Cholinergics Flashcards Preview

Pharm main > Cholinergics > Flashcards

Flashcards in Cholinergics Deck (63)
1

Ach

M agonist
Tx for glaucoma

2

Pseudocholinesterase

rapidly hydrolyzes Ach in the periphery

3

Carbachol- Isopto Carbachol - structure

analog of Ach that is resistant to hydrolysis by cholinesterase

4

Carbachol- Isopto Carbachol

M agonist
Topical tx for Glaucoma

5

Methacholine- Provocoline

M agonist
Pulmonary function tests in asthma

6

Bethanocol- Urocholine

M agonist
Stimulate GI motility
treat urinary retention

7

Pilocarpine- Salagine, Ocusert Pilo

M agonist
Tx for Glaucoma
Tx for Xerostomia

8

Endrophonium (tensilon)

Cholinesterase inhibitor
Tensilon test in MG

9

Endrophonium- Tensilon half life

very short

10

Neostigmine- Prostimin
Pyridostigmine- Mestinon

Cholinesterase inhibitor
Tx Mysesthinia Gravis

11

Pyridostigmine- Mestion

Prexposure antitodal tx for nerve gas poisoning in chemical warfare

12

Physostigmine
Eserine (antilirium)

Cholinesterase Inhibitor
Tx- Atropine or other M antagonist poisoning

13

M agonists

Ach
Carbachol
Methacholine
Bethanechol
Pilocarpine

14

Reversible Cholinesterase Inhibitors

Edrophonium
Physostigmine
Neostigmine
Pyridostigmine
Rivastigmine
Donepezil
Carbamate Insecticides

15

Irreversible Cholinesterase inhibitors- MOA

Pi

16

Reversible Cholinesterase inhibitors- MOA

competitive antagonist

17

Irreversible Cholinesterase inhibitors

Parathoion- organophosphate insecticides
Sarin- other nerve gasses

18

Organophosphate Insectisides

Parathion

19

Organophosphate Insecticides- MOA

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

20

Parathion absorption

Through the skin

21

Parathion poisoning- signs

Signs of cholinesterase inhibitor poisoning

22

Parathion Tx

Atropine
Pralidoxime
symptomatix tx

23

Carbamate Insecticides- Carbaryl- absorption

Cant be absorbed through skin as much as Parathion

24

Carbamate insecticide poisoning- Signs and symptoms

sings of cholinesterase inhibitor poisoning

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