Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0018681 (headache)
 56,091 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Amlodipine, a potent long-acting dihydropyridine calcium antagonist, was compared with placebo in a parallel, randomized, double-blind study in 134 patients with chronic stable angina pectoris maintained on beta-adrenergic blocking agents. After a single-blind, two-week placebo period, patients were randomized to receive either amlodipine (2.5, 5, and 10 mg) or placebo once daily for four weeks. The effects of amlodipine on maximal exercise time, work, time to angina onset, and subjective indices including angina frequency, nitroglycerin tablet consumption, and patient and investigator ratings were assessed. Each dose of amlodipine produced increases in exercise time and calculated total work accomplished compared to baseline. Improvements at 5 and 10 mg were significantly greater than placebo which produced no significant change (p less than 0.05). Qualitative improvements in the severity of angina were produced by amlodipine at 5 and 10 mg daily assessed by patient-rating questionnaires (p less than 0.05). Reductions in angina frequency attacks per week and weekly nitroglycerin tablet consumption occurred but were not statistically significant when compared with placebo. Adverse effects observed during amlodipine treatment prompted discontinuation of treatment in only 2 out of 100 patients. Three patients discontinued treatment for reported lack of efficacy. No laboratory abnormalities prompted treatment discontinuation and minor side effects of dizziness, nausea, headache, and fatigue were observed infrequently. The results of this controlled, large-scale multicenter trial suggest that amlodipine significantly increased exercise capacity and was well tolerated when added to the antianginal regimen of patients remaining symptomatic while receiving beta-blocking agents.
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PMID:Amlodipine combined with beta blockade for chronic angina: results of a multicenter, placebo-controlled, randomized double-blind study. 135 85

Amlodipine and nitrendipine are calcium antagonists of the 1,4-dihydropyridine group which differ in their pharmacokinetic and pharmacodynamic properties. The clinical relevance of these differences was investigated in a study designed to compare the efficacy and safety of once-daily amlodipine (5 mg) and nitrendipine (20 mg) in patients with mild-to-moderate essential hypertension. Ambulatory blood pressure monitoring and conventional measurements showed that amlodipine and nitrendipine produced comparable reductions in blood pressure after 4 weeks of treatment. However, the onset of the antihypertensive effect was gradual for amlodipine, while most of the reduction achieved at the end of treatment with nitrendipine was seen after the first dose. There were no significant changes in heart rate with amlodipine, but significant increases occurred during the first 6 h of nitrendipine treatment. Amlodipine was associated with a significantly lower incidence of vasodilator-related adverse effects at initiation of therapy (headache, flushing, tachycardia) compared with nitrendipine, which may reflect its slower onset of action. The different pharmacodynamic and toleration profiles of amlodipine and nitrendipine at therapeutically equivalent doses suggest that amlodipine may have advantages in the treatment of hypertension, especially in terms of the low incidence of acute side effects, which may ultimately translate into improved patient compliance.
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PMID:Amlodipine compared to nitrendipine in hypertensive patients: the effects on toleration in relationship to the onset of action. 153 15

The frequency and severity of adverse effects during the first 14 days of treatment with amlodipine (5 mg once daily), nifedipine retard (20 mg twice daily) or placebo were compared in a multicentre, three-way, cross-over study involving 97 patients with mild-to-moderate hypertension. All three groups of patients were well matched for age, sex and baseline blood pressure. Amlodipine and nifedipine retard produced highly significant and comparable reductions in blood pressure, indicating that the doses were therapeutically equivalent. The incidence of adverse effects considered to be definitely or probably related to nifedipine retard treatment (41%) was significantly higher than for placebo (16%, p less than 0.01) or amlodipine (27%, p less than 0.05). There were no significant differences in the incidence of vasodilator-related adverse effects between amlodipine and placebo. In contrast, headache, flushing and dizziness were reported more frequently by patients while on nifedipine retard than on placebo or amlodipine. The convenience of once-daily dosing, together with a lower incidence of adverse effects, with consequently fewer withdrawals from therapy, suggests that amlodipine has clinical advantages over nifedipine retard in the treatment of hypertension.
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PMID:Comparison of early side effects with amlodipine and nifedipine retard in hypertension. 153 16

Amlodipine is a dihydropyridine calcium antagonist that has unique pharmacokinetic properties. The drug is absorbed gradually after oral administration and so produces a gradual vasodilatation, reducing the incidence of side effects such as reflex tachycardia and headache, which can be troublesome with other calcium antagonists. Amlodipine also has a long elimination half-life, which makes it suitable for use on a once-daily basis. Controlled clinical studies have confirmed that a suitable dose regimen of amlodipine for use in angina is to start with 5 mg daily and increase this to 10 mg daily if required to control symptoms. Exercise testing carried out 24 hours post dose has confirmed that once-daily doses of amlodipine provide good anti-anginal and anti-ischaemic efficacy for a full 24 hours, a vital aspect of any therapy for ischaemic heart disease. Amlodipine has been shown to have comparable anti-anginal efficacy to the beta-blocker nadolol taken once daily and the calcium antagonist diltiazem taken 3 times daily. When added to the treatment regimen of patients with uncontrolled chronic stable angina despite treatment with nitrates, beta-blockers or both, amlodipine produces improved anti-anginal efficacy. Amlodipine has also been shown to be consistently effective in patients with vasospastic angina. There has been no evidence of tolerance to the anti-anginal effects of amlodipine in formal clinical trials involving treatment for up to 26 weeks.
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PMID:The efficacy of amlodipine in the management of ischaemic heart disease. 183 71

Three hundred and twenty hypertensive out-patients were recruited to this multicentre general practice study of the efficacy and safety of amlodipine. Patients with baseline sitting diastolic blood pressure in the range 95-115 mmHg at two consecutive visits went on to a 12-week active treatment phase of the study. In this study, patients received open-label amlodipine at a starting dose of 5 mg/day, which could be adjusted after 4 weeks to 10 mg/day if necessary to achieve a sitting diastolic blood pressure of less than or equal to 90 mmHg. Amlodipine produced significant (P less than 0.05) blood pressure reductions throughout the study without significant changes in heart rate. The exposure to amlodipine in this study was 873 patient months. Most adverse events were mild or moderate and the investigators' overall evaluation of tolerability was excellent or good for 91% of patients. The most frequently reported adverse events were oedema (13.8%), headache (7.8%) and rashes (3.8%). Analysis of data for subgroups of patients confirmed that there were no important differences in the efficacy and tolerability of amlodipine in elderly or young patients and in patients taking amlodipine as monotherapy or in combination with other antihypertensive agents. This uniformity of response is clearly an important factor in consideration of antihypertensive therapy use in general practice.
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PMID:A study of the efficacy and safety of amlodipine for the treatment of hypertension in general practice. 183 35

The efficacy and tolerability of amlodipine (5 mg, once daily), nifedipine retard (20 mg, twice daily), and placebo were compared in a multicenter, three-way, crossover study involving 97 patients with mild-to-moderate hypertension. Each patient underwent three, 2-week treatment periods separated by 2-week washout periods without therapy. Comparable and significant (p < 0.05) blood pressure reductions were observed after amlodipine and nifedipine retard when compared with placebo, except in the case of supine systolic blood pressure with nifedipine retard. A significantly greater incidence of treatment-related side effects was observed with nifedipine retard (41%) compared with amlodipine (27%, p < 0.05) or placebo (16%, p < 0.01). Amlodipine treatment was associated with significantly fewer reports of headache and flushing than nifedipine retard (p < 0.05). The lower incidence and reduced severity of vasodilator side effects associated with amlodipine resulted in fewer withdrawals and a better overall tolerability profile.
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PMID:Side effects of dihydropyridine therapy: comparison of amlodipine and nifedipine retard. 752 87

The anti-hypertensive efficacy and safety of extended-release (ER) felodipine (5, 10 or 20 mg) and amlodipine (5 or 10 mg) once daily were compared in patients with mild to moderate essential hypertension in a double-blind, double-dummy, randomised, comparative study. One hundred and eighteen patients were randomised to receive either felodipine ER (n = 57) or amlodipine (n = 61) for 12 weeks. Efficacy was assessed by measuring office blood pressure (BP) at baseline and after 4, 6, 8 and 12 weeks, together with 24h ambulatory blood pressure monitoring (ABPM) at baseline, on day 1 of treatment and at the end of the study. The mean office BP changes from baseline to week 12 were -13.4/-11.8 mmHg for felodipine ER (mean daily dose 11.2 mg) and -15.3/-12.9 mm Hg for amlodipine (mean daily dose 7.4 mg). Changes in office BP between treatment groups were not significant. The mean 24h ambulatory BP changes from baseline to end of the study were -11.6/-10.0 mm Hg for felodipine ER and -16.3/-9.6 mm Hg for amlodipine, both significant (P < 0.01). The fall in systolic ambulatory BP was significantly greater (P < 0.001) in the amlodipine-compared with felodipine ER-treated patients but there was no difference between the groups with respect to diastolic ambulatory BP. Both drugs were well tolerated with only seven patients withdrawing because of side-effects, equally distributed between treatment groups. Headache and flushing were significantly (P < 0.05) more frequent in the felodipine ER group. Amlodipine appears to be more potent on a milligram to milligram basis and induces fewer side-effects than does felodipine ER.
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PMID:Comparative effects of amlodipine and felodipine ER on office and ambulatory blood pressure in patients with mild to moderate hypertension. Danish Multicentre Group. 778 10

Amlodipine, a dihydropyridine calcium antagonist, was administered at 2.5-5.0 mg/day for 8 weeks to 35 hypertensive patients with renal dysfunction, and its efficacy and safety were evaluated. The target reduction in blood pressure was achieved in 28 of the 35 patients (80%), while blood pressure was decreased in 4 patients (11.4%) and unchanged in 3 patients (8.6%). A side effect of mild headache was reported by one patient (2.9%). In addition, abnormal changes in laboratory values were observed in five patients, but all of the changes were mild. Blood urea nitrogen and serum creatinine levels both increased in two of these five patients, and serum creatinine levels increased in another two patients. Serum amlodipine concentration was 4.86 +/- 2.57 ng/ml (n = 8) and 3.01 +/- 1.02 ng/ml (n = 8) in patients receiving a daily dose of 2.5 mg for 2-5 weeks and 8-10 weeks, respectively. Serum concentration in patients receiving 5 mg from Weeks 2-6 was 9.72 +/- 6.89 ng/ml (n = 6) after 7-9 weeks, suggesting no tendency for the accumulation of this drug. The drug was rated as of clinical benefit in 27 of the 35 patients (77.1%), and as slightly beneficial in another 5 patients (14.3%). Thus, amlodipine significantly decreased the blood pressure while causing little or no aggravation of renal dysfunction in hypertensive patients with renal impairment.
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PMID:Efficacy and safety of amlodipine in hypertensive patients with renal dysfunction. 807 Jan 49

In a multicentre crossover study of 97 patients with mild hypertension, the incidence and severity of adverse effects were observed during the first 14 days of treatment with amlodipine, nifedipine retard or placebo. Amlodipine (5 mg) once daily was equipotent to nifedipine retard (20 mg) twice daily. At these doses, the incidence of adverse effects was significantly greater during treatment with nifedipine retard (41%) than with amlodipine (27%, P < 0.05) or placebo (16%, P < 0.01). In particular, headache and flushing occurred significantly less frequently during the first 14 days of treatment with amlodipine than with nifedipine retard. The lower incidence and reduced severity of vasodilatory side-effects associated with amlodipine resulted in fewer withdrawals during initiation of therapy (2 on amlodipine compared with 7 on nifedipine retard).
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PMID:Early side-effects of antihypertensive therapy: comparison of amlodipine and nifedipine retard. 845 May 26

Amlodipine belongs to the dihydropyridine class of calcium channel blockers. Both short and long term studies indicate that amlodipine effectively lowers mild to moderately elevated blood pressure and relieves symptoms of angina pectoris. In comparative studies, its antihypertensive efficacy is similar to that of other established agents such as beta-blockers, diuretics, ACE inhibitors and other calcium channel blockers (including the dihydropyridines); limited comparative data are, however, available in patients with angina pectoris. Amlodipine may offer potential in patients with congestive heart failure. Vasodilator adverse events such as oedema, headaches, and flushing are commonly observed with amlodipine. The drug does not appear to cause postural hypotension, reflex tachycardia or cardiac conduction disturbances. Comparative studies suggest that amlodipine is at least as well tolerated as other standard agents. Thus, amlodipine provides an attractive therapeutic option for the treatment of hypertension, and offers potential for patients with angina pectoris. Its beneficial effects in patients with congestive heart failure require confirmation in future studies.
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PMID:Amlodipine. A reappraisal of its pharmacological properties and therapeutic use in cardiovascular disease. 852 73


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