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FIU PPAR Drugs
FIU PPAR Drugs
16
Pharmacology
Professional
12/16/2011

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Term
-fibrates/-fibrozils
Definition
Activate PPAR-alpha.

Traditionally used to treat hyperlipidemia.

Mainly lowers triglycerides. Provides almost no change in cholesterol, although extremely mild lowering of VLDL. Virtually no change in LDL, and very slight rise in HDL*.

Side effects: Some induce gall stones (Clofibrate). Drug type cannot be combined w/ statins or Rhabdomyolysis will occur.
Examples: Clofibrate, Gemfibrozil, Fenofibrate, Bezofibrate, Ciprofibrate

*Point made in class that these meds are not used for cholesterol, only TGs.
Term
Clofibrate
Definition
Used for: Hyperlipidemia

Side effects: Gall stones, do not combine with statins (Rhabdomyolysis).
Term
-glitazones
Definition
Activation of PPAR-gamma

Traditionally used to treat type 2 diabetes. Causes increased insulin sensitivity via increasing glucose transporters, lowering FFA, remodeling adipose tissue, enhancing insulin signalling, reducing necrosis factor alpha.

Takes weeks to get the desired effect

Do not cause hypoglycemia like sulfynyl ureas but dangerous and expensive.


Side effects: Contraindicated for patients with liver problems. Cardiovascular disease, increased fluid volume (unresponsive edema), parasthesias, elevation in creatine phosphokinase.
Term
Troglitazone
Definition
Activates PPAR-gamma

Treats type 2 diabetes via increased insulin sensitivity

Slow Acting (weeks)

Removed from market due to liver toxicity.

Side effects: Contraindicated for patients with liver problems. Cardiovascular disease, increased fluid volume (unresponsive edema), parasthesias, elevation in creatine phosphokinase.
Term
Rosaglitazone
Definition
Activates PPAR-gamma

Treats type 2 diabetes via increased insulin sensitivity

Slow Acting (weeks)

Side effects: Contraindicated for patients with liver problems. Cardiovascular disease, increased fluid volume (unresponsive edema), parasthesias, elevation in creatine phosphokinase.
Term
Pioglitazone
Definition
Activates PPAR-gamma

Treats type 2 diabetes via increased insulin sensitivity

Slow Acting (weeks)

Side effects: Contraindicated for patients with liver problems. Cardiovascular disease, increased fluid volume (unresponsive edema), parasthesias, elevation in creatine phosphokinase.
Term
Gemfibrozil
Definition
Activate PPAR-alpha.

Traditionally used to treat hyperlipidemia.

Mainly lowers triglycerides. Provides almost no change in cholesterol, although extremely mild lowering of VLDL. Virtually no change in LDL, and very slight rise in HDL*.

Side effects: Drug type cannot be combined w/ statins or Rhabdomyolysis will occur. Displace warfarin from protein binding site.

*Point made in class that this med not used for cholesterol, only TGs.
Term
Fenofibrate
Definition
Activate PPAR-alpha.

Traditionally used to treat hyperlipidemia.

Mainly lowers triglycerides. Provides almost no change in cholesterol, although extremely mild lowering of VLDL. Virtually no change in LDL, and very slight rise in HDL*.

Side effects: Drug type cannot be combined w/ statins or Rhabdomyolysis will occur.Displace warfarin from protein binding site.

*Point made in class that this med not used for cholesterol, only TGs.
Term
Bezafibrate
Definition
Activate PPAR-alpha.

Traditionally used to treat hyperlipidemia.

Mainly lowers triglycerides. Provides almost no change in cholesterol, although extremely mild lowering of VLDL. Virtually no change in LDL, and very slight rise in HDL*.

Side effects: Drug type cannot be combined w/ statins or Rhabdomyolysis will occur. Displace warfarin from protein binding site.

*Point made in class that this med not used for cholesterol, only TGs.
Term
Ciprofibrate
Definition
Activate PPAR-alpha.

Traditionally used to treat hyperlipidemia.

Mainly lowers triglycerides. Provides almost no change in cholesterol, although extremely mild lowering of VLDL. Virtually no change in LDL, and very slight rise in HDL*.

Side effects: Drug type cannot be combined w/ statins or Rhabdomyolysis will occur. Displace warfarin from protein binding site.

*Point made in class that this med not used for cholesterol, only TGs.
Term
PPAR-alpha
Definition
Peroxizome Proliferator Activated Receptor type alpha.

Drugs activating this receptor are used to treat hyperlipidemia.

Regulation of genes involved in catabolism of fatty acids. Also causes increase in lipoprotein lipase.
Term
PPAR-Beta
Definition
Peroxizome Proliferator Activated Receptor type beta.

No drugs for this one! Yay! :D
Term
PPAR-gamma
Definition
Peroxizome Proliferator Activated Receptor type gamma.

Activated by leukotrienes, prostaglandins, and anti-diabetic thiazoledinediones.

Drugs activating this receptor are used to treat diabetes via increasing insulin sensitization.

Regulation of genes involved with storage of fatty acids.
Term
Retanoid X Receptor (RxR)
Definition
Part of eventual PP response element activating dimer.

Ligand: Retanoids
Term
Endogenous PPAR (alpha, beta, and gamma) ligands
Definition
fatty acids, prostaglandins, leukotrienes
Term
HbA1C
Definition
Gives average blood sugar over a long period of time. Below 7 is target for diabetic patients.
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