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Pharmacology > Cardiovascular/HTN > Flashcards

Cardiovascular/HTN Flashcards

1
Q

How prevalent is HTN in the USA?

A

30% or more (1/3 of Americans have HTN)

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2
Q

What is HTN?

A

BP 140/90

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3
Q

What causes HTN

A

idiopathic

CO increases and peripheral vascular resistance increases

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4
Q

Why is HTN bad?
if untreated for a long time can cause:
outcome is

A 
not good for t heart 
untreated for a long time can cause:
♣	 CHF
♣	Aneurysm
♣	Vision issues
♣	Renal failure

poor

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5
Q

A person who is normotensive at age 55 has up to a ___% chance of developing HTN

A

90

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6
Q

HTN is the #1 reason for

A

office visits

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7
Q

a decrease in BP of 2mmHg can

A

lower risk of cardiovascular events by 10%

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8
Q

JNC 8 (JNC - Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure) says that the following types of pts should start pharmacotherapy at what BP?

  • Patients <60 years of age
    -Pts with diabetes start tx at
    with CKD
    60+ years old
A

Patients <60 years of age = 140/90
patients with diabetes= 140/90
Patients with CKD= 140/90
Patients 60 years of age or greater =150/90

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9
Q

why would patients 60+ years of age start tx at a higher BP?

A

Systolic is high but diastolic is okay this is called isolated systolic HTN and a lot of old people get this (usually like 170/70)
Arteries get stiffer with age so BP goes up
Don’t start tx until later because their BP is normally higher

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10
Q

What do we tx HTN with?

A

thiazide Diuretics, ACE inhibitors, ARBs, CCBs

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11
Q

How do diuretics work?

A

Diuretics work by depleting sodium (sodium wasting)

“Where sodium goes, so goes water” (if you get rid of Na+, water will also leave and BP will decrease

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12
Q

Only class of diuretics recommended in HTN

A

thiazides

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13
Q

as you move through the nephron less and less ____ happens

explain

A

reabsorption
near the glomerulus 60-70% of absorption occurs there
but as you get down passed the loop of henle it drops down to 25% and then in the distal convoluted tubules it drops to 5%

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14
Q

Loop diuretics—bad because they decrease

A

tons of fluid

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15
Q

Hydrochlorothiazide (HCTZ) (thiazide diuretic)

  • ____ derivative so need to watch out for
  • MOA=
A

-sulfonamide, allergies (people with sulfa allergies)
-decrease reabsorption in distal convoluted tubules
by Blocking Na+-CL- symporter on luminal membrane

**this is where 5% of reabsorption takes place and HCTZ blocks it

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16
Q

HCTZ =hydrochlorotiazide

effects

A 
Na+ and Cl- loss
K+ loss
Mg2+ loss (mechanism unknown)
Decreased Ca2+ excretion
Decreased peripheral vascular resistance (mechanism unknown)
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17
Q

• HCTZ =hydrochlorotiazide has to be secreted into lumen so kidney has to be

A

functioning and working very well. So that means glomerulus has to be perfused and still be filtering (fluid has to be coming out of the glomerulus)

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18
Q

• How does the glomerulus work

in order for thiazides to work, glomerulus has to be very

A

They work on hydrostatic pressure so they are like balloons with a bunch of holes in it
o Not a lot of water is going to come out of holes if you have just a little fluid inside deflated balloon
o If you have a lot of fluid (very perfused) lots of fluid can come out of the holes
o So in order for thiazides to work, glomeruli have to be very perfused

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19
Q

can pts kidney dysfxn take hydrochlorothiazide?

A

no they will not take these drugs –doesn’t work because their kidneys are not perfused

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20
Q

with HCTZ how long does it take to see consistent decrease in BP?

Effective with renal failure?

A

Takes up to 3 weeks to see consistent decrease in BP (it will take a little while)
• Not effective if you have renal failure (ineffective if GFR is below 30ml/min)

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21
Q

HCTZ is called ceiling drugs—because

A

if you Increase dose beyond a certain point does not increase diuresis

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22
Q

adverse affects of HCTZ

A 
o	adverse affects
♣	hypokalemia
♣	hyponatremia
♣	hyperuricemia—gout 
♣	hypercalcemia
♣	hyperglycemia if pt has high blood sugar, or is diabetic, this drug could push them up so diabetic can use it, but you need to monitor their blood sugar and put them on some other drug to help blood sugar 
♣	volume depletion
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23
Q

Drugs that are just like Thiazides (“Thiazide-like” Diuretics)
name 3

which do we prefer, these or HCTZ?

A

chlorthalidone
indapeamide (lozol)
Matolazone (Zaroxolyn)

We prefer to use the first 2 (chlorothalidone and indapeamide) over hydrochlorothiazide

we use to use HCTZ a lot but now we are seeing more chlorthalidone and indapamide

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24
Q

Drug Interactions with Thiazide-Like Diuretics

A

1) Uricosuric agents (namely, probenecid) → compete for secretion into proximal tubule and thiazides interfere with uric acid excretion
2) Sulfonylureas and insulin → decreased effectiveness in maintaining blood sugar
3) **Quinidine → increased risk of QT prolongation; potentially fatal
4) Drugs that potentiate orthostatic hypotension
5) Hypokalemia may increase digitalis toxicity
6) NSAIDs
7) Beta-blockers → hyperglycemia/hyperlipidemia
8) Corticosteroids → hypokalemia

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25
Q

Hypokalemia is an issue with THiazides/Thiazide like diuretics, how can we tx this?

A

diet

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26
Q

Loop Diuretics fxn + names

A

Bumetanide (Bumex)
Furosemide (Lasix)
Torsemide (Demadex)

MOA: Inhibit Na+-K+-2Cl- cotransporter in thick ascending limb of loop of Henle

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27
Q

Knowing that loop diuretics Inhibit Na+-K+-2Cl- cotransporter in thick ascending limb of loop of Henle, do you expect loops to be more potent, less potent, or equipotent to thiazides?

A

More potent!!! Because that act where 25% of Na+ reabsorption occurs and so they are blocking a lot of water from coming back in

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28
Q

Loop Diuretics used for HTN?

A

NO

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29
Q 
Loop Diuretics
half life?
onset?
capable of increasing 
Ca2+ loss?
A

Short half-life, rapid onset
Capable of increasing renal blood flow
Ca2+ is lost but reabsorbed in Distal Convoluted Tubule so hypocalcemia is rare in patients with normal Ca2+ regulation

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30
Q

Loop Diuretics produces a ton of _____

and even effective when

A

urine (pts pee a lot)

pt has very decreased renal function

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31
Q

if pt is old and on Lasix, tell them to take this medicine when?

A

take Lasix in morning so they are not getting up all night and peeing (also because a lot of old pts are on Lasix, and getting up at night a lot can cause injury/fall risk)

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32
Q

Are loop diuretics safe?

side effects?

A

very
o Ototoxicity (hearing loss/vestibular dysfxn)
o Hyperuricemia
o Hypovolemia ** more potent than with thiazides**
o Hypokalemia ** very profound with these drugs**
hypomagnesemia

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33
Q

Loop Diuretics– if you put someone on a loop diuretic you must also give them

A

must give them a a Rx for K+

–> don’t ever forget to give someone potassium if you give them Lasix/loop diuretics **

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34
Q

Drug Interactions with Loop Diuretics

A

Drug interactions
Lithium → increased lithium levels (lithium toxicity)
Aminoglycosides → risk of ototoxicity
NSAIDs → decrease effectiveness of loop diuretics
Hypokalemia may increase digitalis toxicity
Corticosteroids → hypokalemia

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35
Q

Potassium sparing diuretics– not used for

MOA

A

HTN (same with loop diuretics)

• MOA: inhibit sodium reabsorption and potassium excretion in collecting tubule

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36
Q

Potassium sparing diuretics: good diuretics?

use for pt with renal failure?

A

not awesome

Use in renal failure? not sure how effective they are in renal failure

37
Q

Adverse effects of K+ sparing diuretics

A

Hyperkalemia (because they spare potassium)
Gynecomastia (men with boobs), menstrual irregularities (spironolactone)
photosensitivity

38
Q

If you wanted to, can you tx HTN with Potassium sparing diuretics? +

A

yes but needs to be in conjunction with a thiazide diuretic –all it does Is make sure you are not loosing K+

Not part of JNC 8 because you don’t need a loop diuretic to give you K+, you can just have pt change diet, or give them K+

39
Q

K+ sparing diuretics: Drug interactions

A

Drug interactions–main thing is risk of hyperkalemia—avoid things with more K+
Strong CYP3A4 inhibitors (eplerenone only)
**Potassium– they are already going to be hyperkalemic–don’t give them more potassium
ACEIs, ARBs, β-blockers increase risk of hyperkalemia
Trimethoprim (hyperkalemia)
NSAIDs
Lithium
Digoxin (increased t1/2 of digoxin)

40
Q

• What about using K+ sparing diuretics with a loop diuretic?

A

Won’t make a difference because you lose so much K+ in loop diuretics the K+ sparing won’t make up for it

41
Q

Potassium Sparing : Aldosterone Antagonists (ends with one)
name a couple drugs
MOA:

A

Spironolactone (Aldactone), eplerenone (Inspra)

MOA: Prevent aldosterone from binding to target receptors

42
Q

when would you use potassium sparing: aldosterone antagonists

A 
Uses
In combo with K+ wasting diuretics
Secondary hyperaldosteronism (cirrhosis, nephrotic syndrome)
Heart failure
Resistant hypertension
Ascites
PCOS (polycystic ovary syndrome)
43
Q

Potassium-sparing: Sodium Channel Blockers
MOA
drugs
dp not require the presence of _____ to be effective

A

MOA: directly inhibit Na+ influx into collecting duct
Triamterene (Dyrenium), amiloride (Midamor)
aldosterone

44
Q

Angiotensin-Converting Enzyme Inhibitors (ACEIs)

MOA

also prevent the degradation of

end in

A

MOA: Block conversion of angiotensin I to angiotensin II
angiotensin I ——-\/—–> angiotensin II
/\

(so increases)bradykinin (a potent endothelial vasodilator)–> causes the cough

pril

45
Q

Uses of ACE inhibitors

A

Uses:

  • HTN– Both primary and that caused by renal artery stenosis
  • Heart failure- specifically LV systolic dysfxn (loss of inotropy) “baggy heart”
  • Post MI (prevents remodeling of Heart muscles)
  • Patients at high risk of cardiovascular events
  • Pts with diabetes—protects your kidneys from further damage
46
Q

ACEIs are less effective in what population

A

Less effective in African American patients

Still works but not as well

47
Q

Some ACEIs list:

all end in

does it matter which you use?

A 
"pril"--doesn't matter which you use because they are equally efficacious at equivalent doses 
Benazepril (Lotension)
Captopril (Capoten)
Enalapril (Vasotec) 
Enalaprilat (Vasotec Injection)
Fosinopril (Monopril)
Lisinopril (Prinivil, Zestril)
Moexipril (Univasc)
Perindopril (Aceon)
Quinapril (Accupril)
Ramipril (Altace)
Trandolapril (Mavik)
48
Q

Side effects of ACEIs

A

1) First-dose hypotension – watch patients who are salt depleted, CHF, those on multiple antihypertensives, dehydration (Initial dose should be low to minimize side effects )
2) Cough (5-20%) – switch to ARB or another class
3) Hyperkalemia (in presence of other causes)
4) Angioedema-less prevalent than the cough but very prevalent still (swelling of lips, mouth, tongue)

49
Q

One really big side effect of ACEIs
how? _____ presents a problem when given with ACEIs
explain

A

acute renal failure
NSAIDs

ACEIs prevent constriction of efferent arteriole
Normally angiotension II would vasoconstrict at your efferent arteriole (normal)
–but we are blocking this action with the ACEI so we are not getting vasoconstriction at efferent arteriole so stuff flows into the glomerulus and its wide open to flow out

-Prostaglandins normally dilate the AFFerent arterioles
however NSAIDs inhibit formation of prostaglandins so they will not dilate the afferent arterioles
• net effect of thse two drugs: glomerulus doesn’t get fluid –> what fluid is does get can flow right out– damage of glomerulus –> acute renal failure

50
Q

ACEIs prevent constriction of

A

efferent arteriole

51
Q

Prostaglandins normally dilate the

A

Afferent arterioles

52
Q

ACEI contraindications

A
  • Pregnancy- black box warning ** pregnant women do not get ACE inhibitors (anything with pril—get them off of it
  • —–ACEIs must be stopped at the first sign of pregnancy
  • —–Fetal hypotension, renal failure, and death will occur
  • DO not use in hypoperfused state (eg. Dehydration,etc)
    - ->Because of issue of hydrostatic pressure in glomerulus

-Use catuion with drugs that increase potassium or or decrease perfusion

53
Q

ARBs-
fxn:
where does this happen in chain compared to ACEI
bradykinin?

A

angiotensin receptor blockers
Block type 1 angiotensin II (AT1) receptors (prevents angtiotensin II from going to AT1)
Effect is occurring further down the cascade
No disruption in bradykinin degradation != less cough/angioedema

54
Q

ARBs do a little less ______ but better at

can At2 receptors still be activated?

A

A little less vasodilation however better at inhibiting the effects of angiotensin

AT2 receptors can still be activated because angiotensin II is still circulating

55
Q

Fxn of ARB

A

Dilate arteries and veins → decreased preload and afterload
Inhibit cardiac remodeling
Promote Na+ and water excretion
Inhibit aldosterone secretion
Down regulate sympathetic adrenergic activity

56
Q

ARB drugs end in “ “

A 
artan 
Candesartan (Atacand)
Eprosartan (Teveten)	
Irbesartan (Avapro)
Losartan (Cozaar)
Olmesartan (Benicar)
Telmisartan (Micardis)
Valsartan (Diovan)
57
Q

All ARBs are approved to tx

then certain ones are also approved to tx

A

**HTN

diabetic neuropathy (I's)
--->irbesartan, iosartan
Stroke prophylaxis
-->Losartan
Heart failure and post-MI w/LVF
---> Valsartan
58
Q

Calcium Channel Blockers

MOA:

A

MOA: Block calcium influx by binding of L-type (L for long-lasting) calcium channels in the heart and vascular smooth muscle cells

–> normally: Ca2+ influx stimulates contraction (so without it, more relaxation (Relaxation of arterial smooth muscle)

normally In the SA node of the heart, L-type channels allow increased Ca++ entry to hyperpolarize pacemaker channels leading to conduction —> cardiac effects

59
Q

What diuretic can we use according to JNC 8

A

Thiazides (2 good classes)

Chlorothalidone and idampemide

60
Q

End result of CCBs

Can use in some heart conditions like

A

get relaxation of arterial smooth mm—no effect on venous system ***

HTN, angina, antiarrythmics 
Hypertension (systemic and pulmonary)
A-flutter
A-fib
Paroxysmal SVT
61
Q

CCBs effects

A

Main effects :
Decrease contractility (negative inotrope)
Decrease heart rate (negative chronotrope)
Decrease conduction velocity
Vasodilation

62
Q

CCBs are in 3 classes what are they?

A

Dihydropyridines- Amlodipine and Norvasc are most popular

phenylalkylamines–> just one Verapamil (not even used for BP)
(nonydropyridne)

benzothiazepines –> just one Diltiazem (not even used for BP)
(nonydropiridine)

63
Q

Are all CCBs created equal?

A

NO

each does different things and has different characteristics

64
Q

Dihydropiridines

characteristics

A

type of CCB

1) High vascular selectivity - Periph.VascularResistance
2) Potent arteriolar vasodilators
3) Minimal effect on heart**
4) Most useful for the tx of HTN alone
5) Longer t1/2 preparations are better tolerated and are the standard

65
Q

Dihydropyridines (what kind of drug?) and which has the longest half life

what do they bind to?

A

CCB
Amlodipine has longest t1/2

Bind to N binding site of L-type channel

66
Q

Amlodipine…what is it?

what is it a fantastic drug for besides just regular HTN?

A

used as a CCB best choice for HTN when using a dihydropyridine

Because of its affects on arteries specifically, amlodipine (CCB) is a fantastic drug for people with isolated systolic HTN (old people where systolic is high but diastolic is normal)
–> Because you drop the top # without dropping the bottom #

67
Q

Verapimil and Diltizaem—are they used for HTN/BP?

A

no not really, not used for BP –used for arrhythmias

68
Q 
Verapamil
Binds to the
Essentially cardioselective
Less potent\_\_\_\_\_\_\_\_  than dihydropyridines
Used for stable 
Inhibits
A

V binding site of L-type calcium channels
vasodilator
angina and arrhythmias
P-glycoprotein

69
Q

Diltiazem
Binds to the
Something in between
Inhibits

A

D binding site of L-type calcium channels
dihydropyridine and verapamil
P-glycoprotein

70
Q

Verapamil and diltiazem are class IV _____ drugs because of their impact on myocardial function

A

antiarrhythmic

71
Q

Verapamil and diltiazem have ______ half-lives and require tid-qid dosing.

Newer formulations are available that are slow or delayed release allowing less frequent dosing. Pay attention to names with CR, XR, CD.

A

short

72
Q

Which has more side effects dihydropyridines or diltiazem and verapamil
_______ is a big deal in terms of side effect with dihydropirines

A

dihydropyridines

peripheral edema

73
Q

If a pt cannot tolerate amlodipine can we switch them to verapamil/diltizem?

A

NO
amlodopine is a dihydropiridine and it treats HTN, whereas verapamil and dilitzem do not tx blood pressure!!!! Option is to switch to another drug class

74
Q

Dihydropirines, along with verapamil and dilitizem all kind of do the same things on the chart until you get to:

A

Heart Rate and AV conduction

dihydropyridines actually increase HR while diltizaem and verapamil decrease it

dihydropyridine actually does nothing for AV conduction while diltizaem and verapamil decrease it

75
Q

Of dihydropyridines, diltizaem and verapamil, which ones do you have to be careful with if pt is on B-blockers

A

diltizaem and verapamil–need to be careful

dihydropyridines it doesn’t matter

76
Q

CCBS are a Good option specifically in some patients such as

A

Diabetes – no effect on glucose
Airway disease – no effect on bronchial dilation
Depression – does not exacerbate illness
African-American – no angioedema

77
Q

Migraine – ____ &______may decrease migraine frequency by 50%;

A

verapamil and amlodipine

78
Q

Some CCBs inhibit _____ – must watch for drug interactions

A

cytochromes

79
Q

JNC drug choices :

A

thiazide, CCB, ACEI, ARB

Preferred thiazides: chlorthalidone, indapamide

80
Q

how does JNC say to use these drugs?

also need to modify

A

Options
1) Titrate to maximum dose of one drug before adding second drug
OR
2) Start one drug then add a second before maximizing dose of first
OR
3) Start two at the same time
–>Recommended if BP is greater than 20/10 mmHg above goal

Lifestyle

81
Q

o Lifestyle Modifications along with these drug treatments?

A 
healthy lifestyle 
o	Low salt 
o	Exercise
o	Stop smoking (hardens your arteries)
o	Low fat
82
Q

pts with CKD should always get an _____except for

Do not combine an ace and an arb because

A

ACEI or an arb
pregnant people!!

very similar, no benefit and increased risk of hyperkalemia

83
Q

African Americans/blacks should be treated with ____ why?

African Americans have higher ____ risk; so therefore use ____to provide best protection and are more effective than ACEI/ARB
African Americans are more “____ sensitive”

A

thiazide, CCB

ACEI and ARB do not work as well with them–works but not very effectively.

CCB

salt

84
Q

Pts with CKD: tx should include

A

ACEI or ARB (including African Americans/black)

85
Q

ways to improve compliance of these drugs/ efficacy

A

Simplify with once-daily or combo products to improve adherence
Wait 2-3 weeks before increasing dose or adding new drug
home blood pressure reporting

86
Q

______ are more effective at decreasing systolic BP than diastolic

A

thiazides and CCBs

87
Q

do Pts with CKD or CAD benefit from having lower blood pressure targets?

A

no

use normal BP targets

88
Q

correct procedure for measuring BP

A

–> Blood pressure should be measured after the patient has emptied their bladder and has been seated for five minutes with back supported and legs resting on the ground (not crossed).

–>Arm used for measurement should rest on a table, at heart-level.

–>Use a sphygmomanometer/stethoscope or automated electronic device (preferred) with the correct size arm cuff.

–>Take two readings one to two minutes apart, and average the readings (preferred).

–>Measure blood pressure in both arms at initial evaluation. Use the higher reading for measurements thereafter.

Pharmacology (3 decks)

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