blood pressure and orthostatic reactions are possible.Dizziness may occur up to fainting, especially in elderly patients, with heart failure, with combined antihypertensive therapy or with diuretics.

The drug is not recommended for use in patients with low blood pressure.

Treatment with carvedilol should not be abruptly discontinued, especially in patients with angina pectoris.
this can lead to a worsening of the condition. Dose reduction should be gradual within 1-2 weeks.
During the period of carvedilol administration, renal function in patients with renal insufficiency, ischemic heart disease, peripheral vascular disease, arterial hypotension and / or heart failure should be monitored.
If the kidney function worsens, the drug should be discarded.
The appointment of beta-blockers to patients with peripheral vascular disease, with psoriasis and anaphylactic reactions in an anamnesis can lead to a worsening of the course of the disease, and with Prinzmetal angina pectoris may provoke the appearance of chest pain.
In addition, the use of carvedilol may reduce the sensitivity of allergic tests.
The purpose of the drug may mask the symptoms of thyrotoxicosis and the early symptoms of hyperglycemia.
With diabetes, regular monitoring of blood glucose levels and, if necessary, correction of hypoglycemic therapy are recommended.
With the use of Carvedilol with caution should be conducted general anesthesia using drugs with a negative inotropic effect (ether, cyclopropane, trichlorethylene).The patient should inform the doctor about taking Carvedilol.
Before extensive surgical interventions, gradual withdrawal is recommended.
Care should be taken when using the drug in case of severe metabolic acidosis.

When using the drug in patients with pheochromocytoma before the start of therapy, alpha-blockers are prescribed.

Avoid using the drug when wearing contact lenses due to reduced tearing.

During the period of drug use, alcohol should be avoided.

It should be borne in mind that if you need to cancel combination therapy with carvedilol and clonidine, Carvedilol should be canceled first, a few days before the gradual decrease in the dose of clonidine.

Use in Pediatrics

The safety and efficacy of carvedilol in children and adolescents under the age of 18 years have not been established.

Impact on the ability to drive vehicles and manage mechanisms

It should be borne in mind that at the beginning of treatment and with increasing doses of Carvedilol, blood pressure can be excessively reduced, causing dizziness.Therefore, during the treatment period, patients should refrain from engaging in potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

OVERDOSE

Symptoms: severe arterial hypotension, bradycardia, respiratory disorders (including bronchospasm), heart failure, cardiogenic shock, cardiac arrest.

Treatment: if the patient is conscious, vomiting is necessary.
The patient should be given a horizontal position with raised legs.
The unconscious patient should be laid on his side and take measures to remove the non-sucking drug.
In such cases, hospitalization is required.
If necessary, symptomatic therapy is performed, adrenoreceptor agonists are administered.

DRUG INTERACTION

On the background of Carvedilol therapy, diltiazem and verapamil can not be administered IV because of a possible pronounced decrease in heart rate and a pronounced decrease in blood pressure.

Some antiarrhythmic drugs, narcosis drugs, antihypertensive drugs, antianginal drugs, other beta-blockers (including those used in the form of eye drops), MAO inhibitors, sympatholytics (reserpine) and cardiac glycosides can enhance the effect of Carvedilol.
With a simultaneous appointment with Carvedilol, doses of these drugs should be selected with caution.
When applied simultaneously with inducers of liver enzymes (for example, with rifampicin, phenobarbital), the concentration of carvedilol in the blood plasma may decrease, and when combined with inhibitors of hepatic enzymes (eg, cimetidine), the carvedilol concentration in the plasma may increase.

With the simultaneous use of carvedilol may increase the concentration of digoxin in the blood plasma.

Simultaneous administration of carvedilol with ergot alkaloids worsens the peripheral circulation.

Carvedilol may enhance the effect of hypoglycemic drugs and mask the manifestations of hypoglycemia (it is recommended to regularly monitor blood glucose levels).

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be stored out of reach of children, dry, protected from light, at a temperature of no higher than 25 В° C.
Shelf life - 3 years.
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