CARVEDILOL PILLS 25MG

Pharmacology

Pharmacodynamics

Carvedilol blocks alpha-1-, beta-1- and beta-2-adrenoreceptors. It has a vasodilating, antianginal and antiarrhythmic effect. The vasodilating effect is mainly due to blockade of alpha 1 receptors. Due to vasodilation, it reduces total peripheral vascular resistance (OPS). Does not have its own sympathomimetic activity, has membrane stabilizing properties. The combination of vasodilation and blockade of beta-adrenergic receptors leads to the following effects: in patients with arterial hypertension, a decrease in blood pressure (BP) is not accompanied by an increase in OPSS, peripheral blood flow is not reduced (unlike beta-blockers). HR decreases slightly. In patients with coronary artery disease has antianginal effect. Reduces pre- and afterload on the heart. It has no pronounced effect on lipid metabolism and the content of potassium, sodium, and Magnesium in the blood plasma. In patients with impaired left ventricular function or circulatory failure, a positive effect on hemodynamic parameters and improves ejection fraction and size of the left ventricle. It has an antioxidant effect, eliminating free oxygen radicals.

Pharmacokinetics

Carvedilol is rapidly and almost completely absorbed after ingestion from the gastrointestinal tract.It is almost completely bound to plasma proteins (98-99%). Plasma concentration is proportional to the dose taken. Bioavailability of about 25% due to a high degree of metabolism in the liver. At the same time, metabolites with a high ability to block beta-adrenergic receptors are formed.
The maximum plasma concentration is reached after 1 hour. The half-life is 6-10 hours.

In elderly patients, Carvedilol concentration in plasma is approximately 50% higher than in younger patients. Excreted mainly with bile. In patients with impaired liver function bioavailability may increase up to 80%. Gets through a placental barrier, it is allocated with breast milk. Food slows down the absorption of the drug, but does not affect its bioavailability.

Indications

• Hypertension (in monotherapy and combination with diuretics)
• Chronic heart failure (as part of combination therapy)
• Ischemic heart disease: stable angina.

Contraindications

• Hypersensitivity to carvedilol or other components of the drug,
• acute and decompensated chronic heart failure,
• requiring intravenous administration of inotropic agents,
• severe liver failure
• atrioventricular block II-III century.,
• severe bradycardia (less than 50 beats / min),
• sick sinus syndrome,
• arterial hypotension (systolic blood pressure less than 85 mm Hg. Art.),
• cardiogenic shock,
• bronchial asthma,
• chronic obstructive pulmonary disease
• age up to 18 years (efficacy and safety have not been established).

Carefully 
Bronchospastic syndrome, chronic bronchitis, pulmonary emphysema, Prince Metal stenocardia, thyrotoxicosis, occlusive peripheral vascular disease, pheochromocytoma, psoriasis, renal failure, I degree atrioventricular block, extensive surgical interventions and general anesthesia, diabetes mellitus, diabetes mellitus diabetes mellitus, I degree atrioventricular block I, extensive surgical interventions and general anesthesia, diabetes mellitus.

Pregnanacy and breastfeeding

Controlled studies of the use of carvedilol in pregnant women have not been conducted, therefore, the appointment of the drug in this category of patients is possible only in cases where the benefit to the mother outweighs the potential risk to the fetus.
Breastfeeding during carvedilol treatment is not recommended.

Special notes

Therapy should be carried out for a long time and should not stop abruptly, especially in patients with coronary heart disease, as this can lead to a worsening of the course of the underlying disease. If necessary, dose reduction of the drug should be gradual, within 1-2 weeks.
At the beginning of carvedilol therapy or with an increase in the dose of the drug in patients, especially the elderly, an excessive decrease in blood pressure may be observed, mainly when standing up. Correction of the dose of the drug.In patients with chronic heart failure in the selection of the dose may increase the symptoms of heart failure, the appearance of edema. You should not increase the dose of carvedilol, it is recommended the appointment of large doses of diuretics until the patient's condition stabilizes.

Constant monitoring of the electrocardiogram and blood pressure is recommended, while carvedilol and blockers of “slow” Calcium channels, derivatives of phenylalkylamine (verapamil) and benzodiazepine (diltiazem), as well as with class I antiarrhythmic drugs, are prescribed simultaneously.
It is recommended to monitor renal function in patients with chronic renal failure, arterial hypotension, and chronic heart failure.
In the case of surgery using general anesthesia, the anesthesiologist should be warned about prior carvedilol therapy.
Carvedilol does not affect the concentration of glucose in the blood and does not cause changes in the glucose tolerance test in patients with insulin-dependent diabetes mellitus.

During the period of treatment avoid the use of ethanol.
Patients with pheochromocytoma should be given alpha-blockers before therapy.
Patients wearing contact lenses should be aware that the drug may cause a decrease in tearing.
It is not recommended to drive a car at the beginning of therapy and with increasing doses of carvedilol.It should refrain from other activities related to the need for high concentration of attention and quick psychomotor reactions.

Active ingredient

1 pill contains:
active substance: carvedilola 25 mg.

Dosage and administration

Inside, regardless of the meal.
Strictly follow the instructions of the doctor. Without prior consultation with a doctor, you should not stop carvedilol treatment or change its dosage. If you need to cancel the drug, its dose should be reduced gradually over a period of 1 to 2 weeks.
If there is no therapeutic effect from the treatment or a worsening condition is noted, consult your doctor.

Arterial hypertension.
The dose is selected individually. The first 7-14 days, the recommended dose of Carvedilol is 12.5 mg (1 pill of 12.5 mg each) taken in the morning after breakfast. The dose can be divided into two doses of 6, 25 mg of Carvedilol (1/2 pills of 12.5 mg each). Further treatment should be carried out with carvedilol at a dose of 25 mg (1 pill of 25 mg) in the morning or divided into two doses of 12.5 mg of the drug (1 pill of 12.5 mg). If necessary, after 14 days, the doctor can again increase the dose.
Take the drug after a meal with a small amount of liquid.

Stable angina. The initial dose of Carvedilol is 12.5 mg (1 pill of 12.5 mg) twice a day. After 7-14 days under the supervision of a physician, the dose of Carvedilol can be increased to 25 mg (1 25 mg tablet) twice a day. After 14 days, with insufficient efficacy and good tolerability, the dose of Carvedilol can be further increased.

The total daily dose of carvedilol with angina should not exceed 50 mg of the drug (2 pills of 25 mg), administered 2 times a day. If your age exceeds 70 years, the daily dose of Carvedilola should not exceed 25 mg (1 pill of 25 mg) twice a day.
If you missed the next dose, you should take the drug as soon as possible.
However, if the time for taking the next dose is already approaching, then you should only take it, without doubling it.
You must take the drug regularly. If you have not taken the drug for more than 2 weeks, you need to resume treatment with the lowest doses.

Chronic heart failure. The dose is selected individually, under the close supervision of a doctor. The recommended initial dose is 3.125 mg 2 times a day for 2 weeks. With good tolerance, the dose is increased at intervals of at least 2 weeks to 6.25 mg 2 times a day, then at l2.5 mg 2 times a day, then to 25 mg 2 times a day. The dose should be increased to the maximum, which is well tolerated by the patient. In patients with a body weight less than 85 kg, the target dose is 50 mg per day; in patients with a body weight of more than 85 kg, a target dose of 75-100 mg per day.

If treatment is interrupted for more than 2 weeks, then its renewal begins with a dose of 3.125 mg 2 times a day, with a subsequent increase in dose.

Side effects

From the side of the central nervous system: headache, dizziness, syncopal states, muscular weakness (usually at the beginning of treatment), sleep disturbance, depression, paresthesias.

Since the cardiovascular system: bradycardia, orthostatic hypotension, angina pectoris, atrioventricular block, rarely “intermittent” claudication, violation

peripheral circulation, progression of heart failure.

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

From the side of blood-forming organs: thrombocytopenia, leukopenia.

From the urinary system: severe renal dysfunction, edema.

Allergic reactions: allergic skin reactions (rash, urticaria, pruritus, rash), exacerbation of psoriatic rash, sneezing, nasal congestion, bronchospasm, shortness of breath (in susceptible patients).

Other: flu-like syndrome, pain in the limbs, decreased tearing, weight gain.

Drug interaction

Carvedilol can potentiate the action of other concurrently taking antihypertensive drugs or drugs that have a hypotensive effect (nitrates).
When carvedilol and diltiazem are used together, cardiac conduction and hemodynamic disturbances may develop.
With simultaneous use of carvedilol and Digoxin , the concentration of the latter increases and the time of atrioventricular conduction may increase.
Carvedilol may potentiate the effects of insulin and oral hypoglycemic agents, and the symptoms of hypoglycemia (especially tachycardia) may be masked, so regular control of blood sugar levels is recommended for diabetics.

With the simultaneous use of cyclosporine, the concentration of the latter increases (correction of the daily dose of cyclosporine is recommended).
Simultaneous administration of clonidine can potentiate the antihypertensive and cardiovascular effects of carvedilol.
General anesthetics enhance the negative inotropic and hypotensive effect of carvedilol.

Overdose

Symptoms: reduction in blood pressure (accompanied by dizziness or fainting), bradycardia. Dyspnea due to bronchospasm and vomiting may occur. In severe cases, cardiogenic shock, respiratory failure, confusion, conduction disturbances are possible.
Treatment: it is necessary to monitor and correct vital indicators, if necessary - in the intensive care unit. Treatment is symptomatic. It is advisable intravenous administration of m-cholinoblockers (atropine), adrenomimetics (epinephrine, norepinephrine).

Store in a dry, dark place at a temperature not exceeding 25 ° C.