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

Lecture 1: cholinergic agonists and anatgonists Flashcards

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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
how do indirect-acting cholinomimetics effect the cardiovascular system
mimic effects of vagal nerve activation on the heart negative chronotropy, dromotropy and inotropy occurs; cardiac output falls
26
how do indirect-acting cholinomimetics effect the cardiovascular system
increased strength of contraction (of skeletal muscle)
27
what are the clinical uses of acetylcholine
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
28
what are the clinical uses of Bethanchol
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
29
What are the clinical uses of Pilocarpine
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
30
what are direct-acting cholinergic agent drugs
acetylcholine, bethanchol and pilocarpine
31
what drug is used for emergency lowering of intraocular pressure in glacuoma
Pilocarpine
32
how does pilocarpine work on glaucoma treatment
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
33
What are the indirect-acting cholinergic agent medications
edrophonium pyridostigmine/neostigmine physostigmine echothiophate
34
What is the clinicial use of edrophonium
primarily in the diagnosis of M. gravis, an autoimmune disease caused by antibodies to the nicotinic receptor in the NMJ
35
how does endrophonium interact within the body
indirect-acting cholinergic agent binds reversibly to the active center of acetylcholinesterase, preventing hydrolysis of Ach
36
What is the Tensilon test
37
how is pyridostigmine/neostigmine used clinically
chonic management of M. gravis
38
how is pyridostigmine/neostigmine prescribed
taken 4-5 times a day to have a therapeutic effect of M. gravis duration of action is 3-6 hours
39
how is physostigmine used clinically
used to treat atropine (anticholinergic drug) overdoses - miosis, hypotension, bradicardia
40
what does physostigmine stimulate
muscarinic and nicotinic sites of the ANS, as well as nicotinic receptors of the NMJ
41
what does physostigmine bind with
acetylcholinesterase, make it reversibly inactivated
42
how is echothiophate used clinically
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
what is echothiophate
IRREVERSIBLE indirect-acting cholinergic agonist an organophosphate that covalently binds to a phosphate group of AChE, making it permanently inactivated
44
what is commonly used in the US as an insecticide and in chemical warfare
organophosphate compounds are irreversible acetylcholinesterase inhibitors
45
what is anticholinesterase toxicity
both muscarinic and nicotinic signs are present in states of toxicity - increased urination, bradycardia, excessive secretions, pupillary constrictions
46
what medication is used to reverse anticholinesterase toxicity
Pralidoxime - can only reactivate AChE in the periphery; cannot reverse CNS effects of ACHEi toxicity
47
what does Parlidoxime reactivate
AChE in the periphery
48
How are cholinoceptor blocking drugs divided
into muscarinic and nicotinic subgroups Ganglionic blockers - preference for nicotinic receptors neuromuscular-blocking agent (nicotinic antagonists)
49
What type of drug is atropine
'prototype" anti-muscarinic drug
50
what are the clinical uses of atropine
acts primarily on salivary, bronchial and sweat glands some effect on acid secretion by gastric partial cells
51
what is atropine highly selective for
muscarinic receptors - though does not distinguish among subgroups of muscarinic receptors acts centrally and peripherally
52
what organ systems are affected by atropine
CNS Eye respiratory cardiovascular GI GU
53
how does atropine effect the CNS
minimal effect
54
how does atropine effect the Eye
causes mydraisis, cycloplegia (inability to focus for near vision) reduces lacrimation
55
how does atropine effect the respiratory system
causes bronchiodilation - reduces airway secretions
56
how does atropine effect the cardiovascular systems
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
how does atrophine effect GI system
decreases salivary secretions markedly; some gastric acid secretion is suppressed prolongs gastric emptying time and interstitial transit time
58
how does atrophine effect GU system
relates ureteral and bladder wall smooth muscle, may precipitate urinary retention
59
what are the simplified cholinergic antagoists effects
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
What are the therapeutic uses for atropine
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
what is scopolamine used for
used to combat motion sickness - used in patch form - popular agent to use on cruise ships
62
what may scopolamine cause
sedating effect
63
what does scopolamine have a greater effect for
greater CNS effects unlike atropine
64
how is ipratropium and tiotropium used
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
what are iprotropium and tiotropium powerful for
bronchodilator synthetic analogs of atropine
66
why are iprotropium and tiotropium administered via aerosol routes
allows for maximal targeting of bronchial tissue to reduce systemic effects
67
what are ganglionic blockers
agents that block nicotinic receptors of both parasympathetic and sympathetic autonomic ganglion
68
what is the sole drug in the ganglionic blockers
Nicotine
69
what are neuromuscular blockers
drugs that block cholinergic transmission between the motor nerve endings and nictoninic receptors on skeletal muscle
70
how do neuromuscular blockers act
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
when are neuromuscular blockers beneficial
during surgery to facilitate tracheal intubation and provide complete muscle relaxation - allows for more rapid recovery from anesthesia that other sedating agents
72
what are examples of non-depolarizing blockers
rocuronium, vecuronium
73
at low doses what are non-depolarizing blockers competitive for
they competitively block Ach at nicotinic receptors
74
what muscles are paralyzied first with non-depolarizing blockers
smaller muscles (facial and ocular muscles) then fingers, limbs, neck, trunk muscles
75
what muscles are affected last with non-depolarizing blockers
respiration muscles (intercostals, diaphragm)
76
how are non-depolarizing blockers administered
IV and IM they are minimally bioavailable when consumed orally
77
what do non-depolarizing blockers not enter
CNS or cross the blood-brain barrier
78
what is the only depolarizing blockers
succinylcholine - muscle relaxant
79
how do depolarizing blockers work
cause cell membrane depolarization, resulting in an initial discharge that produces transient fasciculations in the muscle itself, followed by flaccid paralysis
80
when using succinylcholine what muscles are paralyzed last
respiratory muscles
81
what is succinylcholine useful for
when rapid intubation is required during induction of anesethia
82
how is succinylcholine administered
IV

Pharmacology Mod 4 (2 decks)

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