W4, 5 Control dyslipidemia (pharma) Flashcards
Importance of cholesterol
Cholesterol is a necessary component of cell membranes and is a precursor of steroid hormones.
From where we get cholesterol
Cholesterol is derived from both exogenous (dietary)
and endogenous (synthesized in the liver) sources.
Four major types of lipoproteins:
Lipids including cholesterol and triglycerides are transported in the plasma as β¦β¦β¦β¦.
lipoproteins
Dyslipidemias can be classified into:
- Hypercholesterolemia
- Hypertriglyceridemia
- Mixed (i.e. hypercholesterolemia and hypertriglyceridemia).
What are THERAPEUTIC STRATEGIES of dyslipidemia
What is Dyslipidemia/ Hyperlipidemia
How does treatment of dyslipidemia work?
Main types of Lipid Lowering Drugs:
- Statins
- Fibrates
- Inhibitors of Cholesterol absorption (Resins and Ezetimibe)
- Nicotinic acid
- Omega-3-fatty acids
- PCSK9 Inhibitors
Statins drug examples
Statins eg lovastatin, Atorvastatin
MOA of statins
Other actions of statins unrelated to its actions on lipids:
Mean half-life in the plasma of statins is
14 hours
Half-life of inhibitory activity for HMG-CoA reductase is β¦. hours & why?
20 to 30 hours due to the contribution of active metabolites
Uses of statins
Adverse effects of statins
β’ Long treatment may cause a rise in serum levels of the liver
enzyme, transaminase.
β’ Other adverse effects include myopathy and ocular damage
(cataract)
Fibrates drug exampls
Fibrates e.g. Clofibrate, gemfibrozil
Mechanism of Action of fibrates
Pharmacokinetics of fibrates
a. Route of administration
b. Half life
c. Metabolism & excretion
Uses of fibrates
β’ Clofibrate is used to treat hyperlipidemias of various etiologies in
which there is an increase in VLDL levels.
β’ It has mild antidiuretic action in individuals with mild or moderate
diabetes insipidus (ADH not produced in diabetes insipidus = increased urine production)
Adverse effects of fibrates
What DRUGS AFFECT PLASMA CHOLESTEROL? Whatβs their MOA?
What are the uses of these drugs?
β’ Treatment of hyperlipidemias.
β’ Cholestyramine is the drug of choice for hypercholesterolemia.
Whatβs their Adverse effects:
- Quite safe, because not absorbed in the intestine.
- Abdominal pain, constipation, nausea.
- Interfere with absorption of some drugs like warfarin and digitalis
What drugs inhibit Cholesterol Absorption
Ezetimibe, resins