HYPERLIPIDEMIA - CARDIOVASCULAR DRUG (PART 6B / 7) | PHARMACOLOGY REVIEW

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 HMG CoA Reductase Inhibitors (Statins) 

3-Hydroxy-3-MethylGlutryl-Coenzyme A reductase inhibitors lower LDL Cholesterol level..Rate limiting step Cholesterol synthesis

MOA=Statin inhibit HMG Co A reductase ...which convert HMG CoA into Mevalonic Acid which convert into Cholesterol…decrease conc. Of Cholesterol within cell

Cardiovascular drugs, hyperlipidemia drug screening test and interview


Low intracellular Cholesterol stimulate synthesis of LDL receptor…Increased LDL receptor promote uptake of LDL from blood

Low intracellular Cholesterol decrease Secretion of VLDL

Increase plasma HDL level

T.E= All types of Hyperlipidemia…..Familial Hypercholeserolemia lack LDL receptor so benefit less

S.E=myopathies, rhabdomylysis, increase LFT, t1/2 1.5-2hr...Lova & Simva prodrug

Contraindicated in pregnancy & lactation, teenage & children…

Niacin (Nicotinic acid)

 reduce LDL(Bad cholesterol), increase HDL(good  cholesterol )

MOA=inhibit Lipolysis in Adipose tissue…decrease level of Free Fatty Acids..liver use these Free Fatty Acid for Triglycerol synthesis…Tg convert into VLDL-LDL..Decrease level of VLDL and LDL…

Boost secretion of tPA & lower plasma Fibrinogen …decrease thrombus associated with Hypercholestrolemia & Atherosclerosis

T.E= used in Familial Hyperlipidemia...niacin metabolize into Nicatinamide,cofactor in NAD+…

S.E= Cutaneous flush...Pruritis...Impaired Glucose Intolerance, Hepatotoxicity…it inhibits tubular secretions of Uric acid so lead to Gout & Hyperuricemia…

Fibrates

Finofibrate & Gemfibrozil= finofibrate more effectiveMOA=bind to PPARs lead to decreased Gene expression of TG….increase expression of Lipoprotein Lipase….decrease Apolipoprotein CII…increase HDL level..

T.E= used in HyperTriacylGlycerolemia, type lll hyperlipidemia….fenofibrate prodrug 

S.E= GIT disturbance, Lithiasis (Gall stone), myoscitis ….interact with Anticoagulant increase INR …contra in Pregnancy, lactation, hepatic, renal dysfunction, in gall bladder disease 

Bile Acid Sequestrant (Resin) 

significant lower LDL 

MOA= Cholestyramine, Colesevelam, Colestipol anionic exchange-resin…bind –vely charged Bile Acid & Bile Salts…..this complex excrete in feces...preventing Bile Acid from returning into Liver...lower Bile Acid conc. Liverincrease conversion of Cholestrol into Bile Acid….decrease Cholesterol & LDL

T.E= Type llA & Type llB Hyperlipidemia….Cholestyramine used to treat Diarrhea & pruritis caused by Accumulation of bile acid 

S.E= Constipation, impaired absorption of Vitamin (A,D,E,K)…

Cholesterol Absorption Inhibitor 

Ezetimibe= selectively inhibit absorption of Dietery & Biliary Cholesterol in Small intestine…..decrease hepatic cholesterol...increase clearance of cholesterol from blood 

Interact with abs. of vitamins


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