Composition, form of production and packaging
Tablets covered with a film coating of white color, oblong; on one side - embossing "12.5", risks on both sides.
1 tab.
carvedilol 12.5 mg
Excipients: microcrystalline cellulose, lactose monohydrate, crospovidone, povidone, colloidal silicon dioxide, magnesium stearate, Opadry II white YS-22-18096 (titanium dioxide, polydextrose, hypromellose 3cp, hypromellose 6cp, triethylcitrate, hypromellose 50c, macrogol-8000).
10 pieces. - blisters (3) - packs of cardboard.
The tablets covered with a film membrane of white color, oblong.
1 tab.
carvedilol 3.125 mg
Excipients: microcrystalline cellulose, lactose monohydrate, crospovidone, povidone, colloidal silicon dioxide, magnesium stearate, Opadry II white YS-22-18096 (titanium dioxide, polydextrose, hypromellose 3cp, hypromellose 6cp, triethylcitrate, hypromellose 50c, macrogol-8000).
10 pieces. - blisters (3) - packs of cardboard.
The tablets covered with a film shell of white color, oblong form; on one side - embossing "6.25".
1 tab.
carvedilol 6.25 mg
Excipients: microcrystalline cellulose, lactose monohydrate, crospovidone, povidone, colloidal silicon dioxide, magnesium stearate, Opadry II white YS-22-18096 (titanium dioxide, polydextrose, hypromellose 3cp, hypromellose 6cp, triethylcitrate, hypromellose 50c, macrogol-8000).
10 pieces. - blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Carvedilol has a combination of non-selective beta 1 , beta 2 and alpha 1- adrenoblocking action. The drug does not have its own sympathomimetic activity, it has membrane-stabilizing properties. Due to blockade of? -adrenoceptors of the heart, blood pressure, cardiac output and heart rate can be reduced. Carvedilol suppresses the renin-angiotensin-aldosterone system) by blocking the? -adrenoceptor of the kidney, causing a decrease in renin plasma activity. By blocking? -adrenoceptors, the drug can cause an increase in peripheral vessels, thereby reducing systemic vascular resistance. The combination of blockade of ОІ-adrenoreceptors 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 by "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 in the "first pass" through the liver.Carvedilol is contraindicated in cases of serious impairment of liver function.
Carvedilol penetrates through the placental barrier, is secreted with difficult milk.
INDICATIONS
- arterial hypertension (in monotherapy and combination with diuretics);
- chronic heart failure (as part of combination therapy);
- IHD: stable angina.
DOSING MODE
Inside, squeezed enough fluids, regardless of food intake.
With 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 hypotensive effect is inadequate after 2 weeks of therapy, the dose can be increased 2 times. The maximum recommended daily dose of the drug is 50 mg 1 time / day (possibly divided into 2 divided doses).
With angina pectoris - the initial dose is 12.5 mg 2 times / day in the first 2 days of treatment. Then 25 mg twice a day. If the anti-angiogenic effect is inadequate, after 2 weeks of therapy, the dose can be increased 2-fold. The maximum recommended daily dose is 100 mg / day, divided into 2 divided doses.
In chronic heart failure, the dose is selected individually, under the strict supervision of a doctor. The initial dose is 3.125 mg 2 times / day for 2 weeks, then (with good tolerability), this 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; inpatients with a body weight of more than 85 kg, a target dose of 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: headache (usually not strong at the beginning of treatment), dizziness, loss of consciousness, myasthenia gravis (often at the beginning of treatment), sleep disorders, depression, paresthesia, fatigue.
From the side of the cardiovascular system: bradycardia, orthostatic hypotension, angina pectoris, AV blockade; rarely - occlusive disorders of peripheral circulation, progression of heart failure.
On the part of the digestive system: dry mouth, nausea, abdominal pain, loss of appetite, diarrhea or constipation, vomiting, increased activity of hepatic transaminases.
From the hemopoietic system: thrombocytopenia, leukopenia.
From the side of metabolism: weight gain, violation of carbohydrate metabolism.
Allergic reactions: skin allergic reactions (exanthema, urticaria, pruritus), exacerbation of psoriasis, nasal congestion.
On the part of the respiratory system: dyspnea and bronchospasm (in predisposed patients).
Other: flu-like syndrome, pain in the limbs, intermittent claudication, reduced tearing, sneezing, myalgia, arthralgia; rarely - a violation of urination, a violation of kidney function.
CONTRAINDICATIONS
- acute and chronic heart failure (in the stage of decompensation);
severe hepatic impairment;
- AV-blockade of II-III st .;
- pronounced bradycardia (less than 50 beats / min);
- syndrome of weakness of the sinus node;
- cardiogenic shock;
- chronic obstructive pulmonary disease;
- arterial hypotension (systolic blood pressure less than 85 mm Hg);
- age under 18 years (safety and efficacy not established);
- hypersensitivity to carvedilol or other components of the drug.
With prudence, prinzmetal angina, diabetes mellitus, hypoglycaemia, thyrotoxicosis, peripheral vascular occlusive diseases, pheochromocytoma, depression, myasthenia gravis, psoriasis, kidney failure, AV blockade of I degree, extensive surgical interventions and general anesthesia.
PREGNANCY AND LACTATION
Controlled studies of the use of carvedilol in pregnant women have not been carried out, 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 FUNCTIONS OF THE LIVER
Carefully.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated:
severe hepatic insufficiency.
APPLICATION FOR CHILDREN
Contraindicated in children under 18 years.
APPLICATION IN ELDERLY PATIENTS
At the beginning of Carvedigamma therapy, or with an increase in the dose of the drug in elderly patients, there may be an excessive decrease in blood pressure, mainly on rising. A dose adjustment is necessary.
SPECIAL INSTRUCTIONS
Therapy should be performed vigorously and should not abruptly cease, 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 Carvedigamma therapy 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. Do not increase the dose of Carvedigam. recommended the appointment of large doses of diuretics until the stabilization of the patient.
It is recommended to monitor ECG and BP continuously while prescribing Carvedigamma 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 Carvedigamma.
Carvedilol does not affect the concentration of glucose in the blood and does not cause changes in the indices of glucose tolerance test in patients with non-insulin-dependent diabetes mellitus.
During treatment avoid the use of ethanol.
Patients with a fechromocytoma before the start of therapy should be prescribed alpha-blockers.
Patients wearing contact lenses should note that the drug can 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 increasing doses of carvedilol. It is necessary to refrain from other activities associated with the need for high concentration of attention and rapid psychomotor reactions.
OVERDOSE
Symptoms: marked decrease in blood pressure (accompanied by dizziness or fainting), bradycardia (less than 50 beats per minute). There may be shortness of breath due to bronchospasm and vomiting. In severe cases, cardiogenic shock is possible. violation of breathing, confusion, conduction disorder, cardiac arrest.
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 iv-choline blockers (atropine), adrenomimetics (epinephrine, norepinephrine) iv.
DRUG INTERACTION
Carvedilol may potentiate the effect of other concurrently taken antihypertensive agents (ACE inhibitors, thiazide diuretics, vasodilators) or agents 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 (nimethidine) 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 increases later (correction of the daily dose of cyclosporine is recommended).
Simultaneous administration 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
Keep the drug in a dark place at a temperature of no higher than 25 В° C. Keep out of the reach of children.
Shelf life - 3 years.
Do not use after the time specified on the package.
