Kardivas

Cardivas is a medicine for the treatment of cardiovascular pathologies; enters the category of α-, as well as β-blockers. It has a blocking effect on α1-, β1- and β2-adrenergic receptors, and in addition, it demonstrates antianginal and vasodilating activity.

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

Indications Kardivas

It is used for the treatment of coronary artery disease (angina pectoris), high blood pressure, and CHF .

Release form

The release of the drug substance is made in tablets (volume 6.25 mg) - 10-current inside the strip; in a pack - 3 such strips. In addition, tablets can have a volume of 12.5 mg, 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 persons with increased blood pressure values 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-blockers). At the same time, the decrease in the heart rate level is quite insignificant.

In people with ischemic heart disease, the drug demonstrates antianginal activity. It also weakens post- and preload. [2]

In patients with insufficient blood flow 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]

Possesses antioxidant properties - by destroying free oxygen 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 reaches marks after 60 minutes.

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

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

The average plasma values of carvedilol in the elderly exceed those in younger individuals by 50%.

Dosing and administration

It is necessary to take the medicine orally - swallowing the tablets whole and drinking it with plain water.

Treatment regimen in case of elevated blood pressure levels.

In the case of increased blood pressure, you first need to take 12.5 mg of the drug 1 time per day over a period of 2 days. In this case, a daily regimen is used with 1-time administration of 1 tablet of 12.5 mg or with 2-time use of 1 tablet of 6.25 mg. The size of the maintenance portion is 25 mg (1-time dose of 25 mg in the morning or 2-time dose of 1 tablet with a volume of 12.5 mg).

In the absence of the required effect, but not earlier than the 14th day of therapy, the daily portion can be increased to a maximum of 50 mg (2-time intake of the 1st 25 mg tablet). At the same time, for 1 application, you can use no more than 25 mg of the drug, and no more than 50 mg per day.

Elderly people should consume 12.5 mg of Kardivas per day throughout therapy. But in the absence of the required reaction, the portion is allowed to gradually increase - with 14-day breaks.

Use in people with stable angina pectoris.

First (during the first 2 days), you need to apply 12.5 mg of the drug 2 times a day. The maintenance dosage is 25 mg with 2 doses per day.

In case of insufficient effectiveness of the medication (but at least after a 2-week period), it is allowed to increase the dosage portion to a maximum of 50 mg with 2-fold administration per day (1 tablet with a volume of 25 mg). You can use no more than 0.1 g of the substance per day.

Elderly persons should first (for the first 2 days) use the medication 2 times, 12.5 mg each. Later, therapy is continued with a 2-day intake of 25 mg (maximum daily portion).

Therapy in case of CHF.

You need to select the dosage personally, carefully monitoring the patient's condition when it is increased. You also need to monitor its condition within 2-3 hours from the moment of the first use of the drug or after the 1st increase in the portion. It is possible to use the medication additionally only in the case of stable clinical indicators.

Serving sizes and other medications (diuretics, digoxin, and ACE inhibitors) should be adjusted prior to using Kardivas. The drug should be used with food (to reduce the likelihood of orthostatic collapse).

First, you need to use 3.125 mg 2 times a day (0.5 tablets 6.25 mg), for 2 weeks. With good tolerability of therapy, it is allowed to increase the dosage portion to 2-time administration of 6.25 mg. In the future, the dosage can also be increased - up to 2-fold use of 12.5 mg per day, and later - up to 2-time intake of 25 mg. It is necessary to increase the portion to the maximum limits of good tolerance of the drug by the patient.

People weighing less than 85 kg need to take 25 mg of the substance 2 times a day. Persons whose weight is over 85 kg (with a mild form of HF), it is necessary to use 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 the dosage is increased, there may be a transient worsening of the manifestations of HF, especially in persons with severe disease, or when using large doses of diuretics. In this case, it is not necessary to cancel therapy and increase the dosage.

If treatment is canceled for a period of more than 14 days, it must be resumed with a 1-fold daily portion of 6.25 mg, with a gradual increase according to the scheme described above.

If it is necessary to complete the treatment, a gradual withdrawal of the medication is made, lasting 14 days.

In the case of a moderate form of hepatic dysfunction or insufficient liver function, the selection of a portion is made for the patient personally.

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

• Application for children

The medication is not used in pediatrics, because there is not enough information regarding its use in persons under the age of 18.

Use Kardivas during pregnancy

During pregnancy, Kardivas is not used. If therapy is required during lactation, breastfeeding is discontinued.

Contraindications

Among the contraindications:

• severe intolerance associated with carvedilol or other elements of the drug;
• СН 4th class according to NYHA rating;
• pulmonary obstructive pathology of a chronic nature, accompanied by bronchial obstruction;
• hepatic dysfunction of the clinical type;
• BA;
• cardiogenic shock;
• Stage 2-3 AV block;
• severe bradycardia (below 50 beats / min);
• SSSU (also includes SA blockade);
• a strong decrease in blood pressure marks (systolic indicator - less than 85 mm Hg);
• metabolic acidosis;
• variant angina pectoris;
• having a severe intensity disorder of blood flow inside the peripheral arteries;
• complex administration with diltiazem or verapamil.

Side effects Kardivas

In the initial phase of therapy (reaction of the 1st dosage) and in the case of an increase in the portion, there may be a strong drop in blood pressure. In such cases, the violation goes away on its own, without changing the dosage of drugs. Among other side signs:

• lesions affecting the central nervous system: dizziness, muscle weakness, headaches and syncope (occasionally and often only during the beginning of the treatment cycle), and at the same time depression, sleep disorders and paresthesias;
• problems with the visual organs: reduced tear production, visual impairment and irritation that affects the eyes;
• disorders associated with the work of the gastrointestinal tract: diarrhea, constipation, nausea, abdominal pain and vomiting;
• disorders of the CVS function: orthostatic symptoms, angina attacks, bradycardia, AV conduction disorder, decreased peripheral blood flow, development of AHF and progression of existing heart failure;
• epidermal lesions: occasionally itching, rashes of an allergic nature, urticaria and manifestations similar to lichen planus appear. Along with this, plaques of psoriasis may occur or an exacerbation of existing psoriasis may develop;
• metabolic disorders: hypervolemia or cholesterolemia, peripheral edema, delayed fluid secretion and hyperglycemia (in diabetics);
• others: leuko- or thrombocytopenia, nasal congestion, problems with urination, pain in the extremities, swelling of the legs or genitals, weakening of renal activity, xerophthalmia, increased serum transaminase activity and weight gain.

Persons with a tendency to develop asthma have attacks of severe suffocation or dyspnea of asthmatic origin.

Occasionally, people with atherosclerosis develop hepatic dysfunction and acute renal failure.

In diabetics, Cardivas can lead to the development of latent diabetes mellitus. The use of drugs can provoke a moderate disorder of the sugar balance, but this happens only occasionally.

Overdose

With intoxication, HF, bradycardia, cardiogenic shock, a strong decrease in blood pressure values and cardiac arrest can occur.

If there is no loss of consciousness, the victim should be induced to vomit, and then laid horizontally on his back in a position with his head lowered and legs raised. If the patient has lost consciousness, he must be laid on his side. In addition, symptomatic actions are performed.

Among the methods of therapy:

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

If the most pronounced sign of poisoning is the expansion of peripheral vessels, it is necessary to apply mezaton or norepinephrine. At the same time, it is necessary to monitor the blood flow processes all the time.

To eliminate bronchial spasm, β-adrenomimetics are used (in / in the way or in the form of an aerosol) or intravenous use of aminophylline.

When seizures occur, clonazepine or diazepam should be administered intravenously at a low speed.

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

The drug is not excreted during dialysis.

Interactions with other drugs

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

Administration together with diltiazem or SG may slow down AV conduction processes.

The drug increases serum digoxin values.

Anesthetics potentiate the negative inotropic and antihypertensive properties of carvedilol.

When used with rifampicin and phenobarbital, an increase in the metabolic rate and a decrease in plasma values of drugs occur.

The introduction of an ACE inhibitor and diuretic drugs increases the severity of hypotension.

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

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

The medicine cannot be used in conjunction with calcium antagonists, which are administered through intravenous injection.

The use of drugs by persons who use diuretics, SG or ACE inhibitors in the development of HF should be done with extreme caution.

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

Storage conditions

Kardivas should be kept out of the way of small children. Temperature level - maximum 25 ° C.

Shelf life

Cardivas can be used for a 24-month term from the date of sale of the therapeutic agent.

Analogs

Analogues of drugs are the medicines Corvazan, Karvidex with Carvedigama, Coriol and Carvedilol with Carvid and Cardilol, and in addition Medocardil and Carvetrend, Cardiostad and Talliton, as well as Protecard with Lacardia.