Composition, form of production and packaging
Tablets are white or white with a yellowish hue of color, biconvex form.
1 tab.
carvedilol 6.25 mg
- "- 12.5 mg
- "- 25 mg
Excipients: sugar (sucrose), magnesium stearate, potato starch, hydroxypropylmethylcellulose (hypromellose), croscarmellose sodium (impellose), silicon dioxide colloid (aerosil), calcium phosphate.
7 pcs. - packings cellular planimetric (2) - packs cardboard.
7 pcs. - packings cellular planimetric (3) - packs cardboard.
7 pcs. - packings cellular planimetric (4) - packs cardboard.
7 pcs. - packings cellular planimetric (5) - packs cardboard.
7 pcs. - packings cellular planimetric (8) - packs cardboard.
7 pcs. - packings cellular planimetric (10) - packs cardboard.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
10 pieces. - packings cellular planimetric (3) - packs cardboard.
10 pieces. - packings cellular planimetric (4) - packs cardboard.
10 pieces. - packings cellular planimetric (5) - packs cardboard.
10 pieces. - packings cellular planimetric (8) - packs cardboard.
10 pieces. - packings cellular planimetric (10) - packs cardboard.
15 pcs. - packings cellular planimetric (2) - packs cardboard.
15 pcs. - packings cellular planimetric (3) - packs cardboard.
15 pcs. - packings cellular planimetric (4) - packs cardboard.
15 pcs. - packings cellular planimetric (5) - packs cardboard.
15 pcs. - packings cellular planimetric (8) - packs cardboard.
15 pcs. - packings cellular planimetric (10) - packs cardboard.
20 pcs. - packings cellular planimetric (2) - packs cardboard.
20 pcs. - packings cellular planimetric (3) - packs cardboard.
20 pcs. - packings cellular planimetric (4) - packs cardboard.
20 pcs. - packings cellular planimetric (5) - packs cardboard.
20 pcs. - packings cellular planimetric (8) - packs cardboard.
20 pcs. - packings cellular planimetric (10) - packs cardboard.
30 pcs. - packings cellular planimetric (2) - packs cardboard.
30 pcs. - packings cellular planimetric (3) - packs cardboard.
30 pcs. - packings cellular planimetric (4) - packs cardboard.
30 pcs. - packings cellular planimetric (5) - packs cardboard.
30 pcs. - packings cellular planimetric (8) - packs cardboard.
30 pcs. - packings cellular planimetric (10) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
PHARMACHOLOGIC EFFECT
Alpha- and beta-adrenoblocker. Carvedilol has a combined non-selective beta 1 -, beta 2 - and alpha 1- blocking action. The drug does not have its own sympathomimetic activity, it has membrane-stabilizing properties. Thanks to blockade of? -adrenoceptors of the heart, there is a decrease in blood pressure, a reduction in cardiac output and heart rate. Carvedilol suppresses RAAS by blocking the? -adrenoceptors of the kidneys, causing a decrease in plasma renin activity. By blocking? -adrenoceptors, the drug can cause an increase in peripheral vessels, thereby reducing systemic vascular resistance.
The combination of blockade of? -adrenoceptors and vasodilation has the following effects: in patients with arterial hypertension, a decrease in 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 digestive tract. Has high lipophilicity. C max in the blood is reached after 1-1.5 hours. T 1/2 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 on 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. Carvedilol penetrates the placental barrier, excreted in breast milk.
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.Carvedilol is contraindicated in cases of serious impairment of liver function.
INDICATIONS
- arterial hypertension (as a monotherapy and combination with diuretics);
- chronic heart failure (as part of combination therapy);
- IHD: stable angina.
DOSING MODE
Inside, regardless of food intake.
Arterial hypertension
The initial dose is 6.25-12.5 mg 1 time / day in the first 2 days of treatment. Then - 25 mg 1 time / 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 / day (possibly divided into 2 divided doses).
CHD
The initial dose is 12.5 mg 2 times / day in the first 2 days of treatment. Then - 25 mg 2 times / 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 / day, divided into 2 divided doses.
Chronic heart failure
The dose is selected individually, under the careful supervision of the doctor. The recommended initial dose is 3.125 mg 2 times / day for 2 weeks. With good tolerance, the dose is increased at intervals of at least 2 weeks to 6.25 mg 2 times / day, then to 12.5 mg 2 times / day, 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.
SIDE EFFECT
From the nervous system: dizziness, headache (usually not strong at the beginning of treatment), loss of consciousness, myasthenia gravis (often at the beginning of treatment), fatigue, depression, sleep disturbance, paresthesia.
From the cardiovascular system: bradycardia, orthostatic hypotension, AV-blockade of II-III degree, rarely - violation of peripheral circulation, progression of heart failure (in the period of increasing doses), edema of the lower limbs, angina, marked decrease in blood pressure.
On the part of the digestive system: dry mouth, nausea, diarrhea or constipation, vomiting, abdominal pain, loss of appetite, increased activity of hepatic transaminases.
From the hemopoietic system: rarely - thrombocytopenia, leukopenia.
From the side of metabolism: weight gain, violation of carbohydrate metabolism.
Allergic reactions: skin allergic reactions, nasal congestion.
On the part of the respiratory system: dyspnea and bronchospasm (in predisposed patients).
Other: exacerbation of psoriasis, impaired vision, reduced tearing, flu-like syndrome, sneezing, myalgia, arthralgia, pain in limbs, intermittent claudication, rarely - urination disorder, renal dysfunction.
CONTRAINDICATIONS
- hypersensitivity to carvedilol or other components of the drug;
- acute and chronic heart failure (in the stage of decompensation);
severe hepatic impairment;
- AV-blockade of II-III degree;
- pronounced bradycardia (less than 50 beats / min);
- SSSU;
- arterial hypotension (systolic blood pressure less than 85 mm Hg);
- cardiogenic shock;
- COPD;
- Children and adolescents under 18 years of age (efficacy and safety not established).
Precautions: Prinzmetal angina, thyrotoxicosis, peripheral vascular occlusive diseases, pheochromocytoma, psoriasis, renal failure, first-degree AV blockade, 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, and therefore the prescription of this category of patients is possible only in cases when the benefit to the mother exceeds the potential risk for the fetus.
Not recommended breastfeeding during treatment with carvedilol.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindications: severe hepatic impairment.
SPECIAL INSTRUCTIONS
Therapy should be carried out for a long time and should not abruptly stop, especially in patients with ischemic heart disease. 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 the drug Carvedilol-OBL 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 Carvedilol-OBL, recommended the appointment of large doses of diuretics until the stabilization of the patient.
We recommend continuous monitoring of ECG and AD with simultaneous prescription of Carvedilol-OBL and slow calcium channel blockers, phenylalkylamine derivatives (verapamil) and benzothiazepine (diltiazem), and also with class I antiarrhythmics.
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 prior therapy with Carvedilol-OBL.
Carvedilol-OBL 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 the treatment should be avoided the use of ethanol.
Patients with pheochromocytoma prior to therapy should be assigned alpha-blockers.
Patients wearing contact lenses should note that the drug may cause a decrease in tearing.
Impact on the ability to drive vehicles and manage mechanisms
It is not recommended to drive at the beginning of therapy and with an increase in the dose of Carvedilol-OBL. It is necessary to refrain from other activities associated with the need for high concentration of attention and rapid psychomotor reactions.
OVERDOSE
Symptoms : decreased 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 indicators, if necessary - in the ICU. Treatment is symptomatic. It is expedient to use iv-choline blockers (atropine), adrenomimetics (epinephrine, norepinephrine) iv.
DRUG INTERACTION
Carvedilol can potentiate the effect of other concurrently taken antihypertensive drugs or drugs that have an antihypertensive effect (nitrates).
With the combined use of carvedilol and diltiazem, cardiac conduction disorders and hemodynamic disorders may develop.
With the simultaneous administration of carvedilol and digoxin, the concentration of the latter increases and the AV-holding time may increase.
Carvedilol can potentiate the action of insulin and oral hypoglycemic agents, and the symptoms of hypoglycemia (especially tachycardia) can be masked, so in patients with diabetes it is recommended that the blood glucose level be monitored regularly.
Inhibitors of microsomal oxidation (cimetidine) increase, and inducers (phenobarbital, rifampicin) weaken the hypotensive effect of carvedilol.
Drugs that reduce the content of catecholamines (reserpine, MAO inhibitors), increase the risk of developing arterial hypotension and severe bradycardia.
With the simultaneous use of cyclosporine, the concentration of the latter increases (a correction of the daily dose of cyclosporine is recommended).
Simultaneous reception of clonidine may potentiate antihypertensive and heart rhythm-slowing effects of carvedilol.
General anesthetics increase the negative inotropic and hypotensive effect of carvedilol.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
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 - 2 years.
