Cholinergic Agonists And Antagonists - Dr. Kruse Flashcards
M1 location
nerves
M2 location
heart, SM, nerves
M3
glands, SM, Endothelium
M4 location
CNS
M5 location
CNS
Nn location
Post-ganglionic cell body, dendrites, CNS
Nm location
skeletal muscles neuromuscular junction
eye contraction receptor
M3 and M2 = constriction of pupil by contracting sphincter of iris + ciliary muscle
lung Rs
M2 and M3 (bronchoconstriction)
GIGU Rs
M2 + M3
Direct -acting cholinergic agonists metabolized by what
acytylcholinesterase
nicotinic vs muscarinic R and absorption
- Nicotinic : uncharge and highly absorbed
2. Muscarinic : charged, highly absorbed
Direct -acting cholinergic agonists 4
- Ach
- Methacholine
- Carbachol
- Bethanechol
indirect-acting cholinergic agonists do what and 3 types
increase Ach
- alcohols (reversible)
- Carbamic acid esters (reversible)
- Organophosphates (irreversible)
Indirect -acting cholinergic agonists and absorption
alcohol + carbamic acid esters = charges + poorly absorbed
Organophosphates = uncharged and absorbed
parasympathetic affect on bladder
relax sphincter
contraction of detrusor
parasympathetic effect on sweat glands
secretion
parasympathetic stimulation on bronchial glands
stimulate
main uses for direct -acting cholinergic agonists
EYE
- glaucoma
2. esotropia (hypermetropic accomodative error)
main uses for direct -acting cholinergic agonists
GIGU
- post-ileus
- congenital megacolon
- urinary retention
- esophageal reflux
- Xerostomia , Sjögren syndrome
muscarinic stimulatants Side effects
N, V, D, urinary urgency, salvation, sweating, increase in glandular secretion = SLUDGE
muscarinic stimulants are contraindicated in
- asthma
- hyperthyroidism
- coronary insufficiency
- acid-peptic disease
Nicotine stimulants side effects
- nicotine poisoning : from cigs and insecticides
2. acute toxicity : CNS, skeletal muscle end plate depolarization , resp paralysis, htn, cardiac arrhythmias
tx side effects of direct -acting cholinergic agonists
- atropine
2. parenteral anticonvulsants (diazepam a benzodiazepine)
Acetylcholine is for what
intraocular during surgery = miosis (constriction of pupil)
Bethanechol is used for what
- urinary retention (can cause UTI if sphincter does not relax)
- heartburn
Carbachol is used for
- glaucoma
- intraocular surgery for miosis
- opthalmic examination
Cevimeline used for
dry mouth in sjögrens syndrome
Pilocarpine used for
- dry mouth in sjögrens syndrome, head/neck cancer
- miosis during surgery
- glaucoma
Varenicline (Chantix) MOA and for who
- stimulation and moderate release of mesolimbic dopamine (bind to Nn)
- for smoking cessation
Varenicline (Chantix) adverse effects
neuropsychiatric sx, agitation, depression, dark behavior
Indirect- acting cholinergic agonists main 6 uses
- Glaucoma
- Dementia
- Antidote to anticholinergic poisoning
- reversal of neuromuscular paralysis
- myasthenia gravis
- Ach.esterase inhibitor toxicity
Ach.esterase inhibitor toxicity sx
SLUDGE SX, EFFECTS NMJ, TX WITH ATROPINE
glaucoma and mAchR stimulation
aqueous humor outflow and reduces intraocular P
anticholinergic poisoning sx and from what
- vasodilation cutaneous , anhidrosis, hyperthermia, mydriasis, delirium, X urination
- atropine, anti-histamines, TCA, sleep aids,
most common cholinergic antagonist
atropine
anticholinergic agents 7 uses
- motion sickness
- GI
- dilation eye
- respiration problems
- urinary problems
- cholinergic poisoning
- movement disorder
parkinsons disease drug to help
anti-cholinergic = reduce tremors, most effective is standard dopamine tx
motion sickness drug
anticholinergic agents = scopolamine
anesthesia
anticholinergic = atropine blocking vagal reflexes, from surgical manipulation of organs
= given with neostigmine (AchE Inhibitor)
when do you need anticholinergic on eye
prolonged eye dilation in
1. LASIK surgery,
(a-adrenergic receptor agonist is shorter acting and less adverse effects)
2. uveitis and iritis prevention
lungs and anticholinergic agents
- Ipratropium and tiotropium
2. for COPD mostly and asthma
anticholinergic agents and GI
travelers D, Lomotil (atropine + diphenoxylate)
anticholinergic agents GU
- urinary urgency (minor inflammatory bladder disorder)
2. agents acting on M3**
4 drugs acting on M3 for the GU
- oxybutynin : dry sx side effects
- Darifenacin
- Solifenacin
- Tolterodine
insectacide poisoning does what and how to tx
cholinesterase inhibitor
=tx with anticholinergics (anti-Muscarininc = ATROPINE)
= no effect is you treat with anti-nAchR (pralidoxime)
anticholinergic agents adverse effects
- dry as a bone
- blind as a bat
- red and beet
- mad as a hatter
- hot has a hare
anticholinergic agents contraindicated in what 3 pts
- glaucoma
- prostatic hyperplasia
- acid-peptic disease