Lipid Drugs

Question 1

Statins

Answer 1

Atorvastatin, Rosuvastatin, Simvastatin, Pravastatin

HMGCoA-Reductase inhibitors in the LIVER that will increase LDL receptors and liver clearance of LDL; take effect in two weeks and also increase HDL

ADRs: Elevated ALT/AST (monitor); Myalgia (Increased CK), especially w/ gemfibrozil, nicotinic acid

CIs: Pregnancy, Liver Disease, Nursing Mothers

Question 2

Simvastatin induced muscle pain

Answer 2

Assoc. w/ CYP2D6*4 allele; will see a huge increase in CK

-Patient can still take it just try a lower dose first before removing it

Question 3

Statins that also decrease TGL levels

Answer 3

Atorvastatin and Rosuvastatin

-Strongest statins that also pick up some IDL due to the dramatic increase in LDL receptors on the liver

Question 4

CYP3A4 inhibiting statins

Answer 4

Atorvastatin, lovastatin, and simvastatin

-Also should avoid grapefruit juice

Question 5

Statins approved for use in kids >8

Answer 5

Pravastatin

Question 6

Ezetimibe

Answer 6

Inhibits dietary cholesterol absorption at the brush membrane of the intestine (NPC1L1)

***Much better reduction in cholesterol levels when combined w/ a statin

Question 7

PCSK9 inhibitors

Answer 7

Alirocumab, Evolumab

Injected drugs that inhibit the function of PCSK9, a protein involved in the degradation of LDL receptors in the liver

-VERY USEFUL DRUG

Question 8

Resins

Answer 8

Cholestyramine, Colestipol

These drugs are never absorbed and bind to bile acids in the intestines; this causes an increased secretion of bile and increased formation of bile from cholesterol due to disinhibition of 7a-hydroxylase
=»Increased LDL receptors on the liver

-Often combined w/ statins, ezetimibe, or fibrinates for maximum effect; can be used in pregnant women

ADRs: Bloating, constipation

*Will also decrease absorption of fat-soluble vitamins and some medications (valproic acid) so take 1 hr before or 4hr after resin

Question 9

Fibrates

Answer 9

Gemfibrozil, Clofibrate, Fenofibrate

PPARa induces that increase LPL activity (decrease APO CIII which inhibits LPL), increase FA oxidation, and decrease hepatic VLDL production

ADRs: Gallstones (clofibrate); Gemfibrozil inhibits OATP2 causing an increased risk of myopathy w/ atorvastatin, rosuvastatin, pravastatin

Question 10

Nicotinic Acid

Answer 10

Decreases production of hepatic VLDL, inhibits lipolysis to decrease delivery of FFAs to the liver, and ***inhibits HORMONE-SENSITIVE lipase in fat cells (other LPL is increased)

=»Lower TGLs and cholesterol

ADRs: SEVERE itching, flushing (give aspirin before) and rash; elevated AST/ALT; possible myalgia w/ statins, ****PPT. PEPTIC ULCERS
HyperuricemiA and WORSENS GLUCOSE INTOLERANCE

CIs: Peptic ulcer disease, Active bleeding disorder, liver disease

Question 11

Tx for Hyperchylomicronemia

Answer 11

DIET; secondary would be fibrates and nicotinic acid

Pt. has elevated chylomicrons and TGLs after fast due to defect in LPL activity and or in Apo C-II

Question 12

Tx for Familial Hypercholesterolemia

Answer 12

Statins, ezetimibe, resins

-Pt. has elevated LDL and cholesterol and at risk for CVD

Question 13

Familial Combined Betalipoproteinemia

Answer 13

Statins

-Pt. has elevated VLDL and LDL

Question 14

Tx for Familial Dysbetalipoproteinemia

Answer 14

Very successful tx w/ fibrates

Increased TGLs and cholesterol due to abnormal Apo-E

Pt. also has increased IDL due to decreased catabolism of VLDL

Question 15

Familial Hypertriglyceridemia

Answer 15

Treat ONLY W/ FIBRATES

-Pts. may have hyperuricemia which could be worsened by Nicotinic acid

Question 16

Secondary drugs that can elevate lipids

Answer 16

Thiazide diuretics

B-blockers

Contraceptives