Pharmacology - Cholinergic Agonists

Front 1

What type of NT is decreased in alzheimer's patients?

Back 1

Ach

Front 2

What 2 lobes of the brain are effected in alzheimer's?

Back 2

1) Temporal lobe
2) Entorhinal cortex.

Front 3

What Rx's are currently given to treat Alzheimer's?

Back 3

AchEi's

Front 4

What are the 6 steps involved in Ach neurotransmission?

Back 4

1) synthesis
2) storage
3) release
4) binding to the receptor
5) degredation
6) recycling of choline

Front 5

How is Choline transported into the presynaptic terminal?

Back 5

Na dependent cotransport.

Front 6

What Rx prevents Choline from being transported into the presynaptic terminal?

Back 6

Hemicholinium.

Front 7

What is the rate limiting step of ACh production?

Back 7

uptake of choline into the cell.

Front 8

Where the the Acetyl CoA come from?

Back 8

Mitochondria via krebb's cycle and FA oxidation.

Front 9

What 3 substances are stored in an Ach storage vesicle?

Back 9

1) Ach
2) ATP
3) proteglycan

Front 10

What Rx blocks the storage of Ach into a vesicle?

Back 10

Vesamicol.

Front 11

What ion causes the release of the Ach vesicles?

Back 11

Ca influx

Front 12

What substance can block the release of the Ach Vesicles?

Back 12

Botulinum toxin.

Front 13

What substance can cause ALL the Ach vesicles to be released?

Back 13

Black widow spider venom.

Front 14

What are the two products of the AchE enzyme?

Back 14

Choline and acetate.

Front 15

What cell type is predominantly effected by M1 R's ?

Back 15

Gastric Parietal cells.

Front 16

What two cell types are found to have M2 R's ?

Back 16

1) Cardiac muscle
2) Smooth muscle

Front 17

What 3 cell types contain M3 R's?

Back 17

1) Bladder
2) Exocrine glands
3) Smooth muscle

Front 18

What is the R protein and second messenger released with M1 and M3 R's?

Back 18

a) Gq
b) IP3 and DAG
Note: this causes increase in intercellular Ca and therefore
1) hyperpolarization
2) secretion
3) contraction.

Front 19

What is the R protein and second messenger formed by M2 R's?

Back 19

a) Gi
b) Blocks adenylate cyclase and therefore slows HR.

Front 20

What Rx antagonizes the M1 R specifically?
What is this used for?
What is the adverse effect?

Back 20

a) Pirenzepine
b) used to tx gastric and duodenal ulcers.
c) adverse effect is reflex tachycardia (via M2 R's)

Front 21

What Rx is used to Tx overactive bladder?
What M subtype does it act on?

Back 21

a) Darifenacin
b) M3 R's

Front 22

What type of R's are muscarinic?

Back 22

Metabotropic

Front 23

What type of R's are nicotinic?

Back 23

Ionotropic.

Front 24

What ion channels does the binding of a Nicotinic R activate?

Back 24

Na Channel

Front 25

What Rx specifically acts on ganglionic nicotinic R's?

Back 25

Hexamethonium.

Front 26

What Rx specifically acts on NMJ N R's?

Back 26

tubocurarine.

Front 27

What 2 factors make Ach a therapeutically ineffective Rx?

Back 27

1) wide spectrum of action
2) fast metabolism by AchE.

Front 28

How does Ach cause vasodilation?

Back 28

Indirect action via M3 R's leading to NO release.
NO than stimulates pkG leading to hyperpolarization.

Front 29

What type of R's are activated by Bethanechol, nicotinic or muscarinic?

Back 29

Muscarinic.

Front 30

What are the actions, indications and adverse effects of bathenacol?

Back 30

a) causes increase in gastric motility and increase in tone of the detrusser muscle.
b) atonic bladder, atonic or megacolon.
c) sweating, salivation etc. (remember dumbbels)

Front 31

What atom on the Bethenacol causes it to be selective for muscarinic R's?

Back 31

Methy group.

Front 32

What R's does carbachol act on.

Back 32

Nicotinic and Muscarinic because it lacks the methyl group.

Front 33

What prevents the breakdown of carbachol and bethanecol?

Back 33

The carbamic acid prevents it from being broken down by AchE.

Front 34

What are the 3 main actions of pilocarpine?

Back 34

1) Rapid miosis
2) Salivation
3) Lacrimation

Front 35

What is the primary use of pilocarpine?

Back 35

Emergency lowering of interoccular pressure for glaucoma.

Front 36

What are two ancillary reasons for using pilocarpine.

Back 36

1) Xerostomia caused by radiation
2) Sjogren's syndrome.

Front 37

What Rx is used to Tx overdose of Atropine, phenotiazine or TCA's?

Back 37

physostigmine.

Front 38

What is the therapeutic use of physostigmine?

Back 38

Bladder or intestinal atonia.
Glaucoma

Front 39

What is the structure of the N group in physostigmine?

Back 39

tertiary (therefore it can enter the CNS).

Front 40

What are the adverse effects of physostimine?

Back 40

1) Bradycardia
2) paralysis
3) convusions

Front 41

What is the N structure of neostigmine?

Back 41

Quaternary.

Front 42

What is neostigmine used for?

Back 42

1) bladder and GI stim
2) tubocurarine poisoning at NMJ
3) myastenia gravis.

Front 43

What toxicity would you tx with physostigmine as opposed to neostigmine?

Back 43

Atropine (or any other CNS acting anti- muscarinics)

Front 44

What Rx's would you use for the chronic management of MG?

Back 44

Pyridostigmine and ambenomium.

Front 45

What Rx would you use to diagnose MG?

Back 45

Edrophonium.

Front 46

What was the first Rx used to treat Alzheimers and what dangerous side effect caused it to be useless?

Back 46

Tacrine.
Side effect was hepatotoxicity.

Front 47

What Rx replaced Tacrine in the Tx of Alzheimer's?

Back 47

Donepezil.

Front 48

Which Rx is an irreversible AchEi?

Back 48

Echothiophate.

Front 49

what is the Tx for a person that has been poisoned by a nerve gas?

Back 49

1) atropine
2) pralidoxime

Front 50

What is the Rx of choice for Tx of a radiation patient with dry mouth?

Back 50

pilocarpine