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Bile acid sequestrants

Bile acid sequestering agents (Resins): The liver uses cholesterol to produce bile acids, which are used in the digestive process. The bile acid sequestrants bind to these acids, reducing their supply. In turn, this stimulates the liver to produce more bile acids, which uses more cholesterol. Unfortunately, the resins can increase triglyceride levels.  When the statins are not sufficient to lower high cholesterol, these drugs can be added. Their use is often limited by side effects, which are primarily gastrointestinal. They can include nausea, bloating, cramping, and an increase in liver enzymes.

Cholestyramine (4-16 grams) or
Colestipol (5 to 20 grams) or
Colesevelam (2.6 to 3.8 grams)
LDL:  15-30%    HDL:  3-5%   TG: No change or increase
cholestyramine
(Questran ®): 
Adult (usual) Hypercholesterolemia/pruritis: initial, 4 grams orally qd to bid; maintenance, 8-16 g in divided doses, Max of 24 g daily. 
colesevelam
(Welchol ®):
Colesevelam is a high capacity bile acid binding molecule.  Adult (usual)-  hypercholesterolemia: 3 tabs (1875 mg) orally bid or 6 tabs orally qd – may increase to 7 tabs (4375 mg) daily
[Supplied: 625 mg tablet ] 
colestipol
(Colestid ®):
Adults: Recommended dose (Maintenance) –
(Tablets): 2 to 16 grams/day given once or in divided doses. The starting dose should be 2 grams once or twice daily. Dosage increases of 2 grams, once or twice daily should occur at 1 or 2 month intervals. If the desired therapeutic effect is not obtained at a dose of 2 to 16 grams/day with good compliance and acceptable side effects, combined therapy or alternate treatment should be considered.
Adult (usual): powder: 5-30 g orally (mixed with liquid) once daily or in divided doses.

Colestipol tablets must be taken one at a time and be promptly swallowed whole, using plenty of water or other appropriate liquid. Do not cut, crush, or chew the tablets. Patients should take other drugs at least one hour before or four hours after colestipol tablets to minimize possible interference with their absorption.

[Supplied: 1 gram coated tablet. 5 grams/dose granules for oral suspension. ]

Fibrates

The fibrates, or fibric acid derivatives, act in part to stimulate the activity of peroxisome proliferator-activated receptors (PPARs), which are involved in fatty acid breakdown. The main action of fibrates is to lower triglyceride levels (by 35 to 50 percent).   Fibrates also raise serum high density lipoprotein (HDL) by 15 to 25 percent. Fibrates are the drugs of choice when treating isolated elevated triglycerides. They can be combined with statins to treat combinations of high triglycerides and LDL cholesterol.

Gemfibrozil (600 mg bid) or
fenofibrate (145 mg) or
Clofibrate (1000 mg bid)
LDL:  5-20%    HDL:  10-20%     TG: 20-50%
clofibrate  Usual dosage (dyslipidemia): 500 mg orally 4 times/day. Some patients may respond to lower doses.
Renal Dosing:
crcl >50 ml/min: Administer every 6-12 hours.
crcl 10-50 ml/min: Administer every 12-18 hours.
crcl <10 ml/min: Avoid use.
      Supplied: 500 mg capsule.
fenofibrate
(Tricor ®): 
Initially: 67 mg (1 cap) orally once daily with meal.   Maximum: 3 caps once daily. 
gemfibrozil
(Lopid ®):
Usual dosage: 600mg orally twice daily.

Niacin

Niacin
Vitamin B3
Hyperlipidemia:
Nicotinic acid and nicotinamide are the two common forms of the vitamin most often referred to as niacin. OTC preparations that are marketed as causing “no flush” may have no free nicotinic acid and are ineffective in treating dyslipidemia.

Regular release formulation (Niacor®): Initial: 250 mg once daily (with evening meal); increase frequency and/or dose every 4-7 days to desired response or first-level therapeutic dose (1.5-2 g/day in 2-3 divided doses); after 2 months, may increase at 2- to 4-week intervals to 3 g/day in 3 divided doses
Extended release formulation (Niaspan®): 500 mg at bedtime for 4 weeks, then 1 g at bedtime for 4 weeks; adjust dose to response and tolerance; can increase to a maximum of 2 g/day, but only at 500 mg/day at 4-week intervals.

Administer with food. Administer Niaspan® at bedtime. Niaspan® tablet strengths are not interchangeable. When switching from immediate release tablet, initiate Niaspan® at lower dose and titrate.
MONITORING— Blood glucose; liver function tests (dyslipidemia, high dose, prolonged therapy) pretreatment and every 6-12 weeks for first year then periodically; lipid profile.
Dose dependent changes:  1.5-3g (IR) or 1-2g (ER or SR)
LDL:  5-25%    HDL:  15-25%     TG: 20-50%

Statins

atorvastatin
Lipitor ®
Initially: 10 mg orally once daily. Maximum of 80 mg/day
Dose dependent changes
(Associate lower end of range with lower dosage):
LDL: 
35-60%    HDL:  5-9%      TG: 19-37%
fluvastatin
Lescol ®
Initially: 20-40 mg orally at bedtime, Maximum of 80 mg/day.
Dose dependent changes
(Associate lower end of range with lower dosage):
LDL: 
22-36%    HDL:  3-9%     TG:  12-23%
lovastatin
Mevacor ®
Initially: 20 mg orally every evening. Maximum: 80 mg/day.
Dose dependent changes
(Associate lower end of range with lower dosage):
LDL: 
21-42%    HDL:  2-9%      TG: 6-27%
pravastatin Pravachol ® Initially: 10-20 mg orally at bedtime,   Maximum of 40 mg/day.
Dose dependent changes
(Associate lower end of range with lower dosage):
LDL: 
22-37%    HDL:  2-12%      TG: 11-24%
Rosuvastatin Crestor ® Initially:  10 mg once daily (20 mg in patients with severe hypercholesterolemia).  Conservative dosing: Patients requiring less aggressive treatment or predisposed to myopathy (including patients of Asian descent): 5 mg once daily.  Titration: After 2 weeks, may be increased by 5-10 mg once daily. Dosing range: 5-40 mg/day (maximum dose: 40 mg once daily)
Dosage restrictions:  Rosuvastatin dose should not exceed 5 mg/day if co-administered with Cyclosporine.  Rosuvastatin dose should not exceed 10 mg/day co-administered with Gemfibrozil.   Patients with crcl <30: Initial: 5 mg/day. Do not exceed 10 mg once daily.
Supplied: 5 mg, 10 mg, 20 mg, 40 mg tablet.

Dose dependent changes (Associate lower end of range with lower dosage):
LDL: 
45-63%    HDL:  8-14%      TG: 10-35%

simvastatin
Zocor ® 
 Initially: 20 mg orally every evening.   Max: 80 mg/day.
Dose dependent changes
(Associate lower end of range with lower dosage):
LDL: 
26-47%    HDL:  8-16%     TG: 12-33%

Combination products

Advicor ®
lovastatin +
niacin SR
Indicated for the treatment of primary hypercholesterolemia (heterozygous familial and nonfamilial) and mixed dyslipidemia.  Usual initial dose: 500 mg/20 mg.  The dose of Advicor should not be increased by more than 500 mg daily (based on the niacin component) every 4 weeks.  Doses > 2000 mg/40 mg daily are not recommended.

Supplied
: 20/500, 20/750mg, 20/1000mg tablet.
Vytorin ®
simvastatin +
ezetimibe
HMG-CoA reductase inhibitor + cholesterol absorption inhibitor.   Usual initial dose: Ezetimibe 10 mg and simvastatin 20 mg once daily in the evening.  Patients who require >55% reduction in LDL-C: Initial: Ezetimibe 10 mg and simvastatin 40 mg once daily.Renal dosing: In severe dysfunction, start only if patient tolerates 5 mg daily of simvastatin. Monitor closely.  Supplied: ( Ezetimibe / simvastatin)  10/10 , 10/20,  10/4010/80.

Dose dependent changes (Associate lower end of range with lower dosage):
LDL: 
45-60%    HDL:  6-10%     TG: 23-31%

Other

ezetimibe
Zetia ®
Selective cholesterol absorption inhibitor.
Adult (usual): Hypercholesterolemia: 10 mg po qd.

Moderate reductions in low-density lipoprotein (LDL) cholesterol (less than 20%) have been reported with monotherapy in patients with hypercholesterolemia. As add-on therapy, it may enable reduced doses of statins. The drug is approved for primary hypercholesterolemia, for homozygous familial hypercholesterolemia (combined with atorvastatin or simvastatin), and for homozygous sitosterolemia.
Supplied: 10 mg tablet.

LDL:  19%    HDL:  5%     TG: 11%

Reference(s)

National Institutes of Health, U.S. National Library of Medicine, DailyMed Database.
Provides access to the latest drug monographs submitted to the Food and Drug Administration (FDA). Please review the latest applicable package insert for additional information and possible updates.  A local search option of this data can be found here.

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