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 systemic and renal hemodyanmic effects of bupicomide were studied in 10 male patients with uncomplicated essential hypertension of moderate severity. Bupicomide significantly reduced systolic, diastolic, and mean arterial pressure and peripheral vascular resistance and this hypotensive effect was associated with a reflexive increase in heart rate, left ventricular ejection rate, and cardiac index; it had no effect upon other reflexive sympathetic adjustments induced by upright tilt and the Valsalva maneuver. Bupicomide also increased renal blood flow and decreased renal vascular resistance, but it had no effect upon the glomerular filtration rate. The hypotensive mechanism of bupicomide therefore is mediated by peripheral arteriolar dilation, through vascular smooth muscle relaxation. The more immediate clinical side effects of bupicomide are related to its strong vasodialting action and include headaches, cutaneous flushing, and tachycardia.
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PMID:Systemic and renal hemodynamic effects of bupicomide: a new vasodilator. 78 20

The antihypertensive effects of the regular immediate release formulation of verapamil (verapamil IR) and the newer sustained release formulation of verapamil (verapamil SR) were compared in Hispanic patients with untreated essential hypertension. Verapamil IR was given in 3 divided doses (80 or 160mg 3 times daily) and verapamil SR was given either as a single daily dose of 240mg or as 240mg every 12 hours. With both formulations there was a significant reduction in systolic (SBP) and diastolic blood pressure (DBP); a greater lowering of BP was observed with verapamil 480 mg/day than with 240 mg/day. With verapamil SR 480 mg/day, 91% of patients had reductions in SBP and DBP greater than 20 and 15mm Hg, respectively. In addition, 83% of patients reached normotension. With the lower dose (240mg once daily), 83% of patients had decreases in DBP greater than 10mm Hg and 73% of patients achieved normotension. Comparable effects were achieved with verapamil IR. With verapamil IR there was a more rapid fall in BP which peaked 3 to 4 hours postdose, whereas with verapamil SR a more gradual and sustained BP reduction was observed. Only small changes in heart rate (HR) were observed with verapamil IR and verapamil SR. For verapamil SR, the mean increase in HR was 5 beats/min (to 80 beats/min) and the mean decrease in HR was 13 beats/min (to 62 beats/min). Both verapamil SR and verapamil IR prolonged the PR interval of the ECG. An equal degree of PR prolongation was observed with 240 and 480 mg/day. The incidence of side effects (headache, palpitations, dizziness and flushing) was dose dependent, decreased with continuous treatment and was much higher with verapamil IR than with verapamil SR. Steady-state plasma verapamil concentrations were monitored. Compared with verapamil IR, verapamil SR produced a more gradual rise and a more sustained elevation of plasma verapamil and norverapamil concentrations. Comparable trough verapamil concentrations (Cmin) were observed with verapamil IR (98 micrograms/L) and SR (81 micrograms/L); morning Cmin verapamil concentrations were higher than daytime Cmin values. The normalised area under the plasma concentration-time curve (AUC) and maximum concentration (Cmax) were 10 to 20% greater for verapamil IR than SR. The 2-fold increase in oral dose produced a 2.2- and 2.4-fold increase in AUC for verapamil IR and SR, respectively, associated with a 20% reduction in metabolism to norverapamil. Fasting increased the rate and extent of absorption of verapamil.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:Comparative efficacy, safety and pharmacokinetics of verapamil SR vs verapamil IR in hypertensive patients. 128 70

In a randomized, parallel, double-blind study, lisinopril (n = 412) reduced systolic and diastolic blood pressure more than nifedipine did (n = 416) after ten weeks treatment in patients (40-70 years) with mild to moderate essential hypertension. Lisinopril was tolerated better than nifedipine, with fewer withdrawals. Adverse experiences reported after a general question on discomfort were significantly lower for lisinopril than for nifedipine. Questions referring specifically to symptoms revealed higher frequency of coughing with lisinopril, while flushing, edema, palpitations, dizziness, tiredness and rash were reported more frequently with nifedipine. Quality of life was similarly assessed by both patients and spouses. No significant differences in well-being during treatment were found for either drug, except in the case of the highest dose level of nifedipine, which caused a deterioration of well-being.
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PMID:[Treatment with lisinopril or nifedipine in essential hypertension. A Norwegian multicenter study of the effect, tolerance and quality of life of 828 patients]. 133 84

Prostacyclin (PGI2) is known to cause vasorelaxation and inhibit platelet aggregation by receptor-mediated mechanisms. While cyclic (c) AMP is known to act as a second messenger for inhibition of platelet aggregation, vasorelaxation by hyperpolarization has been described only recently and may provide an explanation, in addition to stimulation of cAMP for the PGI2 mechanism of action on blood vessels. When PGI2 is infused into healthy volunteers it reduces blood pressure only at infusion rates that also cause significant side-effects, primarily, nausea, emesis, flushing, diaphoresis, and restlessness. In hypertensive patients blood-pressure responses are complex and are influenced to some extent by renin secretion. PGI2 stimulates renin secretion by a direct effect on the juxtaglomerular apparatus, and it also has an indirect effect by activating the sympathetic nervous system. Thus, it is useless as an antihypertensive agent even apart from its debilitating side-effects. Vascular PGI2 is synthesized endogenously by both the endothelial cells and the muscularis of arteries. While the endothelial cells undoubtedly synthesize large amounts of PGI2, the muscularis comprises a much larger tissue mass so that the overall synthesis is about equally distributed between the endothelial and muscle cells. In patients with pregnancy-induced hypertension and some patients with essential hypertension endogenous synthesis of PGI2 has been evaluated by measuring 2,3-dinor-6-keto-PGF1 alpha and has proved to be greatly reduced. Some drugs (thiazides, propranolol) have been shown to stimulate PGI2 synthesis, and inhibition of cyclooxygenase has been shown to reduce their antihypertensive effects. The effects of low- and high-dose aspirin on prostacyclin and thromboxane synthesis are discussed.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:[Prostacyclin in hypertension]. 149 51

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

In a randomized, parallel, double-blind study, lisinopril (n = 412; average dose 18.8 mg) reduced systolic and diastolic blood pressure (change = 20.2/13.8 mmHg; P less than 0.01/P less than 0.01) more than nifedipine (n = 416; average dose 37.4 mg; change = 13.3/11.2 mmHg) after 10-week treatment in patients, aged 40-70 years, with mild-to-moderate essential hypertension. Lisinopril was better tolerated than nifedipine. The withdrawals from treatment were fewer in the lisinopril-treated group (11 versus 46; P less than 0.01). The frequency of adverse experiences reported after a general question of discomfort was significantly lower for lisinopril than for nifedipine (P less than 0.01). When questioned on specific symptoms, frequency of coughing was higher with lisinopril (P less than 0.01), while flushing, edema, palpitations, dizziness, tiredness and rash were reported more frequently (P less than 0.01, for all) in the nifedipine-treated group. Quality of life was assessed by both patients and spouses. No significant changes in wellbeing were observed for either drug, except for the highest dose level of nifedipine which caused a deterioration.
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PMID:Lisinopril or nifedipine in essential hypertension? A Norwegian multicenter study on efficacy, tolerability and quality of life in 828 patients. 166 65

Amlodipine, a basic dihydropyridine derivative, inhibits the calcium influx through 'slow' channels in peripheral vascular and coronary smooth muscle cells, thus producing marked vasodilation in peripheral and coronary vascular beds. Short to medium term clinical trials indicate that amlodipine is effective as both an antianginal agent in patients with stable angina pectoris and an antihypertensive agent in patients with mild to moderate hypertension. In small comparative studies amlodipine was at least as effective as 'standard' agents, including atenolol, verapamil, hydrochlorothiazide or captopril in hypertension, and diltiazem or nadolol in angina pectoris. Amlodipine is well tolerated, and does not appear to cause some of the undesirable effects often associated with other cardiovascular agents (e.g. adverse changes in serum lipid patterns, cardiac conduction disturbances, postural hypotension). The most common adverse effects associated with amlodipine therapy--oedema and flushing--are related to the vasodilatory action of the drug, and are generally mild to moderate in severity. Thus, amlodipine seems to provide a useful alternative to other agents currently available for the treatment of essential hypertension and chronic stable angina pectoris, with certain pharmacodynamic and tolerability properties that should be advantageous in many patients.
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PMID:Amlodipine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in cardiovascular disease. 171 48

In this study of the efficacy and safety of isradipine as first-line therapy in hypertension, 1,647 patients enrolled; 1,472 completed the 4-week placebo run-in period and began treatment with isradipine at 2.5 mg twice daily for 4 weeks. During placebo, 11% (n = 175) of the 1,647 patients withdrew because of normalization of blood pressure, side effects, noncompliance, violation of the study protocol, side effects from concomitant therapy, or other reasons. During isradipine therapy (n = 1,376), blood pressure decreased from 168 +/- 18/102 +/- 8 mm Hg at the end of the placebo period to 155 +/- 17/94 +/- 9 mm Hg after 2 weeks (p less than 0.001) and 151 +/- 16/92 +/- 9 mm Hg after 4 weeks (p less than 0.001). During active treatment, 6.4% (n = 94) were withdrawn because of flushing, headache, edema, palpitations, gastrointestinal side effects, skin rashes, or other side effects, and two patients because of lack of efficacy. The side effect score in the remaining patients worsened for flushing, remained unchanged for edema, but significantly improved for palpitations, fatigue, dizziness, headache, and nervousness. After 4 weeks, 60% of patients had diastolic blood pressures of less than or equal to 90 mm Hg. Thus, isradipine is effective and safe as first-line therapy in patients with primary hypertension as seen in general practice.
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PMID:Calcium antagonists as first-line therapy in hypertension: results of the Swiss Isradipine Study. Swiss Hypertension Society. 172 Apr 76

The efficacy and safety of isradipine and nifedipine retard were compared in 51 patients with mild-to-moderate essential hypertension. A 4-week placebo run-in period was followed by an 8-week course of treatment. Patients were randomly allocated to either isradipine 1.25 mg twice daily (n = 24) or nifedipine 20 mg twice daily (n = 826); dosages were doubled if blood pressure was not normalized [diastolic blood pressure greater than or equal to 90 mm Hg) after 4 weeks of active treatment. Systolic/diastolic blood pressures were significantly reduced (p less than 0.01/p less than 0.01) by isradipine from 162/103 to 145/89 mm Hg, and by nifedipine from 162/104 to 143/88 mm Hg. Normalization rates were 79% with isradipine and 67% with nifedipine. It was necessary to double the dosage in seven of the patients taking isradipine and in three of those taking nifedipine; the mean final dosages were 1.63 mg and 22.4 mg twice daily, respectively. Heart rate did not change significantly with either treatment. There were drug-related adverse events in five patients (21%) taking isradipine (2 edema, 2 headache, 2 palpitations, 1 flushing) and in eight (30%) of those taking nifedipine (5 edema, 2 headache, 1 palpitations). Therapy was withdrawn in one patient in the isradipine group (1 headache) and two patients in the nifedipine group (1 edema, 1 headache). We conclude that isradipine is a highly effective and well tolerated antihypertensive agent.
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PMID:First clinical experience with isradipine in the treatment of hypertension in Portugal. 172 Apr 85

Efficacy and tolerability of antihypertensive monotherapy with the calcium antagonist nitrendipine were investigated in a 6-month open trial in 495 patients with mild to moderate essential hypertension from 101 practicing internists and general practitioners. Previous antihypertensive therapy (57.4%) was stopped for 1 week and therapy then started with nitrendipine, 20 mg once daily. Sixty-one patients discontinued therapy prematurely because of unwanted effects, mostly characteristic with dihydropyridines (headaches, flushing, and ankle edema), and 23 patients because of insufficient efficacy. In 75% of the remaining 411 patients, the goal blood pressure was achieved by nitrendipine monotherapy (10 mg in 17.6%, 20 mg in 73.3%, and 20 mg b.i.d. in 8%) and diastolic blood pressure was between 90 and 95 mm Hg in another 6%. The reduction in blood pressure did not result in changes of heart rate or weight. Nitrendipine was effective in patients of all age groups but patients older than 60 years of age showed a significantly greater fall in systolic pressure than middle-aged or young patients. At the end of the study, 15 patients still reported side effects. Nitrendipine appears to be well suited for first-line therapy of mild to moderate essential hypertension.
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PMID:Antihypertensive monotherapy with nitrendipine in general practice. 172 58


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