| Natural products to lower
cholesterol levels - Don't forget niacin
There are a number of specific natural medicines that effectively
lower cholesterol levels. Since new ones come along all the time
(see previous
newsletter on Delta-tocotrienol - The 21st Century Vitamin
E?) it is easy to forget just how impressive the results
are with niacin.
Before taking a look at the effects of niacin in lowering cholesterol
levels, it is important to have an understanding of exactly what
all the different forms of cholesterol represent. First of all,
cholesterol is a natural substance made by the liver to serve several
important body function including being the backbone for important
hormones like estrogen, testosterone, and cortisone.
Cholesterol travels from the liver and into your circulation by
hitching a ride on protein molecules called low-density lipoprotein
(LDL), often called "bad cholesterol." It is carried away
from tissues and back to the liver aboard high-density lipoprotein
(HDL) ("good" or "protective cholesterol").
Some people find it easier to remember the difference by labeling
LDL "lousy" and HDL "healthy or happy."
The more LDL you have, the more cholesterol is in circulation,
and the greater your risk of heart disease. Currently, experts recommend
that your total blood cholesterol level should be less than 200
mg/dl. The LDL level should be less than 130 mg/dl and the HDL level
should be greater than 35 mg/dl. For every one percent drop in LDL
levels, there's a two percent drop in the risk of heart attack.
By the same token, for every one percent increase in HDL, the risk
of heart attack drops three or four percent.
The ratio of your total cholesterol to HDL and the ratio of LDL
to HDL are clues that indicate whether cholesterol is being deposited
into tissues or is being broken down and excreted. The ratio of
total cholesterol to HDL should be no higher than 4.2, and the LDL-to
HDL ratio should be no higher than 2.5.
Another important lipoprotein to be aware of is a form of LDL called
lipoprotein (a), or Lp(a). This form of LDL has an additional molecule
of an adhesive protein called apolipoprotein. That protein makes
the molecule much more likely to stick to the artery walls and cause
damage. New research suggests that high Lp(a) levels constitute
a separate risk factor for heart attack. For example, it appears
that high Lp(a) levels are ten times more likely to cause heart
disease than high LDL levels. Lp(a) levels lower than 20 mg/dl are
associated with low risk of heart disease; levels between 20 and
40 mg/dl pose a moderate risk, and levels higher than 40 mg/dl are
considered extremely risky.
Niacin does more than lower cholesterol
The cholesterol lowering activity of niacin was first described
in the 1950s. It is now known that niacin does much more than lower
total cholesterol. Specifically, niacin has been shown to lower
LDL cholesterol, Lp(a) lipoprotein, triglyceride, and fibrinogen
levels while simultaneously raising HDL cholesterol levels. Despite
the fact that niacin has demonstrated better overall results in
reducing risk factors for coronary heart disease compared with other
cholesterol-lowering agents, physicians are often reluctant to prescribe
niacin. The reason is a widespread perception that niacin is a difficult
to work with because of the bothersome flushing of the skin. In
addition, since niacin is a widely available "generic"
agent, no pharmaceutical company stands to generate the huge profits
that the other lipid-lowering agents have enjoyed. As a result,
niacin does not benefit from the intensive advertising that focuses
upon the "statin" drugs. Despite the advantages of niacin
over other lipid-lowering drugs, it accounts for less than 10% of
all cholesterol-lowering prescriptions.
Several studies have compared niacin to standard lipid-lowering
drugs including the statin drugs. These studies have shown significant
advantages for niacin. For example, in one 26 week study patients
were randomly assigned to receive treatment with either lovastatin
(Mevacor) or niacin.1 The results
are shown below:
Lovastatin vs. Niacin in a 26-Week Study

These results indicate that while lovastatin produced a greater
LDL cholesterol reduction, niacin provided better overall results
despite the fact that fewer patients were able to tolerate a full
dosage of niacin because of skin flushing. The percentage increase
in HDL cholesterol, a more significant indicator for coronary heart
disease, was dramatically in favor of niacin (33 vs. 7%). Equally
as impressive was the percentage decrease in Lp(a) for niacin. While
niacin produced a 35% reduction in Lp(a) lipoprotein levels, lovastatin
did not produce any effect. Other studies have shown that niacin
can lower Lp(a) levels by an average of 38%.2,3
The most recent comparative study involved niacin vs. atorvastatin
(Lipitor).4 The average dosage
was 3,000 mg with niacin and 80 mg for atorvastatin was used at
80 mg/day. The patients selected had abnormal particle size of LDL
in that the molecules were small and dense - these LDL molecules
are considerably more atherogenic than larger, less dense LDL. The
patients selected also had low levels (less than 40%) of a specific
fraction of HDL associated with a greater protective effect than
HDL alone. Although atorvastatin reduced total LDL cholesterol levels
substantially more than niacin, niacin was more effective in increasing
LDL particle size and raising HDL and HDL2 than the atorvastatin.
Table 1. The Effect of Atorvastatin
(Lipitor) and Niacin on Lipid Profiles
| Parameter |
Atorvastatin |
Niacin |
Atorvastatin
+ Niacin |
| |
Before |
After |
Before |
After |
Before |
After |
| Total LDL (mg/dl) |
110 |
56 |
111 |
89 |
123 |
55 |
| LDL peak diameter |
251 |
256 |
253 |
263 |
250 |
263 |
| Lipoprotein (a) (mg/dl) |
45 |
44 |
37 |
23 |
54 |
35 |
| HDL (mg/dl) |
42 |
43 |
38 |
54 |
38 |
54 |
| HDL2 (%) |
30 |
42 |
29 |
43 |
32 |
37 |
| Triglycerides (mg/dl) |
186 |
100 |
194 |
108 |
235 |
73 |
While statin drugs are also gaining popularity as a prescription
method to lower C-reactive protein (CRP) - a marker of inflammation
and a risk factor for heart disease. It appears that the while majority
of physicians appear to be aware of the effect of Lipitor and Pravachol
on C-reactive protein they do not seem to be aware that natural
products offer even greater activity. For example, vitamin E (800
IU daily) lowered C-reactive protein by 49% and niacin (1500 mg
at night) lowered it by 20%, much more meaningful reductions than
those seen with Pravachol and Lipitor.5,6
Because taking niacin at higher dosages (e.g., 3,000 mg or more)
can impair glucose tolerance, many physicians have avoided niacin
therapy in diabetics, but newer studies with slightly lower dosages
(1,000 to 2000 mg) of niacin have not shown it to adversely effect
blood sugar regulation.7 For
example, during a 16-week, double-blind, placebo-controlled trial,
148 type 2 diabetes patients were randomized to placebo or 1000
or 1500 mg/d of niacin; in the niacin treated groups there was no
significant loss in glycemic control and the favorable effects on
blood lipids were still apparent.8
Other studies have actually shown hemoglobin A1C to drop indicating
improvement in glycemic control.9
If you take a look at the most common blood lipid abnormality in
type 2 diabetic patients it is elevated triglyceride levels, decreased
HDL cholesterol levels, and a preponderance of smaller, denser LDL
particles. Niacin has been shown to address all of these areas much
more significantly than the statin or other lipid lowering drugs.
However, one of the reasons that niacin may not be as popular as
it should be is the bothersome side effect of skin flushing - kind
of like a prickly, heat rash that typically occurs 20-30 minutes
after the niacin is taken and disappears in about the same time
frame. Other occasional side-effects of niacin include gastric irritation,
nausea, and liver damage.
To reduce the side effect of skin flushing you can use some of
the newer time-released formulas including the prescription version
Niaspan or take the niacin just before going to bed. Most people
sleep right through the flushing reaction. Taking cholesterol lowering
agents at night is best because most of the cholesterol manufactured
by the liver happens at night. Another approach to reduce flushing
is to use inositol hexaniacinate. This form of niacin has long been
used in Europe to lower cholesterol levels and also to improve blood
flow in intermittent claudication - a peripheral vascular disease
that is quite common in diabetes. It yields slightly better clinical
results than standard niacin, but is much better tolerated, in terms
of both flushing and, more importantly, long-term side-effects.10
If you start out with trying inositol hexaniacinate and it does
not work, try regular niacin. Our experience is that some people
will only respond to the regular niacin.
If regular niacin or inositol hexaniacinate is being used, start
with a dose of 500 mg at night before going to bed for one week.
Increase the dosage to 1,000 mg the next week and 1,500 mg the following
week. Stay at the 1,500 mg dosage for two months before checking
the response - dosage can be adjusted up or down depending upon
the response. If you are using a time-release niacin product, like
Niaspan, start out at the full dosage of 1,500 mg at night.
Regardless of the form of niacin being used, I strongly recommend
periodic checking (minimum every 3 months) of cholesterol. A1C,
and liver function tests.
Key References:
- Illingworth DR et al. Comparative effects of lovastatin and
niacin in primary hypercholesterolemia. Arch Intern Med 1994;
154: 1586-1595
- Carlson LA, Hamsten A, Asplund A. Pronounced lowering of serum
levels of lipoprotein Lp(a) in hyperlipidaemic subjects treated
with nicotinic acid. J Intern Med 1989; 226: 271-276.
- Pan J, Lin M, Kesala RL, Van J, Charles MA. Niacin treatment
of the atherogenic lipid profile and Lp(a) in diabetes. Diabetes
Obes Metab 2002;4:255-61.
- Van JT, Pan J, Wasty T, et al. Comparison of extended-release
niacin and atorvastatin monotherapies and combination treatment
of the atherogenic lipid profile in diabetes mellitus. Am J Cardiol
2002;89:1306-8.
- Upritchard JE, Sutherland WH, Mann JI. Effect of supplementation
with tomato juice, vitamin E, and vitamin C on LDL oxidation and
products of inflammatory activity in type 2 diabetes. Diabetes
Care 2000;23:733-8.
- Grundy SM, Vega GL, McGovern ME, et al. Efficacy, safety, and
tolerability of once-daily niacin for the treatment of dyslipidemia
associated with type 2 diabetes: results of the assessment of
diabetes control and evaluation of the efficacy of Niaspan trial.
Arch Intern Med 2002;162:1568-76.
- Rindone JP, Achacoso S. Effect of low-dose niacin on glucose
control in patients with non-insulin-dependent diabetes mellitus
and hyperlipidemia. Am J Ther 1996;3:637-639.
- Grundy SM, Vega GL, McGovern ME, et al. Efficacy, safety, and
tolerability of once-daily niacin for the treatment of dyslipidemia
associated with type 2 diabetes: results of the assessment of
diabetes control and evaluation of the efficacy of Niaspan trial.
Arch Intern Med 2002;162:1568-76.
- Kane MP, Hamilton RA, Addesse E, Busch RS, Bakst G. Cholesterol
and glycemic effects of Niaspan in patients with type 2 diabetes.
Pharmacotherapy 2001;21:1473-8.
- El-Enein AMA. The role of nicotinic acid and inositol hexaniacinate
as anticholesterolemic and antilipemic agents. Nutr Rep Intl 1983;
28: 899-911.
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