Salbutamol in the 1980s

Abstract

Salbutamol (albuterol) is a beta 2-selective adrenoceptor agonist which accounts for its pronounced bronchodilatory, cardiac, uterine and metabolic effects. During the intervening years since salbutamol was first reviewed in the Journal (1971), it has become extensively used in the treatment of reversible obstructive airways disease. Numerous studies in this disease (including severe acute, childhood and exercise-induced asthma) have confirmed the bronchodilatory efficacy of salbutamol, and it has been shown to be at least as effective as most of the currently available bronchodilators, if not more effective. The onset of maximum effect of salbutamol is dependent on the formulation used and the route by which it is administered. In most patients inhaled salbutamol is a first-line therapy, since it offers rapid bronchodilation, usually relieving bronchospasm within minutes. Although oral salbutamol has often proved to be less efficacious than the inhaled formulation, it still affords clinically significant bronchodilation, and it is particularly useful in those patients unable to coordinate the use of inhalers. Parenteral formulations of salbutamol are generally reserved for the treatment of severe attacks of bronchospasm and they are one of the treatments of choice in these life-threatening situations. Studies of the concomitant use of salbutamol and other agents such as anticholinergics, methylxanthines and beclomethasone dipropionate have usually shown a complementary response in the majority of patients, as might be expected from the different mechanisms of action of these groups of drugs. Salbutamol is generally well tolerated and any side effects observed are a predictable extension of its pharmacology. Since the frequency of side effects is dose related, and therefore dependent on the route of administration, it is not surprising that they are much more common following intravenous and oral rather than inhalation therapy. Tremor, tachycardia and hypokalaemia are the most frequently reported adverse effects. After nearly 20 years of use, salbutamol is well established as a 'first-choice' treatment in reversible obstructive airways disease. Indeed, throughout this time many new bronchodilatory agents have been studied but none have proved more effective. Clinical evaluation of salbutamol in the treatment of premature labour, hyperkalaemia and cardiac failure awaits further studies, although to date some encouraging results have been reported.

Separation and determination of norepinephrine, epinephrine and isoprinaline enantiomers by capillary electrophoresis in pharmaceutical formulation and human serum

“…It is also used illegally as growth promoters in the liver stock industry [2]. Its residue can be toxic to humans.…”

Association of human serum paraoxonase‐1 with some respiratory drugs

“…Salbutamol sulfate, which has the phenolic group, is a most effective inhibitor compared with other drugs. It has been reported that phenol groups are among inhibitors of paraoxonase1 enzyme . The IC 50 values of tiotropium, varenicline tartrate, and ciprofloxacin hydrochloride (0.997, 1.665, and 4.822 μM, respectively) are smaller than that of the most known potent inhibitor (2‐hydroxyquinoline < 5 μM) of the paraoxonase .…”

“…Kinetic data indicated that the inhibition types of PON1 activity by ciprofloxacin hydrochloride and ampicillin trihydrate were found as mixed (Figure ). There are several studies in the literature about the interaction between antibiotics and hPON1 . Sinan et al demonstrated ciprofloxacin and sodium ampicillin inhibition efficacy of PON1, with IC 50 values of 0.313 and 27.51 mM, respectively.…”

“…It has been reported that phenol groups are among inhibitors of paraoxonase1 enzyme. [17,18] The IC 50 values of tiotropium, varenicline tartrate, and ciprofloxacin hydrochloride (0.997, 1.665, and 4.822 μM, respectively) are smaller than that of the most known potent inhibitor (2-hydroxyquinoline < 5 μM) of the paraoxonase. [19] Tiotropium bromide is a long-acting anticholinergic agent, developed expressly for therapy in patients who have chronic obstructive pulmonary disease (COPD).…”

Determination of salbutamol enantiomers in human urine using heptakis(2,3‐di‐O‐acetyl‐6‐O‐sulfo)‐β‐cyclodextrin in nonaqueous capillary electrophoresis

“…Salbutamol is a sympathomimetic drug with potent b 2 -adrenoceptor stimulating properties, widely used in the treatment of respiratory diseases and it is also applied as tocolytic agent [15]. This drug being administrated as the racemate, each enantiomer needs to be monitored separately.…”