Abstract
A single dose of guanethidine produces a substantial, long-lasting depletion of tissue catecholamines in the rat, whereas a similar dose of bretylium has no effect. Both drugs produce block of the eserine-induced sympathetic pressor effect. Block by guanethidine is induced more rapidly than is amine depletion. When amine depletion is maximal, a noradrenaline infusion is capable of restoring the response to eserine, but no restoration of the response to eserine occurs after noradrenaline infusion into bretylium-treated rats. Catecholamine levels in isolated tissues are not reduced when complete block of sympathetic nerve stimulation has been produced by guanethidine. It is suggested that guanethidine possesses a primary bretylium-like, and a secondary reserpine-like, blocking action. Guanethidine produces a transient lowering of intestinal 5-hydroxytryptamine, and this coincides with increased intestinal motility.
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- BOURA A. L., GREEN A. F. The actions of bretylium: adrenergic neurone blocking and other effects. Br J Pharmacol Chemother. 1959 Dec;14:536–548. doi: 10.1111/j.1476-5381.1959.tb00961.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- BULBRING E., LIN R. C. The effect of intraluminal application of 5-hydroxytryptamine and 5-hydroxytryptophan on peristalsis; the local production of 5-HT and its release in relation to intraluminal pressure and propulsive activity. J Physiol. 1958 Mar 11;140(3):381–407. [PMC free article] [PubMed] [Google Scholar]
- BURN J. H. A new view of adrenergic nerve fibres, explaining the action of reserpine, bretylium, and guanethidine. Br Med J. 1961 Jun 10;1(5240):1623–1627. doi: 10.1136/bmj.1.5240.1623. [DOI] [PMC free article] [PubMed] [Google Scholar]
- BURN J. H., RAND M. J. The action of sympathomimetic amines in animals treated with reserpine. J Physiol. 1958 Dec 4;144(2):314–336. doi: 10.1113/jphysiol.1958.sp006104. [DOI] [PMC free article] [PubMed] [Google Scholar]
- BURN J. H., RAND M. J. The effect of precursors of noradrenalin on the response to tyramine and sympathetic stimulation. Br J Pharmacol Chemother. 1960 Mar;15:47–55. doi: 10.1111/j.1476-5381.1960.tb01209.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- CASS R., KUNTZMAN R., BRODIE B. B. Norepinephrine depletion as a possible mechanism of action of guanethidine (SU 5864), a new hypotensive agent. Proc Soc Exp Biol Med. 1960 Apr;103:871–872. doi: 10.3181/00379727-103-25702. [DOI] [PubMed] [Google Scholar]
- DOLLERY C. T., EMSLIE-SMITH D., MILNE M. D. Clinical and pharmacological studies with guanethidine in the treatment of hypertension. Lancet. 1960 Aug 20;2(7147):381–387. doi: 10.1016/s0140-6736(60)92836-1. [DOI] [PubMed] [Google Scholar]
- Finkleman B. On the nature of inhibition in the intestine. J Physiol. 1930 Sep 18;70(2):145–157. doi: 10.1113/jphysiol.1930.sp002683. [DOI] [PMC free article] [PubMed] [Google Scholar]
- LEISHMAN A. W., MATTHEWS H. L., SMITH A. J. Guanethidine; hypotensive drug with prolonged action. Lancet. 1959 Dec 12;2(7111):1044–1048. doi: 10.1016/s0140-6736(59)91526-0. [DOI] [PubMed] [Google Scholar]
- MAXWELL R. A., MULL R. P., PLUMMER A. J. [2-Octahydro-1-azocinyl)-ethyl]-guanidine sulfate (CIBA 5864-SU), a new synthetic antithypertensive agents]. Experientia. 1959 Jul 15;15:267–267. doi: 10.1007/BF02158076. [DOI] [PubMed] [Google Scholar]
- MCEWEN L. M. The effect on the isolated rabbit heart of vagal stimulation and its modification by cocaine, hexamethonium and ouabain. J Physiol. 1956 Mar 28;131(3):678–689. doi: 10.1113/jphysiol.1956.sp005493. [DOI] [PMC free article] [PubMed] [Google Scholar]
- SHORE P. A., OLIN J. S. Identification and chemical assay of norepinephrine in brain and other tissues. J Pharmacol Exp Ther. 1958 Mar;122(3):295–300. [PubMed] [Google Scholar]