Hyperlipidemia Flashcards
HMG-CoA Reductase Inhibitors (Statins)- All of the drugs in this class end in \_\_\_.
statins
Statins: MOA
Statins are Competitive inhibitors of 3-hydroxy-3-methylglutaryl (HMG) coenzyme A (CoA) reductase. HMG-CoA is involved in the synthesis of ______in the liver
cholesterol
Statins: MOA
Statins are Competitive inhibitors of 3-hydroxy-3-methylglutaryl (HMG) coenzyme A (CoA) reductase. HMG-CoA is involved in the synthesis of cholesterol in the liver.
Bottom line: less cholesterol made in cells results in a compensatory increase in the expression of___ receptors on hepatocyte membranes and a stimulation of LDL catabolism
LDL
We have LDL receptors on hepatocytes. When The body senses we need more ______, it makes more LDL receptors that will trap LDL out of the blood.
cholesterol
Statins: ADRs
- Hepatic: range from increased transaminases to toxicity
- MSK: strains, sprains, myalgias
- CNS: cognitive dysfunction including memory loss, confusion
- Cataracts
- small increase risk in developing diabetes
increased transaminases to hepatic toxicity is an ADR of statins, what should be monitored in the patients because of this?
Monitor liver enzymes- need to order CMP
strains, sprains, myalgias is an ADR of statins. There is an Increased risk of this if pt also has______ or is taking what kind of medications?
renal disease
fibrates, macrolides, “azole”, niacin- these are 3A4 drugs
strains, sprains, myalgias is an ADR of statins, what should be monitored in the patients because of this?
Check creatine kinase (CK) (also called creatine phosphokinase or CPK) levels with pt complaints
if your patients is on a statin and has cognitive dysfunction,memory loss, or confusion what should you do?
stop statin to see if memory gets better
Statins are Major substrate of _____and also weak inhibitor of _____,
CYP3A4
Common drugs that can have major interactions with statins?
Warfarin, protease inhibitors, macrolides, fibrates
If you need a macrolide to treat pneumonia, but macrolides have DDIs with statins, what should you do?
If you need macrolide to treat pneumonia or something, STOP THE STATIN. Because the statin can be started again after.
Statins: CI
3
- Pregnancy- DO NOT USE ON PREGNANCY, the developing baby needs cholesterol, if you block it is can cause birth defects or death of the fetus.
- Breast feeding
- Active liver disease
For statin monitoring, what baseline levels should you get?
o Creatine kinase
o Liver enzymes
o Lipid panel
o Renal function
Thereafter depending on clinical situation
o Lipids q4-8 wk until stable then at least q 6 months
some statins work better if dosed in the ______.
evening, Most dose daily at bedtime
Alternate-day dosing of statins has been shown to be useful and effective if patients have ______.
myalgias (mild muscle pain)
Niacin (nicotinic acid) MOA:
Niacin Inhibits lipolysis in adipose tissue which liver normally uses to produce _____
VLDL/LDL
Niacin (nicotinic acid) MOA:
Niacin Inhibits lipolysis in adipose tissue which liver normally uses to produce VLDL/LDL.This results in Fat cells that won’t break down
It also Increases secretion of tissue plasminogen activator and lowers level of plasma ______
fibrinogen
What is the Most potent agent to raise HDL
statin
Statin Increases secretion of tissue plasminogen activator and lowers level of plasma fibrinogen. this Can potentially cause _____ issues.
bleeding
Are niacin RX products the same as the OTC niacin products?
NO,
Rx products different than OTC vitamin forms
o OTC: <20 mg/day
o Rx: 1000-2000 mg/day (depends on formulation)
Rx Niacin products are often what kind of formulations?
sustained-release
Due to ADRs, Niacin is usually dosed at bedtime, with _____.
ASA and/or small meal
Niacin ADRs
- Cutaneous flushing/pruritus: can be severe and very uncomfortable
- GI: n/v
- Endo: increases risk of gout, Impaired glucose tolerance
- Hepatic disease is rare possibility
- Caution if used with statin
