|
Bile acid
sequestrants: TOP
|
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. ] |
TOP
|
Fibrates:
TOP
|
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. |
TOP
|
Niacin:
TOP
|
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% |
TOP
TOP
|
Combination products:
TOP
|
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, 10/40,
10/80.
Dose
dependent changes (Associate
lower end of range with lower dosage):
LDL: 45-60%
HDL: 6-10%
TG: 23-31% |
|
Other:
TOP
|
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% |
TOP
|
