Bitolterol mesylate (Tornalate) is a short-acting β₂ adrenergic receptor agonist used for the relief of

bronchospasm Bronchospasm or a bronchial spasm is a sudden constriction of the muscles in the walls of the bronchioles. It is caused by the release (degranulation) of substances from mast cells or basophils under the influence of anaphylatoxins. It causes di ...

in conditions such as

asthma Asthma is a long-term inflammatory disease of the airways of the lungs. It is characterized by variable and recurring symptoms, reversible airflow obstruction, and easily triggered bronchospasms. Symptoms include episodes of wheezing, cou ...

and

COPD Chronic obstructive pulmonary disease (COPD) is a type of progressive lung disease characterized by long-term respiratory symptoms and airflow limitation. The main symptoms include shortness of breath and a cough, which may or may not produce mu ...

. In these disorders there is a narrowing of the airways (bronchi and their ramifications) that carry air to the lungs. Muscle spasm and inflammation within the bronchi worsen this narrowing. Bitolterol relaxes the smooth muscles present continuously around the bronchi and bronchioles facilitating the flow of air through them. Colterol

Bitolterol is a

prodrug A prodrug is a medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug ...

colterol Colterol is a short-acting β2-adrenoreceptor agonist. Bitolterol, a prodrug for colterol, is used in the management of bronchospasm in asthma and chronic obstructive pulmonary disease Chronic obstructive pulmonary disease (COPD) is a typ ...

. It has a rapid onset of action (2–5 minutes) and may last up to 6–8 hours. The drug, alone or in co-administration with theophylline, doesn't show cardiotoxic effect. The U.S.

Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is respon ...

(FDA) approved bitolterol in December 1984. The drug was withdrawn from the market by Élan Pharmaceuticals in 2001.

References

Beta2-adrenergic agonists Benzoate esters Prodrugs Withdrawn drugs Tert-butyl compounds Phenylethanolamines 4-Tolyl compounds {{respiratory-system-drug-stub