Carvethrand

Carvetrend has vasodilating activity and non-selective β-blocking effect; it also demonstrates antioxidant effect and selectively blocks the activity of α1-adrenergic receptors.

The drug reduces peripheral vascular resistance by selectively blocking the action of α1-adrenergic receptors, and in addition, by suppressing the effect of RAAS - through non-selective blockade of β-adrenergic receptors. At the same time, there is a decrease in the activity of plasma renin, which reduces the likelihood of fluid retention. [ 1 ]

Indications Carvethrand

It is used in cases of stable angina pectoris of chronic degree, primary hypertension, and also in cases of stable cardiac insufficiency (chronic type).

Release form

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

Pharmacodynamics

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

In case of use at elevated blood pressure, its decrease under the influence of the drug is not accompanied by changes in the processes of intrarenal blood circulation and potentiation of systemic resistance of peripheral vessels, which is often observed when administering β-blockers. [ 2 ]

When administered to individuals with angina pectoris, it prevents the development of pain and myocardial ischemia. [ 3 ]

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

The drug does not alter lipid metabolism.

Pharmacokinetics

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

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

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

Metabolic processes are carried out inside the liver – through oxidation, as well as glucuronidation in the aromatic ring area. Metabolic components demonstrate an intense adrenoblocking and antioxidant effect.

Plasma drug levels are approximately 50% higher in older people.

In individuals with elevated blood pressure and moderate (CC – within 20-30 ml per minute) or severe (CC – <20 ml per minute) renal impairment, a 40-55% increase in plasma LS values was observed.

Dosing and administration

Carvetrend should be taken orally, starting therapy with small doses. Later, the doses are gradually increased until the desired effect is achieved.

In case of primary hypertension, you should first take 12.5 mg of the medicine in the morning (after meals) or 6.25 mg in the morning and then in the evening. After 2 days of this regimen, the dose is increased to 1-time intake of 25 mg or 2-time administration of 12.5 mg. After 2 weeks of treatment, the dose is increased to 2-times per day use of 25 mg.

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

During CH, the medication is initially used in a dose of 3.125 mg (2 doses per day).

For angina of a stable type, 12.5 mg is administered twice a day. After such a 2-day cycle, the dose is increased to 25 mg twice a day.

During chronic angina, a maximum of 50 mg of the drug can be used (in 2 doses).

In patients with heart failure who are being treated for angina, the initial dosage is 3.125 mg (2 doses per day).

• Application for children

Not for use in pediatrics.

Use Carvethrand during pregnancy

Carvetrend is not prescribed during breastfeeding or pregnancy.

Contraindications

Main contraindications:

• severe intolerance to the components of the drug;
• cardiogenic shock;
• having a decompensated form of heart failure (stage 4 according to the NYHA classification), in which it is necessary to use inotropic substances;
• metabolic acidosis;
• "pulmonary heart disease" and hypertension affecting the lungs;
• pheochromocytoma;
• use in combination with verapamil, diltiazem, and other antiarrhythmic drugs;
• AV block stage 2-3 (without the use of a pacemaker);
• SSSU;
• bradycardia (heart rate values are less than 50 beats per minute);
• reduced blood pressure (systolic blood pressure level is less than 85 mm Hg);
• having an uncompensated form of heart failure, in which it is necessary to prescribe positive isotropic agents and diuretic drugs;
• BA and other lung diseases of an obstructive nature;
• severe liver dysfunction;
• use of MAOIs (except MAOI-B type substances).

Side effects Carvethrand

Side effects include:

• changes in blood test data: development of hypo- or hyperglycemia, hypercholesterolemia, -kalemia or -triglyceridemia, as well as 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 levels;
• allergy symptoms: anaphylactic reactions;
• convulsions, dizziness, orthostatic collapse and paresthesia, weight gain, headaches, depression, sleep disturbances and loss of consciousness;
• dryness of the mucous membrane of the eye or irritation in the eye area, as well as visual disturbances;
• edema, 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 liver dysfunction (increased levels of ALT, AST and GGT);
• exanthema, alopecia, urticaria, hyperhidrosis, itching and dermatitis;
• arthralgia and pain affecting the limbs;
• urinary disorders, renal failure, urinary incontinence and hematuria;
• hyperuricemia, glucosuria or albuminuria;
• erectile dysfunction;
• increased temperature, asthenia and flu-like symptoms.

Overdose

In cases of poisoning, heart failure, bradycardia, cardiogenic shock, decreased blood pressure, vomiting, generalized convulsions, respiratory distress, confusion, and cardiac arrest are observed.

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

Interactions with other drugs

The drug should not be used in combination with verapamil, diltiazem or other type I antiarrhythmic agents (IV), as well as MAOIs (other than MAO-B).

Using SG.

Co-administration with digoxin increases its steady-state level by approximately 16% (digitoxin also increases by approximately 13%) in people with elevated blood pressure. Plasma digoxin levels should be monitored at the start of Carvetrend treatment, at its end, and during dose adjustments.

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

Careful monitoring of the condition of individuals using ß-blockers or drugs that lower catecholamine levels (including reserpine or MAOIs) is necessary, as this may provoke severe bradycardia or the development of symptoms of decreased blood pressure.

Other antihypertensive drugs.

The drug potentiates the activity of other hypotensive medications (including α1-ending antagonists). Potentiation of negative antihypertensive effects of phenothiazines, vasodilators, barbiturates with alcohol and tricyclics is also possible.

Cyclosporine.

Plasma cyclosporine levels should be monitored when using Carvetrend, as they are increased by this combination.

Hypoglycemic drugs, including insulin.

Since insulin and other hypoglycemic agents can reduce blood sugar levels more intensively when the drug is administered, and carvedilol itself can mask the signs of hypoglycemia, it is very important to constantly monitor blood glucose levels.

Clonidine.

When discontinuing combination therapy with Carvetrend and clonidine, stop using the former first and then gradually reduce the dose of clonidine.

Anesthetics administered by inhalation.

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

Drugs that induce or inhibit the action of hemoprotein 450 enzymes.

Individuals using medications that induce enzymes of the hemoprotein 450 structure (barbiturates with rifampicin) or inhibit them (including ketoconazole, erythromycin with cimetidine, haloperidol and verapamil with fluoxetine) should be under constant supervision when using such drugs simultaneously with carvedilol, because enzyme inducers can reduce serum levels of the latter, and inhibitors can increase them.

Estrogens with NSAIDs and corticosteroids.

The hypotensive effect of drugs is reduced in the case of using medications that retain Na and fluid in the body.

Sympathomimetics and α- and ß-adrenergic agonists.

Administration together with these drugs potentiates the vasoconstrictive effect.

Muscle relaxants and ergotamine.

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

Xanthine derivatives.

It is necessary to be extremely careful when combining the drug with xanthine derivatives (this includes theophylline and aminophylline), because this weakens the β-adrenergic blocking activity.

Storage conditions

Carvetrend should be stored at temperatures in the range of 15-25°C.

Shelf life

Carvetrend can be used for a period of 36 months from the date of sale of the therapeutic substance.

Analogues

The analogs of the drug are Atram, Kardivas and Coriol with Karvid, as well as Dilator, Cardoz and Carvedigamma with Karvidex, Carvedilol and Cardiostad with Protecard, as well as Karvium, Talliton and Corvazan with Medocardil.