Lipid and Ischemic Heart Disease (Week 7) Drugs Flashcards
1
Q
Atorvastatin
Lovastatin
Simvastation
A
HMGCoA Reductase Inhibitor (Statin) --/RDS of choles synth ^ LDL-R expression (PK)-oral 1st pass OAT-P1B1/ CYP3A4 (X) 1st line hyperCHOL (O) CYP3A4, SLCO1B1 mut (-1) GI (-2) Myopathy (-3) rhabdomyolysis> kidney damage
2
Q
Cholestyramine
A
Bile-Acid Binding Resin ^ liver 7-a-hydroxylase= ^ HMGCOreductase+ ^^LDL-R (PK) IV admin (NOT ABS- POS charge) (X) 2nd agent + statin= hyperCHOL (O) hyperTG (^ TG transient) (-1) constipation, bloat (-2) steatorrhea (-3) ^Cl- abs and reduced abs drugs
3
Q
Niacin
A
vitB2 Complex vitamin
(adipose) inhib FFA mobil
(liver) reduce VLDL-TG synth
inhib HDL:apoA1 uptake
(PK) oral, immediate release, long act, extended
(X) 2nd line for HyperCHOL and hyperTG (^ LDL, low HDL)
(O) gout, diabetes, peptic ulcer, hepatic disease, statins
(-1) cutaneous flush/pruritis
(-2) GI
(-3) liver enz
4
Q
Ezetimibe
A
Cholesterol abs inhibitor --/NPC1L1 (chol abs in intestine) (PK) oral glucuronidation> active* (X) 1o hyperCHOL + statin (+) well tolerated
5
Q
Gemfibrozil
Fenofibrate*
A
Fibrates/ PPAR activator activate PPAR*/RXR--> gene transcrip -^ LDL particle size -^ HDL synth ^ reverse chol transcrip -reduce TG + inflam (PK) Fenofibrate*> Gemfibrozil (X) hyperTG + low HDL (X) metabolic syndrome, tII diab (O) statins (^ renal damage) (O) renal impariement (-1) GI (-2) Gall stones
6
Q
Omega 3 FA
A
HyperTG inhibit lipogenesis (DGAT, LA, HSLipase)= reduce VLDL (-1) ^ LDL (-2) ^ liver enzyme (-3) bleeding (X) + hyperTG tx w TG>500mg/dL (+) reduce fatal arrhythmias, plaque stability, reduce HR, ^ endo funct (O) fish allergy
7
Q
PCSK9 inhibitor
A
HyperCHOL
^ recycling of LDLr
^ removal of LDL from bs
8
Q
Microsomal Triglyceride Transfer Protein (MTP) Inhibitor
A
HyperCHOL prevent apoB-TG lipoprotein synthesis =reduce chylomycrons and VLDL (= reduce LDL) (PK) oral, CYP3A4 (X) homo fam hyperCHOL (-1) GI (-2) hepatotoxic
9
Q
apoB-100 Inhibitor
A
HyperCHOL bind apoB100 mRNA> recruit RNAseH--> digested (PK) sub Q injection 1/week (X) homo fam hyperCHOL (-1) injection site rxn (-2) flu-like sxs (anti Ab) (-3) headache (-4) ^^liver enzymes
10
Q
NItroglycerin
A
Nitrate of IsHD venous vasodilator NO--> GC- -> cGMP--> PKG --reduce O2 demand (PK) sublingual (avoid 1st pass) (X) Acute Angina (-) Tolerance --small dose, nitrate-free period (-) CV effects: headache, hypOtension, reflex tachy, flushing
11
Q
Isosorbide Dinitrate
A
NItrate of IsHD venous vasodilator NO--> GC- -> cGMP--> PKG --reduce O2 demand (PK) metab to active mono* (X) chronic angina (-) Tolerance --small dose, nitrate-free period (-) CV effects: headache, hypOtension, reflex tachy, flushing
12
Q
Isosorbide Mononitrate*
A
Nitrate of IsHD venous vasodilator NO--> GC- -> cGMP--> PKG --reduce O2 demand (PK) t 1/2 ~ 5hrs (X) chronic angina (-) Tolerance --small dose, nitrate-free period (-) CV effects: headache, hypOtension, reflex tachy, flushing
13
Q
Propranolol
A
non-specific B blocker reduce O2 demand -reduce hr -reduce cntxn -reduce bp ^ time in diastole= ^ coronary perf (O) vasospasm (prinzmetal) obstructive airway disease bradycardia/block insulin-treated diabetes (-1) fatigue (-2) sexual dysc (-3) ^^ wall tension* (+) use + niacin
14
Q
Timolol
A
non-specific B blocker reduce O2 demand -reduce hr -reduce cntxn -reduce bp ^ time in diastole= ^ coronary perf (O) vasospasm (prinzmetal) obstructive airway disease bradycardia/block insulin-treated diabetes (-1) fatigue (-2) sexual dysc (-3) ^^ wall tension* (+) use + niacin
15
Q
Carvediol
A
non-specific B blocker reduce O2 demand -reduce hr -reduce cntxn -reduce bp ^ time in diastole= ^ coronary perf (O) vasospasm (prinzmetal) obstructive airway disease bradycardia/block insulin-treated diabetes (-1) fatigue (-2) sexual dysc (-3) ^^ wall tension* (+) use + niacin