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  • Ubiquinol, Active Form of CoQ10 Kaneka North America


    DIETARY SUPPLEMENT

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    Ubiquinol, Active Form of CoQ10
    Kaneka North America

    CLASSES

    Dietary Supplement

    DESCRIPTION

    CoQ10 is a vitamin-like substance which is produced naturally in the body and plays a critical role in the creation of cellular energy. CoQ10 is available in two forms: Ubiquinone (US Pharmacopeia [USP] Name - ubidecarenone), which is the oxidized form of CoQ10, and Ubiquinol, which is the reduced (lipophilic antioxidant) form that has two additional electrons. Ubiquinol is better absorbed than CoQ10 and raises blood levels of Total CoQ10 more effectively than CoQ10.1-3

    CoQ10 (ubiquinone) must be converted to Ubiquinol in the serum where it is transported via plasma lipoproteins to cells. Conversion loses efficiency with aging and in individuals with certain chronic health conditions, resulting in lower levels of CoQ10 in the heart and other major organs.4,5 Administration of Ubiquinol circumvents this problem and therefore Ubiquinol is called the active form of CoQ10.

    Chemical Structure

    HOW SUPPLIED

    Since 2007, supplied by Kaneka Nutrients, developer of the patented technology for producing the active form of CoQ10, Kaneka Ubiquinol™. Prior to its introduction, only the reduced form of CoQ10 was commercially available, also supplied by Kaneka Nutrients. Kaneka Ubiquinol™ is utilized in over 200 brands of consumer products globally and is the only Ubiquinol supplement ingredient available today.

    Available in 50 mg, 100 mg or 200 mg soft gels.

    OTHER COMMON NAMES

    Ubiquinol
    Ultra CoQ10
    Advanced CoQ10
    QH-absorb
    Mega CoQ10

    Ubiquinol supplements may be branded by other names or descriptors, including those noted above. To ensure patients are purchasing and taking the Ubiquinol form of CoQ10, direct them to look for the Kaneka Quality Seal on the label of the supplement bottle.

    Logo

    MECHANISM OF ACTION

    CoQ10/Ubiquinol participates in the mitochondrial electron transport chain as a cofactor at the level of Complex III where it shunts electrons. It also acts as a lipophilic antioxidant in the mitochondrial membranes.

    PHARMACOKINETICS

    Ubiquinol is administered orally. Being lipophilic, it follows the uptake mechanisms of lipids in the gastrointestinal tract. Ubiquinol is first incorporated into chylomicrons following absorption and transported via the lymphatics to the circulation. There it is transported by triacylglycerol-rich lipoproteins to the liver where it is repackaged primarily into VLDL/LDL particles and HDL particles to a minor extent. About 95% of CoQ10 in circulation exists in its reduced form as Ubiquinol in humans.6,7 A major portion of CoQ10 in tissues is in the reduced form as Ubiquinol.8

    CoQ10 has a Tmax of 6.5 h and an elimination half-life of 33.19 h. Chronic administration produces a dose-dependent increase in plasma CoQ10. Compared to CoQ10, administration of Ubiquinol raises serum levels 2-fold higher with chronic dosing and over 4-fold higher with acute dosing.9

    INDICATIONS AND OTHER KNOWN CLINICAL USE

    Supplementation with Ubiquinol replenishes depleted levels and circumvents CoQ10 deficiency.1,2,10-12

    CoQ10 deficiency has been reported in congestive heart failure,113,14 Type 2 diabeties,15,16 hepatitis,17 liver cirrhosis,17 hepatocellular carcinoma,17 ALS,18 Alzheimer's disease,19 juvenile fibromyalgia20 and Down's syndrome.21

    Statin drugs inhibit the endogenous production of CoQ10, which has been implicated in fatigue and myalgia; Ubiquinol replenishes CoQ10 stores in these patients.22,23

    DOSAGE & ADMINISTRATION

    As a dietary supplement, intended for a daily intake of 100-300 mg

    Recommended Use:
    100 mg/d – Maintenance dose
    200 mg/d – To replenish Ubiquinol levels and correct deficiencies
    300 mg/d – For more severe deficiencies or to dose load initially and then decrease to 200 mg

    DOSAGE UNDER CARE OF PHYSICIAN

    450-900 mg - To address depleted levels and deficiencies observed in congestive heart failure patients

    ADMINISTRATION

    Oral administration

    STORAGE

    Store at controlled room temperature (68-77° F)

    CONTRAINDICATIONS / PRECAUTIONS

    None

    ADVERSE REACTIONS

    Ubiquinol is generally well tolerated. As with any dietary supplement, some gastrointestinal discomfort may be experienced.

    DRUG INTERACTIONS

    Because of its structural similarity to vitamin K, it has been suggested that CoQ10 may have procoagulant activity and interfere with warfarin. The available clinical trial evidence does not support such a concern.

    While there are reports of individual case studies showing an interaction of CoQ10 and warfarin24,25, other case studies involving highly monitored patients on warfarin specifically noted no interactions with CoQ10.13 A well-controlled, double-blind, placebo-controlled study designed to assess the effect of CoQ10 on warfarin also showed no effect.26 A prospective study did show an interaction, though by admission of the authors, the results may have been due to chance given a small population that self-reported the data.27

    Until the dynamics of warfarin, vitamin K and CoQ10 are better understood, patients taking these products together should be closely monitored by the prescribing physician. Administration of Ubiquinol may be appropriate for many individuals taking coumarin or other blood-thinning medications. The addition of any nutrient or even gradual changes in medication dosage levels demands close patient monitoring to ensure maintenance of INR within the acceptable range. Emerging pharmacogenomic data indicates that people with certain genotypes may be more susceptible to variables influencing warfarin activity, sensitivity and resistance.28

    PREGNANCY AND LACTATION

    There are no adequate and well-controlled studies in pregnant or lactating women to establish safety.

    REFERENCES

    1Hosoe K, Kitano M, Kishida H, Kubo H, Fujii K, Kitahara M. Study on safety and bioavailability of ubiquinol (Kaneka QH) after single and 4-week multiple oral administration to healthy volunteers. Regul Toxicol Pharmacol. 2007 Feb;47(1):19-28.

    2Miles MV, Horn P, Milesc L, Tanga P, Steele P, DeGrauwa T. Bioequivalence of coenzyme Q10 from over-the-counter supplements. Nutr Res. 2002:22(8):919-929.

    3Langsjoen PH and Langsjoen AM. Comparison study of plasma coenzyme Q10 levels in healthy subjects supplemented with ubiquinol versus ubiquinone. Clinical Pharmacol Drug Dev. 2014;3(1):13-17.

    4Wada H, Goto H, Hagiwara S, Yamamoto Y. Redox status of coenzyme Q10 is associated with chronological age. J Am Geriatr Soc. 2007 Jul;55(7):1141-2.

    5Niklowitz P, Onur S, Fischer A, Laudes M, Palussen M, Menke T, Döring F. Coenzyme Q10 serum concentration and redox status in European adults: influence of age, sex, and lipoprotein concentration. J Clin Biochem Nutr. 2016 Jan. 58(3):240-5.

    6Yamashita S, Yamamoto Y. Simultaneous detection of ubiquinol and ubiquinone in human plasma as a marker of oxidative stress. Anal Biochem. 1997 Jul 15;250(1):66-73.

    7Tang PH, Miles MV, DeGrauw A, Hershey A, Pesce A. HPLC analysis of reduced and oxidized coenzyme Q(10) in human plasma. Clin Chem. 2001 Feb;47(2):256-65.

    8Aberg F, Appelkvist EL, Dallner G, Ernster L. Distribution and redox state of ubiquinones in rat and human tissues. Arch Biochem Biophys. 1992 Jun;295(2):230-4.

    9Bhagavan HN, Chopra RK. Coenzyme Q10: absorption, tissue uptake, metabolism and pharmacokinetics. Free Radic Res. 2006 May;40(5):445-53.

    10Evans M, Baisley J, Barss S, Guthrie N. A randomized, double-blind trial on the bioavailability of two CoQ10 formulations. Journal of Functional Foods. 2009. 1: 65-73.

    11Schmelzer C, Niklowitz P, Okun JG, Haas D, Menke T, Döring F. Ubiquinol-induced gene expression signatures are translated into altered parameters of erythropoiesis and reduced low density lipoprotein cholesterol levels in humans. IUBMB Life. 2011 Jan;63(1):42-8.

    12Mohr D, Bowry VW, Stocker R. Dietary supplementation with coenzyme Q10 results in increased levels of ubiquinol-10 within circulating lipoproteins and increased resistance of human low-density lipoprotein to the initiation of lipid peroxidation. Biochim Biophys Acta. 1992 Jun 26;1126(3):247-54.

    13Langsjoen PH, Langsjoen AM. Supplemental ubiquinol in patients with advanced congestive heart failure. Biofactors. 2008;32(1-4):119-28.

    14Langsjoen PH and Langsjoen AM. Supplemental Ubiquinol in congestive heart failure: 3 year experience. 6th International Q10 Conference Brussels, 27–30 May 2010; 29–30.

    15Lim SC, Tan HH, Goh SK, Subramaniam T, Sum CF, Tan IK, Lee BL, Ong CN. Oxidative burden in prediabetic and diabetic individuals: evidence from plasma coenzyme Q(10). Diabet Med. 2006 Dec;23(12):1344-9.

    16Ates O, Bilen H, Keles S, Alp HH, Keleş MS, Yıldırım K, Ondaş O, Pınar LC, Civelekler M, Baykal O. Plasma coenzyme Q10 levels in type 2 diabetic patients with retinopathy. Int J Ophthalmol. 2013 Oct 18;6(5):675-9.

    17Yamamoto Y, Yamashita S. Plasma ubiquinone to ubiquinol ratio in patients with hepatitis, cirrhosis, and hepatoma, and in patients treated with percutaneous transluminal coronary reperfusion. Biofactors. 1999;9(2-4):241-6.

    18Sohmiya M, Tanaka M, Suzuki Y, Tanino Y, Okamoto K, Yamamoto Y. An increase of oxidized coenzyme Q-10 occurs in the plasma of sporadic ALS patients. J Neurol Sci. 2005 Jan 15;228(1):49-53.

    19Isobe C, Abe T, Terayama Y. Increase in the oxidized/total coenzyme Q10 Q-10 ratio in the cerebrospinal fluid of Alzheimer's disease patients. Dement Geriatr Cogn Disord. 2009;28(5):449-54.

    20Miyamae T, Seki M, Naga T, Uchino S, Asazuma H, Yoshida T, Iizuka Y, Kikuchi M, Imagawa T, Natsumeda Y, Yokota S, Yamamoto Y. Increased oxidative stress and coenzyme Q10 deficiency in juvenile fibromyalgia: amelioration of hypercholesterolemia and fatigue by ubiquinol-10 supplementation. Redox Rep. 2013;18(1):12-9.

    21Miles MV, Patterson BJ, Chalfonte-Evans ML, Horn PS, Hickey FJ, Schapiro MB, Steele PE, Tang PH, Hotze SL. Coenzyme Q10 (ubiquinol-10) supplementation improves oxidative imbalance in children with trisomy 21. Pediatr Neurol. 2007 Dec;37(6):398-403.

    22Zlatohlavek L, Vrablik M, Grauova B, Motykova E, Ceska R. The effect of coenzyme Q10 in statin myopathy. Neuro Endocrinol Lett. 2012;33 Suppl 2:98-101.

    23Fedacko J, Pella D, Fedackova P, Hänninen O, Tuomainen P, Jarcuska P, Lopuchovsky T, Jedlickova L, Merkovska L, Littarru GP. Coenzyme Q(10) and selenium in statin-associated myopathy treatment. Can J Physiol Pharmacol. 2013 Feb;91(2):165-70.

    24Spigset O. Reduced effect of warfarin caused by ubidecarenone. Lancet. 1994 Nov 12;344(8933):1372-3.

    25Landbo C, Almdal TP. [Interaction between warfarin and coenzyme Q10]. Ugeskr Laeger. 1998 May 25;160(22):3226-7. [Article in Danish]

    26Engelsen J, Nielsen JD, Winther K. Effect of coenzyme Q10 and Ginkgo biloba on warfarin dosage in stable, long-term warfarin treated outpatients. A randomised, double blind, placebo-crossover trial. Thromb Haemost. 2002 Jun;87(6):1075-6.

    27Shalansky S, Lynd L, Richardson K, Ingaszewski A, Kerr C. Risk of warfarin-related bleeding events and supratherapeutic international normalized ratios associated with complementary and alternative medicine: a longitudinal analysis. Pharmacotherapy. 2007 Sep;27(9):1237-47.

    28Stargrove MB, Treasure J, McKee DL. Herb, Nutrient and Drug Interactions:Clinical implications and therapeutic strategies. Mosby Elsevier, St. Louis, Missouri, 2008, p. 743.

    PRODUCT PHOTO

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    The product samples shown here have been supplied by the manufacturer and reproduced in full color by PDR as a quick-reference identification aid. While every effort has been made to assure accurate reproduction, please remember that any visual identification should be considered preliminary. In cases of poisoning or suspected over dosage, the drug's identity should be verified by chemical analysis.

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