Anti-Lipid Drugs Flashcards
role of HMG CoA reductase inhibitors
- block the synthesis of cholesterol - increase the uptake of LDL
pharmacokinetics issues with BABAs
- daily doses are in grams (huge) - alternate to statins during pregnancy - can be used with statins
HMG CoA reductase inhibitors role with nitric oxide
- increase endothelial nitric oxide production - vasorelaxation
common, but not serious toxicities with niacin
- flushing - pruritus
MOA of fibric acid derivatives
- increase LDL receptor expression - activates LPL - increase free fatty acid metabolism
what is the significance of some statins being taken at night?
- they have a short half life - want to reach peak effect during cholesterol synthesis peak
gemfibrozil used for
- anti-cholesterol
HMG CoA reductase inhibitors and platelets
- reduce platelet activation - reduce risk of venous thromboembolism
role of NPC1
- cholesterol transport protein
MOA of niacin
- inhibits synthesis of triglycerides in the liver
when does liver cholesterol synthesis peak?
- between midnight at 2 AM
HMG CoA reductase inhibitors and plaques
- stabilize arterial plaques - reduce risk of thrombus
cholesterol absorption inhibitors drug to know
- Ezetimibe
role of PCSK9
- induces LDL-receptor degradation - LDL-receptor bound to PCSK9 is digested in lysosome
serious, not common toxicities of niacin
- hepatotoxicity - insulin resistance
proteins in LDL
- ApoB
HMG CoA reductase inhibitors drug examples
- Atorvastatin - Rosuvastatin - Simvastatin - Pravastatin - Lovastatin
what happens if you inhibits absorption of cholesterol with ezetimibe what happens if you inhibit cholesterol synthesis with statins what do you do?
- you increase cholesterol synthesis so maybe more can be absorbed - you increase cholesterol absorption COMBINE THEM BOTH
BABA example
- colestipol
role of LPL
- breaks down triglycerides
MOA of toxicities of fibric acid derivatives with oral anticoagulants
- kick warfarin off albumin - free serum warfarin - increased bleeding risk
result of class 3 niacin
- decrease LDL - decrease triglycerides - increase HDL
results of class 2 BABAs
- decrease LDL a bit
important drugs that inhibit CYP3A4
- gemfibrozil - amlodipine - warfarin
which statins are the most potent?
- atorvastatin - Rosuvastatin
warfarin used for
- anti-coagulant
HDL composed of
- more protein - less cholesterol/triglycerides
PCSK9 drug
- Alirocumab
MOA of toxicities of fibric acid derivatives with statins
- inhibit statin absorption in liver - increased serum statin leads to myopathy
MOA of bile acid binding agents (BABA)
- increase elimination of bile acids - draw more cholesterol out of the liver - liver expresses more LDL receptors
statin patients highly susceptible to hepatotoxicity
- patients with underlying liver disease - or chronic alcohol abuse
how are cholesterol and triglycerides transported in the plasma?
- in complexes with proteins
proteins in HDL
- ApoA/C/E
local toxicities with BABAs
- GI toxicities (dyspepsia) - flatulence/bloating - diarrhea/constipation
class 2 drug anti-hyperlipidemia drugs
- bile acid binding agents
result of class 1 statins
- decrease LDL - decrease triglycerides
statin myopathy can turn into
- rhabdomyolysis
HMG CoA reductase inhibitors reduce risk of venous thromboembolism by what %
- 43% reduction
importance of niacin use in diabetics
- use cautiously in diabetics
what do you give to pregnant women instead of statins
- Bile acid binding agents
class 6 anti-hyperlipidemia drugs
- cholesterol absorption stimulators - PCSK9 inhibitors
importance of taking other drugs with BABAs
- take other drugs 1 hour before or 3 hours after BABAs
Class 1 of anti-hyperlipidemia drugs
- HMG CoA reductase inhibitors
drug interaction MOA with BABAs
- reduce the absorption of numerous drugs from the gastrointestinal tract
HMG CoA reductase inhibitors and atherogenesis
- reduce inflammation in atherogenesis
class 5 anti-hyperlipidemia drugs
- cholesterol absorption inhibitors
toxicities with fibric acid derivates
- myopathy when used in combination with high dose statins - bleeding when used with anti-coagulants
importance of PCSK9 inhibitors
- antibodies that must be injected intramuscularly biweekly
class 4 anti-hyperlipidemia drugs
- fibric acid derivatives
LDL composed of
- less protein - more cholesterol/triglycerides
what statins should you take in the evening?
- lovastatin - simvastatin - fluvastatin
amlodipine used for
- anti-hypertension
which are the most widely prescribed anti-hyperlipidemia drugs
- class 1 statins
result of class 4 fabric acid derivatives
- decrease triglycerides
toxicities of statins
- birth defects - hepatotoxicity - myopathy - drug interactions
result of class 5 Ezetimibe
- decrease LDL
composition/function of BABA
- polymeric resins - bind and sequester bile salts
bile salts are derivatives of
- cholesterol
another name for HMG CoA reductase inhibitors
- statins
fibric acid derivates drug
- Gemfibrozil - Fenofibrate
MOA of PCSK9 inhibitors
- block LDL-receptor degradation - allows more LDL to be taken into cell in liver
what is an important cytochrome of statin action that inhibitors also act on
- CYP3A4
which statins does amlodipine interact with
- simvastatin - lovastatin - atorvastatin
statin hepatotoxicity occurs in what percentage of patients?
- 1-3%
importance of simvastatin dose with amlodipine
- should not exceed 20 mg/day with amlodipine
MOA of amlodipine drug interaction
- slows metabolism of statins - increases risk of muscle damage/rhabdomyolysis
statin myopathy risk increases with
- dose - age - hepatic or renal dysfunction - interaction with other drugs
Ezetimibe MOA
- NPC1 cholesterol receptor inhibitor - blocks absorption of cholesterol from intestines - stimulates LDL-receptor expression
systematic toxicities with BABAs
- not absorbed systematically, so no systemic toxicities
statins patients highly susceptible to hepatotoxicity should have what tests run before they take the drug?
- baseline and follow up serum aminotransferase activity
another name for niacin
- vitamin B3
result of class 6 PCSK9 inhibitors
- decrease LDL a lot
class 3 anti-hyperlipidemia drugs
- niacin
do daily multivitamins provide a lot of niacin
- no