Flashcards in Just Drugs...Do Drugs, Give Hugs. Deck (29):
block Ach secretion at Pre-synaptic terminals by vesicles bc it cleaves SNARE proteins (Sna25/syntaxin and Synaptobrevin/Vamp)
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)
Decrease post-synaptic EPP amplitude by competition - therefore you need MORE Ach release to overcome and open ion channels
Name the depolarizing NMBA and its mechanism of action
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
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
Slowly degraded by AchE
Acts in the Heart (M2 receptors)
Muscarinic antagonist that does NOT interact with nicotinic receptors
used for post-operative ileus, GERD, or congenital megacolon
Also used to increase Urinary retention
Non-charged Muscarinic Agonist that is a natural alkaloid and used in the eye or to treat dry mouth
Non-charged Muscarinic antagonist that crosses into CNS and can cause amnesia
Used as a dermal patch to prevent Motion sickness (Prophylactically)
Charged, Non-selective muscarinic antagonist
USED in Anasthesia
M1 selective Muscarinic Antagonist
Used for gastric ulcers bc M1 in stomach
M1/M3 Muscarinic Antagonist used as an aerosolized spray in the lung
2 Drugs Used for M3 selective Muscarinic Antagonism of Detrussor Muscles?
2 shortest acting Anti-muscarinics used in the eye?
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
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?
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")
synthetic Catecholamine that only acts on B1 receptors
A1 adrenergic receptor antagonist
A1 Adrenergic receptor Agonist
A2 Adrenergic receptor Antagonist
A2 adrenergic receptor agonst
Metropolol and Atenolol
B1 adrenergic receptor Antagonists
B2 adrenergic receptor agonist
B3 adrenergic receptor Agonist