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43 Cards in this Set

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Drug class of Cholestryamine
bile acid sequestrant
Cholestyramine
Questran, colestipol

bile acid sequestrant
Therapeutic class of Cholestryamine
cholesterol lowering agent
Pharmacodynamics of Cholestryamine

(bile acid sequestrant)
forms a non-absorbable complex with bile acids in small bowel (releasing Cl)

inhibits enterohepatic reuptake of intestinal bile salts

increases fecal loss of bile acids --> increases bile synthesis --> increases cholesterol synthesis --> increases expression of LDL receptors on cell surface of hepatocytes!!!!!! --> reduces LDL cholesterol by 10-20%
Pharmacokinetics of Cholestryamine
virtually no absorption

excreted in feces

peak effect noted in about 3 weeks
Toxicity of Cholestryamine
greater than 10% of patients have GI problems including gas, bloating, diarrhea

may interfere with absorption of fat-soluble vitamins
Drug interactions with Cholestryamine
may diminish absorption of statins, steroids, digoxin, warfarin
Special issues of Cholestryamine
provided as a powder for oral suspension

be sure to drink liquids of it

(this can cause low compliance)
Dose of cholestryamine
4 grams once a day, up to 6 times per day
Nicotinic acid
Niacor

cholesterol lowering agent
Pharmacologic class of Nicotinic acid
its a vitamin
Therapeutic class of nicotinic acid
its a cholesterol lowering agent
Pharmacodynamics of Nicotinic Acid
lowers both TG and LDL cholesterol

decreases the production of VLDL --> decreases production of LDL --> INCREASES LDL RECEPTOR IN THE LIVER


modestly effective as a single agent, usually used in combination
Pharmacokinetics of Nicotinic Acid
Nicotinic acid (a vitamin) is well absorbed

Has a large first pass effect (to nicotinamide)

Tmax: 45 minutes

Half life: 45 minutes

Urinary excretion of unchanged drug and metabolite
Toxicity of Nicotinic acid
many patients develop skin flushing...this skin flushing can be lessened by taking aspirin

Some patients even develop hepatitis (think first pass effect)
Interactions with other drugs using Nicotinic Acid
the absorption is decreased by cholestryamine
Interactions of nicotinic acid with other drugs
absorption decreased by cholestryamine
Special issues with nicotinic acid
in 1930's found to be a vitamin (B3) that cured pellegra; renamed niacin in 1940s;

partically converted in the body to nicotinamide, which is NOT active in lowering lipids, but is active in forming NAD

avoid in patients with CAD and heavy ethanol use
Dose of nicotinic acid
pellegra use 100mg tid

hyperlipidemia use 0.5-2 gm tid after meals

realize that you use A LOT more for hyperlipidemia
Gemfibrozil
Lopid, Clofibrate, Atromid

fibric acid derivative
Drug class of Gemfibrozil
Pharm: fibric acid der.

Therapeutic: lipid lowering agent
Pharmacodynamics of Gemfibrozil
cellular mechanism remains unclear (probably related to inhibiting lipolysis and decrease hepatic fatty acid uptake, inhibits hepatic secretion of VLDL)

produces slight reduction in LDL-cholesterol leves (~4%)

MOST USEFUL in treatment of hypertriglyceridemia in types IV and V hyperlipidemia (31%)

may increase HDL-chol (6%)
Pharmacokinetics of Gemfibrozil
well absorbed

oxidized in liver to two inactive metabolites

half life is 1-2 hours
Toxicity of Gemfibrozil
elevation of LFTs

myositis

GI distress

Avoid in patients with renal, hepatic, or biliary tract disease
Interactions of Gemfibrozil and other drugs
effects increased with statins, buy may potential toxicity (liver, muscle) as well
Indications and dose/route of Gemfibrozil
600 mg po twice daily
Lovastatin
Mevacor

Atorvastatin (Lipitor)
Drug class of Lovastatin
Pharm: LACTONE

Therapeutic class: cholesterol lowering drug

primary and secondary prevention of CAD
Pharmacodynamics of Lovastatin
parent drug is transformed to an active metabolite, which inhibits HMG-CoA reductase, the early and rate-limiting step in the synthesis of cholesterol

Inhibition is not complete...LEADS TO UP-REGULATION OF LDL RECEPTORS ON HEPATOCYTES

leads to reduction in LDL-chol (10-50%), increase in HDL (small)
Pharmacokinetics of Lovastatin
about 30% absorbed

onset of action is 3 days

Peak effects in several weeks

Excreted in feces

Metabolized primarly by CYP 3A4 (which is used to metabolize a LOT of things)
Toxicity of Lovastatin
check LFTs and CPK during first year of use, because of risk of hepatitis, myopathy, myositis
Lovastatin and its interactions with other drugs
additive effects with cholestryamine, nicotinic acid, ezetimibe

Gemfibrozil and niacin may increase risk of myopathy

Erythromycin and others may inhibit CYP 3A4 metabolism, thereby causing increased accumulation and toxicity
Special consideration of Lovastatin
avoid in patients with pre-existing hepatitis, muscle disease, and PREGNANCY (X)!!!!
Indications and dose/route of Lovastatin
20 mg po daily, with dinner, may increase to 80 mg po daily, or switch to more potent statin
Ezetimibe
Zetia
Drug class of Ezetimibe
Pharm class: 2 azetidinone compound

Ther class: cholesterol absorption inhibitor
Pharmacodynamics of Ezetimibe
selectively blocks the intestinal absorption of cholesterol and related phytosterols, by acting at the level of the small bowel brush border

causes reduction of hepatic cholesterol stores and INCREASE IN THE BLOOD CLEARANCE OF CHOLESTEROL
(upregulates the LDL receptors in hepatocytes)

when used as monotherapy, can lower LDL-chol by up to 18%

often used with statin
Pharmacokinetics of Ezetimibe
given orally

Tmax 4-12 hours

extensively metabolized to the glucoronide

F 35-60%

diarrhea in about 4%
Toxicity of Ezetimibe
HA in about 8%

diarrhea in about 4%
Interactions with Ezetimibe
and other drugs
use in combo with dietary therapy, as monotherapy, or in combo with a statin

Bile acid sequestrants may decrease F
Vitorin
ezetimibe + simvastatin

the ezetimibe in combo with a statin
Special considerations of Ezetimibe
use with caution in patients with hepatic or renal impairment
Indications and dose/route of Ezetimibe
10 mg po daily