Karvedilol

When ATH:
C07AG02

Characteristic.

Non-selective beta alpha1-blocking activity. Razemicescuu is a mixture of two enantiomers, which beta1– and beta2-blocking activity characterized by S(-)-jenantiomeru, and alpha1-blocking-R(+) и S(-)-jenantiomeram equally.

White or almost white crystalline powder. Easily soluble in DMSO, soluble in metilenhloride and methanol, It is soluble in 95% ethanol and isopropanol, slightly soluble in ethyl ether, practically insoluble in water. Molecular weight 406,5.

Pharmacological action.
Antianginalnoe, gipotenzivnoe, antioksidantnoe, vazodilatirtee.

Application.

Arterial hypertension, CHD (stable angina), congestive heart failure (in a combination therapy).

Contraindications.

Hypersensitivity, hypotension (Sad less than 85 mm Hg. Art.), decompensated heart failure (IV NYHA functional class), requiring inotropes assignment, vasodilators, diuretics); vыrazhennaya bradycardia, AV блокада II–III степени, sinoatrialynaya blockade, sick sinus syndrome, cardiogenic shock, chronic obstructive pulmonary disease with bronhospasticheskim component, bronchial asthma (two fatal outcomes were reported as a result of the development of status asthmaticus after taking a single dose of carvedilol), severe liver injury.

Restrictions apply.

Stenocardia Prinzmetala, the recent deteriorating course of heart failure, Peripheral Vascular Disease (Raynaud's syndrome, intermittent claudication), diabetes, gipoglikemiâ, pheochromocytoma, hyperthyroidism, general anesthesia, psoriasis, impairment of renal function, advanced age, Children and Youth age (to 18 years).

Pregnancy and breast-feeding.

When pregnancy is possible, if the effect of therapy outweighs the potential risk to the fetus (adequate and well-controlled studies in humans have not held).

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

At the time of treatment should abandon breastfeeding (unknown, whether the carvedilol in breast milk in humans).

Side effects.

From the nervous system and sensory organs: dizziness, headache, asthenia, syncope (rare and, usually, only at the beginning of treatment), muscular weakness (more often at the beginning of treatment), sleep disorders, depression, paraesthesia, xerophthalmia, lowering no tear.

Cardio-vascular system and blood (hematopoiesis, hemostasis): bradycardia, AV conduction disorders, postural hypotension, chest pain, angina, deterioration of peripheral blood circulation, progression of heart failure, exacerbation of Raynaud's syndrome symptoms, edematous syndrome, thrombocytopenia, leukopenia, increased bleeding and bruising education.

From the digestive tract: dry mouth, nausea, vomiting, abdominal pain, diarrhea, constipation, elevated transaminase levels in the blood.

From the respiratory system: nasal congestion, chikhaniye, breathlessness (prone patients), bronhospasticskie reaction.

With the genitourinary system: violation of urination, hematuria, acute renal failure.

Allergic reactions: skin rashes, incl. an allergic rash, hives, itch.

Other: swelling and pain in the limbs, weight gain, giperglikemiâ, giperʙiliruʙinemija, hypercholesterolemia, flu-like symptoms, exacerbation of psoriasis symptoms.

Cooperation.

Potenziruet the other antigipertenziveh funds or HP, providing gipotenzivny effect as side effects. Preparations of beta blocking properties can strengthen gipoglikemicescoe effect of insulin and oral gipoglikemicakih HP, When the symptoms of hypoglycemia (especially the tachycardia) can camouflage (It is recommended that regular monitoring of blood glucose levels). When applied in conjunction with cardiac glycosides, dioretikami and/or ACE inhibitors may slow AV conduction. Increases the content of Digoxin in serum. General anesthetics (R22, diethyl ether, trichlorethylene) reinforce negative inotropy and hypotensive effects of carvedilol. Phenobarbital, rifampicin and other tools, inhibiting mikrosomaiona enzymes, accelerate metabolism and reduce concentration in plasma. Diuretics and ACE inhibitors potenziruut hypotension. The caution should be used with antiarrhythmic medicines and BAC, especially with distiazemom and verapamil (is not compatible with the/in the introduction of calcium antagonists).

Overdose.

Symptoms: severe hypotension (USA 80 mm Hg. Article. and lower), bradycardia (less 50 u. / min), heart failure, cardiogenic shock, cardiac arrest, respiratory function, bronchospasm, vomiting, confusion, generalized seizures.

Treatment: When finding a patient is in the minds of, you need to give it a horizontal position with pripodnatami feet (the patient is unconscious should be stowed on the side), during the first hours — to take measures to remove the drug from the blood (reception/vomiting gastric lavage). Overdose requires intensive treatment. Beta-antagonist adrenoblokirujushhego orciprenaline isoprenaline or is 0.5-1 mg in/in and/or glucagon in a dose of 1-5 mg (the maximum dose - 10 mg). With the development of bradycardia and other vascular complications need atropine (for 0.5-2 mg in/in), While resistant to the treatment of bradycardia demonstrates the use of artificial driver rhythm; to maintain cardiovascular activity — dobutamine, epinephrine, glucagon (on 1-10 mg in/in struino, then on 2-5 mg/h in the form of infusions); in bronhospazme-beta-sympathomimetics in the form of aerosol (with inefficiency —/in) or aminophylline (I /); in the case of seizures is diazepam, clonazepam. Monitoring and correction of the vital indicators recommended in ICU.

Dosing and Administration.

Inside. When hypertension is 25-50 mg 1 once a day (initial dose for the first 2 the day can be 12,5 mg), When strokes — on 25-50 mg 2 once a day, in chronic heart failure-by 12.5-25 mg 2 once a day (the maximum is up to 100 mg / day).

Precautions.

During therapy requires monitoring of the liver and kidney, hemodynamic indices, monitoring concentrations of glucose in the blood, body weight. With the development of bradycardia to 55 BPM drug should be lifted. In patients with insufficiency of blood circulation, gipotenzieй (Sad less than 100 mm Hg. Art.), diffuse vascular changes and/or renal insufficiency it was necessary to monitor kidney function and its deterioration is to reduce the dose or stop the drug.

The caution should be used in the elderly (assigned half dose), with the recent worsening of heart failure flow. In all cases, the treatment starts low doses with subsequent slow their increase to effective. With the progression of heart failure during treatment it is recommended to increase the dose diuretics, in renal failure dose and adjust depending on the functional condition of kidneys. To prevent the syndrome dose should be reduced gradually. People, suffering from severe allergies or undergoing desensitization, It may exacerbate the severity of hypersensitivity reactions. In patients with diabetes mellitus and byhyper-function of the thyroid gland may mask or weaken symptoms, caused by hypoglycemia (If necessary, correct dose gipoglikemicakih funds) or thyrotoxicosis. When pheochromocytoma should be used simultaneously alpha adrenolytics. People, using contact lenses, You must consider the possibility of reducing the slezootdelenija.

When you cancel a combination therapy with clonidine should gradually abolish carvedilol for several days prior to the beginning of a gradual reduction in dose of clonidine. With combination therapy of cardiac insufficiency in the case expressed downward ad originally recommended lower dose diuretics or ACE inhibitors. During treatment excludes alcohol. Be wary appoint patients, concerned with the need for greater attention and speed of reaction.

Cooperation

Active substanceDescription of interaction
AkarʙozaFMR: synergism. Against the backdrop of carvedilol amplified effect and can mask some of the manifestations of hypoglycemia.
VerapamilFMR: synergism. Strengthens (mutually) hypotensive effect; joint application raises in some cases violation of conductivity, rarely with hemodynamic disorders. Against the backdrop of carvedilol is contraindicated in/with the introduction of.
GlimepirideFMR: synergism. Against the backdrop of carvedilol amplified effect and can mask some of the manifestations of hypoglycemia.
GlipizideFMR: synergism. Against the backdrop of carvedilol amplified effect and can mask some of the manifestations of hypoglycemia.
DigoxinFKV. Against the backdrop of carvedilol increases blood.
DiltiazemFMR. Strengthens (mutually) gipotenzivny effect and slows down AV conduction. Against the backdrop of carvedilol is contraindicated in/with the introduction of.
Insulin dvuhfaznыy [human genetic engineering]FMR: synergism. Against the backdrop of carvedilol amplified and extended effect, masked the early symptoms of hypoglycemia.
Insulin soluble [pork monocomponent]FMR: synergism. Against the backdrop of carvedilol amplified and extended effect, masked a developing early signs of hypoglycemia.
KlonidinFMR: synergism. Strengthens (mutually) effect on HELL (gipotenziya) and HEART RATE (bradycardia).
MoclobemideFMR: synergism. Reinforces the effect of the HELL (gipotenziya) and HEART RATE (bradycardia).
PioglitazoneFMR: synergism. Against the backdrop of carvedilol amplified effect and can mask some of the manifestations of hypoglycemia.
ProcarbazineFMR: synergism. Increases gipotenzivny effect and increases the risk of excessive bradycardia.
RifampicinFKV. Accelerates biotransformation, reduces plasma concentration.
RosiglitazoneFMR: synergism. Against the backdrop of carvedilol amplified effect and can mask some of the manifestations of hypoglycemia.
SelegilineFMR: synergism. Reinforces the effect of the HELL (gipotenziya) and HEART RATE (bradycardia).
PhenobarbitalFKV. Accelerates biotransformation, lowers plasma concentration.
FluoxetineFKV. As an inhibitor of CYP2D6 may slow biotransformation and increase the level in the blood.
QuinidineFKV. As an inhibitor of CYP2D6 may reduce speed biotransformation and increase the level in the blood.
CyclosporineFKV. Against the background of the rise in the blood level of carvedilol.
EpinephrineFMR. Against the backdrop of carvedilol reduced antiallergic effect.

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