Hyperlipidemia/Hypertriglyceridemia Flashcards
“-Statin” drug route/MoA
- PO
- MoA: inhibits HMG CoA reductase –> less cholesterol in liver –> increased removal of LDL from blood into liver
“-Statin” drug indications
- homo/heterozygous high cholesterol
- PRIMARY prevention of cardiovascular events
- ex. atorvaSTATIN, simvaSTATIN, rosuvaSTATIN
1ST LINE
“-Statin” AEs
- Common: arthralgia/myopathy/myositis
- Less: hepatitis/jaundice
- Significant: rhabdomyolysis, hepatic failure (rare)
Ezetimibe route/MoA
- PO
- MOA: blocks transport of cholesterol from intestine to liver –> increase of LDL receptors on liver –>more LDL removed from circulation
Ezetimibe indications
- homozygous high chol.
- PRIMARY high cholesterol
- off label: secondary prevention of cardiovascular events
ADJUNCTIVE to -statins or can also be used alone
Ezetimibe D-D interactions
- Fibrates –> avoid combination
- Bile acid sequestrants –> impaired absorption
- cyclosporine
- Warfarin –> possible increase of INR
Ezetimibe AEs
- Common: Diarrhea, Myalgia, resp infection
- Less: elevated AST/ALT
- Sig: rhabdomyolysis, pancreatitis, cholecystitis, anaphylaxis
PCSK9 Inhibitor drug types (2)
- monoclonal antibodies: AlirocuMAB
EvolocuMAB
& - RNA type
Inclisiran
PCSK9 Inhibitors route/MoA (-MABs)
- SubQ
- blocks PCSK9 from degrading LDL receptors –> more LDL receptors to clear LDL from bloodstream
PCSK9 Inhibitors route/MoA (inclisiran)
-SQ
- blocks mRNA that encodes for PCSK9 production –> less PCSK9 = more LDL receptors –> more LDL removed from circulation
PCSK9 Inhibitors Indications
- Homozygous familial high chol.(-MABs)
- heterzygous (RNA)
- primary hyperchol. (-MABs)
- secondary prevention of cardiovascular events
- ADJUNCTIVE after statins/ezetimibe stop working
PCSK9 Inhibitor AEs
- common: injection site reaction
- Less: liver disorder
- Sig: hypersensitivity, angioedema
ATP Citrate Lyase (ACL) inhibitor drug/route/MoA
- Drug: Bempedoic Acid
- route: PO
- MoA: activated in liver; inhibits cholesterol synthesis in liver –> increase in LDL receptor –> increase clearance of LDL from circulation
ACL inhibitor indication
- heterozygous familial chol
- atherosclerotic CVD
-ADJUNCTIVE when -statins/ezetimibe stops working
ACL inhibitor AEs
do not use if pregnant
- Common: gout, hyperuricemia
- Less: liver disorder, BPH in men
- Sig: tendon rupture, A-fib, anemia/thrombocytopenia
Bile Acid Sequestrants route/MoA
- PO
- MoA: promotes bile excretion in feces–> decreased bile acid availability–> increased uptake of LDL to liver, less in circulation
Bile Acid Sequestrants Drug & indication
- Colesevelam
- Heterozygous familial high chol.
- atherosclerotic CVD
- ADJUNCTIVE when -statins and ezetimibe stop working
Bile Acid Sequestrants AEs
- Common: “belly effects” abd pain; constipation, N/V
- Less: vitamin A, D, E, K deficiency
- Sig: hyper-triglyceridemia, pancreatitis, gallbladder calculi
Contraindications of Bile Acid Sequestrants (colesevelam)
- when TG > 500
- if hx of pancreatitis caused by high TG
- bowel obstruction
Fibric Acid derivatives Inidications
- hypertriglyceridemia
- prevention of CVD
- ADJUNCTIVE/alternate to omega 3; also if TGs>500
Fibric Acid derivatives (drugs/route/MoA)
- Gemfibrozil/fenofibrate
- PO
- MoA: activates PPAR-alpha –> more LPL (lipoprotein lipase) –> less fatty acids available in liver to release triglycerides
Contraindications of Fibric acid derivative
- severe renal impairment
- active liver dx
- gallstones
- breast feeding
Fibric Acid derivative SEs
- Common: abdominal pain; N/V/D; dyspepsia; rash/itching; mylagia; increased liver enzymes
- Less: photosensitivity
- Sig: rhabdomyolysis; delayed hypersensitivity
VLDL Synthesis Inhibitors indications
- CV risk reduction with hypertriglyceridemia
- ADJUNCTIVE if statins stop working; also for CVD/DM
VLDL synthesis inhibitors (drugs/route/MoA)
- omega 3/fish oil & icosapent ethyl
- PO
- MoA: inhibition of acyl-CoA –> decreased triglyceride synthesis –> decreased VLDL –> decreased LDL mediated plaque formation
Omega 3 AEs
- common: eructation/dypepsia
- Less: skin rash, increase liver enzymes
- Sig: bleeding tendency disorder; A-fib/A-flutter
Microsomal TG transfer protein (MTP) inhibitor indication
- homozygous familial high chol.
- ADJUNCTIVE to other cholesterol lowering meds, when statins stop working
- only if high chol. is their only condition
MTP inhibitor drug/route/MoA
- Lomitapide
- PO
- MoA: binds MTP in liver & intestine –> blocks transport/formation of VLDL/chylomicron particles –> decrease level of both in blood stream –> decreased LDL formation
MTP inhibitor (lopitamide) AEs
- major GI issues (abd distension, constipation, D/N/V)
- Increased liver enzymes –> additional hepatic lab monitoring required
Angiopoietin-Like Protein 3 (ANGPTL3) inhibitor indication
- Homozygous familial high cholesterol
- ADJUNCTIVE to other LDL lowering meds
(ANGPTL3) inhibitor drug/route/MoA
- Evinacumab
- route: IV
- MoA: inhibits ANGPTL3 –> promotes clearance of VLDL remnants before they are metabolized to LDL
(ANGPTL3) inhibitor AEs
- infusion related rxns
- hypersensitivity/anaphylaxis
- also respiratory infections, GI issues, dizziness, limb pain
- avoid pregnancy during use and for 5 months after last admin
