bitolterol mesylate

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.

Side effects of bitolterol include:

• nervousness,
• tremor,
• headache,
• palpitations,
• fast heart rate,
• elevated blood pressure,
• nausea,
• dizziness,
• heartburn, and
• nosebleeds.

Rare side effects of bitolterol include:

• allergic reactions, which may manifest as
  • rash,
  • hives,
  • swelling,
  • anaphylaxis, or
  • shock.

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

• 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.

• 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.

• 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.

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).