Bitolterol Mesylate
Bitolterol Mesylate is a long-acting beta-2 adrenergic agonist (LABA) bronchodilator. It relaxes airway smooth muscle to improve breathing in patients with reversible obstructive respiratory conditions. This medication was used primarily for maintenance treatment of asthma and chronic obstructive pulmonary disease (COPD).
A bronchodilator medication used to treat asthma and COPD by relaxing airway muscles to make breathing easier.
Key facts at a glance
- RxNorm
- 47187
- Generic
- Bitolterol Mesylate
- Class
- pin-variant
- Brands
- —
- Availability
- rx
- Lactation
- unknown
- Routes
- —
- Forms
- —
- Regions
- US, EU, CN, JP
- Monitoring
- —
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Dosage and administration
- Usual dose
- 500mg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 250mg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 400mg daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
Overdose information
Special Populations
11 groupspregnancy
first trimesteravoid if possible
avoid use during pregnancy unless benefits outweigh risks
regular fetal monitoring
Use with caution and monitor for adverse effects.
pregnancy
second trimesteruse lowest effective dose
use only if clearly needed
fetal heart rate monitoring
Use with caution and monitor for adverse effects.
pregnancy
third trimesteruse lowest effective dose
monitor for potential uterine relaxation
uterine activity monitoring
Use with caution and monitor for adverse effects.
lactation
breastfeedinguse lowest effective dose
monitor infant for signs of beta-agonist exposure
observe infant for tremor or tachycardia
Use with caution and monitor for adverse effects.
geriatric
elderly 65 plusstart with lower dose
use with caution due to increased sensitivity
monitor heart rate and blood pressure
Use with caution and monitor for adverse effects.
pediatric_age
children 12 years and olderstandard adult dosing
approved for use in this age group
standard monitoring
pediatric_age
children 5 to 11 yearsmay require dose adjustment
use under physician supervision
monitor for growth effects with long-term use
Use with caution and monitor for adverse effects.
renal_impairment
mild to moderateno major adjustment needed
use with caution
monitor renal function
Use with caution and monitor for adverse effects.
renal_impairment
severereduce dose
use with close monitoring
monitor drug levels if available
Use with caution and monitor for adverse effects.
hepatic_impairment
mild to moderateno major adjustment needed
use with caution
monitor liver function
Use with caution and monitor for adverse effects.
hepatic_impairment
severereduce dose
use with close monitoring
monitor for adverse effects
Use with caution and monitor for adverse effects.
Statistics and clinical data
Drug class
Bronchodilator class classification
Common uses
Therapeutic indications
Approval status
Current market status
Mechanism of action
Molecular mechanism
Used for the treatment and maintenance of reversible obstructive airway diseases, including asthma and chronic obstructive pulmonary disease (COPD). Typically prescribed for patients requiring long-term bronchodilation.
As a beta-2 adrenergic agonist, bitolterol mesylate stimulates beta-2 receptors in bronchial smooth muscle, causing relaxation of the airways and improved airflow. It has a relatively long duration of action compared to shorter-acting bronchodilators.
This medication is not a rescue inhaler and should not be used for acute bronchospasm attacks. As with other LABAs, there may be cardiovascular considerations. Patients should use only as directed by their healthcare provider and should not discontinue abruptly without medical consultation. Note: This medication may have limited availability in some markets.
Contraindications
Conditions and patient states where this medication should be avoided or used with caution.
Do not use (1)
Known allergy to this medication or its components
Use caution (1)
Consult healthcare provider for benefits vs risks assessment
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed August 24, 2026. · Read our editorial policy