Adrenergic drugs, action

Adrenergic receptor 2 Amino acid variants appear to be associated with receptor function and agonist induced down regulation. Some variants may predispose to some types of asthma and modulate action of (3-2-adrenergic drugs. 

Discuss the uses, general drug actions, contraindications, precautions, interactions, and adverse reactions associated with the administration of adrenergic drugs. 

The amphetamines, such as amphetamine, dextroamphetamine (Dexedrine), and metliainphetainine (Desoxyn), are sympatiiomimetic (ie, adrenergic) dru that stimulate the CNS (see Chap. 22). Their drug action results in an elevation of blood pressure, wakefulness, and an increase or decrease in pulse rate The ability of these drugs to act as anorexiants and suppress the appetite is thought to be due to their action on the appetite center in the hypothalamus. 

Cotecchia, S., Rossier, 0., Fanelli, F., Leonardi, A., and De Benedetti, P. G. (2000) The alpha la and alpha lb-adrenergic receptor subtypes molecular mechanisms of receptor activation and of drug action. Pharm. Acta Helv. 74,173-179. 

Pharmacology These agents are synthetic adrenocortical steroids with basic glucocorticoid actions and effects. Glucocorticoids may decrease number and activity of inflammatory cells, enhance effect of beta-adrenergic drugs on cyclic AMP production, inhibit bronchoconstrictor mechanisms, or produce direct smooth muscle relaxation. Inhaler use provides effective local steroid activity with minimal systemic effect. 

Beta-adrenergic drugs can be administered orally, subcutaneously, or by inhalation. Inhalation of these drugs is often the preferred method of administration in treating respiratory disorders. Inhalation allows the drug to be delivered directly to the respiratory tissues with a minimum of systemic side effects because of its absorption into the systemic circulation.4 The onset of action is also more rapid with inhalation. 

Metaraminol [met a RAM i nole] is a mixed-action adrenergic drug with actions similar to norepinephrine. This agent has been used in the treatment of shock (when an infusion of norepinephrine or dopamine is not possible) and to treat acute hypotension. It is given parenterally as a single injection. It enhances cardiac activity and produces mild vasoconstriction. 

Lima JJ, Thomason DB, Mohamed MHN, Eberle LV, Self TH, Johnson JA. 1999. Pharmacodynamics and drug action impact of genetic polymorphisms of the /S2-adrenergic receptor on albuterol bronchodilator pharmacodynamics. Clin. Pharmacol. Ther. 65 519-25... 

For example, such simple PK/PD models as described in Fig. 13 have been used to describe the effects of beta-2-adrenergic drugs on the heart rate, but models incorporating an effect-compartment [106] or indirect-response model [105] are necessary for other drug actions, such as the effects of glucocorticoids on lymphocytes and endogenous cortisol suppression (for review see Ref. 107). 

---