Carvedilol pills 12.5 mg 30 pcs
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Active ingredients
Carvedilol
Release form
Pills
Composition
Carvedilol 12.5 mg adjuvants: sugar (sucrose), magnesium stearate, potato starch, hydroxypropylmethylcellulose (hypromellose), croscarmellose sodium (primelloza), colloidal silicon dioxide (aerosil), calcium phosphate.
Pharmacological effect
Alpha and beta blocker. Carvedilol has a combined non-selective beta1-, beta2- and alpha1-blocking action. The drug does not have its own sympathomimetic activity, has membrane stabilizing properties. Due to the blockade of β-adrenoreceptors of the heart, there is a decrease in blood pressure, a decrease in cardiac output and heart rate. Carvedilol inhibits RAAS by blocking the β-adrenergic receptors 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%. Meal does not affect bioavailability. Metabolized in the liver to form 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 adrenoblokiruyuschim action. Removal of the drug from the body occurs through the digestive tract. Carvedilol penetrates the placental barrier, is excreted in breast milk. 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 liver function, carvedilol is contraindicated.
Indications
- arterial hypertension (as monotherapy and combination with diuretics); - chronic heart failure (as part of combination therapy); - IHD: stable angina.
Contraindications
- hypersensitivity to carvedilol or other components of the drug; - acute and chronic heart failure (in the decompensation stage); - severe liver failure; - AV-II-III degree blockade; - severe bradycardia (less than 50 beats / min); - SSS - arterial hypotension (systolic blood pressure less than 85 mmHg); - cardiogenic shock; - COPD; - children and adolescents under 18 years of age (efficacy and safety not established). With caution: Prinzmetal angina, thyrotoxicosis, occlusive peripheral diseases vessels, feo chromocytoma, psoriasis, renal failure, AV block I degree, extensive surgical intervention and general anesthesia, diabetes, hypoglycemia, depression, myasthenia.
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. Arterial hypertensionThe initial dose is 6.25–12.5 mg 1 time / day during the first 2 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 daily dose of the drug is 50 mg 1 time / day (possibly divided into 2 doses). The initial dose is 12.5 mg 2 times / day during the first 2 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 / day, divided into 2 doses. Chronic heart failure. The dose is selected individually, under close medical supervision. 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 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 disturbances, paresthesia. orthostatic hypotension, AV-blockade of grade II-III, rarely - impaired peripheral circulation, progression of heart failure (during the period of increasing doses), edema of the lower extremities, angina pectoris, marked decrease in blood pressure. From the digestive system: dry be in the mouth, nausea, diarrhea or constipation, vomiting, abdominal pain, loss of appetite, increased activity of hepatic transaminases. From the hematopoietic system: rarely - thrombocytopenia, leukopenia. : allergic skin reactions, nasal obstruction ralgiya, pain in the extremities, intermittent claudication, rarely - a violation of urination, impairment of renal function.
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, if necessary - in ICU. Treatment is symptomatic. It is advisable to / in the use of m-cholinoblockers (atropine), adrenomimetics (epinephrine, norepinephrine).
Interaction with other drugs
Carvedilol can potentiate the action of other concurrent antihypertensive drugs or drugs that have a hypotensive effect (nitrates). When combined with carvedilol and diltiazem, cardiac conduction disturbances and hemodynamic disturbances can develop. If you take carvedilol and digoxin at the same time, the concentration of the latter can increase and AV-time can increase. Carvedilol can potentiate the action of insulin and oral hypoglycemic agents, with the symptoms of hypoglycemic Kemias (especially tachycardia) can be masked, therefore, patients with diabetes mellitus recommend regular monitoring of blood glucose levels. Inhibitors of microsomal oxidation (cimetidine) increase, and inductors (phenobarbital, rifampicin) weaken the hypotensive effect of carvedilola. MAO), increase the risk of hypotension and severe bradycardia. With simultaneous use of cyclosporine, the concentration of the latter increases (it is recommended tion daily dose cyclosporine) .Odnovremenny clonidine intake may potentiate antihypertensive and heart rate slows effects karvedilola.Obschie 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 IHD patients, because 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 therapy with Carvedilol-OBL or with an increase in the dose of the drug in patients, especially the elderly, an excessive decrease in blood pressure may be noted, 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. At the same time, one should not increase the dose of Carvedilol-OBL, it is recommended to administer large doses of diuretics until the patient's condition stabilizes. Constant monitoring of ECG and blood pressure is recommended while coadministration of Carvedilol-OBL and slow calcium channel blockers derived from phenylalkylamine (verapamil) and benzothiazepine (diltiaze) is obtained. ), as well as with class I antiarrhythmic drugs. It is recommended to control 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 previous therapy with Carvedilol-OBL. Carvedilol-OBL does not affect the concentration of glucose in the blood and does not cause changes in glucose tolerance test indicators in patients with insulin-dependent diabetes mellitus. use of ethanol. Patients with pheochromocytoma should be given alpha-blockers before therapy. Patients wearing contact lenses should take into account That the drug may cause a decrease slezootdeleniya.Vliyanie the ability to drive and control mehanizmamiNe recommended to drive at the beginning of therapy and with increasing doses of the drug carvedilol-OBL. It should refrain from other activities related to the need for high concentration of attention and quick psychomotor reactions.