Block 2 Flashcards
(250 cards)
1
Q
What is the SBP/DBP criteria for HTN urgency/emergency?
A
SBP > 180
DBP > 120
2
Q
HTN urgency is what kind of injury?
A
Crisis w/o end-organ injury
3
Q
HTN emergency is what kind of injury?
A
Crisis w/ end-organ injuray
4
Q
What are some causes of HTN crisis?
A
- Med nonadherence
- Illicit Rx use
- MAOIs
- Advacining diseases
5
Q
In a HTN urgency, what dosage form should you transition to?
A
Oral (usually), IV for very high risk only
6
Q
What are the preferred oral Rx for HTN urgency?
A
- Captopril
- Clonidine
- Labetalol
- Minoxidil
- Nifedipine IR
7
Q
Dose for Captopril?
A
25 to 50mg every 1 to 2 hrs
8
Q
Dose for Clonidine?
A
0.1mg/hr up to 0.8mg total
9
Q
Pearls of Captopril?
A
Caution with renal failure; contraindicated in those with bilateral artery stenosis
10
Q
Pearls of Clonidine?
A
Caution in altered mental status
Contraindicated in those w/ carotid artery stenosis
11
Q
Dose for Labetalol?
A
200 to 400mg every 2-3hrs
12
Q
Dose for Minoxidil?
A
5 to 20mg
13
Q
Pearls of Labetalol?
A
ADR = bronchospasm, HF exacerbation, bradycardia and heart block
14
Q
Pearls of Minoxidil?
A
ADR = tachycardia and edema
Contraindicated in angina and HF
15
Q
Dose for Nifedipine IR?
A
10 to 20mg
16
Q
Pearls of Nifedipine IR?
A
ADR = flushing, headache, edema
Contraindicated in severe aortic stenosis, cerebrovascular disease
Can cause severe BP drop which can cause renal, cerebral, and myocardial ischemic events
17
Q
HTN and end organ damage, what dosage form should you give?
A
First IV, then gradually move to PO
18
Q
What are your goals when treating HTN and end organ damage?
A
Reduce MAP by 25% within 60 min
Next, reduce SBP to 160 and DBP to 100-110 within next 2-6 hours
Additional reduction to BP goal as tolerated after 1-2 days
19
Q
Acute ischemic stroke BP goal?
A
Do not lower unless ≥220/120 or ≥185/110 in tPA candidates
20
Q
Pheochromocytoma crisis BP goal?
A
Lower SBP to <140 within 1 hr
21
Q
Eclampsia or severe preeclampsia BP goal?
A
Lower SBP to <140 within 1 hr
22
Q
Aortic dissection BP goal?
A
Lower SBP to <120 within 1 hr
23
Q
When are PO Rx given in HTN and end-organ damaged pt?
A
After being stable for 24hrs
Pt is discharged when stable on PO Rx for ≥24 hrs
24
Q
Labetolol class?
A
Nonselective beta-blocker and has blocks some alpha 1 receptors
25
Labetalol dose?
20mg every 10 min
Max 300mg
26
Labetalol pearls?
IV; Alpha:BB = 1:7
PO; Alpha:BB = 1:3
27
Labetalol ADRs?
HF exacerbation, bronchospasm, bradycardia, heart block
Caution in acute HF, asthma, heart block
28
Esmolol class?
Beta 1 blocker
29
Esmolol dose?
500 to 1000mcg/kg bolus over 1 min
Then 50mcg/kg/min and increase to a max of 200mcg/kg/min
30
Esmolol pearls?
Rapid hydrolysis in blood (no renal or hepatic metabolism)
Loses selectivity at high doses
31
Esmolol ADRs?
HF exacerbation, bronchospasm, bradycardia, heart block
Caution in acute HF, asthma, heart block
32
Sodium nitroprusside class?
Direct acting vasodilator
33
Sodium nitroprusside dose?
0.3 to 0.5mcg/kg/min
Max = 10mcg/kg/min
34
Sodium nitroprusside pearls?
ADR = cyanide toxicity
Contraindicated in renal or hepatic failure
Caution in those w/ increased intracranial pressure
35
Nitroglycerin class?
Direct acting vasodilator
36
Nitroglycerin dose?
5 to 10mcg/min
Max = 100mcg/min
37
Nitroglycerin pearls?
ADR = headache, tachyphylaxis
Reserved for acute coronary syndrome
Caution in those w/ increased intracranial pressure
38
Nicardipine class?
CCB
39
Nicardipine dose?
5mg/hr
Max of 15mg/hr
40
Nicardipine pearls?
ADR = reflex tachycardia, headache, flushing
Strong cerebral and coronary dilation
3A4 substrate and inhibitor
2C9 inhibitor
41
Clevidipine class?
CCB
42
Clevidipine dose?
1-2mg/hr
Max of 32mg/hr
43
Clevidipine pearls?
ADR = reflex tachycardia, rebound HTN
Contraindicated in soy/egg allergy, poor lipid metabolism
Hydrolyzed by RBC esterases (no hepatic metabolism)
44
Hydralazine class?
Vasodilator
45
Hydralazine dose?
5-10mg every 4 to 6 hrs
Max of 20mg/dose
46
Hydralazine pearls?
ADR = reflex tachycardia
Unpredictable response and prolonged duration, therefore never first line
47
Enalaprilat class?
ACEi
48
Enalaprilat dose?
1.25mg every 4 to 6 hr
Max 5mg every 6 hrs
49
Enalaprilat pearls?
ADR = renal failure, hyperkalemia
Contraindicated in pregnancy
50
Fenoldopam class?
Dopamine agonist
51
Fenoldopam dose?
0.1mcg/kg/min then increase by 0.05 to 0.1
Max 1.6mcg/kg/min
52
Fenoldopam pearls?
ADR = headache, tachycardia, cerebral ischemia
Contraindicated in sulfite allergy
Caution in those w/ glaucoma
53
Phentolamine class?
Alpha 1 blocker
54
Phentolamine dose?
1-5mg bolus
Max of 15mg/dose
55
Phentolamine pearls?
Contraindicated in myocardial infarction and coronary artery disease
Useful for catecholamine excess such as pheochromocytoma, cocaine/amphetamine use, or extravasation
56
Which HTN are characterized by headache, confusion, N/V?
Fenoldopam
Nicardipine
Nitroprusside
Labetalol
57
What Rx should you use to treat ischemic stroke?
Labetalol OR Nicardipine
58
What Rx should you use to treat hemorrhagic stroke?
Labetalol OR Nicardipine
59
What Rx should you use to treat acute coronary syndrome?
BB plus nitroglycerin
If HR <70, use Nicardipine or Clevidipine
60
What Rx should you use to treat acute decompensated heart failure?
Loop diuretics + Nitroprusside
Alternative = Enalaprilat
61
What Rx should you use to treat aortic dissection?
BB first and fast!
Add a vasodilator like nitroprusside, nicardipine, clevidipine
62
Anti-HTN therapy causes worsening kidney function, what RX is an exception?
Fenoldopam (short-term)
63
What is pre-eclampsia/eclampsia?
Pre-eclampsia - proteinuria, edema, and profound HTN
Eclampsia - seizures that occur in women during pregnancy or shortly after birth
64
How do you manage pre-eclampsia/eclampsia?
Give IV magnesium sulfate for seizures
Give labetalol or nicardipine first then hydralazine for BP control
65
What is the Frank-Starling Mechanism in normal and failing hearts?
Normal: Increasing end-diastolic volume enhances cardiac performance
Failing hearts: Muscle is less able to alter force of contraction when fiber is stretched, therefore increased preload decreases systolic volume
66
HFpEF is known as _____ HF
diastolic
67
HPrEF is known as ______ HF
systolic
68
HFpEF is characterized by LVEF of _______%
>50%
69
HFrEF is characterized by LVEF of ______%
<40
70
Angiotensin II causes vaso(constriction/dilation)
Vasoconstriction
71
What hormones does angiotensin II release?
NE and aldosterone
72
Which neurohormone is involved in ventricular hypertrophy and cardiac remodeling?
Angiotensin II + Norepi
73
Angiotensin and Preload/Afterload?
Increases both
74
Norepi causes vaso(constriction/dilation)
Vasoconstriction
75
Which neurohormone lowers threshold for arrhythimias?
Norepi + Aldosterone
76
Norepi and Preload/Afterload?
Increases afterload only
77
Which neurohormone productes cardiac fibrosis?
Aldosterone
78
Aldosterone and Preload/Afterload?
Increases preload only
79
BNP causes vaso(constriction/dilation)
Vasodilation
80
Which neurohormone is responsible for diuresis?
BNP
81
BNP and Preload/Afterload?
Lowers preload only
82
Which neurohormone is elevated in ventricular injury?
BNP
83
Endothelin-1 causes vaso(constriction/dilation)
Vasoconstriction
84
Which neurohormone decreases renal blood flow?
Endothelin-1
85
Which neurohormone is responsible for ventricular hypertrophy?
Angiotensin + NE and Endothelin-1**
**Just ventricular hypertrophy, the other two are for cardiac remodeling
86
Which neurohormone down-regulates beta receptors?
Norepi
87
How does Norepi compensate for decrease in cardiac output?
1. Activates sympathetic NS
2. Increases contractility w/ increased intracellular calcium
3. Increased HR reduces lusitropy (ventricular relaxation) and increases oxygen demand
4. Vasoconstriction; preserve blood supply
88
How does your kidneys compensate for decreased cardiac output?
Kidneys are able to sense decreased organ perfusion and release renin, which causes fluid retention and increased preload
89
What are clinical signs of heart failure?
FACES
```
Fatigue
Activity limitation
Congestion
Edema
Shortness of breath
```
90
What are some lab parameters to look for in HF?
1. >100 BNP or >300 NT-proBNP; Specific for left ventricular dysfunction but may be elevated in other heart issues
2. CBC; measures reduced O2 capacity
3. CMP; hyponatremia in volume overload and potassium goal >4
91
What is Stage A HF?
High risk for HF w/o structural damage
92
What is Stage B HF?
Structural damage, but w/o any symptoms of HF
93
What is Stage C HF?
Structural heart issues w/ prior or current symptoms of HF
Class II and II are comfortable at rest, but less than ordinary activity causes symptoms
Class IV cant carry out any physical activity
94
What is Stage D HF?
Refractory HF requiring specialized intervention
95
What Rx should you use to treat Stage A HF?
Address risk factors only
96
What Rx should you use to treat Stage B HF?
ACEi
BB
MRAs if post MI
97
What Rx should you use to treat Stage C HF?
ACEi / ARBs
BB
MRAs
Diuretics
Devices`
98
What heart effects does digoxin have?
1. Positive inotropic (increase contraction)
2. Negative chronotropic (decrease HR)
3. Negative dromotropic (decrease conduction velocity)
99
MOA of digoxin?
Inhibits Na-K ATPase
Causes increased sodium and calcium levels
100
AE of digoxin?
Visual disturbances; halos and/or yellow/green color aberrations. Also blurred vision
Leads to ectopy and tachycardia due to inhibition of Na/K/ATPase
Decreased AV node conduction leads to bradycardia and AV block
Level should be at 0.5 to 0.9
101
Drug interactions w/ digoxin?
Antacids, cholestyramine, diltiazem, quinidine, and verapamil
Antacids and cholestyramine reduce absorption of digoxin
The other 3 reduce digoxin clearance
102
What can you administer for digoxin toxicity?
Digoxin immune Fab; given IV and the RX binds to digoxin
103
Dobutamine MOA?
Stimulates contractility by activating beta-1 receptors and activates beta-2 in vascular smooth muscles + alpha 1 stimulation (causing vasoconstriction)
Increases cAMP levels by stimulating adenylate cyclase
104
AE of dobumatine?
Excessive vasoconstriction and tachyarrhythmia
105
Milrinone MOA?
Inhibits PDE that converts cAMP to inactive 5-AMP; therefore increases cAMP concentration which increases calcium release
106
Milrinone AE?
Arrhythmias, hypotension, liver toxicity, and thrombocytopenia
107
What are the structures found in digoxin?
2 main groups: glycones and aglycones
Within aglycones are steroid nucleus, which is for activity
Within aglycones are 17-unsaturated lactone, which is for target binding (but not required)
The glycone side is for partitioning and kinetics of action, no biological activity
108
What is a generic structure of a beta-agonist?
Catechol with a primary/secondary amine separated by 2 carbons
If the amine is secondary, most likely is a selective beta-1 agonist
The hydroxyl groups in the catechol give direct action to beta-receptor agonist activity
109
What is a generic structure of a PDE3 inhibitor?
Contains a pyridine group (benzene with a nitrogen in it)
R1 (further from nitrogen) and R2 (next to nitrogen) are related to potency
110
What is the initial and target dose of captopril for chronic HF?
6.25mg TID + 50mg TID
111
What is the initial and target dose of enalapril for chronic HF?
2.5mg BID + 20mg BID
112
What is the initial and target dose of lisinopril for chronic HF?
2.5mg daily + 40mg daily
113
What is the initial and target dose of ramipril for chronic HF?
1.25mg daily + 10mg daily
114
What is the titration strategy for ACEi and chronic HF?
Increase dose every 2 wks until target or max tolerated dose is reached
115
Contraindications of ACEi?
Creatinine >3
History of angioedema or hyperkalemia
Stenosis
Pregnancy
Labile BP or hypotension
116
What is the initial and target dose of valsartan for chronic HF?
40mg BID + 160mg BID
117
What is the initial and target dose of candesartan for chronic HF?
4 mg daily + 32mg daily
118
What is the initial and target dose of losartan for chronic HF?
25mg daily and 150mg daily
119
What is the initial and target dose of carvedilol for chronic HF?
IR; 3.125mg BID + 25mg BID (<85kg) or 50mg BID (>85kg)
CR; 10mg daily + 80mg daily
120
What is the initial and target dose of metoprolol for chronic HF?
Only use succinate variant
12.5mg + 200mg daily
121
What is the initial and target dose of bisoprolol for chronic HF?
1.25mg and 10mg daily
122
When should a beta blocker be initiated in chronic HF?
Only in stable patients and even if they are on ACEi w/ or w/o diuretics
123
Contraindications of BB?
Decompensated HF
Bradycardia
Hypotension
Sick sinus syndrome
AV block
Pulmonary disease
Hemodynamic instability
Fluid overload
124
Who should take aldosterone antagonist with chronic HF?
1. LVEF≤35%
* history of CV hospitalization or elevated BNP
* on standard therapy
* SCr should be ≤2.5 in men or ≤2 in women
* Potassium <5
2. LVEF≤40 who develop symptoms of HF or have history of diabetes (usually pick eplerenone)
125
What is the initial and target dose of spironolactone for chronic HF?
12.5mg + 50mg daily
126
What is the initial and target dose of eplerenone for chronic HF?
25mg + 50mg daily
127
What are some contraindications for spironolactone?
Anuria
CrCl<10
128
What are some contraindications for eplerenone?
CrCl<30 or <50 w/ SCr >2 in men and >1.8 in women
T2DM with microalbuminuria
129
What is the initial and target dose of Bidil for chronic HF?
1 tab TID + 2 tabs TID
130
What is the initial and target dose of hydralazine for chronic HF?
25mg TID + 300mg daily in divided doses
131
What is the initial and target dose of ISDN for chronic HF?
20mg TID/QID + 120mg daily in divided doses
132
Who should be on ivabradine for chronic HF?
Someone w/ symptomatic HF and
* EF≤35%
* Resting HR ≥70
* Max tolerated BB or contraindicated for BB use
* On standard therapy (ACEi or ARB, MRA, BB)
* Persistent symptoms
133
Ivabradine dose?
5mg BID (<75 yrs old) + 7.5mg BID
2.5mg BID (≥75 yrs old) + 7.5mg BID
134
What are some titration strategies for Ivabradine?
After 2 wks, adjust dose to achieve resting HR between 50 and 60
135
Ivabradine contraindications?
Acute decompensate HF
Liver issues
BP <90/60
Resting HR <60
Pacemaker
Sick sinus syndrome
Any heart blockage
Inhibitors of 3A4
136
Ivabradine AE?
Bradycardia
HTN
A. Fib.
Luminous visual phenomena
137
Ivabradine while pregnant?
Fetal harm can occur
Use contraception
138
What is the dosing schedule for Entresto? This drug is a Angiotensin Receptor-Neprilysin Inhibitor (ARNI)
Should not be given within 36 hrs of last ACEi dose
If pt had prior ACEi/ARB use, risk for hypotension, and has moderate hepatic impairment, use 50mg, then 100mg, then 200mg. Change every 2-4 wks as tolerated
If pt only had prior ACEi/ARB use, use 100mg, then 200mg
139
Entresto contraindications?
History of angioedema w/ ACEi or ARB
Concomitant use with ACEi
Concomitant use with aliskiren (Tekturna) in pt w/ diabetes
140
Besides contraindicated points, who should not use Entresto?
If you're breastfeeding or have hepatic impairment
141
RX interactions w/ Entresto?
Dont take w/ ACEi, ARB, or aliskiren
Potassium-sparing diuretics (increases potassium)
Lithium - risk of lithium toxicity
NSAIDs - renal impairment
142
Digoxin dose?
0.125mg + 0.25mg daily
143
Digoxin drug interactions?
Because digoxin is a substrate of P-gp, P-gp inhibitors such as verapamil, amiodarone, and diltiazem will affect it
144
Furosemide dose?
20mg daily + 600mg daily in divided doses
145
Bumetanide dose?
0.5mg daily/BID + 10mg daily in divided doses
146
Torsemide dose?
10mg daily + 200mg daily in divided doses
147
Metolazone dose?
2.5mg taken 30 min before loop diuretic + 10mg (rare)
148
How do you convert furosemide IV to PO?
50mg IV x 2 = 100mg PO
149
How do you convert torsemide IV to bumetanide PO?
1:1
20mg IV Torsemide = 20mg PO Bumex
150
How do you convert from furosemide PO to bumex and torsemide?
40mg PO Furosemide = 1mg Bumex = 10-20mg Torsemide
151
What can you use for diuretic resistance?
Metolazone
It inhibits sodium reabsorption at cortical diluting segment
Creates SYNERGISTIC DIURESIS - MONITOR CAREFULLY
152
What meds can cause fluid retention in HF pt?
NSAIDs + TZD
153
What meds can cause weaker ventricular contractions in HF pt?
Non-DHP CCB *a negative inotrope
154
What meds can cause increased mortality and hospitalizations in HF pt?
TNF alpha antagonists aka "mabs"
155
What meds can cause increased afterload in HF pt?
Serotonin agonists aka "triptans"
156
What are causes of acute decompensated HF?
Nonadherence
Acute myocardial ischemia
Uncorrected HTN
A. Fib + Arrhythmias
Negative inotropes
Drugs that cause salt and water retention
Alcohol
Infections
Pulmonary embolism
***PANDANI AU
157
What is the cutoff for dry and wet HF?
<18 PCWP = Dry
>18 PCWP = Wet
158
What is the cutoff for cold and warm HF?
<2.2 Cardiac Index = Cold
>2.2 Cardiac Index = Warm
159
What are the ceiling doses for loop diuretics on acute decompensated HF?
GFR >50
Lasix = 80-160mg PO or 40-80mg IV
Torsemide = 20-40mg
Bumex = 1-2mg
Edecrine = 30mg
160
What are some pearls of the loop diuretics?
Lasix = Max infusion of 4mg/min in doses ≥160mg; Concerned w/ ototoxicity
Edecrin = Used only in sulfa allergy and is expensive
161
If a diuretic alone isnt working for acute decompensated HF, what can you do?
Add another diuretic
Low dose dopamine (to improve diuresis and renal blood flow)
Ultrafiltration; expensive, requires veno-venous access, and more nursing support
162
When are diuretics needed in acute decompensated HF?
>18 PCWP
163
When are vasodilators needed in acute decompensated HF?
Considered in all warm and wet HF patients
If cold and wet, make sure SBP >90
164
Which parameter reflects preload?
CO
MAP
PCWP
SVR
PCWP
165
Which parameter reflects afterload?
CO
MAP
PCWP
SVR
SVR
166
Arterial dilators vs Venous dilators affect different parameters, what are they?
Arterial dilators = Reduce afterload, Decrease SVR, and Increased SV and CO
Venous dilators = Reduce PRELOAD, Decrease PCWP, and reduce edema
167
What are the vasodilators used for acute decompensated HF?
Nitroglycerin
Nesiritide
Sodium Nitroprusside
168
Nitroglycerin acts more on the (veins/arteries)
veins, arterial only at high doses such as >100mcg/min
169
Nesiritide acts more on the (veins/arteries)
both are equal
170
Sodium Nitroprusside acts more on the (veins/arteries)
both are equal
171
What is a typical dose of nitroglycerin for ADHF?
5 to 200mcg/min (increase in increments of 5mcg/min)
172
What is a typical dose of nesiritide for ADHF?
2mcg/kg IVB
0.01mcg/kg/min; use this if there is a concern for hypotension
173
What is a typical dose of nitroprusside for ADHF?
0.1-0.2mcg/kg/min, then to 0.2-2mcg/kg/min
174
When are inotropes given for ADHF?
PCWP >15, guidelines study up to warm and wet region, but not really used
175
Which RX are positive inotropes?
Dobutamine
Milrinone
Digoxin
176
Which RX are negative inotropes?
BB + Non DHP CCB
177
Nitroglycerin MOA?
Increase production of cGMP, which causes vasodilation
178
Nesiritide MOA?
Recombinant BNP, increases cGMP, which causes vasodilation
179
Nitroprusside MOA?
Nitric oxide stimulation, increases cGMP, which causes vasodilation
180
Which RX should be given for ADHF when on a beta blocker?
Milrinone
181
When are fluids given for ADHF?
Below 2.2 Cardiac Index + Below 15 PCWP = Cold and Dry
182
Content of Chylomicrons?
Large and derived from diet
98-99% is TG
Contains bile acids; involved in absorption of fat from small intestines
183
Function of Chylomicrons?
Transfers TG + cholesterol from gut to liver
184
Metabolism of Chylomicrons?
Catabolized by LPL in free FA and chylomicron remnants
185
Content of VLDL and IDL?
Large and mostly TG, but carries 15-20% of serum cholesterol
Contains apo B, which is atherogenic
186
Function of VLDL and IDL?
Precursors to LDL
187
Metabolism of VLDL and IDL?
VLDL is catabolized by LPL to form IDL and then further to LDL
Hepatic lipase (HTGL) converts VLDL to IDL to LDL by removing TG
188
Content of LDL?
Carries 60-70% serum cholesterol
Contains apo B
189
Function of LDL?
GREATEST contributor to atherosclerosis since is attaches to arterial walls via oxidation
190
Metabolism of LDL?
Liver removes 70% of LDL from circulation
PCSK9 and LDL metabolism; it promotes LDL receptor degradation. Inhibiting PSCK9 increases LDL metabolism
191
Content, Function, and Metabolism of HDL?
Synthesized in liver + intestines (everything else is just liver except chylomicrons, which are intestines only)
Carries 20-30% serum cholesterol
Participates in reverse cholesterol transport
192
What is the response to injury hypothesis?
Injury to endothelium
Inflammatory process
Fibrous cap formation
Plaque rupture
193
What happens in the injury to endothelium phase in the response to injury hypothesis?
Increased LDL transport and it binds to extracellular matrix and oxidizes to trigger an inflammatory response
Increased coagulation + vasoconstriction
194
What happens in the inflammatory phase in the response to injury hypothesis?
Monocytes are recruited and transformed to macrophages
Lipid-filled macrophages = foam cells
Foam cells accumulate to form fatty streaks
195
What happens in the fibrous cap formation phase in the response to injury hypothesis?
Fatty streak grows which leads to plaque
Symptoms first occur at plaque formation
196
What happens in the plaque rupture phase in the response to injury hypothesis?
Clot may cause an arterial occlusion
Clots of this nature (atherosclerotic) is not the same as venous thromboembolism
197
What is a desirable level of total cholesterol?
<200
198
What is a desirable level of non-HDL-C?
<130
199
What is a desirable level of LDL-C?
<100; high value >190 is usually a genetic condition
200
What is a desirable level of HDL-C?
Men <40 (low)
Women <50 (low)
201
What is a desirable level of TG?
<150
202
What are some secondary causes of elevated total cholesterol?
Hypothyroidism
Obstructive liver disease
Steroids, Protease inhibitors, Thiazides, BB
203
What are some primary causes of elevated LDL levels?
Genetics; familial hypercholesterolemia, defective apolipoprotein B-100, polygenic hypercholesterolemia
204
What are some secondary causes of elevated TG?
T2DM, Obese, Cigarettes, Alcohol, High CARB intake
Steroids, Thiazides, BB, Bile acid sequestrants, Atypical antipsychotics
205
What is the difference between type 1 and 2 statins?
Type 1: fungal metabolites such as Lovastatin, Pravastatin, and Simvastatin
Type 2: Generate by organic synthesis such as Fluvastatin, Atorvastatin, and Cerivastatin
206
Statins and HMGR active site, what happens?
Statins exploit flexibility of HMGR to create a hydrophobic binding pocket near active site
207
Common side effects of statin drugs?
HA, myalgia, fatigue, GI issues, Flu-like symptoms, Increased liver enzymes
208
What drug class increases HDL-C % the most?
Nicotinic acid, followed by fibrates
209
What drug class decreases LDL-C % the most?
Statins, followed by nicotinic acid and/or cholesterol absorption inhibitors
210
What drug class decreases TG % the most?
Nicotinic acid and/or Fibrates
211
What drug is known as a cholesterol absorption inhibitor?
Zetia
212
What class of drugs for lipids dont affect TG?
Bile acid sequestrants (could also increase....?)
213
What class of drugs for lipids acts on PPAR alpha ligands that stimulate gene transcription?
Fibrates
214
What class of drugs for lipids AE profile can include gallstones?
Fibrates
215
What class of drugs for lipids is metabolized to its glucuronide in intestinal wall, transported to liver, and excreted via the bile back to duodenum?
Zetia
216
What class of drugs for lipids are anions exchange resins that bind to bile acids and prevent their readsorption?
Bile acid sequestrants
217
What class of drugs for lipids has a lot of GI issues such as bloating, constipation, anorexia, and/or GI bleed?
bile acid sequestrants
218
What non-pharmacologic therapy focuses on lowering TG only?
Wt management
Physical activity
Avoiding sugar and refined foods
Choosing healthier fats
Limit alcohol intake
219
What non-pharmacologic therapy focuses on increasing HDL-C only?
Wt loss (every 10lbs increases it by 1.6)
Physical activity
Moderate alcohol intake
Smoking cessation
220
What are your high intensity statins?
Rosuvastatin 20-40mg
Atorvastain 40-80mg
Decreases LDL by >50%
221
What are your moderate intensity statins?
Pitavastain
Simvastain
Decreases LDL by 30-50% + includes high intensity drugs w/ reduced dose
222
What are your low moderate intensity statins?
Fluvastatin
Lovastatin
Pravastatin
Decreases LDL by <30% + includes moderate intensity drugs w/ reduced dose
223
When should you take statin drugs?
Shorter half life? Evening
EX: Lovastatin, Simvastatin, Pravastatin, Fluvastatin
Longer half life? Any time of day
EX: Atorvastatin, Rosuvastatin, Pitavastatin
224
Statins interact w/ CYP3A4 inhibitors, which one is not metabolized by that enzyme?
Pravastatin
225
What are some warnings for statins?
May worsen or cause new onset DM
Myopathy (especially w/ elderly)
Liver issues
Kidney issues (except w/ atorvastatin)
Cognitive impairment (reverses w/ statin d/c)
226
Contraindications of statins?
Concomitant use with gemfibrozil
Pregnancy or lactation
227
Monitoring parameters and statins?
Lipid panel; 4-12 wks
LFTs; routine monitoring NOT recommended
CPK; cannot rely to diagnose myopathy
228
Zetia AE?
Higher % of AE w/ statins
Diarrhea
Upper respiratory issues
Flu
Arthralgias
Extremity pain
229
Zetia RX interactions?
Cyclosporine + Fibrates increased levels of zetia
Bile acid sequestrants decreased levels of zetia
230
What are the PCSK9 inhibitors? How and often are they administered?
Evolocumab + Alirocumab
SQ every 2 wks or every month
231
What are hte adenosine triphosphate-citrate lyase inhibitors? How and often are they administered? MOA? AE?
Bempedoic acid
PO 180mg tablets daily
Inhibits ACL enzyme to decrease cholesterol synthesis and upregulates LDL-receptors
ADR = muscle spasms, back and ab pain, anemia
232
Who should not use an ACL inhibitor?
Ppl on doses of simvastatin >20mg or pravastatin >40mg
233
What are your bile acid sequestrants?
Colesevelam
Colestipol
Cholestyramine
234
How are bile acid sequestrants administered?
Give other drugs 1 hr before or 4 hrs after
Granules? Mix w/ ≥90 mls of liquid
Tablets? Take 1 at a time w/ fluids
Could suggest a stool softener
235
Contraindications of bile acid seuqestrants?
Elevated TG (>400)
Chronic constipation
Pre Existing biliary obstruction
236
What are your fibric acid derivatives?
Fenofibrate
Gemfibrozil
237
How are the fibric acid derivatives given?
Fenofibrate = 1 tab daily w/ or w/o food ****renally adjusted
Gemfibrozil = 1 tab BID w/ breakfast and dinner
238
Drug interactions and fibric acid derivatives?
Statins + Gemfibrozil
Warfarin
Niacin
Bile acid sequestrants
239
Fibric acid derivatives AE?
Fenofibrate = dose related increased LFTs, respiratory issues, ab pain
Gemfibrozil = dyspepsia, ab pain, diarrhea
240
Omega-3 FA AE?
Dyspepsia + Fishy burps
241
How do you decrease fishy burps w/ Omega-3s?
Store caps in fridge
Avoid hot liquids
Take w/ meals
Use enteric coating
242
Omega 3 Rx interactions?
Anything that increase bleeding risk
Anticoagulants, P2Y12 inhibitors, SNRIs, SSRIs, NSAIDs
243
Patient counseling of Niacin?
Flushing
Hyperuricemia
Hyperglycemia
244
How do you decrease flushing w/ Niacin?
Take w/ food
Pre-medicate w/ aspirin
Avoid hot liquids and alcohol
245
Which drugs primarily reduce TG?
Fibrates, Omega 3s, and Niacin
Everything else does LDL-C reduction :)
246
What RX should you give to prevent severe hypercholesterolemia (LDL ≥190)
Start w/ max tolerated statin
Then add zetia
Then add BAS***fasting TG is ≤300
247
What RX should you give to prevent DM and someone w/ LDL from 70 to 189?
Use moderate intensity statin regardless of ASCVD risk
If multiple risk factors, use high intensity
If ASCVD risk ≥20% add zetia (only high intensity statin w/o DM + if risk is between 7.5 and 20, use moderate intensity***)
both scenarios are for someone aged 40-75
248
Lipid Panels and monitoring frequency??
Non-fasting labs, except for when someone didnt eat anything for the last 6-8hrs or if TG is above 400 or if they are above the age of 20 w/ family issues of hyperlipidemia
4-12 wks after initiation or dose change
Every 3-12 months to assess adherence or safety
249
ALTs and Monitoring frequency?
Not routine unless sx of hepatotoxicity
250
CPKs and Monitoring frequency?
Only when pt has sx of myopathy
