Celiprolol

Uses

Celiprolol is used for hypertension, angina pectoris.

Celiprolol is also used to associated treatment for these conditions: Angina Pectoris, High Blood Pressure (Hypertension)

How Celiprolol works

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. However, at rest minimal impairment of cardiac function is seen.

Dosage

Celiprolol dosage

Adult: 200-400 mg once daily.

Side Effects

Headache, fatigue, dizziness, hot flushes, asthenia, somnolence and insomnia; tremor and palpitations; bronchospasm, skin rashes, visual disturbances.

Toxicity

No data are available regarding celiprolol overdose in humans. The most common symptoms to be expected following overdosage with beta-adrenoceptor blocking agents are bradycardia, hypotension, bronchospasm and acute cardiac insufficiency.

Precaution

Patients with 1st degree heart block, well-controlled CHF, DM, untreated phaeochromocytoma, history of psoriasis. Avoid abrupt withdrawal as it may increase the risk of angina. Patients undergoing surgery involving general anaesth. May mask symptoms of hypoglycaemia and thyrotoxicosis hyperthyroidism. Hepatic and mild to moderate renal impairment. Pregnancy and lactation.

Interaction

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

Food Interaction

• Avoid fruit juice. Orange juice may reduce the absorption of celiprolol.
• Avoid grapefruit products. Grapefruit juice may reduce the absorption of celiprolol.
• Take with or without food. The bioavailability of celiprolol may be reduced when taken with food, however, it is unlikely that this reduction is clinically relevant.

Volume of Distribution

The distribution volume is 4.5L/kg. Celiprolol is hydrophilic and does not cross the blood-brain barrier. The binding to plasma proteins is about 25-30%.

Elimination Route

Absorption of an oral dose is rapid and consistent but incomplete (55% for 200 mg dose and 74% for 400 mg dose) from the gastrointestinal tract. The bioavailability of celiprolol has been shown to be markedly affected by food and one should avoid administration of celiprolol with food. Coadministration of chlorthalidone, hydrochlorothiazide and theophylline also reduces the bioavailability of celiprolol. Following oral dosing, maximal blood concentrations are reached between 2 and 3 hours.

Half Life

5 hours

Clearance

Cleared by both renal and non-renal excretory pathways. Celiprolol is not recommended for patients with creatinine clearance less than 15 mL per minute.

Pregnancy & Breastfeeding use

Pregnancy catagory B in 2nd trimesters and catagory D in 3rd trimesters

Contraindication

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, or severe peripheral arterial circulatory disturbances.

Storage Condition

Store below 25°C.

Innovators Monograph

You find simplified version here Celiprolol