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Flashcards in PDA Drugs Deck (62):
1

Sympathomimetic

Drugs that mimic agonists of the sympathetic system.

2

What are the mechanisms of action of sympathomiemetics?

Act at the postganglionic terminal - directly activate receptors, block breakdown/reuptake, stimulate production and release of catecholamines

3

Sympatholytics

Generally competitive antagonists that inhibit effects of the SNS.

4

Where are α1 receptors located?

1. Eye
2. Arteries
3. Veins,
4. GU smooth muscle (male)
5. Vas deferens (male)

5

Where are α2 receptors located?

Presynaptic nerve terminals and CNS

6

Where are β1 receptors located?

Heart and kidney

7

Where are β2 receptors located?

1. Arteries (skeletal, cardiac muscle)
2. Bronchi
3. Skeletal muscle
4. Liver

8

What 6 drugs are considered direct-acting catecholamines?

1. Norepinephrine
2. Epinephrine
3. Isoproterenol
4. Dopamine
5. Dobutamine
6. Methydopa

9

What are the direct-acting catecholamines used for and what are they metabolized by?

1. Cardiovascular actions
2. MAO and catechol-O-Metransferase
*Must be given parenterally, short half life

10

Norepinephrine

Receptor: α1, α2, β1
Cardio thru α1
Increases PVR, mean BP
Can cause reflexes bradycardia

11

Epinephrine

Receptor: α1, α2, β1, β2

12

What CV, respiratory, and metabolic effects does epinephrine cause?

1. Increases HR, contractile force, CO,
systolic BP-decrease diastolic BP (dose)
constrict most vascular beds except sk muscle (dose)
2. Bronchodilation
3. Hyperglycemia, inc in FFA

13

At low concentrations epinephrine will cause blood vessels in skeletal muscle to _______ and at high concentrations it will cause them to ___________.

1. Dilate ( β2)
2. Constrict α1

14

Isoproterenol

Receptor: β1, β2
Therapeutic use: Emergency use for treatment of bradycardia or heart block

15

What are the effects of isoproterenol on the CV and respiratory systems??

1. Decrease PVR and mean BP, Inc HR, contractile force, CO
2. Bronchodilation

16

Dopamine

Low: "Renal dose" decrease PVR, inc. renal blood flow, dilation of renal/mesenteric a. (D1)
Intermediate dose: "cardiac" inc. HR, contractile force, CO (D1 + β1)
High dose: "pressor dose" vasoconstriction, inc. PVR (D1+β1+α1)

17

Dobutamine

β1 agonist
Inc. HR, contract, CO - minimal change in PVR and BP

18

What are therapeutic uses of dobutamine?

1. Short-term treatment of cardiac decompensation - following cardiac surgery, heart failure, MI
2. Cardiac stress testing

19

Methydopa

Pro-drug
α2 agonist (centrally reduces sympathetic outflow)
Treats HTN
SE: sedation, dry mouth, edema, rebound HTN w/ sudden discontinuation

20

What is an indirect sympathomimetic and when do you need to worry about it?

Tryamine - patients on MAOIs

21

Phenylephrine

α1 agonist
Vasoconstriction, dilate eye - nasal decongestant

22

Clonidine

α2 agonist - decrease sympathetic outflow
SE: Sedation, dry mouth, edema, rebound HTN

23

Albuterol

β2 agonist: Short duration bronchodilator - asthma
SE: Tremor, anxiety

24

Salmeterol

β2 agonist: Long duration bronchodilator - COPD, persistant asthma

25

Pseudoephedrine

α1 agonist - used as a nasal decongestant

26

Guanadrel

Inhibits NE release/depletes neuronal amine stores - Essential HTN
SE: Orthostatic hypotension, male sexual dysfunction, diarrhea, muscle weakness, edema

27

Guanethidine

Inhibits NE release/depletes neuronal amine stores - Essential HTN
SE: Orthostatic hypotension, male sexual dysfunction, diarrhea, muscle weakness, edema

28

Reserpine

Blocks VMAT, inhibits NE release - active in CNS
Depression, sedation, suicidal tendencies

29

Cocaine

Blocks NET - increases duration of NE in synaptic cleft

30

Phenoxybenzoine

Irreversible blocks α receptors - vasodilation proportional to sympathetic tone - pheochromocytoma
SE: Tachycardia, salt/water retention, o. hypotension

31

Phentolamoine

Blocks α receptors - reverse/shorten DOA of anesthesia
SE: Tachycardia, salt/water retention, o. hypotension

32

Prazosin

α1 antagonist - decreases PVR, favorable effect on lipid profile - (short term) congestive heart failure, HTN, BPH
*First dose phenomenon (hypotension)
SE: alt/water retention, o. hypotension

33

Tamsulosin

α1a antagonist - decreases tone in GU tract, little BP effects - BPH

34

Propranolol

β blocker - HTN, angina, cardiac arrhythmias, acute MI, pheochromocytoma, migrane prophylaxis
SE: Cardiac depression, bradycardia, bronchoconstriction, impotence, sedation, nightmares

35

Timolol

β blocker - Glaucoma, HTN, angina, cardiac arrhythmias, acute MI, pheochromocytoma, migrane prophylaxis
SE: Cardiac depression, bradycardia, bronchoconstriction, impotence, sedation, nightmares

36

Metoprolol

(β1 > β2) blocker - Chronic Heart Failure, HTN, angina, cardiac arrhythmias, acute MI
SE: Cardiac depression, bradycardia, impotence, sedation, nightmares, hypotension

37

Atenolol

β1 blocker - not in CNS - HTN, angina, cardiac arrhythimas, acute MI, pheochromocytoma
SE: Cardiac depression, bradycardia, impotence hypotension

38

Carvedilol

βα1 blocker - cardio effects, PVR, has some antioxidant properteis and Ca channels - Chronic Heart Failure, HTN, acute MI

39

Labetalol

βα1 blocker - Essential HTN
Oral: Essential HTN
IV: Hypertensive Emergencies

40

What are the two most important enzymes for NE metabolism?

1. Catechol-O-methyltransferase
2. Monoamine oxidase

41

What is botulinum toxins mechanism of action?

Cleaves snares in the presynaptic nerve at the NMJ - can't release ACh - skeletal muscle paralysis

42

What enzyme is the rate limiting step for NE synthesis?

Tyrosine hydroxylase - converts tyrosine -> DOPA

43

Bethanechol

Muscarinic agonist (orally/SQ) Void bladder

44

Pilocarpine

Muscarinic agonist (orally/SQ) - Salivation, open up angle in eye - glaucoma

45

What are side the side effects of the cholinergic agonists and AChE inhibitors?

S: Salivation
L: Lacrimation
U: Urination
D: Defecation
G: GI upset
E: emesis
Bradycardia, hypotension, blurred vision

46

What two drugs are irreversible AChE substrate inhibitors?

Sarin and Malathion

47

Edrophonium

AChE inhibitor - reverse paralysis, diagnosis of myasthenia gravis

48

Physostigmine

AChE inhibitor (Active in CNS): Treats wide angle glaucoma

49

Neostigmine

AChE inhibitor (Periphery): Treats myasthenia gravis, urinary and GI motility issues

50

Atropine

Muscarinic antagonist (some CNS) Bradyarrhthmias, dilates eye, blocks vagal reflexes - treats AChE and muscarinic toxicity i.e. Sarin

51

Scopolamine

Muscarinic antagonist (More CNS penetration) treats motion sickness and vestibular disease

52

Ipratropium

Muscarinic antagonist (inhaled no CNS) - bronchodilation, treats COPD

53

Tropicamide

Muscarinic antagonist - Dilates eyes

54

Oxygutynin

Muscarinic antagonist (Bladder, some CNS) - Overactive bladder, incontinence (women)

55

Darifenacin

Muscarinic antagonist (some M3, less CNS) Overactive bladder, incontinence (women)

56

Glycopyrrolate

Muscarinic antagonist (NMJ no CNS) - reverse sk muscle paralysis

57

Rocuronium

(Competitive NMJ Blocker) Adjuvent during surgery - metabolized by liver

58

Atracurium

(Competitive NMJ Blocker) Adjuvent during surgery - spontaneously degrades in blood, slight histamine release

59

Vecuronium

(Competitive NMJ Blocker) Adjuvent during surgery - metabolized by liver

60

Pancuronium

(Competitive NMJ Blocker) Adjuvent during surgery - metabolized by kidney, slight increase in HR, BP, and histamine release

61

Succinylcholine

(Depolarizing NMJ Blocker) Flaccid paralysis Allows tracheal intubation

62

Pralidoxime

(Depolarizing NMJ Blocker)