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Medication Safety Issues
Sound-alike/look-alike issues:
Carvedilol may be confused with captopril, carteolol
International issues:
Talliton® [Hungary] may be confused with Talacen® which is a brand name for pentazocine/acetaminophen combination in the U.S.
Pronunciation
(KAR ve dil ole)
U.S. Brand Names
Generic Available
Yes: Tablet
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Mild-to-severe heart failure of ischemic or cardiomyopathic origin (usually in addition to standardized therapy); left ventricular dysfunction following myocardial infarction (MI) (clinically stable with LVEF ?40%); management of hypertension
Use: Unlabeled/Investigational
Angina pectoris
Pregnancy Risk Factor
C (manufacturer); D (2nd and 3rd trimesters - expert analysis)
Pregnancy Considerations
Postimplantation losses were observed in animal studies. No data available on whether carvedilol crosses the placenta. Beta-blockers have been associated with persistent bradycardia, hypotension, and IUGR; IUGR probably related to maternal hypertension. Cases of neonatal hypoglycemia have been reported following maternal use of beta-blockers at parturition or during breast-feeding.
Lactation
Excretion in breast milk unknown/not recommended
Contraindications
Hypersensitivity to carvedilol or any component of the formulation; decompensated cardiac failure requiring intravenous inotropic therapy; bronchial asthma or related bronchospastic conditions; second- or third-degree AV block, sick sinus syndrome, and severe bradycardia (except in patients with a functioning artificial pacemaker); cardiogenic shock; severe hepatic impairment; pregnancy (2nd and 3rd trimesters)
Warnings/Precautions
Concerns related to adverse effects:
• Anaphylactic reactions: Use caution with history of severe anaphylaxis to allergens; patients taking beta-blockers may become more sensitive to repeated challenges. Treatment of anaphylaxis (eg, epinephrine) in patients taking beta-blockers may be ineffective or promote undesirable effects.
• Liver injury: Manufacturer recommends discontinuation of therapy if liver injury occurs (confirmed by laboratory testing).
• Syncope: Patients should be advised to avoid driving or other hazardous tasks during initiation of therapy due to the risk of syncope.
Disease-related concerns:
• Bronchospastic disease: In general, patients with bronchospastic disease should not receive beta-blockers; if used at all, should be used cautiously with close monitoring.
• Conduction abnormality : Consider pre-existing conditions such as sick sinus syndrome before initiating.
• Diabetes: Use with caution in patients with diabetes mellitus; may potentiate hypoglycemia and/or mask signs and symptoms (eg, sweating, anxiety, tachycardia).
• Heart failure (HF): Heart failure patients may experience a worsening of renal function; risks include ischemic disease, diffuse vascular disease, underlying renal dysfunction; systolic BP <100 mm Hg. In severe chronic heart failure, trial patients were excluded if they had cardiac-related rales, ascites, or a serum creatinine >2.8 mg/dL.
• Hepatic impairment: Use with caution in patients with mild-to-moderate hepatic impairment; use is contraindicated in patients with severe hepatic impairment.
• Myasthenia gravis: Use with caution in patients with myasthenia gravis.
• Peripheral vascular disease (PVD): Use with caution in patients with PVD (including Raynaud's).
• Pheochromocytoma (untreated): Adequate alpha-blockade is required prior to use of any beta-blocker.
• Psychiatric disease: Use with caution in patients with a history of psychiatric illness; may cause or exacerbate CNS depression.
• Thyroid disease: May mask signs of hyperthyroidism (eg, tachycardia). If hyperthyroidism is suspected, carefully manage and monitor; abrupt withdrawal may precipitate thyroid storm.
Concurrent drug therapy issues:
• Anesthetic agents: Use with caution in patients receiving anesthetic agents which decrease myocardial function.
• Calcium channel blockers: Use with caution in patients on concurrent verapamil or diltiazem; bradycardia or heart block can occur.
Special populations:
• Pediatrics: Safety and efficacy have not been established in children.
Other warnings/precautions:
• Abrupt withdrawal: Beta-blocker therapy should not be withdrawn abruptly (particularly in patients with CAD), but gradually tapered to avoid acute tachycardia, hypertension, and/or ischemia.
• Initiation of therapy for CHF: Initiate cautiously and monitor for possible deterioration in patient status (including symptoms of CHF). Adjustment of other medications (ACE inhibitors and/or diuretics) may be required.
Adverse Reactions
Note: Frequency ranges include data from hypertension and heart failure trials. Higher rates of adverse reactions have generally been noted in patients with CHF. However, the frequency of adverse effects associated with placebo is also increased in this population. Events occurring at a frequency > placebo in clinical trials.
>10%:
Cardiovascular: Hypotension (9% to 20%)
Central nervous system: Dizziness (2% to 32%), fatigue (4% to 24%)
Endocrine & metabolic: Hyperglycemia (5% to 12%), weight gain (10% to 12%)
Gastrointestinal: Diarrhea (1% to 12%)
Neuromuscular & skeletal: Weakness (11%)
1% to 10%:
Cardiovascular: Bradycardia (2% to 10%), syncope (3% to 8%), peripheral edema (1% to 7%), generalized edema (5% to 6%), angina (2% to 6%), dependent edema (4%), AV block (3%), hypertension (3%), postural hypotension (2%), palpitation
Central nervous system: Headache (5% to 8%), fever (3%), somnolence (2%), insomnia (1% to 2%), malaise, hypoesthesia, vertigo
Endocrine & metabolic: Alkaline phosphatase increased, gout (6%), hypercholesterolemia (4%), dehydration (2%), hyperkalemia (3%), hypervolemia (2%), hypertriglyceridemia (1%), hyperuricemia, hypoglycemia, hyponatremia
Gastrointestinal: Nausea (2% to 9%), vomiting (6%), melena, periodontitis
Genitourinary: Hematuria (3%), impotence
Hematologic: Thrombocytopenia (1% to 2%), prothrombin decreased, purpura
Hepatic: Transaminases increased
Neuromuscular & skeletal: Back pain (2% to 7%), arthralgia (6%), myalgia (3%), muscle cramps, paresthesia (1%)
Ocular: Blurred vision (3% to 5%), lacrimation
Renal: BUN increased (6%), creatinine increased (3%), renal function abnormal, albuminuria, glycosuria, kidney failure
Respiratory: Cough increased (5%), nasopharyngitis (4%), rhinitis (2%), nasal congestion (1%), sinus congestion (1%)
Miscellaneous: Injury (3% to 6%), allergy, sudden death
<1%: Abnormal thinking, alopecia, amnesia, anaphylactoid reaction, anemia, asthma, atypical lymphocytes, AV block (complete), bilirubinemia, bronchospasm, bundle branch block, cerebrovascular disorder, concentration decreased, convulsion, depression exacerbation, diabetes mellitus, diaphoresis, emotional lability, erythematous rash, exfoliative dermatitis, GI hemorrhage, HDL-cholesterol decreased, hearing decreased, hypokalemia, hypokinesis, leukopenia, libido decreased (male), maculopapular rash, micturition (increased), migraine, myocardial ischemia, nervousness, neuralgia, pancytopenia, paranoia, paresis, peripheral ischemia, photosensitivity, pruritus, psoriasiform rash, pulmonary edema, respiratory alkalosis, sleep disorder, tachycardia, tinnitus, xerostomia
Postmarketing and/or case reports: Aplastic anemia (rare, all events occurred in patients receiving other medications capable of causing this effect), cholestatic jaundice, erythema multiforme, interstitial pneumonitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, urinary incontinence (women)
Metabolism/Transport Effects
Substrate of CYP1A2 (minor), 2C9 (major), 2D6 (major), 2E1 (minor), 3A4 (minor)
Drug Interactions
Acetylcholinesterase Inhibitors: May enhance the bradycardic effect of Beta-Blockers. Risk C: Monitor therapy
Alpha-/Beta-Agonists (Direct-Acting): Beta-Blockers may enhance the vasopressor effect of Alpha-/Beta-Agonists (Direct-Acting). Epinephrine used as a local anesthetic for dental procedures will not likely cause clinically relevant problems. Exceptions: Dipivefrin. Risk D: Consider therapy modification
Alpha1-Blockers: Beta-Blockers may enhance the orthostatic effect of Alpha1-Blockers. The risk associated with ophthalmic products is probably less than systemic products. Risk D: Consider therapy modification
Alpha2-Agonists: Beta-Blockers may enhance the rebound hypertensive effect of Alpha2-Agonists. This effect can occur when the alpha2-agonist is abruptly withdrawn. Exceptions: Apraclonidine; Brimonidine. Risk D: Consider therapy modification
Aminoquinolines (Antimalarial): May decrease the metabolism of Beta-Blockers. Risk C: Monitor therapy
Amiodarone: May enhance the bradycardic effect of Beta-Blockers. Possibly to the point of cardiac arrest. Risk D: Consider therapy modification
Anilidopiperidine Opioids: May enhance the bradycardic effect of Beta-Blockers. Anilidopiperidine Opioids may enhance the hypotensive effect of Beta-Blockers. Risk C: Monitor therapy
Antipsychotic Agents (Phenothiazines): May enhance the hypotensive effect of Beta-Blockers. Beta-Blockers may decrease the metabolism of Antipsychotic Agents (Phenothiazines). Antipsychotic Agents (Phenothiazines) may decrease the metabolism of Beta-Blockers. Risk C: Monitor therapy
Barbiturates: May decrease the serum concentration of Beta-Blockers. Risk C: Monitor therapy
Beta2-Agonists: Beta-Blockers (Nonselective) may diminish the bronchodilatory effect of Beta2-Agonists. Risk D: Consider therapy modification
Beta2-Agonists: Alpha-/Beta-Blockers may diminish the therapeutic effect of Beta2-Agonists. Risk D: Consider therapy modification
Calcium Channel Blockers (Nondihydropyridine): May enhance the hypotensive effect of Beta-Blockers. Bradycardia and signs of heart failure have also been reported. Calcium Channel Blockers (Nondihydropyridine) may increase the serum concentration of Beta-Blockers. Risk C: Monitor therapy
Cardiac Glycosides: Beta-Blockers may enhance the bradycardic effect of Cardiac Glycosides. Risk C: Monitor therapy
Cimetidine: May decrease the metabolism of Carvedilol. Risk C: Monitor therapy
CycloSPORINE: Carvedilol may increase the serum concentration of CycloSPORINE. Risk D: Consider therapy modification
CYP2D6 Inhibitors (Moderate): May decrease the metabolism of CYP2D6 Substrates. Risk C: Monitor therapy
CYP2D6 Inhibitors (Strong): May decrease the metabolism of CYP2D6 Substrates. Risk D: Consider therapy modification
Diazoxide: May enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy
Digoxin: Carvedilol may increase the serum concentration of Digoxin. Risk C: Monitor therapy
Dipyridamole: May enhance the bradycardic effect of Beta-Blockers. Risk C: Monitor therapy
Disopyramide: May enhance the bradycardic effect of Beta-Blockers. Risk C: Monitor therapy
Herbs (Hypertensive Properties): May diminish the antihypertensive effect of Antihypertensives. Risk C: Monitor therapy
Herbs (Hypotensive Properties): May enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy
Insulin: Beta-Blockers may enhance the hypoglycemic effect of Insulin. Risk C: Monitor therapy
Lidocaine: Beta-Blockers may decrease the metabolism of Lidocaine. Risk C: Monitor therapy
Methacholine: Beta-Blockers may enhance the adverse/toxic effect of Methacholine. Risk X: Avoid combination
Methylphenidate: May diminish the antihypertensive effect of Antihypertensives. Risk C: Monitor therapy
Midodrine: Beta-Blockers may enhance the bradycardic effect of Midodrine. Risk C: Monitor therapy
Nonsteroidal Anti-Inflammatory Agents: May diminish the antihypertensive effect of Beta-Blockers. Risk C: Monitor therapy
Propafenone: May decrease the metabolism of Beta-Blockers. Propafenone possesses some independent beta blocking activity. Risk C: Monitor therapy
Propoxyphene: May decrease the metabolism of Beta-Blockers. Risk C: Monitor therapy
Prostacyclin Analogues: May enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy
Quinidine: May decrease the metabolism of Beta-Blockers. Risk C: Monitor therapy
Rifamycin Derivatives: May decrease the serum concentration of Beta-Blockers. Exceptions: Rifabutin. Risk C: Monitor therapy
Rituximab: Antihypertensives may enhance the hypotensive effect of Rituximab. Risk D: Consider therapy modification
Selective Serotonin Reuptake Inhibitors: May decrease the metabolism of Alpha-/Beta-Blockers. Exceptions: Fluvoxamine. Risk C: Monitor therapy
Selective Serotonin Reuptake Inhibitors: May enhance the bradycardic effect of Beta-Blockers. Exceptions: Fluvoxamine. Risk C: Monitor therapy
Theophylline Derivatives: Beta-Blockers (Nonselective) may diminish the bronchodilatory effect of Theophylline Derivatives. Risk D: Consider therapy modification
Topotecan: P-Glycoprotein Inhibitors may increase the serum concentration of Topotecan. Risk X: Avoid combination
Ethanol/Nutrition/Herb Interactions
Food: Food decreases rate but not extent of absorption. Administration with food minimizes risks of orthostatic hypotension.
Herb/Nutraceutical: Avoid herbs with hypertensive properties (bayberry, blue cohosh, cayenne, ephedra, ginger, ginseng [American], kola, licorice); may diminish the antihypertensive effect of carvedilol. Avoid herbs with hypotensive properties (black cohosh, California poppy, coleus, golden seal, hawthorn, mistletoe, periwinkle, quinine, shepherd's purse); may enhance the hypotensive effect of carvedilol.
Storage
Store at 15°C to 30°C (59°F to 86°F).
Mechanism of Action
As a racemic mixture, carvedilol has nonselective beta-adrenoreceptor and alpha-adrenergic blocking activity. No intrinsic sympathomimetic activity has been documented. Associated effects in hypertensive patients include reduction of cardiac output, exercise- or beta-agonist-induced tachycardia, reduction of reflex orthostatic tachycardia, vasodilation, decreased peripheral vascular resistance (especially in standing position), decreased renal vascular resistance, reduced plasma renin activity, and increased levels of atrial natriuretic peptide. In CHF, associated effects include decreased pulmonary capillary wedge pressure, decreased pulmonary artery pressure, decreased heart rate, decreased systemic vascular resistance, increased stroke volume index, and decreased right arterial pressure (RAP).
Pharmacodynamics/Kinetics
Onset of action: 1-2 hours
Peak antihypertensive effect: ?1-2 hours
Absorption: Rapid and extensive
Distribution: Vd: 115 L
Protein binding: >98%, primarily to albumin
Metabolism: Extensively hepatic, via CYP2C9, 2D6, 3A4, and 2C19 (2% excreted unchanged); three active metabolites (4-hydroxyphenyl metabolite is 13 times more potent than parent drug for beta-blockade); first-pass effect; plasma concentrations in the elderly and those with cirrhotic liver disease are 50% and 4-7 times higher, respectively
Bioavailability: Immediate release: 25% to 35% (due to significant first-pass metabolism); Extended release: 85% of immediate release
Half-life elimination: 7-10 hours
Time to peak, plasma: Extended release: 5 hours
Excretion: Primarily feces
Dosage
Oral: Adults: Reduce dosage if heart rate drops to <55 beats/minute.
Hypertension:
Immediate release: 6.25 mg twice daily; if tolerated, dose should be maintained for 1-2 weeks, then increased to 12.5 mg twice daily. Dosage may be increased to a maximum of 25 mg twice daily after 1-2 weeks; maximum dose: 50 mg/day.
Extended release: Initial: 20 mg once daily, if tolerated, dose should be maintained for 1-2 weeks then increased to 40 mg once daily if necessary; maximum dose: 80 mg once daily
Congestive heart failure:
Immediate release: 3.125 mg twice daily for 2 weeks; if this dose is tolerated, may increase to 6.25 mg twice daily. Double the dose every 2 weeks to the highest dose tolerated by patient. (Prior to initiating therapy, other heart failure medications should be stabilized and fluid retention minimized.)
Maximum recommended dose:
Mild-to-moderate heart failure:
<85 kg: 25 mg twice daily
>85 kg: 50 mg twice daily
Severe heart failure: 25 mg twice daily
Extended release: Initial: 10 mg once daily for 2 weeks; if the dose is tolerated, increase dose to 20 mg, 40 mg, and 80 mg over successive intervals of at least 2 weeks. Maintain on lower dose if higher dose is not tolerated.
Left ventricular dysfunction following MI: Note: Should be initiated only after patient is hemodynamically stable and fluid retention has been minimized.
Immediate release: Initial 3.125-6.25 mg twice daily; increase dosage incrementally (ie, from 6.25-12.5 mg twice daily) at intervals of 3-10 days, based on tolerance, to a target dose of 25 mg twice daily.
Extended release: Initial: 20 mg once daily; increase dosage incrementally at intervals of 3-10 days. Target dose: 80 mg once daily.
Angina pectoris (unlabeled use): Immediate release: 25-50 mg twice daily
Conversion from immediate release to extended release (Coreg CR™):
Current dose immediate release tablets 3.125 mg twice daily: Convert to extended release capsules 10 mg once daily
Current dose immediate release tablets 6.25 mg twice daily: Convert to extended release capsules 20 mg once daily
Current dose immediate release tablets 12.5 mg twice daily: Convert to extended release capsules 40 mg once daily
Current dose immediate release tablets 25 mg twice daily: Convert to extended release capsules 80 mg once daily
Dosing adjustment in renal impairment: None necessary
Dosing adjustment in hepatic impairment: Use is contraindicated in severe liver dysfunction.
Administration: Oral
Administer with food. Extended release capsules should not be crushed or chewed. Capsules may be opened and sprinkled on applesauce for immediate use.
Monitoring Parameters
Heart rate, blood pressure (base need for dosage increase on trough blood pressure measurements and for tolerance on standing systolic pressure 1 hour after dosing); renal studies, BUN, liver function; in patient with increase risk for developing renal dysfunction, monitor during dosage titration.
Dietary Considerations
Should be taken with food to minimize the risk of orthostatic hypotension.
Patient Education
Do not take any new medication during therapy unless approved by prescriber. Take exactly as directed. Do not alter dose or discontinue this medication without consulting prescriber. Take pulse daily, prior to taking medication; follow prescriber's instruction about holding medication. If you have diabetes, monitor serum glucose closely (drug may alter glucose tolerance or mask signs of hypoglycemia). You may experience fatigue, dizziness, or postural hypotension (use caution when changing position from lying or sitting to standing, driving, or climbing stairs until response to medication is known); decrease in tear production; alteration in sexual performance (reversible); or diarrhea (buttermilk, boiled milk, or yogurt may help). Report unresolved swelling of extremities; respiratory difficulty or new cough; unresolved fatigue; unusual weight gain (>5 lb/week); unresolved constipation or diarrhea; or unusual muscle weakness. Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Do not get pregnant while taking this medications. Consult prescriber for appropriate contraceptive use. Do not breast-feed.
Geriatric Considerations
Due to alterations in the beta-adrenergic autonomic nervous system, beta-adrenergic blockade may result in less hemodynamic response than seen in younger adults. In U.S. trials conducted by the manufacturer, hypertension patients who were elderly (>65%) had a higher incidence of dizziness (8.8% vs 6%) than seen in younger patients. No other differences noted between young and old in these trials.
Additional Information
Fluid retention during therapy should be treated with an increase in diuretic dosage.
Anesthesia and Critical Care Concerns/Other Considerations
Surgery: The ACC/AHA 2007 guidelines on perioperative cardiovascular evaluation and care for noncardiac surgery recommend beta-blockers be continued in patients undergoing surgery who are receiving beta-blockers to treat angina, symptomatic arrhythmias, hypertension, or other ACC/AHA Class I guideline indications (Class I recommendation). The guidelines also recommend that beta-blockers be given to patients undergoing vascular surgery who have myocardial ischemia demonstrated during preoperative testing (Class I recommendation). More recent clinical trials have not shown a benefit to perioperative beta-blockade for non-cardiac surgery (Juul, 2006; Yang, 2006); however, the majority of previously published trials suggest a benefit.
Based on available evidence, beta-blockers should be started days to weeks before elective surgery when possible and titrated to a heart rate <65 beats per minute. Additional data suggest that long-acting beta-blockers may be superior to short-acting ones.
Withdrawal: Beta-blocker therapy should not be withdrawn abruptly, but gradually tapered to avoid acute tachycardia and hypertension.
Cardiovascular Considerations
Atrial Fibrillation: Beta-blocker therapy provides effective rate control in patients with atrial fibrillation.
Chronic Stable Angina: Beta-blockers are effective in the treatment of chronic stable angina as monotherapy or when combined with nitrates and/or calcium channel blockers. In patients with severe intractable angina requiring negative cardiac chronotropic medications, pacemaker placement has been carried out to maintain heart rate in the setting of large doses of beta-blockers and/or calcium channel blockers. Beta-blockers are ineffective in the treatment of pure vasospastic (Prinzmetal) angina.
Heart Failure: Strong evidence supports that beta-blocker therapy, without intrinsic sympathomimetic activity (ISA), should be initiated in select patients with stable congestive heart failure (NYHA Class II-III). Carvedilol is a nonselective beta-blocker with alpha-blocking and antioxidant properties. To date, carvedilol, sustained release metoprolol, and bisoprolol have demonstrated a beneficial effect on morbidity and mortality. It is important that beta-blocker therapy be instituted initially at very low doses with gradual and very careful titration. Because carvedilol has alpha-adrenergic blocking effects, it may lower blood pressure to a greater extent. The definitive clinical benefits of the antioxidant property are not known at this time.
Hypertension: Beta-blocker therapy in the treatment of hypertension has been associated with improved cardiovascular outcomes. According to the 2003 JNC-VII guidelines for the treatment of hypertension, most patients with hypertension will require treatment with at least 2 antihypertensives. First-line therapy for hypertension is a diuretic (eg, hydrochlorothiazide or chlorthalidone). When a diuretic cannot be used or when a compelling indication exists that requires the use of other drugs, other types of antihypertensives may be used (eg, ACEIs, ARBs, beta-blockers, CCBs). Beta-blockers are among the multiple choices of agents that have shown benefit in a number of different patient subtypes. Compelling indications for a beta-blocker include patients with heart failure, postmyocardial infarction, high coronary disease risk, or diabetes. In type 2 diabetic patients, a UK Prospective Diabetes Study Group (UKPDS) trial showed that beta-blocker therapy (atenolol) was as effective as an ACE inhibitor in reducing cardiovascular events and that the benefits of therapy were related more to the degree of antihypertensive efficacy rather than the class of drug used.
Treatment should be targeted to a goal blood pressure of <140/90 mm Hg. If diabetes or renal disease coexists, the blood pressure goal should be <130/80 mm Hg.
ST-Segment Elevation Myocardial Infarction (STEMI): Beta-blockers, without intrinsic sympathomimetic activity (ISA), have been shown to decrease morbidity and mortality when initiated in the acute treatment of STEMI and continued long-term. Oral beta-blockade should be initiated promptly in patients without contraindications (eg, signs of heart failure, evidence of a low output state, risk of cardiogenic shock, or other beta-blocker contraindications) (Class I recommendation). Use of intravenous beta-blockade may be considered and given promptly if the patient is experiencing concomitant hypertension or a tachyarrhythmia (Class IIa recommendation).
Unstable Angina/Non-ST-Segment Elevation MI (UA/NSTEMI): In the treatment of UA/NSTEMI, oral beta-blockade should be initiated within the first 24 hours in patients without contraindications (eg, signs of heart failure, evidence of a low output state, risk of cardiogenic shock, or other beta-blocker contraindications) (Class I recommendation). Use of intravenous beta-blockade should only be considered if the patient is experiencing concomitant hypertension upon presentation (Class IIa recommendation).
Withdrawal: Beta-blocker therapy should not be withdrawn abruptly, but gradually tapered to avoid acute tachycardia and hypertension.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Postural hypotension. Periodontitis has been reported in product labeling for carvedilol; no other reports have confirmed this effect; any possible mechanism for this effect is unknown. Many nonsteroidal anti-inflammatory drugs, such as ibuprofen and indomethacin, can reduce the hypotensive effect of beta-blockers after 3 or more weeks of therapy with the NSAID. Short-term NSAID use (ie, 3 days) requires no special precautions in patients taking beta-blockers.
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause fatigue, insomnia, confusion, and nightmare and clinically look like a major depression
Mental Health: Effects on Psychiatric Treatment
Fluoxetine and paroxetine may increase carvedilol's (a CYP2D6 substrate) serum levels
Nursing: Physical Assessment/Monitoring
Assess potential for interactions with other prescriptions, OTC medications, or herbal products patient may be taking (especially anything that will effect blood pressure). Blood pressure and heart rate should be assessed prior to and following first doses and any change in dose. Caution patients with diabetes to monitor glucose levels closely (beta-blockers may alter glucose tolerance). Assess results of laboratory tests, therapeutic effectiveness (eg, reduction of hypertension or angina), and adverse response (eg, CHF). Teach patient proper use, possible side effects/appropriate interventions, and adverse symptoms to report.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, extended release; as phosphate:
Coreg CR™: 10 mg, 20 mg, 40 mg, 80 mg
Tablet: 3.125 mg, 6.25 mg, 12.5 mg, 25 mg
Coreg®: 3.125 mg, 6.25 mg, 12.5 mg, 25 mg
Pricing: U.S. (www.drugstore.com)
Capsule, 24-hour (Coreg CR)
10 mg (30): $122.71
20 mg (30): $122.71
40 mg (30): $122.71
80 mg (30): $122.71
Tablets (Carvedilol)
3.125 mg (30): $25.99
6.25 mg (30): $14.99
12.5 mg (30): $14.99
25 mg (30): $15.99
Tablets (Coreg)
3.125 mg (60): $131.99
6.25 mg (30): $70.99
12.5 mg (60): $136.00
25 mg (60): $136.00
References
Adams KF, Lindenfeld J, Arnold JMO, et al, “HFSA 2006 Comprehensive Heart Failure Practice Guideline,” J Card Fail, 2006, 12(1):e1–122. Available at http://www.heartfailureguideline.org
Anderson JL, Adams CD, Antman EM, et al, "ACC/AHA 2007 Guidelines for the Management of Patients With Unstable Angina/Non-ST-Elevation Myocardial Infarction: A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Writing Committee to Revise the 2002 Guidelines for the Management of Patients With Unstable Angina/Non-ST-Elevation Myocardial Infarction) Developed in Collaboration With the American College of Emergency Physicians, the Society for Cardiovascular Angiography and Interventions, and the Society of Thoracic Surgeons Endorsed by the American Association of Cardiovascular and Pulmonary Rehabilitation and the Society for Academic Emergency Medicine," J Am Coll Cardiol, 2007, 50(7):e1-e157.
Antman EM, Anbe DT, Armstrong PW, et al, "ACC/AHA Guidelines for the Management of Patients With ST-Elevation Myocardial Infarction: A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee to Revise the 1999 Guidelines for the Management of Patients with Acute Myocardial Infarction)," Circulation, 2004, 110(9):e82-292.
Bristow MR, Gilbert EM, Abraham WT, et al, “Carvedilol Produces Dose-Related Improvements in Left Ventricular Function and Survival in Subjects With Chronic Heart Failure,” Circulation, 1996, 94(11):2807-16.
Colucci WS, Packer M, Bristow MR, et al, “Carvedilol Inhibits Clinical Progression in Patients With Mild Symptoms of Heart Failure. U.S Carvedilol Heart Failure Study Group,” Circulation, 1996, 94(11):2800-6.
Dargie HJ, “Effect of Carvedilol on Outcome After Myocardial Infarction in Patients With Left-Ventricular Dysfunction: The CAPRICORN Randomised Trial,” Lancet, 2001, 357(9266):1385-90.
Fleisher LA, Beckman JA, Brown KA, et al, “ACC/AHA 2007 Guidelines on Perioperative Cardiovascular Evaluation for Noncardiac Surgery: A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Writing Committee to Revise the 2002 Guidelines on Perioperative Cardiovascular Evaluation for Noncardiac Surgery) Developed in Collaboration With the American Society of Echocardiography, American Society of Nuclear Cardiology, Heart Rhythm Society, Society of Cardiovascular Anesthesiologists, Society for Cardiovascular Angiography and Interventions, Society for Vascular Medicine and Biology, and Society for Vascular Surgery,” J Am Coll Cardiol, 2007, 50(17):e159-241.
Gibbons RJ, Abrams J, Chatterjee K, et al, “ACC/AHA 2002 Guideline Update for the Management of Patients With Chronic Stable Angina - Summary Article: A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee on the Management of Patients With Chronic Stable Angina),” J Am Coll Cardiol, 2003, 41(1):159-68.
Hunt SA, Abraham WT, Chin MH , et al, "ACC/AHA 2005 Guideline Update for the Diagnosis and Management of Chronic Heart Failure in the Adult: A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Writing Committee to Update the 2001 Guidelines for the Evaluation and Management of Heart Failure)," available at http://www.acc.org/qualityandscience/clinical/guidelines/failure/update/index.pdf.
Juul AB, Wetterslev J, Gluud C, et al, "Effect of Perioperative Beta-Blockade in Patients With Diabetes Undergoing Major Noncardiac Surgery: Randomized Placebo Controlled, Blinded Multicentre Trial," BMJ, 2006, 332(7556):1482.
Lang DM, “Anaphylactoid and Anaphylactic Reactions. Hazards of Beta-Blockers,” Drug Saf, 1995, 12(5):299-304.
Macdonald PS, Keogh AM, Aboyoun CL, et al, “Tolerability and Efficacy of Carvedilol in Patients With New York Heart Association Class IV Heart Failure,” J Am Coll Cardiol, 1999, 33(4):924-31.
Mokhlesi B, Leikin JB, Murray P, et al, “Adult Toxicology in Critical Care: Part II: Specific Poisonings,” Chest, 2003, 123(3):897-922.
Packer M, Bristow MR, Cohn JN, et al, “The Effect of Carvedilol on Morbidity and Mortality in Patients With Chronic Heart Failure,” N Engl J Med, 1996, 334(21):1349-55.
Packer M, Coats AJ, Fowler MB, et al, “Effect of Carvedilol on Survival in Severe Chronic Heart Failure,” N Engl J Med, 2001, 344(22):1651-8.
Packer M, Colucci WS, Sackner-Bernstein JD, et al, “Double-Blind, Placebo-Controlled Study of the Effects of Carvedilol in Patients With Moderate to Severe Heart Failure. The PRECISE Trial. Prospective Randomized Evaluation of Carvedilol on Symptoms and Exercise,” Circulation, 1996, 94(11):2793-9.
“Randomised, Placebo-Controlled Trial of Carvedilol in Patients With Congestive Heart Failure Due to Ischaemic Heart Disease. Australia/New Zealand Heart Failure Research Collaborative Group,” Lancet, 1997, 349(9049):375-80.
UK Prospective Diabetes Study Group, “Efficacy of Atenolol and Captopril in Reducing Risk of Macrovascular and Microvascular Complications in Type 2 Diabetes: UKPDS 39,” BMJ, 1998, 317(7160):713-20.
Yang H, Raymer K, Butler R, et al, "The Effects of Perioperative Beta-Blockade: Results of the Metoprolol After Vascular Surgery (MaVS) Study, A Randomized Controlled Trial," Am Heart J 2006, 152(5):983-90.
International Brand Names
Lexi-Comp.com
Last full review/revision August 2008
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