Pharmacology of peripheral neurotransmission Flashcards
Triethylcholine
Competitive substrate for choline acetyl trasferase
Makes false transmitter
Vesamicol
Inhibits vAChT for loading ACh into vesicles
alpha-bungarotoxin
binds nAChR at NMJ (not at ganglion) to block
Irreversible
beta-bungarotoxin
blocks ACh release via structural changes to pre-synaptic terminal
alpha latrotoxin
forms pre-synaptic Ca2+ channels
Increases ACh release
Trimethapham
competitive antagonist of nerve nAChR
Hexamethonium
use dependent antagonist of nerve nAChR
Suxamethonium
NMJ nM agonist (causes block) for tracheal intubation
Decamethonium
Depolarising blocker of NMJ nM
Curare and alpha bungarotoxin
NMJ nM antagonist to cause non-depolarising block and flaccid paralysis
Tetracycline
Chelates Ca2+ to inhibit NMJ
Aminoglycosides
Inhibit CaV to decrease ACh
BoTX
Cleaves synaptobrevin at NMJ cholinergic neutrons
TeNT
Cleaves synaptobrevin at inhibitory interneurons in CNS
Edrophonium
AChE used to diagnose myasthenia gravid and treat glaucoma
Neostigmine
AChE used to treat myasthenia gravis
Rivastigmine
Anticholinesterase
To treat Alzheimers
Sarin/Novichok
Irreversible AChE
Use atropine as antidote to cause tachycardia (via blocking M2 stimulation on the heart) and Pralidoxime to regenerating cholinesterase
Bethanechol
ACh agonist to stimulate detrusor muscle via M3
Pilocarpine
ACh agonist used to increase salivation and lacrimal secretion via action on M3
Atropine
Blocks M2 stimulation on heart to treat bradycardia
Ipratropium
Blocks M2 stimulation in asthma
Tropicamide
Blocks M3 stimulation on pupil to cause dilation (mydriasis)
Solifenacin
M3 selective blocker to inhibit detrusor contraction
Glycopyronium
Blocks M3 to stop excessive drooling
Phenylephrine
alpha1 selective agonist
Causes mydriasis and nasal decongestion
Clonidine
alpha2 selective agonist to inhibit transmitter reease
- Reduces BP
alpha-methyl DOPA
false transmitter with alpha2 selectivity
Isoprenaline
beta agonist
Bronchodilation via B2
Increased heart rate via B1
Dobutamine
beta1 agonist to increase CO
Salbutamol
beta2 agonist to relieve bronchospasm
Mirabegran
beta2 agonist to relax detrusor
Prazosin
alpha1 antagonist for treating hypertension
Yohimbine
alpha2 antagonist to reverse veterinary sedation
Propanolol
beta antaongist to decrease HR
Atenolol
beta1 selective antagonist to treat hypertension
alpha methyl tyrosine
pseudo substrate for TOH (rate limiting step of catecholamine synthesis)
Carbidopa
inhibits dopa decarboxylase
methyldopa
converted to false transmitter with highest affinity for pre-synaptic alpha2 recpetors
Reserpine
irreversibly binds VMAT2 to block uptake of catecholamines to load vesicles
Tetrabenzamine
reversibly binds VMAT2
Used in Huntington’s
Guanethidine
taken into nerves by NET and vesicles by VMAT2, depleting it of NA
Causes HR to fall
Dexamfetamine
taken into nerves by NET and into vesicles by VMAT2, in exchange for NA which leaks out so promotes release
Ephidrine
indirectly causes NA release and acts on post synaptic receptors
Nasal decongestant
Tricyclic antidepressants and cocaine
Block high affinity low capacity uptake 1 using NET
Steroid hormone blocking uptake
Blocks uptake 2 using EMT
Phenoxybenzamine
alpha antagonist to counteract large Adr released during adrenal gland removal