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Pharm2: Module 2 > Antihypertensives part 2 > Flashcards

Antihypertensives part 2 Flashcards

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1
Q

What are sympathetic antagonist agents

A

Alpha and Beta Blockers

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2
Q

what are the three different levels of blocking of sympathoplegic drugs

A

peripherally
centrally
ganglionically

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3
Q

what are peripherally blocking sympathoplegic drugs

A

prazosin
doxazosin
metoprolol
pindolol

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4
Q

what are centrally blocking sympathoplegic drugs

A

clonidine
methyldopa

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5
Q

what are ganglionic blocking sympathoplegic drugs

A

trimethaphan

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6
Q

what are the indications for alpha blockers

A

moderately hypertensive patients
pheochromacytoma
BPH (benign prostate hypertrophy)
Raynauds disease
clonidine withdrawal

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7
Q

what are the indications for beta-blockers

A

angina
hypertension
secondary prophylaxis in MI
arrhythmias

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8
Q

what are the possible toxicities associated with alpha-blockers

A

fluid retention
headache
nasal stuffiness
dry mouth

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9
Q

what are the possible toxicities associated with beta-blockers

A

rebound hypertension with sudden withdrawal
bronchoconstriction
GI upset
fatigue
nightmares
decreased libido

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10
Q

what are the two types of alpha receptors

A

alpha 1: present on vascular smooth muscle
alpha 2: presents in the brain stem (centrally) as well as vascular smooth muscle (peripherally)

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11
Q

how do alpha adrenergic receptor antagonists effect norepinepherine and epinepherine

A

alpha adrenergic receptor antagonists INHIBIT the effects of norepinepherine, epinepherine and other sympathomimetic drugs

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12
Q

what is the MOA for Alpha 1 receptors

A

alpha 1 blockers inhibit the effects of norepinepherine (more than epinepherine)

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13
Q

what is the MOA for alpha 2 receptors

A

alpha 2 blockers can cause some decrease in peripheral vascular resistance too
block binding of NE and epinephrine (equally)

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14
Q

what are nonselective - alpha blockers

A

phenoxybenzamine and phentolamine

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15
Q

what is the MOA for phenoxybenzamine

A

irreversible nonselective blockade of peripheral alpha 1 and alpha 2 receptors - decrease vasoconstriction

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16
Q

when is phenoxybenzmine used

A

in treatment of sweating and HTN associated wtih phenochromacytoma

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17
Q

what are the SE/contraindications of phenoxybenzmine

A

reflex tachycardia, orthostatic hypotension
nasal stuffiness, N/V and may inhibit ejaculations

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18
Q

what are the pharmacokinetics of phenoxybenzamine

A

oral or IV admin
long lasting effects

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19
Q

what is the MOA and pharmacokinetics of phentolamine

A

reversible non-selective blockade of peripheral alpha 1 and alpha 2 receptors -> decrease vasoconstruction
IM or IV admin
effects last about 4 hours

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20
Q

what is the use of phentolamine

A

primarily used to diagnose and treat (short term) phenochromocytoma, particularly associated HTN emergency
treat/prevent dermal necrosis following extravasation of norepi
treat HTN crisis s/p abrupt withdrawal of clonidine or ingestion of tyramine-containing foods in pts with MOAIs

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21
Q

what are alpha1 selective blockers

A

Prazosin and Doxazosin

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22
Q

what is the MOA for alpha 1 selective blockers

A

selective alpha 1 inhibition -> decrease vasoconstriction
relaxes both arterial and venous smooth muscle
no effect on renin release or CO

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23
Q

what is the use of Prazosin

A

causes vasodilation
causes urethral and prostate muscle relaxation
has some effect on central aphla receptors
Treat: HTN, BPH and PTSD - associated nightmares

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24
Q

what are the SE of Prazosin and Doxazosin

A

dizziness
lack of energy
nasal congestion
HA
drowsiness
orthostaotic hypotension

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25
what is the use of Doxazosin
HTN BPH PTSD- associated nightmares oral admin - longest acting med in its class
26
what are the non-selective beta blockers
Propranolol Nadolol Pindolol Timolol
27
what is the MOA for Pindolol
partial beta 1 and beta 2 agonist
28
what is the MOA for timolol
non-selective beta1 and beta 2 inhibition -> reduces production of aqueous humor in the eye
29
what is the use of propranolol
low-potency antihypertensive agent performance anxiety postural tremor migraine prophylaxis thyrotoxicosis portal HTN
30
what are the SE of propranolol
risk of bronchoconstriction dizziness, lethargy, fatigue, weakness, visual disturbances, hallucinations, short-term memory loss, vivid dreams, depression
31
what is the use of Nadolol
FDA approved tx of HTN and mgmt of chronic (stable) angina (rarely used in practice) more potent than propranolol half life of 14-24 hours
32
what is the use of pindolol
HTN
33
when should pindolol be avoided
in patient with prior MI/angina
34
what is timolol used for
chronic glaucoma management topical admin, oral can be used for HTN but rare
35
what are Beta-1 selective sympathetic antagonists
metoprolol atenolol nebivolol
36
what is the MOA for Nebivolol
selectively inhibits B1 receptors the most cardioselective of all the selective beta blockers
37
what is the use of Metoprolol
HTN stable and unstable angina acute MI ventricular tachy chronic stable HF migraine prophylaxis - less bronchial constriction
38
what is Metoprolol not approved for
acute Heart failure
39
what are the SE of beta-1 selective antagonists
bradycardia decrease CO AV heart block Rarely, can cause HF
40
what are the uses for Atenolol
less effective than metoprolol HTN, stable and unstable angina, actue MI, supraventricular tachy, ventricular tach, CHF and migraine prophylaxis reduces HR and myocardial work
41
what are the uses of Nebivolol
HTN and HF most beta-1 selective at low dose vasodilating effect on peripheral vasculature
42
what are mixed alpha and beta blockers
Carvedilol and Labetolol
43
what is the MOA for Cavedilol and Labetolol
nonselectively blocks alpha 1, beta 1 and beta 2 receptors -> peripheral vasodilation
44
what is the use of Carvedilol
used primarily in chronic stable HF and decreases mortality in pts after MI second-line antihypertensive half life 7-10 hours given PO BID
45
what are the SE of mixed alpha and beta blockers
orthostatic hypotension and dizziness hypoglycemia
46
what are the uses of Labetolol
HTN due to phenochromocytoma HTN emergencies Pre-eclampsia Safe in pregnancy Oral or IV admin
47
what are the different types of calcium channel blockers
Non-dihydropyridine (cardio-selective) Dihydropyridines (vascular selective)
48
what are the non-dihydropyridine calcium channel blockers
Verapamil Diltiazem
49
what are the dihydropyridine calcium channel blockers
Nifedipine amlodipine felodipine
50
what is the MOA for non-dihydropyridine calcium channel blockers
selectively blocks Ca2+ channels in the myocardium -> decrease arterial pressure, increase coronary perfusion, decrease HR, Decreases AV nodal conduction, decrease force of contraction
51
when should calcium channel blockers be avoided
do not use in heart failure acute coronary syndrome pre-existing conduction disorder symptomatic hypotension
52
when are verapamil and diltiazem used
stable and vasospastic angina essential HTN dysrhythmias
53
what should be monitored with verapamil use
monitor for bradyarrhythmias and heart block
54
when is Diltiazem used
immediate in its action used mostly for anti-arrhythmic effects, though can also lower BP
55
what is the MOA for dihydropyridines (vascular selective) calcium channel blockers
blocks Ca2+ channels in arterioles dose not alter conduction through AV node
56
what is not altered with nifedipine and amlodipine
do not alter conduction through AV node used chiefly for antihypertensive effects
57
when is short active nifedipine avoided
post MI patient as it can increase HR, risk for tachycardias and increase oxygen demand
58
what is Nifedipine used for
HTN Stabole and vasospastic angina migraine reynauds disease
59
what is Amlodipine used for
excellent antihypertensive, in common use stable and vasospastic angina minimal effect on cardiac conduction
60
what are the three mechanisms of action for vasodilator drugs
arterial vasodilators venous vasodilators mixed vasodilators
61
What are venous vasodilators
isosorbide dinitrate Nitroglycerin
62
what is nitroglycerin
venous vasodilator used for all types of angina, severe HTN sublingual tablet stays in the body for short durations
63
what is the MOA for venous vasodilators
converted to nitric oxide in the body -> vasodilation -> decrease cardiac O2 demand
64
what are the SE of nitroglycerine
HA Hypotension tachycardia tolerance can rapidly develop drug interactions with PDE-5i
65
what is isosorbide dinitrate
venous vasodilator prophylaxis of angina, esophageal spasm HF treatment in black people in combo with hydralazine sublingual or immediate release PO
66
what are the SE of Isosorbide dinitrate
tolerance can rapidly develop headache hypotension tachycardia drug interactions with PDE-5i
67
what are the arterial vasodilators
hyralazine diazoxide minoxidil
68
what is hydralazine used for
arterial vasodilator essential HTN, almost always used in combo with beta-blocker used to decrease afterload in pts with HF can be used to treat HTN in pregnancy oral or IV
69
what is the MOA for hydralazine
exact MOA unknown selective dilation of arterioles -> decrease peripheral resistance and decrease BP
70
what are the SE of Hydralazine
*Lupus-like syndrome possible headache Nausea anorexia flushing reflex tachy increases blood volume
71
what is Minoxidil (Rogaine)
arterial vasodilator more intense vasodilation than hydralazine but more severe SE reserved for pts with severe HTN unresposive to safer drugs stimulant for hair growth
72
what is the MOA for Minoxidil (Rogaine)
opens K+ channels in vascular smooth muscle -> K+ flows out, decreases cells ability to contract -> arteriolar dilation -> decrease peripheral resistance and decrease BP Hyper-polarization of cell membranes through K+ channels opening
73
what is diazoxide
arterial vasodilator acute or malignant HTN hypoglycemia: inhibits insulin release from the pancreas
74
what is the MOA for diazoxide
long acting K+ channel opener -> salt and water retention
75
what are the SE of Diazoxide
Excessive hypotension
76
What drug acts as both venous and arterial vasodilators
Nitroprusside used for HTN emergencies
77
what is the MOA for Nitroprusside
breaks down and releases nitric oxide -> activates grauylate cyclase -> catalyzes the production of cyclic GMP -> relaxes smooth muscle of arteriole and veins -> decrease BP
78
what is the pharmacokinetics and SE of nitroprusside
continuous IV infusion (effects begin within second) excessive hypotension cyanide poisoning thiocyanate toxicity
79
What are centrally acting adrenergic agents
clonidine and methyldopa
80
what is the MOA for clonidine and methyldopa
agonist at centrally located alpha 2 receptors -> inhibits further release of norepi and inhbitis sympathetic outflow from the brain
81
what is the primary SE of clonidine
recount hypertension lethargy, sedation, constipation, xerostomia
82
what is clonidine used to treat
HTN menopausal flushing opioid or alcohol withdrawal tourette's syndrome 2nd line agent for ADHD
83
what is Methylodopa used for
Limited use in HTN mostly sued for HTN during pregnancy may cause: sedation, occasional lactation long term use can lead to autoimmune hemolytic anemia
84
what is Methylodopa used for
Limited use in HTN mostly sued for HTN during pregnancy may cause: sedation, occasional lactation (M and F) long term use can lead to autoimmune hemolytic anemia
85
What is the initial therapy recommendation for HTN
thiazide diuretics, ACEi, ARB or CCB (initial choice dependent on guideline used and comorbidity)
86
when should the patient be started on combination therapy
if the BP is greater than 20mmHg above goal for systolic or 10mmHg above diastolic goal

Pharm2: Module 2 (4 decks)

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