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Cholinergics Flashcards

1
Q

Ach

A

M agonist

Tx for glaucoma

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2
Q

Pseudocholinesterase

A

rapidly hydrolyzes Ach in the periphery

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3
Q

Carbachol- Isopto Carbachol - structure

A

analog of Ach that is resistant to hydrolysis by cholinesterase

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4
Q

Carbachol- Isopto Carbachol

A

M agonist

Topical tx for Glaucoma

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5
Q

Methacholine- Provocoline

A

M agonist

Pulmonary function tests in asthma

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6
Q

Bethanocol- Urocholine

A

M agonist
Stimulate GI motility
treat urinary retention

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7
Q

Pilocarpine- Salagine, Ocusert Pilo

A

M agonist
Tx for Glaucoma
Tx for Xerostomia

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8
Q

Endrophonium (tensilon)

A

Cholinesterase inhibitor

Tensilon test in MG

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9
Q

Endrophonium- Tensilon half life

A

very short

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10
Q

Neostigmine- Prostimin

Pyridostigmine- Mestinon

A

Cholinesterase inhibitor

Tx Mysesthinia Gravis

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11
Q

Pyridostigmine- Mestion

A

Prexposure antitodal tx for nerve gas poisoning in chemical warfare

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12
Q

Physostigmine

Eserine (antilirium)

A

Cholinesterase Inhibitor

Tx- Atropine or other M antagonist poisoning

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13
Q

M agonists

A 
Ach
Carbachol
Methacholine
Bethanechol
Pilocarpine
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14
Q

Reversible Cholinesterase Inhibitors

A 
Edrophonium
Physostigmine
Neostigmine
Pyridostigmine
Rivastigmine
Donepezil
Carbamate Insecticides
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15
Q

Irreversible Cholinesterase inhibitors- MOA

A

Pi

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16
Q

Reversible Cholinesterase inhibitors- MOA

A

competitive antagonist

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17
Q

Irreversible Cholinesterase inhibitors

A

Parathoion- organophosphate insecticides

Sarin- other nerve gasses

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18
Q

Organophosphate Insectisides

A

Parathion

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19
Q

Organophosphate Insecticides- MOA

A

activated to Paroxone- happens faster in misquitos and they cant clear the metabolites

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20
Q

Parathion absorption

A

Through the skin

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21
Q

Parathion poisoning- signs

A

Signs of cholinesterase inhibitor poisoning

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22
Q

Parathion Tx

A

Atropine
Pralidoxime
symptomatix tx

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23
Q

Carbamate Insecticides- Carbaryl- absorption

A

Cant be absorbed through skin as much as Parathion

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24
Q

Carbamate insecticide poisoning- Signs and symptoms

A

sings of cholinesterase inhibitor poisoning

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25
Q

Carbamate insecticide poisoning- Tx

A

Atropine

Pralidoxime wont work

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26
Q

DFP/ Isoflurophate- Nerve gasses- MOA

A

Irreversible cholinesterase inhibitors

27
Q

DFP/ Isoflurophate- Nerve Gasses- ex

28
Q

Sarin poisoning- Signs

A

typical of cholinesterase inhibitor poisoning

29
Q

Sarin Poisoning Tx

A

Atropine

Praladoxime

30
Q

DFP/ Isoflurophate- Uses

A

Tx gluacoma

31
Q

Praladoxime/ 2-Pam- Protopam- MOA

A

Cholinesterase reactivator

32
Q

Pralidoxime- Uses

A

Tx organophosphate poisoning w/in 2 hours of exposure

Will not work on Carbamate Insecticides

33
Q

Sildenafil, Vardenafil, Tadalafil- MOA

A

PDE-5 inhibitors

34
Q

why do PDE-5 inhibotors work

A

PDE-5 shuts down M mediated vasodilation

PDE-5 is concentrated mostly in copus cavernosa

35
Q

PDE-5 inhibitor AE

A

reflex inc in HR from systemic vasodilation
visual impairment- blue green color discernment, or more sever
auditory disturbances- tinnitus, hearing loss

36
Q

PDE-5 inhibitor CI

A

CV conditions

37
Q

PDE-5 inhibitor drug interactions

A 
CYP3A4  interactions- ketoconozole, erythromycin, cimetidine
Nitrates
Ca2+ blockers
Alpha 1 blockers
Sympathomimetics
38
Q

PDE-5 inhibitor dose adjustment

A

renal or hepatic disease

39
Q

PDE-5 inhibitor PK

A

Sildenafil and Vardenafil last about 4 hours

Tadalafil last about 36 hours

40
Q

Botolinum toxin- MOA

A

inhibits presynaptic release of Ach @ ANS and NMJ
ANS- anti cholinergic effects
NMJ- paralysis

41
Q

Botulinum toxin poisoning

A

Death is from diaphragmatic paralysis

42
Q

Botolinum toxin poisoning tx

A

Symptomatic support

Ig for toxin

43
Q

Botulinum toxin- medical uses

A

BOTOX
opthalamogic- NMJ blocker
cosmetics

44
Q

Muscarinic Antagonists

A 
Atropine
Scopolamine
Dicylomine
Bentyl
Propantheline
Glycopyrrolate
Itpratopium
Tiatropium
Benztorpine
Tiphexyphenidyl
Tolrodine
oxybutynin
Solifenacin
Tropicamide
45
Q

Atropine/ Homotropine

A

Homotrpine- cant get into CNS

Prototypical M antagonist

46
Q

Scopolamine/ Methoscopolamine

A

Methscopolamine cant get into CNS

CNS depressant- Sedation, Amnesia, prevent motion sickness and vertigo

47
Q

Dicyclomine- Bentyl

A

M antagonist

Tx IBS- intestinal antisposmodic

48
Q

Propantheline- Probanthine

A

M antagonist
Tx IBS- intestinal antispasmodic
quaternary

49
Q

Glycopyrrolate Robinul

A

M antatgonist
used as general M antagonist
preop med in anesthesiology to dry resp secretions and inhibit vagal reflexes

50
Q

Ipratroptium (atrovent) and Tiatropium (spiriva)

A

M antagonist
quaternary
Tx asthma and COPD
tiatropium has longer duration

51
Q

Benztropine (cogentin), Tiphexyphenidyl (Artane)

A

M antagonist- Centrally acting

Tx for PD or drug induced PD- anti D, anti psychotics, anti nemics

52
Q

Tolterodine (detrol), Oxybutynin (ditropan), solifenacin (VESIcare)

A

M antagonist

Tx urinary incontinence form overactive bladder

53
Q

Tropicamide (midriacyl)

A

M antagonist

Dilate pupil during opthamologic exam

54
Q

Pancuronium (pavulon)

A

Competitive NMJ blocker

55
Q

Succinylcholine (annectine)

A

Depolarizing agent- NMJ blocker

56
Q

M agonist- effects

A 
Inc GI motility and secretion
Dec HR
Dec BP b/c dec CO and vasodilation
Bladder contraction, sphincter relax
Miosis and dec in intraocular P
Stim of secretions
Salivation
Lacrimation
GI secretions
sweating
�
57
Q

M agonist- AE

A 
AE- mostly tied to excessive M stim
Hypotension, bradycardia
Bronchoconstriction
Diarrhea
Cramping
Urinary incontinence
Excessive sweating
Salivation
58
Q

Cholinesterase inhibitors- effects

A

Act by preventing Ach breakdown
Inc GI motility and Sec
Bladder contraction, sphincter relaxation
Bradycardia, hypotension
Inc secretions- salivation, lacrimation, sweat
Dec intraocular pressure
Skeletal muscle stim @ low dose, paralysis @ high dose (M vs N effect and dose)
Bronchoconstriction

59
Q

Cholinesterase Inhibitors- signs of poisoning

A 
oxic effects- may be sever in cholinergic crisis OD situation, organophosphate insecticide/nerve gas poisoning
SLUDGE
Salivation
Lacrimation
Urination
Defecation
GI distress
Emesis
Skeletal muscle- fasciculation  paralysis
Bardycardia, hypotension, shock
Severe miosis
CNS stim & seizure  Coma
Chronic exposure assoc w/ demyelination
60
Q

M antagonists- effects

A

Effects- main effect is competitive antagonism @ M
Dry secretions
Dec tone and motility of GI
Relax bladder and urine retention
Bronchodilation
Mydriasis w/ cyloplegia and inc in intracoccular P
Inc HR- Atropine may cause slight transient Brady
CNS- sedation and amnesia @ low dose, excitation and seizure @ high. Not all have CNS effects

61
Q

M antagonists- AE

A 
AE- extension of Anti M axn
Dry mouth
Dry hot skin
Constipation, urine retention
Visual disturbances, blurred vision
Photophobia
CNS effects
Sedation
Confusion
Amnesia esp in elderly pts
62
Q

M antagonist= anticholinergic toxidrome

A 
Anti M= anticholinergic toxidrome
Dry hot skin
Hyperthermia
Severe mydriasis
Blurred vision
Photophobia
CNS stim
Agitation
Hallucinations
Seizures  coma  death
Cessation of GI mobility
Weak, tachy pulse + arrhythmias
63
Q

M antagonist poisoning treatment

A

Tx
Physostigmine or other cholinesterase inhibitors
Benzodiazepines for seizures
Ice baths to reduce hyperthermia
Keep pt in dark, quite area to prevent photophobia and excitement
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