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Lipid-lowering agents
N/A
29
Medical
Professional
02/20/2010

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Cards

Term
Statins effects
Definition
HMG-CoA Reductase inhibitors

Reduce LDL levels by inc hepatic uptake of LDL/VLDL remnants

Reduce susceptibility of lipoproteins to oxidation

Given at night bc chol synth inc at night
Term
Statin mechanism
Definition
Dec chol synth => dec liver chol => inc LDL rec synth => inc chol recall to liver
Term
Statin pharmacokinetics properties
Definition
High first pass effect

Low bioavailbility

High protein binding in plasa

Peak plasma conc 1-4 hrs

70% eliminated by liver
Term
Statin side effects
Definition
RHABDOMYOLYSIS
HEPATOTOXICITY
NEUROPATHY
GI sx, HA, rash, cramps, insomnia
Term
Statin contraindications
Definition
pregnancy and nursing
hepatotoxicity
Term
Statin rx interactions
Definition
Inc coumadin levels

OAT2 inh (gemfibrozil) => inc statin levels
Term
Bile acid-binding resins
Definition
bind anionic bile acids in intestinal lumen

resin-bile acid complex cannot be absorbed and is excreted in stool

Lowering bile acids cx liver to convert lipids to bile acids

IC liver lipid conc dec => inc hepatic uptake of LDL

Useful only where LDL is elevated to reduce LDL 10-20%
Raises HDL only slightly

Reduces major coronary events & mortality
Term
Simvastatin
Definition
Statin w low bioavailability but effective

Taken PO w or w/o food in evening
Term
Atorvastatin
Definition
statin

Taken PO w or w/o food anytime of day
Term
Pravastatin
Definition
statin

Taken w or w/o food in the evening
Term
Cholestipol
Definition
Bile acid-binding resin

Oral, taken w large amounts of fluid

Take other rxs 1 hr before or 4 hrs after, bc they might not be absorbed
Term
Cholestyramine
Definition
Bile acid-binding resin

Taken w large amts of fluid
Take other rx 1 hr before or 4 hr after
Term
Cholesevelam
Definition
Bile acid-binding resin

Taken PO
Term
Bile acid-binding resins side effects
Definition
May inc TG

GI distress/constipation
Dec absorption of other rxs
Term
Bile acid-binding resins contraindications
Definition
high TG w/o high LDL
Term
Ezetimibe
Definition
blocks intestinal sbsoprtion of chil by inh of NPC1L1 transporter

Inh absorption by 55%

Reduces LDL ~18%
Term
Fibric acids
Definition
Dec VLDL synth cxs:

dec VLDL, inc HDL, dec TG

Acts via PPARa agonism and altered gene expression
Term
Fibrate side effects
Definition
Myalgias
Rhabdomyolysis (inc w statin)
Gallstones
Inc tranaminases
GI distress
Term
Fibrate contraindications
Definition
severe renal or hepatic dz
Term
Fibrate rx interactions
Definition
Inc warfarin conc

Inc clearance of cyclosporine (immunosuppressant)
Term
Niacin
Definition
Reduces VLDL and LDL, via inh of lypolysis in adipose tissue

Most effective agent for inc HDL

Near complete absorption, but short half life
Term
Niacin side effects
Definition
flusing
itching
hyperglycemia
hyperuricemia
GI issues
Term
Niacin contraindications
Definition
Liver dz
Severe gout
Peptic ulcer
Term
Probucol
Definition
Antioxidant that inh chol oxidation

Slows atherosclerosis development
Term
Probucol side effects
Definition
mild GI distrubance

prolongs QT interval
Term
Niacin + resin
Definition
First choice against familial hyperchol
Term
Niacin + resin + statin
Definition
most effective
Term
Statin + resin
Definition
safe combo for LDL lowering
Term
Statin + chol abs. inh (Vytorin)
Definition
safe combo for LDL lowering
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