Product Description:
Rivaldo (Carvedilol) is a multi-action adrenergic receptor blocker with α1, β1, and β2 adrenergic receptor blocking properties.
Carvedilol has been shown to have organ-protective effects.
Carvedilol inhibits the renin-angiotensin-aldosterone system through β-blockade, which reduces renin secretion, making fluid retention rare.
Carvedilol reduces peripheral vascular resistance through selective blockade of alpha-1 receptors.
Carvedilol has no negative effect on the lipid profile. The normal ratio of high-density lipoproteins to low-density lipoproteins (HDL/LDL) is maintained.
Properties:
Absorption: Carvedilol is rapidly absorbed after oral administration. Peak plasma concentration is reached after approximately one to two hours. There is a significant first-pass metabolism, and the absolute bioavailability is about 25% (12-49%).
Distribution: The steady-state volume of distribution (VDss) is approximately 2 L/kg. Carvedilol is 98% bound to plasma proteins.
Metabolism: Carvedilol is almost completely broken down into compounds that are primarily eliminated via the biliary route. Carvedilol is mainly metabolized in the liver.
Elimination: The half-life of carvedilol after oral administration is about 6-10 hours. Plasma clearance is 590 ml/min. Elimination is predominantly biliary. The primary route of elimination is via feces. Less than 2% of the unchanged substance is eliminated via urine, and about 15% in the form of metabolites.
Indications:
Rivaldo is used in the following cases:
- Treatment of essential hypertension (mild to moderate) and chronic angina pectoris for the prevention of attacks.
- Treatment of mild to severe cases of stable heart failure (NYHA class II-IV) due to ischemic cardiomyopathy as an adjunct to standard therapy (diuretics, digoxin, ACE inhibitors).
Instructions for Use:
Essential Hypertension:
Adults: The initial dose of Raveldo 12.5 mg is given once daily for the first two days. Thereafter, a dose of 25 mg once daily is recommended. If the effect is insufficient, the daily dose can be increased after at least two weeks to 50 mg taken as a single dose or two doses of Rivaldo. The maximum daily dose for hypertension is 50 mg.
Elderly patients: Initially, a dose of 12.5 mg of Raveldo is given once a day. In some patients, this dose is sufficient for adequate blood pressure control. If the effect is insufficient, the daily dose can be gradually increased at intervals of at least two weeks to a maximum of 50 mg taken as a single dose or two individual doses.
Angina Pectoris:
The initial dose of Raveldo is 12.5 mg twice daily for the first two days. Thereafter, a dose of 25 mg twice daily is recommended. If the effect is insufficient, the dose can be gradually increased at intervals of at least two weeks up to a maximum daily dose of 100 mg taken as two individual doses.
Elderly patients: Generally, a dose of 25 mg of Raveldo twice daily should not be exceeded.
Treatment of severe mild heart failure (NYHA class II-IV):
The dose of Rivaldo must be determined individually, and the patient must be closely monitored during titration. The dose of digitalis, diuretics, and ACE inhibitors must be stabilized before starting Rivaldo. The recommended starting dose is 3.125 mg of Raveldo taken twice daily, then the dose is increased to 12.5 mg twice daily and then to 25 mg twice daily. The dose should be increased to the highest level tolerated by the patient. The maximum recommended dose is 25 mg twice daily for patients up to 85 kg and 50 mg twice daily for patients weighing more than 85 kg.
Before each dose increase, the physician must examine the patient for signs and symptoms of worsening heart failure, vasodilation (hypotension, dizziness), or bradycardia. Transient worsening of heart failure or fluid retention should be treated with increased doses of diuretics, although it will sometimes be necessary to reduce the dose of Raveldo or temporarily stop treatment.
If treatment with Raveldo is stopped for more than two weeks, it should be restarted at a dose of 3.125 mg; this dose should then be increased at two-week intervals, as described above.
Signs and symptoms of vasodilation should initially be treated by reducing the diuretic dose. If they persist, the ACE inhibitor dose should be reduced, and then the Raveldo dose should be reduced. Under these circumstances, the Raveldo dose should not be increased until signs and symptoms of worsening heart failure or vasodilation improve.
The safety and efficacy of Raveldo in patients under 18 years of age have not been investigated.
Patients with renal impairment: No initial dose reduction is required.
Patients with hepatic failure: Careful dose titration should be performed in case of hepatic impairment.
Rivaldo tablets should be taken with a sufficient amount of liquid. Patients with heart failure should take Raveldo tablets with food to slow the absorption rate and reduce the incidence of orthostatic effects.
Treatment with Raveldo is generally a long-term treatment. It should not be stopped abruptly but should be tapered over several days (e.g., by halving the dose every three days); this is especially important in patients who also have coronary artery disease.
Warnings and Precautions:
Contraindications:
- Hypersensitivity to the active substance or any of the excipients.
- Decompensated chronic heart failure (NYHA class II-IV) in patients requiring intravenous inotropic support.
- Chronic obstructive pulmonary disease (COPD).
- Bronchial asthma.
- Allergic rhinitis.
- Glottic edema.
- Cor pulmonale.
- Sick sinus syndrome (including sinoatrial block).
- Second and third-degree AV block.
- Severe bradycardia (less than 45-50 beats/min at rest).
- Cardiogenic shock.
- Myocardial infarction with complications.
- Clinically manifest liver failure.
- Metabolic acidosis.
- Concomitant administration of MAO inhibitors (except MAO-B inhibitors).
- Slow metabolizers of debrisoquine.
Precautions:
- Patients with pheochromocytoma can be treated with carvedilol only in conjunction with effective alpha-receptor blockade.
- Carvedilol should be used with caution in patients with uncompensated heart failure treated with digitalis, diuretics, and/or ACE inhibitors, as digitalis and carvedilol may prolong AV conduction and carvedilol may increase digitalis levels.
- Because therapeutic experience is insufficient, carvedilol should not be used in children.
- Labile or secondary hypertension, unstable angina, complete bundle branch block, end-stage peripheral arterial obstructive disease (as beta-blockers may cause or aggravate signs and symptoms of arterial insufficiency).
- Recent myocardial infarction or tendency to orthostatic hypotension, or in conjunction with certain antihypertensive agents (alpha-1 receptor antagonists).
- Beta-blocker treatment may increase sensitivity to allergens and exposure to severe anaphylactic reactions in patients with a history of serious hypersensitivity reactions undergoing desensitization therapy.
- Patients with psoriasis or a family history of psoriasis should be given beta-blocking drugs, including Carvedilol, only after careful risk-benefit analysis.
- Gradual dose reduction is recommended when stopping carvedilol in hypertensive patients with coronary heart disease.
- Bradycardia occurred in 2% of hypertensive patients and 9% of heart failure patients in clinical studies. If the heart rate is less than 55 beats/min, the dose should be reduced.
- Hypotension (9.7%) and syncope (4%) occurred in heart failure patients treated with carvedilol, primarily during the first 30 days (titration phase).
- Close monitoring of blood pressure and ECG parameters is required during concomitant treatment with calcium antagonists (verapamil or diltiazem type) or other antiarrhythmics.
- In elderly patients, the first dose may be followed by an excessive drop in blood pressure.
- Carvedilol may mask signs of hyperthyroidism (e.g., tachycardia) and hypoglycemia in diabetic patients. Regular blood glucose monitoring is required.
- Symptoms may worsen in patients with intermittent claudication or Raynaud's phenomenon.
- Contact lens wearers should be aware of the possibility of reduced lacrimation.
- Reversible deterioration of renal function has been observed in patients with decompensated heart failure and low blood pressure, coronary heart disease, or other vascular diseases.
Ingredients:
Rivaldo 25: Each film-coated tablet contains 25 mg of Carvedilol in packs of 30 tablets.
Product Details:
Brand: Raveldo
