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Transcript
Dietary Supplement Information for Physicians
with Naturokinetics℠
Pantethine 300 mg Softgels
Product Code: P0487
Category: Lipid Metabolism Support
TECHNICAL SUMMARY

Pantethine is the disulfide form of pantotheine, which in turn is the
amide conjugate of pantothenic acid (vitamin B5) and cysteamine.
 Each molecule of pantethine provides two molecules of pantothenic
acid and is more stable than the latter.
 Pantothenic acid in pantethine is already conjugated with
cysteamine, which is the next
metabolic step in the formation of
coenzyme A.
Chemical Name: D-Bis (N-pantothenyl-2aminoethyl)-disulfide.
Structural Formula: Figure 1.
Molecular Formula: C22H42N4O8S2
Molecular Weight: 554.72
Product Composition: Pantesin®
Pantethine (Coenzyme A Precursor), Rice
Bran Oil, Gelatin (capsule), Glycerin, Water,
Carob, Beeswax and Lecithin.
Delivery Form: Softgel.
ROLE AS A NUTRIENT
Fig. 1 Pantethine
Essentiality: Pantethine is a derivative of pantothenic acid, which is an
1, 2
essential nutrient (vitamin B5) that serves as a precursor to Coenzyme A.
Dietary Sources: Liver, kidney, yeast, egg yolk, tuna, cod, royal jelly, and fresh vegetables are typical dietary sources of
2
pantothenic acid.
Typical Consumption: A typical 2,500 calorie diet from plant and animal sources provides approximately 10 mg of
pantothenic acid. Recommended daily intake for adults is 4-7 mg; for children age 7-10 years old 4-5 mg; and for infants 2
2
mg.
Prevalence of Nutrient Deficiency: In humans, pantothenic acid deficiency is rare and is generally associated with fatigue
2
and depression.
2
Methods of Evaluation: Pantothenic acid concentration can be assessed in blood and urine.
Structural and Functional Role: As a Coenzyme A precursor, pantothenic acid plays an essential role in the synthesis of fatty
acids and modifications of cellular proteins with acetyl or fatty acyl groups including microtubules, which are important to
the cellular exoskeleton. It is also required for the synthesis of cholesterol, steroid hormones, dolichol, vitamin A, vitamin D,
and all compounds formed from isoprenoid units. Pantethine is also well known for its ability to normalize lipid levels,
1, 2
positively affecting chronic conditions such as hyperlipidemia, fatty liver, and cardiovascular disease.
Pantesin® is a registered trademark of Daiichi Fine Chemicals, Inc.
Dietary Supplement Information for Physicians
with Naturokinetics℠
RECOMMENDED USE
Lipid Metabolism Support: The efficacy of pantethine in lipid
metabolism support has been investigated in 28 clinical trials providing
3
a pooled population of 646 hyperlipidemic subjects. The average study
sample size was 22.3 subjects with a mean age of 52.8 years. The
average study trial length was 12.7 weeks with a median pantethine
dosage of 900 mg/day. The mean percent decrease from baseline to 4
months was:
 For total serum cholesterol (TC) - 15.1%
 For low-density lipoprotein cholesterol (LDL) - 20.1%
 For serum triacylglycerols (TG) - 32.9%
 The mean percent increase for high-density lipoprotein cholesterol
(HDL) was 8.4%
In a one-year long clinical trial conducted in 24 patients (mean age 51
years old), the outcome of pantethine supplementation (900 mg/day)
was dependent on the type of dyslipidemia. The most improvement
4
was achieved in the type IIB type of dyslipidemia (Figure 2).
Figure 2: Total cholesterol concentrations in patients
with dyslipidemia type IIA (●●●●) and IIB (— —)
supplemented with pantethine.
In the most recent randomized triple-blinded clinical trial, a total of 120
subjects with low to moderate CVD risk received either Pantesin® (600
mg/day weeks 1-8, 900 mg/day weeks 9-16) or placebo in conjunction
with implementation of lifestyle changes. Pantethine supplementation
5
lowered TC and LDL better than the diet alone (P<0.05).
NATUROKINETICS
SM
Liberation: Dissolution test is not available. P0487 Pantethine 300 mg
passes the standard disintegration test in water (< 60min).
Absorption: Pantethine is absorbed in the small intestine and results in
a significant increase in plasma pantothenate concentration at
6
approximately 2.5h (Tmax) as shown in human volunteers (Figure 3).
Figure 3: Plasma concentration of pantothenate
Distribution: Pantothenic acid is distributed throughout the body
after a single oral dose of pantethine (62 mg/kg).
according to organ perfusion; cysteamine is predominantly found in the
1, 6
kidneys.
Metabolism: Each molecule of pantethine provides 2 molecules of pantetheine, which can serve as a coenzyme A precursor
6
or can be further hydrolyzed into pantothenate and cysteamine.
Excretion: Pantethine is excreted in urine as pantothenate and cysteamine. Elimination half-life (t1/2) of pantothenate is 28
6
hours.
SAFETY INFORMATION
Tolerability: Pantethine is generally very well tolerated. It has been clinically tested in doses ranging from 300 mg to 1,800
mg/day. Daily doses 1,500 mg/day or higher may result in occasional adverse effects that may include softening of stool,
2, 7
nausea, G.I. discomfort, and modest laxation.
Contraindications: Pantethine has been shown to exhibit anti-platelet effects and could increase the risk of bleeding.
8
Individuals with bleeding disorders should be advised to use with caution.
Pantesin® is a registered trademark of Daiichi Fine Chemicals, Inc.
Dietary Supplement Information for Physicians
with Naturokinetics℠
INTERACTIONS
Drug Interactions: Concomitant use of pantethine with anti-coagulant/anti-platelet medications (such as Plavix®,
8
Coumadin® and aspirin) may increase the risk of bleeding.
Supplement Interactions: Concomitant use with supplements that exhibit anti-platelet effects may increase the risk of
8
bleeding. This includes garlic, Ginkgo biloba, red clover, ginseng, and others.
Interactions with Lab Tests: None known.
Storage and Stability: Store in cool dry environment in a tightly sealed container.
References
1.
2.
3.
4.
5.
6.
7.
8.
Pantethine. Monograph. Altern Med Rev. Sep 2010; 15(3): 279-282.
Pins JJ, Keenan JM. Dietary and nutraceutical options for managing the hypertriglyceridemic patient. Prog
Cardiovasc Nurs. Spring 2006; 21(2): 89-93.
Marc P M. Treatment of hyperlipoproteinemia with pantethine: A review and analysis of efficacy and tolerability.
Nutrition Research. 2005; 25(4): 319-333.
Arsenio L, Bodria P, Magnati G, Strata A, Trovato R. Effectiveness of long-term treatment with pantethine in
patients with dyslipidemia. Clin Ther. 1986; 8(5): 537-545.
Rumberger JA, Napolitano J, Azumano I, Kamiya T, Evans M. Pantethine, a derivative of vitamin B5 used as a
nutritional supplement, favorably alters low-density lipoprotein cholesterol metabolism in low to moderate
cardiovascular risk North American subjects: a triple-blinded placebo and diet-controlled investigation. Nutrition
research (New York, N.Y.). 2011; 31(8): 608-615.
Wittwer CT, Gahl WA, Butler JD, Zatz M, Thoene JG. Metabolism of pantethine in cystinosis. J Clin Invest. Oct 1985;
76(4): 1665-1672.
Da Col PG CL, Fonda M. Pantethine in the treatment of hypercholesterolemia: a randomized double-blind trial
versus tiadenol. Curr Ther Res 1984; 36: 314-22.
Agrati AM AG, Ferraro G, Palmieri. Gemfibrozil efficacy vs pantethine in dyslipoproteinemic patients: a controlled
study. Curr Ther Res 1989; 45: 650-653.
Pantesin® is a registered trademark of Daiichi Fine Chemicals, Inc.