Pharmacological action of the drug Coreg

Pharmacological action - antiarrhythmic, antianginal, vasodilating.

Blocks alpha1-, beta1- and beta2-adrenergic receptors. It does not have its own sympathomimetic activity, it has membrane stabilizing properties. It has an antioxidant effect by eliminating free oxygen radicals.

Pharmacodynamics

Reduces OPSS, reduces pre- and afterload on the heart. Does not have a pronounced effect on lipid metabolism and the content of potassium, sodium and magnesium in blood plasma.

Pharmacokinetics

Rapidly and almost completely absorbed from the gastrointestinal tract. It binds to plasma proteins by 98-99%. Bioavailability is about 25% due to the high degree of metabolism in the liver. Metabolites have beta-adrenergic blocking properties. Food slows down absorption, but does not affect bioavailability. Plasma concentration is proportional to the dose taken. Cmax in plasma is achieved after 1 hour. T1/2 - 6-10 hours. It is excreted mainly with bile.

In elderly patients, the plasma concentration is about 50% higher than in young people. In case of impaired liver function, bioavailability can increase up to 80%. Passes through the placental barrier, excreted in breast milk.

Clinical pharmacology

In patients with arterial hypertension, a decrease in blood pressure is not accompanied by an increase in systemic vascular resistance and a decrease in peripheral blood flow. The heart rate decreases slightly. In patients with coronary artery disease, it has an antianginal effect. In patients with impaired left ventricular function or circulatory failure, it has a beneficial effect on hemodynamic parameters and increases the left ventricular ejection fraction.

Indications of the drug Coreg

Arterial hypertension (monotherapy or in combination with other antihypertensive drugs), stable angina pectoris.

Interaction

Strengthens the effect of hypoglycemic agents, increases the concentration of digoxin in the blood. Some antiarrhythmic drugs, anesthetics, antihypertensive, antianginal drugs, other beta-blockers (including in the form of eye drops), MAO inhibitors, sympatholytics (reserpine), cardiac glycosides can enhance the effect. Cimetidine increases the concentration of carvedilol in the blood; rifampicin, phenobarbital - reduce. Simultaneous use with ergot alkaloids impairs peripheral circulation. It is incompatible with intravenous administration of verapamil and diltiazem (a pronounced slowing of the heart rate and a pronounced decrease in blood pressure is possible).

Dosing and Administration

Inside, after meals, with a small amount of liquid. The dose is selected individually.

Arterial hypertension: the recommended dose in the first 7-14 days is 12.5 mg / day in the morning after breakfast or divided into 2 doses of 6.25 mg, then 25 mg / day once in the morning or divided into 2 doses of 12.5 mg ... After 14 days, the dose may be increased again.

Stable angina pectoris: the initial dose is 12.5 mg 2 times a day, after 7-14 days, under the supervision of a physician, the dose can be increased to 25 mg 2 times a day. After 14 days, with insufficient efficacy and good tolerability of the drug, the dose can be further increased. The total daily dose should not exceed 100 mg (50 mg 2 times a day), over the age of 70 years - 50 mg / day (25 mg 2 times a day).

If the next dose is missed, the drug should be taken as soon as possible, however, if the time for taking the next dose is approaching, then only it is taken, without doubling. If it is necessary to discontinue the drug, the dose must be reduced gradually over 1–2 weeks.

Contraindications 

Hypersensitivity, chronic obstructive pulmonary disease, severe hepatic failure, severe bradycardia, sick sinus syndrome, grade II and III AV block (except for patients with a pacemaker), decompensated heart failure, pulmonary hypertension or cardiogenic shock, arterial hypotension, pregnancy , breastfeeding, age up to 18 years (safety and effectiveness in persons under 18 years of age has not been established).

Application during pregnancy and lactation

Contraindicated. During treatment, breastfeeding should be discontinued.

Overdose

Symptoms: marked lowering of blood pressure, bradycardia, impaired respiratory function (including bronchospasm), heart failure, cardiogenic shock, cardiac arrest.

Treatment: gastric lavage, the appointment of adrenergic receptor agonists; symptomatic therapy.

Precautions

Should be used with caution in case of bronchospastic syndrome, chronic bronchitis, pulmonary emphysema, Prinzmetal angina (possible worsening of the course), diabetes mellitus or hypoglycemia (regular monitoring of blood glucose levels is required), hyperthyroidism, peripheral vascular diseases (possible worsening of the course), pheochromocytoma (the appointment of beta-blockers is possible only after preliminary therapy with alpha-blockers), depression, myasthenia gravis, psoriasis, renal failure, severe metabolic acidosis, in patients using contact lenses.

At the beginning of treatment and with increasing doses, orthostatic hypotension, dizziness, fainting may occur (especially in elderly patients with heart failure or with the simultaneous use of other antihypertensive drugs or diuretics). It is recommended to monitor renal function in patients with renal failure, coronary artery disease, diffuse peripheral vascular disease, heart failure (with deterioration of renal function, drug withdrawal is necessary). Desensitization of allergic tests is possible. A gradual withdrawal of the drug is recommended before major surgical interventions. When simultaneous therapy with carvedilol and clonidine is canceled, treatment with carvedilol should be discontinued initially, and clonidine should be discontinued only after a few days.

It is not recommended to consume alcoholic beverages during the treatment period.

Special instructions

Do not stop taking the drug or change its dosage without first consulting a doctor. If the drug is interrupted for 2 weeks or more, treatment should be resumed with the lowest doses. In the absence of a therapeutic effect or worsening of the condition, you should consult a doctor.

It should not be used during work by vehicle drivers and people whose profession is associated with increased concentration of attention.

Side effects

From the nervous system and sensory organs: headache, dizziness, syncope, muscle weakness (more often at the beginning of treatment), sleep disturbances, depression, paresthesia, decreased secretion of lacrimal fluid.

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): bradycardia, AV blockade, orthostatic hypotension, rarely "intermittent" claudication, impaired peripheral circulation, progression of heart failure, thrombocytopenia, leukopenia.

From the respiratory system: sneezing, nasal congestion, bronchospasm, shortness of breath (in predisposed patients).

From the digestive tract: dry mouth, nausea, vomiting, abdominal pain, diarrhea or constipation, increased activity of hepatic transaminases.

From the urinary system: severe renal dysfunction, edema.

From the side of the skin: exacerbation of psoriatic eruptions.

Allergic reactions: exanthema, urticaria, itching, rashes.

Others: flu-like syndrome, pain in the limbs, weight gain.