A review of the toxicology of salbutamol (albuterol)

Abstract

This paper reviews the published toxicology of salbutamol. Salbutamol is a relatively selective β2-Adrenoreceptor stimulant with rapid, potent bronchodilator activity and only minor inotropic or chronotropic effects. It was not found to be mutagenic. LD50 values and other acute studies indicated low toxicity. Findings published for repeat dose studies were mainly uneventful. Tachycardia and flushing of the skin were observed in dogs. There were several findings peculiar to the rat—growth of the salivary gland, enlargement of the Harderian gland, an increase in colloid in the pituitary, and mesovarian leiomyomas. Increases in heart weights associated with inflammation, hypertrophy of muscle fibres, focal myocardial necrosis and fibrosis were seen in rats. Malformation, in the form of cleft palate, was reported in mice but not in rats or rabbits. These treatment related effects reported for salbutamol are not compound-related but rather are class-related. They are an expression of pharmacological activity brought about by the excessive beta stimulant action of high dosage with the drug.

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Correspondence to Susan E. Libretto.

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Libretto, S.E. A review of the toxicology of salbutamol (albuterol). Arch Toxicol 68, 213–216 (1994). https://doi.org/10.1007/s002040050059

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Key words

  • Salbutamol
  • Albuterol
  • Toxicology review
  • β-Adrenergic receptors
  • β-Agonists