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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
Carbamate insecticide poisoning- Tx
Atropine | Pralidoxime wont work
26
DFP/ Isoflurophate- Nerve gasses- MOA
Irreversible cholinesterase inhibitors
27
DFP/ Isoflurophate- Nerve Gasses- ex
Sarin
28
Sarin poisoning- Signs
typical of cholinesterase inhibitor poisoning
29
Sarin Poisoning Tx
Atropine | Praladoxime
30
DFP/ Isoflurophate- Uses
Tx gluacoma
31
Praladoxime/ 2-Pam- Protopam- MOA
Cholinesterase reactivator
32
Pralidoxime- Uses
Tx organophosphate poisoning w/in 2 hours of exposure | Will not work on Carbamate Insecticides
33
Sildenafil, Vardenafil, Tadalafil- MOA
PDE-5 inhibitors
34
why do PDE-5 inhibotors work
PDE-5 shuts down M mediated vasodilation | PDE-5 is concentrated mostly in copus cavernosa
35
PDE-5 inhibitor AE
reflex inc in HR from systemic vasodilation visual impairment- blue green color discernment, or more sever auditory disturbances- tinnitus, hearing loss
36
PDE-5 inhibitor CI
CV conditions
37
PDE-5 inhibitor drug interactions
``` CYP3A4 interactions- ketoconozole, erythromycin, cimetidine Nitrates Ca2+ blockers Alpha 1 blockers Sympathomimetics ```
38
PDE-5 inhibitor dose adjustment
renal or hepatic disease
39
PDE-5 inhibitor PK
Sildenafil and Vardenafil last about 4 hours | Tadalafil last about 36 hours
40
Botolinum toxin- MOA
inhibits presynaptic release of Ach @ ANS and NMJ ANS- anti cholinergic effects NMJ- paralysis
41
Botulinum toxin poisoning
Death is from diaphragmatic paralysis
42
Botolinum toxin poisoning tx
Symptomatic support | Ig for toxin
43
Botulinum toxin- medical uses
BOTOX opthalamogic- NMJ blocker cosmetics
44
Muscarinic Antagonists
``` Atropine Scopolamine Dicylomine Bentyl Propantheline Glycopyrrolate Itpratopium Tiatropium Benztorpine Tiphexyphenidyl Tolrodine oxybutynin Solifenacin Tropicamide ```
45
Atropine/ Homotropine
Homotrpine- cant get into CNS | Prototypical M antagonist
46
Scopolamine/ Methoscopolamine
Methscopolamine cant get into CNS | CNS depressant- Sedation, Amnesia, prevent motion sickness and vertigo
47
Dicyclomine- Bentyl
M antagonist | Tx IBS- intestinal antisposmodic
48
Propantheline- Probanthine
M antagonist Tx IBS- intestinal antispasmodic quaternary
49
Glycopyrrolate Robinul
M antatgonist used as general M antagonist preop med in anesthesiology to dry resp secretions and inhibit vagal reflexes
50
Ipratroptium (atrovent) and Tiatropium (spiriva)
M antagonist quaternary Tx asthma and COPD tiatropium has longer duration
51
Benztropine (cogentin), Tiphexyphenidyl (Artane)
M antagonist- Centrally acting | Tx for PD or drug induced PD- anti D, anti psychotics, anti nemics
52
Tolterodine (detrol), Oxybutynin (ditropan), solifenacin (VESIcare)
M antagonist | Tx urinary incontinence form overactive bladder
53
Tropicamide (midriacyl)
M antagonist | Dilate pupil during opthamologic exam
54
Pancuronium (pavulon)
Competitive NMJ blocker
55
Succinylcholine (annectine)
Depolarizing agent- NMJ blocker
56
M agonist- effects
``` 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
M agonist- AE
``` AE- mostly tied to excessive M stim Hypotension, bradycardia Bronchoconstriction Diarrhea Cramping Urinary incontinence Excessive sweating Salivation ```
58
Cholinesterase inhibitors- effects
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
Cholinesterase Inhibitors- signs of poisoning
``` 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
M antagonists- effects
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
M antagonists- AE
``` 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
M antagonist= anticholinergic toxidrome
``` 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
M antagonist poisoning treatment
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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