0-Adrenergic bronchodilator

Albuterol Ipratropium (Combivent, DuoNeb) [Bronchodilator/Adrenergic, Anticholinergic] Uses coPD ... 

Bronchodilators [adrenergic] -erol Albuterol, pirbuterol Bronchodilation (26)... 

When used concomitantly with other sympathomimet-ics, terbutaline may potentiate the adverse cardiovascular effects of the other drugs however, as an aerosol bronchodilator (adrenergic-stimulator type), concomitant use may relieve acute bronchospasm in patients on long-term oral terbutaline therapy. 

This is an early and important sign of gases that affect the central respiratory compartment (e.g. chlorine). Aggressive treatment is required with bronchodilators (adrenergic agent and theophylline). Steroids should be used if the patient has a history of hyperreactive airways. Steroid doses should be tapered off as rapidly as... 

The modern usage of P2" go Asts for the treatment of asthma dates to 1903 when the effect of injected epinephrine [51-43-4] (adrenaline) C2H23NO2, (1 R = CH3) was investigated (see Epinephrine and norepinephrine) (33). As in some other modem treatments, eg, xanthines and anticholinergics, the roots of P2" go Ast therapy for asthma can be found in historical records which document the use of herbal extracts containing ephedrine [299-42-3] C qH NO, (2) as bronchodilators. Epinephrine and ephedrine are stmcturaHy related to the catecholamine norepinephrine [51-41-2] CgH NO, (1, R = H), a neurotransmitter of the adrenergic nervous system (see Neuroregulators). 

Ephedrine, which is not a catecholamine, has weak oral activity as a bronchodilator and although it has some direct action at adrenergic receptors, its predominant mode of action is by displacing norepinephrine from storage vesicules. 2"Agonists which are in use or are under investigation are the result of quests for improved selectivity, retention of potency, oral activity, and longer duration of action. 

Beta adrenergic agonists also exert bronchodilating effects. These drugs are thus often used in conjunction with theophiline in asthma therapy. A drug that combines both moieties, reproterol (40), has interestingly proved... 

The dose of bronchodilator can be gradually reduced based on both symptomatic and objective improvement until the patient returns to pre-exacerbation use of short-acting P2-adrenergic agonist pharmacotherapy... 

As greater control of the disease state is achieved with aerosol therapy, manufacturers are considering combining some of their most successful products to achieve bronchodilation and anti-inflammatory effect in a single dose. These combinations may increase interest in the use of anticholinergics in addition to fl2-adrenergic agonists. 

Amidephrine (25), an adrenergic agent very closely related to m talol, finds use as a broncho-dilator. -5 Carbuterol (27), another bronchodilator, is made by reacting 3-amino-4-benzyloxyacetophenone with phosgene to give isocyanate 26. Subsequent... 

Derivatives of phenylethanolamine substituted by a phenolic hydroxyl on the para position have been known for some time to exhibit 0-adrenergic agonist activity. As a consequence of this property, the compounds have proven useful as bronchodilators for the treatment of asthma (see Chapter 3). Since such sympathomimetic drugs tend to have undesired activity on the cardiovascular system in addition to the desired activity on the bronchii, considerable work has been devoted to the preparation of compounds that would show selectivity for the adrenergic receptors (02> that predominate in the lung. Attachment of the side chain to a heterocyclic aromatic phenol has been one avenue that has shown promise for achieving this selectivity. 

Effenberger, F. and Jager, J. (1997) Synthesis of the adrenergic bronchodilators (R)-terbutaline and (R)-salbutamol from (R)-cyanohydrins. The Journal of Organic Chemistry, 62, 3867-3873. 

Some failures will be due to the presence of variants in drug handling. Patients who are rapid acetylators of isoniazid have a slower antituberculous response than slow acetylators (Evans and Clarke, 1961). Asthmatics who do not respond well to (32-agonist bronchodilators may have fewer functioning p2-adrenergic receptors (Drysdale et al., 2000). Variations in the synthesis or structure of the serotonin transporter protein, which is involved in selective reuptake of serotonin by presynaptic neurons, may explain why some patients with depressive disorders respond to selective serotonin reuptake inhibitors and others do not (Steimer et al., 2001). 

Sufficient data were not included in other reports to calculate predictive values. For instance, Drysdale et al. (2000) reported over a twofold difference between responses to bronchodilators in asthmatics who differed in haplotypes of the [1,-adrenergic receptor gene, but predictive values could not be calculated because the number of asthmatics in each response and haplo-type category were not given. Marked differences in mean absorption of digoxin between indi-... 

Albuterol serotonin reuptake inhibitor A bronchodilator that blocks selective / -adrenergic receptor. 

Tropane alkaloids act as bronchodilators, but have been replaced clinically by methyixanthines and adrenergic drugs. They inhibit secretions from mucous membranes in the nose, mouth, pharynx, and bronchi. 

Lima JJ, Thomason DB, Mohamed MH, Eberle LV, Self TH, Johnson JA. (1999) Impact of genetic polymorphisms of the beta2-adrenergic receptor on albuterol bronchodilator pharmacodynamics. Clin Pharmacol Ther. 65, 519-525. 

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