Antihyperlipidemic Drugs Flashcards
HMG CoA reductase inhibitors
Statins
Inhibitors of hepatic lipid production
Nicotinic acid
Activators of plasma lipoprotein lipase
Fibric acid derivatives
Inhibitors of intestinal cholesterol absorption
Bile acid binding resins: cholestyramine, colestipol and Ezetimibe
Other drugs used in treatment of hyperlipidemia
D- thyroxine
Neomycin
Probucol
Mention Statins drugs
Lovastatin
Pravastatin
Svastatin
Fluvastatin
Atorvastatin
Pitavastatine
Rosuvastatin
Statins drugs they are prodrugs
Lovastatin
Simvastatin
All statins are taken at night except
Pitavastatine
Atorvastatin
Rosuvastatin
It’s have life is 12 hours
Pitavastatine
It’s half life time is 14 hours
Atorvastatin
It’s half life time is 19
Rosuvastatin
All statins are metabolized in
Liver
Therapeutic uses of statins
Hyperchlolesterolemia
Hyperlipidemia
Acute coronary symptoms
Adverse effects of statins
Elevation of serum hepatic enzymes
Myopathy
Rhabdomyolysis
Git disturbances
Cataract
Renal dysfunction
Statins potentiate action of
Oral anticoagulant (warfarin)
Oral antidiabetic
The CYP3A5 dependent reductase inhibitors are
Lovastatin
Simvastatin
Atorvastatin
Drugs that increase effect of CYP3A4
Macrolide
Ketoconazole
Amiodarone
Verapamil
Drugs that decrease effect of CYP3A4
Phenytoin
Griseofulvin
Barbiturates
Rifampicin
Catabolism of …and …. And to a lesser extent….. Are mediated by CYP2C9
Fluvastatin
Rosuvastatin
Pitavastatine
Inhibitors of CYP2C9 are …
Metronidazole
Amiodarone
Cimetidine
Drugs that increase plasma levels of fluvastatin and rosuvastatin
Metronidazole
Amiodarone
Cimetidine
Drug of choice used with verapamil, ketoconazole and macrolide
Pravastatin
Rosuvastatin
A drug which increase blood concentration of most statins by inhibiting glucuronidation of statins
Gemfibrozil
Contraindications of statins
Pregnancy
Lactation
Advanced hepatic disease
Advanced renal disease
It is the most effective agent for increasing HDL
Niacin( nicotinic acid)
Drug which administered orally and excreted in the urine
Niacin
Drug which inhibits lipolysis thereby reducing production of free fatty acid
Niacin
(In liver )
Drug which inhibits hepatocyte diacylglycerol acyltransferase-2
Niacin
(In plasma)
Drug that increases lipoprotein lipase activity that increase clearance of VLDL and chylomicron
Niacin
Uses of Niacin
Combined hyperlipidemia
Hypertriglyceridemia
Severe hypercholesterolemia in combination with a resin or reductase inhibitors
Statins intolerance
Adverse effects of niacin
✓Cutaneous flush
✓git disturbances
Nausea
Abdominal pain
Gastric distress
Increase gut motility due to histamine reley
✓Hyperuricemia
✓Reversible elevation in aminotransferase up to twice
✓Carbohydrates tolerance
Rarely
✓Platelet deficiency
✓Arrhythmia
✓Macular edema
Contraindications of niacin
Peptic ulcers
Hepatic disease
Niacin may potentiate the action of …
Antihypertensive agents
