Source: Υπουργείο Υγείας (CY) Revision Year: 2020 Publisher: MEDOCHEMIE LTD, 1-10 Constantinoupoleos street, 3011 Limassol, Cyprus
Pharmacotherapeutic group: Selective beta-2-adrenoreceptor agonists
ATC code: R03AC02
Salbutamol is a direct-acting sympathomimetic agent which demonstrates relatively selective action on beta-2 adrenoceptors. The prime action of beta-adrenergic drugs is to stimulate adenyl cylase, the enzyme which catalyzes the formation of cyclic-3, 5-adenosine monophosphate (cyclic AMP) from adenosine triphosphate (ATP). Salbutamol relaxes the smooth muscle of the bronchi, uterus, and skeletal muscle vascular bed. Significant decreases in gastrointestinal motility have also been documented with salbutamol. In the treatment of reversible obstructive airways disease, salbutamol may also reduce chemical mediator release from pulmonary mast cells and improve mucociliary transport mechanisms.
Salbutamol is readily absorbed from the gastrointestinal tract. It is subject to first-pass metabolism in the liver and possibly in the gut wall; the main metabolite is an inactive sulfate conjugate. Salbutamol is rapidly excreted in the urine as metabolites and unchanged drug; there is some excretion in the faeces.
The bio availability of orally administered salbutamol is 50-85%.The total protein binding of the drug was found to be 10%.
Volume of distribution was 156 L ± 38 L which seemed likely to be more in men thus resulting in lower Cmax values and longer elimination half life.
Experimental studies showed that the drug exerts animal teratogenic or embryocidal effects, but there are no controlled studies in women were demonstrated.
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