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

The antihypertensive activity of spirapril given alone or in combination with felodipine was investigated in spontaneously hypertensive rats (SHR) during a 3-week treatment regimen and for one week after drug withdrawal. Systolic blood pressure and heart rate were recorded once a week just before dosing and at varying time intervals up to 6 hr thereafter. Recordings were continued for one week after drug withdrawal. Spirapril alone at 1 and 5 mg/kg p.o. was found to produce dose-related antihypertensive effects throughout the treatment period. Felodipine alone at 5 mg/kg p.o. reduced blood pressure slightly more than did the low dose of spirapril. The combination of spirapril and felodipine induced a marked antihypertensive response which was greater than that observed in rats treated with either drug alone. One week after treatment withdrawal, blood pressure was at initial levels with no evidence of rebound phenomena. No significant heart rate changes were observed in the treated groups, as compared with the controls, except for an increase on the 1st day of treatment in rats given felodipine. These findings indicate that the combination of an angiotensin converting enzyme (ACE) inhibitor with a calcium antagonist leads to an effective control of hypertension over a prolonged period of treatment. Since the combination allows effectiveness with lower doses of ACE inhibitor, it is expected that the antihypertensive efficacy might be associated with a lower liability to untoward effects.
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PMID:Antihypertensive effect of spirapril and felodipine during repeated administration to spontaneously hypertensive rats. 283 72

The effects of small doses of felodipine (10 mg twice daily) on blood pressure, renal function and sodium and water balance were studied in 11 patients with arterial hypertension. Felodipine significantly reduced systolic and diastolic blood pressure: most of the antihypertensive effect was already evident on day 1 of administration (-18/-11 mmHg) and only slightly increased during the subsequent week. Heart rate rose moderately only during day 1 of felodipine administration (+7 beats/min). Sodium excretion was increased during days 1 and 2, and no signs of water and electrolyte retention was observed in the week during which the balance study could be performed (Na, -135 +/- 65 mmol/7 days). At relatively low doses felodipine appears to be an effective antihypertensive agent, initially exerting some diuretic and natriuretic action and subsequently being devoid of a water- and sodium-retaining action.
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PMID:Renal and antihypertensive effects of felodipine in hypertensive patients. 285 95

In a group of 15 men with severe hypertension in a double-blind crossover trial, the new calcium antagonist felodipine has been shown to lower blood pressure as effectively as minoxidil when used in combination with a beta-blocker and a loop diuretic. Felodipine was well tolerated and may have a role in the management of severe hypertension.
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PMID:Felodipine can replace minoxidil in the treatment of refractory hypertension. 285 69

The effects of felodipine and placebo on blood pressure, heart rate and tolerability were investigated in 4 different groups of patients. One group had not received previous therapy, whereas the other 3 groups received concomitant antihypertensive compounds (beta-blockers, diuretics or beta-blocker + diuretics). The haemodynamic effects and tolerability were studied after a single dose, as well as during steady-state conditions. After a single dose of felodipine there was a rapid and significant decrease in blood pressure and increase in heart rate with felodipine alone as well as with combination therapy. During long term treatment, blood pressure was significantly decreased after felodipine during the dosing interval (12h), irrespective of concomitant treatment. Heart rate, however, was not increased, even in patients without a beta-blocker. The reduction in blood pressure was correlated with the plasma concentration of felodipine after single-dose administration, but not during long term treatment. Felodipine was generally well tolerated. In the short term, headache was the most common side effect, while swelling of the ankles was the most frequent adverse effect during long term treatment. In conclusion, felodipine is a promising antihypertensive compound, which may be used in the treatment of high blood pressure, either alone or in combination with other agents.
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PMID:Antihypertensive effects of felodipine compared with placebo. 285 83

Felodipine, a new dihydropyridine, was given to 58 hypertensive patients in combination with an adrenergic beta-receptor antagonist and a diuretic agent. In all but 2 patients the blood pressure was unsatisfactorily controlled on standard triple therapy, i.e. alpha beta-blocker, a diuretic and a vasodilator. A 48-week follow-up was completed by 54 patients. After an initial dose titration period, the maintenance dose of felodipine was 5 mg twice daily in 14 patients and 10 mg twice daily in 34 patients. In the remaining 6 patients, the dose ranged from 5 mg every morning to 25 mg twice daily. The dosages of beta-blocking agent and diuretic were considerably reduced during the study period. Mean supine blood pressure was reduced from 170/101 mm Hg on triple therapy before felodipine to 145/86 mm Hg (p less than 0.001) after 2 weeks on felodipine. This improvement was sustained throughout the study and was measured at 144/86 mm Hg (p less than 0.001) after 48 weeks. There was no increase in resting heart rate and no orthostatic fall in blood pressure. Bodyweight was not increased and felodipine was generally well tolerated. Three patients were withdrawn owing to side effects and 1 was socially non-compliant. It is concluded that felodipine is a potent and well tolerated vasodilator, and will be useful in the long term combination treatment of previously refractory hypertension.
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PMID:Long term experience of felodipine in combination with beta-blockade and diuretics in refractory hypertension. 285 84

The role of felodipine, a new calcium antagonist, as monotherapy in mild and moderate hypertension (supine diastolic blood pressure between 95 and 100mm Hg: phase V) was investigated in a placebo-controlled, double-blind study of 109 patients from 13 centres using 3 different doses. After a 2-week placebo run-in phase the patients were randomised in a double-blind fashion to receive felodipine 2.5mg bid (32 patients), 5 mg bid (30 patients), 10mg bid (24 patients) or placebo (25 patients). Clinical and laboratory measurements were performed after 1, 3 and 8 weeks. 94 patients completed the study. Felodipine reduced supine systolic blood pressure by 22mm Hg from baseline after 8 weeks' treatment on 2.5mg bid, 24mm Hg on 5mg bid and 24mm Hg on 10mg bid at 2 hours after dosage. The corresponding reduction in the placebo group was 6mm Hg. There was a reduction in supine diastolic blood pressure from baseline of 13mm Hg on felodipine 2.5mg bid, 14mm Hg on felodipine 5mg bid and 20mm Hg on felodipine 10mg bid, with no reduction in patients receiving placebo. The percentage of patients completing the study who achieved a supine diastolic blood pressure of 90mm Hg or less after 8 weeks' treatment at 2 hours after dosage was 9% on placebo, 67% on felodipine 2.5mg bid, 57% on felodipine 5mg bid and 92% on felodipine 10mg bid; and at 12 hours after dosage those achieving target supine diastolic blood pressure was 17% on placebo, 37% on felodipine 2.5mg bid, 25% on felodipine 5mg bid and 62% on felodipine 10mg bid. Felodipine was generally well tolerated, although 10 patients on felodipine 10mg bid (42%), 1 on felodipine 5mg bid (3%) and 2 on felodipine 2.5mg bid (6%) withdrew from the study because of adverse effects. One serious adverse event, a myocardial infarction, occurred during the study in a patient with a history of postprandial non-exertional chest pain. In conclusion, felodipine monotherapy appreciably reduces blood pressure in mild and moderate hypertension without significant tachycardia in the short term. Doses of felodipine 2.5mg bid and 5mg bid are better tolerated than 10mg bid and can be recommended for initial treatment in this category of patients.
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PMID:Felodipine, a new calcium antagonist, as monotherapy in mild or moderate hypertension. Cooperative study group. 289 73

1. The antihypertensive efficacy of two different doses of the calcium antagonist felodipine was evaluated in patients with hypertension persisting despite beta-adrenoceptor blocker therapy. Following a single-blind placebo period of 4 weeks, patients were randomized to placebo (n = 36), felodipine 5 mg twice daily (n = 39) and felodipine 10 mg twice daily (n = 35) for another 4 weeks. beta-adrenoceptor blocker therapy remained unchanged throughout the study. 2. Effects on blood pressure (BP) were evaluated after the first dose and after chronic dosing at 2 h after dosing and the end of the dosing interval (12 h). 3. Felodipine decreased systolic and diastolic BP by 30-35/20-25 mm Hg at 2 h. These decreases were similar after acute and chronic treatment. Twelve hours after dosing, decreases of 15-20/10-15 mm Hg were observed compared to 10/5 mm Hg on placebo, and half of the patients still had a controlled BP (supine diastolic BP less than 90 mm Hg). BP responses were rather similar for both doses of felodipine at 2 and 12 h. 4. Multiple regression analysis showed that both initial BP level and plasma felodipine concentrations were significant predictors of the BP response to felodipine, but age was not. 5. Adverse effects attributed to felodipine were mainly related to vascular symptoms (primarily flushing and ankle swelling); these occurred in about 30% of patients, and were pronounced in three patients (4%). 6. Felodipine is therefore highly effective in lowering BP of hypertensive patients on chronic beta-adrenoceptor blocker therapy, with no evidence for a gradual lowering of the BP or for development of tolerance. Both initial BP level and plasma concentrations are better indicators of antihypertensive efficacy of this calcium antagonist than age.
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PMID:Antihypertensive efficacy of the calcium-antagonist felodipine in patients with persisting hypertension on beta-adrenoceptor blocker therapy. The Canadian Felodipine Study Group. 290 54

Felodipine is a dihydropyridine calcium antagonist which selectively relaxes vascular smooth muscle. By acting at peripheral arterioles, it lowers systemic vascular resistance and thereby produces substantial decreases in blood pressure and increases in cardiac output. Felodipine is indicated for the management of hypertension, and in patients with mild to moderate disease felodipine monotherapy markedly lowers blood pressure. It proved as effective as atenolol, and equivalent to hydrochlorothiazide, either with or without amiloride, in terms of antihypertensive activity. Comparative studies also demonstrated that once daily administration with an extended-release formulation provides equivalent antihypertensive efficacy to the same amount of drug administered twice daily as the standard tablets. As a second- or third-line treatment for patients with moderate to severe hypertension refractory to standard drug combinations, felodipine produced considerable reductions in blood pressure when added to beta-blockers and diuretics, either alone or in combination, in studies lasting up to 48 weeks. In comparative studies of multiple-drug treatments felodipine was found to have superior efficacy to hydralazine and prazosin, and was at least as effective as nifedipine, minoxidil and propranolol, when used with diuretics and/or beta-blockers. As an alternative to hydrochlorothiazide, in combination with beta-blockers, felodipine consistently controlled blood pressure in a greater percentage of patients and usually provided greater decreases in blood pressure. The main side effects with felodipine are ankle oedema, headache and flushing. Although the overall incidence of effects is quite high, they are usually mild in nature. Nevertheless, withdrawal due to side effects has been necessary in about 7% of patients overall. Thus, the efficacy of felodipine has been demonstrated in mild, moderate and severe hypertension. At the present time it seems particularly suitable as a second- or third-line treatment in refractory hypertension, but it also can be used as monotherapy for mild to moderate disease.
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PMID:Felodipine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in hypertension. 306 35

We studied the effects of adding felodipine to beta-adrenoceptor blockade on haemodynamics and exercise capacity in 14 patients with stable angina pectoris using a placebo controlled double-blind crossover protocol. Felodipine reduced supine and standing systolic pressure by 13% (P less than 0.01) and 14% (P less than 0.01) respectively and increased supine heart rate 7.4% (P less than 0.05). Felodipine at a plasma concentration of 15.5 +/- 3.0 nmol l-1 increased exercise duration by 16% (P less than 0.01) but failed to attenuate the degree of ST segment depression during exercise. The mean daily number of episodes of angina (0.53 +/- 0.16 on placebo vs 0.37 +/- 0.11 on felodipine) and mean daily GTN consumption (0.51 +/- 0.07 on placebo vs 0.36 +/- 0.12 on felodipine) were not significantly reduced (0.1 less than P greater than 0.05). These findings suggest that felodipine may provide useful additional benefits in patients with hypertension or angina pectoris, who are already receiving beta-adrenoceptor blockers.
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PMID:Effects of felodipine on haemodynamics and exercise capacity in patients with angina pectoris. 310 5

Recently, calcium antagonists have been reported to have a clinically beneficial effect in patients with asthma. Felodipine is a new calcium antagonist of the dihydropyridine group with a high selectivity for arteriolar smooth muscle; it is under clinical investigation for the treatment of hypertension. In this double-blind, randomized crossover trial in 9 patients, the effect of 10 mg felodipine in oral solution on exercise-induced asthma was compared with a placebo on separate days. The FEV1 was at least 80% of the predicted normal value, with variation between study days of less than 10%. Heart rate, blood pressure, and FEV1 were measured before and at 15 and 30 min after each treatment. The exercise test consisted of steady state running at submaximal work loads for 6 to 8 min and started at 30 min after treatments. FEV1 was measured at 1, 2, 5, 10, 15, and 30 min after the end of exercise. The predrug baseline FEV1 values were comparable on the 2 days of the study, and felodipine had no effect on the resting lung function. The mean percentage fall in FEV1 (SEM) after exercise with placebo was 27.0 (4.5)%, and with felodipine it was 13.5 (3.7)%. The difference between felodipine and placebo was statistically significant. While receiving felodipine, the resting heart rate was increased by 15%, with a tendency to lower systolic and diastolic blood pressures. The heart rate after exercise was higher during felodipine treatment than during placebo treatment. One patient receiving placebo and 7 receiving felodipine noted a transient headache. Two patients receiving felodipine also noticed lightheadedness after exercise.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Felodipine, a new calcium antagonist, modifies exercise-induced asthma. 320


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