HYPOLIPIDEMIC DRUGS

EZETIMIBE

1. IN FOOD WE CONSUME CHOLESTEROL AND TG

2. IT IS ABSORBED IN INTESTINE, TAKEN BY LACTEALS

3. FROM LACTEALS CHOLESTEROL AND TG TAKEN THROUGH THORACIC DUCT TO BLOOD VESSEL WITH HELP OF CHYLOMICRONS

4. IN BLOOD VESSEL ,

LIPO PROTEIN LIPASE

TG FATTY ACID + GLYCEROL

FATTY ACID TAKEN UP BY ADIPOSE CELLS AND GETS CONVERTED TO TG AGAIN

FIBRATES

5. REMANANT CHYLOMICRON ENTERS THE LIVER

6. LIVER SECRETE TG AND CHOLESTEROL INTO BLOOD VESSEL AS VLDL

7. THIS TG AGAIN GETS METABOLISED IN BLOOD VESSEL BY LPL

8. THUS NOW VLDL NOW CHANGES TO IDL

TAKEN BACK TO LIVER

IDL CONVERSION TO LDL CONTAINING ONLY CHOLESTEROL AND DISTRIBUTED TO VARIOUS TISSUE

LPL

9. HDL CARRIES CHOLESTEROL FROM PERIPHERY TO LIVER

10.CHOLESTEROL IS EXCRETED IN BILE IN FREE FORM AND AS BILE SALTS

11.BILE SALTS UNDERGO ENTEROHEPATIC CIRCULATION BILE ACID

BINDING RESINS

• STATINS – INHIBIT HMG CO-A

• NIACIN – INHIBIT LIPOLYSIS IN ADIPOSE TISSUE .

DRUGS

• STATINS ( LDL )

• BILE ACID BINDING RESINS

• INTESTINAL CHOLESTEROL ABSORPTION INHIBITORS - EZETIMIBE

• FIBRATES (TG)

• NIACIN (HDL)

HYPER LIPOPROTEINEMIA

• PRIMARY

• SECONDARY

TYPE 1 – FAMILIAL LIPOPROTEIN LIPASE DEFICIENCY

TYPE 2A – FAMILIAL HYPER- LDL

CHOLESTROLEMIA

TYPE 2B – FAMILIAL COMBINED- VLDL , LDL

HYPERLIPIDEMIA

TYPE 3 – FAMILIAL DYSBETA- MutationLIPOPROTEINEMIA

TYPE 4 –FAMILIAL VLDL

HYPERTRIGLYCERIDEMIA

TYPE 5 – FAMILIAL MIXED VLDL , CM

HYPERTRIGLYCERIDEMIA

STATINS

• MECHANISM

• DRUGS – PRAVASTATIN , ATORVASTATIN

• PHARMACOKINETICS – ORALLY, M-LIVER ,

E- KIDNEY

• USES – PLEOTROPIC EFFECT , PRAVASTATIN FIBRINOGEN LEVEL

• A/E – HEPATOTOXITY , MYOPATHY AND RABDOMYOLYSIS ( PRAVASTATIN )

BILE ACID BINDING RESINS

• MECHANISM

• DRUGS – CHOLESTYRAMINE , COLESTIPOL

• PHARMACOKINETICS – ORALLY , EXCRETED IN FAECES

• A/E- FLATULENCE AND CONSTIPATION

INTESTINAL CHOLESTEROL ABSORPTION INHIBITOR

• MECHANISM

• DRUGS - EZETIMIBE

• PHARMACOKINETICS – ORALLY , EXCRETED IN BILE

FIBRATES• MECHANISM

• DRUGS – GEMFIBROZIL , FENOFIBRATE

• PHARMACOKINETICS – ORALLY , M- LIVER , E –URINE

• USE –FIBRATES PLASMA FIBRINOGEN , HYPERURICEMIA

• A/E – MYOPATHY

NIACIN

• MECHANISM

• PHARMACOKINETICS – ORALLY , M- LIVER ,E -URINE

• A/E – FLUSHING , HYPERURICEMIA , HEPATOTOXITY

THANKYOU…..