Table of Contents
What is Carvedilol?
Carvedilol is a drug used for the treatment of high blood pressure, ischemic heart disease and chronic heart failure. The product ingredient is Carvedilol phosphate.
The brand names of Carvedilol in the United States are: Coreg, Coreg CR.
Mechanism of action (MOA) of Carvedilol
ß-vasodilator blocker (selective blocking of alpha-1 adrenoreceptors) non-selective with antioxidant properties.
Without intrinsic sympathomimetic activity and with membrane stabilizing properties.
Therapeutic indications, uses and benefits of Carvedilol:
- High blood pressure (HBP).
- Prolonged treatment of ischemic heart disease (chronic stable angina, silent myocardial ischemia, unstable angina and ischemic dysfunction of the left ventricle).
- Symptomatic moderate to severe Chronic Heart Failure (CHF).
Posology of Carvedilol
Oral dose
Adults:
– High blood pressure: 12.5 mg/day for the first 2 days, continue with 25 mg/day. If necessary, increase at intervals of 2 weeks to 50 mg/day or 25 mg/12 h.
Elderly: 12.5 mg/day, if necessary, adjust doses at 2-week intervals.
– Prolonged treatment of ischemic heart disease: 12.5 mg/12 h for the first 2 days, continue with 25 mg/12 h. If necessary, increase at 2-week intervals to 50 mg/12 h (max. dose).
Elderly people max. dose 25 mg/12 h.
– Moderate-severe symptomatic chronic heart failure: to be determined individually and monitored during dose adjustment. Initial: 3.125 mg/12 h for 2 weeks.
If well tolerated, increase at 2-week intervals to 6.25 mg/12 h, followed by 12.5 mg/12 h until 25 mg/12 h is reached.
Patients with body weight < 85 kg max. dose 25 mg/12 h and with p.c. >85 kg: 50 mg/12 h.
Method of administration of Carvedilol
Oral use:
Administer with or without food.
In case of heart failure administer with food to reduce the risk of orthostatic hypotension.
Contraindications of Carvedilol
- Hypersensitivity; NYHA class IV cardiac insuff. requiring treatment with IV inotropics; COPD with bronchial obstruction; liver dysfunction.
- Bronchial asthma; 2nd and 3rd degree A-V block; severe bradycardia (< 50 bpm); cardiogenic shock.
- Sinus disease (including sinus-auricular node blockage); severe hypotension (systolic pressure < 85 mm Hg); metabolic acidosis; Prinzmetal angina.
- Untreated pheochromocytoma; severe peripheral arterial circulatory disturbances; concomitant IV treatment with verapamil or diltiazem.
Warnings and precautions with Carvedilol
Chronic heart failure controlled with digitalis, diuretics and/or ACEi, diabetes mellitus (masks symptoms of hypoglycemia), peripheral vasculopathy, peripheral circulatory disorders (Raynaud’s disease), general surgery, 1st degree heart block, with a history of severe hypersensitivity reactions as well as undergoing desensitization therapy, labile or secondary hypertension, if pheochromocytoma or Prinzmetal vasospastic angina is suspected, if necessary to treat a NYHA class IV CHF.
Assess benefit/risk in: history of psoriasis associated with ß-blocker therapy and COPD with bronchospastic component and without receiving pharmacological tto.
In patients prone to bronchospasm, close monitoring at the onset of treatment and dose adjustment.
Masks the symptoms of thyrotoxicosis.
Concomitant with Ca antagonists, verapamil or diltiazem type, or other antiarrhythmics, ECG monitoring and blood pressure.
With CHF and low blood pressure (systolic BP < 100 mm Hg), ischemic heart disease and diffuse vascular disease and/or underlying renal failure, control renal function by increasing the dose and, stop or reduce if it worsens.
Gradual withdrawal from treatment.
Not recommended in children and adolescents < 18 years.
Liver failure
Contraindicated in clinically manifest liver dysfunction.
Renal insufficiency
Caution. In CHF with systolic BP < 100 mm Hg, ischemic heart disease and diffuse vascular disease and/or underlying renal failure, renal function should be controlled while increasing the dose, drug administration should be discontinued or the dose reduced if renal function worsens.
Interactions with Carvedilol
- Increases risk of alterations in AV conduction with: verapamil, diltiazem, antiarrhythmic class I; contraindicated by IV.
- Risk of prolongation of atrioventricular conduction time with: digoxin.
- Increases blood pressure and decreases heart rate with: clonidine.
- Power effect of: insulin and oral antidiabetics.
- Risk of hypotension and/or severe bradycardia with: reserpine, MAOI.
- Increased concentration of: cyclosporine.
- Synergy of negative inotropic and hypotensive effects with: anaesthetics.
- Plasma levels decreased by: rifampicin.
- Plasma levels increased by: SSRIs, fluoxetine, paroxetine, quinidine, propafenone, cimetidine.
- Increases blood pressure with: NSAIDS.
Pregnancy
Carvedilol should not be used during pregnancy unless the expected benefits far outweigh the potential risks.
Breastfeeding
Carvedilol is lipophilic and according to the results of studies conducted in lactating animals, carvedilol and its metabolites are excreted in breast milk and therefore breastfeeding is not recommended during administration of carvedilol.
Effects on driving ability
Some people may see their alertness reduced especially at the start of treatment or when medication is adjusted.
Side effects of Carvedilol
Headaches, dizziness, fatigue and asthenia; depressed mood, depression.
Heart failure, bradycardia, edema, hypervolemia, fluid overload; hypotension, postural hypotension, peripheral circulation disorders (cold extremities), exacerbation of symptoms in patients with intermittent claudication or Raynaud’s phenomenon, peripheral edema.
Asthma and dyspnea in predisposed patients, pulmonary edema; gastrointestinal discomfort (nausea, diarrhoea, abdominal pain, dyspepsia, vomiting); anemia; decreased tearing, eye irritation, vision alterations.
Abnormalities of renal function in patients with diffuse vascular disease or underlying renal disease, acute renal failure, urination disorders.
Pain in the extremities; weight gain, hypercholesterolemia, worsening of blood glucose control (hyperglycemia, hypoglycemia) in patients with pre-existing diabetes; asthenia (fatigue), pain.
⭐⭐⭐⭐⭐ VIDEO OF CARVEDILOL/COREG (DRUG)
Source: The content of this active ingredient has been written taking into account the clinical and molecular information of all medicines authorised and marketed in the United States under the Unique Ingredient Identifier (UNII) by the Substance Registration System (SRS) of the Food and Drug Administration (FDA) and the United States Pharmacopeia (USP).
In order to know in detail the information authorized by the FDA for each drug, you should consult the corresponding medication guide authorized by the FDA.
Resources:
UNII: 0K47UL67F2
ChemIDplus
DrugPortal
PubChem CID: 2585
NCI Thesaurus: C28906