Amines, sympathomimetic

Appetite suppressants have been widely used as an adjunct to dietary restriction and sympathomimetic amines have traditionally been used for this purpose. These agents have not proven particularly useful and frequentiy cause unacceptable side effects, hence their popularity has been waning for several years. The most promising newer dmgs work through a serotoninergic mechanism and hold considerable promise at least for certain obese patients. 

Compounds stmcturaHy related to the endogenous sympathomimetic amines epinephrine and norepinephrine have classically been employed as appetite suppressants. These agents, of which amphetamine [300-62-9], is the prototypical example, generally retain the phenethyl amine, but lack... 

Acutrim 16 Hour Steady Control Tablets. Acuttim is an appetite suppressant diet aid available without a prescription and marketed by CIBA Consumer Pharmaceuticals. The active ingredient is phenylpropanolamine hydrochloride [154-41 -6] a sympathomimetic amine (see Antiobesity drugs). Acutrim dehvers its dosage at a precisely controlled rate for up to 16 hours. This is achieved through the OROS technology. 

As already stated, the number of substances made by chemists for pharmacological examination as possible sympathomimetic amines is enormous and the literature voluminous. Fortunately the latter has been reviewed from time to time, and most recently in the symposium in which Hartung dealt with the correlation of structure and pharmacological action in )3-phenylethylamine derivatives, which includes the more impor-... 

Hypertensive reaction resulting from release of noradrenaline by tyramine and other sympathomimetic amine as a consequence of irreversible inhibition of MAO-A. 

Vasoconstrictors are drugs which increase the tone of smooth muscle cells in the vasculature. They include sympathomimetic amines and certain eicosanoids and peptides (angiotensin, vasopressin, urotensin or en-dothelin). 

Chance, M.R.A. Aggregation as a factor influencing the toxicity of sympathomimetic amines in mice. J Pharmacol Exp Ther 87 214-219, 1946b. 

This sympathomimetic amine exudes similar pharmacologic activity as the amphetamines, resulting in central nervous system stimulation and appetite suppression. This drug is indicated for short-term use in conjunction with a reduced-calorie diet and exercise in obese patients with a BMI of 30 kg/m2 or greater following failed attempts of diet and exercise alone.40... 

The answer is g. (Hardman, pp 439 140.) Most MAOls are nonse-lective for MAOA and -B. MAOls mainly act on tissues regulated by sympathomimetic amines and serotonin. 

Midrin is a proprietary combination of acetaminophen, isometheptene mucate (a sympathomimetic amine), and dichloralphenazone (a chloral hydrate derivative) that has shown modest benefits in placebo-controlled trials. It may be an alternative for patients with mild to moderate migraine... 

Phenylephrine (27) is a low-potency sympathomimetic amine used as a decongestant. Solutions become coloured due to an auto-oxidation accelerated by light. In a series of experiments, aqueous solutions of the hydrochloride were left under a UV lamp until a tan colour developed. HPLC analysis showed four main products of which one was identified as adrenaline (19). Even after prolonged irradiation, there was never more than 2% adrenaline in the solution. It was assumed that the catecholamine was removed as it formed by further reaction to adrenochrome and melanine, which accounted for the colour [34],... 

Predictable interactions occur between the MAOIs and any amine precursors, or directly or indirectly acting sympathomimetic amines (e.g. the amphetamines, phenylephrine and tyramine). Such interactions can cause pronounced hypertension and, in extreme cases, stroke. 

The noradrenaline normally contained in the storage granules can be partly or completely replaced by structurally related sympathomimetic amines, either by injection of the amine itself, or of suitable precursors such as a-methyl-DOPA or a-methyl-w-tyrosine. These amines can be depleted from the heart by guanethidine in the same way as the noradrenaline which they had replaced. a-Methylnoradrenaline [337] and metaraminol [338] are depleted less readily than noradrenaline from rabbit or rat hearts, whereas dopamine, octopamine and w-octopamine are depleted more readily than noradrenaline [339]. The more rapid depletion of these last three compounds was attributed to weaker binding in the storage granules [339], but could equally well be due to their greater susceptibility to destruction by monoamine oxidase, since both a-methyl-noradrenaline and metaraminol are resistant to attack by monoamine oxidase. 

Terbutaline is a synthetic sympathomimetic amine. It is one of the most selective direct-acting stimulants of )32 dr6noreceptors. It stimulates smooth muscle )32-adrenoreceptors in the bronchi, relaxing them and relatively minutely acting on the — receptors of the heart. 

Albuterol is a )32-adrenergic sympathomimetic amine with pharmacological similarities to terbutaline. It has almost no effect on jSj-adrenoreceptors of the heart. It has expressed broncholytic effects— prevention or relief of bronchi spasms, lowering respiratory tract resistance, and increasing the vital capacity of the lungs. 

Metaraminol is a sympathomimetic amine of both direct and indirect action that has hemodynamic characteristics similar to norepinephrine. It has the ability to elevate both systohc and diastolic blood pressure. 

Drugs with thyroid hormone activity, alone or with other therapeutic agents, have been used for the treatment of obesity. In euthyroid patients, doses within the range of daily hormonal requirements are ineffective for weight reduction. Larger doses may produce serious or even life-threatening manifestations of toxicity, particularly when given in association with sympathomimetic amines such as those used for their anorectic effects. 

Obesity In euthyroid patients, hormonal replacement doses are ineffective for weight reduction. Larger doses may produce serious or even life-threatening toxicity, particularly when given with sympathomimetic amines such as anorexiants. 

Usual dose response Advise patients to contact a physician if they do not respond to their usual dose of a sympathomimetic amine. 

Pharmacology Amphetamines are sympathomimetic amines with CNS stimulant activity. CNS effects are mediated by release of norepinephrine from central noradrenergic neurons. Peripheral activities include elevation of systolic and diastolic blood pressures and weak bronchodilator and respiratory stimulant action. Pharmacokinetics ... 

Advanced arteriosclerosis symptomatic cardiovascular disease moderate to severe hypertension hyperthyroidism hypersensitivity or idiosyncrasy to the sympathomimetic amines glaucoma agitated states history of drug abuse during or within 14 days following administration of monoamine oxidase (MAO) inhibitors (hypertensive crises may result). 

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