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Bitolterol Mesylate

Pronouncation: (by-TOLE-ter-ole MEH-sih-LATE)
Class: Sympathomimetic

Trade Names:
- Aerosol 0.8% (delivers 0.37 mg/actuation)
- Solution for inhalation 0.2%


Relaxes bronchial smooth muscle through beta-2 receptor stimulation.



Bitolterol, a prodrug, is hydrolyzed by esterases in tissues and blood to active moiety colterol.


Primarily excreted in the urine as metabolites.


2 to 3 min.


At least 6 h.

Indications and Usage

Prevention and treatment of reversible bronchospasm associated with asthma or other obstructive pulmonary diseases.


Standard considerations.

Dosage and Administration

Acute Bronchospasm
Adults and Children older than 12 yr of age

Oral inhalation 2 inhalations at interval of 1 to 3 min, followed by third inhalation if necessary.

Prevention of Bronchospasm
Adults and Children older than 12 yr of age

Oral inhalation 2 inhalations every 8 h, not to exceed 3 inhalations every 6 h or 2 inhalations every 4 h.

Solution for Inhalation

Administer during a 10- to 15-min period.

Continuous flow nebulization

1.5 to 3.5 mg (0.75 to 1.75 mL volume) 3 to 4 times/day with an interval of at least 4 h between treatments. Max daily dose, 14 mg.

Intermittent flow nebulization

0.5 to 1.5 mg (0.25 to 0.75 mL volume) 3 to 4 times/day with an interval of at least 4 h between treatments. Max daily dose, 8 mg.

Drug Interactions

None well documented.

Laboratory Test Interactions

May cause decreased potassium level.

Adverse Reactions


Palpitations; tachycardia; irregular pulse; hypertension; angina.


Tremor; lightheadedness; dizziness; nervousness; headache; tiredness.


Throat and mouth irritation.


Nausea; vomiting.


Cough; increased chest discomfort; dyspnea; bronchospasm.



Category C .




Safety and efficacy in children younger than 12 yr of age not established.


Lower doses may be required.

Labor and Delivery

May inhibit uterine contractions and delay preterm labor.

Cardiovascular disorders

Toxic symptoms may occur.

CNS effects

Drug may cause CNS stimulation; use cautiously in patients with history of seizures or hyperthyroidism.

Diabetes mellitus

Dosage adjustment of insulin or oral hypoglycemic agent may be required.

Excessive use

Paradoxical bronchospasm and cardiac arrest have been associated with excessive inhalant use.


May occur.

Combined therapy

Do not use 2 or more beta-adrenergic aerosol bronchodilators simultaneously because of the potential of additive effects. Do not use as a substitute for oral or inhaled corticosteroids.



Exaggerated adverse reactions, such as tremors, tachycardia, seizures, hypokalemia, anginal pain, and hypertension.

Patient Information

  • Ask patient to demonstrate correct use of inhaler. It may be necessary to repeat instructions and demonstrations more than once. Consider use of spacing device.
  • Explain that tolerance may occur with prolonged use, but temporary cessation of drug usually restores its original effectiveness. Instruct patient to notify health care provider if medication is ineffective.
  • Warn patient to avoid excessive use, which can lead to adverse reactions or loss of effectiveness.
  • Instruct patient to rinse mouth with water or commercial mouthwash after use to remove residue and reduce irritation.
  • Tell patient to store inhaler at room temperature, away from excessive heat or cold.
  • Warn patient receiving concurrent corticosteroid therapy not to stop or reduce medication without consulting health care provider, even if patient feels better.
  • Instruct patient to wash inhaler daily with warm water and to dry thoroughly.
  • Caution patient to avoid getting aerosol spray in eyes.
  • Instruct patient to report the following symptoms to health care provider: palpitations, chest pain, muscle tremors, dizziness, increased nervousness, headache, flushing, breathing problems, difficult urination.