Heart Failure, Left Ventricular Dysfunction, Post-Myocardial Infarction, Hypertension
Dosage and administrations:
Initial: 3.125mg bid for 2 weeks
Titrate: If tolerated, may increase dose to 6.25mg, 12.5mg, and 25mg bid over successive intervals of at least 2 weeks
Max: 50mg bid in patients with mild to moderate heart failure (HF) weighing >85kg.
Left Ventricular Dysfunction Post-Myocardial Infarction
Initial: 6.25mg bid
Titrate: Increase after 3-10 days, based on tolerability, to 12.5mg bid, then again to target dose of 25mg bid
May use lower starting dose and/or slower titration
Initial: 6.25mg bid
Titrate: If needed, based on blood pressure control, may increase to 12.5mg bid, then to 25mg bid over intervals of 7-14 days
Note: in Elderly/Patients at Increased Risk of Hypotension, Dizziness, or Syncope, increase doses, as appropriate, after an interval of at least 2 weeks.
Pregnancy and breastfeeding:
Pregnancy: Category C.
Lactation: Not for use in nursing.
Bronchial asthma or related bronchospastic conditions, 2nd- or 3rd-degree atrioventricular (AV) block, sick sinus syndrome, severe bradycardia, cardiogenic shock, decompensated HF requiring IV inotropic therapy, severe hepatic impairment.
Warning and precautions:
Minimize fluid retention prior to initiation of treatment.
Severe exacerbation of angina and occurrence of MI and ventricular arrhythmias reported in angina patients following abrupt discontinuation; discontinue therapy over 1-2 weeks whenever possible.
If angina worsens or acute coronary insufficiency develops, promptly reinstitute therapy, at least temporarily.
Avoid abrupt discontinuation even in patients treated only for HTN or HF.
Bradycardia reported; reduce dose if HR drops <55 BPM.
Hypotension, postural hypotension, and syncope reported; highest risk during the first 30 days of dosing.
May impair mental/physical abilities.
Worsening HF or fluid retention may occur during up-titration; if such symptoms occur, increase dose of diuretics.
If deemed necessary, use with caution in patients with bronchospastic disease who do not respond to, or cannot tolerate, other antihypertensives.
May mask signs of hypoglycemia and hyperthyroidism (eg, tachycardia).
May exacerbate symptoms of hyperthyroidism or precipitate thyroid storm with abrupt withdrawal.
May lead to worsening hyperglycemia in HF patients with diabetes.
May precipitate or aggravate symptoms of arterial insufficiency in patients with peripheral vascular disease.
Rarely, use in patients with HF resulted in deterioration of renal function; discontinue or reduce dosage if worsening of renal function occurs.
Chronically administered therapy should not be routinely withdrawn prior to major surgery; may augment risks of general anesthesia and surgical procedures.
Caution with pheochromocytoma and Prinzmetal’s variant angina. Patients with history of severe anaphylactic reaction to a variety of allergens may be more reactive to repeated challenge and may be unresponsive to usual doses of epinephrine.
Intraoperative floppy iris syndrome observed during cataract surgery.
Bradycardia, fatigue, hypotension, dizziness, headache, diarrhea, N/V, hyperglycemia, weight increase, increased cough, asthenia.
Potent CYP2D6 inhibitors (eg, quinidine, fluoxetine, propafenone) may increase levels. Monitor closely for signs of hypotension and/or severe bradycardia with drugs that can deplete catecholamines (eg, reserpine, MAOIs).
Potentiated BP- and HR-lowering effects with clonidine; when coadministration is to be terminated, d/c therapy several days before clonidine is withdrawn.
May increase cyclosporine levels; monitor concentrations and adjust dose of cyclosporine as appropriate.
Increased risk of bradycardia with digitalis glycosides. May increase digoxin levels; monitor digoxin. Rifampin may reduce levels.
Cimetidine may increase exposure.
Amiodarone and its metabolite desethyl amiodarone, CYP2C9 inhibitors, and P-gp inhibitors may increase levels.
Amiodarone or other CYP2C9 inhibitors (eg, fluconazole) may enhance β-blocking properties; monitor for signs of bradycardia or heart block.
Conduction disturbance reported with diltiazem; monitor ECG and BP with calcium channel blockers of the verapamil or diltiazem type.
May enhance blood glucose-reducing effect of insulin and oral hypoglycemics; regularly monitor blood glucose.
If treatment is to be continued perioperatively, use caution when anesthetic agents that depress myocardial function (eg, ether, cyclopropane, trichloroethylene) are used.
Additive effects and exaggerated orthostatic component with diuretics.
Store below 30°C. Protect from moisture.
Keep out of reach of children.