Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0020538 (hypertension)
 170,190 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The HOT study (hypertension-optimal treatment) is an international clinical study on primary prevention of cardiovascular events in 19,193 hypertensive patients worldwide. It aims at the recognition of the optimal diastolic blood pressure value (< 90, < 85 or < 80 mmHg?) in order to maximize the possible benefit of an antihypertensive therapy. In addition, the HOT study investigates whether low doses of aspirin (75 mg/day) are able to reduce the occurrence of severe cardiovascular events. In Switzerland a total of 797 patients have been enrolled in the study. Antihypertensive therapy was initiated with felodipine = Plendil (5 mg/day). This vasoelective calcium antagonist could reduce diastolic blood pressure values to < 90 or < 80 mg/Hg, respectively, in one of two or one of three patients within the first three months. In nine or six patients, respectively out of ten a reduction of diastolic blood pressure values to < 90 or < 80 mmHg was reached within one year by combination of felodipine with other antihypertensive drugs (ACE inhibitors, beta blockers and diuretics).
 ...
PMID:[Initial results of the HOT-study in Switzerland (hypertension optimal treatment)]. 853 5

The effects on blood pressure (BP) and heart rate (HR), at rest and during bicycle exercise, of the vascular selective calcium antagonist felodipine, the cardio-selective beta-blocker metoprolol, and of the two drugs in combination, were assessed in a double-blind, three-way cross-over study comprising 23 patients with essential, mild to moderate hypertension. All three treatment regimens were given to each patient in randomised order for 4 weeks after a 4 week placebo run-in period. Felodipine 10-20 mg daily, metoprolol 100-200 mg daily and the combination of felodipine 10-20 mg plus metoprolol 100 mg daily were all effective antihypertensive treatments both at rest and during exercise. The two drugs seemed to have additive effects and the effect on BP of the combination was greater than that of either drug given as monotherapy. The mean sitting BP was 148/103 mmHg at randomisation, after 4 weeks of placebo treatment, and 134/88, 134/94 and 121/84 mmHg, respectively, after 4 weeks' treatment with felodipine, metoprolol and the combination. Maximal exercise capacity was similar irrespective of treatment regimen, and the normal response to exercise BP and HR was maintained during all active treatments. Changes observed in volume regulatory hormones (PRA, aldosterone and ANP) were consistent with a direct tubular natriuretic-diuretic effect of felodipine and of beta-blocker attenuated release of renin. All treatment regimens were well tolerated and adverse events reported were usually mild and transient.
 ...
PMID:Effects of felodipine, metoprolol and their combination on blood pressure at rest and during exercise and on volume regulatory hormones in hypertensive patients. 853 52

Calcium entry through L-type calcium channels is essential for contraction of both arterial smooth muscle and the myocardium, and is important in cardiac conduction. First-generation calcium entry blockers lack or have a modest degree of vascular selectivity and inhibit cardiac function at doses producing therapeutic arterial dilatation. Such agents may cause deterioration in patients with left ventricular dysfunction, and their combination with a beta-adrenergic blocker may adversely affect cardiac contractility and conduction. Development of newer agents has focused on obtaining a higher degree of vascular selectivity. Felodipine is a highly vascular selective calcium entry blocker, with a vascular selectivity ratio greater than 100, as shown experimentally. Isradipine and nicardipine are also vascularly selective calcium entry blockers. Hemodynamic studies in patients with hypertension, coronary artery disease, congestive heart failure, or in patients receiving beta-adrenergic blockade, show that felodipine can produce profound arteriolar dilatation without the negative effects of left ventricular systolic performance. Furthermore, felodipine alone or when added to a beta-adrenergic blocker does not interfere with cardiac conduction. The primary mechanism that accounts for the efficacy of dihydropyridine calcium entry blockers in hypertension and angina pectoris is arterial dilation, whereas nondihydropyridines may also derive part of their effect from inhibition of cardiac performance. As some of these patients, most commonly the elderly, have concomitant left ventricular dysfunction, it should be advantageous to avoid myocardial depression in the treatment of their primary disease. Preliminary studies in patients with heart failure indicate that felodipine and amlopidine may improve hemodynamics, reduce neurohormonal activation, and increase exercise tolerance, but final conclusions must await the randomized clinical trials now underway.
 ...
PMID:Vascular selective calcium entry blockers in the treatment of cardiovascular disorders: focus on felodipine. 857 48

The aim of the present study was to examine the effects of felodipine, a dihydropyridinic calcium ions channels blocker, on mean arterial blood pressure (MAP), cardiac output (CO), peripheral resistances (TPR) and blood flow distribution in spontaneously mildly hypertensive female Wistar 30-34 months old rats. Under pentobarbital anesthesia, CO and regional organ blood flow were measured by the radioactive microspheres method, before and 30 min after administration of felodipine 0.5 mumol/kg b. w. by gastric gavage. They were compared to the corresponding values in normotensive rats of the same strain and age. Fifteen (from twenty five) rats were hypertensive with a MAP averaging 139 +/- 2 mm Hg. CO and TPR were slightly higher in these hypertensive rats. Cerebral blood flow (CBF) was lower, though the difference did not reach significant values. MAP significantly decreased after felodipine with no significant changes in CO and TPR in hypertensive as well as in normotensive animals. Renal blood flow (RBF) was similar before and after felodipine which significantly decreased renal vascular resistance in both groups. Felodipine administration did not induce significant changes in CBF but a significant increase in portal venous inflow (PVI) in hypertensive rats only. In conclusion, in old female rats with mild spontaneously hypertension, acute felodipine oral administration reduced arterial blood pressure without diminishing CBF.
 ...
PMID:Effect of felodipine on systemic hemodynamics of spontaneous mild-hypertensive aged rats. 857 83

We studied the therapeutic substitution of a less expensive but equally effective antihypertensive agent and assessed patient outcome. The medication of 39 patients with hypertension was changed from once-daily diltiazem hydrochloride (Cardizem CD) or nifedipine (Procardia XL) to felodipine (Plendil). Titration to a final dose was based on home and office blood pressure measurements assessed over subsequent follow-up clinic visits. Self-administered questionnaires measured different aspects of well-being and symptoms before and after the change in medication. Eighty percent of the cohort switched successfully to felodipine. Office systolic and diastolic pressures improved after the medication change (systolic: 150 mm Hg versus 144 mm Hg; diastolic: 92 mm Hg versus 87 mm Hg). No statistically significant differences were found among the 39 symptoms measured. A yearly savings potential for our institution was estimated to be $72,000.
 ...
PMID:Felodipine as an alternative to more expensive calcium antagonists in mild to moderate hypertension. 863 95

We assessed the 24-h antihypertensive efficacy of an extended-release (ER) 10-mg formulation of the dihydropyridine felodipine in mild-to-moderate essential hypertension [World Health Organization (WHO) stage I-II]. Thirty patients, 23 men and 7 women, aged 37-70 years (mean 53 +/- 9 years) participated in a double-blind, randomized, cross-over study of felodipine 10 mg ER versus placebo. An ambulatory daytime diastolic blood pressure (DBP) >90 mm Hg at the end of a 4-week run-in period was necessary to enter the 10-week treatment phase. Twenty-nine patients completed the treatment phase. Twenty-two underwent a 2-day single-blind placebo follow-up to assess residual drug effects. All patients underwent ambulatory BP monitoring (ABPM) by Spacelabs 90207 recorders. Recorders were programmed to make automatic BP and heart rate (HR) measurements every 15 min throughout the 24 h. Felodipine 10 mg ER significantly (p < 0.01) reduced ambulatory systolic BP (SBP) and DBP values throughout the 24-h, day (7 a.m. to 11 p.m.) and night (11 p.m. to 7 a.m.) periods, but not influencing average ambulatory HR values. Trough-to-peak (T/P) ratios, calculated on the average ambulatory BP values measured in the 7-9 a.m. 2-h interval of the second day of ABPM (before the new drug administration: trough) and in the 10 a.m. to 12 noon 2-h interval of the first day of ABPM (peak BP-lowering effect), were 0.71 and 0.58 for SBP and DBP, respectively. Individual T/P calculations, after post hoc selection of nonresponders, gave superimposable results, the consistency of which was judged on mean, median, and confidence intervals (CI). However, the wide variability of the individual T/P ratios suggests that this method cannot be the only means to evaluate the duration of action of an antihypertensive drug by ABPM. The long-acting BP-lowering drug effect was clearly shown by the ABPM performed in the follow-up when SBP and DBP average values of the 24-h, day, and night periods were still reduced. Felodipine 10 mg ER effectively reduced BP in patients with mild-to-moderate hypertension, showing prolonged duration of its antihypertensive action beyond the time of the next dose.
 ...
PMID:Twenty-four-hour antihypertensive efficacy of felodipine 10 mg extended-release: the Italian inter-university study. 872 Apr 25

The efficacy and tolerability of felodipine, in a low dose of 5-10 mg daily was assessed in 32 patients with mild-to-moderate hypertension, aged 53 +/- 11 years. The results of office vs 24 h ambulatory blood pressure measurements (ABPM) were compared. Inclusion criteria included an office systolic and diastolic blood pressure (SBP/DBP) > 140/90 mm Hg and a 24 h ABPM SBP/DBP > 135/85 mm Hg. Felodipine was initiated at a dose of 5 mg daily. At day 28 of the study, if office DBP > 90 mm Hg, the dose was doubled to 10 mg daily. At the end of the study (day 84), 24 h ABPM was done again. Side effects were noted throughout the study. Four patients dropped out during the study (two due to headache, one due to pedal edema and one rejected further participation). Of the remaining 28 patients, at day 28, 12 required an increased dose of 10 mg/day. At the end of the study, office BP was below 140 90 mm Hg in 71% of the patients. In the whole group BP decreased from 158 +/- 15/101 +/- 8.4 to 138 +/- 9/85 +/- 5 mm Hg, P < 0.001. ABPM showed that BP was normalized in 82% of the patients. It decreased from 146.8 +/- 9.56/94.8 +/- 7.4 to 130.2 +/- 10.6/83 +/- 6.3 mm Hg, P < 0.001. BP was similarly reduced in working and sleeping hours, with preservation of the circadian rhythm. Heart rate was unaffected by the drug. Five patients showed persistently elevated SBP on office measurements while on ABPM, the values were within normal limits. This finding confirms the existence of a white coat effect in patients with proven hypertension and the superiority of ABPM over office BP measurements in clinical investigations. In summary, ABPM showed that the antihypertensive effect of felodipine was sustained throughout normal 24 h, including the critical (as regards cardiovascular morbidity) awakening hours.
 ...
PMID:Efficacy of low felodipine dose monotherapy in mild-to-moderate hypertension: a comparison between office and ambulatory blood pressure monitoring. 887 49

A total of 411 patients were recruited in the Israeli cohort of the Hypertension Optimal Treatment (HOT) Study, a multinational study conducted to assess the effect on cardiovascular morbidity and mortality in hypertensive patients of three levels of target diastolic blood pressure: < 90, < 85, and < 80 mm Hg. Initial treatment with felodipine in all patients was supplemented with other drugs as needed. When compared to the subjects in the rest of the world, the percentage of Israeli patients getting previous antihypertensive treatment was higher, reflecting a higher proportion of hospital-recruited patients. This accounted for the lower percentage of Israeli patients ending up with low-dose felodipine: 50% vs 56% in other countries. The percentage of patients getting high-dose felodipine plus additional drugs was also higher: 3.8% vs 2.9% for other countries. Felodipine was remarkably well tolerated, and most of the patients were able to continue this drug regimen.
 ...
PMID:Hypertension optimal treatment: the Israeli HOT Study Group. Hypertension Optimal Treatment. 887 51

1. Four groups of New Zealand genetically hypertensive (GH) rats were treated with felodipine as follows: (A) from ages 4-12 weeks; (B) 4-20 weeks; (C) 4-12 weeks then withdrawn from felodipine till age 20 weeks; and (D) 12-20 weeks. 2. Effects on blood pressure (BP), left ventricular (LV) weight and the structure of myograph-mounted mesenteric resistance arteries (MRA) were measured. 3. BP was about 170 mmHg in 4 week old GH rats and did not change substantially from this value in groups A and B but rose to over 230 mmHg in untreated controls. In rats of group D, started on felodipine at 12 weeks, BP fell rapidly and was 173 mmHg at 20 weeks. On withdrawal of felodipine at 12 weeks (group C) BP rose rapidly and exceeded control levels at 20 weeks. 4. LV mass was significantly lower (P < 0.001) in all groups (A, B and D) killed while on felodipine but rose to control levels in the rats taken off felodipine. 5. In the four treated groups there were no significant changes in MRA structure (lumen diameter, medial thickness, media/lumen ratio and volume of medial tissue) as measured on the myograph. 6. Felodipine induces substantial falls in BP in GH rats which are sufficient to prevent cardiac hypertrophy but do not alter MRA structure. Resistance artery structure in GH rats does not seem to relate to the level of hypertension, and may therefore not have a necessary role in the pathogenesis of this hypertensive strain.
 ...
PMID:Effect of felodipine treatment and withdrawal on blood pressure and cardiovascular structure in New Zealand genetically hypertensive rats. 907 13

Felodipine is a second-generation dihydropyridine calcium antagonist used to treat mild to moderate arterial hypertension. The authors used venous occlusion plethysmography to study the effect of this drug on lower limb arterial inflow and venous outflow in 10 at rest patients with mild essential hypertension. They also sought correlations between changes in district blood flow and blood pressure. Plethysmography was carried out at 8 AM and 4, 8, and 24 hours later at baseline (after washout), on the first day of treatment with a single daily administration of 10 mg felodipine ER, and after 7 and 30 days of treatment. The drug was given after the 8 AM evaluation. The authors determined rest flow, maximal venous incremental volume (MVIV) at 40 mmHg and 60 mmHg, and gradient of venous volume between 60 and 40 mmHg divided by the pressure difference (DV/DP) as index of venous distensibility. On the days of plethysmographic evaluation, arterial blood pressure and heart rate were measured continuously over 24 hours by the ABPM (Ambulatory Blood Pressure Monitoring). The results were analyzed by ANOVA. Rest flow, MVIV, and DV/DP were stable at the baseline evaluation. On days 1, 7, and 30 of treatment the rest flow after 4 and 8 hours was significantly greater than at 8 AM but had always returned to normal after 24 hours. No other plethysmographic parameters changed significantly; in particular venous outflow remained unchanged. Mean arterial, systolic, and diastolic blood pressure were significantly reduced, compared with baseline, following treatment on the first day and after 7 and 30 days' treatment. There was no effect on heart rate. The authors conclude that felodipine is useful for the treatment of mild essential hypertension, since it reduces arterial resistance without altering venous capacitance or distensibility.
 ...
PMID:Effect of felodipine on arterial blood flow and venous function at rest in patients with mild essential hypertension. 959 29


<< Previous 1 2 3 4 5 6 7 8 Next >>