Hyperlipidemia Drugs Flashcards
What class of drugs does Lovastatin belong to?
Statins, specifically HMG-CoA reductase inhibitor
What is the mechanism of action of Lovastatin?
Inhibits HMG-CoA reductase (rate limiting enzyme), suppressing lipoprotein synthesis and lowering LDL levels
What condition is primarily treated with Lovastatin?
Hypercholesterolemia, also drug Txt to prevent the (re) occurrence of blood clot formation (MI/Stroke)
What are the cardiovascular benefits of using Lovastatin?
Risk reduction for MI, HF, and sudden death
List three common side effects of Lovastatin.
- Headache
- Myopathy
- Hepatotoxicity
- GI upset
Fill in the blank: Lovastatin is an _______ inhibitor.
HMG-CoA reductase
What class of drug is Gemfibrozil?
Hepatic triglyceride inhibitor (Fibrate)
What is the mechanism of action of Gemfibrozil?
Inhibits hepatic triglyceride synthesis thus suppressing lipoprotein synthesis (VLDLs and sometimes LDLs)
It also increases the production of HDLs that activates reverse cholesterol transport from peripheral vascular beds.
Incr HDL probably from leftover cholesterol not used for LDL and VLDL
What lipoproteins are suppressed by Gemfibrozil?
VLDLs and sometimes LDLs
What effect does Gemfibrozil have on HDLs?
Increases the production of HDLs
What are common side effects of Gemfibrozil?
GI upset, gallstone formation, increased myopathy risk
True or False: Gemfibrozil can increase the risk of myopathy when used with statins.
True
Fill in the blank: Gemfibrozil is a ________ that activates reverse cholesterol transport from peripheral vascular beds.
fibrate
What is Niacin and where is it found?
A triglyceride lipase inhibitor in adipose tissue that reduces hepatic triglyceride synthesis and lipoprotein synthesis
adipose tissue!
What effect does Niacin have on hepatic VLDL synthesis?
Lowers hepatic VLDL synthesis
What effect does Niacin have on HDL cholesterol?
Raises HDL cholesterol
In what condition is Niacin commonly used?
Hyperlipidemia with low HDL and high triglycerides
What are common side effects of Niacin?
Flushing, GI disturbances, hepatotoxicity
Fill in the blank: Niacin is a _______ lipase inhibitor.
triglyceride
What drug type/class is Cholestyramine?
Bile acid sequestrant/ion exchange resin
How does Cholestyramine function?
It binds to bile salts and results in their elimination through the feces
(then they can’t go back to entero-hepatic circulation)
What effect does Cholestyramine have on cholesterol production?
Hepatic production of cholesterol is diverted from production of lipoproteins to bile salts
(since bile salts binded and poo’d out)
What are the indications for using Cholestyramine?
- Hypercholesterolemia
- Pruritus in cholestatic liver disease
What are common side effects of Cholestyramine?
- Constipation
- Bloating
What is Ezetimibe?
Cholesterol transport inhibitor
Ezetimibe is used to decrease cholesterol levels in the body.
What is the mechanism of action of Ezetimibe?
Inhibitor of cholesterol transport protein; blocks absorption of dietary cholesterol and cholesterol that enters the enterohepatic circulation
This mechanism helps in reducing overall cholesterol levels in the bloodstream.
What condition is Ezetimibe often used to treat?
Hypercholesterolemia
Ezetimibe is frequently prescribed alongside statins for better cholesterol management.
What are the common side effects of Ezetimibe?
GI upset, rare liver enzyme elevations
Patients on Ezetimibe should be monitored for lipid panels and liver function.
True or False: Ezetimibe should be used alone to treat hypercholesterolemia.
False
It is often used in conjunction with statins for enhanced effectiveness.
What is Vytorin composed of?
2 drugs
Ezetimibe + Simvastatin
Cholesterol transport inhibitor and a HMG-CoA reductase inhibitor
What is the mechanism of action of Vytorin?
Combines inhibition of intestinal cholesterol absorption with reduced hepatic cholesterol synthesis
Cholesterol transport inhibitor and a HMG-CoA reductase inhibitor
What condition is Vytorin used to treat?
Hypercholesterolemia in high cardiovascular risk patients
What are the side effects of Vytorin similar to?
Individual components (myopathy, liver enzyme elevations, GI upset)
What is Evolocumab also known as?
Repatha
Evolocumab
What type of drug is Evolocumab?
PCSK9 inhibitor (monoclonal antibody)
What is the mechanism of action of Evolocumab?
Inhibits PCSK9, promoting LDL receptor recycling and reducing circulating LDL levels
What conditions is Evolocumab approved to treat?
Familial hypercholesterolemia, high cardiovascular risk
How often are PCSK9 inhibitors like Evolocumab administered and what route?
Once every 2 weeks by injection
What are the FDA-approved uses of PCSK9 inhibitors?
Lowering LDL-particle concentrations when statins and other drugs were not sufficiently effective or poorly tolerated
What are some common side effects of Evolocumab?
Injection site reactions, nasopharyngitis, possible allergic reactions
