Autonomic Pharmacology Flashcards
Which enzymes synthesizes Ach by combining acetyl CoA + choline?
ChAT
True or False: the rate limiting step in Ach synthesis is ChAT.
False! it’s by the amt of choline thats available.
Which pump pumps chiline into presynaptic terminal?
Na/Choline transporter
What drug inhibits the Na/Choline transporter, thus increasing [choline]synapse?
hemocholinium
What is the transporter to get Ach into the secretory vesicle?
H/Ach antiporter
Which drug inhibits the H/Ach antiporter?
Vesamicol
The increase concentration of which ion causes the secretory vesicles to fuse with the terminal membrane of the presynaptic terminal?
Ca++
What is the syndrome that blocks the uptake of Ca++ into the cytoplasm, thus inhibiting Ach release?
Lambert-Easton syndrome
Which toxin blocks exocytosis of presynaptic vesicles, thus blocking the release of Ach?
Botulinum toxin
Which AA are adrenergic hormones synthesized from?
Tyr
Which transporter transports NE into the presynaptic terminal to be released?
NET
Tell me the steps of the synthesis of Tyr –> NE
Tyr –TH–> L-DOPA –> D –> NE –> E
Which enzyme is the RLS of the adrenergic synthesis pathway?
Tyrosine Hydroxylase (TH)
Tryosine degraded only to Dopamine in the cytoplasm, so how is dopamine taken up into secretory vesicles to be potentially further converted to NE/E?
VMAT transporter
Which drug inhibits VMAT, therefore decreasing release of adrenergic hormones?
Reserpine
Which drug inhibits NET, therefore increasing NE in the synpase?
COCAINE
Which drug inhibits tyrosine hydroxylase to make adrenergic hormones?
a-methyltyrosine
For what condition is a-methyltyrosine used to treat?
HTN with pheochromocytoma
True or False: reserpine isnt used any more cuz the cell can just make new vesicles with VMATs.
True
What is the action of tyramine to inhibit NE release from cells?
takes the place of NE in vesicles
“tyramine is MEAN”
Guanethidine act like tyramine by taking the place of NE in vesicles, thus decreasing what cardiovascular factor?
Cardiac output
What are the 3 actions of amphetamine to treat depression and nercolepsy?
- displaces endogenous catecholamines
- weak inhibitor of MAO
- blocks NET reuptake
Ephedrine/pseudoephedrine stimulate beta receptors, thus treating which condition?
nasal/sinus congestion
u can also make meth from this. thanks breaking bad.
Methylphenidate is a structural analogue of amphetamine, and is used to treat what condition?
ADHD
What does tricyclic antidepressants block to treat depression?
NET and serotonin reuptake
This nonselective MAOi causes more catecholamines to be present in the presynaptic vesicles.
Phenelzine
Stimulation of a1-receptors causes what to the BP?
rise cuz it increased peripheral vascular resistance
Stimulation of a2-receptors causes what to the BP?
lowers by acting on brainstem centers
Stimulation of B1-receptors causes what to the BP?
increase HR and force of cardiac muscle contraction –> increase BP
Stimulation of B2-receptors causes what to the BP?
causes relaxation of vascular, bronchial, and GI smooth muscle –> decrease BP
M1- location
autonomic ganglia, viscera, CNS
M1- actions
EPSPs
M2- location
heart
M2-action
slows, decreases contractility
M3- location
smooth muscle
M3- action
constriction
a1- location
vascular smooth muscle, gut smooth muscle
a1- action
vasoconstriction, relaxation of gut
B1- location
heart
B1- action
increase chronotropy and ionotropy
B2- location
smooth muscle, liver, SkM
B2- action
SM relaxation, glycogenolysis
What does tetrodotoxin block to cause fatal paralysis?
NmAchR
What does DUMBBELSS stand for to describe Ach actions?
diarrhea, urination, miosis, bradycardia, bronchoconstriction, excitation, lacrimation, salivation, and sweating
Which cholinomimetric drug ios selective for cardiovascular muscarinic R’s to Dx asthma?
methacholine
What condition does carbachol treat?
glaucoma
Which cholinomimetric drug is used to increase urinary and GI motility, esp after surgery since it only targets muscarinic receptors?
Bethanechol
Cevimeline and Pilocarpine are cholinomimetric drugs that arre used to treat what condition?
Xerostomia in Sjorens syndrome
This nicotinic agonist is used to induce a neuromuscular blockage in surgery and intubation.
Succinylcholine
How do direct acting cholinomimetric agents increase Ach response?
by diorectly acting on the Ach R
So how do indirect acting cholinomimetric agents increase Ach response?
inhibit AchE, thus inc the [Ach]synapse
What are the actions of organophosphates to cause acute Ach toxicity?
strong AchE inhibitor
Which drug can u give for acute organophosphate poisonings?
Pralidoxime (PAM)
What are the Sx of atropine OD?
anti-DUMBBELS
cuz its a muscarinic antagonist
Which indirect acting cholinomimetric to counter the effects of an atropine OD?
pilocarpine
Mecamylamine and trimethaphan are used to treat HTN with acute aortic dissection by blocking what?
Nicotinic Ach R’s in ganglions
Which drug is used to produce mydriasis and cycloplegia?
atropine
Which AchE inhibitor is used to treat parkinsons?
rivastigmine
Which muscarinic R antagonist is used to treat PUD?
methscopolamine
Which muscarinic R antagonist is used to treat asthma?
Tiotropium
Which G-subunit pathway does a1 receptors act on?
Gq
Why are a2 receptors located on presynaptic sympathetic neurons?
to fxn as autoreceptors to mediate feedback inhibition of sympathetic transmission
All 3 beta (B) receptors act on what G-protein subunit pathway?
Gs
Methoxamine is an a1 agonist that is used to Tx what condition?
shock
Phenylephrine, oxymetazoline, and tetrahydrozoline are a1 agonists that are used to Tx what conditions?
nasal congestion and opthalmic hyperemia
Clinidine and methyldopa are a2 agonists that are used to Tx what condition?
HTN by acting in CNS
Isoproterenol is a nonselective B agonist that is used to treat what?
HTN by lowering diastolic BP
Metaproterenol, terbutaline, and albuterol are B2 agonists that are used to treat what?
acute bronchospasm
Epinephrine is more selective towards which receptors, alpha or beta?
beta
thats why we have epi-pens with Epi, cuz it acts mainly on B2
Propanolol is an antagonist to which B-receptors?
nonselective to B-receptors, so B1 and B2
Atenolol is an antagonist to which B-receptors?
B1
Esmolol is an antagonist to which B-receptors?
B1
When is esmolol given?
in acute HTN states (given IV)
Nadolol is an antagonist to which B-receptors?
Non-selective
