Salbutamol, bronchodilation

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. 

Nogami-Itoh, M., I.Yakuo, D.M.Hammerbeck, R.I.Miller, and K.Takeyama. 1997. The equivalent bronchodilator effects of salbutamol formulated in chlorofluorocarbon and hydrofluoroalkane-134a metered dose inhalers on the histamine-induced pulmonary response in dogs. Pharmaceut. Res. 14 208-212. 

Zainudin, B.M.Z., Biddiscombe. M., Tolfree, S.E.J., Short, M., and Spiro, S.G., Comparison of bronchodilator responses and deposition patterns of salbutamol inhaled from a pressurized metered dose inhaler, as a dry powder, and as a nebulized solution, Thorax, 45 469-473 (1990). 

Therefore, the chiral cyanohydrins are valuable and versatile synthons as their single hydroxyl asymmetric centre is accompanied by at least one other chemical functionality. Thus with careful functional group protection, differential and selective chemical transformations can be performed. Such synthetic techniques lead to production of interesting bioactive compounds and natural products. These products include intermediates of j3-blockers 15 1117], j3-hydroxy-a-amino acids 16 [118],chiral crown ethers 17 [lll],coriolic acid 18 [120], sphingosines 19 [121], and bronchodilators such as salbutamol 20 [122] (Fig. 3). 

Acetazolamide is a carbonic anhydrase inhibitor that reduces aqueous humour production and is therefore indicated in glaucoma to reduce the intraocular pressure. Salbutamol is a selective, short-acting beta2-agonist used as a bronchodilator in asthma. Tolbutamide is a short-acting sulphonylurea used in type 2 (non-insulin dependent) diabetes mellitus. Chlorpromazine is an aliphatic neuroleptic antipsychotic drug used in schizophrenia. Zafirlukast is a leukotriene-receptor antagonist that is indicated in the prophylaxis of asthma but should not be used to relieve acute severe asthma. 

Salbutamol is a selective beta2-receptor agonist indicated in the management of asthma as a bronchodilator relieving acute attacks. It may be used in combination with inhaled corticosteroids such as beclometasone. Salbutamol acts within a few minutes and tends to be short-acting, unlike salmeterol. Side-effects of salbutamol include tachycardia and palpitations. It does not cause drowsiness and does not precipitate oral candidiasis. Inhaled corticosteroids may precipitate oral candidiasis. 

Salbutamol is a beta-adrenoreceptor agonist that is used in asthma or chronic obstructive pulmonary disease in order to exert bronchodilation. Side-effects... 

Clinically, it has been confirmed that the drug is an effective bronchodilator with very little cardiovascular activity it does not appear to increase hypoxaemia [439]. A more detailed study [440], comparing salbutamol with isoprenaline and orciprenaline, demonstrated that 200 jug of salbutamol provided effective bronchodilation for at least three hours without detectable cardiac stimulation. Equivalent bronchodilator doses of isoprenaline and orciprenaline were 1000 /ag and 1500 jUg respectively. The bronchial effects of isoprenaline, though initially intense, waned within one hour and cardiac effects were noted. In this trial little objective difference could be detected between salbutamol and orciprenaline at the dose levels used, though most patients expressed preference for salbutamol. 

By virtue of its prolonged effect and high degree of selectivity salbutamol may prove to be a significant development in bronchodilators, apart from its intrinsic interest as a research tool. 

Bronchodilation. P2-Adrenocep-tor-mediated bronchodilation (e.g., with terbutaline, fenoterol, or salbutamol) plays an essential part in the treatment of bronchial asthma (p. 328). 

The data in Table 8.2 are taken from a study reported by Hindle et the purpose of which was to determine whether a new dry powder inhaler (DISK) was equivalent to a traditional metered-dose inhaler (MDI) in its ability to deliver doses of a bronchodilator to the lungs of volunteers. The data are the percentages of an inhaled dose of salbutamol recovered in a urine sample taken 30 min post-inhalation for each method of delivery in nine volunteers. Ameasure of treatment effect is the difference in percentages within volunteers, shown in the fourth column. Of these differences seven are negative and two are positive (fifth column) and the question we need to answer is how likely is it that if there is no difference between the inhalers, we would see this degree of imbalance between negatives and positives ... 

Bronchodilators Mabuteml is an adrenergic jS-2 agonist. It is more selective and potent than salbutamol, the reference bronchodilator used in asthma therapy (Figure 8.49). 

Drugs given by this route are quickly absorbed, which takes place from the vast surface of alveoli and produce rapid action. Various bronchodilators and mast cell stabilizers are used in the treatment and prophylaxis of bronchial asthma i.e. salbutamol (ASTHALIN) and sodium cromoglycate (FINTAL) inhaler. 

Samples from cattle, sheep, horse, poultry, and ratite were tested for the -agonists clenbuterol, salbutamol, and cimaterol. Clenbuterol has restricted use and is registered as a tocolytic agent for tire facilitation and postponement of parturition in cattle and sheep and as a bronchodilator and expectorant in horses. 

Salbutamol is a -receptor antagonist and a bronchodilator. Salbutamol and other -receptor antagonists should not be administered in the presence of hyperthyroidism, myocardial insufficiency, arrythmias, hypertension, and diabetes mellitus. Salbutamol is considered a drug of abuse.46 Salbutamol may cause skeletal muscle tremors, palpitation, muscle cramps, and hypersensitivity reactions. An overdose of salbutamol can cause tachycardia, CNS stimulation, tremor, hypokalemia, and hyperglycemia.47... 

Q1 The most commonly used reliever in asthma therapy is a short-acting bronchodilator, such as the beta-2-agonists (/ -agonists) salbutamol or terbutaline. These are safe and effective agents for mild to moderate symptoms and are taken directly into the respiratory tract via an inhaler device. 

Q6 Salbutamol is a selective beta-2-adrenoceptor (/ -adrenoceptor) agonist which is effective in relieving mild to moderate bronchoconstriction. Inhalation of salbutamol induces bronchodilation by acting on /J2-receptors on bronchial smooth muscle this lasts for approximately three to five hours. It also inhibits mediator release and improves the clearance of mucus from the lung. Stimulation of the /02-receptor increases the cellular concentration of cyclic adenosine monophosphate cAMP and activates a protein kinase. This kinase in turn inactivates myosin-light-chain kinase, an enzyme necessary for contraction in smooth muscle, and so relaxes bronchial smooth muscle. 

CENTRALLY ACTING ANTI HYPERTENSIVES BRONCHODILATORS -BETA-2 AGONISTS Cases of 1 BP when intravenous salbutamol is given with methyldopa Uncertain at present Monitor BP closely... 

IPRATROPIUM BRONCHODILATORS -SALBUTAMOL A few reports of acute angle closure glaucoma when nebulized ipratropium and salbutamol were coadministered Ipratropium dilates the pupil, which i drainage of aqueous humour, while salbutamol t production of aqueous humour Warn patients to prevent the solution to mist or enter the eye. Extreme caution in co-administering these bronchodilators by the nebulized route in patients with a history of acute closed-angle glaucoma... 

ATOMOXETINE BRONCHODILATORS -SALBUTAMOL t risk of arrhythmias with parenteral salbutamol Additive effect Avoid co-administration of atomoxetine with parenteral salbutamol... 

NS AIDs BRONCHODILATORS-BETA-2 AGONISTS Etoricoxib may t oral salbutamol levels Etoricoxib inhibits sulphotransferase activity Monitor PR and BP closely... 

SALBUTAMOL BETAHISTINE 1 or prevents the bronchodilator effect Betahistine causes bronchoconstriction Avoid co-administration... 

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