Carvetrend

Carvetrend has vasodilating activity and an indiscriminate β-blocking effect; also demonstrates antioxidant effects and selectively blocks the activity of α1-adrenergic receptors.

The drug weakens the resistance of peripheral vessels, selectively blocking the action of α1-adrenergic receptors, and in addition suppressing the influence exerted by the RAAS - through the non-selective blockade of β-adrenergic receptors. Along with this, there is a decrease in the activity of plasma renin, which reduces the likelihood of delayed excretion of fluid. [1]

Indications Carvetrend

It is used in the case of a stable type of chronic angina pectoris, primary hypertension , and in addition in the case of a stable cardiac insufficiency (chronic type).

Release form

The release of the drug substance is realized in the form of tablets - 14 pieces inside a cell pack (the volume of tablets is 3.125, 6.25, and also 12.5 mg), 2 packs inside the package. Also produced in 28 pieces inside a separate plate (volume 25 mg) - 1 piece inside the box.

Pharmacodynamics

The drug does not have ICA and has a membrane stabilizing effect. It is a two-stereoisomeric racemate. The development of blocking the action of ß1-, as well as ß2-adrenergic receptors is realized mainly with the help of the S (-) enantiomer, and the α1-blocking effect is provided by the S (-) enantiomers, as well as R (+). Carvetrend has a significant antioxidant effect and scavenges free radicals.

In the case of application with an increased level of blood pressure, its decrease under the influence of drugs is not accompanied by a change in the processes of intrarenal circulation and potentiation of the systemic resistance of peripheral vessels, which is often observed with the introduction of β-blockers. [2]

When administered to persons with angina pectoris, the development of pain and myocardial ischemia is prevented. [3]

In individuals with left ventricular dysfunction or CHF, the medication has a positive effect on hemodynamics, left ventricular size and ejection fraction.

The drug does not alter lipid metabolism.

Pharmacokinetics

The bioavailability of the drug is approximately 25-30% (R-form), as well as 15% (S-form). Plasma level Cmax is noted after 1 hour. The proportions between dosage and plasma values are linear. Food intake does not change the level of drug bioavailability.

Carvedilol is a highly lipophilic element. About 98-99% of the substance is synthesized with protein. The distribution volume is approx. 2 l / kg. 60-75% of the absorbed drug undergoes metabolic processes during the 1st intrahepatic passage.

The half-life of a drug is in the range of 6-10 hours. The clearance level is 590 ml per minute. Excretion is mainly carried out with bile, and then with feces. Part of it is excreted in the form of metabolic elements through the kidneys.

Metabolic processes are carried out inside the liver - through oxidation, as well as glucuronization in the area of the aromatic ring. Metabolic components demonstrate an intense adrenergic blocking and antioxidant effect.

Plasma drug levels in the elderly are approximately 50% higher.

Individuals with elevated blood pressure and moderate (CC - within 20-30 ml per minute) or severe (CC - <20 ml per minute) renal failure showed an increase of 40-55% in plasma values of drugs.

Dosing and administration

Carvetrend should be taken orally, starting therapy with the introduction of small dosages. Later, the portions are gradually increased until the desired effect is obtained.

With primary hypertension, you first need to take 12.5 mg of medication in the morning (after eating) or 6.25 mg in the morning and then in the evening. After 2 days of this regimen, the portion is increased to a 1-time dose of 25 mg or a 2-time dose of 12.5 mg. After 2 weeks of treatment, the portion is increased to 2 times a day of use of 25 mg.

In case of hypertension, no more than 50 mg can be administered per day (divided by 2 doses).

During HF, the medication is first used in portions of 3.125 mg (2 administrations per day).

For angina pectoris of a stable type, 12.5 mg is administered 2 times a day. After such a 2-day cycle, the portion is increased to 2-fold use of 25 mg.

During a chronic type of angina pectoris, a maximum of 50 mg of drugs can be used (for 2 uses).

In people with heart failure who are treating angina pectoris, the initial dosage is 3.125 mg (2 doses per day).

• Application for children

Forbidden to use in pediatrics.

Use Carvetrend during pregnancy

Carvetrend is not prescribed for HB or pregnancy.

Contraindications

The main contraindications:

• severe intolerance to the elements of the drug;
• cardiogenic shock;
• having a decompensated form of CH (4th stage according to the NYHA classification), in which it is necessary to use inotropic substances;
• metabolic acidosis;
• Cor pulmonale and hypertension affecting the lungs;
• pheochromocytoma;
• use in conjunction with verapamil, diltiazem, as well as other antiarrhythmic drugs;
• Stage 2-3 AV block (without the use of a pacemaker);
• SSSU;
• bradycardia (heart rate values are less than 50 beats per minute);
• decreased blood pressure (SBP level is less than 85 mm Hg);
• having an uncompensated form of heart failure, in which it is necessary to prescribe positive isotropic drugs and diuretic drugs;
• BA and other obstructive pulmonary lesions;
• severe hepatic dysfunction;
• use of IMAO products (except for substances of the IMAO-V type).

Side effects Carvetrend

Among the side signs:

• changes in blood test data: the development of hypo- or hyperglycemia, hypercholesterolemia, -kalemia or -triglyceridemia, and in addition thrombocyto- or leukopenia, anemia and hyponatremia, as well as an increase in the values of alkaline phosphatase, creatinine and urea and a decrease in prothrombin values;
• allergy symptoms: anaphylactic manifestations;
• convulsions, dizziness, orthostatic collapse and paresthesias, weight gain, headaches, depression, sleep disturbances and loss of consciousness;
• dryness of the ocular mucosa or irritation in the eye area, as well as visual disturbances;
• swelling, angina pectoris, heart failure, bradycardia, dyspnea, cold extremities and hypotension, palpitations, increased blood pressure, Raynaud's disease and exacerbation of intermittent claudication;
• nasal congestion, pulmonary edema, and asthma;
• abdominal pain, xerostomia, nausea, periodontitis, constipation or diarrhea, melena and hepatic dysfunction (increased ALT, AST and GGT levels);
• exanthema, alopecia, urticaria, hyperhidrosis, pruritus and dermatitis;
• arthralgia and pain affecting the limbs;
• urinary disorders, renal failure, urinary incontinence and hematuria;
• hyperuricemia, glucosuria, or albuminuria;
• erectile disfunction;
• fever, asthenia and flu-like symptoms.

Overdose

In case of poisoning, HF, bradycardia, cardiogenic shock, a decrease in blood pressure, vomiting, generalized seizures, respiratory disorders, confusion and cardiac arrest are noted.

Gastric lavage, the use of sorbents, and also symptomatic actions, monitoring and changing the values of systems important for life are performed; in the case of bradycardia, the administration of 0.5-2 mg of atropine is prescribed.

Interactions with other drugs

You can not use the drug in combination with verapamil, diltiazem or other type I antiarrhythmic substances (IV), as well as MAOIs (in addition to MAO-B).

Using SG.

Administration together with digoxin increases its equilibrium level by about 16% (the digitoxin index also increases by about 13%) in people with elevated blood pressure. It is necessary to monitor the plasma level of digoxin at the beginning of treatment with Carvetrend, at its end, as well as adjusting the portions.

When used with SG substances, prolongation of AV conduction can develop.

It is necessary to carefully monitor the condition of persons who use ß-blockers or drugs that lower the indicators of catecholamines (such as reserpine or MAOIs), since this can provoke severe bradycardia or the development of symptoms of a decrease in blood pressure.

The rest of the antihypertensive drugs.

The drug potentiates the activity of other antihypertensive drugs (among them are α1-terminal antagonists). Potentiation of negative antihypertensive manifestations of phenothiazines, vasodilators, barbiturates with alcohol and tricyclics is also possible.

Cyclosporine.

It is necessary to monitor the plasma level of cyclosporine when using Carverend, because it increases with this combination.

Hypoglycemic drugs, including insulin.

Due to the fact that when the drug is administered, insulin and other hypoglycemic substances can more intensively reduce the blood sugar index, and carvedilol itself is able to mask the signs of hypoglycemia, it is very important to constantly monitor the blood glucose values.

Clonidine.

During the cancellation of the complex treatment with the use of Carvetrend and clonidine, first stop using the first, and then gradually reduce the portion of clonidine.

Inhaled anesthetics.

During the introduction of anesthesia, it is necessary to take into account the negative antihypertensive and isotropic interaction of the drug with anesthetics.

Medicines that induce or slow down the action of hemoprotein enzymes 450.

Persons using medications that induce enzymes of the structure of hemoprotein 450 (barbiturates with rifampicin), or slow them down (including ketoconazole, erythromycin with cimetidine, haloperidol and verapamil with fluoxetine) should be under constant control while using such drugs with carvedilol as enzyme inducers are able to decrease the serum values of the latter, and inhibitors - to increase them.

Estrogens with NSAIDs and corticosteroids.

The antihypertensive effect of drugs is reduced in the case of the use of medications that retain Na and fluid inside the body.

Sympathomimetics and α-, as well as ß-adrenergic agonists.

Administration together with these drugs potentiates the vasoconstrictor effect.

Muscle relaxants and ergotamine.

The combination of a drug and muscle relaxants or ergotamine leads to a potentiation of the blocking neuromuscular effect.

Xanthine derivatives.

It is necessary to very carefully combine the drug with xanthine derivatives (this includes theophylline with aminophylline), because this weakens the β-adrenergic blocking activity.

Storage conditions

The carvetrend must be kept at temperatures in the range of 15-25 ° C.

Shelf life

Carvetrend can be used for a 36-month term from the moment the therapeutic substance is marketed.

Analogs

Analogs of the drug are Atram, Cardivas and Coriol with Carvid, and in addition Dilator, Cardoz and Carvedigamma with Carvidex, Carvedilol and Cardiostad with Protecard, as well as Carvium, Talliton and Corvazan with Medocardil.