Cholinergic Pharm

Question 1

_________ receptors involve electrical signals. _________ receptors involve an action taking place.

Answer 1

Nicotinic; muscarinic

Question 2

What type of receptors are nicotinic receptors?

Answer 2

Ligand activated ion channels

Question 3

Nicotinic receptors have ___ subunits and bind ___ agonists.

Answer 3

5; 2

Question 4

What type of receptors are muscarinic receptors?

Answer 4

GPCR

Question 5

What type of GPCR is linked to M1, M3, and M5 (odd numbered muscarinic receptors)?

Answer 5

Galpha(q)

*Activates DAG and IP3 signaling

Question 6

What type of GPCR is linked to M2 and M4?

Answer 6

Galpha(i)

*inhibits adenylate cyclase

Question 7

What is an indirect acting cholinergic agonist?

Answer 7

It will inhibit cholinesterase so that AcCh will stay in the synapse longer

Question 8

T/F: Carbachol is similar to AcCh except it is hydrolyzed much more slowly.

Answer 8

True

Question 9

T/F: AcCh has a quarternary amine that is always positively charged.

Answer 9

True

Question 10

T/F: AcCh and carbamoylcholine are non-selective for muscarinic/nicotinic receptors.

Answer 10

True

Question 11

Pilocarpine and cevimeline are selective for ________ receptors.

Answer 11

muscarinic

Question 12

Dimethylphenylpiperazinium and succinylcholine are selective for _______ receptors.

Answer 12

nicotinic

Question 13

How is skeletal muscle contraction different than smooth muscle contraction?

Answer 13

Troponin, which normally holds tropomyosin in place, binds Ca++ and lets go of tropomyosin allowing contraction

Question 14

What is the effect of M3 muscarinic receptors in the eye?

Answer 14

When stimulated the M3 receptors cause Ca++ release leading to muscle contraction

Question 15

What effect is seen with the M3 mediated muscle contraction in the eye?

Answer 15

Trabecular drainage and reduced ocular pressure

Question 16

Cardiac muscle contains ____ receptors that ________ cardiac output when activated.

Answer 16

M2; reduce

Question 17

Describe the opposing sympathetic and parasympathetic effects in cardiac muscle.

Answer 17

Symp: Adrenergic beta receptors activate Galpha(s) stimulating adenylate cyclase and increasing muscle contraction

Para: Cholinergic receptors stimulate Galpha(i) which inhibits adenylate cyclase decreasing muscle contraction

Question 18

Most arteries and veins in the body are innervated by ________ ________ nerves.

Answer 18

sympathetic adrenergic

Question 19

T/F: Coronary arteries are controlled by parasympathetic cholinergic and sympathetic cholinergic nerves.

Answer 19

True

Question 20

Vascular endothelial cells express which type of muscarinic receptors?

Answer 20

M3

Question 21

What is the signal cascade that takes place following M3 activation in vascular endothelial cells?

Answer 21

Increase in Ca++ -> formation of Ca++/calmodulin -> activation of NOS to produce NO -> NO travels to smooth muscle cell and enhances cGMP production -> muscle relaxation

Question 22

What type of receptors are found on the bronchial muscles to mediate muscle contraction?

Answer 22

M3

Question 23

What receptors mediate sphincter relaxation in the gastrointestinal tract?

Answer 23

M2

Question 24

____ receptors mediate the release of glandular contents from salivary glands.

Answer 24

M3

Question 25

Activation of which receptors cause the detrusor muscle to contract and empty the bladder?

Answer 25

M3

Question 26

T/F: Carbachol effects last much longer than AcCh effects.

Answer 26

True

Question 27

What is the SLUD response?

Answer 27

Salivation, Lacrimation, Urination, Defecation All negative side effects of over stimulation of muscarinic receptors

Question 28

Patients with certain disorders should be more cautious of the effects of muscarinic agonists. Which disorders?

Answer 28

Asthma, CV disease, ulcers

Question 29

T/F: Topical routes are the most favored for distribution of muscarinic agonists.

Answer 29

True

Question 30

What is the MOA for anticholinesterases?

Answer 30

Inhibit acetylcholinesterase from breaking down AcCh *also called indirectly acting cholinergic agonists

Question 31

What is the use of irreversible anticholinesterases such as malathion (insectiside) and sarin (nerve gas)?

Answer 31

They are not hydrolyzed and are poisonous

Question 32

What is the net effect of anticholinesterases?

Answer 32

Similar to direct acting cholinergic agonists - increase AcCh at effector site

Question 33

T/F: Anticholinesterases produce a muscarinic receptor mediated vasodilation.

Answer 33

False More sympathetic innervation in vascular epithelium

Question 34

Choliergic agonists can be used as therapy to _________ by stimulating musculature of iris and ciliary body.

Answer 34

glaucoma

Question 35

Pilocarpine and cevimeline are cholinergic agonists used to treat ________.

Answer 35

xerostomia

Question 36

__________ are used to terminate a neuromuscular block.

Answer 36

anticholinesterases

Question 37

T/F: Anticholinesterases are used as therapies for Myasthenia Gravis and Alzheimer's.

Answer 37

True

Question 38

T/F: Quaternary amines are absorbed the most easily and can enter the BBB.

Answer 38

False Tertiary amines

Question 39

Muscarinic antagonists with tertiary amines can have negative effects on the ___ receptors in the CNS.

Answer 39

M1

Question 40

In general, muscarinic antagonists will cause a target to be placed under complete control of the __________.

Answer 40

sympathetic nervous system

Question 41

What is unique about sweat gland innervation?

Answer 41

Both sympathetic and parasympathetic act via muscarinic receptors - Antimuscarinics inhibit all sweat gland activity

Question 42

Antimuscarinics will cause pupil _________ and paralysis of the _________ in the eye.

Answer 42

dilation; accommodation

Question 43

What effect do antimuscarinics have on the respiratory tract?

Answer 43

Produce bronchodilation and inhibit mucus production to treat COPD

Question 44

T/F: Antimuscarinics will increase body temp.

Answer 44

True

Question 45

T/F: Antimuscarinics will cause urinary retention.

Answer 45

True

Question 46

What are five key uses for antimuscarinics?

Answer 46

1. Dilate pupils 2. Treat COPD (quat amines, inhalation) 3. Reduce saliva 4. Anti-spasmodics and anti-ulcer 5. Antidote to anti-cholinesterases

Question 47

Antimuscarinics at the lowest doses will have what effect?

Answer 47

Decreases in secretion (saliva, sweat, mucus)

Question 48

Antimuscarinics must be at the highest doses to have effect in the __________.

Answer 48

gastric system

Question 49

T/F: Nicotine will penetrate the BBB.

Answer 49

True Feeling of well being

Question 50

Where are nicotinic AcCh receptors important?

Answer 50

Ganglia and mediators in the CNS

Question 51

How are some nicotininc receptor agonists used to inhibit the receptor activity?

Answer 51

If the agonists stick around they can desensitize the ion channel

Question 52

When are nicotinic antagonists used?

Answer 52

When you want to induce flaccid paralysis

Question 53

What is the most dangerous side effect of nicotinic antagonists?

Answer 53

If they get in your diaphragm you will stop breathing