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Query: UMLS:C0018681 (headache)
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In a double-blind 3-month study in mild-to-moderate essential hypertensive patients over 50 years of age, ketanserin, a selective S2-serotoninergic antagonist with additional alpha 1-adrenergic blocking properties, has been compared with enalapril, an angiotensin-converting enzyme inhibitor. Supine and upright blood pressures and heart rates were recorded for placebo and during active treatment (-4, -2, 0, 2, 4, 6, 8, 10, and 12 weeks). Metabolic profile (plasma glucose, creatinine, sodium, potassium, total and HDL-cholesterol, triglycerides, uric acid) was monitored during treatment with placebo and at the end of the study. Mean blood pressure was equally and significantly (p less than 0.001) lowered by both drugs from 2 weeks of treatment, whereas no changes occurred in mean heart rate or in biochemical variables. Dizziness was observed in three patients on ketanserin and in one patient on enalapril, whereas headache occurred in only one patient on enalapril. These data indicate that ketanserin is as effective and well tolerated as enalapril in hypertensive patients over 50 years of age.
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PMID:Comparison of ketanserin and enalapril in the treatment of mild-to-moderate essential hypertension. 228 42

To assess efficacy and side effects during chronic oral therapy, we studied the effect of ketanserin (Kn) in 17 hypertensive patients for a period up to 1 year. Ketanserin controlled blood pressure satisfactorily in 25%, in part in 50% and had little or no effect in 25%. Reduction in diastolic pressure equalled that in systolic pressure at rest and after exercise and during handgrip. Pulse rate was slowed. Dosage in excess of 60 mg of Kn per day caused troublesome central nervous system symptoms or headache in some patients. A nonsteroidal antiinflammatory drug appeared to antagonize the antihypertensive effect of Kn in one patient. Red cell rigidity and platelet aggregation to ADP and collagen were significantly decreased. Serum potassium and uric acid were significantly decreased; serum creatinine increased during Kn treatment. The antihypertensive and pulse slowing effects of Kn were confirmed during the year's study, in a randomized placebo-controlled crossover study.
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PMID:Clinical studies with ketanserin in hypertension. 241 40

In the Swiss Ketanserin Study the antihypertensive efficacy and tolerability of ketanserin (given in 20 or 40 mg doses twice daily) was investigated, after a placebo run-in phase, as monotherapy (n = 68) as well as in combination with either atenolol (100 mg/day) (n = 30) or the potassium-sparing diuretic hydrochlorothiazide (50 mg/day) and amiloride (5 mg/day) (n = 26) in 124 patients with essential hypertension, aged 41 to 82 years. With the addition of ketanserin, diastolic blood pressure fell by 8 +/- 8, 8 +/- 8, and 7 +/- 9 (+/- SD) mm Hg, respectively (p less than 0.05 for all) in the three treatment groups; heart rate remained unchanged or fell slightly. Ketanserin had no effect on body weight, or biochemical variables, including total serum cholesterol and triglycerides, with the exception of a minor increase in apolipoprotein B. Using a patient self-assessment questionnaire (30 items), the addition of ketanserin was associated with a reduction of most of the symptoms encountered in the placebo phase, including sleep disturbances, general feeling of weakness, headaches, nervousness, and fatigue, but there was a tendency toward increases in stuffy nose and dry mouth. In patients older than 60 years, the antihypertensive efficacy of ketanserin was greater, with 59% achieving a diastolic pressure less than or equal to 95 mm Hg versus 45% in the younger patients. This age trend also emerged when ketanserin was combined with either atenolol or the diuretic.
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PMID:Antihypertensive efficacy of ketanserin alone or in combination with a beta-blocker or a diuretic: the Swiss Ketanserin Study. 244 58

From a hemodynamic point of view, the calcium antagonists represent an interesting way of treating hypertension, because they reduce total peripheral resistance without compromising cardiac output. Blood flow is also maintained during muscular exercise. Verapamil and diltiazem induce slight reduction in heart rate, but this is compensated by increase in stroke volume. Verapamil and diltiazem also prolong atrioventricular conduction time, in contrast to the dihydropyridines. Most clinical data are available for verapamil, diltiazem, and nifedipine. In patients with mild-to-moderate hypertension, these compounds seem as effective as diuretics and beta-blockers. They do not induce disturbances in glucose metabolism, serum uric acid, or serum potassium, and unwanted disturbances in blood lipids have not been described. The dihydropyridines may safely be combined with beta-blockers, but the combination of either verapamil or diltiazem with a beta-blocker should be avoided (because of the high risk of bradycardia). The calcium antagonists seem particularly useful in patients with the combination of hypertension and angina pectoris or peripheral vascular diseases or chronic obstructive lung diseases or diabetes. They are also effective in hypertensive crises. They may also be tried as a first line drug in patients with mild and moderate essential hypertension, particularly when diuretics or beta-blockers are contraindicated. Temporary side effects due to vasodilatation (headache, flushing, and palpitations) are seen frequently, particularly on the dihydropyridines. Edema is the most frequent serious side effect of the dihydropyridines, and constipation is most common with verapamil. At this point, few long-term data are available and it is not known whether the calcium antagonists will give better or worse results, with respect to morbidity and mortality, than the beta-blockers, diuretics, or other more recent antihypertensive agents.
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PMID:Clinical use of calcium antagonists in hypertension: update 1986. 245 35

The clinical pharmacology of potassium channel openers has been reviewed using pinacidil as a prototype drug. When administered acutely or chronically, the hemodynamic and neuroendocrine profile is that of a peripheral arterial vasodilator. The drug produces decreases in peripheral vascular resistance, and subsequent blood pressure decreases are associated with reflex increments in heart rate. When studied, plasma catecholamines increased about twofold during chronic therapy. Plasma renin activity, however, was not increased during chronic therapy with pinacidil monotherapy. When patients were treated with pinacidil doses ranging from 12.5 to 75 mg b.i.d., 66.9% of patients had a decrease in supine diastolic blood pressure to below 91 mm Hg and 10 mm Hg less than baseline, whereas only 23.9% of patients had similar falls during placebo treatment. During maintenance therapy with pinacidil, the average blood pressure during the daytime dosing interval was 137.8 +/- 1.2/83.4 +/- 0.7 mm Hg (mean +/- SEM). Titration of pinacidil as monotherapy resulted in a characteristic adverse event profile dominated by the presence of dose-related edema. Other characteristic events included tachycardia, palpitations and headache. When pinacidil was given to patients unresponsive to hydrochlorothiazide (25 mg b.i.d.), similar efficacy relative to placebo was noted with a change of post-dose supine diastolic blood pressure in the pinacidil group of 13.5 +/- 0.8 mm Hg and 7.3 +/- 0.9 mm Hg in the placebo group.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Clinical pharmacology of pinacidil, a prototype for drugs that affect potassium channels. 246 78

This study involved 113 patients (mean age 50 +/- 14 years) with diastolic blood pressure above 95 mmHg. The patients abstained from taking any antihypertensive drug and received a placebo for one week before entering felodipine, a new calcium antagonist (5 mg x2/day for 2 weeks, then 10 mg x2/day) or atenolol (100 mg/day). There was no significant difference between the two treatment groups. Atenolol tended to be more effective in young subjects and felodipine in subjects aged 60 years or more. Heart rate was more reduced by atenolol than by felodipine (P less than 0.01). Undesirable side-effects were recorded by means of an open questionnaire. Their incidence was 23 per cent during the week under placebo and 84 per cent and 80 per cent respectively during treatment with felodipine or atenolol. The most frequent side-effects were oedema of the ankles and headache under felodipine, fatigue and headache under atenolol. Alkaline phosphatase levels were higher in the felodipine group (P less than 0.05), and a slight rise in blood potassium level (0.2 mmol/l) was noted in the atenolol group (P = 0.001), but these values remained within normal limits.
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PMID:[Treatment of essential hypertension with felodipine or atenolol as first line therapy. Comparative double-blind randomized study]. 252 34

We performed an epidemiological study on the atrial natriuretic factor pattern in a young population. Subjects were recruited in the Ospedale Militare Principale of Rome among young men liable to conscription, whose hospitalization was due either to essential hypertension or to other pathologies (not influencing our study, such as headache etc.). The recruitment lead to the formation of three different groups: normotensives, normotensives with family history of hypertension (mother and/or father) and hypertensives. On the morning of the study (after 7 days of pharmacological wash-out, under a diet containing 120 mEq of Na+/die), blood samples were taken. Plasma atrial natriuretic factor, renin activity and aldosterone were assayed by RIA. Digoxin-like immunoreactive substance was assayed by a solid-phase radioimmunoassay, following the extraction of plasma. Serum creatinine, sodium, potassium and urinary sodium and potassium (24 h before the study) were assayed by standard methods. Urinary kallikrein was assayed by chromogenic substrate S-2266. So far, we have studied 60 subjects (26 hypertensives, 21 normotensives and 13 normotensives with family history) and we wish to discuss in this article the preliminary results concerning the atrial natriuretic factor and its relationship with renin activity, aldosterone and blood pressure. Our results show that the mean plasma levels of atrial natriuretic factor in the hypertensive group were higher, although not significantly, than those of the other two groups and that the normotensives with family history had slightly higher levels as compared to normotensives (Delta % = + 7.4).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:[Atrial natriuretic factor: an epidemiological study. Preliminary results]. 252 19

The effect of cilazapril, a new inhibitor of angiotensin-converting enzyme, in a dosage of 2.5 or 5 mg once daily, was compared with that of hydrochlorothiazide 25 or 50 mg in 169 patients with mild to moderate hypertension. Blood pressure at entry was 158/103 mm Hg (cilazapril) and 160/103 mm Hg (hydrochlorothiazide). Cilazapril 2.5 mg caused a decrease in blood pressure of 14.7 +/- 2.3/12.6 +/- 1.2 mm Hg compared with a decrease of 12.6 +/- 2.2/10.2 +/- 1.2 mm Hg with hydrochlorothiazide 25 mg. Those patients who required an increase of dosage to the higher level then showed decreases of 15.0 +/- 2.1/14.3 +/- 1.2 (cilazapril) and 19.7 +/- 1.9/13.3 +/- 1.2 hydrochlorothiazide. All decreases in blood pressure were statistically significant but were not statistically different from each other. Fifty-one percent of patients reached a sitting diastolic blood pressure of 90 mm Hg or less receiving 2.5 mg of cilazapril and an additional 28 percent of patients reached this goal receiving 5 mg. The figures for patients receiving hydrochlorothiazide were comparable: 36 and 35 percent. Twenty-one adverse events remotely, possibly, or probably related to therapy were reported with cilazapril and 32 with hydrochlorothiazide. Three patients withdrew from cilazapril because of mild angioedema, headaches, and chest pain, respectively, and three patients withdrew from hydrochlorothiazide treatment because of fatigue, dizziness, and gastric hemorrhage. Hydrochlorothiazide caused a decrease in potassium levels and an increase in levels of cholesterol, uric acid, urea and - gamma cilazapril had no adverse biochemical effects. Cilazapril lowered blood pressure to the same extent as hydrochlorothiazide. Young patients had better responses to cilazapril than to hydrochlorothiazide. It is concluded that cilazapril is an effective and safe drug for patients with mild to moderate hypertension.
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PMID:Efficacy of cilazapril compared with hydrochlorothiazide in the treatment of mild-to-moderate essential hypertension. Multicentre Study Group. 253 59

A method of random sampling was applied to 10 CRI patients to analyze the results of 24 hemodialyses with acetate solution for dialysis (35 mmol/l) and 34 hemodialyses with bicarbonate solution for dialysis (35 mmol/l). Significant reduction of complications like headache, nausea, vomiting, tachycardia, dyspnea, extrasystole was observed in bicarbonate dialysis. The concentration of mean molecular uremic toxins was decreased from 5.75 +/- 0.84 mmol/l in acetate dialysis up to 2.63 +/- 0.21 mmol/l in bicarbonate dialysis. The content of intracellular potassium returned to normal. The concentration of serum cholesterol was decreased from 5.6 +/- 0.4 up to 4.8 +/- 0.2 mmol/l. These data indicated a favorable effect of bicarbonate dialysis on intracellular metabolism. Preliminary data did not confirm the normalizing effect of bicarbonate dialysis on the development of uremic osteopathy.
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PMID:[Bicarbonate hemodialysis in the therapy of chronic kidney failure]. 317 34

Headaches may occur in as many as 25% of hypertensive patients and generally bears little relationship to level of diastolic blood pressure. Previous observations, in normotensive patients, suggested that abnormalities in both potassium and ammonia metabolism might be related to the pathogenesis of these headaches. The present study was undertaken to see whether these factors also occurred in hypertensive patients with headaches. The present observations were made in thirteen hypertensive patients with vascular headaches. The major findings include potassium levels of 3.45 +/- 0.25 mEq/L; CO2, 29.85 +/- 1.21 mEq/L; blood ammonia, 41 +/- 8.40 U mol/L and an alkaline pH of the urine. The blood ammonia levels, when factored by the BUN, yielded elevated ammonia to BUN ratios (3.81 +/- 1.82). These findings are similar to those previously observed in normotensive patients with vascular headaches. The profile of hypokalemia and/or alkalosis, increased blood ammonia to BUN ratios and a relatively alkaline urine appears to be a commonly observed pattern in patients with vascular headaches. These data suggest that a biochemical basis exists for the genesis of vascular headaches in patients with hypertension.
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PMID:The pathogenesis of vascular headaches in patients with hypertension; the role of the ammonia-potassium axis. 364 6


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