Vasodilators and sympathoplegics Flashcards

(87 cards)

1
Q

CCBs- DHPs

A

CaCh blockers- dihydropyridines
Amlodipine
Nifedipine
-dipine

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2
Q

CCBs- non-dihydropyridines

A

Diltiazem

Verapamil

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3
Q

KCh openers

A

diazoxide

minoxidil

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4
Q

Dopamine agonist

A

fenoldopam

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5
Q

NO modulators

A

Hydralazine
Nitroprusside
Organic Nitrates: Isoorbide dinitrate, nitroglycerin

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6
Q

vasodilators

A

CCBs
KCh openers
Dopamine agonist
NO modulators

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7
Q

Sympathoplegics

A

beta-blockers

alpha-blockers

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8
Q

beta blockers

A
Atenolol
carvediol 
labetalol
metoprolol
propanolol 
-olol
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9
Q

alpha 1 blockers

A

prazosin

-osin

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10
Q

alpha 2 blockrs

A

clonidine
methyldopa
guanbenz
guanfacine

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11
Q

DHP prototypes

A

nifedipine

amlodipine

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12
Q

DHP MOA

A

blocks vascular L-type CaCh > cardiac Chs

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13
Q

Non DHP prototypes

A

Verapamil

diltiazem

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14
Q

Non DHP MOA

A

nonselective block of vascular and cardiac L-type CaCh

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15
Q

CCBs effects on SM

A

vasodilate -> decrease peripheral resistance
aa more sensitive then vv so orthostatic hypotension not usually an issue
decreases O2 demand and work of heart

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16
Q

CCBs effects on cardiac mm

A

reduced contractility throughout the heart and decreases in SA node pacemaker rate and AV node conduction velocity

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17
Q

CCB pharmacodynamics

A

PO, but high first pass metabolism
high degree of plasma protein binding
Nifedipine, clevidipine, verapamil, and diltiazem are also IV

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18
Q

DHPs adverse effects

A

generally well tolerated

excessive hypotension, dizziness, HA, peripheral edema, flushing, tachycardia, rash, gingival hyperplasia

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19
Q

Non-DHPs adverse effects

A

dizziness, HA, peripheral edema, constipation, AV block ,bardycardia, heart failure, lupus-like rash (diltiazem), pulmonary edema, cough, wheezing

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20
Q

short-acting DHPs

A

nifedipine
increased risk of MI, stoke, death
should NOT be used for management of chronic HTN

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21
Q

Non-DHP contraindications

A

couse w/beta blocker

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22
Q

CCB general contraindications

A

overt heart failure

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23
Q

CCB drug interactions

A

verapamil may increase digoxin in blood levels
DHPS additive w/other vasodilators
Non-DHPs additive w/other cardiac depressants and hypotensive drugs

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24
Q

CCB indications

A

long-term outpatient therapy of HTN
HTN emergencies
angina

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25
Diazoxide MOA
K Ch opener in SM
26
Diazoxide pharmacodynamics
reduced contraction -> arteriolar dilator -> reduced peripheral resistance -> reduced mean arterial pressue
27
Dizaoxide pharmacokinetics
relatively long acting 4-14hrs exhibits high protein binding typically administered in 3-4 injections 5-15min apart, sometimes IV
28
diaoxide adverse effects/contraindications
excessive hypotension resulting in stroke and MI hypotensive effects are greater in renal failure or when on beta-blockers hyperglycemia avoided in patients w/ischemic heart disease causes Na and H20 retention
29
dizoxide clinical uses
HTN emergencies
30
minoxidil MOA
opens KCh in SM
31
minoxidil Pharmacodynamics
increased K permeability -> decrease contraction | dilation of aa, but not vv
32
minoxidil adverse effects/contrainidcations
common- HA, sweating, hypertrichosis reflex sympathetic stimulation and Na and fluid retention resulting in tachycardia, palpitations, angina, and edema minoxidil must be used in combo w/beta blocker and loop diuretic
33
minoxidil clinical uses
long-term outpatient therapy of severe HTN | topical formulations for hair growth
34
Fendolopam MOA
agonist at D1R
35
Fenoldopam pharmacodynamics
peripheral arteriol dilator, natriuretic
36
Fenoldopam pharmacokinetics
administered by continuous IV due to rapid meta and short half life
37
Fenoldopam adverse effects/contraindications
tachycardia, HA, flushing | should be avoided in patients w/glaucoma
38
fenoldopam clinical uses
HTN emergencies | postoperative HTN
39
Hydralizaine MOA
stimulates release of NO from endo
40
Hydralazine pharmacodynamics
dilation of aa, but not vv, reflex tachycardia
41
hydralazine pharmacokinetics
well absorbed, but high first pass | metabolism occurs in part bia actylation, so varied
42
hydralazine adverse effects/contraindications
common: HA, nausea, anorexia, palpitations, sweating, flushing in patients w/ischemic heart disease, reflex tachycardia and sympathetic stimulation may provoke angina or ischemic arrhythmias rarely can cause peripheral neuropathy and drug fever
43
hydralazine indications
long term outpatient HTN combo w/nitrates is effective in heart failure and should be considered in patients (especially african americans) w/both HTN and heart failure first line therapy for HTN in pregnancy parenteral formulation is useful in HTN emergencies
44
Na nitroprusside MOA
drug metabolism releases NO resulting in increased cGMP
45
Na nitroprusside pharmacodynamics
powerful dilation of aa and vv, reduced peripheral vascular resistance and venous return in absence of heart failure blood pressure drops and CO does not chance when CO is already low due to heart failure, CO often increases due to afterload reduction
46
Na nitroprusside pharmacokinetics
rapid meta results in rapid onset and short duration effect | should be administered by IV infusion w/continuous monitoring of arterial blood pressure
47
Na nitroprusside adverse effects
excessive hypotension cyanide poisoning ->metabolic acidoisis, arrythmias, excessive hypotension and death thiocyanate toxicity
48
Na nitroprusside indications
HTN emergencies | severe heart failure
49
organic nitrates protype
nitroglycersin
50
Nitroglycerin MOA
release of NO via enzymatic reaction
51
Nitroglycerin pharmacodynamics
relaxes all types of SM (vv>aa) virtually no direct effect on cardiac or skeletal mm increases venous cpacitance, decreases ventricular preload, pulmonary vascular pressures and heart size are reduced in absence of heart failure CO is reduced decreases platelet aggregation
52
Nitroglycerin pharmacokinetics
high first pass therefore sublingual usually used therapeutic blood levels are reached w/in minutes and last 15-30 PO, transdermal and buccal available for longer duration tolerance may occur
53
nitroglycerin adverse effects/contraindications
common: orthostatic hypotension, syncope, throbbing HA compensatory responses contributing to tolerance: tachycardia, increased cardiac contractility, rentention of Na and H20 contraindicated if intracranial pressure is elevated transdermal patches should be removed before use of external defibrillators
54
nitroglycerin drug-drug interaction
synergistic hypotension w/phosphodiesterase type 5 inhibitos
55
nitroglycerin indications
HTN emergencies, angina, heart failure
56
Non-ISA non-selective beta blockers
propanolol carvediol nadolol timolol
57
ISA Non-selective beta blockers
labetalol (also blocks alpha 1) cartelol penbutolol pindolol
58
non ISA cardioselective beta blockers
``` metopropol atenolol esmolol bisoprolol betazolol ```
59
ISA cardioslective beta blockers
acebutolol | nebibolol (also beta 3 agonist)
60
propanolol MOA
non selective beta blocker
61
beta blocker pharmacodynamics
non-selective agents primarily decrease BP by decreasing CO cadioselective decrease TPR do not usually cause hypotension in healthy people blockade of beta 1 in kidney inhibits renin release several beta-blockers exhibit local anesthetic actions
62
beta blocker oral
except esmolol, all are available as oral preparations
63
beta blockers extended release tablets
carvedilol, metoprolol, and propranolol
64
beta blockers parenteral
``` atenolol esmolol labetalol metoprolol propranolol ```
65
beta blocers adverse/effects contraindicatios
asthma/COPD diabetes cardiac arrhythmias most common side affect is fatigue, bradycardia, sexual dynsfunction, depression chronic used associated w/high VLDL and low HDL sudden withdrawl may cause rebound HTN, angina, possibly MI
66
beta blockers drug-drug interactions
can cause heart block when combined w/CCBs verapamil or dltiazem
67
beta blocker clinical uses
HTN: metoprolol and atenolol heart failure: carvediol, bisoprolol, metoprolol ischemic heart disease cardiac arrythmias glaucoma bradyarrythmias or peripheral vascular disease
68
alpha blockers prototype
prazosin
69
prazosin MOA
reversible antagonist at alpha 1
70
alpha blockers pharmacodynamics
prevent vasoconstriction of both aa and vv, decrease TPR relaxes SM in prostate retention of Na and H2O when used w/o diuretic associated w/either no change or increased HDL levels
71
alpha blockers adverse effects/contraindications
generally well tolerated orthostatic hypotension, dizziness, palpitations, HA, lassitude less incidence of reflex tachycardia than non-selective alpha blockers
72
alpha blockers drug-drug interactions
most effective when used in combo w/other agents
73
alpha blocker indications
men w/HTN and BPH
74
alpha 2 blockers protoypes
clonidine | methydopa
75
alpha 2 agonists MOA
reduce sympathetic outflow from vasomotor centers in brainstem, but allow centers to retain or even increase their sensitivity to baroreceptor reflex
76
alpha agonists indications
with the exception of clonidine these agents are rarely used, methyldopa for HTN in pregnancy
77
clonidine pharmacodynamics
lowers BP by reducing CO and TPR
78
clonidine adverse effects
sedation, dry mouth, depression, sexual dysfunction transdermal prep associated w/less sedation, but may cause skin rxn abrupt withdrawl can lead to life-threatening HTN crisis
79
Methyldopa pharmocodynamics
lowers BP by reducing TPR | varialbe reduction in HR and CO
80
methyldopa adverse effects
sedation, dry mouth, lack of concentration, sexual dysfunction
81
HTN in pregnancy
should be treated at systolic > or equal to 160 and/or diastolic > or equal o 110
82
acute management of HTN in pregnancy
labetalol (IV) hydralazine (IV) CCBs Nitroglycerin (IV)
83
long term treatment of HTN in pregnancy
methyldopa labetalol nifesdipine hydralazine
84
contraindication in pregnancy
ACEIs, ARBs, direct renin inhibitors (fetal renal and cardiac abnormalities) nitroprusside (fetal cyanide poisoning)
85
vasodilators for HTN emergencies
``` Na nitroprusside nitroglycerin nicardipine clevidipine fenoldopam hydralazine (pregnancy HTN emergencies) ```
86
adrenergic antagonists for HTN emergencies
phentolamine (cocain intoxication, phenochromocytoma) esmolol (aortic dissection, postoperative HTN) labetolol (active coronary aa disease)
87
common drug combos
``` ACEIs and CCBs ACEIs and diuretics ARBS and diurectis beta blockers and diuretics centrally acting agent and diuretic diuretic and diuretic ```