Anticholinergics

Question 0

Mode of action

Answer 0

Acts on muscarinic receptors M1, M2, M3

M1- parasympathetic ganglia, nasal submucosal glands (secretion in nose)
M2- Heart, postganglionic autoreceptor (inhibit acetylcholine release)
M3- Smooth muscle, glands (bronchoconstriction, secretion in nose)

Question 1

Clinical indications

Answer 1

COPD maintenance (combined with B-agonist)
or
Severe asthma that does not respond well to B-agonist)
or
Allergic and nonallergic perennial rhinitis and common cold

Question 2

Antimuscarinic effects

Answer 2

HR-increase 
Eye(pupil)-dilate, (lens)-flattened 
Mouth- dry
tear formation- inhibit
urinary- retention
GI- antidiarrheal 
Mucociliary- slow
Broncho- dilate

Question 3

Structure of anticholinergics and its effect on activity

Answer 3

Tertiary ammonium- lipid soluble, easily absorbed (more effects)
-Atropine

Quaternary ammonium- not lipid soluble, not easily absorbed, less effects.
-Ipratropium, tiotropium

Question 4

Ipratropium bromide

Answer 4

ATROVENT
Quaternary
Inhibit M1, M2, M3
Duration 4-6 hrs

Question 5

Tiotropium bromide

Answer 5

SPIRIVA
Quaternary
Selective for M1, M3
Once daily, 24hr duration

Question 6

Aclidinium bromide

Answer 6

TUDORZA
Quaternary
Inhibition of M3
Twice daily

Question 7

Combination drug for COPD

Answer 7

Additive effect

Ipratropium and albuterol (COMBIVENT) taken with MDI Respimat