Maintenance treatment in COPD, including chronic bronchitis and emphysema.
Combined anticholinergic + β
COPD patients who require additional bronchodilation for airflow obstruction relief.
Nasal spray: Perennial rhinitis and colds.
Use in asthma
Anticholinergic bronchodilators do not have a labeled indication for asthma in the U.S.
If used in combined therapy, the effect is additive.
Special uses for asthmatic patients are:
- nocturnal asthma
- psychogenic asthma (P fibers involved?)
- asthma + glaucoma, angina or hypertension
- alternative to theophyllines
- acute severe episodes not responding well to β agonists
Mode of action.
Parasympatholytic bronchodilators are
antimuscarinic: they compete against ACH
for the muscarinic receptors located in the
parasympathetic neuroeffector sites, M3 in
Bronchoconstriction seen in COPD is partially caused by an
autonomic arc reflex which responds to stimuli such as
irritant aerosols, cold air, tobacco smoke, noxious fumes and
Muscarinic receptors in the lung
Facilitators of the cholinergic transmission. They "help" the nicotinic receptors at
the ganglionic synapse.
"Autoreceptors"; they inhibit further release of ACH.
Located in the bronchial smooth muscle, in contact with parasympathetic fibers. its blockade prevents bronchoconstriction.
Antimuscarinic agents block both M1 and M3 receptors.
IB is a non-selective antagonist of M1, M2
and M3 receptors.
Brand name: Atrovent
Dosage forms Adult dosage
MDI 18 μg/puff 2 puffs qid
SVN .02% 2.5 ml tid-qid
IB is a quaternary ammonium compound.
It is fully ionized (fig 7.1, p. 140) and doesn’t distribute well across lipid membranes, limiting its distribution mostly to the lung when inhaled.
It isn’t rapidly removed
from the aerosol site and doesn’t reach the CNS (less side
Onset of action: Within a few minutes
Peak effect: 1-2 hours
Half life: 6 hours (asthma) and 8 hours (COPD)
Brand name: Spiriva
Dosage form: DPI 18 μg/dose
Adult dosage: 18 μg daily
Longer half life
Low side effect profile
Greater FEV1 improvement than IB
Combined therapy: Albuterol + Ipratropium bromide
Brand name: Combivent
Dosage form: MDI (18 μg IB + 90 μg
Adult dosage: 2 puffs qid
Action sites are complementary
Mechanisms of action are different and complementary
Effect is additive (less amount of each, less side effects)
Pharmacokinetics are somewhat complementary
Combined therapy may prevent systemic steroid use.
MDI and SVN (common)
Pharyngitis Eye pain
Dyspnea Urinary retention
Upper respiratory infections
< The eyes must be protected from drug over-spraying
to prevent mydriasis. >