2010/12/12

Atram

Release form, composition and packing

Tablets brownish-yellow, interspersed with, the risk of division on one side and engraved with the figure "12" - to another.

1 tab. carvedilol 12.5 mg

Excipients: sucrose, povidone 30, lactose monohydrate 200, colloidal anhydrous silica, sodium croscarmellose, magnesium stearate, iron oxide yellow, iron oxide red.

Tablets brownish-yellow, interspersed with, the risk of division on one side and engraved with the figure "25" - on the other.

1 tab. Carvedilol 25 mg

Excipients: sucrose, povidone 30, lactose monohydrate 200, colloidal anhydrous silica, sodium croscarmellose, magnesium stearate, iron oxide yellow, iron oxide red.

Pill yellow, interspersed with, the risk of dividing on one side and engraved with the figure "6" - on the other.

1 tab. Carvedilol 6.25 mg

Excipients: sucrose, povidone 30, lactose monohydrate 200, colloidal anhydrous silica, sodium croscarmellose, magnesium stearate, iron oxide yellow.

Clinico-pharmacological group

Beta1-, beta2-blocker. Alpha 1-blocker.

Pharmacological action

Carvedilol has a combined non-selective β1-β2-and α1-blocking action. The drug has its own sympathomimetic activity, has membrane stabilizing properties. Due to the blockade of β-adrenergic receptors of the heart may decrease blood pressure, cardiac output and slowed heart rate, carvedilol inhibits the renin-angiotensin-aldosterone system blockade by β-adrenergic receptors of kidneys, causing a decrease in plasma renin activity. Blocking α-adrenergic receptors, the drug can cause increased peripheral vascular disease, thereby reducing systemic vascular resistance.

The combination of β-adrenoceptor blockade and vasodilatation has the following effects: patients with arterial hypertension - blood pressure reduction, in patients with coronary artery disease - antiischemic and antianginal, in patients with left ventricular dysfunction and circulatory failure - beneficial effect on hemodynamic parameters, improves left ventricular ejection fraction and reduces its size.

Pharmacokinetics

Carvedilol is rapidly absorbed from the gastrointestinal tract. Has a high lipophilicity. Cmaxv blood is achieved by 1-1.5 h. T1 / 2 is 6-10 am bound to plasma proteins in the blood of 95-99%. Bioavailability - 24-28%. Food intake did not affect the bioavailability.

Metabolized in the liver to form several active metabolites. 60-75% of the adsorbed drug is metabolized during first passage through the liver. Metabolites have antioxidant and adrenoblokiruyuschee action.

Withdrawal from the body occurs through the gastrointestinal tract. Carvedilol crosses the placental barrier, excreted in breast milk.

If the kidney function pharmacokinetic parameters of carvedilol does not significantly change.

In patients with impaired liver function a systemic bioavailability of carvedilol is increased by reducing the metabolism of the first passage through the liver. When serious liver Carvedilol is contraindicated.

Indications for use of the drug
hypertension (as monotherapy and combination with a diuretic);
Chronic heart failure (as part of combination therapy);
Coronary heart disease;
stable angina.

Dosing regimen

Inside, regardless of the meal.

Arterial hypertension

The initial dose of 6.25-12.5 mg 1 time in the first 2 days of treatment. Then - 25 mg 1 time / When failure of antihypertensive effect after 2 weeks of therapy, the dose may be increased by a factor of 2. The maximum recommended daily dose is 50 mg 1 time (possibly divided into 2 doses).

Coronary artery disease

The initial dose of 12.5 mg of 2 in the first 2 days of treatment. Then - 25 mg of 2 When failure antianginal effect after 2 weeks of therapy, the dose may be increased by a factor of 2. The maximum recommended daily dose is 100 mg divided into 2 doses.

Chronic heart failure

Dose choose individually, under the close supervision of a physician. The recommended starting dose is 3.125 mg, 2 for 2 weeks. Good tolerability of dose increased at intervals of not less than 2 weeks to 6.25 mg of 2, then - up to 12.5 mg of 2, then - up to 25 mg of 2 dose should be increased to the maximum, which is well tolerated by patients. In patients weighing less than 85 kg target dose is 50 mg, in patients weighing over 85 kg target dose - 75-100 mg /

Side effect
CNS and peripheral nervous system: dizziness, headache (usually not severe and early treatment), loss of consciousness, myasthenia gravis (usually at the beginning of treatment), fatigue, depression, sleep disturbance, paresthesia.
Cardio-vascular system: bradycardia, orthostatic hypotension, AV-block ll-III degree, rarely - a violation of the peripheral circulation, the progression of heart failure (in the period increased doses), edema of the lower extremities, angina, marked reduction in blood pressure.
From the digestive system: dry mouth, nausea, diarrhea or constipation, vomiting, abdominal pain, anorexia, elevation of liver transaminases.
From the hematopoietic system: rarely - thrombocytopenia, leukopenia.
From a metabolism: weight gain, impaired carbohydrate metabolism.

Allergic reactions: allergic skin reactions, exacerbation of psoriasis, a stuffy nose.
With the respiratory system: dyspnea, and bronchospasm (in predisposed patients).

Other: blurred vision, reduced tearing, influenza-like syndrome, sneezing, myalgia, arthralgia, pain in the limbs, intermittent claudication, rarely - a violation of urination, impaired renal function.

Contraindications to the use of the drug
acute and chronic heart failure (in the decompensation stage);
severe hepatic impairment;
AV-block ll-lll degree;
marked bradycardia (less than 50 beats / min);
sick sinus syndrome;
hypotension (systolic blood pressure <85 mmHg. cent.);
cardiogenic shock;
chronic obstructive pulmonary disease;
age of 18 years (the efficacy and safety have not been established);
Hypersensitivity to carvedilol or other ingredients.

Precautions: Prinzmetal angina, thyrotoxicosis, peripheral vascular occlusive disease, pheochromocytoma, psoriasis, kidney failure, AV-block I degree, extensive surgery and general anesthesia, diabetes, hypoglycemia, depression, myasthenia gravis.

Pregnancy and lactation

Controlled trial of carvedilol in pregnant women has been conducted, so the drug in such patients is only possible in cases where the benefits to the mother outweighs the potential risk to the fetus.

Not recommended for breast-feeding during treatment with carvedilol.

Use in hepatic dysfunction

Contraindications: severe hepatic impairment.

Use in renal impairment

Precautions: renal impairment.

Cautions

Therapy should be prolonged and should not be abruptly stopped, especially in patients with CHD, as this may lead to a worsening of the underlying disease. If necessary, reduction in dose should be gradual, over 1-2 weeks.

At the beginning of carvedilol therapy, or at higher doses in patients, especially elderly, may show excessive BP reduction, mainly on rising. Necessary correction doses. In patients with chronic heart failure in the selection of the dose may increase the symptoms of heart failure, the appearance of edema. One should not increase the dose Atrama, recommended the appointment of high doses of diuretics until the stabilization of the patient.

Recommended constant monitoring of ECG and blood pressure while appointing Atrama and slow calcium channel blockers, derivatives fenilalkilamina (verapamil) and benzodiazepines (diltiazem), as well - with class I antiarrhythmics.

Recommended to monitor renal function in patients with chronic renal failure, hypotension and congestive heart failure. In the case of surgery using general anesthesia, the anesthesiologist should be warned about previous treatment with carvedilol.

Atram not affect the concentration of glucose in the blood and causes no changes in indicators glucose tolerance test in patients with insulin-dependent diabetes mellitus.

During treatment avoid using ethanol.