Anticholinergics Flashcards
2 types of anticholinergics
antimuscarinics and ganglionic blockers
action of muscarinic AChR antagonists ( antimuscarinics)
interrupts parasympathetics influence in various tissues
- predominant autonomic tone is parasympathetic ( except: vasculature and sweat glands)
- blocking mAChR-> premits sympathetic influence to become predominant
- effects will be typical of sympathetic activity
how do ganglionic blockers act
antagonising the neuronal nAChRs present on the primary ganglionic cell in all autonomic ganglia ( but arent all antagonists)
- effects are sympathetic-like ( not sweat glands or vasculature) due to blocking all autonomic influence
pharm effects of prototypical anti-muscarinic atropine - on ocular a
ocular-> 1. relaxes iris sphinicter, symp tone predominates on radial muscle
- blocks accommodation -relaxes ciliary muscle-> increases tension on ligaments -> flattens lens
- inhibits lacrimation
pharm effects of prototypical anti-muscarinic atropine - on cardiac
- standard dose increase heart rate and atrioventricular conduction by blocking vagal input
- very low doses may initially decrease hr by first blocking presynaptic receptors
pharm effects of prototypical anti-muscarinic atropine - on respiratory
- bronchial smooth muscle relaxation and dilation
2. inhibit secretions
pharm effects of prototypical anti-muscarinic atropine - on GI
- decreases lower esophageal muscle tone
- relaxes GI tones, prolonging intestinal transit time
- inhibits gastric acid secretions
pharm effects of prototypical anti-muscarinic atropine - on urinary
- relaxes detrusor muscle of the bladder causing urinary retention
pharm effects of prototypical anti-muscarinic atropine - on CNS
1, atropine and scopolamine are tertiary amines
- scopolamine is more sedating than atropine
- atropine-> 1st stimulation followed by sedating effect
- high doses can cause confusion and or hallucinations
other: inhibits sweating and could possibly lead to hyperthermia-> causes cutaneous vasodilation
major clinical uses of atropine
long lasting mydriasis, pharm path to treat amblyopia, cycloplegia , sinus bradycardia and av block, decrease of salivary and respiratory secretions -> prevents airway obstruction
, intestinal spasms and pain , decrease gastric acid secretions, reversal of muscarinic or AChE inhibitor poisoning, prevention of muscarinic side effects in pts receiving AChE inhibitors and neostigmine to reverse nerve block, mixed with diphenoxylate (opioid agonist) its an anti-diarrheal
scopolamine
anti-mus
motion sickness, side effect - drowsiness
tropicamide , cyclopentolate, homatropine
anti-mus
fast but short acting mydriatic agent
may be combined with alpha adrenergic agonist
ipratropium
anti-mus
quaternary amine-> inhalled
bronchodilator
COPD
TIOTROPIUM- similar but longer acting
tolterodine
ant-mus
managment of overactive bladder ( increased freq, nocturia, incontinence)
-fewer side effects_> dry mouth and blurred vision
contraindicated for individuals w/ narrow-angle glaucoma
dicyclomine
anti-mus
releaxes intestinal smooth muscle
IBS-> symptoms