ChemInform Abstract: SUBSTITUTED PHENYLACETYLGUANIDINES, A NEW CLASS OF ANTIHYPERTENSIVE AGENTS

Bream, J. B.; Lauener, Henri; Picard, Claude; Scholtysik, G; White, T. G.

doi:10.1002/chin.197602155

Cited by 8 publications

(8 citation statements)

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“…(N-amino-2-[2,6-dichlorophenyl]acetamide hydrochloride) is an antihypertensive phenylace-.tylguanidine [1,5,25] which possesses a central a-sympathomimetic action. Its pharmacological properties are similar to those of clonidine: central stimulation of the a-adrenergic receptors causing a reduction in sympathetic tone and hence a decrease in peripheral vascular resis tance and a fall in blood pressure [27][28][29].…”

Section: Guanfacinementioning

confidence: 99%

Electroencephalographic and Psychometric Assessment of the CNS Effects of Single Doses of Guanfacine Hydrochloride (Estulic®) and Clonidine (Catapres®)

Yamadera

Ferber²,

Matejcek³

et al. 1985

Neuropsychobiology

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A double-blind, placebo-controlled study was carried out in 10 young healthy volunteers to investigate the effects of single doses of 1 and 2 mg guanfacine hydrochloride (Estulic®) and 0.15 and 0.3 mg clonidine (Catapres®) on the electroencephalogram (EEG), subjective mental and emotional state, blood pressure and heart rate. These doses are considered to be equipotent with regard to their antihypertensive effects, as shown in long-term therapeutic trials. Each subject received all five treatments in random sequence at intervals of 1 week. The EEG tracings were evaluated quantitatively by spectral analysis. Procedures were carried out before and at 1, 2, 4, 6 and 8 h after drug administration. After clonidine the EEG showed increased slow-wave activity and decreased alpha activity, these effects being dose-dependent. They were of the sedative type and did not clearly indicate specific psychotropic properties. The subjective mental and emotional state questionnaire indicated a decrease of alertness, extroversion, concentration and mood (in that order), changes which paralleled the EEG changes. The changes observed after guanfacine were qualitatively similar to those after clonidine, but were of considerably lower intensity. Our data suggest that guanfacine has less central nervous system-depressant activity than clonidine.

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Section: Guanfacinementioning

confidence: 99%

Electroencephalographic and Psychometric Assessment of the CNS Effects of Single Doses of Guanfacine Hydrochloride (Estulic®) and Clonidine (Catapres®)

Yamadera

Ferber²,

Matejcek³

et al. 1985

Neuropsychobiology

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“…Guanfacine (BS 100-141 :N-amidino-2-(2,6-dichlorophenyl acetamide), is a centrally acting antihypertensive drug with a pharmacological profile broadly similar to that of clonidine (Bream, Lavener, Picard, Scholtysik & White, 1975;Scholtysik, Lauener, Eichenberger, Burk, Saltman, Muller, Schweinitzer & Waite, 1975;Dubach, Huwyler, Radielovic & Singelsen, 1977). Differences between the two drugs which may be of clinical significance are that guanfacine has a longer duration of action and fewer side effects (Zamboulis, Reid & Hamilton, 1978).…”

Section: Methodsmentioning

confidence: 99%

Comparison of the Actions of Centrally and Peripherally Administered Clonidine and Guanfacine in the Rabbit: Investigation of the Differences

Barber

Reid

1982

British J Pharmacology

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1Guanfacine was administered intravenously to rabbits and produced a dose-dependent lowering of blood pressure.2 Clonidine and guanfacine, administered to rabbits intravenously (30 Ag/kg and 300 Ag/kg respectively) and intracisternally (3 jLg/kg and 12 gLg/kg respectively) caused a similar degree of hypotension, apparently of central origin. 3 Saliva flow in vivo was estimated. Clonidine (30 jAg/kg, i.v.) caused a significant decrease in salivation (P<0.05) for the first 50min after injection. Guanfacine caused a significant fall (P< 0.05) only at 50 and 180 min after injection. 4 Apparent partition coefficients for an octanol/buffer system at pH 7.4 for clonidine and guanfacine were 5.4 and 21.2 respectively. 5Measurement of guanfacine levels concurrently in both plasma and brain showed that guanfacine had higher brain than plasma levels and that the brain levels were fairly constant over the 3 h measured. Brain:plasma ratios were 2.1:1, 5.3: 1 and 13.6: 1 after 15,90 and 180 min respectively. 6 These results suggest that the long duration of action of guanfacine is due to its persistence at its central site of action.

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“…Guanfacine (Fig. 1) differs from clonidine in that it is a phenylacetylguanidine derivative (Bream et al 1975) and more selective in its α 2 agonism (Doxey 1979). Like clonidine, it lowers blood pressure by activation of brainstem receptors, which results in decreased sympathetic tone (Westfall and Westfall 2006).…”

Section: Pharmacologymentioning

confidence: 99%

Guanfacine and Guanfacine Extended Release: Treatment for ADHD and Related Disorders

2007

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Guanfacine, an α 2A adrenoceptor agonist, is U.S. Food and Drug Administration (FDA)-approved for the treatment of hypertension in adolescents and adults. It also has been used "off-label" for several years in children as a possible treatment for attentiondeficit/hyperactivity disorder (ADHD) and pervasive developmental disorders (PDDs). Small placebo-controlled trials support the use of guanfacine for the treatment of ADHD. There is more limited research on the use of guanfacine in treating hyperactivity occurring in children diagnosed with PDD. Recently, guanfacine extended release (GXR), a oncedaily formulation has been manufactured and studied in phase III clinical trials. Based on preliminary scientific presentations, it also appears to be efficacious in improving ADHD in children. The most common adverse effects associated with guanfacine and GXR treatment is sedation. Adverse cardiovascular effects are uncommon, although modest reductions in blood pressure and heart rate are common. If GXR is FDA-approved, it would be the first α 2A adrenoceptor agonist marketed for ADHD.

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ChemInform Abstract: SUBSTITUTED PHENYLACETYLGUANIDINES, A NEW CLASS OF ANTIHYPERTENSIVE AGENTS

Abstract: Auf verschiedenen Wegen werden Acetylguanidine (I)‐(V) dargestellt.

Cited by 8 publications

References 0 publications

Electroencephalographic and Psychometric Assessment of the CNS Effects of Single Doses of Guanfacine Hydrochloride (Estulic®) and Clonidine (Catapres®)

Electroencephalographic and Psychometric Assessment of the CNS Effects of Single Doses of Guanfacine Hydrochloride (Estulic®) and Clonidine (Catapres®)

Comparison of the Actions of Centrally and Peripherally Administered Clonidine and Guanfacine in the Rabbit: Investigation of the Differences

Guanfacine and Guanfacine Extended Release: Treatment for ADHD and Related Disorders

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