Autonomic Drugs Flashcards
direct acting muscarinic receptor agonists
pilocarpine
bethanechol
direct acting nicotinic receptor agonists
succinylcholine
varenicline
indirect acting reversible AchE Inhibitors
edrophonium (short acting) neostigmine (intermediate acting) pyridostigmine physostigmine donepezil
indirect acting irreversible AchE inhibitors
insecticides
AchE Inhibitor Drugs MOA
binds to activate site and inhibits AchE, undergoes hydrolysis and acidic portion slowly released. Prevents Ach from binding.
2 main types of reversible AchEI inhibitors
- alcohol (edrophonium)
2. carbamate (neostigmine)
Irreversible AchE Inhibitor Drugs MOA
enzyme active site is phosphorylated, requires synthesis of new AchE to overcome
Clinical Uses of AchE Inhibitors
- reverse NMB
- MG dx and tx
- glaucoma
- ileus tx
- postop urinary retention tx
- alzheimers tx
Autonomic AchE Inhibitor Drug Effects
- increased secretions
- increased GI motility
- bronchoconstriction
- bradycardia
- hypotension
- miosis
CNS AchE Inhibitor Drug Effects
used for dementia tx, toxicity can look like possible convulsions r/t excitation followed by a depression and unconsciousness
Edrophonium chemical structure, type of reversible AchE, effect, route of administration, onset, duration
quaternary amine (very polar) alcohol reversible blockade IV, IM onset 30-60sec duration 10 minutes
Neostigmine chemical structure, type of reversible AchE, effect, route of administration, onset, duration
quaternary amine, moderately polar carbamate hydrolyzed by AchE, labile covalent bond IV, PO? onset 10-30 min duration 2-4h
Physostigmine chemical structure, type of reversible AchE, effect, route of administration, onset, duration
tertiary amine, nonpolar (crosses BBB) carbamate hydrolyzed by AchE, labile covalent bond PO, IM, IV onset 3-8min duration 1 hour -useful for tx of anticholinergic toxicity
Cholinergic Crisis Pneumonic
DUMBELLS: Diarrhea, Diaphoresis Urination Miosis Bradycardia Bronchoconstriction Excitation (of skeletal muscle, CNS), Emesis Lacrimation Salivation Sweating
antidote for cholinergic toxicity
atropine
can give pralidoxime to regenerate AchE enzyme if you catch it early
Muscarinic Agonist Drug Effects CV, GI, bladder, lungs, secretions, eye
CV: decreased HR, decreased CO and arterial pressure, vasodilation via NO on endothelium of BV
GI: increased motility
Bladder: contraction
Lungs: bronchoconstriction
Secretions: increased
Eye: miosis, accomodati for near vision, decreased IOP
Muscarinic Agonist SE’s Pneumonic
SLUDGE Salivation Lacrimation Urination Diarrhea GI upset Emesis
Nicotinic M Antagonist Examples
Pancuronium Atracurium Vecuronium Rocuronium Cisatracurium
Nicotinic N receptor effects, uses, adverse effects
- stimulation of post ganglionic neuronal activity, CNS stimulation
- smoking cessation (NRT)
- CNS stimulation, skeletal muscle depolarization, hypertension, increased HR, n/v/diarrhea
Nicotinic M receptor effects, uses, adverse effects
- activated neuromuscular endplates, contraction
- depolarizing skeletal muscle paralysis
- fasciculations
cholinergic drug adverse effects and contraindication
- not indicated if GI/GU obstruction
- CV disease (HTN, increased HR)
- resp d/o (bronchoconstriction)
nonselective muscarinic antagonist examples
atropine
glycopyrrolate
scopalamine