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House Pharmacology > Cholinergic Mechanism > Flashcards

Cholinergic Mechanism Flashcards

1
Q

Primarily, acetylcholine is associated with ____ neurons and the activation of ________.

A

motor

muscle function

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2
Q

Nicotinic receptors function within the ___ nervous system and at the _______

While

muscarinic receptors function in _______ nervous systems, mediating innervation to __________

A

central; neuromuscular junction.

both the peripheral and central; visceral organs

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3
Q

Nicotinic receptors are also used by PNS

T/F

A

F

Only CNS

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4
Q

Choline esters (____,_____), which act at ___ sites, like acetylcholine, but are ____________

A

bethanechol, carbachol

all

resistant to degradation by acetylcholinesterases

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5
Q

Mention 2 examples of choline esters?

A

Bethanecol

Carbachol

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6
Q

Cholinomimetics ______________, esp. acetylcholine.

A

mimick the action of choline

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7
Q

medications that directly act on muscarinic or nicotinic receptors are called _______________, because they mimic acetylcholine.
Examples of these medications include _____,_________ ,_______, and _______

A

direct cholinomimetics

bethanechol, carbachol, methacholine, and pilocarpine.

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8
Q

Cholinesterase are chemicals that __________________.

A

breakdown the neurotransmitter acetylcholine

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9
Q

Cholinesterase

This ____eases the amount of the acetylcholine or ________ in the synaptic cleft that can bind to muscarinic receptors, nicotinic receptors and others

A

Decr

butyrylcholine

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10
Q

Anticholinesterase

Cholinesterase inhibitors, also known as anti-cholinesterase, are chemicals that ___________________. This ___eases the amount of the acetylcholine or butyrylcholine in the synaptic cleft that can bind to muscarinic receptors, nicotinic receptors and others

A

prevent the breakdown of the neurotransmitter acetylcholine or butyrylcholine

Incr

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11
Q

Cholinergics
They are drugs that act on the _______,______, or _______

They ______ the effects that are mediated by acetylcholine

A

peripheral nervous system, central nervous system, or both.

enhance

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12
Q

Cholinergics

Also known ______pathomimetic

A

parasym

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13
Q

Cholinergics

It works in 2 ways;
1. Act ______ by _______ the effects of acetylcholine on acetylcholine receptors present in the body.
2. Act ________ by ____________________

A

Directly; enhancing

indirectly; inhibiting the enzyme that is responsible for the degradation of acetylcholine

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14
Q

Types of anticholineesterases

Reversible –Bind to cholinesterase for a period of ______ to _____
Irreversible –Bind to cholinesterase and form a ________ –

A

minutes to hours

permanent covalent bond

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15
Q

Drug Effects of Cholinergic Agonists

___eased gastric secretions
____eased gastrointestinal motility
____eased urinary frequency

A

Incr
Incr
Incr

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16
Q

Drug Effects of Cholinergic Agonists

(Stimulate or Inhibit?) pupil Constriction (miosis)
(Increased or Reduced?) intraocular pressure
(Increased or decreased?) salivation and sweating

A

Stimulate

Reduced

Increased

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17
Q

Drug Effects of Cholinergic Agonists

(Increased or Decreased?) heart rate

Causes (Vasodilation or Vasoconstriction?)

A

Decreased

Vasodilation

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18
Q

It is important to know that:

At recommended low doses, the cholinergics primarily affect the ________ receptors.

At high doses, cholinergics stimulate the _______ receptors.

A

MUSCARINIC

NICOTINIC

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19
Q

CNS excitation

High dose or low dose

A

High dose

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20
Q

Ganglionic stimulation

High dose or low dose

A

High dose

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21
Q

Adrenaline release

High dose or low dose

A

High dose

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22
Q

RISE in BP

High dose or low dose

A

high dose

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23
Q

Fall in BP

High dose or low dose

A

Low dose

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24
Q

Increased GI motility

High dose or low dose

A

Low dose

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25
Q

Bladder constriction

High dose or low dose

A

Low dose

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26
Q

Salivation

High dose or low dose

A

Low dose

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27
Q

Lacrimation

High dose or low dose

A

Low dose

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28
Q

Bradycardia

High dose or low dose

A

Low dose

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29
Q

Broncho Constriction

High dose or low dose

A

Low dose

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30
Q

Examples of Cholinergic Agonist

Examples of Direct-acting: ______,_____,____,____
Examples of In-direct-acting:
_______,_____,______

A

acetylcholine, carbachol, pilocarpine
Bethanechol

physostigmine, pyridostigmine, donepezil (Aricept)

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31
Q

physostigmine

Direct or indirect cholinergic agonist

A

Indirect cholinergic agonist

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32
Q

pyridostigmine

Direct or indirect cholinergic agonist

A

Indirect cholinergic agonist

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33
Q

donepezil (Aricept)

Direct or indirect cholinergic agonist

A

Indirect cholinergic agonist

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34
Q

carbachol

Direct or indirect cholinergic agonist

A

Direct cholinergic agonist

35
Q

pilocarpine

Direct or indirect cholinergic agonist

A

Direct cholinergic agonist

36
Q

Bethanechol

Direct or indirect cholinergic agonist

A

Direct cholinergic agonist

37
Q

Therapeutic Uses of Cholinergic Agonist

Carbachol and pilocarpine are (direct or indirect?) acting cholinergic agonist Useful for _________ and _______

A

Direct

glaucoma and intraocular pressure in surgery.

38
Q

Bethanechol is a (direct or indirect?) acting cholinergic agonist that is used to ____ease _________ of _______ and ______.

It (constricts or relaxes?) sphincters in _______ and ______, allowing them to _____.

A

Direct ; Incr ; Tone and motility

bladder and GI tract

Relaxes ; bladder and GI tract

empty

39
Q

Which is more important

MUSCARINIC or Nicotinic

A

MUSCARINIC

40
Q

Acetylcholine is used for treatment of:

Myasthenia gravis ( _________)
Alzheimer’s disease (________)

A

Pyridostigmine

rivastigmine

41
Q

Acetylcholine aids the action of muscle relaxants

T/F

A

F

It reverses it

42
Q

Side effects of acetylcholine are:

Ocular side effects:

Corneal ______
Corneal ______
Corneal _______

A

swelling

clouding

decomposition

43
Q

Side effects of acetylcholine are:

Systemic side effects:
_______
difficulty in _____
____tension
______
(slow or fast?) heart rate

A

sweating
Breathing
Hypotension

flushing
Slow

44
Q

Carbachol is primarily used in the treatment of _______, but it is also used during ________.

A

glaucoma

ophthalmic surgery

45
Q

Carbachol eyedrops are used to ___ease the _____ in the eye for people with glaucoma.

A

Decr

pressure

46
Q

Carbachol eyedrops is sometimes used to ______ the ____ during ______ surgery.

A

constrict; pupils

cataract

47
Q

Carbachol

Is metabolized by plasma cholinesterases

T/F

A

F
Is not

48
Q

Carbachol is selective

T/F

A

F

It’s not

49
Q

Therapeutic uses of bethanechol include:

_____eases _______ of ________
It relaxes __________ in _________, allowing them to empty

A

Incr; Tone and motility ; Bladder and GI tract

sphincters in bladder and GI tract

50
Q

Bethanecol

Selective or not?

A

Selective

51
Q

Bethanecol

Is metabolized by plasma cholinesterases

T/F

A

F

52
Q

Structural differences between carbachol and Bethanecol?

A

Carbachol has an amide group only

Bethanecol has an amide group and an ethyl

53
Q

Therapeutic uses of Pilocarpine are:

Pilocarpine is used to treat _______ caused by ______ in people with ___________ and to treat ______ in people with ________

A

dry mouth

radiotherapy; head and neck cancer

dry mouth

Sjögren’s syndrome

54
Q

Sjögren’s syndrome

Is a condition that affects the _____ and causes _____ of certain parts of the body such as the ____________

A

immune system

dryness

eyes and mouth

55
Q

Ophthalmic pilocarpine is used to treat _________, a condition in which increased pressure in the eye can lead to ____________.

A

glaucoma

gradual loss of vision

56
Q

Opthalmic Pilocarpine is in a class of medications called ______. It works by allowing ______ to _________.

A

miotics

excess fluid

drain from the eye

57
Q

Structure of pilocarpine?

A

Has an imidazole attached to it

58
Q

Indirect-Acting Agents

Examples of Indirect-Acting Agents include:
1._________
2. ________

A

physostigmine

pyridostigmine

59
Q

Therapeutic uses of physostigmine

Physostigmine cause ___ muscle (contractions or relaxations?)

Are used for treatment of _______
Are used to _________________ (antidote)

A

skeletal; contraction

myasthenia gravis

reverse anticholinergic poisoning

60
Q

Indirect-Acting Agent—donepezil

Used in the treatment of ____ to ____ ——- disease.

Helps to increase ______ and ______

A

mild to moderate: Alzheimer’s

memory and learning capabilities

61
Q

Drug interactions
Anti______ are known to antagonize cholinergic agents, resulting in decreased responses

A

histamines

62
Q

Cholinergic Antagonist
They are drugs that compete with acetylcholine” for its binding sites at synaptic junctions thereby inhibiting its activity and preventing the transmission of _______pathetic nerve impulses.

A

parasym

63
Q

Depending on the type of receptor to act on, cholinergic antagonists are either classified as ________ or ______

A

muscarinic antagonists or nicotinic antagonists.

64
Q

Mechanism of Action of Cholinergic Antagonists

 Block ACh at the _____ receptors in the PNS
prevent ACh from ______
Once these drugs bind to receptors, they inhibit nerve transmission at these receptors.

A

muscarinic

binding to the receptor site.

65
Q

Cholinergic Antagonist are:

Natural group of ______ found in _____ (_______)
1. ____
2. _______

A

alkaloids; plants

BELLADONA ALKALOIDS

Atropine

Scopolamine

66
Q

Atropine (________/ _____)

Scopolamine ( ____ pills causing ______.

A

properative; antidote

Sleeping; drowsiness

67
Q

Drug Effects of Cholinergic Antagonist

Small doses: ___ease heart rate.
Large doses: ___ease heart rate .
Small doses: ____ease tremors.
Large doses: _____,_____,______ pupils

A

Decr
Incr
Decr

drowsiness, hallucinations.

Dilated

68
Q

Dilated pupils aka ?

A

mydriasis

69
Q

Drug Effects of Cholinergic Antagonist

____ease gastric secretion.
___ease motility and peristalsis.
____eased constriction of internal sphincter causing urinary retention
____eased salivation, sweating.
____eased bronchial secretions

A

Decr
Decr
Incr
Decr
Decr

70
Q

Therapeutic Uses of Cholinergic Antagonists
It is used in treatment of
_______ disease by decreasing _____ and _______

Low doses:___ the heart rate.
High doses: ______ heart rate

A

Parkinson’s

muscle rigidity and power tremors.

slow; increased

71
Q

Therapeutic Uses of Cholinergic Antagonists

Atropine Used primarily for _____ disorders

________ disease.
________ disease.
_________ states

A

cardiovascular

Peptic ulcer

Irritable bowel

GI hypersecretory

72
Q

Cholinergic agonists are used to Used to treat Chronic bronchitis and Asthma

T/F

A

F

It’s cholinergic antagonists Used to treat Chronic bronchitis and Asthma

73
Q

Side effects at cholinergic antagonists

________
_________
_________

_____eased salivation
____eased sweating
____eased bronchial secretions

A

Irritability
disorientation
halucination

Decr
Decr
Decr

74
Q

Structure of acetylcholine can be divided into 3 parts
Name them

A

Acyl group
Ethylene bridge
Onium group

75
Q

Side Effects of Indirect cholinomimetics
____cardia, ___tension, _____ abnormalities
___,___,______
Abdominal _____, ___eased secretions, nausea, vomiting

A

Bradycardia; hypotension; conduction

Headache, dizziness, convulsions

cramps

Incr

76
Q

Side Effects of Indirect cholinomimetics

____eased bronchial secretions
____eased Lacrimation, sweating, salivation
Loss of binocular ______

A

Incr
Incr

accommodation

77
Q

Ganglionic stimulants

Is predominantly on SYMP in what and what ?

A

Blood vessels
Sweat glands

78
Q

Ganglionic blockade

Is predominantly on SYMP in what and what ?

A

Blood vessels

79
Q

Acetylcholine has 3 parts in its structure

Mention them

A

Acyl group
Ethylene bridge
Onium group

80
Q

Modifications in Acyl group(Ch3-COO) of acetylcholine

If the methyl group is substituted with ______, it results in ______ compound

If the ester group is substituted for ____ or ____, _____ compound is formed

A

Primary amine; more potent

Ether; ketone group; more potent

81
Q

Modifications in ethylene bridge(Ch2-Ch2) of acetylcholine

Replacement of hydrogens in methyl group with ______ leads to ______ cholinergic activity. But replacing with a larger group than methyl leads to a _____ in activity

Substitution of methyl group at ____ carbon acts (selectively or non-selectively?) on _______ receptors

A

methyl group

equal or greater ; decrease

beta; selectively

MUSCARINIC

82
Q

Modifications in Onium group (N-Ch3-Ch3-Ch3) of acetylcholine

If methyl group is replaced by ———- or ______ group it produces (active or inactive?) compounds

A

ethyl group or larger alkyl

inactive

83
Q

Which amines is more active?

Pry,sec, tert

Or

Quaternary

A

Quaternary

House Pharmacology (50 decks)

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