Just Drugs...Do Drugs, Give Hugs.

Question 1

Botulinum Toxin/Botox

Answer 1

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

Question 2

Hemicholinium

Answer 2

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

Question 3

Name the non-depolarizing neuromuscular blocking agents

How do they work?

Answer 3

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

Question 4

Name the depolarizing NMBA and its mechanism of action

Answer 4

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

Question 5

Carbamylcholine (carbachol)

Answer 5

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

Question 6

Acetyl-beta-Methylcholine (Methacholine)

Answer 6

Muscarinic Agonist

Slowly degraded by AchE

Acts in the Heart (M2 receptors)

Question 7

Bethanechol

Answer 7

Muscarinic antagonist that does NOT interact with nicotinic receptors

used for post-operative ileus, GERD, or congenital megacolon

Also used to increase Urinary retention

Question 8

Pilocarpine

Answer 8

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

Question 9

Scopolamine

Answer 9

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

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

Question 10

Atropine

Answer 10

Muscarinic Antagonist

Question 11

Glycopyrrolate

Answer 11

Charged, Non-selective muscarinic antagonist

USED in Anasthesia

Question 12

Pirenzepine

Answer 12

M1 selective Muscarinic Antagonist

Used for gastric ulcers bc M1 in stomach

Question 13

Tiotropium

Answer 13

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

Question 14

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

Answer 14

Tolterodine

Darlfenacin

Question 15

2 shortest acting Anti-muscarinics used in the eye?

Answer 15

Tropicamide

Cyclopentolate

Question 16

Edrophonium (Tensilon)

Answer 16

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

Question 17

What are Carbamates as a whole and how do they work?

Answer 17

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

Question 18

Organophosphates

Answer 18

Irreversibly bind in active site of AchE to inhibit it

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

Question 19

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

Answer 19

Physostigmine
Neostigmine
Pyridostigmine

Neostigmine is Charged and so does NOT cross BBB!

Question 20

What are the Oximes? Name them. How are they used?

Answer 20

Pralidoxime and Obidoxime

Used to reverse Organophosphate inhibition of AchE (provided “aging” has not occured”)

Question 21

Dobutamine

Answer 21

synthetic Catecholamine that only acts on B1 receptors

Question 22

PRazosin

Answer 22

A1 adrenergic receptor antagonist

Question 23

Phenylephrine

Answer 23

A1 Adrenergic receptor Agonist

Question 24

Yohimbine

Answer 24

A2 Adrenergic receptor Antagonist

Question 25

Clonidine

Answer 25

A2 adrenergic receptor agonst

Question 26

Metropolol and Atenolol

Answer 26

B1 adrenergic receptor Antagonists

Question 27

Albuterol

Answer 27

B2 adrenergic receptor agonist

Question 28

Mirabegron

Answer 28

B3 adrenergic receptor Agonist

Question 29

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

Answer 29

Tyramine

Amphetamine

Ephedrine