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Cholenergic Drugs Flashcards

(49 cards)

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1
Q

what are cholenergic drugs

A
  • drugs that mimic the action of acetylcholine
  • act on the PSNS
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2
Q

categories of cholenergic drugs

A

cholinomimetics
cholinergic antagonists

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3
Q

what are cholinomimetics

A

drugs that mimic the action of ACh
direct = receptor agonists
indirect = AChE inhibitors

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4
Q

what are cholenergic antagonists

A

durgs that reduce the action of ACh
antimuscorinic or antinicotinic

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5
Q

list all the cholenergic drugs (10)

A

Acetylcholine
Bethanechol
Muscarine
Pilocarpine
Nicotine
Physostigmine
Echothiophate
Atropine
Trimethaphan
D-tubocurarine

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6
Q

which cholenergic drugs are direct acting agonsists

A

Acetylcholine
Bethanechol
Muscarine
Pilocarpine
Nicotine

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7
Q

which cholenergic drugs are indirect acting agonists (AChE inhibitors)

A

Physostigmine - intermediate acting
Echothiophate - long acting

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8
Q

which cholenergic drugs are ACh antagonists

A

atropine - muscorinic receptor antagonist
Trimethaphan - nicotinic N receptor antagonist
D-tubocurarine - nicotinic M receptor antagonist

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9
Q

which cholenergice drug is susceptible to AChE

A

Acetylcholine

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10
Q

which cholenergic drugs are agonist for muscorinic receptors

A

Acetylcholine
Bethanechol
Muscarine
Pilocarpine

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11
Q

which cholenergic drugs are agonists for nicotinic receptors

A

Acetylcholine
Nicotine

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12
Q

families of cholenergic drugs

A

Esters of choline: Not absorbed well = acetylcholine, bethanechol
Alkaloids: Absorbed well = muscarine, nicotine, pilocarpine

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13
Q

what are general features of muscarinic receptor activation

A
  • responses same as PSNS activation
  • sweat glands activated
  • endothelial-deroved relaxation of blood vessels
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14
Q

what are general features of nicotinic receptor activation

A
  • activates PSNS and SNS
  • skeletal muscle contraction
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15
Q

how does nicotine work when it binds to its receptors

A

initially stimulates and then blocks

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16
Q

which component of the SNS contains M3 receptors

A

sweat glands

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17
Q

which receptors are found on endothelial cells

A

M3 mostly (some M5)

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18
Q

examples of organs in the PSNS contain M3 receptors

A

eye
lacrimal and salivary glands
bronchi
stomach
SI
colon
genetals
bladder

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19
Q

what is glaucoma

A

increased intraocular pressure in the eye

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20
Q

which cholenergic drug is commonly used to treat glaucoma

21
Q

what effect does pilocarpine have in the eye

Study These Flashcards
A
  1. binds + activates M3 receptors on ciliary muscle - opens canal of Schlemm to drain excess fluid
  2. activates M3 receptors on sphincter muscle to cause pupil constriction
22
Q

if pilocarpine gets into systemic circulation what are its effects on the CV system

Study These Flashcards
A

heart (M2): decrease rate and force of contraction
Blood vessels (M3): stimulates production of NO (the EDRF) to dialate blood vessels
Bronchi (M3): bronchocontriction and increased mucus secretion

23
Q

effects of nicotine

Study These Flashcards
A
  • activates PSNS and SNS (nerves and adrenal gland)
  • causes skeletal muscle contraction
    = stimulates nicotinic receptors in CNS
24
Q

what is the similarity between nicotines effects in the SNS and PSNS

Study These Flashcards
A

it activates them both at Nn receptors in the ganglia

25
in most organ systems is the PSNS or SNS dominant
PSNS - e.g. when nocotine binds in the GI tract it increases smooth muscle contraction - increases motility and gland secretion
26
which tissues have no PSNS response and what is the effect when nicotine binds at ganglia
blood vessels - only have SNS response BV in organs and skin: a1 receptor = vasoconstriction BV in skeletal muscle: B2 receptor = vasodialation
27
Hydrolysis of ACh
- 2 step process that breaks ACh into acetate and choline - catalyzed by AChE - if inhibitors bind to AChE ir increases local ACh concentration, therefore effect of ACh will be amplified
28
reversible AChE inhibitors
- e.g. physostigmine - makes covalent bond with AChE - half life: 30 min - 6 hrs - usually poor absorption and distribution (but not physostigmine)
29
irreversible ACHE inhibitors
- e.g. echothiophate - covalent bond with AChE stabilized by phosphate - absorbed and distributed well
30
action of AChE inhibitors
- amplifies endogenous ACh - effects similar to direct actong cholinimimetic drugs
31
where is increased ACh seen when an AChE inhibitors act
- PSNS and SNS ganglia - tissues innervated by autonomic ACh-releasing neurons - skeletal muscle - CNS
32
PSNS path from CNS to effector cell
- preganglionic axon is cholenergic (ACh) - postganglionic axon is cholenergic (ACh) - ACh bind to M2 or M3 on effector cell
33
SNS path from CNS to effector cell
- preganglionic axon is cholenergic (ACh) - postganglionic axon is adrenergic (NE) - NE binds to a1, B1 or B2 on effector cell
34
difference with ACh amplification is SNS and PSNS
PSNS = amplified at 2 places (ganglia + neuroeffector junction) SNS = aplified at 1 place (ganglia)
35
what responses will be observed in the CV system after systemic exposure to pilocarpine
- activates M2 receptors in the heart: decreased rate and force of contraction - activates M3 receptors in blood vessels: increased activity of EDRF causing dialation of blood vessels
36
what responses will be observed in the CV system after systemic exposure to nicotine
- *found at ganglia in PSNS and SNS - activates B1 revetors in heart: increases rate and force of contraction - activates a1 in BV (organs and skin): vasoconstriction - activates B2 in BV (skeletal muscle): vasodialation
37
what responses will be observed in the CV system after systemic exposure to physostigmine
- *increase ACh at ganglia and adrenal gland - activate Nn which stimulates SNS and PSNS - activate a1 in BV (organs and skin): vasoconstriction - activate B2 in BV (skeletal muscle): vasodialation - activate M2 in heart: increase decrease rate and force of contraction
38
mushrooms as a muscarinic agonist - associated with toxicity
- contain high levels of muscarine - can cause pilocarpine overdose - cause symptoms of muscarinic excess
39
symptoms of muscarinic excess (hint: DUMBBELS)
Diarrhea - M3 cells of GI tract urination - M3 on walls of bladder Miosis - M3 on SM surrounding pupils Bradycardia - M2 on heart Bronchoconstriction - M3 on SM lining lungs Excitation (CNS) - all M receptors Lacrimation - M3 on lacrimal gland Sweating and salviation - inc. glad secretion
40
toxicities assocuated with nicotinic agonists
- symptoms of muscarinic excess (except bradycardia) - CNS complications: convulsions, coma, respiratory depression - skeletam muscle contraction followed by paralysis - increase BP and heart rate
41
toxicities associated with ortganophosphates (e.g. echothiophate)
- increased levels of AChE inhibitors = increases ACh - used as pesticides (nerve gas) - initial signs = symptoms of muscarinic excess - late signs = CNS stimulation, peripheral Nn and Nm activation
42
why are atropine and pralidoxime used to treat organophosphate poisoning?
atropine = M3 antagonist - will compete with ACh to bind M receptors pralidoxime = reactivates AChE - makes ACh levels go back to normal
43
antimuscarinic drugs - Atropine
- M receptor antagonist - has equal affinities for all M receptor subtypes - absorbed and distributed well - half life = 2 hrs - used in eye drops to dialate pupils
44
antinicotinic drugs - Trimethaphan
- ganglionic blocker - used for hypertensive crisis or dissecting aortic aneurysm - rarely used clinically - only if other drugs are ineffective
45
antinicotinic drugs - D-tubocurarine
neuromuscular blocker - used in surgical procedures to reduce skeletal muscle contraction
46
what drugs could possibly be used to treat glaucoma
pilocarpine (direct agonist) physostigmine (AChE inhibitor) echothiophate (AChE inhibitor)
47
how do pilocarpine and physostigmine work differntly to treat glaucoma
pilocarpine: M3 receptor direct agonist physostigmine: indirect agonist for M3 - increases the amount of ACh by inhibiting AChE
48
what cholenergic drugs should be avoided to treat glaucoma
atropine - muscarinic receptor antagonist would decrease the amount of ACh, therefore fluid accumulation
49
which drugs would be helpful for increasing urination and why
bethanechol: binds M3 - SM contracts - increased urination Muscarine: binds M3 - SM contracts - increased urination Pilocarpine: binds M3 - SM contracts - increased urination Nicotine: binds Nn at PSNS and SNS ganglia - PSNS dominant = contracts bladder Physostigmine: indirect M agonist - increases ACh to bind M3

Pharmacology (21 decks)

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