Niacin Technical Reports
Top Of Page
| Number |
Title |
Karl Loren Comments |
| One |
Membrane fatty acids, niacin flushing and clinical parameters. |
Here is a technical, but useful, mechanical explanation of
"flushing." |
| Two |
Release of markedly increased quantities of prostaglandin D2 in vivo in
humans following the administration of nicotinic acid. |
More on the mechanics of the "flush." |
| Three |
A comparison between nicotinic acid and acipimox in
hypertriglyceridaemia--effects on serum lipids, lipoproteins, glucose tolerance and
tolerability. |
The dose was stupid -- 3,000 mg per day! But, the study at least
shows that niacin reduces cholesterol levels. |
| Four |
Preliminary report of the effects of propranolol HCl on the discomfiture
caused by niacin. |
They have found a way to reduce the flush from niacin -- thereby losing
the most important advantage of niacin! |
| Five |
Reduced levels of prostaglandin precursors in the blood of atopic
patients: defective delta-6-desaturase function as a biochemical basis for atopy. |
|
| Six |
Schizophrenia: a biochemical disorder? |
|
| Seven |
Drug and nutrient interactions in the elderly diabetic. |
|
| Eight |
New developments in the use of niacin for treatment of hyperlipidemia: new
considerations in the use of an old drug. |
A very favorable report on how niacin reduces cholesterol levels -- with
an absurd dosage being administered. And, the "required" warning that the
flush is bad. Here's a quote. "Niacin has been used for many years to treat
hyperlipidemia. It has been shown to reduce coronary death and non-fatal myocardial
infarction and, in a separate analysis of long-term (15-year) follow-up, all cause
mortality. It reduces total cholesterol, low density lipoprotein cholesterol (LDL-C) and
triglycerides and increases high densit lipoprotein cholesterol (HDL-C)." |
| Nine |
Fluvastatin with and without niacin for hypercholesterolemia. |
Another favorable report on niacin -- but, again, coupled with warnings.
This report, like many others, shows that a "regular"
cholesterol-lowering drug works "better" with niacin added. |
| Ten |
Combination of low-dose niacin and pravastatin improves the lipid profile
in diabetic patients without compromising glycemic control. |
Another report on how a drug works better with niacin added. |
| Eleven |
Bioavailability of niacin. |
Report Is Missing -- references only. |
| Twelve |
Niacin for lipid disorders. Indications, effectiveness, and safety. |
"Niacin can be very effective and safe in lowering low-density
lipoprotein cholesterol and triglyceride levels and also in increasing high-density
lipoprotein cholesterol levels. In combination with other lipid-lowering drugs (eg, bile
acid sequestrants), it has reduced the incidence of cardiovascular events and stopped the
progression of coronary artery lesions. It may be the most cost-effective lipid-lowering
agent currently available. At lower doses, sustained-release forms of niacin may also
improve patient compliance. " |
-
- Record 1
- Title
- Membrane fatty acids, niacin flushing and clinical parameters.
- Author
- Glen AI; Cooper SJ; Rybakowski J; Vaddadi K; Brayshaw N; Horrobin DF
- Address
- Highland Psychiatric Research Group, Craig Dunain Hospital, Inverness, UK.
- Source
- Prostaglandins Leukot Essent Fatty Acids, 1996 Aug, 55:1-2, 9-15
- Abstract
- Clinical definitions of schizophrenia are unreliable and difficult to use. The niacin
flush test, which involves prostaglandin-induced vasodilatation, offers a method of
exploring essential fatty acid metabolism in schizophrenic patients and may serve to
define a subgroup of patients. In a multicentre study of schizophrenic patients with
negative symptoms, we have examined the clinical accompaniments of the niacin response.
Patients failing to flush with niacin showed significantly reduced levels of arachidonic
and docosahexaenoic acids. Conversion from non-flushing to flushing during the 6 month
supplementation period was predicted by an increase in arachidonic acid levels in red
blood cell membranes irrespective of nature of supplementation. In this study, patients
were selected for their negative symptoms and, therefore, it was not surprising that
further measures of negative or positive symptoms did not predict flushing. However, an
increased score for affective symptoms was significantly associated with a positive flush
response. The stability of the niacin test needs to be examined in relation to the
periodicity of symptoms in schizophrenia and manic depressive illness. New information on
the anandamide system suggests that it may be associated with periodic phenomena and
should be investigated in relation to the niacin test.
- Language of Publication
- English
- Unique Identifier
- 97042919
- Record 2
Title
- Release of markedly increased quantities of prostaglandin D2 in vivo in humans following
the administration of nicotinic acid.
- Author
- Morrow JD; Parsons WG 3d; Roberts LJ 2d
- Address
- Department of Pharmacology, Vanderbilt University, Nashville, TN 37232.
- Source
- Prostaglandins, 1989 Aug, 38:2, 263-74
- Abstract
- Nicotinic acid (niacin) is a B vitamin which is also a potent hypolipidemic agent.
However, intense flushing occurs following ingestion of pharmacologic doses of niacin
which greatly limits its usefulness in treating hyperlipidemias. Previous studies have
demonstrated that niacin-induced flushing can be substantially attenuated by pre-treatment
with cyclooxygenase inhibitors, suggesting that the vasodilation is mediated by a
prostaglandin. However, the prostaglandin that presumably mediates the flush has not been
conclusively determined. In this study we report the finding that ingestion of niacin
evokes the release of markedly increased quantities of PGD2 in vivo in humans. PGD2
release was assessed by quantification of the PGD2 metabolite, 9 alpha, 11 beta-PGF2, in
plasma by gas chromatography mass spectrometry. Following ingestion of 500 mg of niacin in
three normal volunteers, intense flushing occurred and plasma levels of 9 alpha, 11
beta-PGF2 were found to increase dramatically by 800, 430, and 535-fold. Levels of 9
alpha, 11 beta-PGF2 reached a maximum between 12 and 45 min. after ingesting niacin and
subsequently declined to near normal levels by 2-4 hours. Levels of 9 alpha, 11 beta-PGF2
in plasma correlated with the intensity and duration of flushing that occurred in the 3
volunteers. Release of PGD2 was not accompanied by a release of histamine which was
assessed by quantification of plasma levels of the histamine metabolite, N
tau-methylhistamine. This suggests that the origin of the PGD2 release is not the mast
cell. Only a modest increase (approximately 2-fold) in the urinary excretion of the
prostacyclin metabolite, 2,3-dinor-6-keto-PGF1 alpha, occurred following ingestion of
niacin and no increase in the excretion of the major urinary metabolite of PGE2 was found.
These results indicate that the major vasodilatory PG released following ingestion of
niacin is PGD2. The fact that markedly increased quantities of PGD2 are released suggests
that PGD2 is the mediator of niacin-induced vasodilation in humans.
- Language of Publication
- English
- Unique Identifier
- 89367978
- Record 3
Title
- A comparison between nicotinic acid and acipimox in hypertriglyceridaemia--effects on
serum lipids, lipoproteins, glucose tolerance and tolerability.
- Author
- Tornvall P; Walldius G
- Address
- Department of Internal Medicine, Karolinska Hospital, Stockholm, Sweden.
- Source
- J Intern Med, 1991 Nov, 230:5, 415-21
- Abstract
- Serum and lipoprotein lipid levels, oral glucose tolerance and side-effects were
compared in an open cross-over study of 31 non-diabetic patients with
hypertriglyceridaemia (type II B and IV) before and after 6 weeks of treatment with
nicotinic acid (3 g daily) and acipimox (0.75 g daily), a new nicotinic acid-like drug,
respectively. Acipimox was about equally potent in reducing serum and VLDL lipid levels
and in increasing HDL cholesterol levels. Acipimox had no significant negative effects on
glucose metabolism measured by an oral glucose tolerance test compared with nicotinic
acid, which decreased the late glucose tolerance as well as the area under the glucose
curve (P less than 0.05 for the difference between the two treatments). The incidence and
severity of flush or any other recorded side-effects was higher after nicotinic acid
treatment than after acipimox. In addition, no effects on laboratory parameters such as
liver enzymes and uric acid were seen after treatment with acipimox. The results of this
study demonstrate that acipimox is a satisfactory alternative to nicotinic acid in
patients with hypertriglyceridaemia.
- Language of Publication
- English
- Unique Identifier
- 92044282
[ Home ]
- Record 4
Title
- Preliminary report of the effects of propranolol HCl on the discomfiture caused by
niacin.
- Author
- Estep DL; Gay GR; Rappolt RT Sr
- Source
- Clin Toxicol, 1977, 11:3, 325-8
- Abstract
- Subjective discomfort caused by nausea and hot, pruritic skin has been described in
patients after ingestion of therapeutic dosages of niacin is shown by this study to be
alleviated by propranolol HC1. A dosage of 2 mg, I.V., given incrementally, in a clinical
trial of six patients is described. The peripheral vasodilator effects of niacin were
attenuated in some subjects but not in others. However, all subjects reported relief of
unpleasant symptoms. Serial vital signs were taken and no significant changes were found.
It is postulated that propranolol HC1 exerts a calmative effect at the CNS level. In a
series that utilized doses of 40 and 80 mg of propranolol HC1 taken orally 30 min prior to
the ingestion of 500 or 1000 mg of niacin, a progressive increase in the onset of the
niacin flush was observed. It is proposed that as the available plasma level of
propranolol HC1 falls, the ratio of niacin to propranolol HC1 increases, exceeding the
threshold at which the flush occurs. Both these studies suggest that further work is
indicated to establish the possible therapeutic efficacy of propranolol HC1.
- Language of Publication
- English
- Unique Identifier
- 78023258
- Record 5
- Title
Reduced levels of prostaglandin precursors in the blood of atopic patients: defective
delta-6-desaturase function as a biochemical basis for atopy.
Author
Manku MS; Horrobin DF; Morse N; Kyte V; Jenkins K; Wright S; Burton JL
Source
Prostaglandins Leukot Med, 1982 Dec, 9:6, 615-28
Abstract
In the plasma phospholipids of a group of 50 young adults with atopic eczema, there was
an elevation of cis-linoleic acid associated with a deficit of gamma-linolenic acid and of
the prostaglandin precursors, dihomogammalinolenic acid and arachidonic acid. This
suggests that atopics have a deficit in the function of the delta-6-desaturase enzyme
which converts linoleic acid to gamma-linolenic acid. Carriers of cystic fibrosis tend to
be phenotypically atopic, supporting previous suggestions that in homozygote cystic
fibrosis patients the key defect may be in the delta-6-desaturase enzyme. Atopic patients
may be exceptionally sensitive to side effects of non-steroidal anti-inflammatory agents.
They fail to flush in response to application of niacin compounds to the skin, a reaction
mediated by prostaglandins. A deficit of prostaglandin precursors would explain both of
these observations. That the observed biochemical deficit plays a causative role in the
manifestations of atopy was indicated by the fact that in a double-blind,
placebo-controlled crossover trial, gamma-linolenic acid in the form of evening primrose
oil (Efamol), partially corrected both the biochemical abnormalities and the clinical
state.
Language of Publication
English
Unique Identifier
- Record 6
Title
- Schizophrenia: a biochemical disorder?
- Author
- Horrobin DF
- Source
- Biomedicine, 1980 May, 32:2, 54-5
- Abstract
- There is evidence that schizophrenia may be related to excess biological activity of
dopamine, deficient synthesis of a prostaglandin and to the presence of a normal opioid in
excess or of an abnormal opioid. These three groups of observations seem to be
interrelated since opioids are able to inhibit the formation of prostaglandin E1 and
prostaglandin E1 and dopamine inhibit each other's effects. A low prostaglandin E1 level
will therefore produce and apparent dopamine excess. Niacin causes flushing, apparently by
stimulating production of prostaglandin E1. Much larger doses of oral niacin are required
to produce flushing in schizophrenics than in normal individuals. Most schizophrenics do
not flush when given 250 mg orally and this may be a simple biochemically-based test for a
major group of schizophrenics.
- Language of Publication
- English
- Unique Identifier
- 80221358
- Record 7
- Title
Drug and nutrient interactions in the elderly diabetic.
Author
Roe DA
Address
Division of Nutritional Sciences, Cornell University, Ithaca, NY 14853.
Source
Drug Nutr Interact, 1988, 5:4, 195-203
Abstract
Elderly diabetics take more drugs than other groups of elderly patients. Their multiple
drug use is largely explained by the drugs that they take for complications of their
primary disease; these include cardiovascular drugs for macrovascular disease and
antibiotics for secondary infections. They also take more drugs for control of other
conditions that are etiologically associated with the development and progression of their
diabetes, including antihypertensive agents, antilipemic agents and steroids, and
nonsteroidal antiinflammatory drugs (NSAIDs), which are taken for relief of joint pain
that is intensified by arthritic joints bearing excess weight. Drugs taken by elderly
diabetics that contribute to the high prevalence of drug-nutrient interactions include
those taken as antidiabetic agents, including both insulin and sulfonylureas as well as
calcium channel blockers; they also include thiazides, loop diuretics, sulfa drugs,
cephalosporin antibiotics, tetracyclines, antifungal agents, cholestyramine and
colestipol, niacin, prednisone and other corticosteroids, and NSAIDs. These drugs and drug
combinations contribute to the risk of hyperglycemia, which can cause nonketotic
hyperglycemia in the elderly; to the risk of hypoglycemia, which in the elderly carries
the risk of inducing pseudo-stroke; to the risk of drug-induced nutritional deficiencies
from antilipemics and cephalosporins, which can induce vitamin K deficiency; to the risk
of acute incompatibility reactions, including flush reactions from chlorpropamide, niacin,
and calcium channel blockers; and to the risk of edema, anemia, and hyperkalemia from
NSAIDs.(ABSTRACT TRUNCATED AT 250 WORDS)
Language of Publication
English
Unique Identifier
89196223
HealthGate Documents
Record 8 from database: MEDLINE
- Title
- New developments in the use of niacin for treatment of hyperlipidemia: new
considerations in the use of an old drug.
- Author
- Crouse JR 3rd
- Address
- Bowman Gray School of Medicine, Winston Salem, North Carolina 27157, USA.
- Source
- Coron Artery Dis, 1996 Apr, 7:4, 321-6
- Abstract
- Niacin has been used for many years to treat hyperlipidemia. It has been shown to reduce
coronary death and non-fatal myocardial infarction and, in a separate analysis of
long-term (15-year) follow-up, all cause mortality. It reduces total cholesterol, low
density lipoprotein cholesterol (LDL-C) and triglycerides and increases high densit
lipoprotein cholesterol (HDL-C). Sustained-release niacin may be associated with more
dramatic changes in LDL-C and triglyceride, whereas the short acting preparation causes
greater increases in HDL-C. The increase of HDL-C occurs at a lower dose (1500 mg/day)
than the reduction of LDL-C (> 1500 mg/day). Niacin also favorably influences other
lipid parameters including lipoprotein(a) [Lp(a)], alimentary lipemia, familial defective
apolipoprotein B-100 and small dense LDL. Combination of niacin with a bile acid
sequestrant or a reductase inhibitor represents a powerful lipid-altering regimen. Whereas
the reductase inhibitors and bile acid binding resins primarily affect LDL-C, the combined
therapy has a synergistic effect to reduce LDL-C and, in addition, the niacin reduces
triglycerides and increases HDL-C. The major drawback in the use of niacin is associated
side effects (flushing and palpitations) and toxicity (worsening of diabetes control,
exacerbation of peptic ulcer disease, gout, hepatitis). Niacin has a long history of use
as a lipid lowering agent and has several attractive features. Unfortunately, the side
effect profile of this agent warrants its use only in patients with marked dyslipidemia in
whom side effects and potential toxicity are closely monitored.
- Language of Publication
- English
- Unique Identifier
- 97006291
- MeSH Heading (Major)
- Antilipemic Agents|AD/PD/*TU; Hyperlipidemia|*DT; Niacin|AD/AE/PD/*TU
- MeSH Heading
- Apolipoproteins B|BL; Cholesterol|BL; Follow-Up Studies; Human; Lipoprotein(a)|BL;
Lipoproteins, HDL Cholesterol|BL; Lipoproteins, LDL Cholesterol|BL; Triglycerides|BL
- Publication Type
- JOURNAL ARTICLE; REVIEW; REVIEW LITERATURE
- ISSN
- 0954-6928
- Country of Publication
- UNITED STATES
Record 9 from database: MEDLINE
- Title
- Fluvastatin with and without niacin for hypercholesterolemia.
- Author
- Jacobson TA; Chin MM; Fromell GJ; Jokubaitis LA; Amorosa LF
- Address
- Department of Medicine, Emory University School of Medicine, Atlanta, Georgia 30303.
- Source
- Am J Cardiol, 1994 Jul, 74:2, 149-54
- Abstract
- Seventy-four patients with plasma low-density lipoprotein cholesterol levels > or =
160 mg/dl after an American Heart Association phase 1 diet were randomized to double-blind
treatment with fluvastatin, 20 mg/day, or placebo for 6 weeks. Immediate-release niacin
was then added to both treatment regimens and titrated to a maximum of 3 g/day for a
further 9 weeks. After 6 weeks of fluvastatin monotherapy, low-density lipoprotein
cholesterol levels decreased by 21% (p < 0.001 vs placebo), and after the addition of
niacin, response was potentiated to 40% compared with 25% for the niacin control group at
study end point (p < 0.001). Fluvastatin, alone and in combination with niacin, also
significantly improved high-density lipoprotein cholesterol (increases of about 30%) and
triglyceride profiles (decreases of approximately 28%) from baseline. Lipoprotein(a)
decreased by 37% in those receiving fluvastatin-niacin but was unaltered in those
receiving fluvastatin alone. No serious adverse events were ascribed to fluvastatin, and
no cases of myositis were observed. Small, transient, asymptomatic increases in aspartate
aminotransferase were noted with fluvastatin-niacin treatment but were not considered
clinically relevant. Although the fluvastatin-niacin combination in this study was without
evidence of significant transaminitis, myopathy, or rhabdomyolysis, it would seem prudent
to continue to monitor its safety with longer term use. In conclusion, fluvastatin, both
as monotherapy and in combination with niacin, proved to be an effective, safe, and
well-tolerated therapeutic alternative for hypercholesterolemia.
- Language of Publication
- English
- Unique Identifier
- 94295511
- MeSH Heading (Major)
- Anticholesteremic Agents|AD/AE/*TU; Fatty Acids, Monounsaturated|AD/AE/*TU;
Hypercholesterolemia|BL/DH/*DT; Indoles|AD/AE/*TU; Niacin|AD/AE/*TU
- MeSH Heading
- Adult; Aged; Alanine Transaminase|BL; Aspartate Transaminase|BL; Cholesterol|BL;
Double-Blind Method; Drug Combinations; Drug Tolerance; Female; Follow-Up Studies; Human;
Lipoprotein(a)|BL; Lipoproteins, HDL Cholesterol|BL; Lipoproteins, LDL Cholesterol|BL;
Male; Middle Age; Patient Compliance; Placebos; Triglycerides|BL
- Publication Type
- CLINICAL TRIAL; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
- ISSN
- 0002-9149
- Country of Publication
- UNITED STATES
Record 10 from database: MEDLINE
- Title
- Combination of low-dose niacin and pravastatin improves the lipid profile in diabetic
patients without compromising glycemic control.
- Author
- Gardner SF; Marx MA; White LM; Granberry MC; Skelton DR; Fonseca VA
- Address
- Department of Pharmacy Practice, College of Pharmacy, University of Arkansas for Medical
Sciences, Little Rock 72205, USA. gardner@cop.uams.edu
- Source
- Ann Pharmacother, 1997 Jun, 31:6, 677-82
- Abstract
- OBJECTIVE: To determine the efficacy and tolerability of the addition of low-dose niacin
(1.5 g/d) in a diabetic hypercholesterolemic population who were unable to attain desired
lipid control with low-dose (20 mg) pravastatin monotherapy. RESEARCH DESIGN AND METHODS:
This was a prospective, open-label study conducted over a 14-week period. Twenty-three
diabetic patients with low-density lipoprotein (LDL) cholesterol concentrations of at
least 150 mg/dL after dietary therapy were recruited from the outpatient diabetes clinic
of a university teaching hospital. After 4 weeks of dietary stabilization and baseline
determination of the lipid profile and glycemic control, patients received pravastatin 20
mg once daily for 4 weeks. Laboratory parameters were reassessed and niacin was added to
the regimen in qualifying patients. Over 2 weeks, patients' regimens were titrated to a
maximal dosage of 500 mg tid. Patients continued to receive the combination regimen for 4
weeks and were reassessed. MEASUREMENTS AND MAIN RESULTS: Sixteen patients (14
non-insulin-dependent diabetes mellitus, 2 insulin-dependent diabetes mellitus) completed
the study. Mean fasting blood sugar and fructosamine concentrations were unchanged
throughout the study. Five patients required minor alterations (3 increased, 2 decreased)
in their hypoglycemic regimens during the study. The addition of low-dose niacin to
pravastatin therapy resulted in a significant lowering of LDL cholesterol compared with
pravastatin monotherapy. CONCLUSIONS: Low-dose niacin is a promising addition to
hydroxymethylglutaryl-coenzyme A reductase inhibitor therapy in the treatment of
hypercholesterolemia in patients with diabetes mellitus.
- Language of Publication
- English
- Unique Identifier
- 97328158
- MeSH Heading (Major)
- Anticholesteremic Agents|AD/AE/*TU; Diabetes Mellitus, Insulin-Dependent|BL/CO/*DT;
Diabetes Mellitus, Non-Insulin-Dependent|BL/CO/*DT; Enzyme Inhibitors|AD/AE/*TU;
Niacin|AD/AE/*TU; Pravastatin|AD/AE/*TU
- MeSH Heading
- Adult; Aged; Blood Glucose|ME; Comparative Study; Drug Therapy, Combination; Female;
Fructosamine|BL; Human; Hypercholesterolemia|DT/ET; Lipoprotein(a)|BL; Lipoproteins, LDL
Cholesterol|BL; Male; Middle Age; Prospective Studies; Support, Non-U.S. Gov't
- Publication Type
- CLINICAL TRIAL; JOURNAL ARTICLE
- ISSN
- 1060-0280
- Country of Publication
- UNITED STATES
Record 11 from database: MEDLINE
- Title
- Bioavailability of niacin.
- Author
- van den Berg H
- Address
- TNO Nutrition and Food Research Institute, Zeist, The Netherlands.
- Source
- Eur J Clin Nutr, 1997 Jan, 51 Suppl 1:, S64-5
- Abstract
- Abstract unavailable online.
- Language of Publication
- English
- Unique Identifier
- 97175911
- MeSH Heading (Major)
- Niacin|AD/DF/PH/*PK
- MeSH Heading
- Animal; Biological Availability; Food; Human; Intestinal Absorption
- Publication Type
- JOURNAL ARTICLE; REVIEW; REVIEW, TUTORIAL
- ISSN
- 0954-3007
- Country of Publication
- ENGLAND
Record 12 from database: MEDLINE
- Title
- Niacin for lipid disorders. Indications, effectiveness, and safety.
- Author
- Brown WV
- Address
- Division of Arteriosclerosis and Lipid Metabolism, Emory University School of Medicine,
Atlanta, USA.
- Source
- Postgrad Med, 1995 Aug, 98:2, 185-9, 192-3
- Abstract
- Niacin can be very effective and safe in lowering low-density lipoprotein cholesterol
and triglyceride levels and also in increasing high-density lipoprotein cholesterol
levels. In combination with other lipid-lowering drugs (eg, bile acid sequestrants), it
has reduced the incidence of cardiovascular events and stopped the progression of coronary
artery lesions. It may be the most cost-effective lipid-lowering agent currently
available. At lower doses, sustained-release forms of niacin may also improve patient
compliance.
- Language of Publication
- English
- Unique Identifier
- 95357279
- MeSH Heading (Major)
- Antilipemic Agents|*TU; Hyperlipidemia|*DT; Niacin|AE/CT/*TU
- MeSH Heading
- Drug Eruptions|ET; Female; Human; Liver|DE; Male
- Publication Type
- JOURNAL ARTICLE; REVIEW; REVIEW, TUTORIAL
- ISSN
- 0032-5481
- Country of Publication
- UNITED STATES
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