Drugs, Nerves, & Neurotransmitters. Flashcards
Explain Loewi’s Experiment
Stim of the vagus nerve reduced donor AND recipient heart
Where is the most common site for pharmacological manipulation at synapses?
Receptor
Which PNS systems have 2 fibres? Which has one?
Sympathetic(short pre-ganglionic) and Parasympathetic(long pre-ganglionic) have 2 fibres, each with a ganglion.
Somatic has single fibre
Which two NTs are important in the PNS?
- Acetylcholine
2. Noradrenaline
L-DOPA which in the noradrenaline synthesis pathway is also clinically used for what?
parkinson’s treatment
Where do you get co-transmission of NTs?
in autonomic nerves to get variable responses in time.
How is ACh normally degrade
by AChE in the synapse
What sympathetic activity can noradrenaline NOT mimic?
ACh at sweat glands
ACh at adrenals
Acetylcholine (ACh) binds to what two receptors and what kind of receptors are they?
Nicotinic Receptors (ligand-gated ion-channel) Muscarinic Receptors (GPCR)
Noradrenaline (NA) binds to what two receptors and what kind of receptors are they?
a-adrenoceptors (GPCR)
B-adrenoceptors (GPCR)
What does Atropine do?
Blocks the effects of ACh in Cat Blood pressure
What happens if you inject Atropine plus a crapload of ACh?
increases blood pressure despite atropine due to adrenal gland activation
Receptors are all the same? T/F?
False. Polymorphism is rampant! Personalized medicine here we come.
ACh is released from all PNS nerves except:
Sympathetic post ganglionic terminal
Where are MuscR in the PNS?
Parasympathetic postganglionic terminal
What receptors to the organs innervated by sympathetic PNS have?
a/B adrenoreceptors
how is Noradrenaline inactivated?
recycled via neuronal high affinity uptake 1
Botulinum Toxin inhibits what?
Ach Release itself
What is the condition for increase blink response?
Blepharospasm.
How do you treat Blepharospasm?
Botox to the eye lids
What is the mechanism of action of Botulinum Toxin?
Protease that prevents fusion of SNARE proteins needed to release ACh.
What do you use to keep ACh in the synapse longer? how does it work?
Anticholinesterase, blocks the receptors for AChE
Which junction do Anti-ChE work?
Selectively between Neuromuscular junction and post-ganglionic parasympathetic junctions.
What is Donepezil?
Anticholinesterase used to treat Alzheimer’s as it enters the CNS well
Tell me about Edrophonium.
short acting drug used to Dx myasthenia gravis
Pyridostigmine/Neostigmine is used for what?
- Reverse non-depolarising neuromuscular blockers
2. Treat Myasthenia Gravis
What’s the Anticholinesterase used to treat Alzheimer’s
Donepezil
I forgot, what is the short acting drug used to Dx myasthenia gravis again?
Edrophonium
How do you treat Myasthenia Gravis with a Anticholinesterase?
Pyridostigmine/Neostigmine
What disease triggers an autoimmune response with complement at the Neuromuscular junction?
Myasthenia Gravis
Why would antibodies against AChR in Myasthenia gravis be a problem?
AChR gets cross linked, internalized and degraded destroying the morphology of the neuromuscular junction.
What’s a temporary treatment for Myasthenia Gravis?
ACh-Esterase Inhibitor
What’s a higher level treatment for Myasthenia Gravis?
Plasmaphoresis
Tell me about the Tensilon Test, which drug is used?
Edrophonium is used to dx myasthenia gravis, like they did with that ADORABLE golden retriever!! Dawww…..
Which neuro-receptor is a Ligand Gated Ion Channel?
Nicotinic AChR
Which neuro-receptor is a GPCR?
Muscarinic AChR
What is a partial agonist used to smoking cessation?
Varenicline
What can you clinically treat using nicotinic receptor agonists in the CNS?
Smoking cessation
Stimulating both branches of the ANS (Ganglion) is called what?
Nn Type
What is the Nm type?
contraction of skeletal muscle via somatic
Clinical uses of Nicotinic receptor Antagonists?
Pre-surgical skeletal muscle relaxants
What is a non depolarizing Nicotinic receptor antagonist used as a Pre-surgical skeletal muscle relaxants?
Tubocurarine/Vecuronium
What on earth is Haxamethonium?
Gaglion blocker Nicotinic receptor antagonist
I just had Tubocurarine/Vecuronium and now the surgery is done, how do reverse this?
Use neostigmine of course.
What is the acronym for Autonomic/Muscarinic agonist effects?
You are such a SLUD!! Salivation Lacrimation Urination Defecation
What else besides being a SLUD, do Autonomic/Muscarinic agonist effects have?
Sweating
bradycardia
bronchoconstriction
vasodilation
Your patient has Glaucoma! Help!! Your attending asked you to get the correct Autonomic/Muscarinic agonist. You go to the cart and choose:
Pilocarpine.
What is Pilocarpine?
Autonomic/Muscarinic agonist used to treat glaucoma
What are Autonomic/Muscarinic antagonist effects?
Reduced SLUD
Sometimes reduced tachycardia
Three anti-muscarinic drugs?
Atropine
Hyoscine
Ipratropium
I’m taking Ipratropium rectally for my COPD, cool huh?
You’re an idiot, you need to inhale that shit.
I’m so sick from that roller coaster give me something Doctor….
Suck on some Hyoscine!
What’s an anti-muscarinic to treat COPD?
Ipratropium
Optometrist puts some drops in your eye to dilate your pupils, what are those drops anyways?
Atropine
How would you use Atropine in anaesthesia?
to reduce secretions and produce bronchodilation
What class of drug is Atropine?
anti-muscarinic
You just got exposed to VX gas, a deadly nerve agent / acetylcholinesterase inhibitor. What do you need to inject into your heart RIGHT NOW?
Atropine.
What is Hyoscine?
Anti-muscarinic used to treat motion sickness.
What is the mechanism of Cocaine? Which receptor?
Noradrenaline receptor, blocks reuptake and keeps the cocaine in the synapses
What do the tricyclic anti-depressants do? what is it like?
blocks reuptake of Noradrenaline receptor. just like cocaine
what is Mao?what does it do?
Maonoamine oxidase metabolizes reuptaked NA
How do blockade NA metabolism
use a MAO inhibitor to prevent metabolism of NA and to increase leakage
What is a sympathomimetic?
calcium independent non-exocytotic release of NA. it ‘mimics’
3 examples of indirectly acting Sympathomimetics?
- amphetamine
- ephedrine (pseudoephedrine)
- Tyramine
What is tyramine?
indirectly acting Sympathomimetics
What is ephedrine?
indirectly acting Sympathomimetics
what is amphetamine?
indirectly acting Sympathomimetics
What a bad side effect of indirectly acting Sympathomimetics?
unwanted cardiovascular effects if patient taking MAO-inhibitors for depression.
what kind of receptors are alpha dn beta adrenoreceptors?
G-protein Coupled Receptors
Isoprenaline targets beta 1 or 2?
both!
salbutamol and more potent than isoprenaline for heart rate? T/F?
False.
Why choose salbutomol for airway relaxation when isoprenaline is clearly more potent
Salbutomol is a selective B2 and causes minimal heart rate change
Examplf os a Beta 2 agonist?
salbutamol
What is salbutamol used for?
Asthma Rx
what is the antagonist to isoprenaline?
propranolol
Name me the Beta 1 adrenoceptor agonist and antagonist
Agonist: Dobutamine
Antagonist: atenolol
Treat hypertension with a beta 1 adrenoceptor antagonist please
here’ some atenolol
what’s dobutamine used for?
heart failure (B1-adrenoceptor agonist)
What is atenolol used for?
hypertension
alpha adrenoceptor antagonist:
phentolamine
What do alpha-1 adrenoceptors cause?
vasoconstriction
I have nasal decongestand, what alpha-1 adrenoceptors agonist should I use?
phenylephrine
What is phenyl ephrine
alpha-1 adrenoceptors agonist for nasal congestion cause of nasal constriction effect
what is prazosin? what is it used for?
alpha-1 adrenoceptors antagonist for hypertension
treat my hypertension with a alpha-1 adrenoceptors antagonist please:
ok. one order of Prazosin, comin’ up!
