Pharm Block 2 ( Hyperlipoproteinemia)
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What are their functions:
Chylomicrons- Transports Dietary TG from the intestines to the Tissues
VLDL- Transports TG from the liver to the tissues
LDL- Delivers cholesterol to cells. High LDL= High cholesterol.
HDL- Picks up Cholesterol that is accumulating in the blood vessels. (good for the heart)
What is good about drugs with lower lipoprotein content?
Drugs which lower the lipoproteins have a potential to prevent the CVA and CAD by retarding atherosclerosis.
What are the Normal (desirible) levels of:
- Total cholesterol: <200
- LDL: 100
- HDL: 40-50
- Triglycerides: 150
What is the difference between the Exogenous and Endogenous pathways of Lipoproteins?
Exogenous- Lipids are picked up in the intestines--> chylomicrons deliver some to the tissues, the rest goes to the liver.
Endogenous- VLDL from the LIVER--> transported to the tissue then returned to the liver.
What are the different classes of drugs for Hyperlipoproteinemia?
What are the Drugs for Hyperlipoproteinemia that are Bile acie Squestrants (RESINS)?
how do they work?
- Cholestyramine, Colestipol
- These bile acid binding resins are neither digested nor absorbed in the gut.they increase fecal excretion of bile salts and cholesterol
- The decrease in cholesterol is also due to up regulation of LDL receptors in liver.
What is the Bodies reflex in respose to Cholestyramine and Colestipol?
- The body causes a increase in the activity of HMG CoA reductase results in increased cholesterol synthesis and thus increased VLDL secretion – blunting the long term effectiveness of monotherapy
- -Mild increase in triglycerides can be seen.
What are some Adverse effects of Cholestyramine and Colestipol?
- 1. Constipation
- 2. Deficiency of fat soluble vitamins- No bile to breakdown the fats
What are STATIN drugs?
they are drugs for Hyperlipoproteinemia that are HMG CoA reductase Inhibitors (rate limiting step ofcholesterol syn).
- Lovastatin, Sincastatin,
- Atorvastatin (lipitor)- antioxidant effect.
- Rosuvastatin- has a high Potency.
What is something that you need to consider when using statins on a women?
Statins work by inhibiting the production of Cholesterol. Cholesterol is needed for Progesterone synthesis. Progesterone is needed for maintenance of pregnancy.
So you should check with the women to see if she is pregant before putting her on them.
What are the effects of HMG CoA reductase Inhibitors?
- -Increase in LDL receptors expression on the liver--> decrease LDL--> decrease cholesterol.
- -Hepatic synthesis of VLDL is reduced
- -There is an increase in HDL.
What are some Cardio protective actions of STATIN drugs?
- -Endothelial function – increase endothelial NO synthesis
- -Plaque stability – Suppress smooth muscle cell proliferation, inhibit metalloproteinase
- -Anti-inflammatory action
- -Increase activity of paraoxonase - anti-oxidative enzyme
- -Anticoagulation – reduce platelet aggregation
What are some Adverse effects of statin drugs?
- -Sleep disturbances
- -Hepatotoxicity (esspecially at higher doses) --> Kidney failure.
- -Rhabdomyolysis / myopathy
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