Carvedilol is rapidly and almost completely absorbed after oral administration of the gastrointestinal tract. It is almost completely bound to plasma proteins (98-99%). Plasma concentration is proportional to the dose. The bioavailability of approximately 25% due to the high degree of metabolism in the liver. Thus produced metabolites, having a high ability to block beta-adrenoceptors.
Maximum plasma concentration halotestin for sale is achieved after 1 hour. The half-life – 6-10 hours.
Older patients carvedilol plasma concentration of about 50% higher than in younger patients. It is shown mainly in the bile. Patients with hepatic impairment may increase the bioavailability of up to 80%. It penetrates through the placental barrier, excreted in breast milk. Food slows the absorption of the drug, but does not affect its bioavailability.
– Arterial hypertension. It may be used alone or in combination with other antihypertensive agents.
– Stable angina.
– Chronic heart failure (in combination therapy).
Hypersensitivity to carvedilol or other components of the formulation, severe hepatic insufficiency, severe bradycardia (less than 50 u. / Min.), Sick sinus syndrome, II and III degree AV block (except in patients with artificial pacemaker), chronic heart failure the stage of decompensation, acute heart failure, cardiogenic shock, hypotension (systolic blood pressure less than 85 mmHg), pregnancy and lactation, age 18 years (effectiveness and safety have been established).
Precautions: angina Prinzmetal, thyrotoxicosis, peripheral vascular occlusive disease, pheochromocytoma, psoriasis, renal failure, atrioventricular block I degree, extensive surgery and general anesthesia, diabetes, hypoglycemia, depression, myasthenia gravis.
Dosing and Administration
Inside, regardless of meals.
Be sure to follow your doctor’s instructions. Without prior consultation with your doctor you should not stop treatment with carvedilol or change the dosage. If necessary, discontinuation of the drug, the dose reduction should take place gradually over a 1 -. 2 weeks
if there is no therapeutic effect on the treatment or marked deterioration, consult your doctor.
The dose is adjusted individually. The first 7-14 days, the recommended dose of carvedilol 12.5 mg (1 tablet of 12.5 mg), taken in the morning after breakfast. The dose may be divided into two stages 6, 25 mg Carvedilol (1/2 tablet 12.5 mg). Further Carvedilol treatment should be 25 mg (1 tablet of 25 mg) in the morning or divided into two doses 12.5 mg (1 tablet of 12.5 mg). If necessary, after 14 days the doctor may increase the dose again.
Take the drug after eating a small amount of liquid.
Stable angina . The starting dose of 12.5 mg carvedilol (1 tablet 12.5 mg) twice a day. After 7-14 days under the supervision of a physician carvedilol dose can be increased to 25 mg (1 tablet of 25 mg) twice a day. After 14 days in case of insufficient efficacy and good tolerability of carvedilol dose may be further increased.
The total daily dose carvedilol angina should not exceed 50 mg (2 tablets of 25 mg) designated by 2 times per day. If your age exceeds 70 years, the daily dose of carvedilol should not exceed 25 mg (1 tablet of 25 mg) twice a day.
If you miss a regular dose, then you should take the medication as soon as possible.
However, if you are already nearing time for your next dose, then you should only take it without doubling it.
you have to take the drug regularly. If you do not take the drug for more than 2 weeks, it is necessary to renew the treatment with the lowest dose.
Chronic heart failure. Dose picked individually, under the close supervision of a physician. The recommended starting dose is 3.125 mg 2 times a day for 2 weeks. With good tolerance dose increased at intervals of at least 2 weeks to 6.25 mg 2 times a day, then 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 weighing less than 85 kg target dose is 50 mg per day; in patients weighing more than 85 kg target dose of 75-100 mg per day.
If the treatment is interrupted for more than 2 weeks, then resuming its begin with a dose of 3.125 mg two halotestin for sale times a day, followed by increasing doses.
On the part of the central nervous system: headache, dizziness, syncope, muscle weakness (most often at the beginning of treatment), sleep disturbances, depression, paresthesia.
Since the cardiovascular system: bradycardia, orthostatic hypotension, angina pectoris, atrioventricular block, rare “intermittent” claudication, violation
peripheral circulation, the 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 hematopoiesis: thrombocytopenia, leukopenia.
From the urinary system: severe renal dysfunction, edema.
Allergic reactions: allergic skin reactions (rash, hives, itching, rash), exacerbation of psoriasis rash, sneezing, nasal congestion, bronchospasm, dyspnea (in predisposed patients).
Other: flu-like symptoms, pain in extremities, decrease in lacrimation, increased body mass index.
Interaction with other drugs
Carvedilol should not be given to patients receiving intravenous verapamil or diltiazem, as this can lead to a marked slowing heart rate and a significant decrease in blood pressure.
Some antiarrhythmic drugs, drugs for general anesthesia, antihypertensive drugs, drugs for the treatment of angina, other beta-blockers (eg eye drops), monoamine oxidase inhibitors, sympatholytic (reserpine), and cardiac glycosides can increase the effect of carvedilol. Therefore, care must be taken when selecting doses of these medicines and carvedilol. Simultaneous administration may lead to an increase in the concentration of digoxin in plasma.
The pharmacokinetics of carvedilol may be changed while the appointment with drugs that stimulate or block the activity of liver enzymes (CYP2D6): eg, cimetidine increases the concentration in the blood serum carvedilol and rifampicin, phenobarbital reduces it.
Concurrent use with ergot alkaloids impairs peripheral circulation.
If you cancel the simultaneous treatment with carvedilol and clonidine, you first need to stop treatment with carvedilol, and only a few days later to cancel clonidine.
Carvedilol may potentiate the effect of hypoglycemic drugs and mask the symptoms of hypoglycaemia. It is therefore recommended to regularly monitor blood glucose levels.
Symptoms: severe hypotension, bradycardia, disturbance of respiratory function (including bronchoconstriction), heart failure, cardiogenic shock, cardiac arrest.
Remedy: If the patient is conscious, it is necessary to induce vomiting to empty the stomach and put the patient on his back so that his head was lowered, and the leg slightly raised. The patient is unconscious should be laid on its side. Immediately consult a doctor, so he has taken steps to remove nevsosavsheysya the drug and the patient’s hospitalization.
Treatment – symptomatic and with the use of adrenergic agonists.
Be wary of bronchospastic syndrome, chronic bronchitis, emphysema, Prinzmetal angina, diabetes or hypoglycemia, thyrotoxicosis, peripheral vascular disease, pheochromocytoma, depression, myasthenia gravis, psoriasis, renal failure.
The drug is not recommended for patients with low blood pressure.
At the beginning of treatment with carvedilol and with increasing doses of the drug in patients may experience excessive reduction in blood pressure, especially when standing up. There may be dizziness, and sometimes syncope, especially in elderly patients with heart failure or concomitant treatment with other agents or diuretics antigiperteizivnymi.
Carvedilol treatment should not cease abruptly, especially in patients with angina, as this can lead to deterioration. Reducing the dose should be gradually within 1 – 2 weeks.
It is recommended to monitor renal function in patients with renal failure, coronary artery disease, diffuse halotestin for sale peripheral vascular disease,
arterial hypertension and / or heart failure.
With the deterioration of renal function, carvedilol should be abolished.
Beta-blockers may burden the clinical picture of peripheral arterial angiopathy, psoriasis and anaphylactic reactions, as well as to reduce the sensitivity of the allergy tests.
Beta-blockers may aggravate the course of Prinzmetal angina (provoke the appearance of pain).
Since beta-blockers slow the heart rate, they may mask priznakigiperglikemii in patients with diabetes mellitus and hyperthyroidism in patients with thyroid disease. In patients with diabetes mellitus and heart failure in the blood glucose level may increase or decrease.
Before surgery you should inform the doctor that you are taking Carvedilol. Care should be taken during general anesthesia with the use of drugs that suppress the activity of the heart muscle (such as ether, cyclopropane, trichlorethylene). Before major surgery recommended the phasing out of carvedilol.
Caution should be exercised when using the drug in case of pronounced metabolic acidosis.
Patients with pheochromocytoma be administered beta-adrenoceptor blockers only if they had previously started taking alpha-blockers.
Safety and efficacy of carvedilol in children under 18 years of age has not been established.
Caution should be exercised when using the drug in patients using contact lenses (decrease lacrimation).
During treatment excludes alcohol.
Effects on ability to drive and use other mechanisms
Especially at the beginning of treatment with increasing doses and arterial pressure carvedilol may decrease excessively, causing dizziness. Patients are advised not to drive and therefore should refrain from other activities related to the necessity of high concentration and rapid psychomotor reactions.
Tablets of 12.5 mg and 25 mg. 10 or 30 tablets in blisters. 3 blisters of 10 tablets or 1 blisters of 30 tablets with the instructions for use of the drug in a carton box.
List B. Store in a dry, dark place at a temperature not exceeding 25 ° C. Store in a place inaccessible to children.
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