Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C1323099 (sympathomimetic)
 2,957 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Studies in normal volunteers documented the positive inotropic effects of Etilefrin-HCL, a direct sympathomimetic drug, with increases of systolic blood pressure, renal blood flow and glomerular filtration rate. Sodium and potassium excretion as well as serum potassium decreased. After an additional injection of Metoprolol, a beta 1-sympatholytic drug, blood pressure, renal blood flow and glomerular filtration rate normalized, whereas electrolyte excretion decreased further. Renin release was decreased during administration of Etilefrin as well as during combined Etilefrin and Metoprolol application. Reziprocal to changes of blood pressure, plasma norepinephrine concentration decreased during Etilefrin and increased during combined administration of Etilefrin and Metoprolol. The results lead to the following interpretation: Changes of blood pressure and renal hemodynamics are mediated by beta 1-adrenergic effects of Etilefrin, whereas the electrolyte excretion is influenced by beta 2-adrenergic effects. Renin release seems to be influenced by beta 1 as well as beta 2-adrenergic receptors.
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PMID:[Hemodynamic and humoral changes during administration of a sympathomimetic and a sympatholytic drug with special notes on the regulation of renin release (author's transl)]. 3 50

The autonomic nervous system is divided into the parasympathetic and sympathetic systems, with three types of adrenergic receptors: alpha (smooth muscle contraction), beta1 (cardiac acceleration and fatty acid mobilization) and beta2 (smooth muscle relaxation). Substances affecting the function of the adrenergic system are the agonists or stimulators, which mimic the effects of endogenous norepinephrine or epinephrine, and antagonists or blockers, which block the receptors and prevent stimulation by the agonists. Autonomic stimulation in the eye mediates various changes which apparently affect outflow facility and rate of formation of aqueous humor. Alteration of either or both of these factors by autonomic agonists or antagonists may have a direct or an indirect effect on intraocular pressure. Beta-adrenergic blocking substances have been used to treat a variety of diseases. Some of the effects of these drugs are attributable to properties other than beta blockade, such as intrinsic sympathomimetic activity and local anaesthetic activity. Side effects of this class of drugs require caution in cases of congestive heart failure and in asthmatics. Autonomic agents used in the treatment of ocular hypertension and glaucoma include pilocarpine, a chilinergic agonist, epinephrine, an adrenergic agonist, and various beta adrenergic blockers or antagonists including propranolol, atenolol and timolol. The physico-chemical properties and pharmacokinetics of timolol are reviewed. Data showing a significant reduction in intraocular pressure as a result of ocular instillation of timolol are presented. Reduction of the rate of aqueous formation appears to be the mechanism of action. A low incidence of non-serious side effects is reported.
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PMID:The beta-adrenergic blocking agents and the treatment of glaucoma. 3 5

The newly synthesized alpha-adrenoceptor blocking drug BHC (N,N'-bis[6-(10-methoxybenzyl-amino)-a-hexyl]cystamine) was found to block irreversibly the positive inotropic effect of the sympathomimetic drug phenylephrine on the isolated rat left atrium. BHC was used to test the adrenoceptor interconversion hypothesis which claims that low temperature converts inotropic beta-adrenoceptors in rat atrium and frog ventricle to alpha-adrenoceptors. There was no evidence of adrenoceptor 'interconversion.' In the rat atrium low temperature did not increase the BHC antagonism of phenylephrine and did not cause BHC to inhibit the inotropic effect of noradrenaline or isoprenaline. In the perfused frog heart low temperature did not lead BHC to inhibit the inotropic effect of phenylephrine, adrenaline, or isoprenaline.
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PMID:Inhibition of the cardiac inotropic effect of phenylephrine by a tetramine disulfide with irreversible alpha-adrenoceptor blocking activity. 3 1

A case of fatal gas gangrene occurring after venous catheterization and the administration of sympathomimetic amines is reported. Following a brief discussion, the necessity of observing strict asepsis during the insertion and care of the catheter and of always ensuring that the tip of the catheter is in a large vein is emphasized.
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PMID:[Gas gangrene caused by venous catheterization (apropos of a case)]. 3 99

The effects of 4 beta-adrenoceptor blocking drugs on blood pressure and on exercise tachycardia were compared in a within-patient study of patients with uncomplicated essential hypertension. Twelve patients were treated with propranolol, practolol and atenolol and 7 of the same patients also received oxprenolol. Each patient received each drug separately, withdrawing each drug before starting the next, and each patient was titrated to the lowest attainable blood pressure and heart rate with each compound. All 4 drugs caused reductions in both systolic and diastolic blood pressure and in the heart rate induced by exercise. The maximum reduction by each drug in both systolic and diastolic blood pressure was the same. There were small but significant differences in the effects on heart rate between those drugs which had intrinsic sympathomimetic activity and those which did not have this property.
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PMID:Effects of 4 beta-adrenoceptor blocking drugs on blood pressure and exercise heart rate in hypertension. 3 65

MK-761 is a new class of compound which has beta adrenoceptor antagonist and vasodilating properties in a single molecule. The compound has in vitro beta adrenoceptor blocking activity in the isolated cat heart papillary muscle and isolated rat atria. Unlike propranolol, it did not depress contactile force. Intrinsic sympathomimetic activity was not observed in vitro, (isolated cat papillary muscle, isolated atria) but the compound has some intrinsic sympathomimetric activity because it slightly increased heart rate in reserpinized rats. MK-761 was found to be approximately as potent as timolol and pindolol in blocking cardiac and vascular beta adrenergic receptors in anesthetized dogs. The drug was not, however, cardioselective. Oral beta adrenoceptor blocking activity was observed in rats at doses similar to those which decreased blood pressure.
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PMID:Beta adrenoceptor blocking properties of MK-761. 4 12

Rats with experimental renovascular hypertension were treated with high doses of beta-blocking agents. Pindolol 10 mg/kg per day increased Goldblatt-type hypertension, whereas Propranolol 100 mg/kg per day showed an antihypertensive effect. A linear correlation between the weight of the left-heart ventricle and the systolic blood pressure was found in animals treated with Pindolol as well as in untreated Goldblatt rats. On the contrary, the weights of the left-heart ventricle were significantly higher in those animals treated with Propranolol than in the other groups. The results show that Pindolol in high doses, possibly on account of its sympathomimetic activity, leads to an increase in Goldblatt hypertension, but does not influence the pressure-dependent progression of left-heart hypertrophy. On the other hand, Propranolol, possibly on account of a cardiodepressory effect, leads to a decrease in blood pressure.
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PMID:[High dose betablocker treatment in experimental renal hypertension (author's transl)]. 4 62

DL 071 IT, a new potent non-selective beta-adrenergic blocking drug with intrinsic sympathomimetic activity and weak membrane stabilizing activity, was evaluated alone and in comparison with oxprenolol, in six volunteers, at rest and during an exercise test. Heart rate and systolic pressure were monitored for up to 7 h after oral administration of the drugs. Exercise heart rate and systolic pressure were significantly reduced by both drugs, but only DL 071 IT caused a significant reduction in resting heart rate. As compared to oxprenolol, DL 071 IT has a longer duration of action and is from 5.0 to 13.5 times more potent.
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PMID:Pharmacodynamic studies in man of the beta-adrenoceptor antagonist DL 071 IT. 4 Aug 1

Two new beta-adrenoceptor blocking drugs with acute antihypertensive and positive inotropic effects are described: Compound A (2-[4-(3-tert.butylamino-2-hydroxypropoxy)phenyl]-4-trifluoromethylimidazole) and MK-761 (2-(3-tert.butylamine-2-hydroxypropoxy)-3-cyanopyridine hydrochloride). In SH rats both compounds, given orally, lowered arterial pressure and were more potent than hydralazine. The antihypertensive effect of compound A but not of MK-761 was antagonized by timolol. Both compounds had positive inotropic activity on cat heart papillary muscles; these effects were antagonized by timolol. The pretreatment of animals with reserpine greatly reduced the positive inotropic effect of MK-761 but not of compound A. The acute antihypertensive and positive inotropic effects of compound A are like to be at least partially due to stimulation of beta-adrenoceptors, e.g. intrinsic sympathomimetic activity. The effects of MK-761 on the same parameters appear to be mediated by different mechanisms.
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PMID:Antihypertensive and cardiac effects of two novel beta-adrenoceptor blocking drugs. 4 53

In this study the anti-arrhythmic effectiveness of pindolol has been tested on ventricular effort arrhythmias in a group of 22 cardiopathic patients. The drug, administered for a week at the dose of 5 mg three times a day, obtained positive results due to its beta-blocking action and its intrinsic sympathomimetic activity.
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PMID:[Pindolol in the treatment of arrhythmias caused by exertion]. 4 61


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