Lipids Pharm Flashcards
Mainstay of hyperlipidemia treatment
statins
All patients should have their ___ and ___ measured before starting and after starting a statin if symptoms of ___ are evident
All patients should have their AST and ALT measured before starting and after starting a statin if symptoms of hepatotoxicity are evident
About 1% of patients will develop elevations in LFTs that require D/C the drug
When to prescribe a High intensity statin (3)
- Anyone with atherosclerotic CV disease
- Anyone with a > 7.5% 10 year CV disease risk
- LDL > 190mg/dL
Effectiveness of high intensity statins
daily doses lowers LDL-C by about 50% on average
When to prescribe a Moderate intensity statin (4)
- Anyone with atherosclerotic CV disease > 75
- Cannot take a high dose statin
- ASCVD risk of 7.5% or higher
- You’ve got DB and LDL of 70 to 189 mg/dL
Effectiveness of moderate intensity statins
daily dose lowers LDL-C by ~ 30% to 50% on average
When to prescribe a low intensity statin (1)`
cannot take a high or moderate dose
Effectiveness of low intensity statins
Daily dose lowers LDL-C by less than 30% on average
MOA of statins
Inhibit cholesterol synthesis by inactivating HMG CoA reductase and increasing catabolism of LDL
pitavastatin
rosuvastatin
atorvastatin
potency?
Most potent LDL-C lowering agents
pravastatin
simvastatin
potency?
Intermediate potency
fluvastatin
lovastatin
potency?
lowest potency
Meds primary affect what organ
liver - that’s why you’re check AST and ALT and watching for transaminitis
Patients who are homozygous for familial hypercholesterolemia lack LDL receptors, and therefore, benefit much less from treatment with these drugs
statins
ADE of statins (4)
- elevated LFTs
- hepatic insufficiency can lead to problems
- increased effects on warfarin
- contraindicated in pregnancy
which statin has an increased risk of myopathy and rhabdomyolysis
simvastatin
increased incidences of myopathy and rhadomyolysis occurs in…
patients with renal insufficiency or concurrent use with nephrotoxic drugs
Muscle complaints should be evaluated with ___ levels
Muscle complaints should be evaluated with plasma creatine kinase (CK) levels
Most effective agent for increasing HDL-C
other than exercise… Nicotinic acid
Lowers triglycerides by 20% to 35% at typical doses of 1.5 to 3 grams/day
Nicotinic acid
At gram doses, strongly inhibits lipolysis in adipose tissues, thereby reducing the free fatty acid production
Nicotinic acid
Useful in treatment of familial hyperlipidemias:
- Lowers plasma levels of cholesterol
- Lowers plasma levels of triglycerides
Nicotinic acid
How do you prevent the intense cutaneous flushing and pruritis that is common with Nicotinic acid
Administration of aspirin 30 minutes prior to niacin decreases the flush (prostaglandin-mediated)
ADE of nicotinic acid (4)
- Nausea and abdominal pain
- Niacin inhibits tubular secretion of uric acid, may predispose to hyperuricemia and gout
- Impaired glucose tolerance
- Hepatotoxicity (avoid use of drug in setting of hepatic disease or impairment)
good drug for hypertriglyceridemia and subsequent pancreatitis that can develop from elevated Trig.
Fibric Acid Derivatives: fenofibrate and gemfibrizol
Derivatives of fibric acid, lowers serum ___ and increases ___
Derivatives of fibric acid, lowers serum triglycerides and increases HDL-C
Fenofibrate > ___ in lowering triglyceride levels
Fenofibrate > gemfibrizol in lowering triglyceride levels
Use of fibric acid derivatives
Treatment of hypertriglyceridemias
Particularly useful in treating familial dysbetalipoproteinemia
ADE of fibric acid derivatives (4)
- Mild GI disturbances are common; lessen as therapy progresses
- Gallstone formation due to increased biliary cholesterol excretion
- Myositis can occur; evaluate for muscle weakness or tenderness
- Use with caution in patients with renal insufficiency
- Myopathy and rhabdomyolysis reported if used with statins
Gemfibrizol + ____ is contraindicated
Gemfibrizol + simvastatin is contraindicated
Myopathy and rhabdomyolysis reported if ____ are used with statins
Myopathy and rhabdomyolysis reported if fibric acid derivatives are used with statins
Avoid use of ___ in patients with severe hepatic or renal dysfunction, preexisting gallbladder disease
Fibric Acid Derivatives
cholestyramine
colestipol
colesevelam
Bile Acid-Binding Resins
MOA of ___:
- Anion-exchange resins, bind negatively-charged bile acids and bile salts in the small intestine
- The bound complex is excreted in feces (lowers bile acid concentration)
- Causes hepatocytes to increase conversion of cholesterol to bile acids
- Intracellular cholesterol concentrations decrease, activating an increased uptake of cholesterol-containing LDL particles and a fall in plasma LDL-C
MOA of Bile Acid-Binding Resins
____ can relieve pruritus related to bile acid accumulation in patients with biliary stasis
Cholesytramine
____ is also indicated for DMII due to glucose-lowering effects
Colesevelam
Often used in combination with diet or nicotinic acid
Bile Acid-Binding Resins
Bile Acid-Binding Resins most common ADE
GI related: constipation, nausea, flatulence
Bile Acid-Binding Resin with fewer GI side effects than others in this drug class
Colesevelam
This group may impair absorption of fat soluble vitamins
Bile Acid-Binding Resins
Bile Acid-Binding Resins may increase…
triglyceride levels
ezetimibe
Cholesterol Absorption Inhibitors
- Selective inhibition of dietary and biliary cholesterol in small intestine
- Leads to decrease in hepatic cholesterol stores and increase in clearance of cholesterol from the blood
- Lowers LDL-C by approximately 17%
ezetimibe
adjunct to statin therapy or in statin-intolerant patients
ezetimibe
Drug with little to no ADE
ezetimibe
ezetimibe is primarily metabolized in the ____ and ____ via glucuronide conjugation
primarily metabolized in the small intestine and liver via glucuronide conjugation
Essential fatty acids used mainly for lowering triglyceride levels
Omega-3 polyunsaturated fatty acids (PUFAs)
Inhibit VLDL and triglyceride synthesis in the liver
Omega-3 polyunsaturated fatty acids (PUFAs)
Although effective at lowering triglyceride levels, omega-3 PUFA supplementation has not been shown to reduce ___ morbidity or mortality
Although effective at lowering triglyceride levels, omega-3 PUFA supplementation has not been shown to reduce CV morbidity or mortality
Drug class with greatest effect of lowering LDL?
Second greatest?
- statins (HMG CoA reductase inhibitors)
2. bile acid sequestrants
Drug class with greatest effect of increasing HDL?
Second greatest?
Third?
- Niacin
- Fibrates
- statins
Drug class with greatest effect of decreasing triglycerides?
Second greatest?
Third?
what increases the triglycerides?
- fibrates
- niacin
- statins
Bile acid sequestrants increase
Elevated ___ are independently associated with increased risk of ASCVD
triglycerides
Hypertriglyceridemia primary therapy (2)
diet
exercise
Hypertriglyceridemia secondary therapy (2)
- Nicotinic acid and fibric acid derivatives are most effective
- Omega-3 fatty acids in adequate doses may be beneficial
Myocardial infarction Stroke Retinopathies Nephropathies Impotence
Rhabdomyolysis and renal failure related to statins
Atherosclerosis and associated sequelae of hyperlipidemias
The primary organ at risk in hypoglycemia is the ___
Unlike other tissues, the ___ cannot use free fatty acids as an energy source
brain
Usually results from an imbalance between insulin and glucagon
Hypoglycemia
When glucose levels approach the low 80’s, insulin levels ____ to prevent hypoglycemia
decrease
As glucose levels continue to decrease, ____levels increase
___ is the first line defense against again more severe hypoglycemia
glucagon
____ is the next hormone to combat hypoglycemia; cortisol and other catecholamines also play a role
Epinephrine
- If patient took insulin surreptitiously, there will be a high blood insulin levels and a low blood C-peptide level (exogenous insulin does not contain C-peptide)
- Patients taking exogenous insulin will also develop anti-insulin antibodies
- If the patient took sulfonylurea, check urine or serum for drug levels
Factitious hypoglycemia
Ethanol ingestion
Insulinoma
Reactive (idopathic) hypoglycemia
can all cause…
hypoglcyemia
Insulin-producing tumor arising from beta-cells of the pancreas
Associated with MEN I syndrome
Usually benign (in up to 90% of cases)
Insulinoma
headache, visual disturbances, confusion, seizures, coma
Neuroglycopenic symptoms of an insulinoma
diaphoresis, palpitations, tremors, high blood pressure, anxiety
Sympathetic activation common in an insulinoma
How to dx insulinoma
72 hour fast: insulin levels that are even more elevated than in normal individuals –> even in the hypoglycemic conditions
How to diagnose an insulinoma
whipple triad
- Hypoglycemic symptoms brought on by fasting
- Blood glucose < 50 mg/dl during symptomatic attack
- Glucose administration brings relief of symptoms
whipple triad
whipple triad
- Hypoglycemic symptoms brought on by fasting
- Blood glucose < 50 mg/dl during symptomatic attack
- Glucose administration brings relief of symptoms
Whipple triad is used to diagnose true ___ (i.e., ____ due to underlying disease (like in insulinoma)
hypoglycemia
C-peptide levels are increased in ____ and in an ____
sulfonylurea abuse
insulinoma
Proinsulin levels are increased in ____, decreased in _____, and normal in _____.
Increased in insulinoma
Decreased in Sureptitious insulin
Normal in sulfonylurea abuse
If reactive hypoglycemia is suspected, ____ interventions are appropriate
If reactive hypoglycemia is suspected, dietary interventions are appropriate
If the patient is an alcoholic (or suspected alcohol), give ___ before administration of glucose to avoid Wernicke encephalopathy
thiamine
