Haemodynamic effects of guanfacine.

Magometschnigg, D; Hitzenberger, G; Bonelli, J

doi:10.1111/j.1365-2125.1980.tb04919.x

Cited by 10 publications

(8 citation statements)

References 3 publications

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“…Its long elimination half-life, shown to be over 17 h in pharmacokinetic studies in animals, nonmotensive volunteers and hypertensive patients (Kiechel, 1980;Kirch, 1980) and its long duration of action make guanfacine suitable for twice daily or even once daily dosing, as confirmed by the results of short-term clinical trials (Reid & Zamboulis, 1980;Magometschnigg, Hitzenberger & Bonelli, 1980). This multicentre study was designed to establish the usefulness of guanfacine for long-term treatment of all forms and stages of hypertension in routine practice, with special regard to the following questions:…”

Section: Introductionmentioning

confidence: 78%

“…hospitalized and ambulatory hypertensives has been recorded in a large number of controlled clinical trials THE antihypertensive efficacy of guanfacine (Estulic , (Jiattela, 1976a;1976b;Dubach, Huwyler, Sandoz clinical code BS 100-141, Lon 0798) in Radielovic & Singeisen, 1977;Esch, 1976 Sabel & Heidland, 1978;Kirch & Distler, 1978;Seedat, 1978;Lochaya, Thongmitr & Suvachittannont 1979). Its long elimination half-life, shown to be over 17 h in pharmacokinetic studies in animals, nonmotensive volunteers and hypertensive patients (Kiechel, 1980;Kirch, 1980) and its long duration of action make guanfacine suitable for twice daily or even once daily dosing, as confirmed by the results of short-term clinical trials (Reid & Zamboulis, 1980;Magometschnigg, Hitzenberger & Bonelli, 1980). This multicentre study was designed to establish the usefulness of guanfacine for long-term treatment of all forms and stages of hypertension in routine practice, with special regard to the following questions:…”

Section: Introductionmentioning

confidence: 96%

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Clinical experience with guanfacine in long‐term treatment of hypertension.

Jerie¹

1980

Brit J Clinical Pharma

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1 Of 662 hypertensive patients originally selected for long-term treatment, 580 were evaluated after one year and 169 continued for a second year of treatment with guanfacine.2 There were 257 women (mean age 52.1 yr) and 323 men (mean age 51.7 yr) in the trial: 499 (86%) suffered from essential, 55 (9%) from renal, 22 (4%) from renovascular and 4 (1%) from other forms of hypertension; 200 (34%) were classified as having mild, 275 (47.5%) moderate and 101 (17.5%) severe hypertension. In four patients the degree of severity was not specified. Nearly 40% of all patients had signs of left ventricular hypertrophy, and in 71% a pathological ocular fundus was found; 72% had been pretreated with antihypertensive drugs, 56% suffered from a concomitant disease and 18% had signs of heart failure; 224 patients were classified as having a sedentary mode of life, 316 were moderate and 27 heavy physical workers. In 13 no classification was given. 3 Whenever possible, a wash-out period of 3 weeks with a placebo identical in appearance with the active drug was carried out at the beginning and at the end of the 12-month treatment period to establish the pretreatment blood pressure and the possible withdrawal phenomena after therapy discontinuation. At the beginning, two doses of guanfacine 1 mg were administered daily and the dose was successively increased. A diuretic was added if necessary. To non-responders, a /3-adrenoceptor-blocker or a vasodilator was given. 4 In all trial groups a statistically significant decrease in blood pressure was found. The average reduction in mean arterial pressure was 16% at the end of the first year and 17% at the end of the second year. Normalization of blood pressure was achieved in 54% of the patients at the end of the first year and in 66% after the second year of treatment.5 In patients with hypertension of a higher degree of severity, combined treatment was used more often and higher doses of guanfacine were administered; monotherapy was used predominantly in patients with mild to moderate hypertension. 6 The mean daily dose of guanfacine at the end of the first year was 3.4 mg for monotherapy and 6 mg for combined treatment. After 2 yr, these values were 3.2 mg and 5 mg, respectively. 7 With the once-daily and twice-daily dosage schedules the same antihypertensive effect as with the three times daily dose regimen was observed, with a higher normalization rate and fewer sideeffects. Moreover, the normalization rate was higher with doses up to 3 mg than with doses in the range 4-25 mg. This applied to both monotherapy and combined treatment. 8 It is suggested that low doses of guanfacine are more suitable for the treatment of patients with established but uncomplicated hypertension, because of the lack of peripheral z-mimetic effects is the lower dose range. In view of the relatively long half-life of guanfacine, it is recommended that the drug be given only once daily or at the most twice daily. 9 The ECG analysis after one year of treatment revealed signs of regression in left-ventricul...

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Section: Introductionmentioning

confidence: 78%

Section: Introductionmentioning

confidence: 96%

Clinical experience with guanfacine in long‐term treatment of hypertension.

Jerie¹

1980

Brit J Clinical Pharma

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“…Steady‐state blood levels are achieved within 4 days in most patients. In contrast to clonidine, studies in hypertensive patients have suggested that guanfacine reduces BP mainly by reducing total vascular resistance rather than cardiac output 19,20 . Guanfacine reduces resting heart rate with minimal effect on heart rate during exercise 19 .…”

Section: Guanfacinementioning

confidence: 99%

“…In contrast to clonidine, studies in hypertensive patients have suggested that guanfacine reduces BP mainly by reducing total vascular resistance rather than cardiac output 19,20 . Guanfacine reduces resting heart rate with minimal effect on heart rate during exercise 19 . In contrast, guanfacine reduces TPR similarly both at rest and during exercise with minimal effects on cardiac output 19 .…”

Section: Guanfacinementioning

confidence: 99%

Central Sympatholytic Drugs

Vongpatanasin

Kario

Atlas

et al. 2011

The Journal of Clinical Hypertension

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J Clin Hypertens (Greenwich). 2011;13:658–661. ©2011 Wiley Periodicals, Inc. Key Points Central sympatholytic drugs reduce blood pressure mainly by stimulating central α2‐adrenergic receptors in the brainstem centers, thereby reducing sympathetic nerve activity and neuronal release of norepinephrine to the heart and peripheral circulation. This class of drugs, however, is currently used mainly as fourth‐line (or beyond) drug therapy for hypertension because of side effects of drowsiness, fatigue, and dry mouth. Rebound hypertension is also another major concern in certain drugs with a short half‐life, particularly in patients who are nonadherent to the regimen. Therefore, their use on a “PRN” basis for treatment of blood pressure surge in the absence of symptoms or acute target complications should also be avoided.

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“…The fall in BP due to guanfacine is accom panied by a decrease in peripheral resistance [Ehringer et al, 1980;Magometschnigg et al, 1980]. Indometacin has been showrn to in crease the peripheral resistance in normal volunteers [Wcnmalm.…”

Section: Discussionmentioning

confidence: 99%

Drug Interaction between Guanfacine and Nonsteroidal Antiinflammatory Drugs in Dogs

Thatte¹,

Gupta²,

Satoskar³

1986

Pharmacology

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Nonsteroidal anti-inflammatory drugs (NSAIDs) have been shown to attenuate the hypotensive actions of various antihypertensive agents. This experimental study in dogs was undertaken to find out whether NSAIDs modified the pharmacological actions of an antihypertensive drug, guanfacine. Indometacin and enphenamic acid significantly prolonged the initial hypertensive response and blunted the subsequent hypotension produced by intravenous guanfacine. Ibuprofen and acetyl salicyclic acid also interacted in a similar manner, but to a lesser extent. Phenylbutazone, on the other hand, caused a blunting of the pressor response and potentiated the hypotension following guanfacine. When indometacin was given intracerebroventricularly, there was no interaction. These results suggest the necessity of monitoring hypertensive subjects taking guanfacine when NSAIDs are co-administered.

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Haemodynamic effects of guanfacine.

Cited by 10 publications

References 3 publications

Clinical experience with guanfacine in long‐term treatment of hypertension.

Clinical experience with guanfacine in long‐term treatment of hypertension.

Central Sympatholytic Drugs

Drug Interaction between Guanfacine and Nonsteroidal Antiinflammatory Drugs in Dogs

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