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Flashcards in Auto drugs II and III Deck (48)
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1

Bethanecol: class, mech, therapeutics, important SE's, Other SE's, Misc

Class: Direct acting carbamic acid ester
Mech: Direct-acting muscarinic cholinomimetic
Thera: Post-operative and neurogenic ileus; urinary retention (bowel and bladder smooth muscle ACh-innervated)
Important SE's: SLUDGE

2

Muscarine:

Class: Direct acting non-ester alkaloid
Mech: Direct-acting muscarinic cholinomimetic
Thera: ---
Important SE's: SLUDGE

3

Pilocarpine (Salagen): how different from muscarine?

Thera: Glaucoma (ACh activates sphincter and ciliary muscles of eye)

4

Cevimeline (Evoxac): how different from muscarine?

Thera: Dry mouth (in, e.g., Sjogren's, post-radiation therapy; via increased salivation)

5

Neostigmine (Prostigmin)

Class: Indirect acting carbamate
Mech: AChE inhibitor (short acting)
Thera: Post-operative and neurogenic ileus; urinary retention; myasthenia gravis; reversal of neuromuscular blockade
Important SE's: SLUDGE + general increase in cholinergic neurotransmission; paralysis
Misc: Lasts 0.5-2 hours

6

Physostigmine (Eserine)

Class: Indirect acting carbamate
Mech: AChE inhibitor (short acting)
Thera: Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
Important SE's: SLUDGE + general increase in cholinergic neurotransmission; paralysis
Misc: Lasts 0.5-2 hours

7

Donepezil (Aricept)

Class: Indirect acting non-ester
Mech: AChE inhibitor
Thera: Alzheimer's (amplifies endogenous ACh in brain)
Important SE's: see neostigmine

8

Edrophonium (Enlon)

Class: Indirect acting non-ester
Mech: AChE inhibitor (v. short acting)
Thera: Myasthenia gravis (differentiating deficiency versus ACh crisis); ileus
Important SE's: see neostigmine
Misc: Lasts 5-15 minutes

9

Echothiophate (Phospholine)

Class: Indirect acting organophosphate
Mech: AChE inhibitor (long acting)
Thera: Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
Important SE's: SLUDGE + general increase in cholinergic neurotransmission; paralysis
Misc: Lasts >100 hours

10

Pralidoxime (Protopam)

Class: Strong nucleophile
Mech: Regenerates phosphorylated AChE
Thera: Poisoning by nerve gas, insecticide

11

Sarin

Class: Very potent indirect acting organophosphate
Mech: AChE inhibitor
Thera: Volatile nerve gas
Important SE's: see neostigmine
Other SE's: Death
Misc: Treat with pralidoxime and atropine before aging

12

Atropine

Class: Tertiary amine antimuscarinic
Mech: Blocks muscarinic receptors
Thera: Mydriasis; cycloplegia
Important SE's: General block of muscarinic functions

13

Scopolamine (Transderm-Scop): how different from atropine?

Thera: Prevent or reduce motion sickness
Misc: well-absorbed with central effects, given by injection, mouth, or transdermal patch

14

Dicyclomine (Bentyl): how different from atropine?

Thera: Reduce transient hypermotility

15

Tropicamide (Mydriacyl): how different from atropine?

Thera: Mydriasis; cycloplegia
Misc: Very rapidly metabolized

16

Tolterodine (Detrol): how different from atropine?

Thera: Treat transient cystitis; postoperative bladder spasms; incontinence

17

Benztropine (Cogentin): how different from atropine?

Thera: Treat manifestations of Parkinson's disease
Misc: Crosses BBB

18

Ipratropium (Atrovent)

Class: Quarternary amine antimuscarinic
Mech: Blocks muscarinic receptors
Thera: Bronchodilation in asthma or COPD
Important SE's: General block of muscarinic functions
Misc: can be aerosolized to maximize bronchial effects and minimize central effects

19

Tiotropium (Spiriva): how different from ipratropium?

Misc: Longer acting than ipratropium

20

Hexamethonium (Methium)

Class: Ganglionic blocker (quarternary amine)
Mech: Blocks ganglionic (Nn) receptor at both symp and parasymp ganglia, and sympathetic tone
Thera: Hypertensive crisis; "Bloodless" field surgery
Misc: Rarely used

21

Mecamylamine: how different from hexamethonium?

Can cross the BBB!!!!

22

Succinylcholine (Anectine)

Class: Depolarizing blocker
Mech: Overstimulation of nicotinic receptor (NM), leading to desensitization of muscle unit to further ACh stimulation
Thera: Brief procedures (e.g., tracheal intubation, reset dislocated joints)
Important SE's: Respiratory paralysis; disturbance of autonomic function (could affect NN type nicotinic receptors a bit)
Misc: Produces flaccid paralysis within 1 minute

23

Tubocurarine (Curare)

Class: Nondepolarizing blocker
Mech: Blocks nicotinic (Nm) receptor
Thera: Muscle relaxant for surgery w/o deep anesthesia
Important SE's: Respiratory paralysis; disturbance of autonomic function
Misc: Lasts 30-60 minutes

24

Mivacurium (Mivacron)

Class: Nondepolarizing blocker
Mech: Blocks nicotinic (Nm) receptor
Thera: Muscle relaxant for surgery w/o deep anesthesia
Important SE's: Respiratory paralysis; disturbance of autonomic function
Misc: Rapidly hydrolyzed, short acting

25

Botulinum toxin A (Botox)

Class: Local paralytic
Mech: Blocks vesicle fusion and ACh release on presynaptic terminal by degrading SNAP-25
Thera: Reduce frown lines and wrinkles; achalasia; strabismus; oromandibular dystonia

26

Typical location of the M1 receptor?

CNS neurons, symp postgang neurons, some presynaptic sites

27

M2 receptor locations?

Myocardium, smooth muscle, some presynaptic sites; CNS neurons

28

M3 receptor locations?

Exocrine glands, vessels (smooth muscle and endothelium ); CNS neurons

29

M4 receptor locations?

CNS neurons; possibly vagal nerve endings

30

M5 receptor locations?

Vascular endothelium, especially cerebral vessels; CNS neurons