Carvedilol Verte pills 25mg N30
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Active ingredients
Carvedilol
Release form
Pills
Composition
Carvedilol 25 mg adjuvants: microcrystalline cellulose, lactose (milk sugar), crospovidone (plasdon xl10), sodium fumarate.
Pharmacological effect
Carvedilol has a combined non-selective β 1 -, β2 - and α1-adrenergic blocking action. The drug does not have its own sympathomimetic activity, has membrane stabilizing properties. Due to the blockade of the β-adrenoreceptors of the heart, the blood pressure, cardiac output and heart rate may decrease. Carvedilol inhibits the renin-angiotensin-aldosterone system by blocking the β-adrenoreceptors of the kidneys, causing a decrease in plasma renin activity. By blocking α-adrenoreceptors, the drug can cause expansion of peripheral vessels, thereby reducing systemic vascular resistance. The combination of β-adrenoreceptor blockade and vasodilation has the following effects: in patients with arterial hypertension, a decrease in blood pressure; in patients with coronary artery disease - antiischemic and antianginal effect; in patients with left ventricular dysfunction and circulatory failure - a positive effect on hemodynamic parameters, increases the ejection fraction of the left ventricle and reduces its size.
Pharmacokinetics
Carvedilol is rapidly absorbed from the digestive tract. It has high lipophilicity. Cmax in blood is achieved in 1-1.5 hours. T1 / 2 is 6-10 hours. It binds to plasma proteins in 95-99%. Bioavailability of the drug - 24-28%. Food intake 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 during the first "passage" through the liver. Metabolites have a pronounced antioxidant and adrenergic blocking effect. Removal of the drug from the body occurs through the gastrointestinal tract. In case of impaired renal function, the pharmacokinetic parameters of carvedilol do not change significantly. In patients with impaired liver function, the systemic bioavailability of carvedilol is increased by reducing metabolism during the first "passage" through the liver. In case of serious violations of the liver, carvedilol is contraindicated. Carvedilol penetrates the placental barrier, is excreted in breast milk.
Indications
- Arterial hypertension (in monotherapy and combination with diuretics); - Chonic heart failure (as part of combination therapy); - IHD: stable angina.
Contraindications
- acute and decompensated chronic heart failure, requiring IV administration of inotropic drugs; - severe hepatic failure; - AV-II-III stage III-blockade; - severe bradycardia (less than 50 beats / min); - sinus node weakness syndrome; - arterial hypotension (systolic blood pressure less than 85 mmHg.); - cardiogenic shock; - bronchial asthma; - chronic obstructive pulmonary disease; - age up to 18 years (efficacy and safety not established); - hypersensitivity to carvedilol or other components of the drug With caution w: bronchospastic syndrome, chronic bronchitis, emphysema, Prinzmetal angina, thyrotoxicosis, occlusive peripheral vascular disease, pheochromocytoma, psoriasis, renal failure, AV-block I degree, extensive surgery and general anesthesia, diabetes mellitus, hypoglycaemia, depression, myasthenia gravis.
Precautionary measures
During treatment, psoriasis may worsen. During pheochromocytoma, propranolol can only be used after taking an alpha blocker. After a long course of treatment, propranolol should be discontinued gradually, under the supervision of a physician. during anesthesia, you must stop taking propranolol or find a remedy for anesthesia with minimal negative inotropic effects. The impact on the ability to drive vehicles and control mechanisms of patients whose activities require increased attention, the question of the use of propranolol on an outpatient basis should be addressed only after evaluating the individual response of the patient.
Use during pregnancy and lactation
Controlled studies of the use of carvedilol in pregnant women have not been conducted, therefore, prescribing this category of patients is possible only in cases where the benefit to the mother outweighs the potential risk to the fetus. Breastfeeding is not recommended during treatment with carvedilol.
Dosage and administration
Inside, regardless of the meal. To ensure the following dosing regimen, you can use the drug Carvedilol in the dosage form of a tablet of 6.25 mg. Arterial hypertension. The initial dose is 6.25-12.5 mg 1 time / day during the first two days of treatment. Then - 25 mg 1 time / day. In case of insufficiency of the antihypertensive effect after 2 weeks of therapy, the dose can be increased by 2 times. The maximum recommended dose of the drug is 50 mg 1 time / day (possibly divided into 2 doses). Coronary heart disease Initial dose is 12.5 mg 2 times / day during the first two days of treatment. Then - 25 mg 2 times / day. If the antianginal effect is insufficient, after 2 weeks of therapy, the dose can be increased by 2 times. The maximum recommended daily dose of the drug is 100 mg divided into 2 doses. Chronic heart failure. The dose is selected individually, under the close supervision of a physician. 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 patients. In patients with a body weight 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 effects
On the part of the central nervous system: dizziness, headache (usually not severe and at the beginning of treatment), loss of consciousness, myasthenia (more often at the beginning of treatment), fatigue, depression, sleep disturbance, paresthesia. On the part of the cardiovascular system: bradycardia , orthostatic hypotension, AV-blockade II - III stage, rarely - impaired peripheral circulation, progression of heart failure (in the period of increasing doses), lower limb edema, angina pectoris, marked reduction in blood pressure. From the digestive system we: dry mouth, nausea, diarrhea or constipation, vomiting, abdominal pain, loss of appetite, increased activity of "liver" transaminases. From the hematopoietic system: rarely - thrombocytopenia, leukopenia. From the side of metabolism: weight gain, violation of carbohydrate metabolism. Allergic reactions: skin allergic reactions, exacerbation of psoriasis, nasal congestion. On the respiratory system: dyspnea and bronchospasm (in susceptible patients). Others: blurred vision, decreased tearing, flu-like syndrome, sneezing, ialgiya,arthralgia, pain in the limbs, intermittent claudication; rarely - urination disorders, renal dysfunction.
Overdose
Symptoms: decrease 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 signs, and if necessary, in the intensive care unit. Treatment is symptomatic. It is advisable intravenous administration of m-cholinoblockers (atropine), adrenomimetics (epinephrine, norepinephrine).
Interaction with other drugs
Carvedilol can potentiate the action of other concurrently taking antihypertensive drugs or drugs that have a hypotensive effect (nitrates). When combined with carvedilol and diltiazem, cardiac conduction disturbances and hemodynamic disturbances can occur. Carvedilol may potentiate the action of insulin and oral hypoglycemic agents, with this symptoms of hypoglycemia (especially tachycardia) can be masked, therefore, in patients with diabetes mellitus, regular monitoring of blood sugar levels is recommended. Microsomal oxidation inhibitors (cimetidine) increase, and inductors (phenobarbital, rifampicin) weaken the hypotensive effect of carvedilol. Preparations reducing catechol amines , monoamine oxidase inhibitors), increase the risk of arterial hypotension and severe bradycardia. With simultaneous use of cyclosporine, the concentration increases and the latter (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.
special instructions
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, lowering the dose 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, there may be an excessive decrease in blood pressure, mainly when getting 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. It should not increase the dose of carvedilol, recommended the appointment of large doses of diuretics until the patient's state is stabilized. Continuous monitoring of the electrocardiogram and blood pressure is recommended, while carvedilol and slow calcium channel blockers derived from phenylalkylamine (verapamil) and benzodiazepine (diltiazem) and benzodiazepine (diltiazem) blockers derived from phenylalkylamine (verapamil) and benzodiazepine (diltiazem) are recommended. with class I antiarrhythmic drugs. It is recommended to control renal function in patients with chronic renal failure, arteries In case of surgery using general anesthesia, the anesthesiologist should be warned about prior carvedilol therapy. Carvedilol does not affect blood glucose concentration and does not cause changes in glucose tolerance test indicators in patients with insulin-dependent diabetes mellitus. avoid ethanol use. Patients with pheochromocytoma should be given alpha-blockers before therapy. Patients wearing contact lenses, it should be borne in mind that the drug may cause a decrease in tearing. Influence on the ability to drive vehicles and control mechanisms. It is not recommended to drive a car at the beginning of therapy and with an increase in the dose of carvedilol. It should refrain from other activities related to the need for high concentration of attention and quick psychomotor reactions.