Lipid lowering drugs, Drugs to treat Diabetes Flashcards
What are the steps in plaque formation and growth?
1) Cholesterol particles infiltrate the wall of the artery at the site of the damaged inner lining of the artery
2) Plaque develops in the artery
3) As more cholesterol and materials are incorporated into the plaque, the plaque grows
4) The plaque may continue to grow blocking blood flow through the artery or
5) The plaque may rupture and blood clots may form, completely blocking blood flow through the artery
What are “bad cholesterols”?
LDL - stores cholesterol in the blood stream
What are “good cholesterols”?
HDL - regulates LDL storage and promotes excretion
What contributes to plaque buildup?
LDLs
Triglycerides
Inflammatory component
What are some mechanical procedures to treat plaque buildup in the circulatory system?
Balloon angioplasty to treat blocked coronary artery
Stent placement in carotid artery
High pressure jetting
Dyslipidemia
High cholesterol
An imbalance of lipids circulating in the blood stream
What are drugs used to treat dyslipidemia?
Derivatives of fibric acid Nicotinic acid Bile Acid sequestrants Inhibitors oh HMG CoA Reductase Cholesterol absorption inhibitors
What do fibric acids do?
Increase peripheral lipolysis
Decrease hepatic triglyceride production
What are side effects of fibric acid derivatives?
Abdominal discomfort Diarrhea Nausea Blurred vision Increased risk of gallstones Prolonged prothrombin time Liver studies may show increased function
What are the two mechanisms of action for Nicotinic acid?
1) Agonist for GPR 109A and 109B receptors
2) Inhibitor of diacylglycerol acyltransferase
What is the result of using Nicotinic acid?
Increase HDL-particles
Decrease Triglyceride
What are the side effects of nicotinic acid?
Flushing (due to histamine release)
Pruritis (itching)
GI distress
What happens to cholesterol in the liver?
It is converted to bile acid, which is excreted to the intestine through the action of C7H
By preventing bile acid resorption, the sequestrants increase cholesterol metabolism to bile acid
What are the major actions of bile acid sequestrants?
Reduce LDL-C 15-30%
Increase HDL-C 3-5%
May increase TG
What are the major side effects of Bile acid sequestrants?
GI distress/constipation
Decreased absorption of other drugs
Inhibitors of HMG CoA Reuctase
HMG-CoA reductase is an enzyme along the pathway of cholesterol synthesis
By inhibiting it, it prevents the synthesis of cholesterol
Statins (HMG-CoA Reductase inhibitor) lowers cholesterol, but do they help people live longer?
The current prevailing opinion is that they are helpful for people at risk of having a heart attack
NPC1L1
A transport protein moving cholesterol from the lumen into the enterocyte and ultimately back into the blood
Blocked by Ezetimbie (Cholesterol Absorption inhibitor)
What do Cholesterol Absorption inhibitors do?
Inhibit absorption of both dietary and biliary cholesterol
Lower LDL formation - increases expression of hepatic LDL receptors
What is the mechanism of Cholesterol Absorption inhibitors?
Inhibit LDL formation by increasing hepatic LDL receptors and taking it up to be secreted