CV Drugs Flashcards
1
Q
Watch out in using ACE inhibitors and ARBs in those with _______-kalemia.
A
hyper (as both cause this by counteracting the sodium-potassium exchanger in the collecting duct)
2
Q
Why does hypokalemia increase risk of digoxin toxicity?
A
Because more digoxin binds when there is less potassium to bind (Think of the additional vending machine getting pushed up against the wall when its bananas have been depleted.)
3
Q
Why are beta blockers better at treating supraventricular arrhythmias?
A
Because their strongest effect is in slowing AV node conduction (Think of the heart light whose bottom half is broken.)This effect can also cause heart block (think of the heart shield on Louis Heartstrong’s hat).
4
Q
Long-term digoxin use can lead to what ECG finding?
A
“Scooped” ST segments (Think of the high schooler scooping the taSTy ice cream.)
5
Q
All IA drugs can cause ___________.
A
torsades (think of the banner twisting across the ground floor)
6
Q
Which class III drug has a lot of beta-blocking ability?
A
Sotalol (Think of the guy knocking over soda bottles with his beta-bugle.)
7
Q
Why does prolonged QT interval cause torsades?
A
Because the voltage-sensitive sodium channels can fire again
8
Q
What is unique about nitroprusside compared to the other nitrate drugs?
A
It causes equal arterial and venous dilation, whereas the other nitrates mostly cause venous dilation. (Think of the guy driving the nitro-pressure boat with equally dilated sleeves and pants.)
9
Q
What is one common use of dihydropyridine blockers?
A
Control of hypertension in pregnant women, because they have been shown to be safe.(Think of the pregnant woman cutting an apple for the DIPpIN’ station with a large knife –the knife represents nifedipine.)
10
Q
The class I anti-arrhythmics have _______ dependence.
A
use (because they only bind to open Na channels)
11
Q
How do the dihydropyridines treat angina?
A
They decrease afterload and thus decrease oxygen demand. (Think of the older woman throwing off her oxygen cannula AFTER finishing her LOAD of soft serve.)
12
Q
The IA drugs also ________________.
A
block potassium channels (just like the prom queen tossing back the banana curtains), thus prolonging the depolarization of the ventricles
13
Q
Explain the action of angiotensin II on GFR.
A
It causes the efferent arteriole to constrict, which preserves GFR. This is important because in low-volume states, the kidneys might not have the pressure needed to filter the blood. (Think of the guy with two tense red suspenders sipping coffee from the Grounds Filter Rate machine.)
14
Q
Be careful using the non-dihydropyridines in those with ______________.
A
heart block (represented by the heart-block shield)
15
Q
Sympathetic innervation causes the AV node ______________.
A
conduction velocity to increase
16
Q
What side effects do you need to keep in mind when administering hydralazine?
A
• Hypotension (woman fainting) from excess arteriolar dilation • Exacerbation of angina from reflex tachycardia (angina anvil on fire hose) –can be blocked with B1 blocker •Lupus (wolf on boat) –also remember that hydralazine is the H in SHIPP-E (the lupus-causing drugs)
17
Q
Digoxin should be used in extreme caution with drugs that _______________.
A
can cause heart block (like beta-blockers); this is because digoxin can also cause AV nodal heart block(Think of the girl on the dance floor blocking the guy’s advances at the AV node location; also, the exit to the gym needs to remain unßlocked.)
18
Q
Common side effects of digoxin include _________________.
A
xanthopsia (objects appearing yellow) and GI upset(Think of the guy in the dance hall about to vomit –he’s bathed in a yellow spotlight.)
19
Q
Which drug is mostly non-dihydropyridine but has some vasodilatory effects?
A
Diltiazem (so the Dark Chocolate Diltiazem is in the middle, between Very Vanilla Verapamil and the Dairy Berry Dihydropyridines)
20
Q
Digoxin should be used in extreme caution with drugs that _______________.
A
can cause heart block (like beta-blockers); this is because digoxin can also cause AV nodal heart block(Think of the girl on the dance floor blocking the guy’s advances at the AV node location; also, the exit to the gym needs to remain unßlocked.)
21
Q
Where do the class I anti-arrhythmics act?
A
On the His-Purkinje system (think of the neon lights on the HP system, not the SA or AV)
22
Q
Any drug that blocks __________ can cause torsades.
A
potassium channels (because it prolongs the QT interval)
23
Q
Because digoxin stimulates vagus nerve activity, it can lead to ______________.
A
bradycardia from SA node slowing(Think of the Las VeGaS theme –representing increased vagal nerve tone –with John Cusack on the SA node holding a dangling heart-shaped pocket watch.)
24
Q
What are the classic class IV drugs?
A
Verapamil (Very Vanilla ice cream)Diltiazem (Delicious Dark chocolate)
25
What does adenosine do to the heart?
It temporarily causes heart block, thus being an ideal drug for treating supraventricular tachycardia.
26
What type of calcium channels do the class IV drugs block?
L-type, also called non-dihydropyridine (think of the L-shaped handle of the Non-Dairy soft-serve dispenser)
27
Those with digoxin toxicity often have what symptom?
PVCs
28
All CCBs are contraindicated in _________________.
those with CHF(Think of how the kid with the deflated heart balloon – representing CHF – is locked out of the store.)
29
How does digoxin exert antiarrhythmic effects?
It directly stimulates the vagus nerve, leading to increased parasympathetic input on the SA and AV nodes – think of the "Las Vegas" sign next to DJ Foxglove.
30
Why should IC drugs not be used in someone with structural defects?
Because they tightly bind sodium channels and thus have the strongest effect on the phase 0 upslope
31
The class III antiarrhythmics uniquely share ______________.
some properties of all the categories of drugs: they block inactivated sodium channels (I), block beta-receptors (II), and block calcium channels (IV) (Think of the three singers counting off "uno dos tres cuatro!")
32
What ECG finding might you see in someone taking class I anti-arrhythmics?
A widened QRS (think of the wide QRS-shaped crack in the neon sign) because the His-Purkinje fibers have been slowed and the ventricles take longer to depolarize
33
True or false: milrinone and nesiritide are acute agents.
True! (Think of the "Acute Issues" campaign.)
34
_____________ is an indicator of digitalis toxicity.
Hyperkalemia
35
Severe muscle weakness is a symptom of _______-kalemia.
hypo
36
Nitroprusside causes what adverse effect, particularly in those with renal impairment?
Cyanide poisoning (like the CN pipe pumping cyan gas in the driver's face)
37
What is the mechanism of nesiritide?
It is a BNP analog, stimulating vasodilation of arteries and veins as well as diuresis of sodium. (Think of the elephant with the dilated arterial trunk and venous legs who is pouring out water onto peanuts.)
38
What does sympathetic innervation do to the SA node?
It increases the rate of the SA node automaticity.
39
The class I drugs target the _________. What effect does this have on the cardiac action potential?
Open sodium channels (think of the singer clutching the jar of peanut butter that is OPEN) This decreases the slope of the action potential (think of him leaning the microphone over, decreasing the slope of the cord's wave), this ultimately slows the action potential through the cardiac tissue.
40
True or false: milrinone and nesiritide are acute agents.
True! (Think of the "Acute Issues" campaign.)
41
Which antiarrhythmics do not bind to potassium channels?
The IC. (Think of the untouched curtain on the 3rd floor.) As such, they do not prolong the action potential.
42
Dermatologically, amiodarone can _______________.
cause gray-blue discoloration in sun-exposed areas
43
Class IB drugs have what effect?
They have the lowest affinity for sodium channels of the class I drugs, so they don't cause torsades or prolonged QT. Also, they don't block potassium channels as much (think of Libby closing the potassium curtain), and thus speed up the action potential – shortening its duration. (think of Libby shutting the potassium blinds quickly).
44
_____________ is an indicator of digitalis toxicity.
Hyperkalemia
45
What is the mechanism of milrinone?
It is a phosphodiesterase inhibitor that leads to increased inotropy and arteriolar vasodilation.(Think of the politician with the cAMPaign: "one in a MILlion." He is trying to PHOSter interest. He also has floppy dilated ears.)
46
What antiseizure medication has antiarrhythmic effects?
Phenytoin (it is a class IB drug – think of the friendly towing truck outside Libby's window)
47
The antiarrhythmic that is also a purine interacts with what cardiac receptor?
The A1 receptor (this being adenosine) (Think of the doorway allowing only A1-level swing dancers onto the floor.)
48
Which arrhythmias are treatable with class III drugs?
Both supraventricular (atrial) and ventricular arrhythmias, such as atrial fibrillation (they specifically control the rhythm of atrial fibrillation)
49
Gingival hypertrophy is a side effect of which CCB?
Verapamil (like how the janitor is blowing a bubble with his gum)
50
Which three agents are recommended for first-line treatment of essential hypertension?
• Hydrochlorothiazides (kid on HIGH dive with muscular THIGHs) • Dihydropyridine calcium channel blockers (Calci-YUM ice cream machine) • ACE inhibitors (gambling Aces table near hot tub)
51
True or false: class IV drugs can cause increased QT interval.
False. They cause increased PR interval, because they slow conduction between the atria and ventricles.
52
Other than systolic heart failure, digoxin can also treat _____________.
atrial arrhythmias, because it has a greater effect on the atria
53
What can increase the half life of digoxin?
- Kidney failure- Antiarrhythmic drugs (Think of the overturned, kidney-shaped juke box, with the rival high schooler standing over it with a long, tapering flag. There are also records thrown over the floor – symbolizing antiarrhythmics like verapamil and amiodarone that can prevent renal clearance of digoxin.)
54
Because digoxin stimulates vagus nerve activity, it can lead to ______________.
bradycardia from SA node slowing(Think of the Las VeGaS theme – representing increased vagal nerve tone – with John Cusack on the SA node holding a dangling heart-shaped pocket watch.)
55
What kind of channel is the L-type, non-dihydropyridine calcium channel?
Voltage-gated
56
What is the basic function of class IV antiarrhythmics?
They, like the class II drugs, slow heart rate. Class IV drugs do so by blocking nodal calcium channels.
57
Arterial vasodilators decrease ________-load.
after
58
What is the mechanism of adenosine?
It allows more potassium to exit the cell and less calcium to enter, allowing the membrane to remain negative and suppressing AV nodal action potentials. (Think of the swing dancers on the musical NODE – in the middle of the heart – with the banana flying up and the calci-yum fallen onto the ground.)
59
What is the mechanism of milrinone?
It is a phosphodiesterase inhibitor that leads to increased inotropy and arteriolar vasodilation.(Think of the politician with the cAMPaign: "one in a MILlion." He is trying to PHOSter interest. He also has floppy dilated ears.)
60
What agents can be given to someone with hypertensive emergency?
• IV B1 antagonists (like the bugles being blocked on the deck) • IV labetalol (like the labetalol organ) • Dihydropyridine CCBs (woman in lifeboat with Calci-Yum) • Hydralazine (HYDRo lifeboat) • Nitroprusside (NO agent that stimulates GMP like the GruMP next to the NITRO-powered boat in the background) • Fenoldopam (OLD mam PAM)
61
What unique problem can magnesium treat?
Torsades The mechanism is not understood. (Think of the guy moonwalking over the torn torsades banners
62
Two antihypertensive drugs are usually needed for patients with BPs more than ______________ above the upper recommended limit.
20/10 (Think of the life preservers: "2 recommended for more than 20 lbs.")
63
Specifically, IA drugs can treat ______________.
Wolff-Parkinson-White syndrome
64
How does fenoldopam work?
It is a D1 agonist (like the single dope rope held by OLD lady PAM). It causes dilation of the arteries (like the dilated arm sleeves) with increased renal perfusion (represented by the spilling peanuts and kidney that she's standing on).
65
What is the mechanism of digoxin?
It inhibits the Na/K pump, preventing sodium from being pumped out and potassium from being pumped in. The excess intracellular sodium then leaves the cell through increase Na/Ca exchange, thereby providing more calcium for the sarcoplasmic reticulum. (Think of the coach with peanuts, unable to leave the gym and the Calci-Yum sneaking in through the door opened by the kid sneaking out with peanuts.)
66
What are key clinical components of hypertensive emergency?
• BP above 180/120 (like the 180º protractor near the 12" ruler on the workstation in the boiler room) • New-onset signs of organ damage such as pulmonary edema, neurologic damage, or kidney failure (this is somewhat loosely represented by the "end-organ damage" done to the Titanic's boiler room)
67
IB drugs target ___________ tissue.
ischemic/damaged (B = Broken) As such, they're great for treating ischemia-induced arrhythmias.
68
What can treat digoxin overdose?
Digoxin Fab! (Just like the FABulous Las Vegas theme!)
69
Beta blockers cause prolonged phase __________.
4 (thereby decreasing heart rate)
70
Renin is produced, stored, and released from _____________.
the juxtaglomerular apparatus
71
What is the name of the cardiac action potential's initial upslope?
Phase 0
72
List four antihypertensive agents that are safe in pregnancy.
• Alpha methyldopa (pregnant Christine in the phantom Sketch) • Nifedipine (pregnant woman cutting apple in CCB Sketch) • Labetalol (pregnant organist in beta-blocker Sketch) • Hydralazine (pregnant woman being loaded onto HYDRo rescue lifeboat in this Sketch)
73
Beta-blockers and ACE inhibitors decrease the ______________ after MIs.
undesired remodeling
74
Which CCBs are used in hypertensive emergency?
The dihydropyridines, specifically nicardipine and clevidipine (like the NIce CARD read by the woman in the lifeboat that has a CLoVer on it)
75
What can treat digoxin overdose?
Digoxin Fab! (Just like the FABulous Las Vegas theme!)
76
What is the main side effect of verapamil?
Constipation(Think of the janitor with the plumber next to the vanilla dispenser.)
77
What do calcium-channel blockers do to the cardiac action potential?
It slows the phase 0 upslope, thereby decreasing sinus activity, prolonging conduction velocity, and lengthening refractory period – all nodal effects.
78
True or false: A1 stimulation can lead to vasodilation.
False. The A2 receptors (also stimulated by adenosine) mediate vasodilation.
79
Though there isn't much research on this, verapamil is often the first choice for prevention of ______________.
migraines (Think of the referee hitting the migraine bell on the contest table.)
80
ACE inhibitors should be prescribed to those with hypertension and ________________.
past MIs or current diabetes (guy playing broken heart string guitar near jar of candy on Aces table)
81
What disorder is symbolized by the fingerless gloves?
Raynaud's; the dihydropyridines can be used to treat Raynaud's, so the man with the fingerless gloves is holding some of the DIPpIN' toppings.
82
What suffix is common in the class III drugs?
-tilide (as in dofetilide and ibutilide)(Think of the "TILl I DiE" marriage proposal to the girl sitting at the table.)
83
IA can treat ______________.
supraventricular and ventricular arrhythmias
84
What is the mechanism of class III antiarrhythmics?
They block potassium channels, thus prolonging both depolarization and repolarization of the His-Purkinje fibers and cardiac myocytes. (Think of the mariachi singer throwing aside the banana curtain, thus flattening out the action-potential wave.)
85
ACE inhibitors reduce mortality in those with _____________.
MI and heart failure (Think of the guardian angel flying above the couple.)
86
What two drugs can inhibit the effects of adenosine?
Caffeine and methylxanthine (represented by the guy drinking the xanthine energy drink, blocking the entrance to the Swing Dance podium)
87
True or false: all L-type channels are found in the heart.
False. There are L-type dihydropyridine receptors in smooth muscle.
88
Why does hypokalemia increase risk of digoxin toxicity?
Because more digoxin binds when there is less potassium to bind (Think of the additional vending machine getting pushed up against the wall when its bananas have been depleted.)
89
Which antiarrhythmics can cause neurologic effects?
IB (think of Libby and her boyfriend's hats – the hat "he got on their first date" that looks like a brain) IB can cause paresthesias or slurred speech.
90
A cardiac patient presenting with muscle weakness might have what ECG sign?
U waves (indicative of hypokalemia)
91
What is the key role of beta-blockers in treating arrhythmias?
Slowing the SA node automaticity and the AV node conduction (Think of the two musical nodes on Beta Fitzgerald's music sheet.)
92
True or false: amiodarone causes hyperthyroidism.
True, but it can also cause hypothyroidism! (Think of the two singers: one has an untied bowtie, and the other has a large, tied bowtie.)
93
ACE inhibitors can cause ________________ because of the sudden decrease in vasoconstriction.
hypotension
94
Nimodipine is administered to all patients with ______________, preferably within four days of the event.
subarachnoid hemorrhage(Think of the guy with the berries on his brain-like ice cream – symbolizing berry aneurysm – next to the "Need MOre DIPpIN'?" sing.)
95
What can increase the half life of digoxin?
- Kidney failure- Antiarrhythmic drugs (Think of the overturned, kidney-shaped juke box, with the rival high schooler standing over it with a long, tapering flag. There are also records thrown over the floor – symbolizing antiarrhythmics like verapamil and amiodarone that can prevent renal clearance of digoxin.)
96
CCBs and thiazides are particularly helpful in which patients?
Elderly African-American patients (like the older AA man in the hot tub near the Dippin' Calci-Yum machine and his muscular thighs)
97
What do you need to keep in mind when prescribing nifedipine?
It has an extremely short half-life, so it acts quick and can cause reflex tachycardia. This will worsen angina, represented by the pregnant woman using the large knife to cut into the apple-shaped heart.
98
The beta blockers _____________ calcium current. Why is this important in their effects?
decrease (by decreasing cAMP); this slows the upstroke of the nodal action potentialRecall that the nodes have slowly leaking sodium channels that create the phase 4 gradual depolarization, and that the action potential in the nodes is triggered by VSCC.
99
What is symbolized by the singers' glasses?
The fact that amiodarone can cause gray corneal deposits (in almost all patients with a couple weeks)
100
What kind of arrhythmias can class IV drugs treat?
Atrial fibrillation and atrial flutter (think of the TV with static in the shop) because they prolong conduction time and can prevent the atria from inducing ventricular tachycardias
101
The three class IA drugs are ________________.
quinidine, procainamide, and disopyramide
102
What are the side effects of quinidine?
Cinchonism (tinnitus – tin plates – headache, and dizziness) and thrombocytopenia (broken plates)
103
What two effects do the non-dihydropyridine blockers have?
Decreased contractility and heart rate(This is represented by the weak kid – who can't pull down the lever and has a dangling watch.)
104
The dihydropyridine channels end in the __________ suffix.
-dipine
105
Angiotensin II acts on the ____________ to directly stimulate increased sodium reabsorption.
PCT (Think of the guy watching the Pro Cart Track TV eating salty peanuts.)
106
Do not give disopyramide to those with heart failure! Why?
Because at high doses it has a negative inotropic effect
107
Long-term digoxin use can lead to what ECG finding?
"Scooped" ST segments (Think of the high schooler scooping the taSTy ice cream.)
108
ACE inhibitors and angiotensin-receptor blockers can cause a temporary increase in creatinine. Why?
Because they temporarily decrease GFR; think, if angiotensin increases GFR by constricting the efferent arteriole, then ACE inhibitors decrease GFR by dilating the efferent arteriole.
109
IC drugs are great at treating _____________.
atrial fibrillation (at least, the rhythmic aspect of it; other drugs are used to slow the rate) Think of the static, irregularly irregular rhythm on the TV and the guy zapping the channel to a more regular rate.
110
Long-term use of procainamide can cause ______________.
lupus (think of the PROm king's wolf)
111
Common side effects of digoxin include _________________.
xanthopsia (objects appearing yellow) and GI upset(Think of the guy in the dance hall about to vomit – he's bathed in a yellow spotlight.)
112
Patients with hypertension and _______________ should be given an ACE inhibitor.
albuminuria (think of the ALBUM in the Diasweeties Shop with high pressure pipes)
113
The nodal upstroke relies on __________, and so is not affected by class I anti-arrhythmics.
calcium
114
In what situations would you not use an ACE inhibitor?
Pregnancy (think of the tarantula on the jacket of the woman being escorted out)C1 esterase deficiency (a hereditary condition of angioedema in which people lack the enzyme that inhibits the complement pathway; think of the girl with the C-shaped lip ring)NSAID useBilateral renal artery stenosis (the two purses with red straps)
115
Beta blockers and ___________ should be first-line in the treatment of angina, but calcium channel blockers can be used if those don't work or aren't tolerated.
nitrates
116
Which kind of calcium channel blocker is used in hypertensive emergencies?
The dihydropyridines, specifically nicardipine and clavidipine
117
What kind of arrhythmias can digoxin treat?
Atrioventricular (such as atrial fibrillation represented by the TVs behind DJ Foxglove), because it controls the rate (which is the first priority in treatment of atrial fibrillation)
118
Beta-blockers are great at treating __________.
atrial fibrillation – they slow the heart rate, the first goal of treating atrial fibrillation
119
What are the IC drugs?
Propafenone (PuRPle PHONE on the 3rd floor) and flecainide (FLaKes cereal)
120
What is the mechanism of digoxin?
It inhibits the Na/K pump, preventing sodium from being pumped out and potassium from being pumped in. The excess intracellular sodium then leaves the cell through increase Na/Ca exchange, thereby providing more calcium for the sarcoplasmic reticulum. (Think of the coach with peanuts, unable to leave the gym and the Calci-Yum sneaking in through the door opened by the kid sneaking out with peanuts.)
121
What is the mechanism of nesiritide?
It is a BNP analog, stimulating vasodilation of arteries and veins as well as diuresis of sodium. (Think of the elephant with the dilated arterial trunk and venous legs who is pouring out water onto peanuts.)
122
What neurologic side effects does amiodarone have?
Tremor, ataxia, neuropathy, and sleep disturbances
123
Hydralazine combined with ___________ has been shown to prevent mortality in CHF patients.
nitroglycerin (like the heart balloon tied to the TNT being thrown at the ice berg)
124
All of the potent arterial dilators can cause what two counterproductive side effects?
• Reflex tachycardia (doctor with heart-shaped reflex hammer) • Activation of the RAAS system (doctor with yellow umbrella)
125
What cardiopulmonary side effects does amiodarone have?
Pulmonary fibrosis (duh); heart block (represented by the singer's heart-block-shaped hat); and torsades (like every potassium-channel-blocking agent) – though dofetilide, ibutilide, and sotalol are more likely to cause torsades(Think of the twisting banners everywhere.)
126
Those with digoxin toxicity often have what symptom?
PVCs
127
What hepatic effects does amiodarone have?
It can cause hypersensitivity hepatitis, and it is an inhibitor of CYP450.
128
What are possible side effects of the dihydropyridines?
Lightheadedness and peripheral edema (Think of the overwhelmed patron next to the DIPpIN' station: he's dizzy and has baggy pants.)
129
The potassium current is found in which phases of the cardiac action potential?
2 (during which it competes with calcium) and 3 (during which it repolarizes the cell)
130
Which part of the heart can class IV drugs treat?
The atria (think of the broken bottom half of the heart sign), because class IV drugs block nodal rhythms
131
Other than systolic heart failure, digoxin can also treat _____________.
atrial arrhythmias, because it has a greater effect on the atria
132
What is the mechanism of aliskiren?
It is a direct renin inhibitor, thus preventing the conversion of angiotensinogen to angiotensin I.
133
Cholesterol is packaged into chylomicrons as _____________.
cholesteryl ester (like the cholesterol gold bars being packaged in CH-ESTs before being loaded onto the hot air balloon)
134
What is on the outside of chylomicrons?
Triglycerides (think of the hot air balloon with the TRI-pronged pitchforks sticking out)Also, keep in mind that chylomicrons have more triglycerides than cholesterol (just like how the hot air balloon is mostly pitchfork-wielding passengers and not so many chests)
135
___________ are on the surface of chylomicrons.
Apolipropoteins
136
Prior to being resorbed by the liver, chylomicrons deliver ________________.
triglycerides to peripheral tissues in the form of free fatty acids (just like the pitchfork-wielding passengers deboarding at the LipoProtein Lighthouse – LPL – above the muscle-clams on the beach)
137
Remnant lipoprotein is taken up by the liver by ________________.
apolipoprotein E-mediated endocytosis (think of the hot air balloon landing on the LoaD – L dock)
138
After being absorbed into hepatocytes, cholesterol from remnant lipoprotein can take one of two fates: ________________.
it can be secreted into bile acid (and then pooped out) or it can be packaged into circulating lipoproteins
139
Describe the composition of VLDL.
Mostly triglyceride (just like the airship VLDL mostly filled with pitchfork-wielding passengers) with apolipoprotein B100 (like the B-shaped anchor)
140
What is IDL?
Intermediate-density lipoprotein
141
LDLs are formed by ______________.
the continual loss of triglycerides from VLDL (think of the little LDL ship with only CHESTs on it)
142
What is the basic function of LDL?
It delivers cholesterol to the body (such as to the adrenals for steroid synthesis).
143
How do cells regulate their cholesterol levels?
When low on cholesterol, they express more apolipoprotein B100 receptors, leading to endocytosis of LDL. When cholesterol is abundant in cells, they express fewer B100 receptors, leading to less endocytosis.
144
How is LCAT depicted in this sketch?
As the diver moving free cholesterol bars (cholesterol) to the chests on the HDL submarine (cholesteryl ester)
145
HDL helps get cholesterol back to the liver (where it can be excreted as bile) by two mechanisms: ______________.
directly – by absorbing cholesterol as cholesteryl ester via LCAT – and indirectly – by using CETP to package cholesterol onto LDL(Think of the submarines directly taking chests back and adding chests onto the platforms beneath the LDL boat.)
146
Statins work in a one-two mechanism: _______________.
they decrease the synthesis of cholesterol by inhibiting HMG co-a reductase which then stimulates the liver to reel in more circulating LDL(Think of the Steampunk Statin pirate disrupting the gold-bar smelting and the other pirate making the sailors pull in more LDL by the B100 anchor.)
147
Remember, statins are the only lipid-lowering drug shown to ____________.
prevent CV mortality
148
It is standard practice to prescribe statins even in a patient with normal lipid levels if ___________.
they've had an MI, have diabetes, or have signs of peripheral vascular disease(Think of the pirate playing the banjo with broken strings, the pirate eating candy, and the clogged pipe.)
149
Remember an important contraindication for statins is _____________.
pregnancy (the teratogen tarantula on the submarine)
150
Statin-induced myopathy usually presents as ____________.
proximal bilateral muscle soreness
151
Remember to check for drug interactions with ____________.
CYP450-affecting drugs (because all statins except one are metabolized by CYP450) (Think of the CYP license plate on the tank.)
152
True or false: statins are idiosyncratic hepatotoxins.
False, but they can lead to a usually asymptomatic elevation in LFTs.
153
Cholestyramine is a _____________.
bile-acid-binding resin
154
Explain the bile circuit.
Bile is synthesized in the liver from cholesterol and sent down the hepatic duct into the intestine. It gets reabsorbed by the distal ileum.
155
What is an undesirable effect that cholestyramine has on serum values?
It also ramps up triglyceride synthesis. (Think of the men with pitchforks being chased off the liver dock by the cho-lobster-amine lobster.)
156
Because it ramps up cholesterol synthesis, cholestyramine can cause _____________.
gallstones
157
In the GI tract, cholestyramine can cause two worrisome things: ____________.
constipation (represented by the lobster squeezing the pipes of the intestinal airship) and decreased absorption of drugs and fat-soluble vitamins (including statins, represented by the steampunk statin clashing with the lobster)
158
Ezetimibe works by ________________.
blocking the dietary absorption of cholesterol, preventing loading into chylomicrons (just like the Z-shaped eel blocking the loading of gold onto the chylomicron hot air balloon)
159
What is the mechanism of evolocumab?
It is a monoclonal antibody that blocks PCSK9, thus preventing LDL receptor degradation.
160
The most common side effects of ezetimibe are ____________.
diarrhea and elevation of LFTs (represented by the LFT flag in the water and the diarrhea behind the ezetimibe eel)
161
The main triglyceride-carrying molecules in the blood are ____________.
chylomicrons and VLDL
162
What drug works by upregulating lipoprotein lipase?
Gemfibrozil; it does so by activating the PPAR-alpha receptor(Think of the guy burning the PPAR PaPeRs to signal more triglycerides down from the VLDL airship to help protect from the gemfibrozil jellyfish attack.)
163
After stimulating lipoprotein lipase, gemfibrozil ultimately _____________.
lowers VLDL levels (and consequently LDL levels); they also increase HDL levels (Think of the VLDL airship sinking with the jellyfish on top; the LDL boat sinking; and the HDL submarine being raised out of the water.)
164
When given with statins, gemfibrozil increases risk of ___________.
myopathy
165
What is the most potent HDL-raising medication?
Niacin (just like the Loch Niacin monster raising the HDL submarine more than any other drug)
166
In addition to raising HDL, niacin also _______________.
inhibits release of VLDL (just like the other Loch Niacin monster in the background who is biting the VLDL airship)
167
Taking ____________ before taking niacin can reduce the most common side effect of niacin therapy.
aspirin (because flushing is mediated by prostaglandins)
168
Niacin has what two side effects that are similar to thiazides?
Hyperglycemia (the diver throwing candy into the air) and hyperuricemia (the diver knitting with yellow needles)
169
How does fish oil work?
It inhibits the production of triglycerides and VLDL (think of the fish with oil trails swimming among the flotsam of triglycerides)
170
Nitric oxide activates __________ in vascular smooth muscle.
guanylyl cyclase
171
What does increased level of cGMP do inside cells?
It decreases intracellular calcium and deactivates myosin-light-chain kinase.(Think of how John Nitro gets to cut the P locks off of his Chain gang, just like how cGMP gets to cut phosphate groups off of myosin and prevent contraction.)
172
True or false: nitrates primarily affect arteries.
False. It affects veins most, but also arteries (just like the blue pants of the prisoners set free by John Nitro).
173
Nitrates mostly decrease ____-load.
pre (because of their effect on veins)
174
Why are sublingual tablets commonly used for nitroglycerine?
Because the liver has a high first-pass metabolism on nitroglycerine, so bypassing it is helpful.
175
Nitroglycerine has an extremely short half-life, so ___________ are used as maintenance therapies.
isosorbide dinitrate and isosorbide mononitrate (large doses)
176
Although it has not been shown to decrease mortality, nitroglycerine has been shown to help with __________ in acute coronary syndrome.
pain and symptom relief
177
Nitrates should be avoided in what kind of MI?
A right-sided MI, because they decrease pre-load; in this case, administer fluids to increase pre-load.
178
Nitroglycerine can acutely reduce ___________ in the lungs.
pulmonary edema (Think of the pump operator with the wet lung spots.)
179
What is pulmonary edema a possible symptom of?
Hypertensive emergency (think of the shutoff valve and how it represents NO shutting off hypertension)
180
Nitroglycerine can lead to venous dilation that causes blood to pool in the extremities. What cardiac effect does this cause?
Reflex tachycardia (just like the doctor with his heart-shaped reflex hammer rushing in to help the fainting woman); beta-blockers can be given to counteract this undesirable effect
181
What non-cardiac symptoms can nitro cause?
Facial flushingThrobbing headachesMethemoglobinemia (Think of the red-faced assistant, his obvious headache signs, and the rusty – oxidized – heme on the cart wheels.)
182
What is tachyphylaxis?
Rapidly decreasing efficacy of a drug
183
What drug can you not co-administer with nitrates?
Sildenafil and other PDE-5 inhibitors
