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Query: UMLS:C0020538 (hypertension)
 170,190 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The results of the treatment of 28 patients with mild to moderate hypertension using guanfacin (Estulic) monotherapy and of 24 patients receiving combined antihypertensive therapy containing Estulic are reported on. The blood pressure was lowered and stabilized during the first month of therapy. No addiction or loss in effectivity was seen. There were no changes in ECG or laboratory results during the mean follow up time of 11 months. Four patients discontinued the drug because of subjective side-effects. The single daily dose, the reliable effectivity, the safety of the drug makes it an important antihypertensive drug in general practice.
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PMID:Estulic--a well tolerated and effective antihypertensive drug in general practice. 146 81

The antihypertensive effect of Estulic has been examined over a 12-month period in 101 hypertensive patients. Estulic tablet proved to be effective in form of monotherapy especially in the treatment of mild hypertension, in form of combination therapy in hypertension of medium severity. Using Estulic the number and doses, of the formerly administrated drugs could be reduced. The blood pressure of the patients was stabilized on a significantly lower level, changes in the laboratory parameters were not observed. In 60% of the patients improvement of the subjective complaints was observed. On the basis of the examinations guanfacin proved to be an effective drug in the treatment of hypertension of different severity degrees due to its favourable antihypertensive action, few side-effects, and the possibility of drug administration in daily single doses.
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PMID:Estulic monotherapy and combined antihypertensive therapy. 194 83

30 patients with hypertension and diabetes mellitus type II were treated with guanfacine (Estulic--"Sandoz" Switzerland) 1 mg tablets in the course of 6 months. The trial began with a placebo period at the end of which the patients were classified into groups: I groups--mild hypertension--14 patients, II group--moderate hypertension--8 patients and III group--severe hypertension - 8 patients. The treatment began in all patients with 0.5 mg Estulic once a day in the evening. According to the effect the dose was increased in one week intervals to 1, 2 and 3 mg daily. A very good effect was achieved in 24 patients (80%), good effect--in 3 patients (10%). There was no effect in 3 patients (10%) with diastolic pressure at the end of the placebo period of 15.3 kP (115 mm Hg). The drug Estulic did not deteriorate the glucose tolerance and in 22 patients (73.3%) a decrease of the blood sugar levels with mean 3.47-1.98 mmol/l was found.
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PMID:[Guanfacine in the treatment of arterial hypertension in diabetics]. 209 82

The observations of a 16-week Tensiomin therapy of 10 hypertensive patients treated with hemodialysis have been discussed. The patients have been treated for about 5 years with hemodialysis, suffered from anuria and required besides systhematical ultrafiltration a combination antihypertensive therapy. Tensiomin was combined with Minipress, Trasicor, Depressan, Estulic and Corinfar by using three- or four-drug combinations. In the course of the administration of Tensiomin the doses of the other antihypertensive drugs could be decreased by 50% on average, while the blood pressure of the patients was normalized. By controlling the patients on weeks 1, 4, 12 and 16 of therapy toxic side-effects or notable pathological changes of the examined laboratory parameters (WBC, serum total protein, Na, K, Ca, P, bilirubin, blood sugar and SGOT values) were not seen. It has been concluded that Tensiomin is an effective drug in combination therapy applied for normalizing the hypertension of dialysed patients.
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PMID:Use of tensiomin (captopril) in the antihypertensive treatment of haemodialysis patients. 219 78

The authors assessed the antihypertensive effect of guanfacine (Estulic Sandoz) in 28 stage II hypertensive patients with a pronounced pressure response to the isometric test. Over a period of 4.3 months on the average, they managed to normalise both resting and exercise blood pressure in 89% of subjects. In another study, the authors administered guanfacine to 30 I- and II- type diabetics with essential, primarily stage I, hypertension. Over an average of 6 months, blood pressure normalised in 81% and, when using a guanfacine-saluretic combination, in additional 11%, that is, in a total of 92% of patients. It has been demonstrated that guanfacine has no adverse metabolic action. By contrast, the level of compensation of diabetes mellitus improved allowing 50% of patients to decrease their doses of oral antidiabetic drugs and insulin as well. The authors believe that, in diabetics with hypertension, guanfacine can be rightly regarded as the drug of first choice since it is effective in single-drug therapy and can be used with advantage in patients with whatever complication of diabetes mellitus.
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PMID:Guanfacine in the treatment of hypertensives with a pronounced response to exercise and diabetes mellitus. 331 48

The paper offers therapeutic experience with guanfacine (Estulic Sandoz) in large and small doses in patients with hypertension. A daily dose of 3-4 mg of guanfacine led to a decrease in blood pressure in about half of patients with moderate to severe hypertension. However, therapy had to be discontinued in several instances due to frequent occurrence of adverse side effects. The recently recommended smaller doses (2 x 1 mg) of guanfacine indicated primarily in patients with renal dysfunction or diabetes mellitus resulted in an extremely good therapeutic response; the frequency of undesirable effects was about the same as with other antihypertensive therapeutic protocols. The drug seems to offer more benefits in special indications with a concomitant disease rather than as a third drug of a combination used in severe hypertension.
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PMID:Small and large doses of guanfacine (Estulic Sandoz) in the treatment of hypertension. 331 49

The pharmacology of central alpha-adrenoceptor-stimulating agents is discussed, with particular reference to clonidine (Catapres; Boehringer Ingelheim) and guanfacine (Estulic; Sandoz), and their haemodynamic effects are compared and contrasted. The main differences between the effects of clonidine and guanfacine on hypertension are: guanfacine activates presynaptic alpha-adrenoceptors 10 times more selectively than clonidine; guanfacine has an alpha 2/alpha 1-selectivity ration 25 times higher than clonidine; clonidine decreases cardiac output and guanfacine decreases peripheral resistance, clonidine has no effect on stroke volume but guanfacine increases it; and when the clonidine withdrawal syndrome in the spontaneously hypertensive rat is compared with cessation of guanfacine treatment at an equipotent antihypertensive dose, the withdrawal syndrome after guanfacine appears later and is much less severe. Guanfacine may be preferable to clonidine as a central alpha-adrenoceptor stimulant in the treatment of hypertension.
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PMID:Clonidine and guanfacine--comparison of their effects on haemodynamics in hypertension. 388 93

Clonidine (Catapres, Catapresan), guanfacine (Estulic), and methyldopa (Aldomet) are the prototypes of centrally acting antihypertensive drugs. Clonidine and guanfacine are lipophilic drugs that readily penetrate into the brain, where they stimulate alpha-adrenergic receptors in the pontomedullary region. The stimulation of these central alpha-adrenergic receptors has been shown to activate an inhibiting neuron, which causes a reduction of peripheral sympathetic tone and a subsequent fall in arterial blood pressure and heart rate. Both a centrally initiated reduction of vagus reflex activity and the activation of presynaptic alpha 2-adrenergic blocking agents in the heart may contribute to the bradycardia. Studies indicate that methyldopa also penetrates into the brain, where it is converted into alpha-methylnorepinephrine. This amine may stimulate the same central alpha-adrenergic receptors as those activated by clonidine, which will result in a hypotensive effect. Possibly, alpha-methyldopamine might also play a role. Accordingly, the modes of action of clonidine and alpha-methyldopa probably are very similar at a basic level. The central adrenergic receptors probably are located postsynaptically. Their receptor demand corresponds more closely to that of the alpha 2-subtype. Central alpha 1-adrenergic receptors might possibly play a part in the modulation of vagally induced baroreflex bradycardia. A discussion on the pharmacological basis of the side effects of the centrally acting antihypertensives has been limited to those adverse reactions that are somehow related to alpha-adrenergic receptors. Sedation, a common side effect, appears to be mediated by central alpha 2-adrenergic receptors, at least in animal models.(ABSTRACT TRUNCATED AT 250 WORDS)
Hypertension
PMID:The hypotensive activity and side effects of methyldopa, clonidine, and guanfacine. 609 46

Estulic (guanfacine), a new centrally acting antihypertensive agent derived from guanidine, was administered to 13 patients with established essential hypertension. Therapeutic effect and safety were evaluated in all patients during the first year. Blood pressure normalization was elicited in 6 patients and a good therapeutic response in 5. Two patients did not respond to the monotherapy. Dryness of the mouth was observed in 11 patients during the first year and tiredness in 4. At the end of the first year, 3 patients out of 7 who completed the 1-year treatment still complained of dry mouth. Five patients continued for a second year of treatment. In all of them the blood pressure was normalized and only one patient suffered from dryness of the mouth. Estulic was usually given once daily in the evening; in some patients it was given twice daily. At the end of the first year, doses between 2 and 7 mg were used (mean 3.4 mg); during the second year 2 mg/day was administered to 2 patients, 3 mg/day to 2 patients and 5 mg to 1 patient. No impairment of laboratory values was seen during long-term treatment. In one patient with renal insufficiency the treatment had to be discontinued owing to deterioration of the underlying disease. After withdrawal of the drug, no rebound hypertension was observed.
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PMID:[Estulic in the long-term treatment of hypertension]. 678 68

1. The antihypertensive effect and side-effects of the new centrally acting agent guanfacine (BS 100-141, Estulic) and guanethidine (Ismelin) were compared in a single-blind, cross-over study. The study consisted of two active treatment periods of 6 weeks each, both preceded by a 1-3 weeks placebo period. 2. Sixteen ambulant patients (six male, ten female) with mild or moderate hypertension were admitted to the study. The patients were also receiving diuretic therapy (clopamide 10-20 mg daily). On average the optimal daily dose of guanfacine was 3 mg and of guanethidine 20 mg. 3. An equally large and significant decrease in blood pressure was produced by both drugs. Both guanfacine and guanethidine caused a very slight reduction in heart rate. Mild orthostatic hypotension occurred in 11 patients during guanethidine therapy. Dryness of the mouth occurred in 13 patients taking guanfacine.
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PMID:Comparative study of two antihypertensive agents: guanfacine and guanethidine. 699 86


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