Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0020538 (hypertension)
 170,190 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Fifty-five patients with mild to moderately severe essential hypertension were treated with guanabenz (2, 6-dichlorobenzylidene aminoguanidine acetate) in doses from 4 to 16 mg twice daily in a randomized, placebo-controlled study. The patients treated with placebo in the initial phase of the study were subsequently treated with guanabenz. The mean arterial pressure in the guanabenz group decreased from 130.6 to 107.6; that in the placebo group decreased from 129.6 to 126.6 standing and from 126.6 tp 109.9 and 128.8 to 120.5, respectively, supine. The principle adverse effects included sedation, dry mouth, weakness, and tiredness. Of the guanabenz-treated patients 84% had sustained decrease in supine diastolic blood pressure of 10 mm Hg or more, whereas in the placebo-treated patients only 32% had such a response. There was no significant orthostatic hypotension. Guanabenz thus appears to be an effective antihypertensive drug in patients with mild to moderately severe hypertension.
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PMID:Guanabenz in essential hypertension. 31 38

The peripheral decarboxylase inhibitor carbidopa, given (100 mg/day) for 6 wk in a double-blind trial, lowered supine diastolic pressure of 10 patients with essential hypertension treated with alpha methyldopa by a small (6 mm Hg) but significant (p less than 0.05) amount. Large doses of benserazide (1.5 gm) did not modify the hypotensive effect of 1.0 gm of alpha methyldopa in untreated hypertension but significantly reduced the central nervous side effects of sedation and dry mouth. These studies indicate that extensive peripheral decarboxylation is not necessary for alpha methyldopa to lower blood pressure and would be compatible with the central nervous site of hypotensive action of this drug.
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PMID:Clinical and cardiovascular effects of alpha methyldopa in combination with decarboxylase inhibitors. 32 21

A New Antihypertensive of the Imidazoline Series: 5-Fluoro-2-methyl-imidazolidinylidene-benzamine-monohydrochloride. 5-Fluoro-2-methyl-imidazolidinylidene-benzamine-hydrochloride (flutonidin, ST 600), a new antihypertensive imidazoline compound, was tested over 3 weeks in 20 patients with moderate to severe hypertension. Blood pressure was significantly lowered in both supine and upright position. In nearly 2/3 of the patients treated normalization of blood pressure was achieved. Side effects like sedation, dry mouth or orthostatic complaints were present in 30%. Toxic effects were not registered. It is recommended to reduce the dosage slowly especially in the aged to prevent, in part severe findings after abrupt withdrawal.
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PMID:[New antihypertensive agent of the imidazoline series: 5-fluoro-methyl-imidazolidinylidene-benzamine-monohydrochloride (flutonidin)]. 33 88

Fourty-six men and 6 women aged 45 years and having arterial hypertension newly diagnosed at routine medical examinations were given out-patient antihypertensive treatment with prazosin, prazosin + hydrochlorothiazide, or prazosin + hydrochlorothiazide + clonidine. The mean values of blood pressure after the 3-week placebo period were 157/109 mmHg in the supine and 160/115 mmHg in the standing position. Treatment with prazosin (1--2 mg t.i.d.) produced normotension in 4/52 patients only, yet supine diastolic blood pressure and standing blood pressure were significantly lowered within 9 weeks. The addition of hydrochlorothiazide (25 mg daily) for 3 weeks to the regimen led to normotension in 12/46 patients. The remaining 34 patients still having an average supine blood pressure of 152/106 mmHg after prazosin + hydrochlorothiazide, responded well to low doses of clonidine added for 6 weeks to the treatment. Only 7 patients having initially high blood pressure still had a diastolic blood pressure greater than or equal to 100 mmHg at the end of the trial. The subjective side-effects were frequent but mild being roughly similar during placebo and active drug periods, except that fatigue and dry mouth due to clonidine were common, yet tolerable. No "first tablet reactions" to low inital doses of prazosin were found.
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PMID:Antihypertensive drug combinations: prazosin, hydrochlorothiazide and clonidine. 35 19

Among the newer antihypertensive agents are the beta-blocking drugs, such as propranolol. These agents are useful as second-step drugs to be used if diuretic therapy alone is not effective. In mild to moderately severe hypertension, propranolol, in does of up to 480 mg/day in combination with a thiazide diuretic, has been found to be effective in over 80% of patients on long-term therapy. This degree of response is essentially similar to that noted with a combination of reserpine and a diuretic agent. Although some observers believe that propranolol produces many fewer side effects than the other step 2 drugs (reserpine and alpha-methyldopa), there are some patients who do experience restlessness, insomnia, and depression. Clonidine may be substituted for another step 2 drug, is of moderate potency, but may not be tolerated by a large number of patients because of the severe dry mouth and drowsiness that it produces. Prazosin appears to be a suitable substitute for hydralazine as an effective vasodialator if thiazides plus propranolol or thiazides plus reserpine or alpha-methyldopa are not effective. In some instances, it many be an acceptable second-step drug because of its alpha-adrenoreceptor-blocking properties. The angiotensin II competitive inhibitors or converting enzyme inhibitors may in the future have some place in the management of hypertension.
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PMID:Propranolol and newer antihypertensive drugs in the management of hypertension. 42 60

11 coronary patients, 8 with mild hypertension, were treated with clonidine, at a dose of 75 micrograms b.i.d. per os for a week. The effect of the drug on coronary heart disease was assessed by means of a symptom-limited multistage exercise test on the cycloergometer. Clonidine was effective in reducing the exercise-induced increases in blood pressure (by 15.5 +/- 6.1%), the double product (by 34.8 +/- 20.8%) and the electrocardiographic ischemic changes. In 2/4 patients, effort related ventricular extrasystoles were reduced by greater than 50% after clonidine. The drug worsened the anginal pain in 3 and relieved the pain in 3 patients. However, it reduced the exercise-induced ST-T segment downsloping in 7 patients. The tolerance was good, since only 3/11 patients reported slight dry mouth, sedation and pyrosis. In view of the electrocardiographic effect, further studies with clonidine on myocardial ischemia should be performed.
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PMID:The therapeutic value of clonidine in patients with coronary heart disease. 49 82

The demonstration that long-term administration of relatively low doses of clonidine decreased the responsiveness of blood vessels to vasodilator and vasoconstrictor drugs in animals led to its investigation in the prevention of migraine in man. Results of placebo-controlled and open therapeutic trials have shown that clonidine in low dosages (75 to 150 mug daily) is useful in preventing migraine headaches in about 30%-50% of patients. A 50% or greater reduction in headache frequency or headache indices has been reported in 40% of patients in controlled and open studies. Thus clonidine, like other drugs used in the interval therapy of migraine, can be expected to be effective in only a proportion of patients. Although clonidine has not been compared directly with other drugs used in the prophylactic treatment of migraine, the general clinical impression is that it is less effective then pizotifen or methysergide. Because it is relatively well tolerated at dosages of 75 to 150 mug daily it is worthy of a trial, particularly in patients considered to need prophylactic migraine therapy for the first time, and when migraine occurs in association with hypertension. At the dosages used in migraine prophylaxis, which are almost invariably lower than used in hypertension, clonidine does not cause hypotension and can be used in patients with cardiovascular disease. The principal side-effects are drowsiness and dry mouth which tend to diminish as treatment continues.
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PMID:Low-dose clonidine: a review of its therapeutic efficacy in migraine prophylaxis. 120 7

At their first visit to a hospital clinic 178 patients referred with a diagnosis of hypertension were given a self-administered questionnaire. They received a similar questionnaire 12 months later. Of the 178 patients 99 were not initially on treatment. Similarly 78 normotensive subjects were drawn randomly from the local population and sent a second questionnaire 10 months later. The symptoms at the first visit of the normotensive controls, the untreated hypertensive patients, and 477 patients on long-term treatment in the hypertension clinic were compared. Treated and untreated hypertensive patients complained more of nocturia and also of unsteadiness either on standing or in the morning. Treated hypertensives complained more of sleepiness, dry mouth, diarrhoea, and, in men, impotence and failure of ejaculation. Similarly, untreated hypertensives complained of excessive depression, blurred vision, and waking headache. Fifty-five of the normotensive subjects and 110 of the newly referred hypertensive patients responded to the second questionnaire. The proportions losing and gaining symptoms were calculated together with the proportions always complaining and never complaining of a symptom. Hypertensive patients tended to lose the complaints of unsteadiness and headache but to gain the symptoms of vivid dreams, a slow walking pace, and diarrhoea. The net improvement for a symptom was defined as the excess of patients who lost a symptom over those who gained the symptom, expressed as a percentage. Over the follow-up period the control subjects had a net improvement averaged over 14 symptoms of +2-4 per cent. A similar result was obtained for the hypertensive patients of +2-0 per cent, the symptoms lost being balanced by those gained. The changes in symptoms with time were related to the changes in blood pressure and it is suggested that only headache, 'unsteadiness, lightheadedness, or faintness' and nocturia can actually result from raised blood pressure and then only in a proportion of patients complaining of these symptoms.
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PMID:Change in symptoms of hypertensive patients after referral to hospital clinic. 125 26

Interest in centrally acting antihypertensive agents has recently been renewed with the development of drugs that are associated with fewer central adverse effects (e.g. sedation, dry mouth) than the older drugs in this class. Moxonidine reduces sympathetic outflow and hence lowers blood pressure through stimulation of central imidazoline receptors. Blood pressure is decreased by 10 to 20% during moxonidine treatment, with about 70% of patients with mild to moderate hypertension achieving a diastolic pressure of < 90mm Hg. The relatively few published comparative studies demonstrate that moxonidine has efficacy comparable with that of clonidine, prazosin, atenolol, nifedipine, captopril and hydrochlorothiazide. It is at least as well tolerated as these agents in trials and, importantly, appears to cause less sedation and dry mouth than clonidine. Compliance may be aided by the once- or twice-daily administration schedule with moxonidine, and dosage adjustment is only necessary in patients with moderate renal impairment. While its published clinical data base needs further expanding, moxonidine thus appears to be a more attractive option than oral clonidine, and may be considered along with the other classes of drug used to treat patients with mild to moderate hypertension.
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PMID:Moxonidine. A review of its pharmacology, and therapeutic use in essential hypertension. 128 69

Rilmenidine (RIL) is a novel antihypertensive drug selectively acting at the sites of imidazoline receptors. Compared with diuretics, beta-blockers, Ca2+ antagonists and angiotensin converting enzyme inhibitors, the four major groups recommended by the US Joint National Committee as first-line antihypertensive drugs, RIL appears to meet the same criteria of efficacy, safety, and acceptability. Rilmenidine dose-dependently decreases blood pressure (BP), acting as a vasodilator by decreasing vascular resistance through inhibition of the adrenergic nervous system, even while the BP changes due to standing and exercise. In comparison with placebo, RIL significantly decreased BP. In double-blind comparative trials versus first-line diuretics and beta-blockers, RIL normalized BP in approximately 60% patients, showing a similar efficacy to other drugs. In contrast with hydrochlorothiazide, RIL decreased total cholesterol and did not change plasma potassium levels. No tachyphylaxis was observed during long-term treatment. Central side effects, which have contributed to the limitation of the use of alpha 2-agonists as second- or third-line therapy for hypertension, were significantly less frequent with RIL than with clonidine or methyldopa. Indeed, the incidence of dry mouth and drowsiness during double-blind comparative trials versus clonidine and methyldopa was significantly lower with RIL. This absence of central side-effects was confirmed in double-blind comparative trials versus hydrochlorothiazide and atenolol. In contrast with clonidine, no sodium retention or weight gain were observed during chronic treatment with RIL.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Rilmenidine: a novel approach to first-line treatment of hypertension. 135 Jul 33


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