Just Drugs...Do Drugs, Give Hugs. Flashcards
Botulinum Toxin/Botox
block Ach secretion at Pre-synaptic terminals by vesicles bc it cleaves SNARE proteins (Sna25/syntaxin and Synaptobrevin/Vamp)
Hemicholinium
Interferes with Ach synthesis in pre-synaptic terminals by blocking high affinity Choline Transporter
Name the non-depolarizing neuromuscular blocking agents
How do they work?
D-tubocurarine (Curare - prototype)
Pancuronium
Cisatracurium
Vecuronium
Rocuronium
Decrease post-synaptic EPP amplitude by competition - therefore you need MORE Ach release to overcome and open ion channels
Competitive antagonist
Name the depolarizing NMBA and its mechanism of action
Succinyl Choline
Extended depolarization of post-synaptic AchR and cannot repolarize again preventing further activation AND inactivates NA channels - dual block
Degraded by Butrylylcholine-Esterase and NOT by AchE
Carbamylcholine (carbachol)
Muscarinic Agonist (although more nicotinic than muscarinic) that acts in the Gut, Eye and bladder
Used topically in the eye!!
Resistant to hydrolysis by AchE
Acetyl-beta-Methylcholine (Methacholine)
Muscarinic Agonist
Slowly degraded by AchE
Acts in the Heart (M2 receptors)
Bethanechol
Muscarinic antagonist that does NOT interact with nicotinic receptors
used for post-operative ileus, GERD, or congenital megacolon
Also used to increase Urinary retention
Pilocarpine
Non-charged Muscarinic Agonist that is a natural alkaloid and used in the eye or to treat dry mouth
Scopolamine
Non-charged Muscarinic antagonist that crosses into CNS and can cause amnesia
Used as a dermal patch to prevent Motion sickness (Prophylactically)
Atropine
Muscarinic Antagonist
Glycopyrrolate
Charged, Non-selective muscarinic antagonist
USED in Anasthesia
Pirenzepine
M1 selective Muscarinic Antagonist
Used for gastric ulcers bc M1 in stomach
Tiotropium
M1/M3 Muscarinic Antagonist used as an aerosolized spray in the lung
2 Drugs Used for M3 selective Muscarinic Antagonism of Detrussor Muscles?
Tolterodine
Darlfenacin
2 shortest acting Anti-muscarinics used in the eye?
Tropicamide
Cyclopentolate
Edrophonium (Tensilon)
Reversible AchE inhibitor
blocks AchE at a peripheral site (not catalytic triad) and temporarily inhibits
CHARGED! So does not cross BBB and no CNS effects
used to DX Myasthenia Gravis
What are Carbamates as a whole and how do they work?
Reversible AchE inhibitors
covalent bond formed with active site of enzyme and then carbamate cleaved to reverse inhibition….acts like Ach in AchE but much slower
Organophosphates
Irreversibly bind in active site of AchE to inhibit it
Inhibition MAY be reversible if enzyme has not “aged” with use of Oximes
Name the Carbamates. Which one is charged? Which one is not charged?
Physostigmine
Neostigmine
Pyridostigmine
Neostigmine is Charged and so does NOT cross BBB!
What are the Oximes? Name them. How are they used?
Pralidoxime and Obidoxime
Used to reverse Organophosphate inhibition of AchE (provided “aging” has not occured”)
Dobutamine
synthetic Catecholamine that only acts on B1 receptors
PRazosin
A1 adrenergic receptor antagonist
Phenylephrine
A1 Adrenergic receptor Agonist
Yohimbine
A2 Adrenergic receptor Antagonist
Clonidine
A2 adrenergic receptor agonst
Metropolol and Atenolol
B1 adrenergic receptor Antagonists
Albuterol
B2 adrenergic receptor agonist
Mirabegron
B3 adrenergic receptor Agonist
Name the 3 Indirect-Acting NE Releasers (non-catecholamines)
Tyramine
Amphetamine
Ephedrine
