Fight Cholesterol with Niacin

Posts Tagged ‘nicotinic acid’

Nicotinic acid: an old drug with a promising future

Wednesday, December 31st, 2008

by ET Bodor and S Offermanns
Institute of Pharmacology, University of Heidelberg, Im Neuenheimer Feld, Heidelberg, Germany - British Journal of Pharmacology (2008) 153, S68–S75; doi:10.1038/sj.bjp.0707528

Excerpts from…

• Nicotinic acid has been used for decades to treat dyslipidaemic states. In particular its ability to raise the plasma HDL cholesterol concentration has led to an increased interest in its pharmacological potential. The clinical use of nicotinic acid is somewhat limited due to several harmless but unpleasant side effects, most notably a cutaneous flushing phenomenon.

• Nicotinic acid has profound and unique effects on lipid metabolism and is thus referred to as a ‘broad-spectrum lipid drug’ (Carlson, 2005). In addition to elevating HDL cholesterol (Parsons and Flinn, 1959; Shepherd et al., 1979) as well as decreasing both LDL and total cholesterol (Altschul et al., 1955; Carlson et al., 1977), nicotinic acid also induces a decrease in the concentrations of both ‘very-low-density lipoproteins’ (VLDL) and plasma triglyceride (TG) (Table 1; Carlson et al., 1989).
• The plasma concentration of lipoprotein Lp(a), which has been suggested to play a role as an independent risk factor for coronary heart disease, is also decreased by nicotinic acid (Carlson et al., 1989; Berglund and Ramakrishnan, 2004).

Soon after the initial discovery of the lipid-modifying effect of high doses of nicotinic acid (Altschul et al., 1955), the water-soluble vitamin nicotinic acid was introduced into clinical therapy as the first lipid-modifying drug.

• In the Coronary drug project, conducted from 1966 to 1975, nicotinic acid administered as monotherapy at 3 g day_1 was shown to lead to an efficient secondary prevention of myocardial infarction (Table 2) (Coronary Drug Project Research Group, 1975).

A follow-up study of the Coronary Drug project revealed that nicotinic acid also reduced the mortality of patients who had been treated with nicotinic acid (Canner et al., 1986). The Stockholm ischaemic heart disease secondary prevention study came to similar findings (Carlson and Rosenhamer, 1988).

• The most rapid effect of nicotinic acid on lipid metabolism is a decrease in plasma levels of free fatty acid, which can be observed within minutes upon administration of the drug.

• Nicotinic acid, when given at pharmacological doses, has several unwanted yet harmless effects. The most common and most prominent unwanted effect of nicotinic acid is a cutaneous vasodilation, most prominently in the upper half of the body and in the face, which lasts for 1–2 h after an oral dose of nicotinic acid (Goldsmith and Cordill, 1943). This cutaneous reaction, called flushing, is relatively unpleasant and therefore negatively influences patients’ compliance.
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Tags: cholesterol, Enduracin, flushing, lipid, lipoprotein Lp(a), niacin, nicotinic acid, triglyceride
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Reducing risk by raising HDL-cholesterol: the evidence

Sunday, September 28th, 2008

Heinz Drexel

Vorarlberg Institute for Vascular Investigation and Treatment (VIVIT), Academic Hospital, Carinagasse 47, A-6807, Feldkirch, Austria

Low HDL-cholesterol is common among patients with cardiovascular disease. Well-designed epidemiological studies carried out over the previous three decades have defined the prognostic significance of low HDL-cholesterol.

Indeed, a recent valuation of patients undergoing coronary angiography showed that factors related o HDL-cholesterol, but not to LDL-cholesterol, were primarily responsible for driving the elevated risk of atherosclerosis and cardiovascular events associated with dysglycaemia within this population.

Randomized intervention studies have demonstrated significant inhibition of atherosclerosis and/or improvement in cardiovascular event rates with treatments that increase HDL-cholesterol (nicotinic acid or a fibrate).

Nicotinic acid is the most powerful HDL-cholesterol raising agent currently available, and a combination of this agent with a statin facilitates simultaneous control of both HDL-cholesterol and LDL-cholesterol. Indeed, the HDL Atherosclerosis Treatment Study demonstrated a reduction in major cardiovascular events of 90% vs. placebo in patients randomized to nicotinic acid & simvastatin.

In addition, patients randomized to nicotinic acid in the Coronary Drug Project benefited from a significant reduction in mortality after 15 years, 9 years after the trial ended.

A new prolonged-release formulation of nicotinic acid, Niaspanw, has superior tolerability compared with immediate-release nicotinic acid and facilitates the delivery of this therapy. The evidence base supporting intervention to correct low HDL-cholesterol in addition to reducing LDL-cholesterol is now sufficiently strong to support the introduction of this strategy into routine clinical practice.
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Tags: Atherosclerosis, cardiovascular, Enduracin, fibrate, HDL cholesterol, nicotinic acid, simvastatin
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Interview: Nicotinic Acid – The New Old Wonder Drug

Thursday, September 4th, 2008

Below, H. Robert Superko, MD., F.A.C.C. is interviewed by C. Richard Conti, MD., M.A.C.C.Dr. Conti is Eminent Scholar, Cardiology; Prof of MedicineUniversity of Florida College of MedicineDr.Superko is Chairman, Molecular,Genetic, and Preventive CardiologySaint Joseph Hospital, Atlanta, GA

Yes, niacin requires some extra time for you or your nurses, in order to get good compliance from your patients. But the important thing to remember is that niacin addresses a much larger medical problem than the LDL problem. Plus, we have some niacin formulations that are better tolerated and there is more of a push from the scientific medical community that this is the right thing to do in the appropriate patient population.

…If we’re talking to patients with coronary disease, they need to realize they have a deadly disease. You can make an analogy with cancer; if you have cancer and I give you a drug that’s going to extend or maybe save your life, but you’re going to flush a little bit, I suspect patients would take it. We need to look at coronary disease the same way. We have to be very aggressive and, if necessary, tolerate some minor side effects, because it’s going to extend their life and maybe even stop progression of their disease.

Dr. Conti:I’m Richard Conti with Robert Superko. Rob is executive director of the Center for Genomics and Human Health at St. Joseph’s Translational Research Institute in Atlanta, Georgia. We’re talking about, “Nicotinic Acid: The New Old Wonder Drug.” We’re going to review some of the history of nicotinic acid; talk about mechanism of action; discuss why it’s not been used very often in the past; and then look at the clinical evidence of its success. Robert, let’s start with the history.

Dr. Superko:It was 1955 when Altschul first reported that nicotinic acid lowers blood cholesterol in humans12 and since then a whole series of clinical trials and basic science research has progressed. In 2001, Lorenzen discovered a nicotinic acid receptor.13 So there’s a long, long history of both scientific and clinical use of this compound.

Dr. Conti:What about its mechanism of action?

Dr. Superko:The mechanism of action was not known for many years; it was simply known to improve cholesterol, particularly it lowered triglycerides and raised HDL. Now the mechanism has been worked out with the recent identification of a nicotinic acid receptor. It’s a G-coupled protein receptor and, interestingly, at least four SNPs and five haplotypes have been identified. This means people respond to nicotinic acid very differently, in part due to genetic reasons.One thing it does is inhibit free-fatty acid mobilization from fat tissues and this accounts for the triglyceride reduction, but it also has a powerful impact on HDL by inhibiting the degradation or removal of apo A1. That’s primarily why it raises HDL cholesterol so dramatically, particularly the really beneficial HDL2.

Dr. Conti:Robert, why has the pharmaceutical industry tried to develop a drug that raises HDL when we already have a drug that raises HDL?

Dr. Superko:If we look at the clinical trial evidence, it was primarily developed through the NIH and through studies in Europe; very little of it was done by pharmaceutical companies. Yet the evidence is overwhelming that if you combine HDL raising with LDL lowering you get profoundly better results than LDL lowering alone.This was obvious to everybody in the field, including people in the pharmaceutical industry. The problem was that the best drug in the world for raising HDL was nicotinic acid, a simple compound for which no one held a patent or had any kind of intellectual property. It was not until a company that’s now been sold to Abbott, called Kos, started developing a better form of niacin several years ago that commercial interest took off.Now we have Abbott providing a very effective delayed-release or time-released nicotinic acid and Merck is working on another version. Consequently, we may see a lot of competition soon and many physicians will be invited to a lot more nicotinic acid dinner talks. Also, there are a few products coming out that involve different combinations of a statin plus nicotinic acid.

Dr. Conti:Over the years that I’ve been using nicotinic acid, it hasn’t been commonly used by most physicians. What was the reason for that? Was it because of the flushing or because it wasn’t marketable in a big pharmaceutical business sort of way?

Dr. Superko:In the past, we were using 4 or 5 grams of immediate-release niacin a day. It was very effective and was absolutely the right thing to do in the appropriate patient, but it took a fair amount of effort. You had to talk to the patient a lot; they’d come back – you’d hear the flushing complaint, which is the one most people appreciate. It certainly was not an easy drug to use compared to the statins.Around this time the LRC-CPPT (Lipid Research Clinics Coronary Primary Prevention Trial) was completed and the whole field of lowering LDL cholesterol took off. Subsequently, we’ve had tremendous success designing drugs that primarily lower LDL cholesterol – the statins – that are well tolerated with very few side effects. As physicians, we have gotten used to the concept of, “Let me give you this pill. You’re not likely to have any side effects.” The numbers look better on the lab report and we think we’ve done our job. Yet, we’ve known for 20 years that LDL cholesterol is not the most common cause of coronary disease; it’s the triglyceride-rich particles and the low HDLs, that are more common and more important — and statins don’t address them adequately.Yes, niacin requires some extra time for you or your nurses in order to get good compliance from your patients, but the important thing to remember is that niacin addresses a much larger medical problem than the LDL problem. Plus, we have some niacin formulations that are better tolerated and there is more of a push from the scientific medical community that this is the right thing to do in the appropriate patient population.

Dr. Conti:Why don’t you tell our audience the David Blankenhorn story?Dr. Superko:Dave Blankenhorn unfortunately passed away recently; a great man who did the CLAS (Cholesterol Lowering Atherosclerosis Study I and II) trial. The average dose of nicotinic acid in the CLAS trial was about 5 grams per day. That’s a high dose and Dave told me that patients would come in and complain about the flushing. Dave would open up their shirt and point to the bypass scar on their chest and say, “Hey, do you want another one of these?” In other words, “Do you want surgery or do you want to put up with a little flushing?” The patients put up with the flushing.

Dr. Conti:A good story. Let’s review some of the clinical evidence for success with this drug.

Dr. Superko:The clinical evidence goes back a long way to the Stockholm Heart Study, a non-randomized study that showed about a 26% mortality reduction associated with nicotinic acid.14 The evidence proceeds through the Coronary Drug Project and finally into the NIH trials – Greg Brown’s FATS and HATS trial and our ownSCRIP study.If you line these studies up and compare them against the statin studies, you would ask, “What’s the reduction in clinical events?” In the statin studies you get about a 25% relative risk reduction – not absolute, but relative: and that’s considered a success. If you look at the combination studies that used, for example, a resin and niacin or a statin and niacin, you get an 80-90% risk reduction; far, far better. If you look at the arteriographic studies using QCA, statins reduce the rate of disease progression but there’s essentially no regression. It’s only in the combination studies that used niacin and an LDL-lowering agent that you actually got arteriographic regression.By any parameter of success, the combination of adding nicotinic acid to an LDL-lowering program is overwhelmingly successful and I’ve just been amazed that this has not been embraced by the cardiology community over the past 10-15 years.

Dr. Conti:Yes, it is amazing. I guess it all boils down to side effects; people don’t like them and doctors don’t like patients complaining about side effects. I’ve used the old trick of telling my patients, “Well, you’re flushing. You’re flushing the bad cholesterol right out of your system,” and that seems to work in some cases.

Dr. Superko:That’s a good analogy. If we’re talking to patients with coronary disease, they need to realize they have a deadly disease. You can make an analogy with cancer; if you have cancer and I give you a drug that’s going to extend or maybe save your life but you’re going to flush a little bit, I suspect patients would take it. We need to look at coronary disease the same way. We have to be very aggressive and, if necessary, tolerate some minor side effects, because it’s going to extend their life and maybe even stop progression of their disease.

Dr. Conti:We’ll end this discussion on that wise advice, Robert. Thank you very much for coming and discussing this with our ACCEL audience.

Dr. Superko:Thank you, Dick. It’s always a pleasure.

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Tags: cardiovascular, cholesterol, flushing, HDL cholesterol, niacin, nicotinic acid
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What Should I Know About Niacin Preparations and Dyslipidemia?

Friday, March 14th, 2008

Ask the Experts about Cardiology for Advanced Practice Nurses
From Medscape Nurses

Question…
I have read conflicting reports regarding the use of various niacin preparations for dyslipidemia. Would you describe the effectiveness of niacin, nicotinic acid, inositol, and niacinamide?

WL Edwards Response from W. Lane Edwards, Jr., MSN, ARNP, ANP
Nurse Practitioner, Internal Medicine, Ft. Myers, Florida

You have asked an excellent and timely question, as the data from the Arterial Biology for the Investigation of the Treatment Effects of Reducing Cholesterol (ARBITER 2) study provide an excellent look at the impact of combination therapy for the treatment of dyslipidemias.^[1] ARBITER 2 has shown us that the addition of extended-release niacin ( Niaspan ) 1000 mg to statin therapy for the treatment of dyslipidemias slows the progression of atherosclerosis compared with statin monotherapy in patients with coronary artery disease and low levels of high-density lipoprotein.^[1]

Niacin is a water-soluble B vitamin and the common name for 2 very different compounds: nicotinic acid (used for cholesterol management) and niacinamide (used for those with diabetes/arthritis). Three preparations of nicotinic acid (which have been used for cholesterol management) are available as nutritional supplements or prescription medications: immediate-release ( Niacor ), extended-release ( Niaspan, Advicor — by prescription), and slow-release ( Endur-Acin ), and inositol niacinate ( Niacinol ), to name a few. READ FULL TEXT - PDF

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Tags: cholesterol, Dyslipidemia, inositol, niacin, niacinamide, nicotinic acid
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First presented in 1999 to leading cardiovascular specialists in Moscow, Russia

Saturday, December 8th, 2007

Wax-Matrix Sustained-Release Nicotinic Acid

Joseph M. Keenan, M.D.
Professor, University of Minnesota
Department of Family Practice

INTRODUCTION:
Today we have more options than ever for the pharmacological management of hyperlipemia. Some of the newer agents have unprecedented potency in lowering LDL cholesterol while others may be better at reducing triglycerides or improving HDL. Keeping track of which drugs are best for which lipid problems can be a challenge in the everyday practice of medicine. I offer here a simple rationale for selecting a first choice in lipid management. If you follow this rationale I think you will find that nicotinic acid or niacin is the best first choice, and that among the niacin preparations wax-matrix CNA (controlled release niacin) is by far the best available.
SELECTING A LIPID LOWERING DRUG:. . .

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Tags: cholesterol, controlled release, Enduracin, HDL, hyperlipemia, LDL, lipid management, lipoproteins, niacin, nicotinic acid, triglycerides, Uncategorized, Wax-matrix
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