Treatment Of Hyperlipidemias

Front 1

Type I Hyperlipidemia

Back 1

Deficiency in Lipoprotein Lipase

Increased Chylomicrons

TREAT: Niacin + Fibrate

Front 2

Type IIA Hyperlipidemia

Back 2

Defect in the synthesis or processing of LDL receptors

Increase in LDL

Ischemic Heart disease is accelerated

TREAT: Niacin + Statin + Ezetimibe

Front 3

Type IIB Hyperlipidemia

Back 3

Overproduction of VLDL by the liver

Increase in VLDL and LDL

TREAT: Restriction of Cholesterol

Front 4

Type III Hyperlipidemia

Back 4

Overproduction or underutilization of IDL

Mutant ApoE

Increased IDL

Xanthomas, Accelerated vascular disease

Middle Aged

Front 5

Type IV Hyperlipidemia

Back 5

Overproduction or decreased removal of VLDL and TG in serum

Increased VLDL

Seen in obese, diabetic and hyperuricemic

Front 6

Type V Hyperlipidemia

Back 6

Increased Production of Decreased Clearance of VLDL and Chylomicrons

Genetic Defect

Adults with obesity and/or Diabetes

Front 7

FIBRATES

Gemofibrozil, Fenofibrate, Clofibrate

MOA

Back 7

Activate PPARs to bind to fatty acids and increase expression of LPL leading to a decrease in Triglycerides

*Increase expression of ApoAII leading to an increase in HDL

Front 8

Fibrates are used to treat...

Back 8

Hyperlipidemias Types III, IV, and V

Front 9

Fibrate Adverse Effects

Back 9

GI: Mild GI Disturbance

Biliary: Increased incidence of gallstones

Front 10

Fibrate Drug-Drug Interactions and Contraindications

Back 10

Potentiates warfarin and coumarin

Can displace acidic drugs as it is converted to an acid metabolite

Contraindicated in those predisposed to gallstones and those with liver/ renal disease

Front 11

Bile Acid Binding Resins

Cholestyramine and Colesevelam

MOA

Back 11

Drugs bind negatively charged bile acids which are then excreted in the feces.

The decrease in [bile acid] causes hepatocytes to convert cholesterol to bile acids.

This causes a decrease in intracellular [cholesterol], leading to an increased hepatic uptake of LDL (they have cholesterol in them), thus reducing the plasma [LDL]

Front 12

Bile Acid Binding Resins are used to treat...

Back 12

Type IIA and IIB Hyperlipidemia

Cholestyramine - Pruitus

Colesevelam - Diabetes Type 2

Front 13

Bile Acid Binding Resins Adverse Effects and Contraindications

Back 13

GI: Constipation, Nausea, Flatulence

Impair the absorption of fat soluble vitamins (ADEK)

Contraindicated in pregnancy/ nursing, hepatic/renal dysfunction, elevated TG

Front 14

Cholesterol Absorption Inhibitor
Ezetimibe

MOA

Back 14

Selectively inhibits the absorption of dietary and biliary cholesterol in the small intestine

Decreases LDL

Often used with Statins to increase LDL removal

Front 15

Ezetimibe Adverse Effects and Contraindications

Back 15

DO NOT co-administer with Bile Acid Resins

Can causes GI distress, headache

Front 16

HMG-CoA Reductase Inhibitors

Statin Drugs

MOA

Back 16

Inhibit HMG-CoA Reductase (no de novo synthesis of cholesterol)

Cause an increase in cell surface LDL receptors

Reduction in plasma cholesterol and TGs

Front 17

Beneficial Effects of Statin Drugs

Back 17

Enhance endothelial production of NO

Increase plaque stability

Decrease platelet aggregation

Reduce lipoprotein oxidation

Front 18

Metabolism of Statins

Back 18

CYPT3A4 - Lovostatin, Simvastatin, Atorvostatin

CYP2C9 - Fluvastatin and Rosuvastatin

Front 19

Therapeutic Uses of Statin Drugs

Back 19

Prevent Cardiovascular Disease

Treat dyslipidemias and hyperlipidemias (all types)

Front 20

Statin Drugs Adverse Effects and Contraindications

Back 20

MUST ASSES LIVER FUNCTION

Myopathy/ Rhabomyolosis

Renal Insufficiency

SLE like syndrome

Contraindicated in Pregnancy/Nursing, teens and children, those with liver disease

Front 21

Statin Drug-Drug Interactions

Back 21

Increases Coumarin and Warfarin (monitor clotting time)

Amiodarone, Amlodipone and Ranolazine

Front 22

Drugs that Inhibit Statins

Back 22

Cyclosporine, AZOLES, HIV protease inhibitors (-AVIR), Cimetidine, Erythromycin, Verapamil

Front 23

Drugs that Stimulate Statins

Back 23

Phenytoin, Griseofulvin, Barbituates, Rifampin, Thiazolidionediones

Front 24

Niacin MOA

Back 24

Inhibits lipolysis in adipose tissue. This leads to a decrease in VLDL and LDL synthesis

Inhibits apoprotein synthesis

Enhances VLDL clearance

Increases tPA

Decreases Fibrinogen

Front 25

Niacin Therapeutic Uses

Back 25

Combined with other drugs to treat dyslipidemias

Used to decrease TG

Peripheral Vascular Disease

Pellagra

Front 26

Niacin Adverse Effects and Contraindications

Back 26

Cutaneous Flush and Pruitus, Nausea and -pain, Impaired Glucose tolerance, Gout

Contraindicated in those with liver disease, peptic ulcers, arterial bleeding

Front 27

Rimonabant

MOA, Side Effects and Contraindications

Back 27

MOA: Modulates glucose tolerance and increases HDL; Decreases TGs

Side Effects: GI, headache, dizziness, anxiety

Contraindications: Depression

Front 28

Orlistat

Back 28

Inhibits Pancreatic and Gastric Lipase enzymes; Decrease fat absorption, LDL, cholesterol and TG; Increase HDL

Front 29

Sibrutamine

Back 29

Monoamine Reuptake Inhibitor;

Increases HDL, Decreases TG

Front 30

Omega 3 Fatty Acids

Back 30

Treat Increased TGs, Type III and IV H

Front 31

Plant Sterols

Back 31

Reduce LDL

Front 32

Combination Therapy: decrease LDL

Back 32

Statin + Ezetimibe

Statin + Bile Acid Resin

Bile Acid Resin + Ezetimibe

Front 33

Combination Therapy: raise HDL

Back 33

Statin + Niacin

Statin + Fibrate

Front 34

Probucol

Back 34

Prolongs QT Interval

Causes GI disturbances and Digitalis