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Pharmacology > Parasympathetic Drugs > Flashcards

Parasympathetic Drugs Flashcards

0
Q

Metacholine

A
  • M agonist
  • PS effects
  • to Tx glaucoma
  • 4o amine-poorly absorbed
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1
Q

Acetylcholine

A
  • N and M agonist
  • PS effects
  • to tx glaucoma
  • 4o amine-poorly absorbed
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2
Q

Carbachol

A
  • N and M agonist
  • AChE resistant
  • PS effects
  • used to Tx glaucoma
  • 4o amine- poorly absorbed
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3
Q

Bethanechol

A
  • M agonist (M1-M3 R’s)
  • AChE resistant
  • PS effects, and: +GI motility and tone, expel urine
  • Tx: urinary retention, post-op ileus
  • 4o amine- poorly absorbed
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4
Q

Cevilimine

A
  • M agonist (M3 selective)
  • increase secretions (tears and salivation)
  • to Tx Sjögren’s syndrome
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5
Q

Pilocarpine

A
  • M agonist
  • AChE resistant
  • PS effect + rapid miosis, accomodation spasm
  • Tx: glaucoma, Sjögren’s syndrome
  • 3o amine/alkaloid (CNS access)
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6
Q

Muscarine

A
  • M agonist (minorly N)

- alkaloid, 4o amine

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7
Q

Nicotine

A
  • N agonist (minorly M)
  • for smoking cessation
  • alkaloid, has CNS access
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8
Q

Vareniciline

A
  • N agonist (and alpha2, beta3) in CNS

- for smoking cessation

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9
Q

Lobeline

A
  • N agonist (minorly m)

- alkaloid)

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10
Q

Edrophonium

A
  • AChE block -> ^ACh
  • side effect: cholinergic crisis (Tx w/ atropine)
  • use to diagnose myasthenia gravis (Tensilon test)
  • short acting, reversible
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11
Q

Ambenonium

A
  • AChE block -> ^ACh
  • carbamate
  • to Tx myasthenia gravis
  • oral admin
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12
Q

Demecarium

A
  • AChE block -> ^ACh
  • carbamate
  • to Tx glaucoma
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13
Q

Physostigmine

A
  • AChE block -> ^ACh
  • intensifies NMJ action, decrease intraocc P, bronchoconstriction
  • Tx: glaucoma; TCA, phenothiazine, & atropine (anticholinergic) OD; post-op ileus and urinary retention
  • med acting; 3o amine; reversible
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14
Q

Neostigmine

A
  • AChE block -> ^ACh
  • Tx: post-op ileus, urinary retention, myasthenia gravis, NMJ block reversal
  • med acting
  • 4o amine- poorly absorbed; reversible; stronger NMJ effect
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15
Q

Carbaryl

A
  • AChE block -> ^ACh
  • carbamate
  • reversible
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16
Q

Pyridostigmine

A
  • AChE block -> ^ACh
  • carbamate
  • Tx: chronic management of myasthenia gravis
  • med acting; 4o amine-poorly absorbed
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17
Q

Tacrine

A
  • AChE block -> ^ACh
  • to Tx Alzheimers
  • reversible
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18
Q

Donepezil, Galantamine, Rivastigmine

A
  • selective AChE block -> ^ACh
  • to Tx Alzheimers
  • reversible
19
Q

Echothiophate

A
  • AChE block -> ^ACh
  • organophosphate (irreversible, long acting)
  • to Tx glaucoma
  • not well absorbed
20
Q

Parathion/Paraoxon

A
  • AChE block -> ^ACh
  • organophosphate (irreversible, long acting)
  • insecticide- poisonous humans can convert to active form, paraoxon
  • well-absorbed
21
Q

Malathion/Malaoxon

A
  • AChE block -> ^ACh
  • organophosphate (irreversible, long acting)
  • insecticide
  • well-absorbed
22
Q

Soman and Sarin

A
  • AChE block -> ^ACh
  • chemical warfare poison
  • organophosphate (irreversible, long acting)
  • absorbed excessively well; high toxicity
23
Q

anti-muscarinic effects and clinical uses

A
  • increase: HR, CNS (excitation), intraocc P, pupil dilation
  • decrease: glandular secretions, GI/bladder motility (via SM relaxation)
  • to Tx: cholinergic reversal (organoP OD), ulcers, IBS, bradycardia, sedation; CONTRAINDICATED in glaucoma
24
Q

atropine

A
  • M block
  • anti-muscarinic effects and clinical uses; mandatory for cholinergic OD
  • 3o amine- CNS access
  • most potent anticholinergic
25
Q

Scopolamine

A
  • M block
  • anti-muscarinic effects and clinical uses; to Tx: motion sickness; causes sedation (Amazonian zombie death)
  • 3o amine- CNS access (more than atropine)
26
Q

Ipratropium

A
  • M block
  • anti-muscarinic effect and clinical uses +Tx: COPD and asthma
  • 4o amine- local effects in lung
27
Q

Pirenzapine

A
  • M1 block
  • anti-muscarinic effects and clinical uses
  • tricyclic; targets gastric parietal cell
  • CNS access (tertiary amine)
28
Q

Oxybutinin (and daritenacin and Solifenacin- more selective)

A
  • M3 block
  • decrease detrussor mm tone/spasms via SM relaxation
  • to Tx urge incontinence and post-op spasms
29
Q

Dicyclomine

A
  • M block
  • to Tx peptic disease, hyermotile gut, IBS, minor diarrhea
  • CNS access (tertiary amine)
30
Q

Tropicamide

A
  • M block
  • to Tx mydriasis, cycloplegia; used by ophthalmologist to dilate eye
  • CNS access (tertiary amine)
31
Q

Propantheline

A
  • M block
  • to Tx peptic disease, hypermotile gut
  • quaternary amine- stays in GI tract
32
Q

Glycopyrrolate

A
  • M block
  • to Tx peptic disease, hypermotile gut
  • quaternary amine- stays in GI tract
33
Q

Tiotropium

A
  • M block
  • decreases secretions to Tx asthma, COPD
  • 4o amine- local fx in lung
34
Q

Benztropine

A
  • M block
  • to Tx Parkinsons
  • 3o amine- CNS access
35
Q

Hexamethonium

A
  • Ganglionic blocker (Nn antag)

- depends on prevailing autonomic tone

36
Q

Decamethonium

A
  • ganglionic blocker (Nn antag)

- fx depend of prevailing autonomic tone

37
Q

Mecamylamine

A
  • ganglionic blocker (Nn antag)
  • fx depend on prevailing autonomic tone
  • CNS access- can cause sedation, tremor, mental aberrations
  • erratic oral absorption
38
Q

Tetraethylamine

A
  • ganglionic blocker (Nn antag)
  • fx depend on prevailing autonomic tone
  • can’t cross BBB; very short acting
39
Q

Trimethaphan

A
  • ganglionic blocker (Nn antag)
  • sympa dominates arterioles -> ganglionic block causes BP to fall
  • to Tx HTN emergency
  • can’t cross BBB; short acting; inactive orally
40
Q

Pralidoxime (2-PAM)

A
  • hi affinity (magnet) for P’s -> rescues aging of P groups that occurs d/t AChEI’s
  • to Tx early-stage (48hrs) AChEI poisoning
  • not effective against carbamates
41
Q

Diacetylmonoxime

A

-rescue aging of P groups d/t AChEI’s

42
Q

Hemocholinium

A

blocks pre-synaptic choline txporter (no ACh synth)

-> decrease ACh

43
Q

Vesamicol

A

ACh vesiclular txporter block (no ACh packaging)

-> decrease ACh

44
Q

Spider venom (black widow)

A

ACh release -> ^ACh

45
Q

Botulinum toxin

A

ACh exocytosis block

-> decrease ACh

Pharmacology (2 decks)

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