Carvidex

Karvidex is a complex drug that non-selectively blocks the activity of α1- and ß-adrenoreceptors. It does not demonstrate endogenous sympathomimetic effects; the proportion of blocking effects relative to α1- and ß-endings is 1:100. The drug has an antioxidant effect, as well as a moderate antagonistic effect relative to calcium ions.

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

Indications Carvidex

It is used in cases of CHF, coronary heart disease, and also with increased blood pressure.

Release form

The medicinal element is released in tablet form - 10 pieces inside a separate strip. Inside the box - 2 such strips.

Pharmacodynamics

The process of vasodilation is realized mostly with antagonistic interaction with α-adrenoreceptors. The drug is a racemic compound consisting of 2 stereoisomers. The blocking effect relative to ß-adrenoreceptors is performed by enantiomers S(-). Carvidex does not have its own sympathomimetic effect.

The drug significantly improves myocardial activity in people with CHF associated with left ventricular dysfunction – it reduces afterload without having a negative effect on left ventricular end-diastolic volume. [ 2 ]

In individuals with moderate primary hypertension, the use of drugs results in a decrease in left ventricular hypertrophy. [ 3 ]

Pharmacokinetics

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

The bioavailability level is approximately 25-35%, due to the exchange processes after the first intrahepatic passage. Increased bioavailability values are observed in people with liver pathologies and the elderly. In liver cirrhosis, this indicator increases fourfold or more. Taking with food does not change the Cmax and bioavailability values, but shortens the period of reaching the Cmax level.

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

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

Dosing and administration

Use for elevated blood pressure.

The dosage is selected individually. At first, you need to take 12.5 mg once a day (during the first 1-2 weeks), and the portion can be divided into 2 administrations at a dose of 6.25 mg; after that, 25 mg of the drug is taken once a day.

If it is necessary to increase the dosage, it should be carried out with a minimum 14-day interval; the maximum daily dose is 50 mg with 1-time administration (or this dose is divided into 2 applications).

Administration to individuals with coronary heart disease.

Portion sizes are selected individually. At the initial stage, 12.5 mg of the medication is taken twice a day (the first 1-2 weeks), and later, 25 mg is used twice a day.

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

Use in people with CHF.

The dosage should be selected individually, under medical supervision. At first, 3.125 mg of the drug is administered twice a day (for the first 14 days). If this dose is well tolerated, it is increased with at least 14-day breaks to 6.25 mg twice a day. Then, it is increased to 12.5 mg twice a day, and then to 25 mg twice a day. The dosage should be increased to the maximum limits within which the drug is tolerated without complications.

People with severe 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.

Individuals whose weight is over 85 kg, with moderate or mild CHF, should take a maximum of 50 mg of Carvidex 2 times a day.

Before increasing the dosage, the patient should be examined by a physician to determine whether the manifestations of vasodilation or heart failure have worsened.

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

The medicine should be taken with food 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

Should not be prescribed in pediatrics (under 18 years of age).

Use Carvidex during pregnancy

Carvidex is not used during breastfeeding and pregnancy.

Contraindications

Among the contraindications:

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

Side effects Carvidex

Main side effects:

• problems with the central nervous system: dizziness, headaches and weakness. Occasionally, paresthesia, depressed mood, asthenia and sleep disorders are observed;
• CVS dysfunction: decreased blood pressure, bradycardia and orthostatic symptoms. Occasionally, peripheral blood flow is impaired (cold extremities), manifestations of Raynaud's disease or intermittent claudication are exacerbated and fainting occurs. Progression of heart failure and AV conduction disorder are observed sporadically;
• Gastrointestinal disorders: stomach pain, nausea, diarrhea and xerostomia. Constipation, vomiting and increased intrahepatic transaminase levels are occasionally observed;
• changes in metabolic processes: hypo- or hyperglycemia, as well as hypercholesterolemia and weight gain;
• disorders of hematopoietic processes: leukopenia or thrombocytopenia;
• urinary tract disorders: in people with renal dysfunction, the disorders may worsen. Occasionally, swelling or renal failure may occur;
• respiratory disorders: sneezing, nasal congestion and bronchial spasm;
• signs of allergy: epidermal manifestations of allergy (urticaria and itching), as well as exacerbation of eczema;
• damage to the visual organs: irritation in the eye area and visual impairment;
• others: arthralgia or myalgia. Rarely – erectile dysfunction.

Overdose

In case of intoxication, heart failure, bradycardia, vomiting, cardiogenic shock, a strong decrease in blood pressure, as well as generalized convulsions, confusion, respiratory distress and cardiac arrest may develop.

Symptomatic actions are performed. The activity of vital organs is monitored and corrected; if necessary, the patient can be placed in intensive care.

Interactions with other drugs

Combined use of the drug with digoxin causes an increase in the latter's indicators. Administration together with SG prolongs the period of AV conduction. Because of this, with the onset of carvedilol use, during the selection of its dosage, or when the drug is discontinued, it is necessary to constantly monitor plasma digoxin values.

The drug may potentiate the activity of other antihypertensive drugs or substances with antihypertensive effects.

There is a risk of increased plasma levels of cyclosporine when combined with carvedilol. Cyclosporine levels should be monitored continuously from the start of Carvidex and the dosage of the former adjusted as needed.

General anesthesia should be administered with extreme caution to persons using the drug, because when combined with individual anesthetics, a synergistic negative isotropic effect of the drug may be observed.

Substances that exhibit ß-blocking activity are capable of increasing the antidiabetic effect of insulin or hypoglycemic drugs taken orally.

Combination with clonidine may provoke bradycardia and potentiate the hypotensive effect of carvedilol. When discontinuing combined treatment with clonidine, first stop taking Carvidex, and after a few days – clonidine.

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

The use of the drug together with agents blocking the activity of Ca channels (with verapamil) or antiarrhythmic agents of type I requires monitoring of ECG readings and blood pressure levels, because there is data on conduction disorders when using the drug together with diltiazem. The drug cannot be used in people who are receiving intravenous injections of verapamil or diltiazem, since this can provoke severe bradycardia and a decrease in blood pressure.

Medications that reduce catecholamine levels (this includes MAOIs and reserpine) increase the likelihood of intense bradycardia and decreased blood pressure.

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

Storage conditions

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

Shelf life

Carvidex can be used for a period of 2 years from the date of release of the pharmaceutical product.

Analogues

Analogues of the drug are the medicines Coriol, Kardivas and Corvazan with Carvedigama, and also Carvid, Carvedilol, Cardiostad with Carvetrend and Cardilol. In addition, the list includes Medocardil with Talliton, Protecard and Lacardia.