Parasympathetic Drugs Flashcards
0
Q
Metacholine
A
- M agonist
- PS effects
- to Tx glaucoma
- 4o amine-poorly absorbed
1
Q
Acetylcholine
A
- N and M agonist
- PS effects
- to tx glaucoma
- 4o amine-poorly absorbed
2
Q
Carbachol
A
- N and M agonist
- AChE resistant
- PS effects
- used to Tx glaucoma
- 4o amine- poorly absorbed
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
4
Q
Cevilimine
A
- M agonist (M3 selective)
- increase secretions (tears and salivation)
- to Tx Sjögren’s syndrome
5
Q
Pilocarpine
A
- M agonist
- AChE resistant
- PS effect + rapid miosis, accomodation spasm
- Tx: glaucoma, Sjögren’s syndrome
- 3o amine/alkaloid (CNS access)
6
Q
Muscarine
A
- M agonist (minorly N)
- alkaloid, 4o amine
7
Q
Nicotine
A
- N agonist (minorly M)
- for smoking cessation
- alkaloid, has CNS access
8
Q
Vareniciline
A
- N agonist (and alpha2, beta3) in CNS
- for smoking cessation
9
Q
Lobeline
A
- N agonist (minorly m)
- alkaloid)
10
Q
Edrophonium
A
- AChE block -> ^ACh
- side effect: cholinergic crisis (Tx w/ atropine)
- use to diagnose myasthenia gravis (Tensilon test)
- short acting, reversible
11
Q
Ambenonium
A
- AChE block -> ^ACh
- carbamate
- to Tx myasthenia gravis
- oral admin
12
Q
Demecarium
A
- AChE block -> ^ACh
- carbamate
- to Tx glaucoma
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
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
15
Q
Carbaryl
A
- AChE block -> ^ACh
- carbamate
- reversible
16
Q
Pyridostigmine
A
- AChE block -> ^ACh
- carbamate
- Tx: chronic management of myasthenia gravis
- med acting; 4o amine-poorly absorbed
17
Q
Tacrine
A
- AChE block -> ^ACh
- to Tx Alzheimers
- reversible
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
atropine
- M block
- anti-muscarinic effects and clinical uses; mandatory for cholinergic OD
- 3o amine- CNS access
- most potent anticholinergic
25
Scopolamine
- 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
Ipratropium
- M block
- anti-muscarinic effect and clinical uses +Tx: COPD and asthma
- 4o amine- local effects in lung
27
Pirenzapine
- M1 block
- anti-muscarinic effects and clinical uses
- tricyclic; targets gastric parietal cell
- CNS access (tertiary amine)
28
Oxybutinin (and daritenacin and Solifenacin- more selective)
- M3 block
- decrease detrussor mm tone/spasms via SM relaxation
- to Tx urge incontinence and post-op spasms
29
Dicyclomine
- M block
- to Tx peptic disease, hyermotile gut, IBS, minor diarrhea
- CNS access (tertiary amine)
30
Tropicamide
- M block
- to Tx mydriasis, cycloplegia; used by ophthalmologist to dilate eye
- CNS access (tertiary amine)
31
Propantheline
- M block
- to Tx peptic disease, hypermotile gut
- quaternary amine- stays in GI tract
32
Glycopyrrolate
- M block
- to Tx peptic disease, hypermotile gut
- quaternary amine- stays in GI tract
33
Tiotropium
- M block
- decreases secretions to Tx asthma, COPD
- 4o amine- local fx in lung
34
Benztropine
- M block
- to Tx Parkinsons
- 3o amine- CNS access
35
Hexamethonium
- Ganglionic blocker (Nn antag)
| - depends on prevailing autonomic tone
36
Decamethonium
- ganglionic blocker (Nn antag)
| - fx depend of prevailing autonomic tone
37
Mecamylamine
- ganglionic blocker (Nn antag)
- fx depend on prevailing autonomic tone
- CNS access- can cause sedation, tremor, mental aberrations
- erratic oral absorption
38
Tetraethylamine
- ganglionic blocker (Nn antag)
- fx depend on prevailing autonomic tone
- can't cross BBB; very short acting
39
Trimethaphan
- 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
Pralidoxime (2-PAM)
- 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
Diacetylmonoxime
-rescue aging of P groups d/t AChEI's
42
Hemocholinium
blocks pre-synaptic choline txporter (no ACh synth)
| -> decrease ACh
43
Vesamicol
ACh vesiclular txporter block (no ACh packaging)
| -> decrease ACh
44
Spider venom (black widow)
ACh release -> ^ACh
45
Botulinum toxin
ACh exocytosis block
| -> decrease ACh
