Celiprolol

Celiprolol is an Antihypertensive belonging to the pharmacology class of β-blocker.

It is used in the Treatment of angina, hypertension.

Celiprolol is incompletely absorbed from the GI tract. Food may impair its bioavailability which Crosses the placenta with Plasma protein binding: Approx 25% and undergoes Minimal metabolism which gets excreted Via urine and faeces (as unchanged drug). Elimination half-life: Approx 5-6 hr.

Celiprolol is available in the form of dosage forms as tablets.

Celiprolol is available in India, France, Japan, and the USA.

Celiprolol is a vasoactive beta-1 selective adrenoceptor antagonist with partial beta-2 agonist activity. The beta-2 agonist activity is thought to account for its mild vasodilating properties. It lowers blood pressure in hypertensive patients at rest and on exercise. The effects on heart rate and cardiac output are dependent on the pre-existing background level of sympathetic tone. Under conditions of stress such as exercise, celiprolol attenuates chronotropic and inotropic responses to sympathetic stimulation.

Celiprolol is available in the form of tablets.

Celiprolol tablets to be swallowed whole with water.

Celiprolol comes as a tablet to be taken by mouth. It is usually taken two times a day.

Celiprolol is used in the Treatment of angina, hypertension.

Celiprolol is a cardio-selective β-blocker. It exhibits intrinsic sympathomimetic and direct vasodilator activity.

Celiprolol is approved for use in the following clinical indications

• Angina
• Hypertension

Celiprolol is available in the form of Tablet.

Celiprolol is available in various dosage strengths as 200 mg, 400 mg.

Celiprolol is available in the form of Tablet.

Dose Adjustment in Hepatic Impairment Patient:

CrCl >40 mL/minute: There are no dosage adjustments provided in the manufacturer’s labeling.

CrCl 15 to 40 mL/minute: Reduce dose by 50%.

CrCl <15 mL/minute: Use not recommended.

Celiprolol may be contraindicated in the following:

Heart block (2nd or 3rd degree), sick-sinus syndrome, cardiogenic shock, uncontrolled heart failure, severe bradycardia, severe renal impairment (CrCl <15 mL/min), acute episodes of asthma, untreated phaeochromocytoma, metabolic acidosis, hypotension, severe peripheral arterial circulatory disturbances.

The adverse reactions related to molecule Celiprolol can be categorized as

• Common Adverse effects:

Headache, fatigue, dizziness, hot flushes, asthenia, somnolence and insomnia

• Less Common adverse effect:

Tremor and palpitations; bronchospasm, skin rashes and/or visual disturbances.

• Rare adverse effects:

Depression, hypersensitivity pneumonitis.

The clinically relevant drug interactions of Celiprolol are briefly summarized here:

• May exacerbate rebound HTN upon withdrawal of clonidine.
• May increase AV conduction time w/ digitalis glycosides.
• Reduced bioavailability w/ concomitant hydrochlorothiazide, chlorthalidone or theophylline.
• Concomitant dihydropyridine Ca channel blockers (e.g. nifedipine)
• May increase the risk of hypotension and heart failure.

The common side of Celiprolol include the following:

Headache, fatigue, dizziness, hot flushes, asthenia, somnolence and insomnia.

The use of Celiprolol should be prudent in the following group of special populations:

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.

Geriatric Use

There is no FDA guidance on the use of Celiprolol in geriatric settings.

Pharmacodynamics:

Celiprolol is a vasoactive beta-1 selective adrenoceptor antagonist with partial beta-2 agonist activity. The beta-2 agonist activity is thought to account for its mild vasodilating properties. It lowers blood pressure in hypertensive patients at rest and on exercise. The effects on heart rate and cardiac output are dependent on the pre-existing background level of sympathetic tone. Under conditions of stress such as exercise, celiprolol attenuates chronotropic and inotropic responses to sympathetic stimulation.

Pharmacokinetics:

Absorption:

Incompletely absorbed from the GI tract. Food may impair its bioavailability.

Distribution:

Crosses the placenta. Plasma protein binding: Approx 25%.

Metabolism:

Minimal metabolism.

Excretion:

Via urine and faeces (as unchanged drug). Elimination half-life: Approx 5-6 hr.

• https://www.pfizer.com/products/product-detail/altace
• https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/022021s008lbl.pdf
• https://go.drugbank.com/drugs/DB00178