Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2020 Publisher: Norton Healthcare Ltd., T/A IVAX Pharmaceuticals UK, Ridings Point, Whistler Drive, Castleford, West Yorkshire, WF10 5HX, United Kingdom
Pharmacotherapeutic group: Selective beta2 adrenoceptor agonists.
ATC Code: R03AC02
At therapeutic doses salbutamol acts on the β2-adrenoceptors of bronchial muscle with little or no action on the β1-adrenoceptors of cardiac muscle.
Salbutamol provides short acting (4-6 hour) bronchodilatation with a fast onset (within 5 minutes) in reversible airways obstruction.
Paediatric clinical studies conducted at the recommended dose (SB020001. SB030001. SB030002) in patients <4 years with bronchospasm associated with reversible obstructive airways disease, show that Salbutamol CFC-Free Inhaler has a safety profile comparable to that in children >4 years, adolescents and adults.
Salamol Easi-Breathe CFC-Free Inhaler has been shown to be therapeutically equivalent to salbutamol metered dose inhaler formulated with chlorofluorocarbon (CFC) propellants.
Salbutamol is readily absorbed from the gastro-intestinal tract.
Salbutamol is subject to first pass metabolism in the liver, about half is excreted in the urine as an inactive sulfate conjugate following oral administration (the rest being unchanged salbutamol). Salbutamol does not appear to be metabolised in the lung, therefore its behaviour following inhalation depends upon the delivery method used which determines the proportion of inhaled salbutamol relative to the proportion inadvertently swallowed.
The plasma half-life has been estimated to range from about two to seven hours, the longer values have followed aerosol inhalation.
Toxicological studies in rats and dogs with salbutamol formulated in propellant HFA-134a have shown a comparative safety profile to the current CFC-containing products. The adverse effects noted at high doses were consistent with the known effects of salbutamol inhalation.
Toxicological effects of propellant HFA-134a consisted of narcosis and a relatively weak cardiac sensitising potential at very high exposure concentrations only. Safety margins of 2200, 1314 and 381 for mouse, rat and dog with respect to humans have been observed.
Salbutamol has been used clinically for over 20 years and its safety and efficacy have been proven.
Please see Sections 4.3 to 4.9 for further guidance.
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