Cholinergics

Question 1

Cholinoreceptors

Answer 1

-nicotinic (NM, NN)
-muscarinic (M1, M2, M3)

Question 2

Nm receptor

Answer 2

-skeletal muscle

Question 3

NN receptor (neural)

Answer 3

-postganglionic
-adrenal medulla

Question 4

Nicotinic receptor responses

Answer 4

-depolarization
-ligand opening of Na/K

Question 5

Muscarinic receptor responses

Answer 5

QIQ

Question 6

M1 receptor

Answer 6

-postganglionic
-depolarization
-GQ mech

Question 7

M2 receptor

Answer 7

-heart
-inhibition
-G1 activation

Question 8

M3 receptor

Answer 8

-smooth muscles (contract)
-exocrine glands (secrete)
-endothelium (relax)
-Gq activation

Question 9

acetylcholine has higher affinity for which receptor

Answer 9

muscarinic

Question 10

acetylcholine biosynthesis and neurotransmission

Answer 10

1. choline transported to presynaptic nevere terminal by CHT
2. Ach synthesize from choline and acetyl-CoA by ChAT
3. ACh transported to storage vesicle by VAT
4. action potential opens gated channels and increases calcium, fusion of vesicles with the surface membrane results in the release of ACh
   -ACh binds to cholinoreceptors on post synaptic cell
5. ACh action terminated by metabolism by AChE
6. auto receptors and receptors on presynaptic nerve end transmitter release

Question 11

sodium-dependent choline transporter (CHT)

Answer 11

-transport choline to presynaptic nerve terminal
-inhibited by hemicholinium

Question 12

choline acetyltransferase (ChAT)

Answer 12

-forms ACh from choline and acetyl coA

Question 13

vesicle-associated transporter (VAT)

Answer 13

-carries ACh to storage vesicle
-inhibited by vesamicol

Question 14

botulinum toxin

Answer 14

-botox
-block release of ACh

Question 15

acetylcholinesterase (AChE)

Answer 15

-metabolizes ACh

Question 16

Cholinergic agents

Answer 16

-acetylcholine
-parasympathetic

Question 17

Parasympathetic direct agonist

Answer 17

-activate cholinoceptors
-muscarinic receptor agonists
-choline esters and alkaloids

Question 18

PSNS indirect agonist

Answer 18

-stimulate ACh release
-inhibit AChE
-reversible or irreversible

Question 19

PSNS antagonists

Answer 19

-direct or indirect
-many drug side effects

Question 20

Muscarinic AGONIST effect on heart

Answer 20

-M2
-DECREASE HR, conduction, and force

Question 21

muscarinic agonist effect on exocrine glands

Answer 21

-M3 increase secretion
-lachrymal, tracheobronchial, salivary, digestive, sweat

Question 22

muscarinic agonist effect on smooth muscles

Answer 22

-M3 increase contraction
-M2 inhibit relaxation

Question 23

muscarinic agonist effect on sphincters

Answer 23

-M3
-relaxation

Question 24

Muscarinic Agonist effects on CNS

Answer 24

-not all agonist can access CNS
-mostly M1 receptor
-tremor, hypothermia, increased locomotor activity, improved cognition

Question 25

Direct acting cholinergic receptor agonists: esters

Answer 25

-ACh -methacholine -carbachol -bethanechol

Question 26

Direct acting cholinergic receptor agonists: alkaloids

Answer 26

-muscarine -pilocarpine

Question 27

Mushroom poisoning (muscarinic agonists)

Answer 27

-bradycardia -nausea, cramps -bronchoconstriction -salivation -visual disturbances -sweating (SNS) -hypotension (SNS)

Question 28

charged muscarine

Answer 28

does not cross BBB well

Question 29

Pilocarpine

Answer 29

-promote sweating, urine, salivation -treat gluacoma (outflow aq humor = decrease pressure)

Question 30

Xerostomia

Answer 30

-dry mouth -treat with pilocarpine (M3)

Question 31

Sjogren's syndrome

Answer 31

-autoimmune disorder mostly women -reduced salivary gland secretions

Question 32

Muscarinic effect on cardiovascular

Answer 32

-fall in BP, HR -M2

Question 33

muscarinic agonist effect on M3

Answer 33

-GI (muscle contract, sphincter relax) -bladder -eye (miosis) -sweating (increase)

Question 34

ACh clinical use

Answer 34

-Muscarinic and nicotinic receptors -cholinesterase sensitive -use for miosis during surgery

Question 35

Carbachol clinical use

Answer 35

-muscarinic and nicotinic receptor -use for miosis during surgery and gluacoma

Question 36

Pilocarpine clinical use

Answer 36

-muscarinic receptor -glaucoma -dry mouth

Question 37

bethanechol

Answer 37

-muscarinic receptor -urinary retention -GI stimulation

Question 38

Varencicline clinical use

Answer 38

-nicotinic receptor -smoking cessation

Question 39

Side effects of muscarinic agonists

Answer 39

-Diarrhea -Urination -Miosis -Bradycardia -Bronchoconstriction -Emesis -Lacrimation -Salivation + Sweating (SNS effect)

Question 40

Methacholine clinical use

Answer 40

-provacative test for hyperactive airways