Pharmacology- Ch 4 Cholinergic Agonists

Front 1

Neurotransmission in cholinergic neurons

Back 1

1.synthesis
2.storage
3.release
4.binding of ACh to receptor
5.degradation of the neurotransmitter in the synaptic cleft
6.recycling of choline and acetate

Front 2

Where is Acetyl CoA derived from?

Back 2

The mitochondria and is produced by the pyruvate oxidation and fatty acid oxidation.

Front 3

Cholinergic drugs act on receptors activated by?

Back 3

acetylcholine

Front 4

Where is ACh packaged and stored?

Back 4

Presynaptic vesicles by an active transport process coupled to the efflux of protons.

Front 5

When is ACh released?

Back 5

When an action potential propagated by voltage-sensitive sodium channels arrives at nerve endings, voltage-sensitive calcium channels on the presynaptic membrane open, causing an increase in the concentration of intracellular calcium.

Front 6

What two classes of postsynaptic cholinergic receptors are there?

Back 6

1. muscarinic
2. nicotinic

Front 7

Where are muscarinic receptors located?

Back 7

Receptors have been found on ganglia of the peripheral nervous system and on the autonomic effector oragns.

Front 8

Darifenacin

Back 8

a competitive muscarinic receptor antagonist with a greater affinity for the M3 receptor than for the other muscarinic receptors. Used in the treatment of overactive bladders.

Front 9

Muscarinic Receptors

Back 9

Muscarine>Acetylcholine>>Nicotine

Front 10

Nicotinic receptors

Back 10

Muscarine<

Front 11

Where are nicotinic receptors located?

Back 11

CNS, adrenal medulla, autonomic ganglia, and the neuromuscular junction (NMJ)

Front 12

Nicotinic receptor

Back 12

composed of 5 subunits and it functions as a ligand-gated ion channel.

Front 13

Direct-acting cholinergic agonists

Back 13

mimic the effects of ACh by binding directyl to cholinoceptors. Longer duration of action.

Front 14

Acetylcholine

Back 14

cannot penetrate membranes, therefore lacks therapeutic importance because of multiplicity of actions and its rapid inactivation by the cholinesterases. Has both muscarinic and nicotinic activity

Front 15

ACh actions

Back 15

1.Decrease in heart rate and cardiac output
2.Decrease in BP
3.increase salivary secretion and stimulates intestinal secretions.
4. Expulsion of urine.

Front 16

How is ACh effect the eye?

Back 16

stimulates the ciliary muscle contraction for near vision and in the constriction of the pupillae sphincter muscle causing miosis.

Front 17

Pilocarpine

Back 17

-Reduces intraocular pressure in open-angle and narrow angle glaucoma.
-binds preferentially at muscarinic receptors
-uncharged, tertiary amine that can penetrate the CNS

Front 18

Bethanechol

Back 18

-used in treatment of urinary retention
-binds preferentially at muscarinic receptors

Front 19

Carbachol

Back 19

-Produces miosis during ocular surgery
-used to reduce intraocular pressure in open-angle or narrow angle glaucoma especially in pts that are tolerant to pilocarpine.

Front 20

Indirect-acting cholinergic agonists: acetylcholinesterase inhibitors (reversible)

Back 20

reversible AChE inhibitors are short-acting or intermediate-acting agents.

Front 21

Physostigmine

Back 21

-Increase intestinal and bladder motility
-Reduces intraoccular pressure in glaucoma
-Reverse CNS and cardiac effects of tricyclic antidepressants
-Reverses CNS effects of atropine
uncharged tertiary amine that can penetrate the CNS

Front 22

Neostigmine

Back 22

-Prevents post-op abdominal distentions and urinary retention
-Used in treatment of myasthenia gravis
-used as an antidote for tubocuraine
-long duration of action (2-4hrs)

Front 23

tubocuraine

Back 23

-cholinergic receptor and nicotinic
-block specifically at the NMJ
-nondepolarizing neuromuscular blocking drug
-affects skeletal muscles

Front 24

edrophonium

Back 24

-For diagnosis of myasthenia gravis
-antidote for tubocuraine
-short duration (10-20mins)

Front 25

Pyridostigmine

Back 25

-Cholinesterase inhibitor used in chronic management of myasthenia gravis
-duration of action (3-6hrs)

Front 26

Rivastigmine, galantamine, Donepezil

Back 26

-First-line treatments for Azheimer disease
-Not show to delay of effects of disease
-can be used with memantine with moderate to severe disease

Front 27

A patient on a diagnostic test for myasthenia gravis would be expected to have improved neuromuscular function after being treat with...?

Back 27

Edrophonium, a short acting inhibitor of AChE that is used to diagnose myasthenia gravis.

Front 28

The drug of choice for treating decreased salivation accompanying head and neck irradiation is...?

Back 28

Pilocarpine.

Front 29

Pralidoxime (PAM)

Back 29

-unable to penetrate CNS
-weak AChE inhibitor
-cannot overcome toxicity of reversible AChE inhibitors.

Front 30

How do cholinergic and adrenergic drugs act?

Back 30

Both act by either stimulating or blocking receptors of the autonomic nervous system.

Front 31

What happens when the M1 or M3 receptors are activated?

Back 31

the receptor undergoes a confromational change and interacts with a G protein, designated Gq protein, which in turn activates phospholipase C.

Front 32

What happens when M2 is activated?

Back 32

The subtype on the cardiac muscle stimulates a G protein designated Gi, that inhibits adenylyl cyclase, and increase K+ conductance, to which the heart responds with a decrease in rate and force of contraction.