Introduction
Illustrated mechanism of action
Examples of Medication Brand Names (with Images)
Indication
Side Effects
Precautions & Contraindications
Monographs
Reference
These drugs are administered as inhaled solutions or powders, often via nebulizers or inhalers, allowing direct delivery to the lungs with minimal systemic absorption and side effects
Besides bronchodilation, some inhaled anticholinergics have anti-inflammatory effects, reducing airway inflammation and hyperresponsiveness, which is beneficial in asthma
Inhaled anticholinergics are medications primarily used to treat chronic obstructive pulmonary disease (COPD) and sometimes asthma, by dilating the bronchial airways.
They work by blocking acetylcholine, a neurotransmitter that binds to muscarinic receptors on airway smooth muscles and gland cells, causing muscle contraction and mucus secretion.
By inhibiting these receptors, inhaled anticholinergics relax airway muscles, reduce mucus production, and improve airflow, easing symptoms like shortness of breath, wheezing, and cough.
>1. Normal Cholinergic Transmission:
Acetylcholine (ACh) is released from presynaptic neurons.
It binds to muscarinic receptors (M1–M5) on effector organs (e.g., smooth muscle, glands, heart).
This results in parasympathetic effects: salivation, bronchoconstriction, bradycardia, GI motility, etc.
> 2- Introduction of Anticholinergic Drug:
The drug enters the synaptic cleft.
Blocks muscarinic receptors by competitive inhibition (reversible binding).
Prevents ACh from binding to its receptor.
>3.Effect of Receptor Blockade:
Decreased parasympathetic activity.
Results in:
Dry mouth (↓ salivation)
Bronchodilation
Tachycardia
Decreased GI motility
Mydriasis (pupil dilation)
Urinary retention
Atrovent
Berodual
Ellipta
Spiriva Respimat
Indication
1. Chronic Obstructive Pulmonary Disease (COPD)
Primary indication:
Both short-acting (e.g., ipratropium) and long-acting (e.g., tiotropium, aclidinium, glycopyrronium) anticholinergics are used.
Help reduce symptoms, improve lung function, and reduce exacerbations.
2. Asthma
Adjunctive therapy, usually in moderate to severe asthma or when beta-agonists are not sufficient.
Ipratropium is sometimes used in acute exacerbations (especially in the emergency setting with SABA).
Long-acting muscarinic antagonists (LAMAs) like tiotropium can be used as add-on maintenance therapy in uncontrolled asthma.
3. Acute Bronchospasm
Often used in combination with beta-agonists (e.g., albuterol + ipratropium = Combivent) during acute exacerbations of asthma or COPD.
Common side effect:
→Dry mouth (most common)
→Cough
→Throat irritation
→Hoarseness
→Bitter taste
Less Common but Possible:
→Urinary retention, especially in older men with prostate issues
→Constipation
→Blurred vision (especially if the mist contacts the eyes)
→Nasal dryness or congestion (when used intranasally)
→Paradoxical bronchospasm (rare but serious)
Ocular Effects (if mist gets into the eyes):
→Pupil dilation (mydriasis)
→Increased intraocular pressure
Angle-closure glaucoma (in susceptible individuals).
1. Elderly patients:
More sensitive to side effects like dry mouth, constipation, urinary retention, confusion, and dizziness.
Increased risk of falls and cognitive impairment.
2. Glaucoma (especially narrow-angle):
May increase intraocular pressure — should be used cautiously after eye examination.
3. Benign Prostatic Hyperplasia (BPH) or urinary retention:
Can worsen symptoms by relaxing the bladder muscle, leading to urinary difficulty or retention.
4. Gastrointestinal disorders (e.g., paralytic ileus or obstruction):
These drugs slow down GI motility, which can worsen such conditions.
5 . Driving or operating machinery
May cause drowsiness, blurred vision, or dizziness, so caution is needed.