Cholinergic Drugs

Front 1

Bethanechol

Back 1

-useful for managing urinary retention
-used to decrease esophageal tone in patients with GERD and reflux esophagitis

Front 2

Methacholine

Back 2

-May be useful as an agent to test for and aid in the diagnosis of asthma (methacholine challenge)
-Also useful for chronic myasthenia gravis

Front 3

Carbachol

Back 3

-Treatment of glaucoma, decreases intraocular pressure

Front 4

Pilocarpine

Back 4

-Treatment of glaucoma, decreases intraocular pressure
-induces salvation for the treatment of dry-mouth due to Sjogren's Syndrome

Front 5

Vernicline

Back 5

-Use in smoking cesssation by indirectly stimulating the mesolimbic dopamine system in the CNS impt. to reward experience of smoking.

Front 6

Donepezil

Back 6

-Useful for treatment of Alzheimer's disease

Front 7

Tacrine

Back 7

-Well known drug-induced hepatotoxicity
-Useful for patient's with Alzheimer's disease

Front 8

Edrophonium

Back 8

-Useful in the diagnosis of myasthenia gravis

Front 9

Galantamine

Back 9

-Useful for patient's with Alzheimer's disease

Front 10

Neostigmine

Back 10

-Useful for urinary retention

Front 11

Pyridostigmine

Back 11

-Useful for chronic myasthenia gravis

Front 12

Rivastigmine

Back 12

-Useful for chronic myasthenia gravis
-Useful for patient's with Alzheimer's disease

Front 13

Which cholinergic drugs are useful for patient's with Alzheimer's disease?

Back 13

Galantamine, Rivastigmine, Donepezil, Tacrine

Front 14

Which cholinergic drugs are useful for myasthenia gravis?

Back 14

Edrophonium, Pyridostigmine, Rivastigmine

Front 15

Which 2 cholinergic drugs are useful for treatment of glaucoma?

Back 15

Carbachol, pilocarpine

Front 16

Which 2 cholinergic drugs are useful for urinary retention?

Back 16

Bethanechol, Neostigmine

Front 17

Which two drugs are completely resistant to acetylcholinesterase?

Back 17

Bethanechol and Carbachol

Front 18

Which drug is less suspectible to acetylcholinesterase degradation?

Back 18

Methacholine

Front 19

Name two types of chemical modifications that have been made to acetylcholine?

Back 19

1. Addition of a methyl side-chain and
2. Modification of the ester moiety of ACh to a carbamic ester

Front 20

Name the two cholinergic drugs which are carbamic acid moiety?

Back 20

Carbachol and Bethanechol

Front 21

Name the two cholinergic drugs which have more selectivity for muscarinic receptors and why?

Back 21

Methacholine and Bethanechol have significant muscarinic selectivity because they are the ACh to which a methyl side chain has been added to the beta-carbon.

Front 22

Which 2 alkaloids are found in nature?

Back 22

Pilocarpine and muscarine

Front 23

Pilocarpine is a tertiary amine, why is this important?

Back 23

Muscarine, due to it's permanently charge quaternary amine moiety, has limited absorption relative to pilocarpine, which is a tertiary amine.

Front 24

Which cholinergic drug has selectivity for neuronal nicotinic receptors?

Back 24

Varenicline

Front 25

Which 2 cholinergic drugs are reversible ACh inhibitors which bind competetively in a non-covalent manner, acts like ACh by binding to the active site of AChE in a noncovalent manner?

Back 25

Edrophonium and Galantamine

Front 26

Which 2 cholinergic drugs are Reversible noncompetitive (non-classic) AChE inhibitors?

Back 26

Tacrine and Donepezil

Front 27

Name 3 cholinergic drugs which are slow reverisble and noncompetitive AChE inhibitors?

Back 27

Neostigmine, pyridostigmine, and rivastigmine

Front 28

What are irreversible AChE inhibitors called?

Back 28

Organophosphates

Front 29

How do cholinergic drugs affect cardiac contractility?

Back 29

Negative inotropic effect (decreases contractile strength) due to M2 stimulation in cardiac contractile cells

Front 30

How do cholinergic drugs affect heart rate?

Back 30

Negative chronotropic effect (decrease in HR) due to M2 stimulation at SA node

Front 31

How do cholinergic drugs affect the lower respiratory tract?

Back 31

Contraction of bronchial smooth muscle and increased mucous secretion due to M3 stimulation

Front 32

How do cholinergic drugs affect the GI tract?

Back 32

Increased peristalsis due to M3 stimulation

Front 33

How do cholinergic drugs affect the Genitourinary tract?

Back 33

Contraction of bladder wall muscle and relaxation of urinary sphincter resulting in increased ease of urination (M3 receptors)

Front 34

How do cholinergic drugs affect the eye?

Back 34

Contraction of pupillary constrictor muscle (miosis); contraction of ciliary muscle leading to outflow of aqueous humor and decrease in IOP (M3 receptors)

Front 35

What is a short-acting AChE inhibitor?

Back 35

Edrophonium

Front 36

Which 2 cholinergic drugs are used for chronic management of myasthenia gravis and why?

Back 36

Pyridostigmine, Rivastigmine, and neostigmine because they are longer acting AChE inhbitors

Front 37

Why is Varenicline useful for treatment of smoking?

Back 37

It decreases craving by replacing the reward/pleasure experience secondary to cigarette smoking.

Front 38

Symptoms of acute nicotine toxicity include:

Back 38

convulsions, respiratory paralysis, hypertension, and cardiac arrythmias.

Front 39

Toxicity of the direct-acting muscarinic cholinergic drugs are simply excess of usual pharmacological effects. These include:

Back 39

excess salvation, miosis, sweating, nausea, vomiting, diarrhea, and bronchial constriction

Front 40

Name the AChE inhibitor toxicities.

Back 40

They are a combination of the toxicities seen from nicotine and the direct-acting muscarinic cholinergic drugs.

Front 41

What is the most common cause of AChE inhibitor toxicity?

Back 41

Accidental exposure to insecticides (many insecticides are organophosphates AChE inhibitors)

Front 42

What can be used if there is acute poisoning of AChE inhibtors exposure to insecticides?

Back 42

An Antidote such as pralidoxime (2-PAM), which may aid in the regeneration of AChE if the patient is treated quickly enough

Front 43

What are the toxicities that Alzheimer's patients will experience when taking AChE inhibitors?

Back 43

significant nausea and vomiting especially with Tacrine and rivastigmine

Front 44

What happens if a patient is taking a anticholinergic drug with a cholinergic drug?

Back 44

Drugs with anticholinergic effects may decrease the efficacy of cholinergic agents.

Front 45

Name the 4 muscarinic ACh Receptor Agonist.

Back 45

Bethanechol, Carbachol, Methacholine, Pilocarpine

Front 46

Name the nicotinic ACh receptor Agonist.

Back 46

Varenicline

Front 47

Name the 7 AChE Inhibitors.

Back 47

Donepezil, Tacrine, Edrophonium, Galantamine, Neostigmine, Pyridostigmine, and Rivastigmine