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Carvedilol (Systemic)


VA CLASSIFICATION
Primary: CV100
Secondary: CV409

Commonly used brand name(s): Coreg.

Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).



Category:


Antihypertensive{01}

congestive heart failure treatment adjunct{01}

Indications

Accepted

Congestive heart failure (treatment adjunct)—Carvedilol is indicated, in conjunction with digitalis, diuretics, and/or angiotensin-converting enzyme (ACE) inhibitors, for the treatment of mild or moderate (New York Heart Association [NYHA] class II or III) heart failure of ischemic or cardiomyopathic origin, to slow the progression of disease as evidenced by cardiovascular death, cardiovascular hospitalization, or the need to adjust other heart failure medications {01}. Carvedilol may be used in patients unable to tolerate an ACE inhibitor or in patients who are or are not receiving digitalis, hydralazine, or nitrate therapy {01}.

Hypertension (treatment) {01}— Carvedilol is indicated, either alone or in combination with other antihypertensive agents, such as thiazide diuretics, in the treatment of essential hypertension {01}.
—For additional information on initial therapeutic guidelines related to the treatment of hypertension, see Appendix III.


Pharmacology/Pharmacokinetics

Physicochemical characteristics:
Molecular weight—
    406.5 {01}

Mechanism of action/Effect:

Carvedilol is a nonselective beta-adrenergic blocking agent with alpha 1-adrenergic blocking activity and no intrinsic sympathomimetic activity {01}. The exact mechanism of the antihypertensive effect produced by beta-adrenergic blockade is not known, but may involve suppression of renin production {01}. The beta-adrenergic blocking activity of carvedilol decreases cardiac output, exercise- and/or isoproterenol-induced tachycardia, and reflex orthostatic tachycardia {01}. The alpha 1-adrenergic blocking activity of carvedilol blunts the pressor effect of phenylephrine, causes vasodilation, and reduces peripheral vascular resistance {01}. The effect of alpha 1-adrenergic blockade is a reduction in standing blood pressure (more than supine), potentiating symptoms of postural hypotension and possibly syncope {01}.

The mechanism by which carvedilol produces a beneficial effect in congestive heart failure is not known, but may be attributable to beta-adrenergic blockade and vasodilation {01}.

Absorption:

Carvedilol is rapidly and extensively absorbed {01}. Absolute bioavailability of carvedilol is 25 to 35%, due to significant first-pass metabolism {01}. Food slows the rate of absorption but does not appear to affect the extent of the bioavailability of carvedilol {01}.

Distribution:

Volume of distribution (Vol D)—Steady-state: Approximately 115 L {01}.

Protein binding:

Very high (98%), primarily to albumin {01}; concentration-independent {01}.

Biotransformation:

Hepatic {01}; carvedilol is extensively metabolized, primarily by aromatic ring oxidation and glucuronidation by the cytochrome P450 2D6 enzyme {01}. Other isozymes, such as P450 2C9 and P450 3A4, are involved to a lesser extent {01}. Three active metabolites with beta-receptor blocking activity are produced by demethylation and hydroxylation at the phenol ring {01}. The active metabolites show weak vasodilating (alpha 1-antagonist) activity when compared with carvedilol; however, in preclinical studies, the beta-blockade effect of the 4´-hydroxyphenyl metabolite was found to be approximately 13 times more potent than that of carvedilol {01}.

Half-life:


Elimination:

Apparent mean terminal: 7 to 10 hours {01}; may be affected by induction or inhibition of cytochrome P450 enzymes {01}.


Elimination:
    Fecal (biliary) {01}.


In dialysis—
        Carvedilol does not appear to be cleared significantly by hemodialysis {01}.



Precautions to Consider

Carcinogenicity

No evidence of carcinogenicity was found in 2-year studies in rats and mice given doses of up to 75 mg per kg of body weight (mg/kg) per day (12 times the maximum recommended human dose [MRHD] on a mg per square meter of body surface area [mg/m 2] basis) and 200 mg/kg per day (16 times the MRHD on a mg/m 2 basis), respectively {01}.

Mutagenicity

Mutagenicity was not detected in the Ames test or the CHO/HGPRT assay {01}. Clastogenicity was not detected in the in vitro hamster micronucleus or the in vivo human lymphocyte cell tests {01}.

Pregnancy/Reproduction
Fertility—
Impaired fertility was observed in rats given doses ³ 200 mg/kg per day (³ 32 times the MRHD on a mg/m 2 basis). Administration of carvedilol at this dose was associated with a reduced number of successful matings, prolonged mating time, significantly fewer corpora lutea and implants per dam, and complete resorption of 18% of the litters {01}.

Pregnancy—
Adequate and well-controlled studies in humans have not been done {01}.

Reproduction studies in rats and rabbits revealed increased postimplantation loss in rats at doses of 300 mg/kg per day (50 times the MRHD on a mg/m 2 basis) and in rabbits at doses of 75 mg/kg per day (25 times the MRHD on a mg/m 2 basis) {01}. In rats, a decrease in fetal body weight and an increase in the frequency of fetuses with delayed skeletal development (missing or stunted 13th rib) also occurred {01}.

FDA Pregnancy Category C {01}.

Breast-feeding

It is not known whether carvedilol is distributed into breast milk {01}.

Studies in lactating rats have shown that carvedilol and/or its metabolites were distributed into milk and caused an increased mortality in rat neonates {01}. Because of the potential for a serious reaction in nursing infants from beta-adrenergic blockade (bradycardia), a decision should be made about whether to discontinue nursing or to discontinue carvedilol {01}.

Pediatrics

No information is available on the relationship of age to the effects of carvedilol in pediatric patients {01}. Safety and efficacy in pediatric patients have not been established {01}.


Geriatrics


Use of carvedilol in patients 65 years of age and older has not demonstrated geriatric-specific problems that would limit the usefulness of carvedilol in the elderly {01}. However, plasma levels of carvedilol in the elderly are about 50% higher on the average as compared with younger subjects, and the incidence of dizziness as a side effect is higher in the elderly than in younger patients {01}.


Pharmacogenetics

In clinical trials, black patients with hypertension were less responsive to the antihypertensive beta-adrenergic blocking effects of carvedilol than nonblack patients {01}.

Patients who are poor metabolizers of debrisoquin, a marker for the cytochrome P450 2D6 isozyme, may experience two- to threefold increases in carvedilol plasma concentrations, increasing the risk of adverse effects {01}.

Surgical

Use of carvedilol perioperatively with anesthetic agents, such as cyclopropane, ether, and trichloroethylene, may further depress myocardial function {01}.

Drug interactions and/or related problems
The following drug interactions and/or related problems have been selected on the basis of their potential clinical significance (possible mechanism in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):


Note: Combinations containing any of the following medications, depending on the amount present, may also interact with this medication.

Anesthetics{01} , general, such as:
Cyclopropane{01}
Ether{01}
Trichloroethylene{01}    (concurrent use with carvedilol may further depress myocardial function {01})


» Antidiabetic agents, sulfonylurea{01} or
» Insulin{01}    (concurrent use with carvedilol may increase the serum glucose–lowering effects of insulin and sulfonylurea antidiabetic agents {01}; regular monitoring of blood glucose is recommended when using carvedilol and insulin or sulfonylurea antidiabetic agents concurrently {01})


» Calcium channel blocking agents{01} , especially
Diltiazem{01} or
Verapamil{01}    (concurrent use of carvedilol with diltiazem has resulted in isolated cases of conduction disturbances {01}; electrocardiogram and blood pressure measurements are recommended when carvedilol is used concurrently with calcium channel blocking agents {01})


Catecholamine-depleting agents, such as:{01}
Monoamine oxidase inhibitors{01}
Reserpine{01}    (concurrent use of carvedilol with drugs that can deplete catecholamines may cause hypotension and bradycardia {01})


Clonidine{01}    (concurrent use with carvedilol may have additive blood pressure– and heart rate–lowering effects {01})


Digoxin{01}    (in hypertensive patients, concurrent use with carvedilol increased steady-state area under the plasma concentration–time curve [AUC] and trough concentrations of digoxin by 14% and 16%, respectively {01}; slowing of atrioventricular [AV] conduction may be additive {01}; monitoring of plasma digoxin concentrations is recommended when carvedilol is used concurrently {01})


Enzyme inducers, hepatic, cytochrome P450{01} (see Appendix II ), such as
Rifampin{01} or
Enzyme inhibitors, hepatic, cytochrome P450{01} (see Appendix II ), such as:
Cimetidine{01}
Fluoxetine{01}
Paroxetine{01}
Propafenone{01}
Quinidine{01}    (concurrent use may affect the metabolism and pharmacokinetics of carvedilol by inducing or inhibiting cytochrome P450 enzymes {01}; in healthy male subjects, concurrent use of rifampin decreased the AUC and peak plasma concentration [C max] of carvedilol by about 70% {01}; in healthy male subjects, concurrent use of cimetidine increased the steady-state AUC of carvedilol by 30% with no change in C max {01})



Laboratory value alterations
The following have been selected on the basis of their potential clinical significance (possible effect in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):

With physiology/laboratory test values
Bilirubin concentrations, serum{01} or
Transaminase values, serum{01}    (increases have occurred rarely; carvedilol should be withdrawn if laboratory signs of liver injury or jaundice occur)


Glucose, serum{01}    (beta-adrenergic blocking agents, e.g., carvedilol, increase the serum glucose–lowering effects of insulin and sulfonylurea antidiabetic agents and delay the recovery of serum glucose levels {01}; however, in patients with both diabetes and congestive heart failure, hyperglycemia may be worsened {01}; in clinical trials with congestive heart failure patients, the incidence of hyperglycemia was 12.2% {01})


Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).


Except under special circumstances, this medication should not be used when the following medical problems exist:
» Asthma, bronchial{01} or
» Bronchospastic conditions, related{01}    (carvedilol aggravates bronchial asthma and related bronchospastic conditions by blocking endogenous and exogenous beta agonists; two cases of death from status asthmaticus have been reported in patients receiving a single dose of carvedilol {01})


» Atrioventricular (AV) block, 2nd- or 3rd-degree{01} or
» Bradycardia{01} , severe or
» Cardiogenic shock{01} or
» Sick sinus syndrome, without a pacemaker{01}    (risk of further depression of myocardial contractility and conduction {01})


» Cardiac failure, decompensated, severe, requiring intravenous inotropic therapy, New York Heart Association (NYHA) class IV{01}    (in clinical trials, area under the plasma concentration–time curve [AUC] and time to peak plasma concentration [C max] increased by 50 to 100% in six patients with NYHA class IV heart failure {01}; myocardial contractility may be further depressed in these patients {01})


» Hepatic function impairment, clinically manifested{01}    (because carvedilol is hepatically metabolized, blood concentrations may be increased approximately four- to sevenfold following a single dose {01})


» Hypersensitivity to carvedilol{01}
Risk-benefit should be considered when the following medical problems exist
» Anaphylactic reaction to a variety of allergens, severe{01} , history of    (administration of beta-adrenergic blocking agents may make these patients more reactive to allergen exposure and less responsive to the usual doses of epinephrine used to treat the allergic reaction {01})


Angina, Prinzmetal's variant{01}    (nonselective beta-adrenergic blocking agents, such as carvedilol, may provoke chest pain in patients with this condition {01}; caution should be used {01})


» Bronchospastic conditions, nonallergic, such as:
Chronic bronchitis{01} and
Emphysema{01}    (because carvedilol blocks the effect of endogenous and exogenous beta-adrenergic agonists, nonallergic bronchospastic conditions may be aggravated by carvedilol {01}; only the smallest effective dose of carvedilol should be used, if it is used at all {01}; in clinical trials, patients with congestive heart failure and bronchospastic disease received carvedilol only if treatment of their bronchospastic condition did not require oral or inhaled medication {01})


Congestive heart failure{01} , if accompanied by:
Hypotension (systolic blood pressure < 100 mm Hg){01} or
Ischemic heart disease{01} or
Renal insufficiency{01} or
Vascular disease, diffuse{01}    ({01}patients with these conditions may be at risk for worsening of renal function if treated with carvedilol {01}; renal function should be monitored and a dosage adjustment or discontinuation of carvedilol may be necessary if renal function deteriorates {01}; heart failure may be worsened or fluid retention may occur when the dosage of carvedilol is increased {01}; in such cases, dosages of diuretics should be increased, and carvedilol dosage increases should be postponed until the patient is clinically stable {01}; carvedilol dosage may need to be reduced or temporarily discontinued in such cases {01}. The AUC and C max may be increased in patients with congestive heart failure {01})


» Diabetes{01} or
» Hypoglycemia    (beta-adrenergic blocking agents may mask symptoms of hypoglycemia, especially tachycardia {01}; insulin-induced hypoglycemia may be potentiated and the recovery of serum glucose levels may be delayed {01}; in patients with diabetes and congestive heart failure, hyperglycemia may be worsened with use of carvedilol; blood glucose concentrations should be monitored at each dosage adjustment {01})


» Hyperthyroidism{01}    (beta-adrenergic blocking agents, such as carvedilol, may mask symptoms of hyperthyroidism, such as tachycardia {01}; abrupt withdrawal of beta-adrenergic blocking agents may potentiate symptoms of hyperthyroidism or precipitate thyroid storm {01})


Peripheral vascular disease{01}    (carvedilol may precipitate or aggravate symptoms of arterial insufficiency {01})


Pheochromocytoma{01}    (in patients with this condition, therapy with alpha-adrenergic blocking agents should be initiated prior to beta-adrenergic blocking therapy {01}; although carvedilol has both alpha- and beta-adrenergic blocking activity, there is no experience with use of carvedilol in this condition {01})


Renal function impairment{01}    (increases in carvedilol plasma concentrations of approximately 40 to 50%, based on mean AUC data, were reported in patients with moderate to severe renal function impairment; peak plasma levels were approximately 12 to 26% higher in patients with renal function impairment {01})



Patient monitoring
The following may be especially important in patient monitoring (other tests may be warranted in some patients, depending on condition; » = major clinical significance):

» Blood pressure determinations, standing systolic{01}    (measurements should be taken about 1 hour after dosing as a guide for tolerance and after 7 to 14 days to determine whether a dose increase is needed {01}; monitoring is recommended when carvedilol is used concurrently with calcium channel blocking agents)


Blood glucose concentrations{01}    (for diabetic patients)


Electrocardiogram (ECG) determinations{01}    (monitoring is recommended when carvedilol is used concurrently with calcium channel blocking agents, such as diltiazem and verapamil, because of the possibility of cardiac conduction disturbances {01})


» Heart rate determinations    (in clinical trials in hypertensive patients, heart rate decreased by 7.5 beats per minute with a 50-mg per day dose of carvedilol {01}; if heart rate drops below 55 beats per minute, the carvedilol dosage should be reduced {01})


Hepatic function determinations{01}    (monitoring may be necessary {01})


Renal function determinations{01}    (monitoring may be necessary, especially in patients with congestive heart failure, during dosage increases {01})




Side/Adverse Effects
Use of carvedilol in patients with congestive heart failure has resulted in deterioration of renal function {01}. Renal function returned to baseline when carvedilol was discontinued {01}. Other rare side/adverse effects that have occurred with carvedilol therapy are complete atrioventricular (AV) block, bundle branch block, and myocardial ischemia {01}.

The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention
Incidence more frequent
    
Allergy{01} —increased sensitivity to allergens{01}
    
bradycardia{01} (slow heartbeat)—incidence 2% in patients with hypertension and 9% in patients with congestive heart failure{01}
    
chest pain{01} —incidence 14.4% in patients with congestive heart failure{01}
    
dizziness{01} —incidence 6% in patients with hypertension and 32% in patients with congestive heart failure{01}
    
dyspnea{01} (shortness of breath)
    
edema, generalized{01} (generalized swelling)
    
edema, peripheral{01} (swelling of feet, ankles, or lower legs)
    
hypotension{01} (dizziness, lightheadedness, or fainting)
    
pain{01} —incidence 8.6% in patients with congestive heart failure{01}
    
syncope{01} (fainting)
    
weight increase{01} —incidence 9.7% in patients with congestive heart failure{01} ; may be a sign of fluid retention and worsening of heart failure{01}

Note: Hypotension and postural hypotension were reported in 9.7% and syncope was reported in 3.4% of patients with congestive heart failure {01}. In patients with hypertension, postural hypotension was reported in 1.8% and syncope in 0.1% {01}. These problems may occur following the initial dose or at the time of a dosage increase {01}.


Incidence less frequent
    
Fever{01} —incidence 3.1% in patients with congestive heart failure
    
hematuria{01} (blood in urine)
    
hepatic injury{01} (pruritus; dark urine; persistent anorexia; yellow eyes or skin; influenza (flu)-like symptoms; right upper quadrant tenderness)
    
depression, mental{01}
    
thrombocytopenia{01} (unusual bleeding or bruising)

Note: Mild, reversible hepatic injury with minimal symptoms has been reported after short- and long-term therapy with carvedilol {01}. Carvedilol should be discontinued if jaundice or laboratory evidence of hepatic injury occurs {01}.




Those indicating need for medical attention only if they continue or are bothersome
Incidence more frequent
    
Back pain{01}
    
diarrhea{01}
    
fatigue{01} (unusual tiredness or weakness)
    
paresthesia{01} (prickling or tingling sensation)

Incidence less frequent
    
Abdominal pain{01}
    
arthralgia{01} (joint pain)
    
blurred vision{01}
    
headache{01}
    
insomnia{01} (trouble in sleeping)
    
lacrimation, decreased{01} (decreased tearing)—in patients who wear contact lenses
    
myalgia{01} (muscle pain)
    
nausea{01}
    
pharyngitis{01} (sore throat)
    
rhinitis{01} (stuffy or runny nose)
    
sweating, increased{01}
    
vomiting{01}





Overdose
For specific information on the agents used in the management of carvedilol overdose, see:    • Aminophylline in Bronchodilators, Theophylline (Systemic) monograph;
   • Atropine in Anticholinergics/Antispasmodics (Systemic) monograph;
   • Bronchodilators, Adrenergic (Inhalation-Local) monograph;
   • Bronchodilators, Adrenergic (Systemic) monograph;
   • Clonazepam and Diazepam in Benzodiazepines (Systemic) monograph;
   • Dobutamine, Epinephrine , Isoproterenol, and Norepinephrine in Sympathomimetic Agents—Cardiovascular Use (Parenteral-Systemic) monograph; and/or
   • Glucagon (Systemic) monograph.

For more information on the management of overdose or unintentional ingestion, contact a Poison Control Center (see Poison Control Center Listing ).

Clinical effects of overdose
The following effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:
Acute and chronic
    
Bradycardia, severe {01}
    
bronchospasm {01}
    
cardiac arrest {01}
    
cardiac insufficiency {01}
    
cardiogenic shock {01}
    
hypotension, severe {01}
    
lapses of consciousness {01}
    
respiratory problems {01}
    
seizures, generalized {01}
    
vomiting {01}


Treatment of overdose
For symptoms of shock (with severe intoxication), treatment with antidotes must be continued for an appropriate length of time consistent with the 7- to 10-hour half-life of carvedilol {01}. Treatment is symptomatic and supportive and may include the following:


Monitoring:
The patient should be placed in a supine position and observed and treated under intensive care conditions {01}.



To decrease absorption:
If overdose was recently ingested, gastric lavage or drug-induced emesis may be used {01}.



Specific treatment:
For excessive bradycardia—Intravenous atropine may be used {01}. If bradycardia is resistant to therapy, pacemaker therapy is recommended {01}.

For bronchospasm—Intravenous or inhaled beta-adrenergic sympathomimetics or intravenous aminophylline is recommended {01}.

For cardiovascular support—Intravenous glucagon or sympathomimetics such as dobutamine, isoproterenol, or epinephrine may be used {01}.

For peripheral vasodilation—Epinephrine or norepinephrine with continuous monitoring is recommended {01}.

For seizures—Intravenous diazepam or clonazepam is recommended {01}.



Supportive care:
Patients in whom intentional overdose is confirmed or suspected should be referred for psychiatric consultation.



Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Carvedilol (Systemic) .

In providing consultation, consider emphasizing the following selected information (» = major clinical significance):

Before using this medication
»   Conditions affecting use, especially:
Hypersensitivity to carvedilol





Breast-feeding—Not recommended in mothers who are breast-feeding because of potential for serious reaction in nursing infant
Other medications, especially sulfonylurea antidiabetic agents; calcium channel blocking agents, especially diltiazem or verapamil; or insulin
Other medical problems, especially bronchial asthma or related bronchospastic conditions; atrioventricular block, 2nd- or 3rd-degree; bradycardia, severe; history of severe anaphylactic reaction to a variety of allergens; bronchospastic conditions, nonallergic; cardiac failure, decompensated, NYHA class IV; cardiogenic shock; diabetes or hypoglycemia; hepatic function impairment, clinically evident; hyperthyroidism; or sick sinus syndrome, without a pacemaker

Proper use of this medication
Taking medication at the same time each day to maintain the therapeutic effect

Taking medication with food {01}

Not interrupting or discontinuing medication without consulting the physician {01}

» Proper dosing
Taking as soon as possible; not taking if almost time for next dose; not doubling doses

» Proper storage

Precautions while using this medication
Making regular visits to physician to check progress

Not taking other medications unless discussed with physician

Caution when driving or doing other tasks requiring alertness, because of the possible dizziness, lightheadedness, or fainting due to postural hypotension {01}

Caution when standing quickly because of possible drop in blood pressure, which may result in dizziness or fainting; sitting or lying down may help alleviate these symptoms {01}

Checking with physician if experiencing dizziness or faintness; a dosage adjustment may be necessary {01}

Caution if any kind of surgery (including dental surgery) or emergency treatment is required {01}

For diabetic patients—Checking with physician if any changes in blood sugar concentrations occur {01}

For congestive heart failure patients—Checking with physician if experiencing weight gain or increasing shortness of breath, because of possible worsening of heart failure {01}

For patients who wear contact lenses—Checking with physician if decreased lacrimation occurs {01}


Side/adverse effects
Signs of potential side effects, especially allergy; bradycardia; chest pain; dizziness; dyspnea; edema, generalized; edema, peripheral; hypotension; pain; syncope; weight increase; fever; hematuria; hepatic injury; depression, mental; and thrombocytopenia


General Dosing Information
Dosage must be adjusted to meet the individual requirements of each patient, on the basis of clinical response {01}.

When concurrent carvedilol and clonidine treatment is to be discontinued, carvedilol should be discontinued before clonidine is discontinued {01}. Clonidine should be withdrawn gradually; dosage should be decreased over several days {01}.

When carvedilol is discontinued, its dosage should be tapered over a 1- to 2-week period, especially in patients with ischemic heart disease {01}.

If the patient's pulse rate drops to below 55 beats per minute, the dosage of carvedilol should be reduced {01}.

Hypotensive effects may be additive and orthostatic hypotension may be exaggerated when carvedilol therapy is added to diuretic therapy, or vice versa {01}.

Diet/Nutrition
Taking carvedilol with food may slow the rate of absorption and minimize the risk of orthostatic hypotension {01}.


Oral Dosage Forms

CARVEDILOL TABLETS

Usual adult dose
Congestive heart failure
Initial: Oral, 3.125 mg two times a day for two weeks, taken with food {01}. If tolerated, the dose may be increased to 6.25 mg two times a day {01}. The dosage may then be doubled every two weeks to the highest dose tolerated by the patient {01}.

At each dosage increase, the patient should be observed for one hour for signs of dizziness or lightheadedness {01}.

In patients currently receiving digitalis, diuretics, and/or angiotensin-converting enzyme (ACE) inhibitors, the dosages of these medications should be stabilized prior to starting carvedilol therapy {01}. Before each carvedilol dosage increase, tolerability of carvedilol should be determined by evaluation of the patient for symptoms of worsening heart failure, vasodilation (dizziness, lightheadedness, symptomatic hypotension), or bradycardia {01}. Transient worsening of heart failure may be treated with increased doses of diuretics or it may be necessary to lower the carvedilol dose or temporarily discontinue it {01}. Symptoms of vasodilation may respond to a reduction in the dose of diuretics or ACE inhibitors, and, if still not relieved, a reduction in the carvedilol dose {01}. The dose of carvedilol should not be increased until symptoms of worsening heart failure or vasodilation have stabilized {01}.

Hypertension
Initial: Oral, 6.25 mg two times a day, taken with food {01}. Dose should be maintained for seven to fourteen days and then increased to 12.5 mg two times a day, if tolerated, if blood pressure is not adequately controlled (based on trough blood pressure) {01}. If after the new dose is maintained for seven to fourteen days blood pressure is still not controlled, the dose may be increased to 25 mg two times a day, if tolerated {01}. Standing systolic blood pressure taken one hour after dosing may be used as a guide for tolerance {01}.

Maintenance: Oral, 6.25 to 25 mg two times a day {01}. The full antihypertensive effect occurs within seven to fourteen days {01}.


Usual adult prescribing limits
Congestive heart failure
25 mg two times a day in patients weighing less than 85 kg (187 lbs) and 50 mg two times a day in patients weighing more than 85 kg {01}.

Hypertension
25 mg two times a day {01}.


Usual pediatric dose
Children younger than 18 years of age—Safety and efficacy have not been established {01} {01}.

Strength(s) usually available
U.S.—


3.125 mg (Rx) [Coreg]


6.25 mg (Rx) [Coreg]


12.5 mg (Rx) [Coreg]


25 mg (Rx) [Coreg]

Packaging and storage:
Store between 15 and 30 °C (59 and 86 °F) in a tight, light-resistant container {01}. Protect from moisture {01}.

Auxiliary labeling:
   • Do not take other medicines without your doctor's advice.
   • Take with food.



Developed: 08/13/1998



References
  1. Coreg package insert (SmithKline Beecham—US), Rev 9/95, Rec 10/95; Rev 5/97, Rec 9/97.
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