Cholinergic Drugs Flashcards
1
Q
Direct-acting cholinomimetics
A
- Ach
- Bethanechol
- Carbachol
- Cevimeline
- Methacholine
- Pilocarpine
- Varenicline (Chantix)
2
Q
Cholinesterase inhibitors
A
- Ambenonium
- Donepezil
- Echothiophate
- Edrophonium
- Galantamine
- Neostigmine
- Physostigmine
- Pyridostigmine
- Rivastigmine
- Tacrine
3
Q
Cholinesterase regenerator
A
Pralidoxime
4
Q
Drugs used for respiratory disorders (asthma, COPD)
A
- ipratropium
- tiotropium
5
Q
Drugs used for urinary disorders
A
- Darifenacin
- fesoterodine
- Oxybutynin
- Solifenacin
- Tolterodine
- Trospium
6
Q
What drugs are used for cholinergic poisoning?
A
Atropine (+ pralidoxime)
7
Q
What drugs are used for movement disorders?
A
- Benztropine
- Biperiden
- Orphenadrine
- Procyclidine
- Trihexyphenidyl
8
Q
What is the example given of a ganglion blocker?
A
Mecamylamine
9
Q
What drug is used for motion sickness?
A
Scopolamine
10
Q
What drugs are used for GI disorders?
A
- Atropine
- Dicyclomine
- Glycopyrrolate
- Hyoscyamine
11
Q
What drugs are used in ophthalmology?
A
- Atropine
- Cyclopentolate
- Homatropine
- Scopolamine
12
Q
M1 receptor
- location:
- GPCR pathway:
- mechanism:
A
- nerves
- Gq
- IP3, DAG
13
Q
M2 receptor
- location:
- GPCR pathway:
- mechanism:
A
- heart, nerves, smooth muscle
- Gi
- inhibition of cAMP, K+ channel activation
14
Q
M3 receptor
- location:
- GPCR pathway:
- mechanism:
A
- glands, smooth muscle, endothelium
- G1
- IP3, DAG
15
Q
M4 receptor
- location:
- GPCR pathway:
- mechanism:
A
- CNS
- Gi
- inhibition of cAMP
16
Q
M5 receptor
- location:
- GPCR pathway:
- mechanism:
A
- CNS
- Gq
- IP3, DAG
17
Q
NN receptor
- location:
- GPCR pathway:
- mechanism:
A
- postganglionic cell body, dendrites, CNS
- alpha and beta only
- Na+, K+ depolarizing ion channel
18
Q
What is the predominant receptor in most organs?
A
M3
19
Q
Which receptor predominates in the heart?
A
M2
20
Q
Which receptor predominates in smooth muscle?
A
M2, M3
21
Q
Which receptor types are found in the eye, lungs, and GI/GU?
A
M3, M2
22
Q
What is the MOA of choline esters?
A
cholinergic agonist
- choline esters permanently charged = poor absorption and CNS distribution
- metabolized by acetylcholinesterase
23
Q
What is the MOA of alkaloids?
A
cholinergic agonist
- uncharged tertiary structure = well absorbed
- muscarine is charged, but can still cross BBB
24
Q
What are the 3 groups of AChE inhibitors?
A
- alcohols (reversible)
- carbamic acid esters (reversible)
- organophosphates (irreversible**)
25
Which AChE inhibitors are insoluble in lipids?
charged AChE inhibitors
- do not cross BBB
- quaternary agents (edrophonium, physostigmine, neostigmine, echothiophate, ambenonium)
26
Which AChE inhibitors are lipid-soluble?
neutral AChE inhibitors
- can cross BBB
- most organophosphates, teriary agents (physostigmine, doneppezil, galantamine, rivastigmine, tacrine)
27
What is the parasympathetic response of the sphincter muscle of the iris?
contraction (miosis)
28
What is the parasympathetic response of the ciliary muscle of the eye?
contraction for near vision
29
What is the parasympathetic response of the SA node?
negative chronotropy (decreases HR)
30
What is the parasympathetic response of the atria?
negative inotropy (decreases contractility)
31
What is the parasympathetic response of blood vessels?
dilation via EDRF
NOTE: at high doses, direct effect causes constriction
32
What is the parasympathetic response of bronchial muscle?
bronchoconstriction
33
What is the parasympathetic response of GI motility?
increases motility
34
What is the parasympathetic response of GI secretions?
stimulates secretion
35
What is the parasympathetic response of GI sphincters?
relaxes sphincters
36
What is the parasympathetic response of urinary detrusor muscle?
contraction (parasympathetic makes you pee)
37
What is the parasympathetic response of urinary trigone and sphincter?
relaxation
38
What is the parasympathetic response of sweat, salivary, lacrimal and nasopharyngeal glands?
increases secretion
39
What is Bethanechol?
selective mAChR agonist that primarily affects urinary and GU tracks
- used to treat urinary retention and heartburn
- little CV stimulation
- may produce UTI if sphincter fails to relax
40
What is Carbachol?
nonspecific cholinergic agonist used to treat glaucome, or produce miosis during surgery
41
What is Cevimeline?
oral tablet used to treat dry mouth (xerostomia) in patients with Sjogren syndrome
42
What is Pilocarpine?
pure mAChR agonist
| - approved for xerostomia in patients with Sjogren syndrome, head/neck cancer treatment, or during opthalmic procedures
43
What is Varencline (Chantix)
FDA approved drug for smoking sessation
- partial agonist that binds with high affinity and selectivity for NN
NOTE: sustained release of dopamine thought to reduce craving and withdrawal symptoms of smoking
44
What are the major uses of direct-acting cholinergic agonists in GI/GU disorders?
- postoperative ileus
- congenital megacolon
- urinary retention
- esophageal reflux
- xerostomia, Sjogren syndrome
45
What are the contraindications for direct-acting cholinergic agonists?
patients who have asthma, hyperthyroidism, coronary insufficiency, acid-peptic disease
46
What are the clinical uses of indirect-acting cholinergic agonists?
- glaucoma
- dementia
- antidote to anticholinergic poisoning
- reversal of neuromuscular paralysis
- myasthenia gravis
- AChE inhibitor toxicity
47
What are the most clinically useful cholinergic antagonists?
antimuscarinic agents
48
What anticholinergics are used for respiratory disorders?
Ipratropium and tiotropium
- inhalation mAChR antagonists
- Tiotropium has longer bronchodilator action, can be dosed once daily
49
What anticholingergics are used for GI disorders?
mAChR antagonists can treat common travelers diarrheaand other mild conditions of hypermotility
NOTE: often combined with an opiod antidiarrheal drug
50
What anticholinergics are used for GU disorders?
agents with selectivity to M3 subtype are beneficial due to presence in bladder wall and sphincter smooth muscle
- Oxybutynin (but has side effects of dry mouth/eyes, dizziness, constipation)
- Darifenacin, solifenacin and tolterodine are advantageous because of longer half-lives and reduced incidence of zerostomia and constipation
51
What anticholinergics are used for cholinergic poisoning?
Atropine! given to reduce mAChR stimulation
- no effective treatment at nAChR
- useless in delayed-onset mushroom poisoning
52
What are the adverse effects of anticholinergics?
good for one system, bad for another
- mydriasis (pupil dilation) and cycloplegia (ciliary muscle paralysis) may be adverse effects of antimuscarinic agents used to reduce GI secretion
53
What do high systemic concentrations of anticholinergics lead to? How do you treat it?
will block parasympathetic function
| - treat with AChE inhibitors
54
What are the contraindications of anticholinergics?
- glaucoma
- prostatic hyperplasia
- acid-peptic disease
