Beta Blocker (with Intrinsic Sympathomimetic Activity)

Hypersensitivity to celiprolol or other beta-blocking agents; sinus bradycardia; heart block greater than first-degree (except in patients with a functioning artificial pacemaker); cardiogenic shock; uncompensated cardiac failure

Administer cautiously in compensated heart failure and monitor for a worsening of the condition. Avoid abrupt discontinuation in patients with a history of CAD; slowly wean while monitoring for signs and symptoms of ischemia. Use caution with concurrent use of beta-blockers and either verapamil or diltiazem; bradycardia or heart block can occur. In general, beta-blockers should be avoided in patients with bronchospastic disease. Use cautiously in PVD (can exacerbate arterial insufficiency). Can mask signs of thyrotoxicosis. Dosage adjustment is required in patients with renal dysfunction. Use care with anesthetic agents that decrease myocardial function.

Cardiovascular: Bradycardia, A-V block, Raynaud's syndrome, congestive heart failure, sinus bradycardia, myocardial depression

Central nervous system: Insomnia, dizziness, headache, depression

Gastrointestinal: Nausea, diarrhea, xerostomia

Neuromuscular & skeletal: Tremors

Expected interactions:

Ampicillin, in single doses of 1 gram, decrease celiprolol's pharmacologic actions.

Antacids (magnesium-aluminum, calcium antacids or salts) may reduce the bioavailability of celiprolol.

Clonidine: Hypertensive crisis after or during withdrawal of either agent.

Drugs which slow AV conduction (digoxin): Effects may be additive with beta-blockers.

Glucagon: Celiprolol may blunt the hyperglycemic action of glucagon.

Insulin and oral hypoglycemics: Celiprolol masks the tachycardia that usually accompanies hypoglycemia.

NSAIDs (ibuprofen, indomethacin, naproxen, piroxicam) may reduce the antihypertensive effects of beta-blockers.

Salicylates may reduce the antihypertensive effects of beta-blockers.

Sulfonylureas: Beta-blockers may alter response to hypoglycemic agents.

Verapamil or diltiazem may have synergistic or additive pharmacological effects when taken concurrently with beta-blockers.

Selective beta₁-adrenergic blocking agent with weak alpha₂ receptor blocking activity; beta₂-adrenergic agonist and intrinsic sympathomimetic activity

Absorption: 30% to 74% (reduced by food)

Protein binding: 25%

Half-life: 4-10 hours

Peak plasma level: 2-4 hours

Elimination: Renal (50%)

Oral: 200-600 mg once daily; no dosage alteration needed the in elderly

Monitor blood pressure, apical and radial pulses, I & O, daily weight, respirations, and circulation in extremities before and during therapy

Celiprolol is a selective beta-1 blocking agent with intrinsic sympathomimetic activity (ISA). This drug possesses intrinsic sympathomimetic activity. While beta-blockers with intrinsic sympathomimetic activity induce fewer side effects, the cardiovascular benefits listed below are less clear than for beta-blockers without intrinsic sympathomimetic activity.

Myocardial infarction: Beta-blockers, in general without intrinsic sympathomimetic activity (ISA), have been shown to decrease morbidity and mortality when initiated in the acute treatment of myocardial infarction and continued long-term. In this setting, therapy should be avoided in patients with hypotension, cardiogenic shock, or heart block. See the Special Topic - Myocardial Infarction.

Surgery: Atenolol has also been shown to improve cardiovascular outcomes when used in the perioperative period in patients with underlying cardiovascular disease who are undergoing noncardiac surgery. Bisoprolol in high-risk patients undergoing vascular surgery reduced the perioperative incidence of death from cardiac causes and nonfatal myocardial infarction. See the Special Topic - Perioperative Considerations for Noncardiovascular Surgery in Patients With Heart Disease.

Atrial fibrillation: Beta-blocker therapy provides effective rate control in patients with atrial fibrillation.

Angina: Beta-blockers are effective in the treatment of 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. See the Special Topic - Angina.

Withdrawal: Beta-blocker therapy should not be withdrawn abruptly, but gradually tapered to avoid acute tachycardia and hypertension.

Heart failure: There is emerging evidence that beta-blocker therapy, without intrinsic sympathomimetic activity (ISA), should be initiated in select patients with stable congestive heart failure (NYHA Class II-III). 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. See the Special Topic - Heart Failure.

Can cause decrease in serum cholesterol. HDL increases noted. Can cause increase in thyroid function tests. Reduction in fibrinogen levels have been described.

"Consensus Recommendations for the Management of Chronic Heart Failure. On Behalf of the Membership of the Advisory Council to Improve Outcomes Nationwide in Heart Failure," Am J Cardiol, 1999, 83(2A):1A-38A.

Gibbons RJ, Chatterjee K, Daley J, et al, "ACC/AHA/ACP-ASIM Guidelines for the Management of Patients With Chronic Stable Angina: a Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines," J Am Coll Cardiol, 1999, 33(7):2092-197.

Ryan TJ, Anderson JL, Antman EM, et al, "ACC/AHA Guidelines for the Management of Patients With Acute Myocardial Infarction. A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee on Management of Acute Myocardial Infarction)," J Am Coll Cardiol, 1996, 28(5):1328-428.