Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0027497 (nausea)
23,468 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A large, open, multi-centre study was carried out in general practice to evaluate the effectiveness and tolerance of a combination of 10 mg pindolol plus 5 mg clopamide, in single tablet form, in the treatment of patients with essential hypertension. Computer analysis of the records of 8989 patients who completed the 8-weeks' study period showed that treatment with the combination product, in a dosage of 1 tablet daily in 83% of the patients, resulted in excellent blood pressure control in the majority (75%) of cases, irrespective of age or previous antihypertensive treatment, and was particularly effective in those with mild to moderate hypertension who had previously not received any therapy. Side-effects were generally not troublesome and only 8.3% of patients stopped treatment for this reason. The most commonly reported side-effects were dizziness, nausea, tiredness and headache.
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PMID:A multi-centre general practice trial of a pindolol/clopamide combination ('Viskaldix') in essential hypertension. 39 10

1. One hundred patients with severe essential hypertension have been treated with minoxidil for a mean period of 8-4 months in a study involving eleven European centres. Seventy-two males and twenty-eight females were included in the group; the mean age was 55 years and the initial supine systolic and diastolic pressures averaged 212 (range 150-270) and 125 (range 90-150) mmHg respectively. 2. Reduction of supine diastolic pressure to less than 100 mmHg occurred in 94% of patients within 4 weeks. After the average follow-up period of 8-4 months the mean pressures were 151/91 mmHg. Concomitant therapy with beta-receptor-blocking agents and diuretics resulted in satisfactory control of heart rate and weight gain. 3. Side effects included increased hair growth, nausea, fatigue, rash and darkening of the skin. ECG showed mainly T-wave changes and echocardiographic examination indicated improved ventricular emptying.
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PMID:The use of minoxidil in the treatment of severe essential hypertension: a report on 100 patients. 107 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

Cilazapril is a new once-daily angiotensin-converting (ACE) enzyme inhibitor which has been administered to 4,500 patients with mainly mild to moderate essential hypertension in a multinational clinical research program. Sitting diastolic blood pressure was reduced by about 9 mm Hg from baseline (p less than 0.01) after 4 weeks of treatment with cilazapril 1.25-10 mg/day in double-blind placebo-controlled studies. Total responder rates to cilazapril were usually 50-60% compared with 30% to placebo. Adding hydrochlorothiazide 12.5 mg/day to cilazapril 5.0 mg/day increased the total responder rate from 52 to 71%. Double-blind dose titration studies for 8 weeks showed that cilazapril 2.5-5 mg/day possessed equivalent efficacy to usual therapeutic regimens of sustained release propranolol, captopril, hydrochlorothiazide, atenolol and enalapril, Cilazapril did not affect heart rate. During long-term open administration for 52 weeks, or longer, cilazapril, either alone or in combination with hydrochlorothiazide, effectively maintained control of blood pressure. Treatment of patients with severe hypertension with cilazapril plus hydrochlorothiazide achieved a total responder rate of 73%. Adverse events were mostly observed within the first 8-16 weeks of treatment, with headache, dizziness, fatigue, nausea, cough and chest pain being the most frequent. Non-life-threatening angioedema, facial edema and mild hypotension occurred in less than or equal to 0.2% of patients, and orthostatic hypotension was reported in 2%. Abnormal laboratory test values were rarely found with cilazapril treatment. Of the 2.3% of patients with elevated serum creatinine, at any time point during the study and irrespective of outcome on continuation with cilazapril therapy, about two thirds had prior renal impairment.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Cilazapril: an overview of its efficacy and safety in hypertension. 153 34

A total of 555 hypertensive patients took part in a 2-year multicenter, open-label study to determine the efficacy, tolerance, and safety of long-term therapy with ramipril. In the beginning, all patients were to receive 5 mg of ramipril/day. The dosage was then adjusted in accordance with response to treatment and ranged from 1.25-20 mg of ramipril daily. Of these patients, 129 also received 25 mg of hydrochlorothiazide daily at some point during the trial. To evaluate whether tolerance to ramipril developed during long-term treatment, a subgroup of 202 patients was analyzed for efficacy maintenance. Prior to enrolling in the 2-year study, these patients had received ramipril monotherapy in a short-term, double-blind study and had been classified as responders, i.e., their diastolic blood pressure had been maintained at less than or equal to 90 mm Hg. At the end of 104 weeks of treatment, 45.9% of patients were on 2.5 mg of ramipril alone and 43.6% were on 5 mg of ramipril alone. Only four patients required the addition of 25 mg of hydrochlorothiazide. No clinically important changes occurred, and kidney function was well maintained. The most frequently reported adverse events excluding intercurrent illnesses were dizziness/vertigo (6%), asthenia (4%), nausea (3%), headache (2%), and abdominal pain, gastrointestinal disorder, rash, and increased cough (1% each). Ramipril was safe, effective, and well tolerated in the long-term treatment of patients with mild-to-moderate essential hypertension.
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PMID:Antihypertensive efficacy, tolerance, and safety of long-term treatment with ramipril in patients with mild-to-moderate essential hypertension. 172 24

Delapril, a new angiotensin converting enzyme (ACE) inhibitor discovered in the laboratory of Takeda Chemical Industries, Ltd., is the result of drug design based on the structure-activity relationships of ACE inhibitors. Delapril is an antihypertensive agent with a relatively long duration of action and no SH moiety in its structure. Following administration, it is converted into two active metabolites. Delapril effectively lowered blood pressure in 73% of 1,008 patients with hypertension during clinical trials in Japan. Efficacy rates were 73% for essential hypertension, 85% for renal hypertension, and 80% for renovascular hypertension. Excellent hypotensive response was observed in all age groups, from young to elderly patients. Side effects during administration of delapril, based on subjective evidence, were reported in 80 out of the 1,008 cases (7.9%). The main symptoms included orthostatic dizziness (1.7%), dizziness (1.3%), and nausea (1.1%). Dry cough, which has attracted attention in recent years as a side effect of ACE inhibitors, was reported at a low incidence of 1.1%. In a double-blind, controlled study in patients with mild to moderate essential hypertension in which captopril served as a positive control, delapril showed superior hypotensive effect and greater safety. Data derived from the Japan Study Group on Delapril indicate that this ACE inhibitor has excellent hypotensive effects and a high level of safety. It is suitable as a first-line drug in both monotherapy and combined therapy.
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PMID:Clinical evaluation of delapril in Japan. Report from the Japan Study Group on Delapril. 200 47

The efficacy, tolerability and safety of dilevalol in essential hypertension has been documented in an international clinical trials programme which was conducted with doses up to 1600mg daily. Initial double-blind trials confirmed the superiority of dilevalol over placebo in essential hypertensive patients and documented the suitability of a once-daily dosage. Almost all of the subsequent trials have been randomised, double-blind comparative trials of dilevalol versus established anti-hypertensive agents with the duration of treatment ranging from four weeks up to one year. The recommended dosage range of dilevalol, of 200-400 mg once-daily, has generally been shown to be at least as effective at lowering raised blood pressure as established antihypertensive agents given according to their recommended doses. In one study in elderly hypertensives, dilevalol was significantly more effective than atenolol in lowering systolic blood pressure. Safety data is available from a consolidated database of 2011 dilevalol-treated patients representing over 500 patient-years exposure. Overall, dilevalol was well tolerated and evidence of dose-related adverse effects became apparent only for nausea and dizziness above the recommended dose range. The most common adverse effects considered probably or definitely related to treatment were fatigue (2.5%), nausea (1.9%), headache (1.8%) and dizziness (1.7%). 'Typical' beta-blocker adverse effects were observed, though many of these effects were less frequent than seen with comparator beta-blockers. Evidence of excessive vasodilation was rarely found, consistent with the counter-balancing effect of beta-blockade.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Overview of clinical trials of dilevalol in essential hypertension. 214 8

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 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, diphoresis and restlessness. In hypertensive patients blood pressure responses are complex and are influenced to some extent by secretion. PGI2 stimulates renin secretion by a direct effect on the juxtaglomerular apparatus, and 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 larger 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 defective. Some drugs (cicletanine, thiazides, propranolol) have been shown to stimulate PGI2 synthesis, and inhibition of cyclooxygenase has been shown to abolish their antihypertensive effects. Whether stimulation of PGI2 synthesis affects the antihypertensive efficacy of these drugs is not yet known.
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PMID:Prostacyclin in hypertension. 225 88

In this multicentre controlled single blind trial the effectiveness and safety of cicletanine (100 mg/day) were compared with those of enalapril (20 mg/day) and of the combination of both drugs in the same doses in 72 patients (41 men, 31 women, mean age 64.1 +/- 8.3 years) with permanent moderate essential hypertension without severe cardiovascular complications. In the course of the trial, one patient in each of the three therapeutic groups was excluded either for insufficient effectiveness in monotherapy or for photosensitization under the combined treatment. After two months of treatment, the fall in blood pressure and the number of patients with normalized BP were similar in the groups treated with cicletanine or enalapril alone. In contrast, the cicletanine-enalapril combination produced a significantly greater fall of diastolic arterial pressure than cicletanine alone. In addition, there was a greater reduction of functional symptoms associated with arterial hypertension. Apart from the lone case of photosensitization observed with the combined treatment, only minor side-effects were encountered, including an episode of diarrhoea and a case of extrasystoles with the combination, and a case or nausea with lipothymia under cicletanine alone. There were no significant variations of biochemical values.
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PMID:[Evaluation of the effectiveness of a cicletanine-enalapril combination in hypertensive patients]. 255 22

In a multicentre open trial involving 229 investigators, cicletanine, a new antihypertensive agent, was administered orally in doses of 50 to 100 mg/day either alone (1,238 patients) or combined with another drug (430 patients). In this second group of patients with essential hypertension whose BP had not been normalized by a beta-blocker (n = 157), a calcium inhibitor (n = 67), an angiotensin-converting enzyme inhibitor (n = 134) or an alpha-blocker (n = 7), cicletanine normalized BP (less than 160/95 mmHg) in 48.8% of the patients and significantly lowered BP values which fell from 177.7 +/- 15.9/103.3 +/- 6.3 mmHg to 157.2 +/- 17.6/88.8 +/- 8.7 mmHg. The addition of cicletanine to treatments with beta-blockers, calcium inhibitors and angiotensin-converting enzyme inhibitors normalized BP in 48%, 52% and 47% of patients respectively. A significant reduction of symptoms was noted, notably as regards headache, dizziness, palpitations, lower limb oedema, asthenia, auditory disorders and dyspnoea. The side-effects reported (headache, dizziness, gastralgia, nausea, pruritus) were minor and non-specific; they accounted for the withdrawal of only 8 patients. The only significant, though moderate, biochemical variations observed were decreases in natremia and cholesterolaemia unconfirmed by qualitative analysis. Altogether, cicletanine proved to be effective and well tolerated when administered in combination with other antihypertensive drugs belonging to three main therapeutic classes.
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PMID:[Antihypertensive effectiveness and tolerance of cicletanine. Results obtained with bitherapy]. 257 67


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