Antilipemic drugs Flashcards
What are the two primary forms of lipids in the blood?
Triglycerides and Cholesterol
What are apolipoproteins
Specialized lipid-carrying proteins
What is the term for the combo of triglycerides and/or cholesterol with an apolipoprotein?
Lipoprotein
What are the 4 subcategories of lipoproteins and what is the “good” one
Very low density
Immediate density
Low-density
High-density (good because it recycles cholesterol)
How much greater is the risk of coronary heart disease in patients with cholesterol levels of 5.2 mmol/L compared to those with levels less than 4 mmol/L
3-4x
What choosing drug therapy for a patient with dyslipidemia, what tests need to be done first
Phenotyping: Determining the specific lipid profile of the patient
What are the 5 established classes of antilipemics
Hydroxymethylglutaryl–coenzyme A (HMG–CoA) reductase inhibitors (statins)
Bile acid sequestrants
B vitamin niacin
Fibric acid derivatives
Cholesterol absorption inbitor
How do statins/HMG-CoA reductase inhibitors treat hypercholesterolemia
Decreases rate of cholesterol production.
When less is produced, the liver increases the number of LDL receptors to recycle LDL from circulation back into the liver where it is needed for synthesis of steroids, bile and cell membranes
What is the suffix for (HMG–CoA) reductase inhibitors (statins)
“statin”
Name 2 HMG-CoA reductase inhibitors (Statins)
Atorvastatin
Rosuvastatin sodium
What are the adverse effects of HMG-CoA reductase inhibitors (statins)
Mild GI disturbances
Rash
Headache
Myopathy
Rhabdomyolysis
What is rhabdomyolysis and what are the signs?
Breakdown of muscle proteins and urinary elimination of the muscle protein myoglobinuria that can lead to acute kidney injury and death
Usually reversible when caught early and the drug is discontinued
Signs are muscle soreness or changes in urine colour to tea-coloured
What are drug interactions with statins
Anticoagulants,
Erythromycin,
HIV and Hep C protease inhibitors
Grapefruit
Clarithromycin
Amlodipine
How and when are atorvastatin calcium and rosuvastatin taken
Once daily, usually with the evening meal or at bedtime
Name a bile acid sequestrant and what else they can be called
Cholestyramine resin
AKA bile acid-binding resins or ion-exchange resins
What is the MOA of bile acid sequestrants
Prevent reabsorption of bile acids from SI (bile absorbs cholesterol). The more bile acids are excreted, the more the liver converts cholesterol to bile acids, removing it from circulation
What are the indications for bile acid sequestrants?
Type 2 Hyperlipoproteinemia
Relief of pruritus (itching) from biliary obstruction
Used in adjunct with statins
What are the adverse effects of bile acid sequestrants
Constipation
Heartburn
Nausea
Burping
Bloating
Mild increase in triglyceride levels
Overdose can cause ______ because the bile acid sequestrants are not absorbed.
obstruction
What is a consideration to make about the timing of administering bile acid sequestrants
All other drugs must be taken 1 hour before or 4-6 hours after admin of bile acid sequestrants
What can high doses of bile acid sequestrants cause
Decrease the absorption of fat soluble vitamins (A,D,E,K)
What are the contraindications of cholestyramine resin
Complete biliary obstruction
Pregnancy and lactation
Diarrhea treatments
What is the MOA of niacin
Inhibits lipolysis in adipose tissue
Decreases esterification of triglycerides in the liver
Increases activity of lipase
Reduces metabolism of cholesterol and triglycerides
As a result: Decreased triglyceride, LDL levels and increased HDL levels
Also breaks down fibrin clots
What is another name for niacin
Vitamin B3
Nicotinic acid
What are the indications for niacin
Effective and inexpensive way to lower LDL and triglyceride levels
When are the therapeutic and maximum effects of niacin
Therapeutic: 1-4 days
Maximum: 3-5 weeks
What are the contraindications of niacin
Peptic ulcer disease, HTN, active hemorrhagic process
What are the adverse effects of niacin
Flushing, Pruritus, GI distress
What is another name for fibric acid derivates and name 1 example
Gemfibrozil
AKA fibrates
What is the MOA of fibric acid derivatives
Activates lipoprotein lipase to break down cholesterol
Suppresses the release of fatty acids from adipose tissue
Inhibits synthesis of triglycerides in the liver
Increases secretions of cholesterol in the bile
What are the indications for fibrates?
Types 3, 4 and 5 hyperlipidemias
Can decrease HDL level by as much as 25%
What are the contraindications for fibrates
Allergy
Sever liver or kidney disease
Cirrhosis
Gallbladder disease
What are the adverse effects of fibric acid derivatives?
Abdominal discomfort
Diarrhea
Blurred vision
Headache
Prolonged prothrombin time
Increased risk of gallstones
Increased enzyme levels
What are the drug interactions with Gemfibrozil
Enhances anticoagulants
Always given with statins which increases the risk of myositis, myalgia, and rhabdomyolysis
What results would you expect to see in a blood test of a patient taking fibric acid derivatives
Decreased Hb, hematocrit and WBC
Increased aspartate aminotransferase (AST), activated clotting time, lactate dehydrogenase and bilirubin level
Name 1 cholesterol absorption inhibitor
Ezetimibe
What is the MOA of cholesterol absorption inhibitor
Inhibits absorption of cholesterol in SI
Reduces total LDL, apolipoprotein and triglycerides levels
Increases HDL
What treatments can garlic be used for?
Antispasmodic, antiseptic, antibacterial, antiviral, antihypertensive, antiplatelet, lipid reducer
What are the adverse effects of garlic
Dermatitis, vomiting, diarrhea, anorexia, flatulence, decrease coagulation
What are possible drug interactions with garlic
Warfarin, Diazepam, Protease inhibitors
May enhance bleeding when taken with NSAIDs
What are the indications for flax
Atherosclerosis, Hypercholesterolemia, Hypertriglyceridemia, GI distress, Menopausal symptoms, Bladder inflammation
What are adverse effects and possible interactions with flax
Diarrhea and allergic reactions;
Antihyperglycemic drugs and anticoagulants
what are adverse effects, interactions and contraindications and indications for omega 3 fatty acids
They reduce cholesterol
May cause rash, belching, allergic reactions
May interact with anticoagulants
Contraindicated in pregnancy
Patients on long-term therapy of antilipemics may need __________________
supplemental fat-soluble vitamins (A, D, E, K).
T/F: Powder forms must be taken with a liquid that is stirred or it should be taken dry
False: It should be mixed thoroughly but not stirred, and never taken dry
What can be taken 30 minutes before niacin to minimize flushing
Small doses of aspirin or NSAIDs
