Beta adrenoceptor antagonists

Taylor, D. C., Pownall, R., Burke, W., The absorption of beta adrenoceptor antagonists in rat in-situ small intestine the effect of lipophilicity, J. Pharm. Pharmacol. 1985, 37, 280-283. 

Weinstock, M., Weiss, C., and Gitter, S. (1977) Blockade of 5-HT receptors in the central nervous system by beta-adrenoceptor antagonists. Neuropharmacology, 16 273-276. 

Nielsen HM, and Rassing MR (2000a) TR146 cells grown on filters as a model of human buccal epithelium IV. Permeability of water, mannitol, testosterone, and beta-adrenoceptor antagonists. Comparison to human, monkey and porcine buccal mucosa. Int. J. Pharm. 194 155-167. 

Add pindolol (a 5-HTid antagonist as well as a beta adrenoceptor antagonist), which is well researched but there are contradictory findings in the literature with regard to its efficacy. So far, the clinical data suggest that the response to a standard antidepressant is accelerated. 

The dramatic effect of a single unit is shown in Figure 3.8 for a series of beta-adrenoceptor antagonists. 

Cardiovascular drugs - digitalis preparations, beta adrenoceptor antagonists, some antiarrhythmic drugs... 

Beta-adrenoceptor antagonists are used to treat hypertension, angina pectoris, arrhythmias and secondary myocardial infarct prevention following primary infarction (timolol, metoprolol and propranolol). 

Beta-adrenoceptor antagonists, particularly propranolol, have been shown to be effective for anxiety symptoms particularly in situational anxiety and GAD. Buspirone, an azaspirodecanedione, is an agonist at 5-HTlA receptors and seems to have anxiolytic effects, though it is less potent than the BDZs and the effects take up to three weeks to become evident. There is high first pass metabolism and a considerable proportion of the effect is due to a metabolite (1-PP). The principal adverse effects of buspirone are nausea, gastrointestinal upset and headache. Antidepressant drugs, both the older tricyclic antidepressants and the newer drugs, have been demonstrated to have anxiolytic effects in mixed anxiety-depressive patients, GAD and panic disorder. 

A.Wellstein, D.Palm, G.Wiemer, M.Schafer-Korting and E.Mutschler, Simple and reliable radioreceptor assay for beta-adrenoceptor antagonists and active metabolites in native human plasma, Eur. J. Clin. Pharmacol, 27, 545 (1984). 

Ellison KE, Gandhi G Optimising the use of beta-adrenoceptor antagonists in coronary artery disease. Drugs 2005 65 787. [PMID 15819591]... 

The effect of beta-adrenoceptor antagonists on thyroid hormone metabolism is unlikely to play a significant role... 

However, contrary to popular belief, beta-adrenoceptor antagonists do not by themselves increase the risk of hypoglycemic episodes in insulin-treated diabetics, in whom their use was concluded to be generally safe (192). Indeed, in 20 such patients treated with diet or diet plus oral hypoglycemic agents, both propranolol and metoprolol produced small but significant increases in blood... 

Theeuwes, F., Swanson, D. R., Guittard, G., et al. Osmotic delivery systems for the beta-adrenoceptor antagonists metoprolol and oxprenolol Design and evaluation of systems for once-daily administration. Br. J. Clin. Pharmacol. 19 (suppl 2) 69S-76S, 1985. 

Tolerance, physical dependence and withdrawal are a natural consequence of the properties of drugs of dependence. They can be produced in experimental animals as readily as they can in man but the symptoms do not always imply that the individual is dependent on a drug of abuse. For example, a patient with hypertension who is receiving a beta-adrenoceptor antagonist such as propranolol will probably exhibit a withdrawal syndrome consisting of a rebound hypertension when the drug is abruptly withdrawn. 

Waeber C, Palacios JM. Non 5-HT1A/5-HTlc [3H]5-HT binding sites in the hamster, opossum and rabbit brain show similar regional distribution but different sensitivity to beta-adrenoceptor antagonists. Synapse 1992 12 261-270. 

Harron and Kobinger (1984) used capsaicin to elicit the Bezold-Jarisch reflex in anesthetized artificially respi-rated dogs pretreated with a beta-adrenoceptor antagonist to evaluate the activity of clonidine-like drugs on central alpha2 adrenoceptors after intracistemal administration. 

Drug treatment of thyrotoxicosis involves using antithyroid drugs carbimazole, propylthiouracil, beta-adrenoceptor antagonists and iodine. 

Beta-adrenoceptor antagonists are effective antihypertensives and operate partly by blocking /31-receptors on the heart and juxtaglomerular cells of the kidney and partly by central actions which reduce sympathetic activity. 

Q5 Beta-blockers can have a number of adverse effects. In fact, all drugs used to treat hypertension have some side effects. Beta-adrenoceptor antagonists are... 

Q10 Beta-adrenoceptor antagonists are contraindicated in patients with asthma or respiratory obstructive diseases, bradycardia, heart block or heart failure. Adrenergic agonists are contraindicated in patients with closed-angle glaucoma and should be used cautiously in patients with hypertension or heart disease. Parasympathomimetics cause poor night vision and dimming of vision, because of development of miosis, headache and brow ache. Carbonic anhydrase inhibitors have a weak diuretic action and can induce depression, drowsiness, paraesthesia, electrolyte disturbance such as hypokalaemia, acidosis and lack of appetite. 

Viloxazine, a bicyclic compound, is related structurally (but not pharmacologically) to the beta-adrenoceptor antagonists. In animal tests, its profile shows properties of both the imipramine-like compounds (reversal of reser-pine-induced hypothermia) and amphetamine (stimulation of the electroencephalogram). A review of animal and clinical data confirmed the impression that viloxazine has efficacy comparable to that of imipramine but with a different adverse effects profile (1). There is a reduced frequency of anticholinergic and sedative effects and a tendency to lose rather than to gain weight. However,... 

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