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Pharmacology Mod 4 > Lecture 1: cholinergic agonists and anatgonists > Flashcards

Lecture 1: cholinergic agonists and anatgonists Flashcards

1
Q

What type of neurologic function is not under direct, conscious control

A

Autonomous neurologic function

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2
Q

what is the autonomic system primarily concerned with

A

visceral functions necessary to sustain life

i.e. cardiac output, blood flow distribution and digestion

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3
Q

What is the autonomic neurologic system broken into

A

sympathetic and parasympathetic nervous systems and enteric nervous system is the third division

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4
Q

What are the primary transmitter molecules

A

acetylcholine and norepinephrine

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5
Q

what type of fibers release acetylchonile

A

cholinergic fibers

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6
Q

what type of fibers are cholinergic

A

preganglionic efferent autonomic fibers and the somatic (non-automatic) motor fibers to skeletal muscle

most parasympathetic prostaganglionic and some sympathetic postganglionic fibers

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7
Q

what is released by adrenergic fibers

A

norepinepherine

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8
Q

what are the primary acetylcholine receptor subtypes

A

muscarinic and nicotinic receptors

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9
Q

what is an adrenoceptor

A

receptor that respond to catecholamines such as norepinepherine

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10
Q

what does the term cholinoceptor denote

A

receptors (both muscarinic and nicotinic) that respond to acetylcholine

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11
Q

what are adrenoceptos subdivided into

A

alpha-adrenoceptor and beta-adrenoceptor and dopamine-receptor types

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12
Q

How are cholinomimetics classified

A

by their MOA because some bind directly to (and activate) cholinoceptors, whereas others act indirectly by inhibiting the hydrolysis of endogenous acetylcholine

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13
Q

what do direct acting cholinomimetic agents bind to and activate

A

muscarinic and nicotinic receptors

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14
Q

What do the muscarinic receptors effect

A

nerve, heart and smooth muscles, glands and endothelium

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15
Q

what do nicotinic receptors effect

A

neuromuscular end plate, skeletal muscles, autonomic ganglion cells and central nervous system

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16
Q

What organ systems are effected by cholinoceptor-activating agents (muscarinic agonists)

A

eyes
Cardiovascular system
respiratory system
GI system
GU system

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17
Q

How do muscarinic agnoists effect the eyes

A

contraction of of the smooth muscle of the iris (resulting in miosis) and ciliary muscle (resulting in accommodation of the lens)

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18
Q

how do muscarinic agonists effect the cardiovascular system

A

increase in potassium current in the cells of the SA and AV nodes and Purkinjecentricular cells

decrease in slow inward calcium current

reduction in current that underlies diastolic depolarization

end result = slowing of the pacemaker rate

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19
Q

how do muscarinic agonists effect the respiratory system

A

contraction of smooth muscle in bronchial tree
increased secretion by glands in tracheobrachial mucosa

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20
Q

how do muscarinic agonist effect the GI system

A

increased motor and secretory activity of the gut
stimulation of salivary and gastric glands

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21
Q

how do muscarinic agonists effect the GU system

A

stimulation of detrusor muscle
relaxation of the trigone and sphincter muscles

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22
Q

what are the side effects of cholinergic agonists

A

diarrhea
diaphoresis
miosis
nausea
urinary urgency

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23
Q

what organ systems are effected by indirect-acting chilinomimetics

A

eye, respiratory tract, GI, urinary tract, CNS, cardiovascular and Neruomuscular junction

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24
Q

how do indirect acting cholinomimetics effect the CNS

A

diffuse EEG activation and subjective alter response improvement

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25
Q

how do indirect-acting cholinomimetics effect the cardiovascular system

A

mimic effects of vagal nerve activation on the heart
negative chronotropy, dromotropy and inotropy occurs; cardiac output falls

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26
Q

how do indirect-acting cholinomimetics effect the cardiovascular system

A

increased strength of contraction (of skeletal muscle)

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27
Q

what are the clinical uses of acetylcholine

A

direct-acting cholinergic agonist

causes brief decrease in HR and cardiac output

decreased BP due to vasodilation via activity of muscarinic receptors that cause endothelial release of nitric oxide

increase salivation and intestinal motility; increase bronchial secretions, detrusor muscle action

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28
Q

what are the clinical uses of Bethanchol

A

mostly used in GU disease (stimulates detrusor muscle of the bladder and relaxes the trigoone and spincter msucles - resulting in urination)

used to stimulate atonic bladder, mostly in post-partum or post-operative settings

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29
Q

What are the clinical uses of Pilocarpine

A

primarily used in ophthalmology
applied topically to the eye to produce rapid miosis and contraction of ciliary muscles (glaucoma)

may be useful in promoting salivation in patients with xerostomia

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30
Q

what are direct-acting cholinergic agent drugs

A

acetylcholine, bethanchol and pilocarpine

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31
Q

what drug is used for emergency lowering of intraocular pressure in glacuoma

A

Pilocarpine

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32
Q

how does pilocarpine work on glaucoma treatment

A

acts on the muscarinic receptors of the iris, causing it to contract - leads to construction of the pupil and movement of the iris away from the angle

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33
Q

What are the indirect-acting cholinergic agent medications

A

edrophonium
pyridostigmine/neostigmine
physostigmine
echothiophate

34
Q

What is the clinicial use of edrophonium

A

primarily in the diagnosis of M. gravis, an autoimmune disease caused by antibodies to the nicotinic receptor in the NMJ

35
Q

how does endrophonium interact within the body

A

indirect-acting cholinergic agent

binds reversibly to the active center of acetylcholinesterase, preventing hydrolysis of Ach

36
Q

What is the Tensilon test

A
37
Q

how is pyridostigmine/neostigmine used clinically

A

chonic management of M. gravis

38
Q

how is pyridostigmine/neostigmine prescribed

A

taken 4-5 times a day to have a therapeutic effect of M. gravis

duration of action is 3-6 hours

39
Q

how is physostigmine used clinically

A

used to treat atropine (anticholinergic drug) overdoses - miosis, hypotension, bradicardia

40
Q

what does physostigmine stimulate

A

muscarinic and nicotinic sites of the ANS, as well as nicotinic receptors of the NMJ

41
Q

what does physostigmine bind with

A

acetylcholinesterase, make it reversibly inactivated

42
Q

how is echothiophate used clinically

A

only therapeutic use is in the treatment of ocular hypotension in chronic glaucoma
- produces intense miosis when used topically on the eyes
- symptoms be reversed with high doses of atropine
can cause cataracts at high doses; limit its use

43
Q

what is echothiophate

A

IRREVERSIBLE indirect-acting cholinergic agonist
an organophosphate that covalently binds to a phosphate group of AChE, making it permanently inactivated

44
Q

what is commonly used in the US as an insecticide and in chemical warfare

A

organophosphate compounds are irreversible acetylcholinesterase inhibitors

45
Q

what is anticholinesterase toxicity

A

both muscarinic and nicotinic signs are present in states of toxicity
- increased urination, bradycardia, excessive secretions, pupillary constrictions

46
Q

what medication is used to reverse anticholinesterase toxicity

A

Pralidoxime - can only reactivate AChE in the periphery; cannot reverse CNS effects of ACHEi toxicity

47
Q

what does Parlidoxime reactivate

A

AChE in the periphery

48
Q

How are cholinoceptor blocking drugs divided

A

into muscarinic and nicotinic subgroups
Ganglionic blockers - preference for nicotinic receptors
neuromuscular-blocking agent (nicotinic antagonists)

49
Q

What type of drug is atropine

A

‘prototype” anti-muscarinic drug

50
Q

what are the clinical uses of atropine

A

acts primarily on salivary, bronchial and sweat glands
some effect on acid secretion by gastric partial cells

51
Q

what is atropine highly selective for

A

muscarinic receptors - though does not distinguish among subgroups of muscarinic receptors
acts centrally and peripherally

52
Q

what organ systems are affected by atropine

A

CNS
Eye
respiratory
cardiovascular
GI
GU

53
Q

how does atropine effect the CNS

A

minimal effect

54
Q

how does atropine effect the Eye

A

causes mydraisis, cycloplegia (inability to focus for near vision)
reduces lacrimation

55
Q

how does atropine effect the respiratory system

A

causes bronchiodilation - reduces airway secretions

56
Q

how does atropine effect the cardiovascular systems

A

causes tachycardia (via blockage of vagal slowing), though little effect on BP
Reduces PR interval
blocks vasodilation of coronary arteries (and of skeletal muscle vascular bed)

57
Q

how does atrophine effect GI system

A

decreases salivary secretions markedly; some gastric acid secretion is suppressed
prolongs gastric emptying time and interstitial transit time

58
Q

how does atrophine effect GU system

A

relates ureteral and bladder wall smooth muscle, may precipitate urinary retention

59
Q

what are the simplified cholinergic antagoists effects

A

blurry vision, mydriasis
decreased lacrimation, salivation, sweating
confusion
constipation, Urinary retention

“mad as a hatter, hot as hell, red as a beet, dry as a bone and blind as a bat”

60
Q

What are the therapeutic uses for atropine

A

topical can be used to induce mydriasis and cycloplegia in order to measure refractive errors in the lens
IV - reverse dangerous bradycardia

sometimes used as an anti-secretory agent to block secretions in the upper and lower respiratory tract prior to surgery

used to reverse the effect of organophosphate toxicity, mushroom poisoning

61
Q

what is scopolamine used for

A

used to combat motion sickness - used in patch form - popular agent to use on cruise ships

62
Q

what may scopolamine cause

A

sedating effect

63
Q

what does scopolamine have a greater effect for

A

greater CNS effects unlike atropine

64
Q

how is ipratropium and tiotropium used

A

used as inhalation drugs in COPD, either alone or in combination with a long acting beta-adrenoceptor agonists; tiotropium is long-acting form of ipratropium

65
Q

what are iprotropium and tiotropium powerful for

A

bronchodilator

synthetic analogs of atropine

66
Q

why are iprotropium and tiotropium administered via aerosol routes

A

allows for maximal targeting of bronchial tissue to reduce systemic effects

67
Q

what are ganglionic blockers

A

agents that block nicotinic receptors of both parasympathetic and sympathetic autonomic ganglion

68
Q

what is the sole drug in the ganglionic blockers

A

Nicotine

69
Q

what are neuromuscular blockers

A

drugs that block cholinergic transmission between the motor nerve endings and nictoninic receptors on skeletal muscle

70
Q

how do neuromuscular blockers act

A

either as antagonist of ACh (non-depolarizing type) at the nicotinic receptor
or
agnostic that causes desensitization of ACh (depolarizing type) at the receptors on the endplate of the MNJ

71
Q

when are neuromuscular blockers beneficial

A

during surgery to facilitate tracheal intubation and provide complete muscle relaxation - allows for more rapid recovery from anesthesia that other sedating agents

72
Q

what are examples of non-depolarizing blockers

A

rocuronium, vecuronium

73
Q

at low doses what are non-depolarizing blockers competitive for

A

they competitively block Ach at nicotinic receptors

74
Q

what muscles are paralyzied first with non-depolarizing blockers

A

smaller muscles (facial and ocular muscles) then fingers, limbs, neck, trunk muscles

75
Q

what muscles are affected last with non-depolarizing blockers

A

respiration muscles (intercostals, diaphragm)

76
Q

how are non-depolarizing blockers administered

A

IV and IM
they are minimally bioavailable when consumed orally

77
Q

what do non-depolarizing blockers not enter

A

CNS or cross the blood-brain barrier

78
Q

what is the only depolarizing blockers

A

succinylcholine - muscle relaxant

79
Q

how do depolarizing blockers work

A

cause cell membrane depolarization, resulting in an initial discharge that produces transient fasciculations in the muscle itself, followed by flaccid paralysis

80
Q

when using succinylcholine what muscles are paralyzed last

A

respiratory muscles

81
Q

what is succinylcholine useful for

A

when rapid intubation is required during induction of anesethia

82
Q

how is succinylcholine administered

A

IV

Pharmacology Mod 4 (2 decks)

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