Name the 2 major drugs.
IPATROPIUM BROMIDE
Tiotropium
Name the drug class.
Quarternary amines
Hydrophilic (poor oral bioavailability and CNS penetration)
Describe the mechanism of action.
Bronchodilation (Competitive inhibition of muscarinic receptors prevents bronchoconstriction.)
A nonselective competitive antagonist at muscarinic receptors present in airways and other organs.
Relaxes smooth muscles of bronchi and bronchioles.
Blocks acetylcholine-induced stimulation of guanyl cyclase and reduces formation of cyclic guanosine monophosphate (cGMP), a mediator of bronchoconstriction.
Exhibits greater antimuscarinic activity on bronchial smooth muscle than on secretory (e.g., salivary, gastric) glands.
Tolerance to bronchodilating effect does not develop with prolonged use.
List the indication.
Ipatropium bromide (short-acting muscarinic antagonist/SAMA:
Short duration of action (SAMA)
Treatment of COPD grade I and higher
Acute management of refractory asthma
Tiotropium bromide (long-acting muscarinic antagonist/LAMA):
Longer duration of action(LAMA)
Long-term treatment of COPD (grade II and above)
What are drug interactions?
Anticholinergic drugs: ↑ risk of potentiation of effects
Antimuscarinic side effects (table).
Which muscarinic receptors are targeted in the airways?
M3 (Smooth muscle) in airway
List common adverse effects.
Bronchitis, upper respiratory tract infection,cough, and dryness of the mouth, throat, or tongue with ipratropium aerosol. Adverse effects resulting in discontinuance of nebulized ipratropium most frequently include bronchitis, dyspnea, and bronchospasm.
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