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Celiprolol: Uses, Dosage, Side Effects & Warnings | DrugsAtlas

Authoritative Clinical Reference

DRUG NAME: Celiprolol

Therapeutic Class: Antihypertensive

Subclass: β1-selective Beta-blocker with Partial β2 Agonist Activity

Specialty: Cardiology

Schedule (India): Schedule H

Route(s): Oral

Formulations Available in India:
• Tablets: 200 mg, 400 mg

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

Indication	Starting Dose	Titration	Maintenance Dose	Maximum Dose	Clinical Notes
Essential Hypertension	200 mg once daily	Increase to 400 mg once daily after 2–4 weeks if inadequate response	200–400 mg once daily	400 mg once daily	Administer on empty stomach (≥30 min before meals); taper gradually before discontinuation, particularly in ischaemic heart disease
Stable Angina Pectoris (mild to moderate)	200 mg once daily	Increase to 400 mg once daily if clinically indicated	200–400 mg once daily	400 mg once daily	Not first-line for angina; consider in patients with concurrent bronchospastic airway disease requiring beta-blocker therapy

Secondary Indications — Adults (Off-label, if any)

Indication	Dose	Duration	Notes	Evidence
Vascular Ehlers-Danlos Syndrome (vEDS) — OFF-LABEL	400 mg once daily	Long-term	Specialist only; requires confirmed genetic diagnosis and multidisciplinary management (cardiology/genetics)	French RCT (Boutouyrie et al.) demonstrated reduction in arterial events; limited data; not standard practice in India

PAEDIATRIC DOSING (Specialist Only)

Primary Indications:
• NOT APPROVED for any indication in children in India
• No paediatric formulations available

Secondary Indications — Paediatrics (Off-label, if any):
• NOT RECOMMENDED in children
• Insufficient safety and efficacy data
• No established Indian practice consensus
• Use only under specialist supervision in exceptional circumstances

RENAL ADJUSTMENT

Renal Function	Recommendation
Mild impairment (eGFR 60–89 mL/min)	No dose adjustment required
Moderate impairment (eGFR 30–59 mL/min)	No dose adjustment required
Severe impairment (eGFR <30 mL/min)	Initiate at 200 mg once daily; monitor blood pressure and heart rate closely
Haemodialysis	Not significantly dialysable; no supplemental dose required

HEPATIC ADJUSTMENT

Child-Pugh Class	Recommendation
Class A (Mild)	No dose adjustment required
Class B (Moderate)	Initiate at 200 mg once daily; monitor for hypotension and bradycardia
Class C (Severe)	Avoid use — impaired hepatic metabolism leads to unpredictable drug effects

CONTRAINDICATIONS

• Sinus bradycardia (<50 beats per minute)
• Second-degree or third-degree atrioventricular block (without pacemaker)
• Acute decompensated heart failure
• Cardiogenic shock
• Severe peripheral arterial occlusive disease
• Active bronchospasm or recent status asthmaticus
• Hypersensitivity to celiprolol or any beta-blocker

CAUTIONS

• Controlled bronchospastic airway disease — use only when benefit exceeds risk; partial β2 agonism offers relative safety
• Diabetes mellitus — may mask autonomic signs of hypoglycaemia
• First-degree AV block — monitor for progression
• Psoriasis — potential exacerbation with beta-blockers
• Pheochromocytoma — use only after adequate alpha-blockade
• Myasthenia gravis — may worsen muscle weakness
• Abrupt discontinuation — taper over 1–2 weeks to prevent rebound tachycardia, hypertension, or angina exacerbation

PREGNANCY

Parameter	Details
Risk summary	Limited human data; animal studies suggest relatively low risk
Preferred alternatives	Labetalol, methyldopa
When may be used	Only if benefit outweighs risk; under obstetric cardiology supervision
Monitoring	Maternal blood pressure; fetal growth (beta-blockers associated with IUGR); neonatal bradycardia and hypoglycaemia

LACTATION

Parameter	Details
Compatibility	Likely compatible — minimal excretion into breast milk
Preferred alternatives	Labetalol if beta-blocker required
Drug level in milk	Low
Infant monitoring	Bradycardia, poor feeding, inadequate weight gain

ELDERLY

• Starting dose: 200 mg once daily
• Titration: Slower increments over 3–4 week intervals preferred
• Special considerations:

Increased susceptibility to orthostatic hypotension
Greater risk of bradycardia and conduction disturbances
Reduced hepatic and renal reserve may prolong drug effects
Fall risk assessment advised

MAJOR DRUG INTERACTIONS

Interacting Drug	Effect	Recommendation
Verapamil, Diltiazem	Severe bradycardia, AV block, myocardial depression	Avoid combination
Class I antiarrhythmics (disopyramide, quinidine)	Additive negative inotropy and conduction delay	Avoid combination
Clonidine	Rebound hypertensive crisis on clonidine withdrawal	Discontinue celiprolol first; then taper clonidine
MAO inhibitors	Potential hypertensive crisis	Avoid concurrent use

MODERATE DRUG INTERACTIONS

Interacting Drug	Effect	Recommendation
ACE inhibitors, ARBs, diuretics	Additive hypotensive effect	Monitor blood pressure
NSAIDs	Attenuation of antihypertensive efficacy	Monitor blood pressure; consider alternatives
CYP2D6 inhibitors (fluoxetine, paroxetine)	Potential increase in celiprolol levels	Monitor clinical response
Insulin, sulfonylureas	Masking of hypoglycaemic symptoms (tachycardia, tremor)	Counsel diabetic patients; monitor glucose closely
Digoxin	Additive bradycardia	Monitor heart rate

COMMON ADVERSE EFFECTS

• Headache
• Fatigue
• Dizziness
• Gastrointestinal disturbances (nausea, dyspepsia)
• Palpitations (related to partial β2 agonist activity)
• Cold extremities

SERIOUS ADVERSE EFFECTS

• Symptomatic bradycardia requiring intervention
• Bronchospasm (particularly in susceptible patients)
• Worsening or precipitation of heart failure
• Severe hypotension
• High-grade AV block
• Skin reactions (rare)
• Peripheral vasospasm (Raynaud’s phenomenon) — rare

MONITORING REQUIREMENTS

Phase	Parameters
Baseline	Blood pressure, heart rate, ECG (if cardiac history present), renal and hepatic function
After initiation/dose change	Blood pressure and heart rate weekly for 2–4 weeks
Long-term	Blood pressure, heart rate, clinical assessment for heart failure signs; periodic renal and hepatic function in elderly or at-risk patients

BRANDS AVAILABLE IN INDIA

• Cardiatens (400 mg)
• Celol (200 mg, 400 mg)
• Celipro (200 mg, 400 mg)

PRICE RANGE (INR)

Formulation	Approximate Price
Tablet 200 mg	₹10–15 per tablet
Tablet 400 mg	₹18–25 per tablet

• Not included in NLEM; not under NPPA price control
• Limited availability in government supply chains

CLINICAL PEARLS

• Partial β2 agonist activity distinguishes celiprolol from other beta-blockers; may offer relative bronchospasm protection in selected patients with airway disease
• Less bradycardic than atenolol or metoprolol — useful in patients with borderline low heart rate
• Bioavailability reduced by food — counsel patients to take on empty stomach, at least 30 minutes before breakfast
• Long elimination half-life supports once-daily administration
• Not routinely preferred for post-myocardial infarction or heart failure — lacks strong outcome evidence in these settings
• Consider alternatives in significant hepatic impairment due to unpredictable metabolism

Clinical Responsibility

This platform is designed strictly for healthcare professionals. Data provided is synthesized from authoritative pharmacological sources and clinical registries. Do not use for consumer medical decisions. Always verify critical dosing and contraindications with official institutional protocols and peer-reviewed journals.

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