STATINS
TRUE OR FALSE: This class of drugs works by inhibiting cholesterol synthesis and increasing the number of HDL receptors on liver cells in order to reduce the amount of HDL circulating in the blood stream
FALSE
What's true: This class of drugs works by inhibiting cholesterol synthesis and increasing the number of LDL receptors on liver cells in order to reduce the amount of LDL circulating in the blood stream
TRUE OR FALSE: This class of drug essentially "sequesters the cholesterol" so that more of it goes to the liver, and more cholesterol is needed to bind to LDL receptors in the liver in order to make bile acids (which are key to emulsifying fats), so as a result, LDL levels in the blood DECREASE
TRUE
The drugs in this class work on the "Brush Border Cells" that line this part of the anatomy:
(a) Stomach
(b) Small Intestine
(c) Bile Duct
(d) Large Intestine
(B) SMALL INTESTINE
The drugs in this catagory are "Monoclonal Anti-Body" drugs, which is why their generic name ends with the suffix "-mab," and also why they are so expensive (they cost a lot to develop). TRUE OR FALSE: The net effect of these PCSK9 inhibitors is to block this protein that takes up space on LDL receptors on hepatocytes, therefore allowing more of these LDL receptors to clear LDL out of the bloodstream
TRUE!
By blocking the protein (PCSK9) that gets in the way of this receptor process, it helps to REDUCE LDL levels in the blood
All of the drugs on this part of the unit, which help to treat dyslipidemia/hyperlipidemia especially by lowering the dangerous kinds of cholesterol in the blood which is called:
(A) HDL (High-Density Lipoprotein)
(B) LDL (Low-Density Lipoprotein)
BONUS: What is the desirable level (i.e. ideal lab range)
for this dangerous type of cholesterol?
(B) LDL (Low-Density Lipoprotein)
BONUS: The American Heart Association (AHA) recommends that desirable levels are reached when maintaining LDL under 100
Name the prototype drug in this category,
both its generic name and its Trade name
HINT:
the generic form ends in the suffix "-STATIN"
The prototype is atorvastatin (Lipitor)
Name the most common Side Effect (SE) or
Adverse Reaction (AR) of
cholestyramine (Questran)
OR if you missed that mentioned in class, instead
NAME AT LEAST FOUR COMMON ARs
Most common SE: CONSTIPATION
Other common Adverse Reactions include:
BLOATING, INDIGESTION, NAUSEA, VOMITING, INCREASED VLDL LEVELS; INCREASED TRIGLYCERIDES; + HORRIBLE TASTE
Name both the generic and Trade name of the prototype drug in this class of "gut dietary cholesterol absorption inhibitor" drugs
It is ezetimibe (Zetia)
How are the drugs in this category commonly administered?
(a) PO (pill form)
(b) SL (sublingual)
(c) subQ (subcutaneous inj)
(d) IM (intramuscular inj)
(e) IV (intravenously)
(C) SUB-CUTANEOUS INJECTION (subQ)
NOTE: They are working on a PO version as well, but it is not available at this time
Of the three drugs in this unit that are designed to lower LDL cholesterol and taken PO, two can be taken with or without regard to food,
but one in particular SHOULD be taken at the same time as food and water (and perhaps combined into food or liquids), which is THIS drug
The drug cholestyramine (Questran)
SHOULD be taken with a meal
and possibly combined with food or liquids
(According to the notes: Take with meal and full glass of water." Plus the powder form can be mixed in 8oz of H2O or mixed with soups, applesauce, or cereals, followed by a big glass of water)
List AT LEAST TWO elements of the PATIENT TEACHING for atorvastatin (Lipitor)
(1) TAKE ONCE DAILY IN EVENING, WITH EVENING MEAL OR JUST BEFORE BED
(2) AVOID GRAPEFRUIT OR POMEGRANATE JUICE
(3) GET LIVER FUNCTION TESTS INITIALLY AND ON A PERIODIC BASIS (often 1x/year) WHEN TAKING THIS DRUG
(4) CALL MD IF YOU HAVE ANY S/S OF MYOPATHY
TRUE OR FALSE: Although cholestyramine (Questran) can decrease the absorption of atorvastatin (Lipitor), reducing that drug's effectiveness, nevertheless the two drugs are commonly prescribed together in "combo" therapy (ideally taken at least an hour apart)
TRUE
TRUE OR FALSE: The drugs in this category are often given together (an "adjunct") with a "statin" drug as part of combination therapy for dyslipidemia
TRUE
NOTE: If the two are prescribed together, the 2 tablets can be taken together at night
Give both the generic and the Trade name of the prototype monoclonal antibody drug in this class
alirocumab (Praluent)
The statins such as atorvastatin (Lipitor) is used to treat hypercholesterolemia, to lower the risk for primary or secondary CV events, for post-MI tx, and to
lower the risk for CV events related to Diabetes.
List AT LEAST TWO OTHER disease-processes (beyond those of the CV system) for which this class of drugs is often used
ALZHEIMERS DISEASE
KIDNEY DISEASE
RHEUMATOID ARTHRITIS
Certain EYE CONDITIONS
Some CANCERS
Name AT LEAST THREE COMMON
Adverse Reactions (ARs) of patients taking atorvastatin (Lipitor)
BONUS: Name AT LEAST TWO RARE ARs
Most Common ARs: HEADACHE, RASH,
MEMORY LOSS, GI DISTURBANCE
BONUS - Rare ARs: MYOPATHY, such as RHABDOMYOLYSIS, and HEPATOTOXICITY/ LIVER INJURY. Also potentially teratogenic - if taken by a pregnant person, there is risk of harming the fetus
Explain why it is important to take cholestyramine (Questran) with food,
to swallow it right away when taken PO (whether in tablet or powder form) and
to practice good oral hygiene afterward
BECAUSE THIS DRUG WILL DAMAGE ONE'S TEETH IF LEFT IN THE MOUTH (+ it tastes horrible!)
NOTE: This also may be the reason that patients should be instructed to take the medicine WITH A FULL GLASS OF WATER if not directly combined with food
List AT LEAST TWO COMMON and TWO RARE potential ARs for ezetimibe (Zetia)
Common: HEADACHE, DIARRHEA, NAUSEA, RASH
More Rare: Rhabdomyolysis, Hepatitis, Pancreatitis, Thrombocytopenia (low blood platelets)
NAME AT LEAST ONE of the specific classes of patients that this class of drugs was designed to treat (see our class handout under "uses")
(1) Patients with ASCVD
(=Atherosclerotic Cardio-Vascular Disease)
(2) Patients with familial (ie genetic?)
HYPERCHOLESTEROLEMIA
MATCH EACH PROTOTYPE WITH A CLASS DESCRIPTOR
(1) ezetimibe (Zetia) (a) Absorption Inhibitor (in Gut)
(2) atorvastatin (Lipitor) (b) Bile Acid Sequestrants
(3) alirocumab (Praluent) (c) HMG-CoA Reductase Inhib
(4) cholestyramine (Questran) (d) PCSK9 Inhibitor
(1) ezetimibe (Zetia) =(A) Absorption Inhibitor (in Gut)
(2) atorvastatin (Lipitor) =(C) HMG-CoA Reductase Inhib
(3) alirocumab (Praluent) =(D) PCSK9 Inhibitor
(4) cholestyramine (Questran) =(B) Bile Acid Sequestrants
In addition to the beneficial effects on blood LIPID levels (decrease LDL; decrease VLDL, increase HDL, decrease triglycerides), the drugs in this class also have beneficial cardiovascular (CV) actions.
NAME TWO BENEFICIAL CV ACTIONS
(1) PROMOTES PLAQUE STABILITY (thus less likely to break open/break off)
(2) DECREASES THE RISK FOR CV EVENTS (such as an MI)
Describe the way that this drug gets removed from the body (e.g. voided in the urine, excreted in feces, or eliminated by sweat glands?), and explain why that might be important for a patient to know
IT IS NOT ABSORBED IN THE BODY AT ALL, IT IS EXCRETED UNCHANGED IN THE FECES
That's important for the patient to know because taking the drug may change the consistency and color of the feces, often producing a much darker color stool, but sometimes to other colors as well (e.g. dark green)
The drug ezetimibe (Zetia) must be used with extreme caution in patients with hepatic/liver impairment, even if mild to moderate. In addition, there is a special warning for patients of THIS AGE GROUP
NOT RECOMMENDED FOR CHILDREN
UNDER TEN YEARS OLD
Most of the Patient Education for alirocumab (Praluent) revolves around the methods of proper drug administration and potential ARs that may come from that "route" to watch out for. List as many elements of both ARs and Patient Ed as you are able (AT LEAST THREE OF EACH)
ARs: Hypersensitivity reactions around the subQ INJECTION SITE including rash, urticaria, muscle pain, and vasculitis
(also note ARs not near inj site: influenza, diarrhea)
Pat Ed: Read drug lit.; Rotate the injection sites;
watch for ARs (eg rash and/or itch) around injection sites; store and dispose of needles safely;
store this drug in a refrigerator and warm up before injecting
Give the full names (generic + Trade) of the TWO drugs used for dyslipidemia therapy in this week's unit that are COUNTER-INDICATED FOR USE IN PREGNANCY AS WELL AS
FOR MOTHERS WHO BREAST FEED
The two are:
(1) atorvastatin (Lipitor)
and
(2) ezetimibe (Zetia)