50 Pharmacology: Cholinomimetic, Cholinesterase Inhibitors

Question 1

Cholinergic Receptor Agonists

• These are direct acting agents.
  
  • What are the 4 general clinical application for these?

Answer 1

Question 2

Direct Acting Agents

• Esters
  
  • What are the 4 drugs in this group?

Answer 2

Question 3

Direct Acting Agents

• Alkaloids
  
  • What are the 3 drugs in this group?

Answer 3

Question 4

Direct Acting Agents

• Synthetics
  
  • What is the drug in this group?

Answer 4

Question 5

Esters

• These are structured similarly to acetylcholine
  
  • What are the 2 reasons to not just use acetylcholine?
• What kind of esters are selective for muscarinic receptors?
• What kind of esters are resistant to degradation by acetylcholinesterase?

Answer 5

Question 6

Ester Properties

• For each of these choline esters, give the following:
  
  • The susceptibility to degradation by cholinesterase
  • The action on muscarinic receptors
  • The action on nicotinic receptors

Answer 6

Question 7

Ester Properties

• Esters with Quaternary Amines
  
  • Are these charged or uncharged?
  • Are these hydrophilic or hydrophobic?
  • Are these highly absorbed or poorly absorbed PO?
  • Can these efficiently enter the CNS?

Answer 7

Question 8

Methacholine

• Do these receptors act on muscarinic or nicotinic receptors?
  
  • These cause contraction of bronchiole smooth muscle via acting on ________ receptors?
• What are these used for?
• ADRS
  
  • What are the 2 common ADRS?
  • What is a serious ADR?

Answer 8

Question 9

Carbachol

• What receptor does this act on?
• What muscle does it cause contraction of?
• What condition is it used to treat?
  
  • What is the MOA behind this Tx?

Answer 9

Question 10

Bethanechol

• What receptor does this act on?
• What muscle does it cause contraction of?
  
  • What does it cause the relaxation of?
• What condition is it used to treat?

Answer 10

Question 11

Bethanechol and Carbachol

• What are the 3 common ADRS for these 2 drugs?

Answer 11

Question 12

Alkaloids

• What are the plants associated with each of these drugs?
• What is the relationship between these drugs and acetylcholinesterase?

Answer 12

Question 13

Alkaloid Properties

• Tertiary Amines
  
  • Which of these drugs falls under this category?
  • What is known about the absorption of these types of amines?
• Quaternary Amines
  
  • Which of these drugs falls under this category?
  • What is known about the bioavailability of these types of amines?

Answer 13

Question 14

Pilocarpine

• What drug does this have similar uses and ADRS to?
• What condition is this used to treat?
  
  • What syndrome is the above condition secondary to?

Answer 14

Question 15

Synthetic

• What is the only drug for this group?
• What receptor does it act one, and what does it stimulate?
• What 2 treatments are is this drug considered for?
• What are the common ADRs for this drug?

Answer 15

Question 16

I ndirect-Acting Cholinomimetics

• What is the main MOA for these drugs?

Answer 16

Question 17

Indirect-Acting Cholinomimetics

• What are the 4 areas that these cause non-selective increases in ACetylcholine?
  
  • What receptors do these act on in each location?

Answer 17

Question 18

Indirect-Acting Cholinomimetics

• For these sympathetic, parasympathetic, and somatic neurons, decide if each letter represents a muscarinic or nicotinic receptor.

Answer 18

Question 19

Indirect-Acting Cholinomimetics

• Decide if each letter represents either somatic, sympathetic, or parasympathetic fibers.
  
  • Give an explanation why

Answer 19

Question 20

Indirect-Acting Cholinomimetics

• What are the 2 main ways that we can minimize the non-selective systemic effects of these drugs?
  
  • Which one is used specifically to decrease CNS distribution?

Answer 20

Question 21

Indirect-Acting Cholinomimetics

• What are the 6 clinical applications for indirect acting cholinomimetics?

PIG RUM

Answer 21

Question 22

Indirect-Acting Cholinomimetics

• What are the 2 categories for reversible acetylcholinesterase inhibitors?
• What are the 3 categories for irreversible acetylcholinesterase inhibitors?

Answer 22

Question 23

Reversible Acetylcholinesterase Inhibitors

• What are the 4 peripheral only acting agents?
  
  • What kind of amines are these?
• What are the peripheral AND CNS acting agents?
  
  • What kind of amines are these?

Answer 23

Question 24

Irreversible Acetylcholinesterase Inhibitors

• What is the water-soluble agent?
• What are the lipid-soluble agent? (3)
• What are the nerve gases? (2)

Answer 24

Question 25

Reversible Acetylcholinesterase inhibitors * Edrophonium * What kind of amine is this? * What are the 2 indications for this drug? * What kind of duration of action does this have? * What kind of molecule is this, separating it from most other reversible acetylcholinesterase inhibitors?

Answer 25

Question 26

Reversible Acetylcholinesterase inhibitors * Neostigmine, Pyridostigmine, Ambenonium * What kind of amine are these? * What condition do they all treat? * What one is not used as a reversal for a neuromuscular blockade? * Which one is used for both ileus and urinary retention? * Although they all have an intermediate DOA, which one has the shortest DOA and which has the longest DOA? * What kind of molecule are all of these, separating them from edrophonium?

Answer 26

Question 27

Reversible Acetylcholinesterase inhibitors * Physostigmine * What kind of amine is this? * What are the 2 indications for this drug? * What kind of duration of action does this have? * What kind of molecule is this, separating it from edrophonium?

Answer 27

Question 28

Myasthenia Gravis * What kind of receptors are affected by this condition? * What kind of muscles show weakness? * What improves or worsens this weakness? * What kind of vision problems to patients have? * What other symptoms to patients have?

Answer 28

Question 29

Acetyclonesterase inhibitors * How can these drugs be used to dx myasthenia gravis? * What drug, in particular, is used in the test to dx myasthenia gravis? * Treatment of Myasthenia Gravis * What are the 3 Acetyclonesterase inhibitors used in Tx for this? * Why?

Answer 29

Question 30

Acetyclonesterase inhibitors: Reversible Indirect Acting Agents * Systemic side effects * What does SLUD mean? * Besides SLUD, what other side effects exist?

Answer 30

Question 31

Irreversible Acetyclonesterase inhibitors: Organophosphates * How do these drugs block Acetyclonesterase action? * Why is it irreversible?

Answer 31

Question 32

Irreversible Acetyclonesterase inhibitors * Echothiophate * Is this a tertiary amine or quaternary? * I sit long-acting or short-acting? * What type of solution is it stable in? * What conditions is this drug indicated in?

Answer 32

Question 33

Irreversible Acetyclonesterase inhibitors * Malathion * What solution is this stable in? * What gross ass shit is this prodrug used in? * What is the clinical application for this?

Answer 33

Question 34

Irreversible Acetyclonesterase inhibitors * Which are TOXIC pesticides? Which are biological weapons? * What are the muscarinic symptoms of these * What are the CNS symptoms of these? * What are the nicotinic symptoms of this?

Answer 34