bitolterol mesylate

Medically Reviewed on 5/20/2022

Generic Name: bitolterol mesylate

Brand Name: Tornalate (discontinued)

Drug Class: beta-2-adrenergic receptor agonists

What is bitolterol mesylate, and what is it used for?

Bitolterol is a bronchodilator used in the treatment of asthma. It is similar to albuterol (Ventolin).

Asthma is a disorder of breathing in which there is narrowing of the airways that carry air to the lungs including the bronchi. This narrowing is caused by muscle spasm and inflammation within the airways. Bitolterol relaxes the smooth muscles surrounding these airways, increasing the diameter and thus easing the flow of air through the airways.

Bitolterol probably does not affect inflammation in the lung either with asthma or other inflammatory lung disorders such as bronchitis. Nevertheless, if spasm of the airways occurs because of bronchitis, bitolterol may be useful therapy for the asthmatic component of the illness. Bitolterol is unique in that it is a "prodrug." It must first be converted by the body into its active form. Bitolterol has a rapid onset of action (2-5 minutes), and its effects may last up to 6-8 hours.

The FDA approved bitolterol in December 1984.


  • Do not administer bitolterol mesylate to children, as its safety for use in children under the age of 12 has not been established.

What are the side effects of bitolterol mesylate?

Side effects of bitolterol include:

Rare side effects of bitolterol include:

Worsening of diabetes and lowering of potassium have also been reported. In rare patients, inhaled bitolterol can paradoxically precipitate life-threatening bronchospasm.

What is the dosage for bitolterol mesylate?

  • The recommended adult dose for treating asthma is 2 inhalations every 8 hours.
  • Maximum dose is 2 inhalations every 4 hours or 3 inhalations every 6 hours.
  • This drug was not approved for use in children under 12 years old.

Which drugs interact with bitolterol mesylate?

  • Tricyclic antidepressants (for example, amitriptyline [Elavil, Endep]), monoamine oxidase inhibitors (for example, tranylcypromine) should not be combined with bitolterol because of their additive effects on the vascular system (increased blood pressure, heart rate, etc.). A period of two weeks should elapse between treatment with bitolterol and tricyclic antidepressants or monoamine oxidase inhibitors.
  • Use of bitolterol with other stimulant medications is discouraged because of their combined effects on heart rate, blood pressure, and the potential for causing chest pain in patients with underlying coronary heart disease.
  • Beta-blockers, for example, propranolol (Inderal, Inderal LA), block the effect of bitolterol and may induce bronchospasm in asthmatics. Bitolterol may cause hypokalemia (low potassium). Therefore, combining bitolterol with loop diuretics, for example, furosemide (Lasix), which lowers potassium levels in the blood, may increase the likelihood of hypokalemia.


Asthma is a chronic respiratory disease. See Answer

Pregnancy and breastfeeding

  • It's not known if bitolterol is excreted in breast milk or if there are any potential risks for fetal harm when administered to pregnant women.

What else should I know about bitolterol mesylate?

Do I need a prescription for bitolterol mesylate?
  • Yes
What preparations of bitolterol mesylate are available?
  • Inhaler: 0.37 mg/Inhalation; Solution for Inhalation: 0.2%
How should I keep bitolterol mesylate stored?
  • Bitolterol should be stored at room temperature, 15 C to 30 C (59 F to 86 F).


Bitolterol mesylate is a drug prescribed for the treatment of bronchospasms due to asthma and other respiratory illnesses. Side effects of bitolterol include nervousness, tremor, headache, palpitations, fast heart rate, elevated blood pressure, nausea, dizziness, heartburn, and nosebleeds. Bitolterol mesylate is not for use in children under the age of 12. Consult your doctor if pregnant or breastfeeding.

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Medically Reviewed on 5/20/2022
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