Autonomic Pharmacology Flashcards
[SNS/PNS: Eye]
mydriasis
sympathetic (alpha 1)
[SNS/PNS: Eye]
miosis
parasympathetic (M3)
[SNS/PNS: Heart]
Tachycardia
sympathetic (beta 1)
[SNS/PNS: genitourinary]
Detrusor muscle relaxation
sympathetic (beta 2)
[SNS/PNS: genitourinary]
Detrusor muscle contraction
parasympathetic (M3)
[SNS/PNS: genitourinary]
Trigone and bladder sphincter contraction
sympathetic (alpha 1)
[SNS/PNS: genitourinary]
Trigone and bladder sphincter relaxation
parasympathetic (M3)
[SNS/PNS: genitourinary]
Pregnant uterus relaxation
sympathetic (beta 2)
[SNS/PNS: genitourinary]
Pregnant uterus contraction (not sensitive)
parasympathetic (M3)
[SNS/PNS: genitourinary]
ejaculation
sympathethic (alpha)
[SNS/PNS: genitourinary]
erection
parasympathetic (erection)
[SNS/PNS: skin]
this has no effect on the skin
parasympathetic
[SNS/PNS: skin]
sympathetic but mediated by Ach
eccrine sweat glands
[Enzyme: product]
choline acetyltransferase
Ach
This drug inhibits choline transport
hemicholinium
A drug that is a ganglion blocker
Hexamathonium
Acetylcholine is transported into vesicles for storage by ____
vesicle-associated transporter (VAT)
the vesicle-associated transporter is inhibited by this drug
Vesamicol
this drug prevents the release of acetylcholine through the enzymatic removal of 2 amino acids from one or more fusion proteins
botulinum toxin
Physiologic release of Acetylcholine is triggered by the influx of this ion
calcium
this drug prevents the fusion of the vesicle membrane (containing acetycholine) to the terminanal membrane and opening pore into the synapse
Botulinum toxin
the enzyme that degrades acetylcholine to choline and acetate
acetylcholinesterase
The indirect-acting cholinomimetics inhibit this enzyme
acetylcholinesterase
What acetycholinesterase inhibitor is found in the liver?
Butyrylcholinesterase
What acetycholinesterase inhibitor is found in the plasma?
pseudocholinesterase
___ is the only DEPOLARIZING neuromuscular blocker
succinylcholine
___ us a short acting NON-DEPOLARIZING neuromuscular blocker
mivacurium
what drugs are metabolized by butyrycholinesterase/pseudocholinesterase?
succinylcholine, mivacurium
[Cholinoreceptors]
stimulation of the M1 cholinoreceptor will lead to what secondary messenger changes?
increase IP3/DAG
increase intracellular Ca
[Cholinoreceptors]
stimulation of the M2 cholinoreceptor will lead to what secondary messenger changes?
opening of K channels
decrease cAMP production
[Cholinoreceptors]
stimulation of the M3 cholinoreceptor will lead to what secondary messenger changes?
increase IP3/DAG
increase intracellular Ca
[Cholinoreceptors]
stimulation of the M4 cholinoreceptor will lead to what secondary messenger changes?
decrease cAMP
[Cholinoreceptors]
stimulation of the M5 cholinoreceptor will lead to what secondary messenger changes?
increase IP3/DAG
increase intracellular Ca
[Cholinoreceptors]
stimulation of the NN cholinoreceptor will lead to what secondary messenger changes?
Opening of Na and K channels, depolarization
[Cholinoreceptors]
stimulation of the NM cholinoreceptor will lead to what secondary messenger changes?
Opening of Na and K channels, depolarization
[Cholinoreceptors]
What are the cholinoreceptors seen in the CNS
M4, M5
[Cholinoreceptors]
the myocardium contains what type of cholinoreceptor?
M2
[Cholinoreceptors]
skeletal muscles contain what kind of cholinoreceptor?
NM
[Cholinoreceptors]
NN cholinoreceptor are seen where?
ganglion, neuronal type
[Cholinoreceptors]
the exocrine gland vessels contain what type of cholinoceptor?
M3
These are the types of drugs that mimics the action of acetylcholine?
cholinomimetics
[Sympa/Parasympa]
cholinomimetics exhibit a ___ efect
parasympathomimetic effect
[Direct-Acting Cholinomimetic]
uses during mitotic ocular surgery
Acetylcholine
[Direct-Acting Choline Esters]
carbamic acid esters that are resistant to hydrolysis of AChE
Bethanecol, Carbachol
[Direct-Acting Choline Esters]
used for postoperative and neurogenic ileus and urinary retention
bethanechol
[Direct acting muscarinic]
used for glaucoma, Sjogren Syndrome
pilocarpine
Acts by contraction of the iris sphincter
[Direct acting muscarinic]
Similar to pilocarpine but are M3 selective
cevimeline
[Direct acting muscarinic]
drug that facilitates the aqueous humor outflow
pilocarpine
[Direct acting muscarinic]
causes hypertension after a brief period of hypotension
pilocarpine
due to activation of sympathietic M1 receptors
[Direct-acting, nicotinic]
what is the fatal amount of nicotine?
40mg
Nicotine is associated with greater release of dopamine in the mesolimbic system
What is the treatment for muscarinic toxicity?
atropine
What are the symptoms of muscarinic toxicity?
S - salivation L - lacrimation U - urination D -defecation G - GI cramping E - emesis
Atropine addresses these
What are the nicotinic toxicity symptoms?
M - muscle cramps T - tachycardia W - weakness T - twitching F - fasciculations
Para, sympa, neuromuscular junctions are affected
[Indirect-acting cholinomimetics]
what is the mechanism of action of indirect acting cholinomimetics?
bind to cholinesterase and undergo prompt hydrolysis
[Indirect-acting cholinomimetics]
short acting, quatrenary amine, used in Tensilon test, cant cross the BBB
Edophonium
[Indirect-acting cholinomimetics]
intermediate-acting, treatment for myasthenia gravis and postoperative and neurogenic ileus
neostigmine
[Indirect-acting cholinomimetics]
similar to neostigmine byt has good lipid solubility, can enter the CNS due to its tertiary amine structure
physostigmine
[Indirect-acting cholinomimetics]
drug used to reverse the effects of neostigmine or edrophonium
atropine
What are the signs of organophosphate toxicity?
D - diarrhea U - urination M - miosis B - bradycardia B - bronchospasm E - emnesis L - lacrimation S - salivation S - sweating
What antibiotic may worsen patients with myasthenia gravis?
aminoglycoside antibiotics
[Long acting cholinesterase inhibitors/organophosphate]
insecticide, used in ectoparasite, scabies
Malathion
[Long acting cholinesterase inhibitors/organophosphate]
insecticide, harmful in humans, agricultural use
Parathion
[Long acting cholinesterase inhibitors/organophosphate]
also called nerve gas, used in warfare and terrorism
sarin, tabun, soman
Drug used in Alzheimer’s disease by amplifying endogenously released acetylcholine; available as transdermal patch
rivastigmine
Drug used in Alzheimer’s disease by amplifying endogenously released acetylcholine often combined with an NMDA antagonist (memantine)
Donepezil
An NMDA receptor blocker used for moderate to severe dementia
memantine
Notorious in causing hyperthermia; only addresses the nicotinic signs of toxicity
atropine
What are the effects of direct acting muscarinic agonis in heart rate, secretion, and smooth muscle?
- Decrease HR
- increase secretion
- increase smooth muscle contraction
[Treatment for cholinergic poisoning]
very high activity to phosphorous of organophosphate; reverses organophosphate poisoning by regenerating AChE
pralidoxime
[Treatment for cholinergic poisoning]
antidote for early stage cholinesterase inhibitor
pralidoxime
