Celiprolol

BRAND NAMES

• Cardem 

• Selectol 

• Celipres / Celipress 

• Celipro 

• Celol 

• Cordiax 

MECHANISM OF ACTION 

Celiprolol works as a selective beta-blocker. It mainly blocks β1-adrenergic receptors in the heart, which reduces heart rate, decreases the force of contraction, and lowers cardiac output—leading to reduced blood pressure. At the same time, it has partial β2-agonist activity, which can cause mild vasodilation (relaxation of blood vessels) and may reduce bronchoconstriction compared to non-selective beta-blockers.

PHARMACOKINETICS

Absorption

Celiprolol is moderately absorbed after oral administration. Its bioavailability is about 30–50%, and it is absorbed mainly in the small intestine. Food can slightly reduce or delay its absorption.

Ditribution

Celiprolol is moderately distributed in the body, with relatively low protein binding (about 25–30%). It does not easily cross the blood–brain barrier, so central nervous system effects are limited. It is distributed mainly in extracellular fluids.

Metabolism

Celiprolol is minimally metabolized in the liver. Most of the drug remains unchanged in the body and is primarily excreted through the kidneys, which reduces the likelihood of significant drug interactions.

Excretion

Celiprolol is mainly eliminated unchanged in the urine via the kidneys. About 70–80% of the administered dose is excreted in urine within 24 hours, with a half-life of 8–10 hours, allowing for once- or twice-daily dosing.

PHARMACODYNAMICS

Celiprolol is a β₁-selective blocker with β₂ agonist activity that slows the heart, reduces contraction force, and lowers blood pressure, while mild vasodilation helps maintain blood flow and reduce side effects.

Administration

Celiprolol is given orally (by mouth) in tablet form. It is usually taken once or twice daily, preferably at the same time each day, as prescribed by a doctor. It should be taken regularly for best control of blood pressure and not stopped suddenly without medical advice.Top of FormBottom of Form

Dosage and Strength

• Adults: Typically start with 200 mg once daily in the morning.

• Dose may be increased to up to 400 mg once daily based on blood pressure response.
• Can be taken with or without food.
• Elderly or patients with kidney/liver impairment may require dose adjustment.
• Do not stop suddenly; taper gradually under medical supervision to avoid worsening angina or blood pressure.

DRUG INTERACTIONS

• Other antihypertensives (e.g., ACE inhibitors, diuretics, calcium channel blockers) may enhance blood pressure-lowering effects, sometimes causing hypotension. 
• Antiarrhythmic drugs (e.g., amiodarone, digoxin) can increase the risk of bradycardia or heart block. 
• NSAIDs may reduce the blood pressure-lowering effect of celiprolol. 
• Insulin or oral antidiabetic drugs: celiprolol can mask symptoms of low blood sugar (like rapid heartbeat). 
• CYP2D6 inhibitors may slightly increase celiprolol levels, although it is minimally metabolized. 

FOOD INTERACTIONS

Celiprolol can be taken with or without food, as food does not significantly affect its absorption or effectiveness. However, alcohol should be limited, as it may increase blood pressure-lowering effects and cause dizziness or fainting. Grapefruit juice does not have a major impact on celiprolol.

CONTRAINDICATIONS

Celiprolol is contraindicated in patients with severe asthma orbronchospasm, bradycardia, heart block, severe heart failure, or very low blood pressure. It should also be avoided in individuals with a known allergy to celiprolol or other beta-blockers, and caution is required in those with severe kidney or liver impairment, as the drug may accumulate and cause adverse effects.

SIDE EFFECTS

1. Dizziness and headache

2. Fatigue and sleep disturbances

3. Nausea and dry mouth

4. Cold hands or feet

5. Slow heartbeat (bradycardia)

6. Shortness of breath (rare)

7. Mood changes or depression (rare)

8. Erectile dysfunction (rare)

OVER DOSE

1. Severe low blood pressure (hypotension)

2. Extremely slow heart rate (bradycardia)

3. Heart block or cardiac shock

4. Dizziness, fainting, fatigue

5. Shortness of breath

TOXICITY

Toxicity occurs mainly in overdose and results from excessive β-blockade. It can cause severe bradycardia, hypotension, dizziness, bronchospasm, and heart failure, and in extreme cases may lead to shock or cardiac arrest. Treatment is supportive and requires urgent medical care.