ANSWERS WITH COMPLETE VERIFIED SOLUTION, UPDATED
2024.
PNS: cholinergic receptors
1. nicotinic (N): all ANS ganglia and medulla
2. nicotinic (M): neuromuscular junction
3. muscarinic: PNS organs
site of action: PNS rx
-synapse
-rx alters synaptic transmission (AcH)
SNS: Adrenergic receptors
-alpha 1, alpha 2, beta 1, beta 2
-also effects epi/norepi, dopamine
breakdown of AcH
-via AChE or MAO
1. AcH=reuptake into nerve cell
2. degraded by MAO
3. diffusion of waste out of cell
sites where Rx act/influence
1. receptor: rx binds to activate, enhance response, or block
2. synthesis of neurotransmitter: increases or decreases receptor activation/response
3. reuptake/termination cycle: blocking=prevents reuptake, inhibiting=prevents
breakdown of trasmitter
muscarinic receptors: M1 vs M2 vs M3
M1= CNS; salivary glands
M2= HEART ONLY
M3= bladder detrusor, eyes, salivary glands
*most muscarinic agonists (cholinesterase inhibitors) are non-selective; more side
effects!!
agonist vs antagonist
agonist=activate
antagonist=block
epinephrine: secreted and broken down where?
secreted = medulla
broken down = liver
muscarinic agonists/cholinesterase inhibitors
-MOA: prevents breakdown of AcH within SYNAPSE to make more available for
receptor sites
-Rx for: dementia + alzheimer's (both r/t excessive AcH breakdown), MG, neurogenic
bladder, GERD, IBS, post-op
-CI: hyperthyroidism
-ex: rivastigmine, donepizil (aricept), galatamine
Bethanechol (Urecholine)
, MOA: cholinesterase inhibitor; increases detrusor muscle tone to allow strong start to
voiding for clients with postoperative urinary hesitancy.
Precautions/interactions: PO ONLY ON EMPTY STOMACH; do not administer IV or IM
CI: hypotension or decreased CO, hyperthyroidism
SE: excessive saliva, increased urinary output
Cevimeline (Evoxac)
-MOA: muscarinic receptor agonist; admin PO only
-CI: narrow eye glaucoma d/t increased pupillary constriction
-also rx for sjorgen's
Pilocarpine (Pilocar)
-Direct-Acting Cholinergic Agonists; fewer SE, admin to eyes only; safe for
kids/pregnant/breastfeeding
-Use: constrict pupils (glaucoma; NOT NARROW ANGLE)
cholinesterase inhibitors/agonists: common SE
-bradycardia, hypotension
-miosis/blurred vision
-ABD cramping, diarrhea, increased gastric acid and salivation
-bronchoconstriction (AVOID IN ASTHMASTICS IF ABLE)
*most SE are reversible
myasthenia gravis (MG): Rx
-chronic disease characterized by muscle weakness and thought to be caused by a
defect in the transmission of AcH
-cholinesterase inhibitors used to increase AcH availability
-assess for swallowing prior to giving PO; may need to be parenteral
-can develop into MG crisis; treat w/ Neostigmine (AcH inhibitor)
treating cholinesterase inhibitor overdose
1. atropine: muscarinic antagonist
2. benzo to decrease seizure risk
3. pralidoxime: reverse binding on enzyme cholinesterase
**too much AcH=bradycardia, hypotension, flaccid muscles
muscarinic antagonists/anticholinergics
-MOA: block receptor to decrease availability of AcH or prevent reuptake
-SE: dry eyes, tachy, decreased sweating/increased temp, constipation, confusion,
dizziness
-s/s of toxicity=hot temp/skin/dry mucous membranes, increased anx/agitation,
decreased vision
-CI: hx prolonged QT, hx MG (can cause crisis), hx myocardial ischemia, BPH/urinary
retention, elderly (R/O dementia and alzheimer's), pregnancy (less blood flow to fetus).
*safe for children tho!