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CARVID Carvedilol 6.25mg Tablet 1's

RXDRUG-DR-XY36161-1pc
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Description

Indications/Uses

Hypertension: Management of essential hypertension. May be used alone or in combination with other antihypertensives.
Angina Pectoris: Prophylactic treatment of stable angina.
Symptomatic, Stable, Chronic Heart Failure: Treatment of mild to severe chronic heart failure of ischemic or cardiomyopathic origin in combination with diuretics, ACE inhibitors and digitalis, to increase survival and, also, to decrease the risk of hospitalization.
Left Ventricular Dysfunction Following Myocardial Infarction: Decreases cardiovascular mortality in clinically stable patients who have survived the acute phase of a myocardial infarction and have a left ventricular ejection fraction of ≤40% (with or without symptomatic heart failure).

Dosage/Direction for Use

General Dosing Recommendations: Carvedilol dosage must be individualized and closely monitored by a physician.
Fluid retention should be minimized before starting carvedilol treatment.
Carvedilol treatment is a long-term therapy. Do not discontinue treatment abruptly but rather gradually reduce at weekly intervals. This is particularly important in patients with concomitant coronary heart disease.
Recommended Oral Carvedilol Dose: Hypertension: Recommended Starting Dose: 12.5 mg once daily or 6.25 mg twice daily.
Thereafter, the recommended dosage is 25 mg once daily or 12.5 mg twice daily.
Dosage may be increased at intervals of at least 2 weeks to the maximum recommended dose of 50 mg, given once daily or in divided doses (twice daily).
The full antihypertensive effect of carvedilol is seen within 7-14 days.
Co-administration with a diuretic may produce additive effects and exaggerate the orthostatic component of carvedilol.
Angina Pectoris: Adults: Recommended Starting Dose: 12.5 mg twice daily for the first 2 days. Thereafter, the recommended dosage is 25 mg twice daily.
Dosage may be increased at intervals of at least 2 weeks to the maximum recommended dose of 100 mg, given in divided doses (twice daily).
Elderly: Recommended Maximum Dose: 50 mg given in divided doses (twice daily).
Symptomatic, Stable, Chronic Heart Failure: In patients receiving diuretics and/or digoxin and/or ACE inhibitors, dosing of these other drugs should be stabilized before starting carvedilol.
Recommended Starting Dose: 3.125 mg twice daily for 2 weeks.
If this dose is tolerated, dosage should be increased subsequently to 6.25 mg twice daily, followed by 12.5 mg twice daily and thereafter 25 mg twice daily, at intervals of not less than 2 weeks. Maintain patients on lower doses if higher doses are not tolerated.
At initiation of each new dose, observe patients for signs of dizziness or light-headedness for 1 hr.
Maximum Recommended Dose: Patients with Severe Heart Failure; Mild to Moderate Heart Failure Weighing <85 kg (187 lbs): 25 mg twice daily. Patients with Mild to Moderate Heart Failure Weighing >85 kg: 50 mg twice daily.
Treat fluid retention (with or without transient worsening heart failure symptoms) with increased doses of diuretics. Occasionally, it may be necessary to lower carvedilol dose and, rarely, temporarily discontinue carvedilol.
If carvedilol treatment is discontinued for >1 week, resume therapy at half the dose the patient is previously taking and up-titrate in line with the above dosing recommendation. If carvedilol treatment is discontinued for >2 weeks, resume therapy at 3.125 mg twice daily and up-titrate in line with the above dosing recommendation.

Overdosage

Quantities ingested in carvedilol overdose cases exceeded 1000 mg.
Symptoms: Severe hypotension, bradycardia, cardiac insufficiency, cardiogenic shock, and cardiac arrest. Respiratory problems, bronchospasms, vomiting, lapses of consciousness, and generalized seizures may also occur.
Treatment: Place the patient in a supine position and, where necessary, keep under observation and treat under intensive-care conditions. Gastric lavage or pharmacologically induced emesis may be used shortly after ingestion. The following agents may be administered:
For excessive bradycardia: Atropine 2 mg IV.
To support cardiovascular function: Glucagon 5-10 mg IV rapidly over 30 sec, followed by a continuous infusion of 5 mg/hr. Sympathomimetics (eg, dobutamine, isoprenaline, epinephrine) at doses according to body weight and effect. If positive inotropic effect is required, phosphodiesterase (PDE) inhibitors (eg, milrinone) must be considered. If peripheral vasodilation dominates, it may be necessary to administer epinephrine or norepinephrine with continuous monitoring of circulatory conditions.
For therapy-resistant bradycardia, pacemaker therapy should be performed.
For bronchospasm, β-sympathomimetics (as aerosol or IV) or aminophylline IV should be given. In the event of seizures, slow IV injection of diazepam or clonazepam is recommended.

Administration

Should be taken with food.

Contraindications

Hypersensitivity to any component of the Carvid tablet; unstable/decompensated heart failure; clinically manifest hepatic impairment; marked fluid retention or overload requiring IV inotropic support; second or third degree AV block (unless a permanent pacemaker is in place); severe bradycardia (<50 beats/min); sick-sinus syndrome (including sino-atrial block); severe hypotension (systolic blood pressure <85 mm Hg); cardiogenic shock; metabolic acidosis; history of bronchospasm or asthma, or other obstructive lung disorders.

Special Precautions

Cessation of Carvedilol Therapy: Advise patients with coronary artery disease against abrupt discontinuation of therapy. Severe exacerbation of angina and occurrence of myocardial infarction and ventricular arrhythmias have been reported in angina patients after the abrupt discontinuation of β-blocker therapy. When discontinuation of carvedilol is planned, carefully observe patient and advise to limit physical activity to a minimum. Carvedilol should be discontinued over 1-2 weeks whenever possible. If angina worsens or acute coronary insufficiency develops, carvedilol should be promptly reinstituted, at least temporarily. It may be prudent not to discontinue carvedilol abruptly even in patients treated only for hypertension or heart failure since coronary artery disease is common and may be unrecognized.
Bradycardia: Carvedilol may cause bradycardia. Reduce carvedilol dose if pulse rate drops <55 beats/min.
Hypotension: Starting with a low dose, administration with food, and gradual up-titration should decrease the possibility of syncope or excessive hypotension. During initiation of carvedilol treatment, advise the patient to avoid situations such as driving or hazardous tasks, where injury could result should syncope occur.
Heart Failure/Fluid Retention: Worsening heart failure or fluid retention may occur during up-titration of carvedilol patients with heart failure. If such symptoms occur, diuretics should be increased and carvedilol dose should not be advanced until clinical stabilization occurs. Occasionally, decreasing carvedilol dose may be necessary or, in rare cases, temporarily discontinue carvedilol. Such episodes do not preclude subsequent successful carvedilol titration. Carvedilol should be used with caution in combination with digitalis glycosides, as both medicines slow AV conduction.
Non-Allergic Bronchospasm: In general, patients with bronchospastic disease (eg, chronic bronchitis and emphysema) should not receive β-blockers. However, carvedilol should be used with caution in patients who do not respond to, or cannot tolerate, other antihypertensives. If carvedilol is used, it is prudent to use the lowest effective dose, so that inhibition of endogenous or exogenous β-agonists is minimized.
Diabetes and Hypoglycemia: β-blockers may mask some of the manifestations of hypoglycemia, particularly tachycardia. Nonselective β-blockers may potentiate insulin-induced hypoglycemia and delay recovery of serum glucose levels. Patients subject to spontaneous hypoglycemia, or diabetic patients receiving insulin or oral hypoglycemic agents, should be cautioned about these possibilities and carvedilol should be used with caution. In congestive heart failure patients, there is a risk of worsening hyperglycemia, which responds to intensification of hypoglycemic therapy. Blood glucose should be monitored when carvedilol dosing is started, adjusted, or discontinued.
Peripheral Vascular Disease: β-blockers can precipitate or aggravate symptoms of arterial insufficiency in patients with peripheral vascular disease. Exercise caution in such individuals.

Use In Pregnancy & Lactation

Pregnancy Category C: β-blockers decrease placental perfusion, which may result in intrauterine fetal death, and immature and premature deliveries. Also, adverse effects (particularly hypoglycemia and bradycardia) may occur in the fetus and neonate. An increased risk of cardiac and pulmonary complications in the neonate in the postnatal period may be observed. There are no adequate and controlled studies to date using carvedilol in pregnant women. Carvedilol should be used in pregnancy only when the potential benefits justify the potential risks to the fetus.
Use in lactation: In animal studies, carvedilol and its metabolites are excreted in breast milk. It is not known whether carvedilol is excreted in human milk. Thus, breastfeeding is not recommended during carvedilol administration.

Adverse Reactions

Body as a Whole: Asthenia, allergy, fatigue, fever, hypovolemia, malaise, edema (generalized, peripheral, dependent, genital, leg, hypervolemia, fluid overload), flu syndrome, pain in extremities.
Cardiovascular: Bradycardia, hypotension/postural hypotension, fluid overload, syncope (including presyncope), AV block, palpitation, angina pectoris (including chest pain), cardiac failure, hypertension, peripheral ischemia, tachycardia, bundle branch block, myocardial ischemia, peripheral circulation disturbances (eg, cold extremities, peripheral vascular disorder, exacerbation of intermittent claudication, Reynaud's phenomenon).
Gastrointestinal: Diarrhea, nausea, vomiting, melena, periodontitis, gastrointestinal pain, abdominal pain, bilirubinemia, dry mouth, gastrointestinal hemorrhage, constipation.
Hematologic: Prolongation of prothrombin time, purpura, thrombocytopenia, anemia, leukopenia, pancytopenia, atypical lymphocytes, aplastic anemia (rare).
Metabolic and Nutritional: Hyperglycemia, hypoglycemia, hyperuricemia, hyponatremia, hypercholesterolemia, hyperkalemia, hypokalemia, hypertriglyceridemia, glycosuria, weight increase, weight loss, diabetes mellitus, gout; Elevations of the following: alkaline phosphatase, aspartate aminotransferase (AST), alanine aminotransferase (ALT), γ-glutamyl transferase (GGT), blood urea nitrogen (BUN), non-protein nitrogen (NPN), creatinine; decreased high-density lipoprotein.

Drug Interactions

Inhibitors of CYP2D6; Poor Metabolizers of Debrisoquin: Interactions of carvedilol with strong inhibitors of CYP2D6 (eg, quinidine, fluoxetine, paroxetine, and propafenone) have not been studied, but these drugs would be expected to increase blood levels of the R(+) enantiomer of carvedilol. In clinical studies, poor 2D6 metabolizers had a higher rate of dizziness during up-titration resulting from the vasodilating effects of the higher concentrations of the α-blocking R(+) enantiomer.
Catecholamine Depleting Agents: Patients taking both agents with β-blocking properties and a drug that can deplete catecholamines (eg, reserpine and monoamine oxidase inhibitors) should be observed closely for signs of hypotension and/or severe bradycardia.
Clonidine: Concomitant administration of clonidine with agents with β-blocking properties may potentiate blood pressure- and heart-rate-lowering effects. When concomitant treatment with agents with β-blocking properties and clonidine is to be terminated, the β-blocking agent should be discontinued first. Clonidine therapy can then be discontinued several days later by gradually decreasing the dosage.
Cyclosporin: Due to wide interindividual variability in the dose adjustment required, it is recommended that cyclosporin concentrations be monitored closely after initiation of carvedilol and that the dose of cyclosporin be adjusted as appropriate.
Digoxin: Both carvedilol and digoxin slow atrioventricular conduction and decrease heart rate. Concomitant use may increase the risk of bradycardia. Digoxin concentrations are increased by about 15% when digoxin and carvedilol are administered concomitantly. Thus, increased monitoring of digoxin is recommended when initiating, adjusting, or discontinuing carvedilol.
Inducers and Inhibitors of Hepatic Metabolism: Rifampicin reduced plasma concentrations of carvedilol by about 70%. Cimetidine increased AUC by about 30% but caused no change in Cmax. Exercise caution in patients taking inducers of mixed function oxidases (eg, rifampicin) as serum carvedilol levels may be decreased, or inhibitors of mixed function oxidases (eg, cimetidine) as serum carvedilol levels may be increased.

Storage

Store at temperatures not exceeding 30°C.

Action

Pharmacology: Pharmacodynamics: Carvedilol is a racemic mixture in which nonselective β-adrenoceptor blocking activity is present in the S(-) enantiomer and alpha-adrenergic blocking activity in both R(+) and S(-) enantiomers at equal potency. It has no intrinsic sympathomimetic activity and has membrane-stabilizing properties.
Carvedilol is a potent antioxidant, a scavenger of reactive oxygen radicals, and an antiproliferative agent.
Carvedilol has no adverse effect on lipid profile. The normal ratio of high-density lipoproteins to low density lipoproteins (HDL/LDL) is maintained.
Vasodilation resulting in decreased total peripheral resistance mediated through carvedilol's α1-adrenergic blockade and decreased sympathetic tone plays a major role in the drug's hypotensive effects. Carvedilol causes reductions in cardiac output, exercise-induced tachycardia, isoproterenol-induced tachycardia, and reflex orthostatic tachycardia. Significant β-blocking activity of carvedilol is usually observed within 1 hr of oral use.
Carvedilol's α-adrenergic blocking effects, which contribute to the drug's hypotensive effects, are seen within 30 min of drug administration and include reduction in phenylephrine-induced pressor effects, vasodilation, and decreased peripheral vascular resistance. The dose-dependent hypotensive effect of carvedilol results in blood pressure (systolic and diastolic) reductions of 5-46% with little, if any, reflex tachycardia. This hypotensive effect occurs about 30 min after oral use and has a maximum effect 1.5-7 hrs after oral administration.
Due to carvedilol's α1-receptor blocking activity, blood pressure is reduced more in the standing than in the supine position, and symptoms of postural hypotension, including rare instances of syncope, may occur. The frequency and severity of orthostatic hypotension may be decreased by administering carvedilol with food and by strictly adhering to the usual starting dose and titration recommendations.

MedsGo Class

Beta-Blockers

Features

Brand
Carvid
Full Details
Dosage Strength
6.25 mg
Drug Ingredients
  • Carvedilol
Drug Packaging
Tablet 1's
Generic Name
Carvedilol
Dosage Form
Tablet
Registration Number
DR-XY36161
Drug Classification
Prescription Drug (RX)
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