INTRODUCTIONThe need for the rational development of newer and adjuvant drugs to treat epilepsy has prompted this study of the potential anticonvulsant effect of amlodipine.

METHODSThe acute effect was studied in mice in single doses of 1 mg/kg, 2 mg/kg and 4 mg/kg of amlodipine and the chronic effect was studied in doses of 1 mg/kg and 4 mg/kg (administered daily for 21 days) using the maximal electroshock seizure and pentylenetetrazole-induced seizure models of epilepsy. Sodium valproate and normal saline were used as the standard and control, respectively.

RESULTSFor the acute study, in the maximal electroshock seizure model, the administration of 1 mg/kg of amlodipine resulted in the complete abolition of seizures in 33 percent of the mice, and this was increased to 67 percent with the administration of 4 mg/kg. In the pentylenetetrazole-induced seizure model, the administration of 1 mg/kg and 2 mg/kg amlodipine protected 33 percent of the animals from mortality, and 67 percent were protected with the administration of 4 mg/kg. For the chronic study, in the maximal electroshock seizure model, the administration of 1 mg/kg amlodipine resulted in the complete abolition of seizures in 40 percent of the mice and in 60 percent, with the administration of 4 mg/kg. In the pentylenetetrazole-induced seizure model, 50 percent of the mice were protected from mortality with 1 mg/kg amlodipine and 60 percent, with 4 mg/kg amlodipine.

CONCLUSIONThese findings indicate that amlodipine may be a good candidate as an add-on therapy for epilepsy.

Amlodipine ; therapeutic use ; Animals ; Anticonvulsants ; therapeutic use ; Calcium Channel Blockers ; therapeutic use ; Convulsants ; toxicity ; Disease Models, Animal ; Electroshock ; adverse effects ; Female ; Male ; Mice ; Mice, Inbred Strains ; Pentylenetetrazole ; toxicity ; Seizures ; drug therapy ; etiology ; prevention & control ; Time Factors ; Valproic Acid ; therapeutic use

OBJECTIVETo compare the effects of amlodipine, benidipine and nifedipine on myocardial hypertrophy and evaluate the underlying mechanism.

METHODSMyocardial hypertrophy model was created by transverse aortic constriction (TAC) in C57 BL/6 mice, and plasma catecholamine concentrations were measured 7 days after surgery to confirm the sympathetic activation. The 3 drugs were administered in TAC mice for 7 days and cardiac hypertrophy was evaluated according to the heart-to-body weight ratio (HW/BW). Effects of those drugs on the protein synthesis stimulated by phenylephrine in cultured neonatal cardiac myocytes were also examined.

RESULTSHW/BW and plasma concentrations of catecholamine were significantly increased in TAC mice one week after surgery in comparison with to sham-operated mice. One week after TAC, the HW/BW ratio was significantly lower in the amolodipine but not nifedipine-treated group than in the TAC group. Administration of nifedipine via minipump infusion for one week did not decrease HW/BW ratio. Treatment with amlodpine or benidipine, but not nifedipine, decreased the neonatal rat myocyte protein synthesis induced by phenylephrine stimulation.

CONCLUSIONAntihypertrophic effect of DHEs on myocardium is dependent on their potential of blocking N-type calcium channel, and the underlying mechanism involves the sympathetic inhibition.

Amlodipine ; pharmacology ; therapeutic use ; Animals ; Calcium Channel Blockers ; pharmacology ; therapeutic use ; Calcium Channels, N-Type ; drug effects ; Cardiomegaly ; drug therapy ; etiology ; Dihydropyridines ; pharmacology ; therapeutic use ; Disease Models, Animal ; Male ; Mice ; Mice, Inbred C57BL ; Nifedipine ; pharmacology ; therapeutic use

No abstract available.
Amlodipine/*therapeutic use ; Antihypertensive Agents/*therapeutic use ; Blood Pressure/*drug effects ; Calcium Channel Blockers/*therapeutic use ; Heart Failure/*prevention & control ; Humans ; Hypertension/*drug therapy ; Myocardial Infarction/*prevention & control ; Stroke/*prevention & control

Adult ; Aged ; Amlodipine ; adverse effects ; Drug Overdose ; diagnostic imaging ; drug therapy ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Humans ; Male ; Middle Aged ; Radiography, Thoracic ; Treatment Outcome

This experiment on rats was aimed to investigate the expression of intermedin (IMD) in hypertrophic cardiac myoctye of renal vascular hypertension induced by incomplete ligation of the left renal artery, and so to detect and compare the changes of the expression after administration of Valsartan, Amlodipine and Enalapril respectively. The criterion for standard modeling was systolic pressure > or = 140 mmHg. At 4 weeks after successful modeling, 60 SD male rats were randomly divided into 5 groups, namely the hypertrophy group, the 3 drug-treatment groups, and the sham-operation group as control. Blood pressure, left ventricular mass index (LVMI), and the left ventricular mean transverse diameter of myocardial cell (LVTDM) were investigated at the 10th week after model establishment. Gene expression of IMD mRNA was detected by reverse transcription-polymerase chain reaction (RT-PCR), and the optical density of the band was measured by use of the Gel Documentation System. The ratio of IMD mRNA to beta-actin mRNA was considered the relative amount of IMD. When compared with control, the blood pressure increased significantly in the hypertrophy group. There was no statistically significant difference between the treatment groups. No significant difference in heart rate was noted at 4 weeks after operation in all groups. LVMI and LVTDM levels were significantly higher in the hypertrophy group than in the other groups; LVMI and LVTDM levels showed no significant difference among the treatment groups but they were obviously higher than those of the Sham-operation group. The gene expression of IMD mRNA in the hypertrophy group was upregulated in the myocardium, when compared with that in the other groups. Meanwhile, although IMD mRNA in the treament groups was higher than that in the Sham-operation group, no statistically significant difference of myocardial IMD mRNA was found between the treament groups. These results suggested that, in this experiment, intracardiac IMD mRNA was upregulated and could participate in the regulation of cardiac remodeling in renal vascular hypertension-induced cardiac hypertrophy. This upregulation could improve the pathologic and physiologic process of cardiac hypertrophy, and could associate with the pressure loading or myocardia hypertrophy. However, the change did not display any difference that could be attributed to the variety of hypotensive drugs.
Adrenomedullin ; genetics ; metabolism ; Amlodipine ; therapeutic use ; Animals ; Antihypertensive Agents ; therapeutic use ; Cardiomegaly ; etiology ; metabolism ; Enalapril ; therapeutic use ; Hypertension, Renovascular ; complications ; drug therapy ; metabolism ; Male ; Myocardium ; metabolism ; Neuropeptides ; genetics ; metabolism ; RNA, Messenger ; genetics ; metabolism ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Tetrazoles ; therapeutic use ; Valine ; analogs & derivatives ; therapeutic use ; Valsartan

OBJECTIVETo investigate the effects and safety of Western medicine combined with Chinese medicine (CM) based on syndrome differentiation in the treatment of elderly polarized hypertension (PHPT), or isolated systolic hypertension with low diastolic blood pressure (DBP).

METHODSA total of 125 elderly patients with PHPT were randomly assigned to two groups: 59 in the control group treated by Western medicine and 66 in the intervention group treated by Western medicine combined with CM treatment. Based on syndrome differentiation, the patients in the intervention group were further divided into subgroups of yang-qi deficiency and yin-qi deficiency. All subjects were treated with Western medicine of Amlodipine Besylate Tablets and Irbesartan Tablets (or Irbesartan and Hydrochlorothiazide Tablets), to decrease their systolic blood pressure (SBP) slowly to 125-135 mm Hg in 2-6 weeks. In the intervention group, Shiyiwei Shenqi Capsule was given additionally to the subgroup of yang-qi deficiency at the dosage of 3-5 capsules, thrice a day, while Dengzhan Shengmai Capsule was given additionally to the subgroup of yin-qi deficiency at the dosage of 2 capsules, 2-3 times per day. For all subjects, SBP, pulse pressure (PP), and DBP were measured before treatment and at the terminal of a 6-week treatment. For subjects in the intervention group, left ventricular ejection fraction (LVEF) was also recorded.

RESULTSAfter a 6-week treatment, the SBP in the two groups and the PP in the intervention group decreased significantly compared to those before treatment (P<0.05), while the PP in the control group showed no significant difference between prior and post-treatment (P>0.05). After treatment, the DBP in the control group decreased (P>0.05), while the DBP and LVEF in the intervention group showed an increase tendency although it had no statistical significance (P>0.05). When subjects in the intervention group were classified further by the course of disease, the DBP and LVEF of subjects whose course of disease were less than 2 years, increased significantly after treatment (P<0.05).

CONCLUSIONWestern medicine combined with CM treatment based on syndrome differentiation was safer and more effective than Western medicine alone in the treatment of elderly PHPT, because it not only reduced SBP but also improved DBP, which might lower the incidence of the cardiovascular and cerebrovascular events.

Aged ; Amlodipine ; adverse effects ; pharmacology ; therapeutic use ; Antihypertensive Agents ; adverse effects ; pharmacology ; therapeutic use ; Biphenyl Compounds ; adverse effects ; pharmacology ; therapeutic use ; Blood Pressure ; drug effects ; Diastole ; drug effects ; Drugs, Chinese Herbal ; adverse effects ; pharmacology ; therapeutic use ; Female ; Humans ; Hypertension ; drug therapy ; physiopathology ; Male ; Stroke Volume ; drug effects ; Syndrome ; Tetrazoles ; adverse effects ; pharmacology ; therapeutic use

BACKGROUNDCombination of angiotensin-converting enzyme inhibitors and calcium channel blockers has been successfully used in the antihypertensive therapy for many years. Fixed dose combinations of ramipril/amlodipine have a benefit effect for patients to achieve target blood pressure (BP). This study aimed to assess the efficacy and safety of fixed dose combinations of ramipril and amlodipine (Egiramlon®) in hypertensive diabetic patients.

METHODSHypertensive diabetic patients who were enrolled into the RAMONA trial were included in this open, prospective, Phase IV observational clinical study. Patients had mild-to-moderate hypertension and failed to reach target BP levels through their previous therapy. During the four months of observation, patients took part in three visits (1st day = visit 1, 1st month = visit 2, and 4th month = visit 3) where they received a fixed dose combination of 5/5, 5/10, 10/5, or 10/10 mg ramipril/amlodipine, respectively, with the possibly required dose titrations, based on the decision of their attending physician. Target BP for diabetic patients was <140/85 mmHg. BP levels were measured in all visits, by taking two readings at 2-min interval. Laboratory tests including full blood count, renal function test, electrolytes, blood glucose, serum cholesterol, uric acid, triglycerides, liver function test, creatinine kinase, and midstream urinalysis were performed at visit 1 and visit 3.

RESULTSThe 6423 patients completed the study. Among these patients, 1276 (19.9%) patients suffered from type 2 diabetes mellitus. The mean age of these diabetic patients was 64.2 ± 10.0 years; 707 (55.4%) patients were males. Target BP was achieved by 891 (69.8%) of diabetic patients at visit 3 (primary endpoint). BP decreased from 157.5/91.3 ± 9.6/7.6 mmHg (visit 1) to 130.9/79.6 ± 7.4/5.8 mmHg (visit 3). As for the secondary endpoint of the study, total cholesterol decreased from 5.50 ± 1.13 mmol/L (visit 1) to 5.20 ± 0.95 mmol/L (P = 0.000), low-density lipoprotein cholesterol decreased from 3.20 ± 0.93 mmol/L to 3.00 ± 0.77 mmol/L (P = 0.000), triglyceride decreased from 2.20 ± 1.14 mmol/L to 2.00 ± 1.97 mmol/L (P = 0.000), while high-density lipoprotein cholesterol increased from 1.30 ± 0.42 to 1.35 ± 0.30 mmol/L (P = 0.001) until the end of the 4th month (visit 3). Fasting blood glucose of the hypertensive diabetic patients decreased from 7.20 ± 1.88 mmol/L to 6.70 ± 1.38 mmol/L (P = 0.000), while HbA1c decreased from 7.90 ± 1.78% to 7.60 ± 1.83% (P = 0.000). Various fixed dose combinations of ramipril/amlodipine were well tolerated and no adverse event related to the use of the medicine has appeared.

CONCLUSIONSThe fixed dose combination of ramipril/amlodipine was effective in hypertensive diabetic patients who failed to reach target BP previously.

Aged ; Amlodipine ; administration & dosage ; therapeutic use ; Angiotensin-Converting Enzyme Inhibitors ; administration & dosage ; therapeutic use ; Antihypertensive Agents ; administration & dosage ; therapeutic use ; Blood Pressure ; drug effects ; Diabetes Mellitus, Type 2 ; drug therapy ; Female ; Humans ; Hypertension ; drug therapy ; Male ; Middle Aged ; Ramipril ; administration & dosage ; therapeutic use

OBJECTIVEThis prospective randomized double-blinded clinical trial was designed to explore the effects of amlodipine and the combination of amlodipine with terazosin in improving postvoid residual (PVR) in patients with lower urinary tract symptoms (LUTS) and concomitant hypertension.

METHODSWe randomly divided 360 LUTS patients with concomitant hypertension into a 5 mg amlodipine group, a 2 mg terazosin group and a 5 mg amlodipine plus 2 mg terazosin group, and measured PVR at the baseline and 4 weeks after the treatment.

RESULTSFor male patients with LUTS associate with hypertension, all of amlodipine (APVR = 6.8) , terazosin (APVR = 7. 6), and combination group (APVR = 8.8) can significant reduced the PVR (P < . 0.1), but no significant difference was found among three groups.

CONCLUSIONAmlodipine alone or combined with terazosin can improve the PVR of the LUTS patient effectively, but had no significant difference compared with terazosin.

Adrenergic alpha-Antagonists ; therapeutic use ; Aged ; Amlodipine ; therapeutic use ; Antihypertensive Agents ; therapeutic use ; Double-Blind Method ; Drug Therapy, Combination ; Humans ; Hypertension ; complications ; drug therapy ; Male ; Middle Aged ; Prazosin ; analogs & derivatives ; therapeutic use ; Prospective Studies ; Prostatic Hyperplasia ; complications ; drug therapy ; Treatment Outcome ; Urinary Retention ; complications ; drug therapy ; Urodynamics ; drug effects

OBJECTIVETo evaluate the efficacy of Breviscapine on essential hypertension (EH) patients complicated with micro-albuminuria of renal impairment.

METHODSSeventy-six EH patients were randomly assigned to the control group and the treated group, the former was given amlodipine, captopril/uropidil and the latter was given in addition Breviscapine intravenously dripped for 2 treatment courses. The indexes of serum creatinine (Cr), blood urea nitrogen (BUN), blood and urinary beta(2)-microglobulin (beta(2)-MG), and quantitative determination of 24 hrs urinary protein were evaluated before and after treatment.

RESULTSIn the control group, compared with before treatment, the quantitative determination of 24 hrs urinary protein got reduced significantly (P < 0.05), while in the treated group, both urinary beta(2)-MG and quantitative determination of 24 hrs urinary protein got lowered significantly (P < 0.05 and P < 0.01). But after treatment, compared with the control group, urinary beta(2)-MG and quantitative determination of 24 hrs urinary protein in the treated group were obviously reduced (P < 0.05).

CONCLUSIONBesides lowering blood pressure effectively, Breviscapine could improve the renal function significantly and reduce the urinary micro-albuminuria, hence showing promising effect on renal protection.

Adult ; Aged ; Albuminuria ; etiology ; physiopathology ; Amlodipine ; therapeutic use ; Antihypertensive Agents ; therapeutic use ; Blood Pressure ; drug effects ; Captopril ; therapeutic use ; Drug Therapy, Combination ; Female ; Flavonoids ; administration & dosage ; adverse effects ; therapeutic use ; Flushing ; chemically induced ; Humans ; Hypertension ; complications ; drug therapy ; physiopathology ; Injections, Intravenous ; Kidney Diseases ; etiology ; urine ; Male ; Middle Aged ; Proteinuria ; etiology ; physiopathology ; beta 2-Microglobulin ; urine

BACKGROUNDG-protein β-polypeptide 3 (GNB3) is a β subunit isoform of G-protein that plays important role in signal transduction of membrane G-protein coupled receptors (GPCRs). The GNB3 splice variant C825T (rs5443) is associated with risk for essential hypertension (EH) and efficacy of therapeutic drugs targeting GPCRs. It is unknown whether the polymorphism is associated with blood pressure (BP) response to telmisartan or amlodipine, two widely prescribed antihypertensive drugs.

METHODSA total of 93 subjects initially diagnosed as EH were recruited and underwent a 4-week treatment with telmisartan (42 patients) or amlodipine (51 patients) monotherapy. Both baseline and after-treatment BP were measured. GNB3 C825T polymorphism was genotyped by polymerase chain reaction-restriction fragment length polymorphism.

RESULTSBaseline systolic BP (SBP) and diastolic BP (DBP) were comparable among C825T genotypes in both telmisartan and amlodipine treatment groups. Patients with the CT or TT genotypes showed significantly lower body mass index (BMI) as compared with CC homozygotes in both groups (P < 0.05, respectively). GNB3 825TT homozygotes showed significantly higher after-treatment DBP and mean arterial pressure (MAP) than those carrying at least one 825C allele (P < 0.01) in the telmisartan treatment group. No difference in after-treatment SBP, DBP, and MAP levels among C825T genotypes was observed in the amlodipine treatment group. No significant difference in absolute changes in BP levels was observed among the genotypes in either treatment group.

CONCLUSIONThe GNB3 C825T splice variant is associated with the DBP-lowering effect of telmisartan but not amlodipine in Chinese EH patients.

Adult ; Aged ; Amlodipine ; therapeutic use ; Antihypertensive Agents ; therapeutic use ; Benzimidazoles ; therapeutic use ; Benzoates ; therapeutic use ; Blood Pressure ; drug effects ; Essential Hypertension ; Female ; Genotype ; Heterotrimeric GTP-Binding Proteins ; genetics ; Humans ; Hypertension ; drug therapy ; genetics ; Male ; Middle Aged ; Polymorphism, Genetic ; genetics ; Polymorphism, Restriction Fragment Length ; genetics