bitolterol

Action and Spectrum

Actions and Spectrum 

Bitolterol acts as a beta-2 adrenergic agonist, it targets beta-2 receptors in the smooth muscle of the bronchioles in the lungs. 

Activation of beta-2 receptors stimulates the enzyme adenylate cyclase, leading to increased intracellular levels of cyclic AMP (cAMP).

Drug Interaction

Adverse Reaction

Frequency not defined  

Closing of throat 

Lightheadedness 

Insomnia 

Diarrhea 

Dry mouth 

Tremor  

Nervousness 

Sweating 

Chest pain or irregular heartbeats 

Headache 

Dizziness 

Vomiting

Black Box Warning

Black Box Warning 

None

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Bitolterol is contraindicated in individuals with a known hypersensitivity or allergy to any of its components. 

Caution: 

• Caution is advised in individuals with pre-existing cardiovascular conditions. 
• Caution is advised in individuals with a history of seizure disorders. 

Pregnancy / Lactation

Pregnancy consideration: 

Pregnancy category: N/A 

Lactation: Excretion into human milk is unknown  

Pregnancy Categories:         

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.  

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women. 

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 

Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology  

Bitolterol stimulates beta-2 adrenergic receptors in the bronchial smooth muscle, leading to the activation of adenylate cyclase.  

This activation increases intracellular cyclic AMP (cAMP) levels, resulting in bronchial smooth muscle relaxation and subsequent bronchodilation. 

Pharmacodynamics 

Activation of PKA results in the phosphorylation of proteins involved in smooth muscle contraction. 

Phosphorylation leads to relaxation of bronchial smooth muscle, causing dilation of the airways. 

Pharmacokinetics 

Absorption   

Bitolterol is rapidly absorbed from the respiratory tract into the bloodstream. 

Distribution 

Bitolterol is distributed throughout the body via the systemic circulation. 

Metabolism 

Bitolterol undergoes rapid metabolism in the liver. 

Elimination and excretion 

Bitolterol is excreted in the urine. 

Adminstartion

Administration 

Bitolterol is administered via inhalation as an aerosol. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: bitolterol 

Why do we use bitolterol? 

Bitolterol is indicated for the relief of acute bronchoconstriction in individuals with asthma.  

Bitolterol may be used in the management of chronic obstructive pulmonary disease (COPD).