Carvidex

Karvidex is a complex medicine that indiscriminately blocks the activity of α1- as well as β-adrenergic receptors. Does not show endogenous sympathomimetic effects; the proportion of the blocking effect relative to the α1- and ß-endings is 1d100. The drug has an antioxidant effect, as well as a moderate antagonistic effect on calcium ions.

Long-term use of drugs has a positive effect on lipid parameters within the blood serum. The drug does not change blood sugar values and reduces left ventricular hypertrophy. [1]

Indications Carvidex

It is used in the case of CHF , ischemic heart disease , as well as with increased blood pressure.

Release form

The release of the drug element is made in tablet form - 10 pieces inside a separate strip. There are 2 such strips inside the box.

Pharmacodynamics

The process of vasodilatation is realized for the most part with antagonistic interaction with α-adrenergic receptors. The drug is a racemic compound consisting of 2 stereoisomers. S (-) enantiomers have a blocking effect on β-adrenergic receptors. Karvidex does not have its own sympathomimetic effect.

The drug significantly improves myocardial activity in people with CHF associated with left ventricular dysfunction - it weakens afterload without negatively affecting the left ventricular end-diastolic volume. [2]

In persons with a moderate stage of primary hypertension, when using drugs, there is a decrease in left ventricular hypertrophy. [3]

Pharmacokinetics

When administered orally, rapid absorption occurs with obtaining plasma Cmax values after 1-2 hours.

The bioavailability level is approximately 25-35%, due to metabolic processes after the 1st intrahepatic passage. An increase in bioavailability values is observed in persons with hepatic pathologies and the elderly. With hepatic cirrhosis, this figure increases fourfold and higher. Consumption with food does not change the Cmax value and bioavailability, but shortens the period of reaching the Cmax level.

About 99% of drugs are involved in protein synthesis. During intrahepatic hydroxylation and demethylation, 3 metabolic elements are formed that have a more intense β-blocking effect and antioxidant effect than carvedilol.

The term half-life lasts in the range of 6-10 hours. Most of the drug is excreted in feces and bile in the form of metabolic components. A small amount is excreted in the urine.

Dosing and administration

Use with increased blood pressure.

The dosage selection is made personally. First, you need to use 12.5 mg 1 time per day (during the first 1-2 weeks), while the portion can be divided into 2 administrations at a dose of 6.25 mg; after that, 25 mg of drugs are used once a day.

If there is a need for an increase in dosage, it should be carried out with a minimum of 14 days; the maximum daily portion is 50 mg in 1 dose (or this portion is divided into 2 applications).

Introduction to persons with ischemic heart disease.

Serving sizes are personalized. At the initial stage, 12.5 mg of the drug is consumed 2 times per day (the first 1-2 weeks), and later used 2 times per day at a dosage of 25 mg.

If an increase in dosage is required, then it is carried out with a minimum of 2-week break; the maximum per day is 0.1 g (divided by 2 injections).

Application in people with CHF.

The dosage should be selected personally, under medical supervision. First, a 2-time injection per day of 3.125 mg of the drug is prescribed (for the first 14 days). With good tolerance of this portion, it is increased with a minimum of 14-day breaks to 2-fold use per day of 6.25 mg. Further, an increase is carried out to a 2-time intake of 12.5 mg per day, and then up to a 2-time intake of 25 mg. The dosage should be increased to the maximum limits in which the drug is tolerated without complications.

People with a severe stage of CHF (and people with mild or moderate CHF weighing less than 85 kg) can take a maximum of 25 mg of the drug 2 times a day.

Persons weighing more than 85 kg, with moderate or mild CHF, should use a maximum of 50 mg of Karvidex 2 times a day.

Before increasing the dosage, it is necessary to conduct a medical examination of the patient to determine whether the manifestations of vasodilation or HF have increased.

If there is a need to cancel the medication, it is carried out gradually, in the period of 7-14 days. If therapy was interrupted for a period of more than 2 weeks, it is resumed with a portion of 3.125 mg, 2 times a day, after which the dosage is selected, following the instructions above.

The medicine should be taken with food in order to reduce the rate of absorption of the therapeutic substance and the severity of orthostatic symptoms.

If dosages below 6.25 mg are required, tablets of the appropriate volume are used.

• Application for children

Cannot be prescribed in pediatrics (under the age of 18).

Use Carvidex during pregnancy

Carvidex is not used for breastfeeding or pregnancy.

Contraindications

Among the contraindications:

• severe intolerance caused by carvedilol or other elements of the medication;
• active phase of heart failure or heart failure at the stage of decompensation;
• hepatic dysfunction;
• blockade in the 2-3rd stage (in the absence of a permanent pacemaker);
• severe bradycardia (below 50 beats per minute);
• SSSU;
• SA blockade;
• a strong decrease in blood pressure values;
• having an obstructive form of lesions of the respiratory tract, including bronchial spasm;
• a history of asthma.

Side effects Carvidex

The main side symptoms:

• problems with the work of the central nervous system: dizziness, headaches and weakness. Paresthesias, mood suppression, asthenia, and sleep disturbance are rare;
• dysfunction of the CVS: a decrease in blood pressure, bradycardia and orthostatic signs. Occasionally, peripheral blood flow is disturbed (cold extremities), manifestations of Raynaud's disease or intermittent claudication are aggravated, and fainting occurs. HF progression and AV conduction disorder are observed singly;
• disorders of the gastrointestinal tract: stomach pain, nausea, diarrhea and xerostomia. Occasionally, constipation, vomiting and an increase in the values of intrahepatic transaminases are noted;
• changes in metabolic processes: hypo- or hyperglycemia, as well as hypercholesterolemia and weight gain;
• violations of hematopoietic processes: leuko- or thrombocytopenia;
• urinary tract damage: in people with renal dysfunction, the impairment may worsen. Occasionally, swelling or failure of the kidneys appears;
• respiratory disorders: sneezing, nasal congestion and bronchial spasm;
• signs of allergies: epidermal manifestations of allergies (urticaria and itching), as well as exacerbation of the course of eczema;
• damage to the visual organs: irritation in the eye area and visual impairment;
• others: arthralgia or myalgia. Occasionally, erectile dysfunction.

Overdose

With intoxication, HF, bradycardia, vomiting, cardiogenic shock, a strong decrease in blood pressure can develop, and in addition, generalized seizures, confusion, respiratory distress and cardiac arrest.

Symptomatic actions are performed. Control and correction of the activity of organs important for life is carried out; if necessary, the patient can be placed in intensive care.

Interactions with other drugs

The combined use of the drug with digoxin causes an increase in the latter. Administration together with SG prolongs the AV conduction period. Because of this, with the beginning of the use of carvedilol, during the selection of its dosage, or when the drug is canceled, it is necessary to constantly monitor the plasma values of digoxin.

The drug can potentiate the activity of other antihypertensive drugs or substances that have an antihypertensive effect.

There is a risk of increased plasma levels of cyclosporine when combined with carvedilol. It is necessary to constantly monitor the level of cyclosporine with the beginning of the use of Karvidex and adjust the dosage of the former if necessary.

Extremely carefully it is necessary to carry out general anesthesia in persons using the drug, because when combined with individual anesthetics, a synergistic negative isotropic effect of drugs can be noted.

Substances that have ß-blocking activity can increase the antidiabetic effect of insulin or hypoglycemic drugs taken by mouth.

The combination with clonidine can provoke bradycardia and potentiate the hypotensive effect of carvedilol. During the cancellation of the combined treatment with clonidine, first you need to stop taking Karvidex, and after a few days - clonidine.

Substances that induce intrahepatic microsome oxidases (such as rifampicin with phenobarbital) increase the rate of metabolic processes, reducing the plasma values of carvedilol; at the same time, agents that slow down the above process (such as cimetidine) increase the plasma level of drugs.

The use of the medication together with agents blocking the activity of Ca channels (with verapamil), or type I antiarrhythmic substances requires monitoring of ECG readings and blood pressure levels, because there is evidence of conduction disorders when drugs are used together with diltiazem. The drug should not be used in persons who are given intravenous injections of verapamil or diltiazem, as this can provoke severe bradycardia and a decrease in blood pressure.

Medicines that reduce catecholamine levels (this includes MAOIs and reserpine) increase the likelihood of intense bradycardia and a decrease in blood pressure.

It is necessary to very carefully combine the drug with substances that slow down the action of enzymes of the structure of hemoprotein P450 2D6 (this includes propafenone and omeprazole with quinidine, as well as tricyclics), since it participates in the metabolic processes of carvedilol (it can increase the likelihood of negative symptoms of drugs - in particular, lowering blood pressure ).

Storage conditions

Carvidex should be stored in a dark place, out of the reach of small children, protected from moisture penetration. Temperature indicators - no more than 25 ° С.

Shelf life

Carvidex can be used for a 2-year term from the date of release of the pharmaceutical product.

Analogs

Analogues of drugs are the medicines Coriol, Cardivas and Corvazan with Carvedigama, and in addition Carvid, Carvedilol, Cardiostad with Carvetrend and Cardilol. In addition, Medocardil with Talliton, Protekard and Lacardia are on the list.