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Flashcards in Just Drugs...Do Drugs, Give Hugs. Deck (29):
1

Botulinum Toxin/Botox

block Ach secretion at Pre-synaptic terminals by vesicles bc it cleaves SNARE proteins (Sna25/syntaxin and Synaptobrevin/Vamp)

2

Hemicholinium

Interferes with Ach synthesis in pre-synaptic terminals by blocking high affinity Choline Transporter

3

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

4

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

5

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

6

Acetyl-beta-Methylcholine (Methacholine)

Muscarinic Agonist

Slowly degraded by AchE

Acts in the Heart (M2 receptors)

7

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



8

Pilocarpine

Non-charged Muscarinic Agonist that is a natural alkaloid and used in the eye or to treat dry mouth

9

Scopolamine

Non-charged Muscarinic antagonist that crosses into CNS and can cause amnesia

Used as a dermal patch to prevent Motion sickness (Prophylactically)

10

Atropine

Muscarinic Antagonist

11

Glycopyrrolate

Charged, Non-selective muscarinic antagonist

USED in Anasthesia

12

Pirenzepine

M1 selective Muscarinic Antagonist

Used for gastric ulcers bc M1 in stomach

13

Tiotropium

M1/M3 Muscarinic Antagonist used as an aerosolized spray in the lung

14

2 Drugs Used for M3 selective Muscarinic Antagonism of Detrussor Muscles?

Tolterodine
Darlfenacin

15

2 shortest acting Anti-muscarinics used in the eye?

Tropicamide
Cyclopentolate

16

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

17

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

18

Organophosphates

Irreversibly bind in active site of AchE to inhibit it

Inhibition MAY be reversible if enzyme has not "aged" with use of Oximes

19

Name the Carbamates. Which one is charged? Which one is not charged?

Physostigmine
Neostigmine
Pyridostigmine

Neostigmine is Charged and so does NOT cross BBB!

20

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")

21

Dobutamine

synthetic Catecholamine that only acts on B1 receptors

22

PRazosin

A1 adrenergic receptor antagonist

23

Phenylephrine

A1 Adrenergic receptor Agonist

24

Yohimbine

A2 Adrenergic receptor Antagonist

25

Clonidine

A2 adrenergic receptor agonst

26

Metropolol and Atenolol

B1 adrenergic receptor Antagonists

27

Albuterol

B2 adrenergic receptor agonist

28

Mirabegron

B3 adrenergic receptor Agonist

29

Name the 3 Indirect-Acting NE Releasers (non-catecholamines)

Tyramine

Amphetamine

Ephedrine