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COM: Neuro II (Exam I) > Cholinergic Drugs > Flashcards

Flashcards in Cholinergic Drugs Deck (69):
1

List the direct acting cholinergic agonists

ACh
Bethanechol
Carbachol
Cevimeline
Methacholine
Pilocarpine
Varenicline

2

What drug is a cholinnesterase regenerator?

Pralidoxime

3

What muscarinic antagonist is used for motion sickness?

Scopolamine

4

What muscarinic antagonists are used for GI disorders?

Atropine
Dicyclomine
Glycopyrrolate
Hyoscyamine

5

What anti muscarinic drugs are used in ophthalmology?

Atropine
Cyclopentolate
Homatropine
Scopolamine
Tropicamide

6

What antimuscarinic drugs are used for respiratory disorders such as asthma and COPD?

Ipratropium
Tiotropium

7

What antimuscarinic drugs are used for urinary disorders?

Darifenacin
Fesoterodine
Oxybutynin
Solifenacin
Tolterodine
Trospium

8

What antimuscarinic drugs are used for cholinergic poisoning?

Atropine + Pralidoxime

9

What antimuscarinic drugs are used or movement disorders?

Benztropine
Biperiden
Orphenadrine
Procyclidine
Trihexyphenidyl

10

What drugs are considered ganglion blockers?

Mecamylamine

11

Where are M1 receptors located and what signaling cascade do they utilize?

Nerves

Gq

12

Where are M2 receptors located and what signaling cascade do they utilize?

Heart
Nerves
Sm

Gi

13

Where are M3 receptors located and what signaling cascade do they utilize?

Glands
SM
endothelium

Gq

14

Where are M4 receptors located and what signaling cascade do they utilize?

CNS

Gi

15

Where are M5 receptors located and what signaling cascade do they utilize?

CNS

Gq

16

Where are Nm receptors located and what signaling cascade do they utilize?

Skeletal muscle
NMJ

Pentamer -> alpha2/betadelta; use Na/K depolarizing channel

17

Where are Nn receptors located and what signaling cascade do they utilize?

Postganglionic cell body
Dendrites
CNS

alpha and beta only; Na/K depolarizing channel

18

What cholinergic receptors are found on skeletal muscle?

Only nAChRs, so only those agents that activate nAChRs produce any effect (muscle contraction)

19

All cardiac actions of the PNS are mediated by what cholinergic receptor?

M2

20

T/F: PNS innervation of the ventricles is much less extensive than that of the atria and activation of ventricular mAChRs cause much less physiologic effects than mAChR activation in the atria

True

21

In the GI and GU tracts, The ____ mAChR is required for direct activation of smooth muscle contraction

M3

22

In the GI and GU tract, the ______ mAChR reduces cAMP formation and reduces relaxation caused by adrenergic effects (this results in contraction)

M2

23

Sphincter relaxation in the GI and GU tract is via _____ signaling mediated by _____ mAChRs

NO; M3

24

The brain is relatively richer in __________ cholinergic receptors while the spinal cord contains predominately _________ cholinergic receptors

mAChhRs in brain and nAChRs in SC

25

What cholinergic drug is approved for intraocular use during surgery, causes miosis and is rarely given systemically?

Ach

26

What cholinergic drug is administered by inhalation for the diagnosis of Ron hill airway hyperactivity in pts who dont have clinically apparent asthma?

Methacholine

**Rarely used due to need for emergency resuscitation equipment

27

What selective mAChR agonist can be used to treat pts with urinary retention and heartburn and may produce a UTI if the sphincter fails to relax?

Bethanechol

28

What drug is a nonspecific cholinergic agonist that is used for the treatment of glaucoma or to produce miosis during surgery or ophthalmic exam?

Carbachol

29

What cholinergic drug is an oral tablet used to treat dry mouth (xerostomia) in pts with Sjögren’s syndrome?

Cevimeline

30

What drug is a pure mAChR agonist approved for xerostomia tx in pts with Sjögren’s syndrome or head and neck cancer treatment related xerostomia, miosis during ophthalmic procedures and glaucoma?

Pilocarpine

31

What is the most common adverse effect of Varenicline?

Nausea

**Must stop immediately is behavioral changes are noticed

32

What is the most important use of AChEsterase inhibitors?

Tx of myasthenia gravis

33

Explain the MOA of Varenicline

- Partial agonist that binds with high affinity and selectivity to nAChR’s located in the brain to stimulate receptor-mediated activity but at a lower level than nicotine
- stimulation and subsequent sustained release of dopamine are thought to reduce craving and withdrawal symptoms associated with smoking cessation

34

What are the 3 chemical groups of acetylcholinesterase inhibitors?

Alcohols
Carbamic acid esters
Organophosphate

35

What are examples of AChEsterase inhibitors that contain an alcohol group and a quaternary ammonium group?

Edorphonium

36

What is an example of an AChEsterase inhibitor that contains carbamic acid esters of alcohols bearing quaternary or tertiary ammonium groups

Neostigmine
Pyridostigmine
Physostigmine
Carbaryl

37

Psyostigmine, donepezil, tacrine, rivastigmine, and galantamine are all examples of what type of AChEsterase inhibitors?

Tertiary and uncharged

38

AChE inhibitors can reverse the paralysis induced y neuromuscular blocking drugs during surgical anesthesia. What 2 drugs are preferred for this?

Neostigmine
Edrophonium

39

What drug is used as an antidote to anti cholinergic intoxication?

Physostigmine

40

Nondepolarizing neuromuscular blocking agents combined with AChE inhibitors will diminish the neuromuscular blockade. One exception is ____________ which is metabolized by plasma AChE causing the neuromuscular blockade to be prolonged

Mivacurium

41

A combination of beta blockers and AChE inhibitors may enhance what symptom?

Bradycardia

42

Coadministration of systemic corticosteroids with AChE inhibitors may affect what pts?

May enhance muscle weakness in pts with myasthenia gravis

43

What are the dominant initial signs of AChE intoxication?

Miosis
Salivation
Sweating
Bronchial constriction
Vomiting
Diarrhea

44

Current antidotal therapy for organophosphate exposure resulting from warfare, terroism, or other sources of parenteral atropine are _____________ and a _______________ as an anticonvulsant

Pralidoxime; benzodiazepine

45

Atropine is a naturally occurring tertiary amine alkaloid ester found int he plant Atropa belladonna The tertiary amines are used for their effects on the eye or CNS system. There are 3 of these, what are they?

Atropine
Tropicamide
Benztropine

46

Atropine is a naturally occurring tertiary amine alkaloid ester found in the plan Atropa belladonna. The quaternary amines are charged and elicit their antimuscarinic effects in the periphery. There are 2 of these, what are they?

Ipratropium
Glycopyrrolate

47

Parasympathetic effects of antimuscarinic compounds decline rapidly in all organs except ______________ where effects can last for 72 hours or longer

The eye

48

What tissues are most sensitive to atropine?

Salivary, bronchial and sweat glands

** acid secretion by the gastric parietal cells is the least sensitive

49

T/F: mAChR antagonists have no significant effect on the uterus

True

50

MAChR antagonists particularly the long-lasting _________________, are used to prevent synechia formation in uveitis and irititis

Homatropine

51

What is the first line therapy in the treatment of asthma and COPD?

Inhaled ipratropium

52

What is the first drug of choice for symptomatic bradycardia in an advanced cardiac life support setting?

Atropine

53

The prototype antimuscarinic agent used in disorders of the GU tract is ___________, which is somewhat selective for M3 mAChRs with side effects that include dry mouth, dizziness, constipation, blurred vision, dry eyes and UTI’s

Oxybutynin

54

____________ is a nonselective antimuscarinic agent that is comparable in efficacy and side effects with oxybutynin

Trospium

55

_____________, _____________, and _____________ are antimuscarinic agents that are selective for the M3 subtype and are advantageous bc of their longer half-lives and reduced incidence of xerostomia and constipation

Darifenacin, solifenacin, tolterodine

56

What agents are utilized to treat both CNS and peripheral effects of excessive stimulation of mAChRs due to cholinergic poisoning?

Tertiary antimuscarinic agents, preferably atropine

57

___________agents are contraindicated in pts with glaucoma and should be used with cation inn elderly men with a history of BPH

Antimuscarinic agents

58

Nonselective antimuscarinic agents (atropine) should be avoided in pts with _________ Disease, however, those that are selective may be of benefit

Acid-peptic disease

59

_____________ is selective for M1 and inhibits gastric secretion by acting at the ganglia

Pirenzepine

**Has little effect on SM or CNS and doesnt have the GI and CNS associated side effects that nonspecific mAChR antagonists have

60

All ganglion blocking drugs are synthetic ____________

Amines

61

________________ is a tertiary amine and was developed from initial ganglion blockers and has improved GI tract absorption

Mecamylamine

62

What is the MOA of ganglion-blocking drugs?

Ganglion-blocking drugs competitively lock the action of ACh and similar agonists at nAChRs of both parasympathetic and sympathetic autonomic ganglia

63

Where in the body is parasympathetic innervation absent?

Vascular SM

64

What effects do ganglion blocking drugs have on the CNS?

Uncharged ones (mecamylamine) cross the BBB and cause sedation, tremor, choreiform movements, and mental aberrations

65

What effects do ganglion-blocking drugs have on the eye?

- cycloplegia wwith loss of accommodation
- moderate dilation of the pupil bc PNS tone usually dominates

66

What effects do ganglion blocking drugs have on the CV system?

- decreased BP
- diminished contractility and moderate tachycardia of the heart

67

What effect do ganglion-blocking drugs have on the GI tract?

Reduced secretion and profoundly inhibited motility

68

What effect do ganglion-blocking drugs have on the GU system?

- urination hesitancy and possible urinary rention in men with BPH
- erection and ejaculation may be prevented

69

What are the clinical applicationof ganglion-blocking drugs?

- use is infrequent bc more selective autonomic locking agents are available and bc toxicity limits the willingness of pts to use these agents

- mecamylamine is approved for use to treat HTN and is being investigated for use in smoking cessation therapy