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Flashcards in Vasodilators Deck (46)
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1

Primary Mechanisms of Action of Vasodilators

Increasing intracellular cGMP
Preventing the depolarization
Decreasing intracellular Ca2+
Increasing intracellular cAMP

2

Nitric Oxide Donors: Mechanisms of Action and Pharmacology

Release NO when metabolized
Relax smooth muscle
Vascular
Corpora cavernosa
Short-lived in others (e.g. bronchial, GI)
Inhibit platelet aggregation

3

NO mech of action

increases cGMP, which causes the breakdown of myosin and actin, causing relaxation in vascular smooth muscle

4

Organic Nitrites and Nitrates

Isosorbide dinitrate
Nitroglycerin

5

Inorganic NO Donors

Nitroprusside

6

Organic NO Donors: Pharmacodynamics (site of action)

NO broken down in veins (relax coronary arteries)
-effect on preload (decreases O2 demand in heart)

7

Inorganic NO Donors: Pharmacodynamics (site of action)

dialate veins and arteries (good antihypertensive)

8

adverse effect of inorganic NO donors

cyanide toxicity

9

Isosorbide

Angina
Heart failure

10

Nitroglycerin clinical use

Acute myocardial infarction†
Anal fissure
Angina (stable and unstable)
Hypertensive emergency* (*=IV)
Hypotension induction*
Perioperative hypertension*
Pulmonary edema†

11

Nitroprusside

Hypertensive emergency (only IV)

12

angina

short-lived ischemia

13

short acting

nitroglycerin, nitroprusside (good for acute events)

14

long acting

isosorbide dinitrate, nitroglycerin (long term use)

15

NO donor tolerance

nitrate-free period of greater than 10 hours are necessary to prevent or attenuate tolerance
-want coverage during the day only (during activity that will lead to angina)

16

nitric oxide donor side effects

Hypotension
Dizziness
Headache
Flushing
Syncope

17

Nitroglycerin and nitroprusside are both pregnancy category

C

18

Isosorbide dinitrate and Nitroglycerin interaction

Sildenafil

19

PDE V

breaks down cGMP

20

Sildenafil mech of action

blocks action of PDE V (build up of cGMP--> relaxation)

21

Sildenafil clinical use

pulmonary hypertension, erectile disfunction

22

Sildenafil side effects/ adverse reactions

Severe hypotension and death if combined with nitrates, dyspepsia, priapism

23

Hydralazine clinical use

Hypertension; CHF

24

Hydralazine Side effects/Adverse Reactions

Dizziness, headache, angina, tachycardia, peripheral edema; Pregnancy category C

25

Nitroglycerine + Hydralazine

decreases tolerance of NO donor

26

Hydralazine is not used for

angina; healthy artery will dialate more than injured

27

Hydralaine half life is

relatively short; making it a non ideal hypertensive

28

Calcium-Channel Blockers: Mechanisms of Action and Pharmacology

Block calcium channels
Decrease calcium influx into cells
Decrease ER/SR calcium loading
Effects depend on selectivity

29

DHPs act on

blood vessels (L type receptors)

30

non DHPs act on

heart and blood vessels (L and T type receptors)

31

DHP action

promotes diuresis; main effect on resistance arterioles, some effect on capacitance venules; some effect on kidneys

32

non DHP

decreases heart rate and force of contraction

33

DHP drugs

Amlodipine and nifedipine

34

non DHP drugs

Diltiazem and Verapamil

35

Amlodipine half life

good for hypertension treatment

36

Long-acting CCB

1st line antihypertensive; great for treating low renin producers (esp africans and elderly)

37

Dihydropyridine CCBs have less effect on exercise performance than ________ and will not affect

b-blockers; electrolytes like diuretics do

38

Long duration of CCB action provides

superior long-term outcomes (also applicable to other anti-HTN meds).

39

Typically antihypertensives will be compensated for in the body unless

more than 1 drug is used

40

Treatment of Isolated Systolic Hypertension without Other Compelling Indications

Long-acting DHP CCB (good for isolated systolic bc won't drop diastolic that much bc doesn't have direct effect on heart)

41

nonDHPs and DHPs are both useful for ______, but

angina, but non DHPs have a stonger effect (bc they have an effect on the heart)

42

non DHPs treat these types of angina

stable angina-exertion, unstable angina-plaque, variant angina-spasm

43

DHPs treat these types of angina

stable (exertion) and variant (spasm)

44

DHP interactions

beta blocker withdrawal-increased rate of contraction in heart, then CCB will increase blood flow->bad! (not as severe for non DHPs)

45

non DHPs main use

arrhythmias, also angina

46

DHP main use

hypertension, also angina