Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0020473 (hyperlipidemia)
 15,891 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The effects of celiprolol 200 mg or 400 mg once daily on blood pressure (BP), serum lipids, plasma fibrinogen and airways function was compared with the effects of metoprolol 100 mg or 200 mg once daily in 171 patients with mild to moderate hypertension and coexistent hyperlipidaemia in a double-blind, multicentre study lasting 1 year. Significant decreases in systolic and diastolic blood pressure and heart rate were observed compared with baseline (DBP: celiprolol -13.3 mm Hg, P < 0.0001; metoprolol -14.3 mm Hg, P < 0.0001; SBP: celiprolol -18.2 mm Hg, P < 0.0001; metoprolol -20.5 mm Hg, P < 0.0001; heart rate celiprolol -4 beats/min, P < 0.003; metoprolol -12 beats/min, P < 0.0001). There was no difference between the effects of the two treatments on BP but celiprolol had less effect on heart rate than metoprolol, (celiprolol-metoprolol 7.3 beats/min, P = 0.0002). When compared with baseline values celiprolol significantly reduced serum low density lipoprotein cholesterol (LDL-C) (-5.8%, P = 0.0401) and produced a slight increase in high density lipoprotein cholesterol (HDL-C) which approached statistical significance (4.1%, P = 0.0659). Metoprolol significantly increased serum triglycerides (32%, P = 0.0001) and the total/HDL-C ratio (7.4%, P = 0.0192). Compared with metoprolol, celiprolol significantly reduced LDL-C (-7.3%, P = 0.0062), total cholesterol (-4.5%, P = 0.0085), apoliproprotein B (-10.1%, P = 0.0001), the apolipoprotein B/A1 ratio (-10.9%, P = 0.0001), the total cholesterol/HDL-C ratio (-10.8%, P = 0.0001) and triglycerides (-24.8%, P = 0.0001), and significantly increased HDL-C (6.0%, P = 0.0043).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Effect of celiprolol and metoprolol on lipids, fibrinogen and airways function in hyperlipidaemic hypertensives: a randomised double-blind long-term parallel group trial. 775 74

Recently, various clinical studies have indicated that lipophilic beta-blockers reduce the coronary mortality in diabetic patients; however, systematic studies have not been reported. The objective of the present investigation was to compare the effects of chronic treatment with metoprolol and atenolol on cardiovascular complications in streptozotocin (STZ)-induced diabetic rats. Injection of STZ produced hyperglycemia, hypoinsulinemia, hyperlipidemia, increased blood pressure, cardiac hypertrophy, reduction in heart rate, and structural alterations in cardiac tissues. Metoprolol and atenolol effectively prevented the development of hypertension in diabetic rats. Metoprolol treatment produced a slight but significant reduction in serum glucose levels with elevation in serum insulin levels, while atenolol produced a slight increase in glucose levels but no effect on insulin levels. Moreover, neither metoprolol nor atenolol treatment reduced the elevated cholesterol levels in diabetic rats. Metoprolol treatment significantly prevented STZ-induced increase in triglyceride levels, but atenolol failed to produce this effect. Metoprolol exhibited a minimal improvement in STZ-induced bradycardia, whereas atenolol produced a further reduction in heart rate. Histological examination showed metoprolol treatment also prevented STZ-induced hypertrophy and some of the alterations in cardiomyocytes. In conclusion, our data suggest that metoprolol has some beneficial effects over atenolol with respect to cardiovascular complications associated with diabetes mellitus.
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PMID:Comparative evaluation of atenolol and metoprolol on cardiovascular complications associated with streptozotocin-induced diabetic rats. 1790 94

Metoprolol is a widely used cardioselective beta-blocker. However, like all other beta-blockers it is also a racemic mixture of R- and S- isomers. The beta 1 blocking activity (cardioselectivity) of metoprolol resides in S-isomer while R-isomer exhibits beta 2 blocking activity. As both these isomers have different pharmacological properties, racemic metoprolol can be considered a combination of two different drugs in a fixed 1:1 ratio. The needless administration of the non beta-blocking R-enantiomer that makes up 50% of racemate actually puts the patient at an increased risk of side-effects, drug interactions and loss of cardioselectivity with up-titration of dosing. Clinical experience with chirally pure S-metoprolol at half the dose of racemate has shown it to be as effective as racemate in the treatment of patients with hypertension and angina. S-metoprolol has been shown to be effective and well-tolerated in patients with coexisting diabetes, COPD, and hyperlipidaemia. This confirms higher cardioselectivity of S-metoprolol in clinical settings. Less interaction potential of S-metoprolol compared to R-isomer further makes it a sensible choice in patients taking CYP2D6 inhibitors or in patients with heart failure or hepatic insufficiency. This article reviews differing properties of two isomers of metoprolol with focus on clinical experience with S-metoprolol.
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PMID:S-metoprolol: the 2008 clinical review. 1882 49