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Query: UMLS:C0020538 (hypertension)
 170,190 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Felodipine is a vascular-selective, dihydropyridine calcium antagonist previously investigated as a conventional tablet formulation administered twice daily. More recently considerable experience has been gained with an extended release (ER) formulation which has the convenience of once daily administration. Felodipine ER has been well studied in patients with essential hypertension. As monotherapy in mild to moderate essential hypertension, felodipine ER is at least as effective in reducing blood pressure as other calcium antagonists, beta-blockers, diuretics and ACE inhibitors, with some results favouring felodipine ER at a statistically significant level at the dosages used. It is also effective combined with controlled release metoprolol or enalapril in patients with mild to moderate essential hypertension. In patients with more severe forms of essential hypertension uncontrolled by beta-blocker and/or diuretic therapy, felodipine ER was effective as an 'add-on' therapy in placebo-controlled trials, and, at the dosages used, more effective than either sustained release nifedipine or nitrendipine. Felodipine produces effective control of blood pressure without negative effects on cardiac performance. In addition to its antihypertensive action, results suggest that felodipine therapy is associated with significant regression of left ventricular hypertrophy. Furthermore, it appears suitable for use in patients with concomitant diabetes, renal dysfunction or asthma, and is also being investigated for use in patients with congestive heart failure or angina pectoris. Felodipine ER is an effective drug for the treatment of all grades of essential hypertension, and can be used both as monotherapy and in combination with other antihypertensive agents. Further clinical experience should fully establish the long term tolerability of felodipine ER and consequently its place in therapy relative to other accepted antihypertensive drugs. However, with the convenience of once daily administration, felodipine ER is a worthwhile innovation in the treatment of hypertension.
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PMID:Felodipine. A review of the pharmacology and therapeutic use of the extended release formulation in cardiovascular disorders. 138 18

Felodipine is a dihydropyridine calcium antagonist which may be administered once daily in an extended release (ER) formulation. As monotherapy in older patients with mild to moderate essential hypertension, felodipine ER once daily provides effective control of blood pressure (BP). The drug has also been effective, either as monotherapy or in combination with other antihypertensive medications, in comparisons with other antihypertensive agents, and does not adversely affect lipid profiles or, in patients with diabetes mellitus, glycaemic control. Results in patients with angina pectoris and congestive heart failure indicate a potential role for felodipine ER in these indications and data also suggest the drug reduces left ventricular hypertrophy. In addition, felodipine ER appears suitable for use in patients with concomitant respiratory disease, renal or hepatic dysfunction, cerebrovascular or peripheral ischaemic disease, or gout, making it particularly useful in the elderly who often have more than one significant clinical condition. Felodipine ER has generally been well tolerated by older patients in clinical trials, although further confirmation in the long term is desirable. Thus, felodipine ER effectively lowers BP in older patients with essential hypertension with the added convenience of once daily administration. It may be used as monotherapy or in combination with other antihypertensive agents and is a practical advance in the treatment of hypertension in the elderly.
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PMID:Felodipine. A review of the pharmacology and therapeutic use of the extended release formulation in older patients. 139 20

The antihypertensive effect of felodipine was examined in various hypertensive animal models. In spontaneously hypertensive rats, felodipine administered singly at 0.1-1.0 mg/kg (p.o.) had a dose-dependent antihypertensive effect. Nifedipine was effective at 1 mg/kg. In the repeated oral administration experiment, both the maximum decrease in blood pressure and duration of the effect increased gradually and reached steady levels at 3 weeks of administration, which were maintained thereafter. Similar results were noted with nifedipine, but felodipine was longer-acting (4-6 hr) in the steady state than nifedipine (1-2 hr). No development of tolerance was observed during the administration period. In DOCA-salt and renal hypertensive (2K1C) rats, felodipine at 0.1-0.5 mg/kg (p.o.) was superior to nifedipine in the maximum decrease in blood pressure and duration of the effect. Felodipine up to 1 mg/kg (p.o.) caused no significant heart rate increase in any rat model. In renal hypertensive (2K2C) dogs given felodipine at 0.2-0.5 mg/kg (p.o.), the effect lasted for 2 hr after injection. This felodipine effect was stronger and longer lasting than the nifedipine one. At 0.5 mg/kg of felodipine, the heart rate was transiently increased. The present results show that felodipine has a stronger and long-lasting antihypertensive effect than nifedipine in the hypertension models.
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PMID:[Antihypertensive effect of felodipine, a new calcium antagonist]. 146 3

Felodipine is a dihydropyridine calcium antagonist which lowers total peripheral resistance and blood pressure in doses which have no effect on cardiac conduction and contractility. It increases the urinary excretion of sodium and water due to decreased renal tubular reabsorption from the glomerular ultrafiltrate. This is observed at low doses which do not affect blood pressure, renal blood flow (RBF) or glomerular filtration rate (GFR). Felodipine decreases total renal vascular resistance and causes a transient increase in RBF in patients with normal RBF. In patients with low pretreatment values, RBF is increased during chronic treatment. Felodipine does not affect normal GFR. Thus filtration fraction may decrease. In patients with severe hypertension and reduced GFR, felodipine treatment results in good blood pressure control and increased GFR. In animal models of progressive renal disease due to hyperfiltration, felodipine has no negative effect on GFR, glomerulosclerosis or survival although proteinuria may increase. In salt-sensitive rats given high salt diet, resulting in hypertension, hypoperfused kidneys and progressive renal damage, felodipine treatment results in reduced blood pressure, increased RBF and GFR, and reduced proteinuria and glomerulosclerosis. In patients with previously refractory hypertension and progressive impairment of renal function, felodipine treatment results in good blood pressure control and a reduced rate of progression. In animals, felodipine limits the extent of renal damage after ischemia and reperfusion.
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PMID:Renal effects of felodipine--a review. 161 69

Felodipine, a dihydropyridine calcium antagonist, was used to treat eight patients with severe uncontrolled hypertension: five had essential hypertension, two had renovascular disease, and one chronic pyelonephritis. Mean blood pressure (BP) was 221 +/- 14/120 +/- 4 mm Hg despite treatment with three or more antihypertensive drugs. All patients experienced an immediate and pronounced lowering of BP after adding felodipine, which persisted during long-term treatment in combination with previous medication except for vasodilating drugs. In all cases, an increase in glomerular filtration rate (51Cr-EDTA clearance) after 6 and 12 months of felodipine treatment was seen (59 +/- 10 to 63 +/- 7 and 70 +/- 6 ml/min, respectively, p less than 0.05). Renal plasma flow (PAH clearance) exhibited only a slight increase (315 +/- 68 to 340 +/- 63 and 314 +/- 69 ml/min), giving a nonsignificant rise in filtration fraction (18 +/- 1 to 21 +/- 1 and 20 +/- 1%, respectively). It is concluded that felodipine decreases BP dramatically in patients with previously refractory hypertension and that the drug causes an improved renal function in these patients.
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PMID:Long-term effects of felodipine on blood pressure and renal hemodynamics in severe hypertension. 169 10

Felodipine is a new calcium antagonist with vascular selectivity. It has a high potency in arterial resistance vessels and no apparent action on capacitance vessels. It lacks significant effects on myocardial contractility and cardiac conduction. It is an effective antihypertensive agent and may be safely combined with beta-adrenoceptor blockade. This report outlines work confirming the vascular selectivity of felodipine by examining its clinical effects in hypertension, ischemic heart disease, and congestive heart failure.
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PMID:Vascular selectivity of felodipine: clinical experience. 169 18

Felodipine is a dihydropyridine that blocks the slow entry channel for calcium. It is highly vascular selective and reduces blood pressure (BP) by dilatation of peripheral arterioles. It reduces BP in mild, moderate, and severe hypertension, and the fall in BP depends upon the initial level. It has been compared with a variety of other drugs as monotherapy or as add-on therapy. In these studies, felodipine (10-40 mg/day) has caused a similar or greater fall in BP and a similar or greater percentage of patients have achieved a diastolic BP less than or equal to 90 mm Hg. The plain tablet of felodipine needs to be given twice a day but an extended-release form can be given once daily. Some patients respond to 5 mg/day and most patients respond to a daily dose of 20 mg or less. The adverse effects are few except for a constellation of symptoms related to the vasodilator ability of the drug. These include palpitations, flushing, fatigue, dizziness, and headaches. These occur, if at all, usually within the first 2 weeks and diminish as the drug is continued. They can be limited by starting on a small dose of felodipine (5 mg/day). People who have these adverse effects usually have a good response to the drug. Another adverse effect, which is the most frequent reason for drug withdrawal, is ankle edema. This is more common on the higher doses of the drug. It is due to dilatation of the precapillary resistance vessels rather than sodium and water retention. Felodipine is a useful and effective antihypertensive drug and can be used as monotherapy or added to other antihypertensive drugs. It is effective in people with all grades of hypertension.
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PMID:A review of the antihypertensive effects of felodipine alone or in combination. 169 35

A double-blind, parallel-group study was performed to assess the antihypertensive effects and tolerability of felodipine and hydrochlorothiazide (HCT) in black patients with mild to moderate uncomplicated hypertension [entry supine diastolic blood pressure (DBP) of 96-116 mm Hg]. The medicines were given as monotherapy and the additional effect of metoprolol was assessed in patients unresponsive to felodipine or HCT alone. After a 4-week placebo period, 45 patients were randomly allocated to treatment with felodipine (21) or HCT (24). Initial doses of felodipine 2.5 mg or HCT 12.5 mg twice daily were doubled after 1 week and doubled again after week 4 in cases with supine DBP above 90 mm Hg. At week 8, metoprolol 100 mg twice daily was added to the regimen of uncontrolled patients (supine DBP greater than 90 mm Hg) and maintained for the remaining 4-week trial period. Felodipine significantly reduced supine and erect systolic BP (SBP) and DBP after 4, 8, and 12 weeks of treatment. Responses to HCT were similar although standing diastolic BP at week 4 and standing SBP at week 8 were not significantly reduced. After 4 weeks, the mean fall in supine DBP was significantly greater for the felodipine than the HCT group. Eight patients on felodipine and 14 in the HCT group required additional metoprolol to achieve BP control. A significantly greater number of adverse effects were associated with HCT than felodipine treatment. Monotherapy with felodipine produced a more rapid control of hypertension, was more frequently effective, and was associated with a lower incidence of side effects than HCT.
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PMID:Comparison of felodipine and hydrochlorothiazide for the treatment of mild to moderate hypertension in black Africans. 169 38

Felodipine, a dihydropyridine calcium-channel antagonist, significantly reduces systolic and diastolic blood pressure (BP) in patients with hypertension and has been associated with beneficial hemodynamic effects in patients with chronic stable angina pectoris or congestive heart failure (CHF). In hypertensive patients, felodipine does not appear to significantly affect glomerular filtration rate, creatinine clearance, glucose tolerance, or plasma lipoprotein concentrations. Studies comparing felodipine with other agents as monotherapy in mild to moderate hypertension have demonstrated felodipine to be at least as efficacious as hydrochlorothiazide (HCTZ) and HCTZ plus amiloride hydrochloride in combination. Comparisons of felodipine with other agents as adjuncts to beta-blocker or diuretic therapy have shown felodipine to be at least as effective as HCTZ, propranolol hydrochloride, prazosin hydrochloride, and nifedipine. Evaluations of patients with chronic stable angina are limited, and additional studies are needed before felodipine can be recommended for the routine management of angina pectoris. Similarly, additional studies are essential to delineate the role of felodipine, if any, in the management of CHF. In the management of hypertension, felodipine 5-40 mg/d significantly reduces systolic and diastolic BP. Although some patients may be controlled throughout the entire dosing interval when felodipine is administered bid, many patients will require more frequent dosing to obtain adequate BP control. Adverse effects associated with felodipine are similar to those of other dihydropyridine calcium-channel antagonists and include peripheral edema, headache, dizziness, flushing, and fatigue. A potentially clinically important drug interaction was observed when felodipine was administered concomitantly with theophylline aminopropanol; significant decreases in theophylline concentrations were noted. In summary, felodipine appears to be safe and effective for the management of hypertension when used alone or in combination with other antihypertensive agents. The efficacy of felodipine in the management of chronic stable angina pectoris and CHF requires further investigation.
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PMID:Felodipine: a new dihydropyridine calcium-channel antagonist. 176 37

It is not yet known how blood pressure variability contributes to the vascular changes associated with hypertension, but 2 possibly relevant factors are mean blood pressure levels over time and pressure peaks. It has been observed that patients in whom the variability in 24-hour blood pressure is low have a lower prevalence and severity of target organ damage. We carried out a whole-day continuous intraarterial blood pressure recording (Oxford method) in 12 essential hypertensive patients after a 2-week placebo period and after a 4-week felodipine treatment, administered in an extended release formulation, 10 mg once daily at 7 am. Felodipine significantly lowered systolic and diastolic blood pressure values throughout the 24 hours (p less than 0.005 to 0.001). Also, hourly variabilities of systolic and diastolic blood pressure during whole-day monitoring were significantly reduced (p less than 0.05 to 0.001), evaluated on the basis of the hourly means of standard deviation of systolic and diastolic blood pressure. In addition, felodipine significantly lowered the values of blood pressure reached during both dynamic exercise (bicycle ergometer, p less than 0.001) and isometric exercise (handgrip, p less than 0.001).
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PMID:[Circadian pressure variability and pressure peaks during treatment of mild to moderate essential hypertension with felodipine]. 207 38


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