Coreg


Also found in: Dictionary, Thesaurus.
Related to Coreg: Beta blockers, Coreg CR

carvedilol

Apo-Carvedilol (CA), Coreg, Dom-Carvedilol (CA), Eucardic (UK)

carvedilol phosphate

Coreg CR, Novo-Carvedilol (CA), PHL-Carvedilol (CA), PMS-Carvedilol (CA)

Pharmacologic class: Beta-adrenergic blocker (nonselective)

Therapeutic class: Antihypertensive

Pregnancy risk category C

Action

Blocks stimulation of cardiac beta1-adrenergic receptor sites and pulmonary beta2-adrenergic receptor sites. Shows intrinsic sympathomimetic activity, causing slowing of heart rate, decreased myocardial excitability, reduced cardiac output, and decreased renin release from kidney.

Availability

Capsules (extended-release): 10 mg, 20 mg, 40 mg, 80 mg

Tablets: 3.125 mg, 6.25 mg, 12.5 mg, 25 mg

Indications and dosages

Hypertension

Adults: Initially, 6.25 mg P.O. b.i.d. (Coreg). May be increased q 7 to 14 days to a maximum dosage of 25 mg b.i.d. Or, 20 mg P.O. daily (Coreg CR). If tolerated, using standing systolic pressure about 1 hour after dosing, maintain dosage of Coreg CR for 7 to 14 days; then increase to 40 mg once daily if needed based on trough systolic standing blood pressure. Maintain this dosage for 7 to 14 days and adjust to 80 mg once daily if tolerated and needed. Total daily dose of Coreg CR shouldn't exceed 80 mg.

Heart failure caused by ischemia or cardiomyopathy

Adults: Initially, 3.125 mg P.O. b.i.d. (Coreg) for 2 weeks. May increase to 6.25 mg b.i.d. Dosage may be doubled q 2 weeks as tolerated, not to exceed 25 mg b.i.d. in patients weighing less than 85 kg (187 lb) or 50 mg b.i.d. in patients weighing more than 85 kg. Or, 10 mg P.O. daily (Coreg CR) for 2 weeks. If tolerated, increase dosage to 20 mg, 40 mg, and 80 mg over successive intervals of at least 2 weeks.

Left ventricular dysfunction following myocardial infarction

Adults: Initially, 6.25 mg P.O. b.i.d. (Coreg); increase after 3 to 10 days to 12.5 mg b.i.d. (based on tolerability), then increase to target dosage of 25 mg b.i.d. A lower starting dose (3.125 mg b.i.d.) or slower titration may be used if clinically indicated. Or, 20 mg P.O. once daily (Coreg CR); increase after 3 to 10 days to 40 mg daily (based on tolerability), then increase to target dose of 80 mg daily. A lower starting dose may be used (10 mg daily) or the rate of up titration may be slowed if clinically indicated.

Off-label uses

• Angina pectoris

• Idiopathic cardiomyopathy

Contraindications

• Hypersensitivity to drug

• Uncompensated heart failure

• Pulmonary edema

• Cardiogenic shock

• Bradycardia or heart block

• Severe hepatic impairment

• Bronchial asthma, bronchospasm

Precautions

Use cautiously in:

• renal or hepatic impairment, pulmonary disease, diabetes mellitus, hypoglycemia, thyrotoxicosis, peripheral vascular disease, hypotension, respiratory depression

• elderly patients

• pregnant or breastfeeding patients

• children.

Administration

• Ensure that patient is hemodynamically stable and fluid retention has been minimized before starting therapy.

• Give immediate-release form with food to slow absorption and minimize orthostatic hypotension.

• Give extended-release form in the morning with food and instruct patient to swallow capsule whole.

• For patients who can't swallow capsules whole, carefully open capsules and sprinkle contents on applesauce; have patient swallow contents immediately without chewing. Don't use warm applesauce; doing so could affect the modified-release properties of this formulation.

• When drug is used to treat heart failure, check apical pulse before administering. If it's below 60 beats/minute, withhold dosage and contact prescriber.

• When drug is used for hypertension, check standing systolic pressure about 1 hour after dosing for use as a guide for patient tolerance.

• Be aware that addition of diuretic may cause additive effects and may worsen orthostatic hypotension.

• Know that full antihypertensive effect takes 7 to 14 days.

Don't withdraw drug abruptly, because this may lead to withdrawal phenomenon (angina exacerbation, myocardial infarction, ventricular arrhythmias, and even death).

Adverse reactions

CNS: dizziness, fatigue, anxiety, depression, insomnia, memory loss, nightmares, headache, pain

CV: orthostatic hypotension, peripheral vasoconstriction, angina pectoris, chest pain, hypertension, bradycardia, heart failure, atrioventricular block

EENT: blurred or abnormal vision, dry eyes, stuffy nose, rhinitis, sinusitis, pharyngitis

GI: nausea, diarrhea, constipation

GU: urinary tract infection, hematuria, albuminuria, decreased libido, erectile dysfunction, renal dysfunction

Hematologic: bleeding, purpura, thrombocytopenia

Metabolic: hypovolemia, hypervolemia, hyperglycemia, hyponatremia, hyperuricemia, glycosuria, gout, hypoglycemia

Musculoskeletal: arthralgia, back pain, muscle cramps

Respiratory: wheezing, upper respiratory tract infection, dyspnea, bronchitis, bronchospasm, pulmonary edema

Skin: pruritus, rash

Other: weight gain, lupuslike syndrome, viral infection, anaphylaxis

Interactions

Drug-drug. Antihypertensives: additive hypotension

Calcium channel blockers, general anesthetics, I.V. phenytoin: additive myocardial depression

Cimetidine: increased carvedilol toxicity

Clonidine: increased hypotension and bradycardia, exaggerated withdrawal phenomenon

Digoxin: additive bradycardia

Dobutamine, dopamine: decrease in beneficial cardiovascular effects

Insulin, oral hypoglycemics: altered efficacy of these drugs

MAO inhibitors: hypertension

Nonsteroidal anti-inflammatory drugs: decreased antihypertensive action

Rifampin, thyroid preparations: decreased carvedilol efficacy

Theophyllines: reduced theophylline elimination, antagonistic effect that decreases theophylline or carteolol efficacy

Drug-diagnostic tests. Antinuclear antibodies: increased titers

Blood urea nitrogen, glucose, lipoproteins, potassium, triglycerides, uric acid: increased levels

Drug-food. Any food: delayed drug absorption

Drug-behaviors. Acute alcohol ingestion: additive hypotension

Patient monitoring

• Watch for signs and symptoms of hypersensitivity reaction.

• Assess baseline CBC and kidney and liver function test results.

• Monitor vital signs (especially blood pressure), ECG, and exercise tolerance. Drug may alter cardiac output and cause ineffective airway clearance.

• Weigh patient daily and measure fluid intake and output to detect fluid retention.

• Measure blood glucose regularly if patient has diabetes mellitus. Drug may mask signs and symptoms of hypoglycemia.

Patient teaching

• Instruct patient to take drug with food exactly as prescribed.

• Tell patient to take extended-release capsule in the morning with food, to swallow capsule whole, and not to chew, crush, or divide its contents.

• Instruct patient who can't swallow capsule whole to carefully open capsule, sprinkle contents on cool or cold applesauce, and swallow contents immediately without chewing. Tell patient not to store mixture for future use.

Caution patient not to stop taking drug abruptly, because serious reactions may result.

• Advise patient to move slowly when sitting up or standing, to avoid dizziness or light-headedness from sudden blood pressure drop.

• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.

• Inform male patient that drug may cause erectile dysfunction. Advise him to discuss this issue with prescriber.

• Advise patient to use soft-bristled toothbrush and electric razor to avoid gum and skin injury.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, and behaviors mentioned above.

carvedilol

(kar-ve-di-lole) ,

Coreg

(trade name),

Coreg CR

(trade name)

Classification

Therapeutic: antihypertensives
Pharmacologic: beta blockers
Pregnancy Category: C

Indications

Hypertension.HF (ischemic or cardiomyopathic) with digoxin, diuretics, and ACE inhibitors.Left ventricular dysfunction after myocardial infarction.

Action

Blocks stimulation of beta1(myocardial) and beta2 (pulmonary, vascular, and uterine)-adrenergic receptor sites.
Also has alpha1 blocking activity, which may result in orthostatic hypotension.

Therapeutic effects

Decreased heart rate and BP.
Improved cardiac output, slowing of the progression of HF and decreased risk of death.

Pharmacokinetics

Absorption: Well absorbed but rapidly undergoes extensive first-pass hepatic metabolism, resulting in 25–35% bioavailability. Food slows absorption.
Distribution: Unknown.
Protein Binding: 98%.
Metabolism and Excretion: Extensively metabolized (primarily by CYP2D6 and CYP2C9; the CYP2D6 enzyme system exhibits genetic polymorphism); genetic implication ∼7% of population may be poor metabolizers and may have significantly ↑ carvedilol concentrations and an ↑ risk of adverse effects); excreted in feces via bile, <2% excreted unchanged in urine.
Half-life: 7–10 hr.

Time/action profile (cardiovascular effects)

ROUTEONSETPEAKDURATION
POwithin 1 hr1–2 hr12 hr
PO-CRunknown5 hr24 hr

Contraindications/Precautions

Contraindicated in: History of serious hypersensitivity reaction (Stevens-Johnson syndrome, angioedema, anaphylaxis);Pulmonary edema;Cardiogenic shock;Bradycardia, heart block or sick sinus syndrome (unless a pacemaker is in place);Uncompensated HF requiring IV inotropic agents (wean before starting carvedilol);Severe hepatic impairment;Asthma or other bronchospastic disorders.
Use Cautiously in: HF (condition may deteriorate during initial therapy);Renal impairment;Hepatic impairment;Diabetes mellitus (may mask signs of hypoglycemia);Thyrotoxicosis (may mask symptoms);Peripheral vascular disease;History of severe allergic reactions (intensity of reactions may be increased); Obstetric: Crosses placenta and may cause fetal/neonatal bradycardia, hypotension, hypoglycemia, or respiratory depression); Lactation / Pediatric: Safety not established; Geriatric: ↑ sensitivity to beta blockers; initial dose reduction recommended.

Adverse Reactions/Side Effects

Central nervous system

  • dizziness (most frequent)
  • fatigue (most frequent)
  • weakness (most frequent)
  • anxiety
  • depression
  • drowsiness
  • insomnia
  • memory loss
  • mental status changes
  • nervousness
  • nightmares

Ear, Eye, Nose, Throat

  • blurred vision
  • dry eyes
  • intraoperative floppy iris syndrome
  • nasal stuffiness

Respiratory

  • bronchospasm
  • wheezing

Cardiovascular

  • bradycardia (life-threatening)
  • HF (life-threatening)
  • pulmonary edema (life-threatening)

Gastrointestinal

  • diarrhea (most frequent)
  • constipation
  • nausea

Genitourinary

  • erectile dysfunction (most frequent)
  • ↓ libido

Dermatologic

  • stevens-johnson syndrome (life-threatening)
  • toxic epidermal necrolysis (life-threatening)
  • itching
  • rashes
  • urticaria

Endocrinologic

  • hyperglycemia (most frequent)
  • hypoglycemia

Musculoskeletal

  • arthralgia
  • back pain
  • muscle cramps

Neurologic

  • paresthesia

Miscellaneous

  • anaphylaxis (life-threatening)
  • angioedema (life-threatening)
  • drug-induced lupus syndrome

Interactions

Drug-Drug interaction

General anesthetics, IV phenytoin, diltiazem, and verapamil may cause ↑ myocardial depression.↑ risk of bradycardia with digoxin.Amiodarone or fluconazole may ↑ levels.↑ hypotension may occur with other antihypertensives, acute ingestion of alcohol, or nitrates.Concurrent use with clonidine ↑ hypotension and bradycardia.May ↑ withdrawal phenomenon from clonidine (discontinue carvedilol first).Concurrent administration of thyroid preparations may ↓ effectiveness.May alter the effectiveness of insulins or oral hypoglycemic agents (dose adjustments may be necessary).May ↓ effectiveness of theophylline.May ↓ beneficial beta1-cardiovascular effects of dopamine or dobutamine.Use cautiously within 14 days of MAO inhibitor therapy (may result in hypotension/bradycardia).Cimetidine may ↑ toxicity from carvedilol.Concurrent NSAIDs may ↓ antihypertensive action.Effectiveness may be ↓ by rifampin.May ↑ serum digoxin levels.May ↑ blood levels of cyclosporine (monitor blood levels).

Route/Dosage

Oral (Adults) Hypertension—6.25 mg twice daily, may be ↑ q 7–14 days up to 25 mg twice daily or extended-release—20 mg once daily, dose may be doubled every 7–14 days up to 80 mg once daily; HF—3.125 mg twice daily for 2 wk; may be ↑ to 6.25 mg twice daily. Dose may be doubled q 2 wk as tolerated (not to exceed 25 mg twice daily in patients <85 kg or 50 mg twice daily in patients >85 kg) or extended-release—10 mg once daily, dose may be doubled every 2 wk as tolerated up to 80 mg once daily; Left ventricular dysfunction after MI—6.25 mg twice daily, ↑ after 3–10 days to 12.5 twice daily then to target dose of 25 mg twice daily; some patients may require lower initial doses and slower titration or extended-release—20 mg once daily, dose may be doubled every 3–10 days up to 80 mg once daily.

Availability (generic available)

Tablets: 3.125 mg, 6.25 mg, 12.5 mg, 25 mg Cost: Generic — All strengths $7.18 / 100
Extended-release capsules: 10 mg, 20 mg, 40 mg, 80 mg Cost: all strengths $175.36 / 30

Nursing implications

Nursing assessment

  • Monitor BP and pulse frequently during dose adjustment period and periodically during therapy. Assess for orthostatic hypotension when assisting patient up from supine position.
  • Monitor intake and output ratios and daily weight. Assess patient routinely for evidence of fluid overload (peripheral edema, dyspnea, rales/crackles, fatigue, weight gain, jugular venous distention). Patients may experience worsening of symptoms during initiation of therapy for HF.
  • Hypertension: Check frequency of refills to determine adherence.
  • Lab Test Considerations: May cause ↑ BUN, serum lipoprotein, potassium, triglyceride, and uric acid levels.
    • May cause ↑ ANA titers.
    • May cause ↑ in blood glucose levels.
  • Monitor patients receiving beta blockers for signs of overdose (bradycardia, severe dizziness or fainting, severe drowsiness, dyspnea, bluish fingernails or palms, seizures). Notify health care professional immediately if these signs occur.

Potential Nursing Diagnoses

Decreased cardiac output (Side Effects)
Noncompliance (Patient/Family Teaching)

Implementation

  • Do not confuse carvedilol with captopril.
    • Discontinuation of concurrent clonidine should be gradual, with carvedilol discontinued first over 1–2 wk with limitation of physical activity; then, after several days, discontinue clonidine.
  • Oral: Take apical pulse before administering. If <50 bpm or if arrhythmia occurs, withhold medication and notify health care professional.
    • Administer with food to minimize orthostatic hypotension.
    • Administer extended-release capsulesin the morning. Swallow whole; do not crush, break, or chew. Extended-release capsules may be opened and sprinkled on cold applesauce and taken immediately; do not store mixture.
    • To convert from immediate-release to extended-release product, doses of 3.125 mg twice daily can be converted to 10 mg daily; doses of 6.25 mg twice daily can be converted to 20 mg daily; doses of 12.5 mg twice daily can be converted to 40 mg daily; and doses of 25 mg twice daily can be converted to 80 mg daily.

Patient/Family Teaching

  • Instruct patient to take medication as directed, at the same time each day, even if feeling well. Do not skip or double up on missed doses. Take missed doses as soon as possible up to 4 hr before next dose. Abrupt withdrawal may precipitate life-threatening arrhythmias, hypertension, or myocardial ischemia.
  • Advise patient to make sure enough medication is available for weekends, holidays, and vacations. A written prescription may be kept in wallet in case of emergency.
  • Teach patient and family how to check pulse and BP. Instruct them to check pulse daily and BP biweekly. Advise patient to hold dose and contact health care professional if pulse is <50 bpm or BP changes significantly.
  • May cause drowsiness or dizziness. Caution patients to avoid driving or other activities that require alertness until response to the drug is known.
  • Advise patient to change positions slowly to minimize orthostatic hypotension, especially during initiation of therapy or when dose is increased.
  • Caution patient that this medication may increase sensitivity to cold.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other Rx, OTC, or herbal products, especially cold preparations, concurrently with this medication.
  • Patients with diabetes should closely monitor blood glucose, especially if weakness, malaise, irritability, or fatigue occurs. Medication may mask some signs of hypoglycemia, but dizziness and sweating may still occur.
  • Advise patient to notify health care professional if slow pulse, difficulty breathing, wheezing, cold hands and feet, dizziness, confusion, depression, rash, fever, sore throat, unusual bleeding, or bruising occurs.
  • Instruct patient to inform health care professional of medication regimen before treatment or surgery.
  • Advise patient to carry identification describing disease process and medication regimen at all times.
  • Hypertension: Reinforce the need to continue additional therapies for hypertension (weight loss, sodium restriction, stress reduction, regular exercise, moderation of alcohol consumption, and smoking cessation). Medication controls but does not cure hypertension.

Evaluation/Desired Outcomes

  • Decrease in BP without appearance of detrimental side effects.
  • Decrease in severity of HF.

Coreg

(kôr′ĕg′)
A trademark for the drug carvedilol.
References in periodicals archive ?
Impax Laboratories Inc (NASDAQ:IPXL) reported on Friday the receipt of US Food and Drug Administration (FDA) tentative approval for its Abbreviated New Drug Application (ANDA) for the generic version of Coreg CR (carvedilol phosphate) extended-release capsules in 10, 20, 40 and 80 mg.
COREG CR will utilize Flamel's proprietary Micropump[R] technology, which controls the delivery of carvedilol helping to maintain appropriate amounts of medicine in the body over a 24-hour span.
The drug is a generic version of GSK's (NYSE: GSK) Coreg CR.
Bestsellers such as Coreg for high blood pressure and antidepressant Wellbutrin faced pressure from generic versions in the quarter, the final three-month period before Chief Executive Officer Jean-Pierre Garnier retires next month.
Despite this, however, Deutsche Bank said that the patent on Coreg CR, the once-a-day drug for the treatment of three key cardiovascular conditions, is likely to be protected from generic competition until 2023.
In 2007, seven popular products--Norvasc (amlodipine besylate), Ambien (zoldipem tartrate), Zyrtec (cetirizine), Lotrel (amlodipine/benazepril), Coreg (carvedilol), Lamisil (terbinafine), and Tequin (gatifloxicin), are due to lose patent protection, noted PCMA, which could lead to $700 million in savings that year.
Since making changes in my diet, adding regular exercise, and taking a medication called Coreg, my ejection fraction has been as high as 59 percent, which is outstanding.
Earlier in his career, Derkacz has worked for more than 15 years at GlaxoSmithKline for major brands including Levitra, Paxil, Coreg and its adult vaccine portfolio.
Medco managers credited the early release of some generic medications, including versions of the popular high blood-pressure treatments Toprol XL and Coreg, as well as strong mail-order volume.
Although sales of asthma drug Advair and diabetes drug Avandia are likely to have disappointed over the final quarter, GSK is expected to have benefited from a good performance in its vaccine business as well as heart drug Coreg.