Pharmacology for Systems Flashcards
Hyperlipidemia: Statins inhibit _________ resulting in decreased synthesis of cholesterol and increased LDL receptor expression.
HMG coA reductase
Hyperlipidemia: Statins are metabolized by _____ enzymes and have a 2-3 hour 1/2 life. They peak in the _______.
Metabolized by CYP 3A enzymes
Peak in Evening
Hyperlipidemia: What are the side effects of statins?
- LIver toxicity
(inc. ALT enzymes) - Muscle
(myalgia, myosisis, rhabdomyolisis)
Hyperlipidemia: What are contraindications of statins?
- erythromycin
- azoles
- anti-depressants
- HIV protease inhibitors
Hyperlipidemia: Bile acid binding resins include
- Colestipol
- Colestyramine
- Cholesevelam
What is their MOA?
Bind bile acids
- -inhibiti bile acid resorption
- -inc. cholesterol usage
- -inc. LDL receptors
Hyperlipidemia: Bile acid binding resins are not metabolized in the gut. Because of this, when is it best to take them?
Before meals, bedtime
*oral
Hyperlipidemia: What is the main side effect of bile acid binding resins?
Constipation
Hyperlipidemia: What are contraindications of bile acid binding resins?
absorption of digoxin and TH
NOTE: bile acid binding resins most useful in patients who don’t tolerate other drugs
Hyperlipidemia: Ezetemibe inhibits ____ reabsorption in the small intestine (brush border). It increases HDL and lowers LDL and TG’s.
sterol reabsorption
Hyperlipidemia: How is ezetemibe metabolized?
conjugated with glucuronate
- 80% excreted (feces)
- can be used alone or combined with statin
Hyperlipidemia: Fibrates are taken orally to treat hypertriglyceridemia and in cases of low HDL.
What are its actions?
Binds PPAR-a receptor
Inc. Lipoprotein Lipase
Inc. HDL apoprotein
Thus, Dec. TG’s, Inc. VLDL clearance, Inc. HDL
Hyperlipidemia: What are the adverse effects of fibrates?
Myopathy, rhabdomyolisis, bone marrow
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.
Inhibits VLDL from the liver
Hyperlipidemia: What are the adverse effects of Niacin?
a. cutaneous flushing
b. gastric irritation
c. myopathy
d. cough
A-C
*also glucose intolerance
Cx: diabetic patients
Hyperlipidemia: What drugs may be used to treat hypercholesterolemia and hyperTG?
statins + niacin
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.
Inhibits Vit. K reductase
*CYP 450 metab.
Thromboembolic drugs: When does warfarin have its max effect on the system?
3-5 days after beginning treatment
Thromboembolic drugs: Heparin is given by I.V. It indirectly increases AT-III, which inhibits ___ and ____.
inhibits thrombin and Xa
NOTE: enox, dalte, fondaparinuz are subcutaneous
Thromboembolic drugs: Rivaroxaban (oral) and Bivalirudin (injection) are anti-coagulants that directly inhibit thrombin. What are their mechs of action?
- Rivaroxaban
- -inhibits Xa
- -similar to warfarin, less monitoring - Bivalirudin
- –inhibits thrombin
- -coronary intervention or heparin-induced thrombocytopenia
Thromboembolic drugs: Anti-platelet drugs include:
- aspirin
- clopidogrel, prasugrel
- eptifibitide, tirofiban
Which of the above acts by decreases thromboxane a-2 by inhibiting COX-1?
Aspirin
Thromboembolic drugs: Anti-platelet drugs include:
- aspirin
- clopidogrel, prasugrel
- eptifibitide, tirofiban
Which of the above decreases GP receptors by inhibiting ADP (P2Y12)?
clopidogrel, prasugrel
Thromboembolic drugs: Anti-platelet drugs include:
- aspirin
- clopidogrel, prasugrel
- eptifibitide, tirofiban
Eptifibitide and Tirofiban act to decrease fibrinogen crosslinking by inhibiting ____ and ___.
inhibit GPIIb, IIIa
Thromboembolic drugs: Fibrinolytics function to lyse clots and increase plasmin.
True/False: Alteplase, Reteplase and Tenecteplase increase plasminogen (clot-bound).
True
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?
Inc. risk of bleeding
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
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
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
Thromboembolic drugs: Which of the following can be used to treat STEMI?
a. fibrinolytic
b. aspirin
c. heparin
d. Vit. K
A-C