Cholinergic & Anticholinergic Flashcards
located in the CNS and gastric parietal cells
M1
increase gastric acid - HCL
CNS excitation
M1
M1 and M3 have what mechanism
Gq - IP3, DAG - increase in Ca2+ concentration
M2 mechanism
Gi - inhibits adenyl cyclase, decrease cAMP and opening of K+ channel
located in heart - SA and AV node, presynaptic terminal
M2
decrease rate of impulse generation, velocity of conduction decreased, contractility decreased
M2
located in smooth muscles in exocrine glands, GIT, genitourinary system, constrictor pupilae, glands
M3
increase in exocrine secretion, smooth muscle contraction, miosis
M3
binds to activate endothelial NO synthase, vasodilation due to release fo EDRF - increases cGMP to dephosphorylate myosin LC
acetylcholine
M3 stimulation increases bowel movements and bladder contractions - emptying
bethanechol
treats paralytic ileus - reduced bowel movements; urinary retention
bethanechol
SE: CNS stimulation, miosis, bradycardia, bronchoconstrictor, accommodation of near vision, abdominal cramps, flushing, salivation
bethanechol
Contraindications: asthma, peptic ulcer, MI
bethanechol
increases aqueous humor outflow; increases peristalsis and treats glaucoma
carbachol
stimulates bronchial construction and used in diagnosis of asthma
methacholine
M3 stimulation - increase salivation, lacrimation, increase aqueous humor outflow (glaucoma); ciliary muscle - contraction
pilocarpine
used to treat xerostomia, stimulates salivary secretion in post op, open angle glaucoma, iris-cyclitis adhesions
pilocarpine
selective muscarinic: found in mushrooms, responsible for cholinergic symptoms in mushroom poisoning
muscarine
neurally occurring tertiary amine that is well absorbed and crosses BBB
nicotine
synthetic partial agonist at alpha 4 beta 2 subtype nicotinic receptors used in the treatment of smoking cessation
varenicline
stimulates M3 (salivary glands) - increase secretion; used to treat xerostomia in chemo patients and sjogren syndrome
cevimeline
M3 - enters CNS; penetrates cornea
Treats: open angle glaucoma and atropine overdose antidote (IV-Belladonna poisoning)
physiostigmine
shortest duration of action
Dx: of MG and differentiate between Myasthenic and Cholinergic crisis - Tension test
edrophonium
crisis in which patient gets better
Myasthenci crisis
crisis in which patient gets worse because their already on AchE inhibitors
Cholinergic crisis
used in acute myasthenia gravis cases; atony of bladder, paralytic ileus, reversible skeletal muscle blocker
dont use in glaucoma
neostigmine
used in treatment of long term MG
DOA: 6 hrs
pyridostigmine
increase CNS Ach
used to treat Alzheimers
Danoprezil
rivastigmine
galantine
tacrine
increase aqueous humor outflow
used to treat glaucoma
irreversible Ache inhibitor
ecothoiophate
irreversible Ache inhibitors
organophosphates
malathion parathion sarin tabun soman voltile X
Treatments of OP poisoning
atropine - muscarinic symtoms
pralidoxime (2-PAM) - antidote AchE reactivator for nicotinic symptoms
DUMBBELLS (OP SE)
diarrhea urination miosis bradycardia bronchospasm emesis lacrimation lethargy salivation
used to control head lice
carbaryl
inhibits choline transporter
hemicholinium
inhibits Ach from entering into vesicle
vesamicol
inhibits SNAPS
botulinum
blocks M2; M3 and M1 anti motion sickness
atropine
used in treatment for OP poisoning, cholinergic poisoning, mushroom poisoning, 2nd degree HB and bradycardia
atropine
M1 and M3 blocker; absorbed through skin
scopolamine
used in motion sickness and nausea associated with opioid analgesia, and to reverse central Nn receptors in cholinergic poisoning
scopolamine
decreases secretion, relax smooth muscle of bronchi and bronchioles, decrease airway resistance, bronchodilation
ipratropium
tiotropium
used to treat exercise induce bronchospasm, chronic bronchitis, asthma, COPD
ipratropium
tiotropium
produce mydriasis
cyclopentolate
tropicamide
homatropine
used in measurement of refractory error
tropicamide
ophthalmic exam
cyclopentolate
break adhesion iris and anterior surface of lens
homatropine
decrease secretions of GIT, relaxation of smooth muscle, decreased GI motility and peristalsis
dicylomine
flavoxate
glycopyrrolate
used in irritable bowel syndrome
dicylomine
used in pre op medication to reduce salivary and respiratory secretions and in post op in combo with neostigmine to reverse effects of non depolarizing skeletal muscle relaxants
glycopyrrolate
blocks M3 helps in urine retention in adults and children
oxybutinin
tolterodine
derifenacin
used in antispasmodic effects seen in overreactive bladder and in urinary incontinence; detrusor hyper reflex; enuresis
oxybutinin
tolterodine
derifenacin
decrease secretion of GIT, relax smooth muscle of GIT, decrease GI motility and peristalsis
pirenzepine
treats peptic ulcers
pirenzepine
work centrally in the brain
used in Parkinson’s dz - helps decrease salivation, spasticity, and tremors;
treats drug induced extra pyramidal reactions
trihexyphenidyl
benztropine
biperiden
treatment for anticholinergic overdose
physostigmine
abolish baroreceptor reflex HR change; prevents PANS and SANS stimulation
mecamylamjne
hexamethonium
trimethoprim
