Cardivas

Kardivas is a medication for the treatment of cardiovascular pathologies; it belongs to the category of α- and β-adrenergic blockers. It has a blocking effect on α1-, β1- and β2-adrenergic receptors, and in addition, it demonstrates antianginal and vasodilatory activity.

The vasodilating effect develops mainly through selective blockade of α1-endings. During vasodilation, the systemic resistance of peripheral vessels is weakened. The drug does not have its own antioxidant properties, but has a membrane-stabilizing effect. [ 1 ]

Indications Cardivas

It is used to treat coronary heart disease (angina pectoris), high blood pressure, and CHF.

Release form

The medicinal substance is released in tablets (volume 6.25 mg) - 10 inside a strip; in a pack - 3 such strips. In addition, tablets can have a volume of 12.5, as well as 25 mg - a dozen inside a strip, 1 or 3 such strips inside a box.

Pharmacodynamics

Vasodilation together with blocking the activity of β-adrenergic receptors in individuals with increased blood pressure indicators causes their decrease, against the background of which there is no increase in systemic resistance of peripheral vessels and weakening of peripheral circulation (this distinguishes the drug from β-adrenergic blockers). At the same time, the decrease in the heart rate is quite insignificant.

In people with coronary heart disease, the drug demonstrates antianginal activity. In addition, it reduces post- and preload. [ 2 ]

In patients with blood flow insufficiency or left ventricular dysfunction, it has a positive effect on hemodynamic values, stabilizes the size of the left ventricle and improves its ejection fraction. [ 3 ]

It has antioxidant properties – by destroying oxygen free radicals.

Pharmacokinetics

The drug is absorbed at high speed, almost completely, after oral administration; protein synthesis is 99%, and the bioavailability index is 25%. Plasma Cmax marks are reached after 60 minutes.

Intrahepatic metabolic processes lead to the formation of metabolic elements with therapeutic effects, which have antioxidant and adrenergic blocking effects.

Excretion of most of the drug is carried out with bile. In case of liver failure, the level of bioavailability increases to 80%. The half-life is in the range of 7-10 hours.

Mean plasma carvedilol levels in elderly individuals are 50% higher than those in younger individuals.

Dosing and administration

The medicine must be taken orally – by swallowing the tablets whole and washing them down with plain water.

Treatment regimen in case of elevated blood pressure levels.

In case of increased blood pressure, you should first take 12.5 mg of the drug once a day for 2 days. In this case, a daily regimen is used with 1 tablet of 12.5 mg taken once or 1 tablet of 6.25 mg taken twice a day. The maintenance dose is 25 mg (1 dose of 25 mg in the morning or 1 tablet of 12.5 mg taken twice a day).

If the desired effect is not achieved, but not earlier than the 14th day of therapy, the daily dose can be increased to the maximum value of 50 mg (2 times a day of 1 tablet of 25 mg). In this case, no more than 25 mg of the drug can be consumed per application, and no more than 50 mg per day.

Elderly people should take 12.5 mg of Cardivas per day throughout the therapy. However, if there is no desired response, the dose can be gradually increased – with 14-day breaks.

Use in people with stable angina.

At first (during the first 2 days) it is necessary to use 12.5 mg of the drug 2 times a day. The maintenance dosage is 25 mg with 2 administrations per day.

If the drug is not effective enough (but at least after a 2-week period), the dosage portion may be increased to a maximum of 50 mg with 2-fold administration per day (1 tablet of 25 mg). No more than 0.1 g of the substance may be used per day.

Elderly people should initially (the first 2 days) take the medication 2 times a day at 12.5 mg. Later, therapy is continued with a daily 2-time intake of 25 mg (maximum daily dose).

Therapy in case of CHF.

The dosage should be selected individually, carefully monitoring the patient's condition when increasing it. It is also necessary to monitor his condition during the period of 2-3 hours from the moment of the first use of the drug or after the 1st increase in the dose. The drug can be used additionally only in case of stable clinical indicators.

Portion sizes and other medications (diuretics, digoxin, and ACE inhibitors) should be adjusted before using Cardivas. The drug should be taken with food (to reduce the likelihood of orthostatic collapse).

At first, 3.125 mg (0.5 tablets of 6.25 mg) should be used twice a day for 2 weeks. If the therapy is well tolerated, the dosage portion may be increased to 6.25 mg administered twice a day. Later, the dosage may also be increased to 12.5 mg administered twice a day, and later to 25 mg administered twice a day. The dosage should be increased to the maximum limits of the patient's good tolerance of the drug.

People weighing less than 85 kg should take 25 mg of the substance twice a day. People weighing more than 85 kg (with a mild form of heart failure) should take the medication in a 2-fold portion of 50 mg per day. The dosage should be increased to 50 mg very carefully and under constant medical supervision.

In the initial phase of therapy or when increasing the dosage, a transient worsening of the manifestations of heart failure may be observed, especially in individuals with a severe form of the disease, or when using large doses of diuretics. In this case, there is no need to cancel the therapy or increase the dosage.

If treatment is discontinued for a period exceeding 14 days, it must be resumed with a 1-time daily dose of 6.25 mg, with a gradual increase according to the scheme described above.

If it is necessary to stop treatment, the medication is gradually discontinued over a period of 14 days.

In case of moderate liver dysfunction or liver failure, the dose is selected individually for the patient.

The medication is used without regard to food intake, but people with heart failure should take it with food to slow down absorption and reduce the likelihood of orthostatic collapse.

• Application for children

The drug is not used in pediatrics because there is not enough information regarding its use in individuals under 18 years of age.

Use Cardivas during pregnancy

Cardivas is not used during pregnancy. If therapy is required during lactation, breastfeeding is stopped.

Contraindications

Among the contraindications:

• severe intolerance associated with carvedilol or other components of the drug;
• CH 4th class according to NYHA rating;
• chronic pulmonary obstructive pathology accompanied by bronchial obstruction;
• clinical type liver dysfunction;
• BA;
• cardiogenic shock;
• AV block 2-3 stages;
• pronounced bradycardia (below 50 beats/min);
• SSSU (also includes SA block);
• a sharp decrease in blood pressure levels (systolic indicator – less than 85 mm Hg);
• metabolic acidosis;
• variant angina;
• a severe disorder of blood flow within the peripheral arteries;
• complex administration with diltiazem or verapamil.

Side effects Cardivas

In the initial phase of therapy (reaction of the first dose) and in case of increasing the dose, a strong drop in blood pressure may be observed. In such cases, the disorder goes away on its own, without changing the dosage of the drug. Among other side effects:

• lesions affecting the central nervous system: dizziness, muscle weakness, headaches and syncope (rarely and often only at the beginning of the treatment cycle), as well as depression, sleep disorders and paresthesia;
• problems with the visual organs: decreased lacrimation, visual damage and irritation affecting the eyes;
• disorders associated with the gastrointestinal tract: diarrhea, constipation, nausea, pain in the abdominal area and vomiting;
• disorders of the cardiovascular system: orthostatic symptoms, angina attacks, bradycardia, AV conduction disorder, decreased peripheral blood flow, development of acute heart failure and progression of existing heart failure;
• epidermal lesions: occasionally itching, allergic rashes, urticaria and manifestations similar to lichen planus appear. At the same time, psoriasis plaques may appear or an exacerbation of existing psoriasis may develop;
• metabolic disorders: hypervolemia or -cholesterolemia, peripheral edema, fluid retention and hyperglycemia (in diabetics);
• Others: leukopenia or thrombocytopenia, nasal congestion, problems with urination, pain in the extremities, swelling of the legs or genitals, decreased renal function, xerophthalmia, increased serum transaminase activity and weight gain.

People with a tendency to develop asthma experience attacks of severe suffocation or dyspnea of asthmatic origin.

Rarely, liver dysfunction and acute renal failure have developed in people with atherosclerosis.

In diabetics, Cardivas may lead to the development of latent diabetes mellitus. The use of the drug may provoke a moderate disorder of sugar balance, but this occurs only rarely.

Overdose

In case of intoxication, heart failure, bradycardia, cardiogenic shock, a sharp decrease in blood pressure and cardiac arrest may occur.

If the victim has not lost consciousness, vomiting should be induced, after which he should be laid horizontally on his back with his head down and legs raised. If the patient has lost consciousness, he should be laid on his side. In addition, symptomatic actions are performed.

Among the methods of therapy:

• in case of severe bradycardia, 0.5-2 mg of atropine is administered;
• use of sympathomimetics (taking into account the intensity of their action, as well as the patient's weight) - isoprenaline, dobutamine or adrenaline.

If the most pronounced symptom of poisoning is dilation of peripheral vessels, mesaton or norepinephrine should be used. At the same time, blood flow processes should be monitored all the time.

To eliminate bronchial spasm, β-adrenergic agonists (intravenously or in aerosol form) or intravenous aminophylline are used.

If convulsions occur, clonazepine or diazepam should be administered intravenously at low speed.

In cases of severe poisoning, with predominant signs of shock, therapy is continued until the patient's condition stabilizes, taking into account the half-life of carvedilol (which is within 6-10 hours).

The drug is not excreted during dialysis.

Interactions with other drugs

The drug potentiates insulin activity (reduces the intensity or masks the manifestations of hypoglycemia).

Administration together with diltiazem or SG may cause slowing of AV conduction processes.

The drug increases serum digoxin levels.

Anesthetics potentiate the negative inotropic and antihypertensive properties of carvedilol.

When used with rifampicin and phenobarbital, there is an increase in the rate of metabolism and a decrease in plasma values of the drug.

The introduction of ACE inhibitors and diuretics increases the severity of hypotension.

It is prohibited to use Cardivas in combination with tricyclics, tranquilizers, sleeping pills and ethanol - because this can potentiate the therapeutic activity.

Combination with NSAIDs leads to a decrease in the antihypertensive properties of the drug.

The drug should not be used together with calcium antagonists, which are administered through intravenous injections.

The use of drugs by individuals who use diuretics, CG or ACE inhibitors in the development of heart failure should be done with extreme caution.

It is prohibited to prescribe the medication in combination with substances that block the action of Ca channels (with verapamil) and class I antiarrhythmic drugs.

Storage conditions

Cardivas should be stored in a place out of reach of small children. Temperature level – maximum 25°C.

Shelf life

Cardivas can be used for a period of 24 months from the date of sale of the therapeutic agent.

Analogues

Analogues of the drug are the medications Corvazan, Carvidex with Carvedigama, Coriol and Carvedilol with Carvid and Cardilol, as well as Medocardil and Carvetrend, Cardiostad and Talliton, as well as Protecard with Lacardia.