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)

In 15 centres of the Czech Republic the antihypertensive effect of Amlodipine-Norvasc of Pfizer Co. was tested in 155 patients with mild or medium severe hypertension. The patients were treated by monotherapy, using doses of 5 mg (92%) and 10 mg (8%) per day. In all investigated hypertensive subjects a statistically significant decline of the systolic and diastolic blood pressure occurred in the course of the 12-week investigation (P smaller than 0.01) without affecting the heart rate. The rate of undesirable effects of treatment was very low: only three patients (1.9%) discontinued treatment on account of undesirable effects. The most frequent ones included perimalleolar oedema, the sensation of fullness, headache, cardiac palpitations, vertigo and insomnia. Evaluation of the antihypertensive effectiveness and tolerance of the preparation by the physician and patient is positive, and Amlodipine-Norvasc of Pfizer Co. holds therefore, because of its pharmacokinetic and pharmacodynamic properties, an important place among calcium channel inhibitors of the second generation.
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PMID:[Personal clinical experience in the treatment of arterial hypertension using amlodipine]. 868 1

Preclinical studies indicate that dihydropyridine-type calcium channel antagonists modulate dopamine neurotransmitter function and can reduce cocaine-reinforced behaviors. Amlodipine, a long-acting dihydropyridine-type calcium channel antagonist related to isradipine and nifedipine, was administered in open label fashion for 12 weeks to 26 cocaine-dependent patients. In subjects expressing cocaine craving, craving significantly declined during the course of the 12 weeks. Five individuals reported flushing, headache, fatigue, nocturia, nausea, and lightheadedness. No conclusions regarding efficacy can be made due to the small number of subjects and the open-label design.
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PMID:Amlodipine treatment of cocaine dependence. 1043 93

We designed a study to determine the efficacy and safety of amlodipine given once daily in the pediatric population. Twenty-one patients (mean age 13.1 years) with either essential (n=160) or renal (n=5) hypertension, and newly diagnosed (n=15) or poorly controlled or intolerant on existing antihypertensive therapy (n=6), were included. Patients received amlodipine once daily at a starting mean dose of 0.07+/-0.04 mg/kg per day. The total daily dose of amlodipine was increased 25%-50% every 5-7 days if the mean home blood pressure measurements (HBPM) were above the 95th percentile for age and gender. A baseline followed by a repeat 24-h ambulatory blood pressure monitor study (ABPM) was performed in 20 patients when the mean HBPM was below the 95th percentile goal. The mean titrated dose required to control BP was 0.29+/-0.11 mg/kg per day for those < 13 years, 0.16+/-0.11 mg/kg per day for those > or = 13 years, 0.23+/-0.14 mg/kg per day for essential, hypertension and 0.24+/-0.13 mg/kg per day for renal hypertension. The ABPM demonstrated that amlodipine provided effective BP control as primary therapy in 14 essential patients. Adverse effects included fatigue (n=6), headache (n=5), facial flushing (n=4), dizziness (n=3), edema (n=3), abdominal pain (n=3), chest pain (n=2), nausea (n=1), and vomiting (n=1). Quality of life appeared to improve during therapy. Amlodipine was an effective once daily antihypertensive agent with an acceptable safety profile. Higher doses of amlodipine were required for younger patients, and monotherapy was effective in patients with essential hypertension.
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PMID:Efficacy of amlodipine in pediatric patients with hypertension. 1045 79

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

Blood pressure and headache frequency were evaluated in normotensive male and female cocaine-dependent patients (N=43) participating in a placebo-controlled, double-blind trial of amlodipine for the treatment of cocaine dependence. Amlodipine produced a significant reduction in both systolic (p=0.04) and diastolic (p=0.01) blood pressures without producing dizziness or faintness. Placebo subjects had about three times the frequency of headaches compared to the amlodipine-treated subjects (p=0.004). The high frequency of headaches reported by cocaine-dependent individuals was significantly reduced by amlodipine and may reflect improved cerebrovascular tone.
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PMID:Amlodipine reduces blood pressure and headache frequency in cocaine-dependent outpatients. 1256 10

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

The paper deals with the comparative study of the effects of lercamen (lercadipine) and amlodipine, two third-generation long-acting calcium channel blocker medicine of the dihydropyridine type used in the treatment of hypertension. 80 patients of both sexes, aged from 48 to 76 were treated with lercamen (10-20 mg) or amlodipine (10 mg) for twelve weeks. Some adverse reactions of the above mentioned drugs such as headache, ankle oedema and others were observed and studied with great care. A two-week treatment with lercamen (10 mg) resulted in significant decrease of both systolic and diastolic blood pressure in 74% patients. Further decrease of blood pressure was observed during the following 10 weeks. The doze of lercamen had to be doubled for 26% of patients. After 12 weeks blood pressure in lercamen group was 126+/-4.5/80.4+/-5.3 mmHg (p<0.01 versus baseline). Amlodipine caused similar decrease of blood pressure. Sympathetic activation occurs neither with lecramene not with amlodipine during chronic therapy. Less adverse drug reactions were observed among lercamen group, which equaled with 12% than among the amlodipine group, which was 26,3%. We believe that adverse reactions are weakly expressed in lercamen group than in amlodipine group due to high lypophility and unique membrane kinetic of lercamen. Lercamen has proved not only better efficiency but also better endurance in chronic treatment of essential hypertension in patients.
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PMID:[Some aspects of the clinical use of lercamen (lercadipine)]. 1964 90


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