Hyperlipidemia Flashcards
Define statins and list some examples
INhibits HMG-CoA Reductase (produces cholesterol in the liver)
eg: Simvastatin, Lovastatin, Pravastatin, Atorvastatin, Rosuvastatin
Define PCSK9 inhibitors and list some examples
Inhibit PCSK9 which is an enzyme responsible for degrading LDL receptors in lysosomes in the liver
eg: Alirocumab, Evolocumab
Define Fibrates and list some examples
Fibric acid inhibitors / Fibrates activate peroxisome proliferator activated receptor alpha (PPAR-alpha) in the nucleus of hepatocytes, adipocytes and skeletal muscle fibers
eg: Clofibrate, Gemfibrozil, Fenofibrate, Bezafibrate, Ciprofibrate
Define ezetimibe
It is taken oraly and inhibits the NPC1L1 transport protein on enterocytes in the small intestines
Define bile-acid binding resins (sequestrants)
The positively charged bile-acid binding resins are taken orally and bind onto the negatively charged bile acids, preventing the bile acids from being reabsorbed by the small intestines back to the liver
eg: Colestyramine, Colestipol, Colesevelam
List the clinical indications for statins
1) Prevent the development of atherosclerosis for high-risk patients with other risk factors (eg: HTN)
2) Prevent MI or stroke in patients with atherosclerotic causing symptoms (eg: angina or transient ischemic attacks) or following MI or stroke
List the clinical indications for PCSK9 inhibitors
1) Familial Hypercholesterolemia (Type IIA Hyperlipidemia), especially in patients intolerant to statins
2) High risk patients with atherosclerotic cardiovascular disease requiring additional LDL lowering even after Statin therapy and diet control
List the clinical indications for fibrates
1) Familial Mixed Hyperlipidemia (Type IIB), especially in patients with elevated VLDL particles in the blood
2) Familial Dysbetalipoproteinemia (Type III), especially in patients with elevated VLDL particles in the blood
3) Familial Hypertriglyceridemia (Type IV), especially in patients with elevated VLDL particles in the blood
List the clinical indications for ezetimibe
1) Familial Hypercholesterolemia (Type IIA) when a Statin is contraindicated
2) Patients requiring additional attenuation even after Statin therapy and diet control is not enough
List the clinical indications for bile-acid binding resins
1) Familial Hypercholesterolemia (Type IIA)
2) Familial Mixed Hyperlipidemia (Type IIB)
List the contraindications of statins
Pregnancy
List the contraindications of PCSK9 inhibitors
Patients who develop hypersensitivity reactions or have severe allergies requiring hospitalisation
List the contraindications of fibrates
1) Acute Liver and Renal Failure
2) Pregnancy
3) Patients on statins with renal impairment
List the contraindications of ezetimibe
1) Breast-feeding women
2) Patients taking bile-acid binding resins
List the side effects of statins
1) Mild Hepatotoxicity
2) Myalgia
3) Gastrointestinal Problems (Abdominal cramps, constipation, diarrhoea)
4) Insomnia
5) Skin Rash
6) Myopathy (Rhabdomyolysis)
List the contraindications of bile-acid binding resins
None
List the side effects of PCSK9 inhibitors
1) Injection Site Inflammatory Reactions
2) Increased risk of infections (URTI/UTIs)
3) Increased incidence of nasopharyngitis and sinusitis
List the side effects of fibrates
1) Gastrointestinal problems (nausea)
2) Skin itchiness (pruritus) and rash
3) Gallstones
4) Myositis (muscle inflammation)
5) Myopathy (Rhabdomyolysis)
List the side effects of ezetimibe
1) Abdominal Pain and Diarrhoea
2) Headache
3) Skin Rash
4) Angioedema
List the side effects of bile-acid binding resins
1) Diarrhoea
2) Constipation
3) Dyspepsia (Indigestion)
4) Bloating
5) Impairs Lipid-Soluble Vitamin (A, D, E, K) Absorption, causing vitamin deficiency
When should statins be given?
Statins are usually given at night because the liver produces most of its cholesterol for the body during the night (peaks between 12am-2am) as there is no need for the liver to produce so much cholesterol during the day as it can be obtained from the diet during the day.
Give an example of a statin with a long half life
Atorvastatin and rosuvastatin