Antihyperlipidimia Drugs Flashcards
(7 cards)
Statins
Are HMG-COA Reductase inhibitor
Atorvastatin
Simvastatin
Lovastatin…
MOA- inhibit el limiting step of cholesterol synthesis. Liver reuptake the cholesterol from blood
Drug interactions- inhibitor p450, grape juice, red yeast rice
Adverse effects- myalgia
Myositis
Risk with gemfibrozil and nicotinic acid
Elevates 3x AST discontinue
Colestipol
Cholestyramine
Colesevelam
Bile acids sequestrans
MOA- bind to the bile acid in GI and forms an insoluble complex that is excreted in feces
Contraindicated-
Hypertriglyceridemia, because they increase the VLDL and TG
Adverse effect-
Fat malabsorption and malabsorption of fat vit ADEK
Cholestyramine is used in Pruritis due to biliary obstruction as the liver cannot eliminate bile.
Nicotinic acid - niacine
For lipid lower effects
Is given in a more higher dose than as vitamin
Inhibits hepatic production of VLDL ( precursor for LDL)
Increases HDL by delaying the clearance
Increases lipoprotein lipase activity ( degrades TG)
Adverse effect
Flushing
Pruritis
Paresthesia
Nausea
Pretreatment with aspiring lowers side effects
Hyperuricemia - risk to gout (similar to Pyrazinamide from RIPE)
Fibrates
For more than >500 mg of cholesterol. If LDL is less tan 500 better give statins
Fenofibrate and Gemfibrozil
PPARA-alpha (Peroxisome proliferator- activated receptor alpha agonist.
They regulate gene transcription controlling carbohydrate and fat metabolism.
Activate Lipoprotein lipase ( like Nicotinic acid)
Decrease VDL, TG and LDL
Mildly increase HDL
Indicated in treatment for Hyperlipidemia ( unlike Bile acids sequestrans)
Adverse effects:
1. Myositis when combined with statins
2. Hepatitis
3. Cholelithiasis ( gall stones)
Ezetimibe
Cholesterol uptake inhibitor
If we cannot lower the LDL with statins we give Ezetimibe
Inhibits the absorption of dietary and biliary cholesterol at the intestine. Inhibits Niemann Pick C1 like protein ( cholesterol transporter)
Used with statins to reach the LDL goal in patients with MI. Vytorin is the drug
Adverse:
Headache
Myalgia
Sinusitis
Pharyngitis
Mipomersen
Antisense oligonucleotide against Apo B-100 mRNA (Protein involve in the formation of LDL )
FDA approved fro homozygous familiar hypercholesterolemia
Given weekly by Subcutaneous injection
Adverse:
Hepatic fat accumulation
PCSK9 inhibitors
Evolocumab
Alirocumab
MOA:
Inhibits PCSK9 proprotein convertase subtilizing Kexin type 9
Decrease recycling of LDL
Indicated in heterozygous familiar hypercholesterolemia for those who cannot use statins
adverse:
hypersensitivity reaction
ALT and AST increased
MSK pain
