Following oral administration, carvedilol is rapidly absorbed from the gastrointestinal tract. It is metabolized in the “first” pass through the liver, its bioavailability is about 25%. The maximum plasma concentration is reached about 1 hour after ingestion of the drug. The pharmacokinetics of carvedilol is linear (plasma concentrations proportional to the dose). Concomitant food has no effect on the bioavailability of carvedilol and its maximum concentration in plasma, but may increase the time to maximum blood concentration.
What is tren is a lipophilic compound, its binding to plasma proteins reaches 98-99%. The apparent volume of distribution is approximately 2 l / kg and is largely increased by cirrhosis of the liver. Metabolism of Carvedilol is metabolized primarily in the liver, primarily due to the formation of glucuronides. Demethylation and hydroxylation of the phenyl ring results in the formation of active metabolites with three beta adrenoblokiruyuschey activity. 4-hydroxy metabolite, beta-blocker, is 13 times more active carvedilol. At the same time, active metabolites are weaker vasodilator and two gidroksikarbazolovyh more metabolite are strong antioxidants compared to the parent compound. The average half-life of carvedilol – 6-10 hours and plasma clearance Carvedilol is released mainly in the bile. Carvedilol and its metabolites can cross the placenta and are excreted in the mother’s milk. Carvedilol is practically not removed from blood by hemodialysis. Specific categories of patients Elderly patients : The concentration of carvedilol in plasma in elderly patients is 50% higher than in the young. Patients with renal impairment : Since carvedilol is derived mainly what is tren through the gastrointestinal tract, impairment of renal function is not accompanied by his cumulation. Patients with liver disease : in liver cirrhosis the bioavailability of carvedilol in 4 times, and the maximum plasma concentration – 5 times higher than normal.
- essential hypertension – either alone or in combination with a diuretic
- stable angina
- Chronic heart failure *, in combination with a diuretic, digoxin or angiotensin converting enzyme inhibitors
- Hypersensitivity to the drug
- Heart failure in decompensation stage
- conduction disorders (sick sinus syndrome, sinoatrial block, atrioventricular block degree II-III), except for patients with artificial pacemaker
- Severe bradycardia (heart rate less than 50 beats per minute)
- Arterial hypotension (systolic blood pressure less than 85 mmHg)
- Cardiogenic shock
- Bronchial asthma
- Severe hepatic dysfunction
- Metabolic acidosis what is tren
- Children under the age of 18 years (due to lack of clinical application experience)
- Sharing intravenous verapamil, diltiazem or other antiarrhythmics (especially antiarrhythmics class I) (see. Also “Interactions”).
Precautions : (see also special instructions)
- Chronic obstructive pulmonary disease;
- Prinzmetal angina;
- Hypoglycemia, hyperthyroidism;
- Pheochromocytoma (only stabilized the appointment of alpha-blockers)
- Occlusive peripheral vascular disease;
- Atrioventricular block of I degree;
- Unstable angina;
- Impaired renal function;
- Myasthenia gravis;
- In the treatment of α 1 adrenoblokatorami or α 2 -adrenomimetikami;
- The combined use of what is treninhibitors .