Autonomic Pharmacology Flashcards Preview

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Flashcards in Autonomic Pharmacology Deck (77):
1

AA origin of NE, epi

tyrosine --> L-DOPA --> DA --> NE --> Epi

2

AA origin of 5-HT

tryptophan

3

AA origin of histamine

histidine

4

AA origin of NO

arginine

5

1st order neuron of ANS uses ____ on _____ receptor.

ACh, Nn

6

2nd order neurons of ANS in PSNS use _____ on _____ receptor.

ACh, M

7

2nd order neurons of ANS in SNS use _____ on ______ receptors.

- ACh, M (sweat glands)
- NE, a/B (most)
- DA, D1 (kidneys)
- epi from adrenal medulla acting diffusely

8

NMJ uses ____ on ____ receptors.

ACh, Nm

9

Removal of ACh from the synapse occurs by:

AChesterase, acetate (diffuses away) + choline (recycled)

10

NE degraded by ____ vs epi degraded by:

reuptake, MAO/COMT (epi is more processed so requires more enzyme for uptake)

11

GPCR receptor types

- a1 - Gq
- a2 - Gi
- B1 - Gs
- B2 - Gs
- M1 - Gq
- M2 - Gi
- M3 - Gq
- D1 - Gs
- D2 - Gi
- H1 - Gq
- H2 - Gs
- V1 - Gq
- V2 - Gs

"qiss and qiq til you're siq of sqs"

12

a1 receptor roles:

- Gq
- vasoconstriction
- mydriasis
- intestinal/bladder sphincter contraction

13

a2 receptor roles:

- Gi
- decreased SNS
- decreased insulin release from B cells and lipolysis from adipocytes
- decreased production of aqueous humor
- increased platelet aggregation

14

B1 receptor roles:

- Gs
- increase in heart rate and contractility
- increase in renin release from in cells
- increased lipolysis

15

B2 receptor roles:

- Gs
- vasodilation
- bronchodilation
- increased lipolysis and insulin release from B cells
- decreased uterine/bladder tone
- ciliary muscle relaxation (opposite of accommodation)
- increased aqueous humor production

16

M2 receptor roles:

- Gi
- decreased heart rate and contractility
- relaxation of internal sphincter

17

M3 receptor roles:

- Gq
- increased exocrine gland secretions
- increased gut peristalsis
- bladder contraction
- bronchoconstriction
- miosis
- accommodation (contraction of ciliary muscle)

18

D1 receptor roles:

- Gs
- relaxes renal vascular smooth muscle

19

H1 receptor roles:

- Gq
- increased nasal/bronchial mucus production
- increased vascular permeability
- contraction of bronchioles
- pruritus
- pain
- constricts the venules causing edema

20

H2 receptor roles:

- Gs
- gastric acid secretion

21

V1 receptor roles:

- Gq
- vascular smooth muscle contraction

22

V2 receptor roles:

- Gs
- increased H2O permeability and reabsorption in collectube duct of nephron via AQ2 channels

23

bethanechol

- cholinergic agonist resistant to AChesterase
- postop ileus, neurogenic ileus, urinary retention, xerostomia

24

carbachol

- cholinergic agonist resistant to AChesterase
- causes miosis and decrease in IOP

25

methacholine

- cholinergic agonist with very short t 1/2
- dx of asthma

26

pilocarpine

- cholinergic agonist resistant to AChesterase
- stimulates sweat, tears, saliva and treats open and closed angle glaucoma

"cry, drool, and sweat on my pillow"

27

galantamine, rivastigmine, donepezil

AChesterase inh specific to CNS used to boost ACh for memory consolidation in Alzheimer dz

28

edrophonium

AChesterase inh used to test for myasthenia gravis

29

neostigmine

AChesterase inh used for ileus, urinary retention, reversal of NMJ blockade

"NeO CNS penetration"

30

physostigmine

AChesterase inh that can cross BBB and thus used to treat anticholinergic toxicity

"phyxes atropine OD"

31

pyridostigmine

AChesterase inh. used for myasthenia gravis

"get RID of myasthenia gravis"

32

organophosphate

- irreversible AChesterase inh
- DUMBBELSS - diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of NMJ, lacrimation, sweating, salivation
- also nausea and vomiting

33

atropine

muscarinic antagonist, eye/heart

34

benztropine

muscarinic antagonist, CNS (Parkinson's)

35

glycopyrrolate

muscarinic antagonist, GI/resp

36

-tropium

muscarinic antagonist, bronchi (bronchodilation)

37

oxybutynin

muscarinic antagonist, GI (overactive bladder)

38

scopolamine

muscarinic antagonist, motion sickness

39

succinylcholine

- depolarizing Nm antagonist --> paralysis
- very short half life

40

"-cur-" drugs

- non-depolarizing Nm antagonist --> paralysis
- long half life --> need AChesterase inh + muscarinic antagonist to bring them off after surgery

41

malignant hyperthermia

- AD genetic disorder
- hyperthermia + hyperkalemia in response to inhaled anesthetics and succinylcholine releasing Ca 2+ from sarcoplasmic reticulum which activates ATPase to produce heat
- treat with dantrolene (prevents Ca 2+ release from sarcoplasmic reticulum)

42

-terol drugs

B2 > B1 agonists (works in smaller, more peripheral airways)

43

dobutamine

B1 > B2 agonist used for HF and cardiac stress testing as well as cardiogenic shock

44

dopamine

D > B > a agonist depending on dose used to preserve blood flow to kidneys and vital organs during shock

45

epinephrine

- B1,2 > a1,2 agonist used for anaphylaxis and asthma
- increase in SBP (a1) but decrease in DBP (B2) so MAP remains the same --> used with local anesthetics for vasoconstriction since it won't raise BP

46

isoproterenol

- B1,2 agonist
- SBP only slightly increases, but DBP drops significantly so MAP decreases

47

norepinephrine

- a1 > a2 > B1 agonist used for hypotension
- SBP increased significantly, DBP unchanged so MAP increases
- can cause reflex bradycardia

48

phenylephrine

- a1 > a2 agonist
- used for hypotension, rhinitis (decongestant), priapism

49

amphetamine (Adderall)

- displaces NE/DA in vessicles
- partial adrenergic agonist
- blocks catecholamine re-uptake transporters
- used for narcolepsy and ADHD

50

cocaine

- inhibits DRTs causing vasoconstriction
- never give B blockers if cocaine use is suspected (unopposed a1)

51

ephedrine

- displaces NE in vessicles
- partial adrenergic agonist
- used for nasal congestion, urinary incontinence, hypotension

52

ritodrine

B2 agonist used to relax uterus and prevent premature delivery

53

methylphenidate (Ritalin)

- DRT, NERT in RAS
- first-line ADHD treatment

54

What should people on MAO inhibitors avoid?

consuming tyramine (in fermented foods/beverages)

55

NE will casue reflex ____.

bradycardia

56

isoproterenol will cause reflex ____.

tachycardia

57

clonidine, guanfacine

- a2 agonist that reduces SNS output
- used to treat hypertensive urgency, ADHD, Tourette
- rebound HTN if taken off too quickly

58

a-methyldopa

- a2 agonist that reduces SNS output
- treats HTN in pregnancy

59

phenoxybenzamine

- irreversible a1/a2 antagonist
- used before pheochromocytoma surgery

60

phentolamine

- reversible a1/a2 antagonist
- given to patients on MAO inhibitors who eat tyramine-containing foods

61

-azosin drugs, tamsulosin

- a1 antagonist
- urinary retention due to BPH, PTSD, HTN

62

mirtazapine

- a2 antagonist
- used for depression

63

-olol drugs

- B blockers
- angina pectoris, MI, SVT, HTN, CHF, glaucoma

64

acebutolol, atenolol, betaxolol, bisoprolol, emolol, metoprolol are ____ antagonists.

B1 selective (A --> M)

65

Avoid ____ in cocaine users.

B blockers --> unopposed a1 action and HTN

66

carvedilol, labetalol

a and B antagonists - great for HTN!!

67

homatropine

muscarinic antagonist - eye

68

tropicamide

muscarinic antagonist - eye

69

trihexyphenidyl

muscarinic antagonist - CNS (acute dystonia)

70

hyoscyamine

muscarinic antagonist - GI (prevents spasm in IBS)

71

dicyclomine

muscarinic antagonist - GI (prevents spasm in IBS)

72

solifenacin

muscarinic antagonist - bladder (reduces urge incontinence)

73

tolterodine

muscarinic antagonist - bladder (reduces urge incontinence)

74

BB used for SVT

metoprolol, esmolol

75

BB used for HF

metoprolol, bisoprolol, carvedilol

76

BB used for glaucoma

timolol

77

BB used for variceal ppx

propanolol