BACKGROUND: Celiprolol is a beta-adrenergic blocker characterized by selective blokade of beta1 receptors and partial agonist activity at beta2 receptors. This study was designed to evaluate the antihypertensive efficacy, metabolic effects and safety of celiprolol in patients with essential hypertension. METHODS: Celiprolol 200mg was administered once daily in 20 hypertensive Korean adults(9 males and 11 females) for ten weeks with dose titration every 2 weeks. RESULTS: The supine blood pressure was decreased from 168.8+/-20.6/106.5/12.0mmHg(mean/S.D) to 131.2+/-12.8/88.2+/-7.9mmHg at the end treatment(P<0.05). Heart rate was not changed significantly throughout the period. Total cholesterol(TC) was decreased from 211.3+/-12.6mg/dl to 186.7+/-10.4mg/dl(P<0.05) and triglyceride(TG) from 223.7+/-24.5mg/dl to 198.4+/-12.9mg/dl after 10 weeks treatment(P<0.05). LDL(low-density lipoprotein)-cholesterol was decreased from 126.4+/-13.4mg/dl to 118.5+/-12.3mg/dl after 10 weeks treatment(P<0.05). During the period of the study, headache and fatigue developed in a few patient but were not troublesome enough to stop medication. CONCLUSIONS: Celiprolol 200mg once daily regimen was well tolerated and effective in the treatment of essential hypertensiove patients with favorable effects on blood lipids.
Blood Pressure ; Celiprolol* ; Fatigue ; Headache ; Heart Rate ; Humans ; Hypertension ; Male

BACKGROUND: Celiprolol is a new generation beta-adrenoreceptor blocking agent with intrinsic sympathomimetic activity characterized by selective blockade of beta1 receptors and partial agonist activity at beta2 receptors. This study was designed to investigate the antihypertensive efficacy and safety of celiprolol in patients with essential hypertension. METHODS: The study subjects consisted of 36 patients(mean age : 55 years, 11 males, 25 females). Celiprolol was administered orally in a aily dose of 200-800mg once or two divided dose for 10 weeks after the admimstration of placebo for 2 weeks. RESULTS: Blood pressure was significantly reduced from 171+/-19/106.8mmHg to 153+/-20/92+/-12mmHg(p<0.01) after 2 week of therapy and this effect was maintained throughout the study periods. The efficacy rates were total 94%(marked improve : 53%, moderate improve : 22%, mild improve : 19%). The cumulative efficacy rate was 72% at 200mg/day, 91% at 400mg/day, and 94% at 800mg/day. Heart rate did not change throughout 10 weeks. There were no significant change in hematologic and blood chemistry variables. During the period of medication, headache developed in 3 cases(8%) and each of dry cough, dyspnea, epigastric pain and diarrhea and facial flushing developed in 1 case(2.8%) but they were tolerable. CONCLUSIONS: This results suggest that celiprolol is effective and safe drug in the treament of patients with essential hypertension.
Blood Pressure ; Celiprolol* ; Chemistry ; Cough ; Diarrhea ; Dyspnea ; Flushing ; Headache ; Heart Rate ; Humans ; Hypertension* ; Male

To investigate the inhibitory effect of Pluronic on P-glycoprotein (P-gp) drug efflux pump, Caco-2 cells and animal models were established to study the influence of Pluronic on celiprolol transport across Caco-2 cell monolayer and intestinal mucous membrane with verapamil set as a positive control. Drug concentration was measured by HPLC and the apparent permeability coefficient (P(app)), absorption rate constant (k(a)) and the effective permeability coefficient (P(eff)) were calculated. P(app) of basolateral to apical side and apical to basolateral side was (2.10 +/- 0.13) x 10(-6) and (0.333 +/- 0.018) x 10(-6) cm x s(-1), respectively. Transports of celiprolol across Caco-2 cell monolayer were influenced by both verapamil and Pluronic. The absorption constants (k(a)) of celiprolol at duodenum, jejunum, ileum, and colon were (0.09 +/- 0.03), (0.14 +/- 0.04), (0.11 +/- 0.03) and (0.05 +/- 0.02) h(-1), k(a) of celiprolol in verapamil group were (0.14 +/- 0.03), (0.24 +/- 0.02), (0.25 +/- 0.03) and (0.23 +/- 0.02) h(-1), and k(a) of celiprolol in Pluronic group were (0.13 +/- 0.02), (0.22 +/- 0.02), (0.22 +/- 0.03) and (0.20 +/- 0.03) h(-1), respectively. Pluronic showed significant effect on inhibiting P-gp of Caco-2 cell and intestinal mucosa in rats.
ATP-Binding Cassette, Sub-Family B, Member 1 ; metabolism ; Animals ; Biological Transport ; drug effects ; Caco-2 Cells ; Celiprolol ; pharmacokinetics ; Excipients ; Humans ; Intestinal Absorption ; drug effects ; Intestinal Mucosa ; metabolism ; Jejunum ; metabolism ; Male ; Permeability ; Poloxamer ; administration & dosage ; pharmacology ; Rats ; Rats, Sprague-Dawley