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Hypertension is a prevalent systemic disease in the elderly, who can suffer from several pathological skeletal conditions simultaneously, including osteoporosis. Benidipine (BD), which is widely used to treat hypertension, has been proved to have a beneficial effect on bone metabolism. In order to confirm the osteogenic effects of BD, we investigated its osteogenic function using mouse MC3T3-E1 preosteoblast cells in vitro. The proliferative ability of MC3T3-E1 cells was significantly associated with the concentration of BD, as measured by methylthiazolyldiphenyl-tetrazolium bromide (MTT) assay and cell cycle assay. With BD treatment, the osteogenic differentiation and maturation of MC3T3-E1 cells were increased, as established by the alkaline phosphatase (ALP) activity test, matrix mineralized nodules formation, osteogenic genetic test, and protein expression analyses. Moreover, our data showed that the BMP2/Smad pathway could be the partial mechanism for the promotion of osteogenesis by BD, while BD might suppress the possible function of osteoclasts through the OPG/RANKL/RANK (receptor activator of nuclear factor-κB (NF-κB)) pathway. The hypothesis that BD bears a considerable potential in further research on its dual therapeutic effect on hypertensive patients with poor skeletal conditions was proved within the limitations of the present study.
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Objective :To explore influence of benidipine on blood pressure ,left ventricular hypertrophy (LVH) ,u—rine microalbuminuria／creatinine ratio (UACR ) and brachial—ankle pulse wave velocity (baPWV ) in patients with morning hypertension (MH).Methods : A total of 142 patients with essential hypertension treated in our department were randomly and equally divided into benidipine group and amlodipine group .The 24h ambulatory blood pressure (24hABP) before and two months after treatment ,ultrasonography ,urine microalbumin (UMA ) and creatinine (Ucr) and baPWV before and six months after treatment were measured in two groups ,and UACR was calculated . Results : Compared with before treatment , there were significant reduction in blood pressure in two groups after treatment ( P＝0.001 all) ,but there were no significant difference in blood pressure between two groups after treat—ment , P＞0. 05 all .Compared with amlodipine group after treatment ,there were significant rise in total effective rates of MH (56.06% vs .74.24%) and daytime blood pressure (62.12% vs.78.79%) in benidipine group , P＜0.05 both .Compared with before treatment , after treatment , there was significant reduction in UACR in two groups ( P＝0. 001 both) ,but there were no significant difference in UCG indexes and baPWV , P＞0.05 all.Com—pared with amlodipine group after treatment ,there was significant reduction in UACR [ (18.25 ± 1.53) μg／mg vs. (16.54 ± 1.42) μg／mg , P＝0.001] in benidipine group ,there were no significant difference in UCG indexes and baPWV between two groups ,P＞0.05 all.Conclusion : Both amlodipine and benidipine can effectively control blood pressure ;and benidipine possesses more significant therapeutic effect on total effective rates and UACR .
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Objective To investigate the antagonism of third generation dihydropyridine calcium channel antagonist beni-dipine in contraction induced by potassium chloride(KCl)in human internal mammary artery(IMA),and in order to explore the possibility of using benidipine as an antispastic agent during coronary artery bypass grafting(CABG). Methods The IMAs were taken from 19 patients undergoing CABG. The vasodilator effect(n = 7)on KCl-induced contraction and the inhibition effect(n = 6)after incubation with benidipine were studied in a myograph. The caveolin 1. 2 was detected(n = 3,2 cases re-spectively)by enzyme-linked immunosorbent assay (ELISA). Results The maximum relaxation caused benidipine was (87. 7 ± 4. 9)％ . Incubation with benidipine significantly depressed the contraction by KCl[from( 16. 9 ± 4. 4)mN to (9. 1 ± 3. 4 )mN,P < 0. 01]. The concentration of caveolin 1. 2 was down-regulated after incubation with benidipine(P < 0. 05). Conclusion Benidipine has a potent inhibitory effect on KCl-induced vasoconstriction. The relaxation may be related with the expression of caveolin 1. 2. Using benidipine in patients undergoing CABG may provide antispastic effects in grafts.
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Objective To investigate the curative effect of benidipine hydrochloride on patients with coronary slow flow angina pectoris(CSFA).Methods Sixty cases patients with CSFA were randomly divided into two groups of 30 patients each.In the control group patients were received aspirin(100 mg,1 times/d) and atorvastatin(20 mg,1 times/d) as basic treatment;in the treatment group patients were received basic treatment plus benidipine hydrochloride(4 mg,1 times/d).Follow up for 6 mouths,the effectiveness rate of treatment(relief of angina and electrocardiogram of myocardial ischemia),the correction of thrombolysis in myocardial infarction(TIMI) frame count(CTFC) before and after the different intervention,and the incidence of adverse cardiovascular events were compared between the treatment group and the control group.Results The effectiveness rate of treatment in the treatment group(86.7%,26/30) was significantly higher than that in the control group(63.3%(19/30);χ2=4.356,P=0.037).There were significant reductions of CTFC in both groups after the different intervention(treatment group:(28.43±3.95) frames vs.(18.40±3.73) frames,t=10.254,P=0.000;control group:(27.87±4.14) frames vs.(21.87±4.17) frames,t=5.580,P=0.000).There was more significant reductions of CTFC in the treatment group as compared to the control group(t=2.138,P=0.037).The incidence of adverse cardiovascular events in the treatment group(10.0%(3/30)) was significantly lower than that in the control group(33.3%(10/30),P=0.028).Conclusion Benidipine hydrochloride is effective in the treatment of CSFA.
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METHODS: With random and double-blinded method in multicenters, 201 eligible patients aged from 18 to 75 years with mild to moderate hypertension were devided into two groups after received placebo for 2 weeks, 99 patients in experimental group received benidipine 2 mg once a day, 102 patients in control group were given lacidipine 4 mg, once a day for 4 weeks. The dose is adjusted after 4 weeks in the patients not reaching the blood pressure target of DBP or SBP. The whole treatment was continued for 8 weeks, patients must finish one visit every 2 weeks for observing efficacy and adverse events.
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OBJECTIVE:To establish a method for the dissolution determination of Benidipine hydrochloride tablets.METHODS:According to Chinese Pharmacopeia(2005 edition),Benidipine hydrochloride tablets were added into hydrochloride acid 0.1 mo?lL-1 at rotation speed of 50 r?min-1,then samples were obtained after 30 min.The absorbance of samples was detected at detection wavelength of 359 nm and accumulative dissolution was calculated.RESULTS:The linear range of benidipine hydrochloride was 5～30?g?mL-1(r=0.999 9)with an average recovery of 99.76%(RSD=0.47%).The accumulative dissolutions of 3 batches of samples were all above 80%.CONCLUSIONS:Established method is simple and reliable for the dissolution determina-tion of Benidipine hydrochloride tablets.
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Objective The effect of combined treatment of statins and calcium channel blockers(CCB) in elderly patients with isolated systolic hypertension(ISH) are not well understood.The purpose of the present study was to assess the additive effect of benidipine-atorvastatin combination therapy in old patients with ISH.Methods Ninety patients with ISH were randomized to receive: placebo(n=15),benidipine treatment(4-8 mg/d,n=25),atorvastatin(20 mg/d,n=25) and benidipine plus atorvastatin treatment(4-8 mg/d+20 mg/d,n=25) for 5 months.Serum concentrations of IL-6,IL-8,hsCRP,flow-mediated dilatation of the brachial artery,urine microalbumin,left ventricular mass index(LVMI),carotid intima-media thickness(CIMT),BP and plasma lipids profiles were examined before and after treatment.Results After 5-months of treatment,the combination treatment significantly reduced IL-6(IL-6 reduction magnitude,combination group: 6.5+6.3 ng/L vs benidipine group: 3.1?3.2 ng/L vs atorvastatin group: 3.3?2.3 ng/L,P
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Objective To search for the effect of benidipine,a kind of Ca2+ blocker,on NO and ET-1 of patients with coronary heart disease.Methods Benidipine(2~4 mg/d)were given to the patients with coronary heart disease diagnosed definitely for 8 weeks.Forty healthy candidates were enrolled in the control group,and their morning fasting blood were tested for NO and ET-1 levels at the 4th,8th week in order to compare with the control group.Results Blood NO level of CHD patients was lower and blood ET-1 level was higher than the control group remarkably.After treatment NO level was increased and ET-1 level was decreased separately.Conclusion Benidipine can increase NO level and decrease ET-1 level,which demonstrated the protective effect of benidipine for endothelia.
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BACKGROUND AND OBJECTIVES: This study was designed to evaluate the appropriate dose and dose-dependent effect of benidipine hydrochloride, a Ca+ +/- channel blocker, in patients with mild-moderate essential hypertension. Material and MethodsBenidipine was administered in 2 mg, 4 mg and 8 mg once daily with 1 month interval in 41 hypertensive patients with diastolic blood pressure over 90 mmHg and systolic blood pressure from 140 to 210 mmHg. Blood pressure, heart rate, subjective symptoms and adverse effects were checked every 4 weeks after benidipine administration. Laboratory examinations were performed before and after benidipine administration. RESULTS: The dose-dependent, antihypertensive effect of benidipine was evaluated in 41 patients. The blood pressure significantly reduced from 166+/-15 mmHg/103+/-7 mmHg to 13815 mmHg/88+/-11 mmHg at 12 weeks administration of benidipine and overall effective rate was 95%. The systolic and diastolic blood pressure was reduced significantly in proportion to dose of benidipine (p<0.0001). Antihypertensive effect was prominent at 4mg of benidipine. The heart rate was not affected by benidipine. No significant laboratory changes were observed. CONCLUSION: Benidipine has a dose-dependent effect in the treatment of mild-moderate hypertension, and the dosage to be needed may be 4mg or more for sufficient antihypertensive effect.
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Humans , Blood Pressure , Heart Rate , HypertensionABSTRACT
BACKGROUND: This study was designed to evaluate the antihypertensive efficacy and safety of benidipine hydrochloride, a Ca(++)-channel blocker, in patients with mild to moderate essential hypertension. METHODS: Benidipine was administered in 2-8mg once daily for 10 weeks in 16 hypertensive patients with diastolic blood pressure over 95mmHg and adverse effects were checked every two weeks after benidipine administration. Chest X-ray, ECG, funduscopy, and laboratory examination were performed before and after benidipine administration. RESULTS: The antihypertensive effect of benidipine was evaluated in 15 patients and the safety in 16 patients. The blood pressure significantly reduced from 170+/-12mmHg/102+/-5mmHg to 137+/-15mmHg/86+/-8mmHg at 10-week administration of benidipine and the overall effective rate was 100%. Heart rate was not affected by benidipine. The slight increase of total protein, BUN, potassium, and glucose was observed at 10 weeks of benidipine administration. Four cases of headache and 1 case of frequent urination were observed and the medication was discontinued in one patient due to headache. CONCLUSION: Benidipine proved effective and safe in the treatment of essential hypertension.