Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0016382 (flushing)
 6,387 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The safety and efficacy of Amlodipine (AML) for mild to moderate hypertension was evaluated in a "real life" setting. This open non-comparative trial included 123 men and 143 women (age 30-91 years, mean 59.4). All had sitting diastolic blood pressure (DBP) between 95 and 115 mmHg, confirmed in most by 2 baseline measurements, 2 weeks apart. Eligible patients were given AML 5 mg daily as add-on or monotherapy and were evaluated 4 weeks later. If DBP was then > 90 mmHg, the daily dose was raised to 10 mg; those with < 90 mmHg remained on 5 mg. AML was continued for 8 weeks. Other BP-lowering drugs were unchanged. Of the original 266 patients 22 (8.2%) withdrew due to adverse events (AE), and others were protocol violators, lost to follow-up or withdrew, leaving 211 available for efficacy analysis. In this major group BP was reduced from 165 +/- 15/101 +/- 4 to 139 +/- 11/83 +/- 5 after 12 weeks of AML (p < 0.05). The reduction was greater in those under 70 years, from 173 +/- 12/100 +/- 5 to 142 +/- 12/80 +/- 4 (p < 0.05). In those with BMI > 30 kg/m2, BP decreased from 165 +/- 15/101 +/- 5 to 140 +/- 12/83 +/- 5 (p < 0.05). Mean change in heart rate was -1.5 bpm (p < 0.05). Mean final AML dose was 5.5 mg/day. The most common AML-related AE requiring cessation of the drug was pedal edema in 2.6% of the 266 patients; in 3.7% it persisted during therapy. Other AE occurring in > 1% were dizziness in 1.8%, headache 1.5%, flushing 1.1% and fatigue 1.1%. We conclude that AML is an effective and well-tolerated antihypertensive suitable for most hypertensive patients.
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PMID:[Multicenter community-based trial of amlodipine in hypertension in Israel]. 1095 90

Amlodipine, a long-acting dihydropyridine calcium channel blocking agent, was administered to 55 children (age: 11.5 +/- 5.4 years) with hypertension, 49 of whom (89%) had secondary hypertension. Efficacy was assessed by comparing pretreatment blood pressure (BP) to follow-up BP obtained in our outpatient Pediatric Nephrology clinic. Thirty-two (58%) patients achieved BP control with amlodipine alone, and 31 (55%) patients received amlodipine twice daily. Eleven patients received amlodipine as a suspension. Mean amlodipine dose was 0.16 +/- 0.12 mg/kg/day; there was an inverse relationship between patient age and amlodipine dose. Follow-up BP were significantly lower than pretreatment BP: systolic BP fell from 129 +/- 12 to 122 +/- 12 mm Hg (P = .004), and diastolic BP fell from 78 +/- 13 to 70 +/- 19 mm Hg (P = .003). A small, clinically insignificant increase in heart rate (from 91 +/- 19 beats/min to 99 +/- 26 beats/min; P = .02) occurred during amlodipine treatment. Adverse effects reported included dizziness (three patients), fatigue (two patients), flushing (two patients), and leg edema (one patient). All improved with dose reduction. We conclude that amlodipine provides effective BP control without significant adverse effects in children with hypertension, and can be used as monotherapy in most children. Young children appear to require significantly higher doses per kilogram of body weight than older children. Twice-daily dosing may be required in many children to achieve BP control. Detailed pharmacokinetic studies are needed to confirm these observations.
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PMID:Treatment of hypertensive children with amlodipine. 1104 Nov 59

Amlodipine is a potent peripheral and coronary vasodilator with high selectivity for vascular smooth muscle, and is widely used in mild to moderate hypertension, chronic stable angina and vasospastic angina. Its most prevalent side effects are peripheral edema, flushing and headache. Cutaneous adverse reactions associated with amlodipine have been rarely reported. Herein, a male patient is described to develop oral mucosal and cutaneous hyperpigmentation one year after starting amlodipine, which became more noticeable with time. Although cutaneous hyperpigmentation was most prominent on the photoexposed areas, there was no history of previous photosensitivity, pruritus or flushing. To our knowledge, no case of oral and cutaneous hyperpigmentation associated with amlodipine has been formally reported up to date.
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PMID:Amlodipine associated hyperpigmentation. 1475 92

Structural features of amlodipine give the molecule physicochemical and pharmacokinetic properties that are unique among calcium antagonists. Amlodipine is absorbed gradually after oral administration (peak plasma levels 6-12 h postdose) and has an absolute bioavailability of 64%. Low clearance and a high volume of distribution give amlodipine a long elimination half-life, and mean effective plasma levels are maintained with once-daily doses. With repeated once-daily dosing, the steady state is achieved after the seventh to ninth dose. The pharmacokinetic properties of amlodipine avoid the sharp fluctuations in plasma level seen with other calcium antagonists that are associated with vasodilatation-induced side effects such as tachycardia, headache, and flushing. The pharmacokinetics of amlodipine are not significantly altered in elderly or renally impaired patients, but there is reduced clearance in patients with hepatic impairment. There are no pharmacokinetic interactions between amlodipine and cimetidine or digoxin.
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PMID:Amlodipine: pharmacokinetic profile of a low-clearance calcium antagonist. 1629 97

A previous article on the safety of amlodipine reviewed data from over 4,000 subjects who participated in clinical trials sponsored by Pfizer Central Research. Once-daily amlodipine was shown to be a well-tolerated treatment of hypertension and myocardial ischemia. Although amlodipine is a potent vasodilator, there was a low incidence of side effects such as headache, flushing, and dizziness. Amlodipine was not associated with adverse effects on hematologic or biochemical safety parameters nor on serum cholesterol or triglyceride levels. Amlodipine did not alter electrical conduction in the heart. Amlodipine had a favorable safety profile in comparative trials vs. beta-blockers. The data base of comparative trials vs. other calcium antagonists was small but the toleration of amlodipine was similar to that of verapamil and diltiazem. No data from comparative trials vs. another calcium antagonist of the dihydropyridine class have been available. This article reviews data from recently completed trials vs. nitrendipine and from trials in which amlodipine was used in combination with other agents. Amlodipine was better tolerated than nitrendipine and had a much lower incidence of side effects usually related to vasodilatation. This difference in side-effect profile was especially marked during the first days of treatment. Amlodipine was well tolerated when used in combination with beta-blockers, diuretics, ACE inhibitors, and nitrates. The gradual onset of action and relatively long half-life of amlodipine are the probable cause for the improved toleration in comparison with other dihydropyridines. Besides the low incidence of trivial side effects, increasing clinical experience with amlodipine provides no evidence that amlodipine is a cause of rare but serious adverse effects. It is concluded that amlodipine is an antihypertensive and anti-ischemic agent that has the combined advantages of a good safety profile with once-daily dosage and a smooth onset and long duration of action.
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PMID:An update on the safety of amlodipine. 1629 14

All children aged > or = 3 years should have an annual blood pressure (BP) measurement taken during a routine physical examination. Physicians should become familiar with recommended pediatric normative BP tables. BP above the 95th percentile may require drug therapy. There are several categories of antihypertensives available to the clinician. Calcium channel antagonists (CCAs) are a class of drugs that exert their antihypertensive effect by inhibiting the influx of calcium ions across the cell membranes. This results in dilatation of peripheral arterioles. When given orally, CCAs are metabolised in the liver by cytochrome P450 (CYP) enzyme CYP3A4; hence, some CCAs will affect the half-life of drugs that share this enzyme system for their metabolism. CCAs can be safely used in children with renal insufficiency or failure and as a general rule there is no need to modify drug dosage in this population. CCAs are generally well tolerated; most adverse effects appear to be dose related. Headache, flushing, gastrointestinal upset, and edema of the lower extremities are the most common symptoms reported with the use of CCAs. Pediatric data regarding safety and efficacy of CCAs have mostly been obtained from retrospective analyses. Extended-release nifedipine and amlodipine are the two most commonly used oral CCAs in the management of pediatric hypertension. These drugs can be given once a day, although many children require twice-daily administration. Extended-release nifedipine has to be swallowed whole; hence, its use in younger children who cannot swallow pills is limited. Amlodipine can be made into a solution without compromising its long duration of action; therefore, it is the CCA of choice for very young children. Oral short-acting nifedipine and intravenous nicardipine are safe and effective CCAs for the management of hypertensive crisis in children. Short-acting nifedipine can cause unpredictable changes in BP; hence, it should be used cautiously and in low doses. Intravenous nicardipine has a rapid onset of action and a short half-life. Intravenous infusion of nicardipine can be titrated for effective control of BP. Intravenous nicardipine has been used safely in hospitalized children and newborns for the management of hypertensive crisis, and for controlled hypotension during surgery. CCAs are a class of antihypertensives that are safe and effective in pediatric patients. They have relatively few adverse effects and are well tolerated by children. This article reviews CCAs as antihypertensives in the management of pediatric hypertension.
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PMID:A review of calcium channel antagonists in the treatment of pediatric hypertension. 1715 43

Amlodipine is a dihydropyridine calcium channel blocker that is used in the management of both hypertension and angina. Amlodipine induced side effects are headache, dizziness, edema, flushing, palpitations, and rarely gingival hyperplasia. The exact reason of amlodipine-induced gingival hyperplasia is not known. We presented a case with chronic renal failure (CRF) that developed gingival hyperplasia due to amlodipine use, which improved after ceasing the drug.
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PMID:Amlodipine-induced gingival hyperplasia in chronic renal failure: a case report. 2351 9


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