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Pharmacology for Systems Flashcards

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1
Q

Hyperlipidemia: Statins inhibit _________ resulting in decreased synthesis of cholesterol and increased LDL receptor expression.

A

HMG coA reductase

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2
Q

Hyperlipidemia: Statins are metabolized by _____ enzymes and have a 2-3 hour 1/2 life. They peak in the _______.

A

Metabolized by CYP 3A enzymes

Peak in Evening

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3
Q

Hyperlipidemia: What are the side effects of statins?

A
  1. LIver toxicity
    (inc. ALT enzymes)
  2. Muscle
    (myalgia, myosisis, rhabdomyolisis)
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4
Q

Hyperlipidemia: What are contraindications of statins?

A
  1. erythromycin
  2. azoles
  3. anti-depressants
  4. HIV protease inhibitors
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5
Q

Hyperlipidemia: Bile acid binding resins include

  1. Colestipol
  2. Colestyramine
  3. Cholesevelam

What is their MOA?

A

Bind bile acids

  • -inhibiti bile acid resorption
  • -inc. cholesterol usage
  • -inc. LDL receptors
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6
Q

Hyperlipidemia: Bile acid binding resins are not metabolized in the gut. Because of this, when is it best to take them?

A

Before meals, bedtime

*oral

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7
Q

Hyperlipidemia: What is the main side effect of bile acid binding resins?

A

Constipation

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8
Q

Hyperlipidemia: What are contraindications of bile acid binding resins?

A

absorption of digoxin and TH

NOTE: bile acid binding resins most useful in patients who don’t tolerate other drugs

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9
Q

Hyperlipidemia: Ezetemibe inhibits ____ reabsorption in the small intestine (brush border). It increases HDL and lowers LDL and TG’s.

A

sterol reabsorption

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10
Q

Hyperlipidemia: How is ezetemibe metabolized?

A

conjugated with glucuronate

  • 80% excreted (feces)
  • can be used alone or combined with statin
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11
Q

Hyperlipidemia: Fibrates are taken orally to treat hypertriglyceridemia and in cases of low HDL.

What are its actions?

A

Binds PPAR-a receptor

Inc. Lipoprotein Lipase
Inc. HDL apoprotein

Thus, Dec. TG’s, Inc. VLDL clearance, Inc. HDL

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12
Q

Hyperlipidemia: What are the adverse effects of fibrates?

A

Myopathy, rhabdomyolisis, bone marrow

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13
Q

Hyperlipidemia: Niacin is used to treat hypercholesterolemia and hyper-TG-emia.

It acts to decrease TG’s and LDL by inhbiiting _____ from the liver. It also increases HDL and decreases lipolysis.

A

Inhibits VLDL from the liver

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14
Q

Hyperlipidemia: What are the adverse effects of Niacin?

a. cutaneous flushing
b. gastric irritation
c. myopathy
d. cough

A

A-C

*also glucose intolerance

Cx: diabetic patients

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15
Q

Hyperlipidemia: What drugs may be used to treat hypercholesterolemia and hyperTG?

A

statins + niacin

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16
Q

Thromboembolic drugs: Anti-coagulants act on coagulation factors.

Warfarin is an example. It is an oral drug that acts by inhibiting ______, preventing thrombin formation from prothrombin.

A

Inhibits Vit. K reductase

*CYP 450 metab.

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17
Q

Thromboembolic drugs: When does warfarin have its max effect on the system?

A

3-5 days after beginning treatment

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18
Q

Thromboembolic drugs: Heparin is given by I.V. It indirectly increases AT-III, which inhibits ___ and ____.

A

inhibits thrombin and Xa

NOTE: enox, dalte, fondaparinuz are subcutaneous

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19
Q

Thromboembolic drugs: Rivaroxaban (oral) and Bivalirudin (injection) are anti-coagulants that directly inhibit thrombin. What are their mechs of action?

A
  1. Rivaroxaban
    - -inhibits Xa
    - -similar to warfarin, less monitoring
  2. Bivalirudin
    - –inhibits thrombin
    - -coronary intervention or heparin-induced thrombocytopenia
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20
Q

Thromboembolic drugs: Anti-platelet drugs include:

  1. aspirin
  2. clopidogrel, prasugrel
  3. eptifibitide, tirofiban

Which of the above acts by decreases thromboxane a-2 by inhibiting COX-1?

A

Aspirin

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21
Q

Thromboembolic drugs: Anti-platelet drugs include:

  1. aspirin
  2. clopidogrel, prasugrel
  3. eptifibitide, tirofiban

Which of the above decreases GP receptors by inhibiting ADP (P2Y12)?

A

clopidogrel, prasugrel

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22
Q

Thromboembolic drugs: Anti-platelet drugs include:

  1. aspirin
  2. clopidogrel, prasugrel
  3. eptifibitide, tirofiban

Eptifibitide and Tirofiban act to decrease fibrinogen crosslinking by inhibiting ____ and ___.

A

inhibit GPIIb, IIIa

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23
Q

Thromboembolic drugs: Fibrinolytics function to lyse clots and increase plasmin.

True/False: Alteplase, Reteplase and Tenecteplase increase plasminogen (clot-bound).

A

True

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24
Q

Thromboembolic drugs: Fibrinolytics function to lyse clots and increase plasmin.

Streptokinase and Anistreplase play a role in non-specific plasminogen binding. What is an adverse effect?

A

Inc. risk of bleeding

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25
Thromboembolic drugs: Which of the following may be used for treatment of pulmonary embolism? a. heparin b. fibrinolytic c. aspirin d. clopidogrel/prasugrel
heparin and fibrinolytic
26
Thromboembolic drugs: Which of the following may be used for coronary angioplasty? a. LMW heparin b. bivalirudin c. eptibifitide d. aspirin e. clopidogrel
all of the above
27
Thromboembolic drugs: Which of the following may be used to treat unstable angina/non-STE ACS? a. aspirin b. LMW heparin c. clopidogrel d. eptifibitide
Al of the above
28
Thromboembolic drugs: Which of the following can be used to treat STEMI? a. fibrinolytic b. aspirin c. heparin d. Vit. K
A-C
29
Anti-arrhythmics: Class 1A (open channels) include the drugs: 1. Quinidine 2. Disopyramide 3. Procainamide _______ is used for life threatening arrhythmias. It restores normal sinus rhythm, and prolongs QT.
Quinidine *pregnancy ok
30
Anti-arrhythmics: Quinidine (class 1A) is used for life threattning arrhythmias. What are adverse effects of quinidine?
1. torsades 2. inc. digoxin 3. inc. mortality
31
Anti-arrhythmics: A class 1A drug that is given either IM or I.V. It can induce lupus like symptoms, but can be used in pregnancy.
Procainamide
32
Anti-arrhythmics: Class 1B drugs are "inactivated" channels. They include: 1. Mexilitine 2. Lidocaine ____ is used for acute ventricular arrhythmias. It can be used in pregnancy
Lidocaine * NOT 1st choice * heart block, bradycardia
33
Anti-arrhythmics: A class 1B drug that is used as long term prophylaxis
Mexilitine *oral
34
Anti-arrhythmics: Fleicanide is a class I C drug that is used for what?
Fetal SVT and Pregnancy
35
Anti-arrhythmics: What are adverse effects of FLeicanide?
Bronchospasm, Seizure
36
Anti-arrhythmics: Propafenone is a class 1C drug that has what adverse effects?
agranulocytosis, anemia
37
Anti-arrhythmics: Class III drugs are associated with K+ channels. They prolong effective refractory period. 1. Amiodarone 2. Ibutilide 3. Dofetilide What is a contraindication for CLass III drugs?
Pregnancy *amiodarone can in cases of life threatening arrhythmias
38
Anti-arrhythmics: Amiodarone (Class III) is a short term drug that can be administered either 1. oral (long term) 2. acute w/ epinephrine True/False: Amiodarone is the major form of treatment for torsade
False *NOT for torsade
39
Anti-arrhythmics: Adverse effects of amiodarone include a. blue-gray discoloration b. thyroid issues c. pulmonary fibrosis
all of the above
40
Anti-arrhythmics: This class III drug is administered via I.V. It is used to treat A-fib/flutter and torsades.
Ibutilide *significant patient harm
41
Anti-arrhythmics: This class III drug blocks IKr. It is NOT for use with QTc > 440.
Dofetilide * can treat torsade * must be titrated
42
Anti-arrhythmics: Sotalol is a class II/III drug that can be used to treat torsades. What are its contraindications?
Not for QTc > 440 *bronchospasm
43
Anti-arrhythmics: True/False - Beta blockers are the only drugs that decreased mortality in asymptomatic patients
true
44
Class IV drugs are calcium channel blockers. They block calcium channels in the heart and in SM, and prevent re-entry in the AV node. 1. Verapamil 2. Diazepam What are the most often used to treat?
SVT **
45
Anti-arrhythmics: Which of the class IV drugs is most often used in pregnancy?
Verapamil
46
Anti-arrhythmics: The number 1 drug for torsades
MgS
47
Anti-arrhythmics: This drug is a nucleoside that is adminstered as an IV bolus. It acts to convert paroxysmal supraventricular tachycardia
Adenosine
48
Anti-arrhythmics: Which of the following best describes digoxin? a. Na/K+ pump inhibitor b. + inotrope c. - chronotrope d. good for pregnancy
all of the above
49
Anti-arrhythmics: List the antiarrhythmics that can be used for pregnancy
Lidocaine Adenosine Verapamil Digoxin
50
Anti-arrhythmics: List the drugs that can be used to treat torsades
Quinidine SOtalol Ibutilide Dofetilide
51
Heart failure: List the drugs for Tx of angina
Nitrates, CCB (variant angina)
52
Heart failure: List the drugs used to decrease preload
Digoxin, ACE, ARBS, nitrates (low dose), diuretics
53
Heart failure: List the drugs used to decrease afterload
ACE/ARBs, CCB, Nitrates, Hydralazine, a-agonist
54
Heart failure: Positive inotropes include: 1. Digoxin 2. B-agonists 3. PDE-1 Digoxin acts by inhibiting _____, leading to increased free calcium and increased contractility of the heart.
inhibits Na/K pump * taper * doesn't dec. mortality
55
Heart failure: What are the adverse effects of digoxin?
Hyperkalemia-induce arrhythmia
56
Heart failure: B-agonists include dobutamine and dopamine. Which of the above is more specific for the B1 receptors?
Dobutamine B1 > B2 > a
57
Heart failure: True/False: Dopamine increases renal perfusion, but is nonspecific.
True D1 = D2 > B > a
58
Heart failure: PDE-I's include Milrinone. Milrinone acts to increase CAMP and contractility by inhibiting _____.
Inhibits PDE-3
59
Heart failure: What are adverse effects of Milrinone? What are contraindications?
Adverse: -nausea, vomiting CX; - -furosamide - -selenide - -selegiline
60
Heart failure: Non-positive inotropes include 1. Vasodilators 2. B-blockers 3. Diuretics List the vasodilators
1. ACE/ARBs 2. Hydralazine (arteriodilation) 3. Nitrates (nitroprusside; venodilation) 4. Neprilysin inhibitor (sacubitril + ARB)
61
Heart failure: ______ can be used to treat HF by acting as vasodilators. They decrease heart remodeling, wall thinning and overall morbidity.
ACE * inc. ventricular performance * cough; renal artery stenosis
62
Heart failure: Hydralazine is NOT for monotherapy. It is a direct vasodilator used MC for
acute HF
63
Heart failure: _______ like carvedilol and metoprolol decrease mortality with low dose. Must titrate up
B-blockers
64
Heart failure: Diuretics decrease edema and heart size without increasing the risk of arrhythmya. Spironolactone is often used for severe heart failure, however, it can cause what adverse side effect?
ototoxicity
65
Angina drugs: What is a useful drug for treating patients with aspirin sensitivity?
clopidogrel
66
Angina drugs: CCB's can be used in the treatment of angina. 1. DHP's decrease arterial tone and TPR. This helps to relieve wall tension and decrease O2 demand. 2. non-DHP's are good for the heart and vessels. They decerase heart rate and contractility. Which of the above is not approved for the treatment of HF?
non-DHP's
67
Angina: Nitrates are effective drugs for the treatment of angina. 1. _____ may be used as an immediate treatment for angina. It is administered sublingually.
Nitroglycerin - sublingual oral, buccal, transdermal - maintenance *don't give nitrates with viagra
68
Angina: B-blockers are effective for treating what type of angina?
stable * dec. HR, b.p, contractility * prevent reflex tachycardia carvedilol, labetalol, metoprolol
69
Angina: Last choice therapy for treating angina. It inhibits Na influx
Ranolazine
70
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