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SP18: Pharm > Cholinergic Pharm > Flashcards

Cholinergic Pharm Flashcards

1
Q

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

A

Nicotinic; muscarinic

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2
Q

What type of receptors are nicotinic receptors?

A

Ligand activated ion channels

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3
Q

Nicotinic receptors have ___ subunits and bind ___ agonists.

A

5; 2

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4
Q

What type of receptors are muscarinic receptors?

A

GPCR

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5
Q

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

A

Galpha(q)

*Activates DAG and IP3 signaling

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6
Q

What type of GPCR is linked to M2 and M4?

A

Galpha(i)

*inhibits adenylate cyclase

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7
Q

What is an indirect acting cholinergic agonist?

A

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

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8
Q

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

A

True

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9
Q

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

A

True

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10
Q

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

A

True

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11
Q

Pilocarpine and cevimeline are selective for ________ receptors.

A

muscarinic

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12
Q

Dimethylphenylpiperazinium and succinylcholine are selective for _______ receptors.

A

nicotinic

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13
Q

How is skeletal muscle contraction different than smooth muscle contraction?

A

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

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14
Q

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

A

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

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15
Q

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

A

Trabecular drainage and reduced ocular pressure

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16
Q

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

A

M2; reduce

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17
Q

Describe the opposing sympathetic and parasympathetic effects in cardiac muscle.

A

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

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18
Q

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

A

sympathetic adrenergic

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19
Q

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

A

True

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20
Q

Vascular endothelial cells express which type of muscarinic receptors?

A

M3

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21
Q

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

A

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

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22
Q

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

A

M3

23
Q

What receptors mediate sphincter relaxation in the gastrointestinal tract?

A

M2

24
Q

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

A

M3

25
Q

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

A

M3

26
Q

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

A

True

27
Q

What is the SLUD response?

A

Salivation, Lacrimation, Urination, Defecation

All negative side effects of over stimulation of muscarinic receptors

28
Q

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

A

Asthma, CV disease, ulcers

29
Q

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

A

True

30
Q

What is the MOA for anticholinesterases?

A

Inhibit acetylcholinesterase from breaking down AcCh

*also called indirectly acting cholinergic agonists

31
Q

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

A

They are not hydrolyzed and are poisonous

32
Q

What is the net effect of anticholinesterases?

A

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

33
Q

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

A

False

More sympathetic innervation in vascular epithelium

34
Q

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

A

glaucoma

35
Q

Pilocarpine and cevimeline are cholinergic agonists used to treat ________.

A

xerostomia

36
Q

__________ are used to terminate a neuromuscular block.

A

anticholinesterases

37
Q

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

A

True

38
Q

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

A

False

Tertiary amines

39
Q

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

A

M1

40
Q

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

A

sympathetic nervous system

41
Q

What is unique about sweat gland innervation?

A

Both sympathetic and parasympathetic act via muscarinic receptors

  • Antimuscarinics inhibit all sweat gland activity
42
Q

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

A

dilation; accommodation

43
Q

What effect do antimuscarinics have on the respiratory tract?

A

Produce bronchodilation and inhibit mucus production to treat COPD

44
Q

T/F: Antimuscarinics will increase body temp.

A

True

45
Q

T/F: Antimuscarinics will cause urinary retention.

A

True

46
Q

What are five key uses for antimuscarinics?

A
  1. Dilate pupils
  2. Treat COPD (quat amines, inhalation)
  3. Reduce saliva
  4. Anti-spasmodics and anti-ulcer
  5. Antidote to anti-cholinesterases
47
Q

Antimuscarinics at the lowest doses will have what effect?

A

Decreases in secretion (saliva, sweat, mucus)

48
Q

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

A

gastric system

49
Q

T/F: Nicotine will penetrate the BBB.

A

True

Feeling of well being

50
Q

Where are nicotinic AcCh receptors important?

A

Ganglia and mediators in the CNS

51
Q

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

A

If the agonists stick around they can desensitize the ion channel

52
Q

When are nicotinic antagonists used?

A

When you want to induce flaccid paralysis

53
Q

What is the most dangerous side effect of nicotinic antagonists?

A

If they get in your diaphragm you will stop breathing

SP18: Pharm (8 decks)

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