Celiprolol Hydrochloride

• Essential Hypertension:
  Used alone or in combination with other antihypertensive agents to lower elevated blood pressure in adults.
• Angina Pectoris:
  Treatment of stable angina to reduce frequency and severity of anginal attacks.
• Off-label/Additional Uses:
  Occasionally used in prevention of migraine and to improve symptoms in some patients with heart failure, though not a first-line indication.

Adults:

• Hypertension:
  Initial dose is typically 200 mg orally once daily. Maintenance dose ranges from 200 mg to 400 mg daily in one or two divided doses.
• Angina Pectoris:
  Usual dose is 200 mg once daily; may increase up to 400 mg daily depending on response.

Elderly:

• Start at lower doses with cautious titration, usually 200 mg once daily; adjust based on tolerance and effect.

Pediatrics:

• Safety and efficacy not established.

Renal Impairment:

• Use with caution in severe renal impairment; dosage adjustment may be necessary.

Hepatic Impairment:

• Use caution; start with lower doses and monitor.

Administration:

• Oral tablets taken with water; may be administered with or without food.

Celiprolol is a selective β1-adrenergic receptor antagonist with additional β2-adrenergic receptor partial agonist activity. By selectively blocking β1 receptors in cardiac tissue, it reduces heart rate, myocardial contractility, and cardiac output, leading to decreased oxygen demand and lowering blood pressure. The β2 partial agonist effect causes vasodilation, especially in peripheral blood vessels, which helps reduce vascular resistance and contributes to antihypertensive effects. This dual action improves myocardial oxygen supply and reduces angina symptoms.

• Absorption:
  Well absorbed orally with bioavailability approximately 40–50% due to first-pass metabolism.
• Distribution:
  Volume of distribution ~3.4 L/kg; plasma protein binding approximately 13%.
• Metabolism:
  Hepatic metabolism via cytochrome P450 enzymes, primarily CYP2D6.
• Elimination:
  Excreted mainly by the kidneys as unchanged drug and metabolites.
• Half-life:
  Approximately 5 to 8 hours.
• Onset of Action:
  Antihypertensive effect observed within 2 hours; peak effect at 3 to 4 hours.

• Pregnancy:
  Classified as FDA Pregnancy Category C. Animal studies show adverse effects at high doses; limited human data. Use only if benefits outweigh risks.
• Lactation:
  Excreted in breast milk in small amounts; caution advised when administered to nursing mothers.

• Beta-adrenergic receptor blocker (Beta-blocker)
• Selective β1 antagonist with β2 partial agonist properties

• Known hypersensitivity to celiprolol or other beta-blockers.
• Bradycardia (<50 bpm), severe sinus node dysfunction.
• Second- or third-degree atrioventricular block without pacemaker.
• Cardiogenic shock or overt cardiac failure.
• Severe peripheral arterial disease (e.g., Raynaud’s disease).
• Severe asthma or bronchospastic conditions.

• Cardiac Monitoring: Use with caution in patients with heart failure or conduction abnormalities.
• Abrupt Withdrawal: Avoid sudden discontinuation to prevent angina exacerbation or myocardial infarction.
• Bronchospastic Disease: Use cautiously in patients with reactive airway disease due to potential β2 blockade.
• Diabetes: May mask hypoglycemia symptoms; monitor blood glucose carefully.
• Peripheral Vascular Disease: May worsen symptoms.

Common:

• Cardiovascular: Bradycardia, hypotension, palpitations
• CNS: Dizziness, headache, fatigue
• Gastrointestinal: Nausea, diarrhea
• Respiratory: Dyspnea, wheezing (rare)

Serious/Rare:

• Severe bradycardia, heart block
• Bronchospasm
• Hypoglycemia masking
• Depression or mood changes (rare)

• Calcium Channel Blockers (verapamil, diltiazem): Additive negative chronotropic effects; risk of bradycardia and heart block.
• Other Antihypertensives: May potentiate hypotensive effects.
• Insulin and Oral Hypoglycemics: May mask hypoglycemia symptoms; adjust doses carefully.
• CYP2D6 Inhibitors (e.g., fluoxetine, paroxetine): May increase celiprolol plasma concentrations.
• NSAIDs: May reduce antihypertensive effect.

• Recent hypertension management guidelines acknowledge celiprolol as an effective selective beta-blocker with vasodilatory properties, favorable in patients with peripheral vascular disease.
• No major new safety warnings reported recently.
• Emphasis on gradual dose tapering to avoid rebound cardiovascular events.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from moisture and light.
• Keep in a tightly closed container.
• Do not freeze.
• Keep out of reach of children.