Celiprolol
Brand name:- Celipres 100, 200mg tab.
Celiprolol is a beta blocker that works specifically on the heart. It works by slowing down the heart rate and makes the heart more efficient at pumping blood around the body.
Pharmacodynamic:-
In animals, the β-adrenoceptor blocking activity of celiprolol is more potent than that of sotalol and practolol, and about equipotent with that of propranolol but in man it is about 4 times less potent than atenolol. However, dose-ranging studies employing a range of doses in the same subjects have not been reported and it is possible that celiprolol’s potency has been underestimated. β-Blockade following a single oral dose of 400mg in man can be detected at 24 hours and once-daily dosing is effective in hypertension and angina.
Using the standard animal models celiprolol is more selective for the β1- than the β2-adrenoceptor, and in patients with angina the reduction in blood pressure following exercise was larger after treatment with celiprolol than propranolol, suggesting a degree of cardioselectivity. Studies in guinea-pig atria show that celiprolol has a small degree of partial agonist activity and one report suggests that it has no membrane stabilising activity.
Celiprolol has weak α-adrenoceptor antagonist activity which in early studies was thought responsible for the bronchodilating and vasodilating effects of the drug in animals, but these effects are now considered to be due to β2-adrenoceptor agonist activity and/or a direct (papaverine-like) smooth muscle relaxing effect.
In animals celiprolol caused a smaller reduction in the maximum rate of change of left ventricular pressure than metoprolol, acebutolol, atenolol and propranolol and actually increased stroke volume and femoral artery flow. After experimental coronary artery occlusion in dogs celiprolol had little effect on heart rate, stroke volume, left ventricular output and total peripheral resistance, while atenolol and propranolol had the expected depressant effects. Similar effects have been observed in patients with coronary artery disease in studies comparing celiprolol with atenolol, metoprolol, propranolol and pindolol.
Studies in animals have shown celiprolol to have a bronchodilator action unaffected by propranolol. Single-dose studies in man indicate that, while propranolol and atenolol reduce FEV1 and FVC in asthmatic patients, celiprolol is not significantly different from placebo and may increase lung function in some patients. The apparent effects of celiprolol on respiratory function have been confirmed in a 12-week study in hypertensive patients with reversible bronchial obstruction, although further well designed trials in large numbers of asthmatic patients are required to determine its long term effects in patients with asthma.
Only limited data are available on the effects of celiprolol on carbohydrate and lipid metabolism. Using the glucose clamp technique there was no difference in insulin requirements in 10 Type I diabetic patients who were treated with either celiprolol or placebo but in Type II patients celiprolol 300mg caused significantly reduced blood glucose concentrations in the middle of the afternoon compared with placebo. In patients with Fredrickson Type II or IV hyperlipidaemia 4 weeks’ treatment with celiprolol increased high density lipoprotein concentrations but not the concentrations of other lipids, while there were no changes after metoprolol or placebo.
Pharmacokinetics:-
Pharmacokinetics of celiprolol in man are limited. Absorption is dose-dependent, increasing with higher doses. The drug is eliminated from the plasma with a half-life of about 4 to 5 hours. Half of an intravenously administered dose and 10 to 15% of an oral dose appear in the urine within 3 days, the rest being excreted in the faeces. In patients with renal dysfunction, systemic clearance was reduced and may necessitate a reduction in dosage. Preliminary data suggest that bioavailability is decreased and renal clearance increased in patients with cirrhosis.
Mechanism of action:-
🚫 NOT AVAILABLE.
Used:-
Used in the treatment of Hypertension (high blood pressure) and Angina (heart-related chest pain).
Side effects:-
Nausea, Headache, Dizziness, Sleepiness, Depression, Raynaud's phenomenon, Xerostomia, Erectile dysfunction.
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