Celiprolol HCL PCH
Celiprolol HCL PCH Uses, Dosage, Side Effects, Food Interaction and all others data.
Celiprolol HCL PCH is a cardioselective β-blocker. It exhibits intrinsic sympathomimetic and direct vasodilator activity.
Trade Name | Celiprolol HCL PCH |
Generic | Celiprolol |
Celiprolol Other Names | Celiprolol, Celiprololum |
Type | |
Formula | C20H33N3O4 |
Weight | Average: 379.501 Monoisotopic: 379.247106555 |
Protein binding | 25-30%. |
Groups | Approved, Investigational |
Therapeutic Class | Beta-adrenoceptor blocking drugs, Beta-blockers |
Manufacturer | |
Available Country | Netherlands |
Last Updated: | September 19, 2023 at 7:00 am |
![Celiprolol HCL PCH Celiprolol HCL PCH](https://www.medicinesfaq.com/media/png/celiprolol-hcl-pch.png)
Uses
Celiprolol HCL PCH is used for hypertension, angina pectoris.
Celiprolol HCL PCH is also used to associated treatment for these conditions: Angina Pectoris, High Blood Pressure (Hypertension)
How Celiprolol HCL PCH works
Celiprolol HCL PCH 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 HCL PCH 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 HCL PCH 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 HCL PCH 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 HCL PCH
Celiprolol HCL PCH contains Celiprolol see full prescribing information from innovator Celiprolol HCL PCH Monograph, Celiprolol HCL PCH MSDS, Celiprolol HCL PCH FDA label