Ubiquinone

Scientific Name(s): Coenzyme Q-10 , Ubidecarenone , mitoquinone

Common Name(s): Adelir , Heartcin , Inokiton , Neuquinone , Taidecanone , Udekinon , Ubiquinone

Clinical Overview

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Uses of Ubiquinone

Ubiquinone may have applications in treating ischemic heart disease, congestive heart failure, toxin-induced cardiopathy and hypertension, and protects ischemic myocardium during surgery. Limited data is available to support the use of ubiquinone for any condition.

Ubiquinone Dosing

Ubiquinone has been studied in clinical trials at doses of 90 to 200 mg/day for heart failure, cirrhosis, and antioxidant properties. 1 , 2 , 3 , 4 , 5 , 6 , 7 , 8

Contraindications

Use is not recommended in pregnancy and lactation and in people with demonstrated hypersensitivity.

Pregnancy/Lactation

Information regarding safety and efficacy in pregnancy and lactation is lacking.

Ubiquinone Interactions

Findings are conflicting. Ubiquinone may decrease the anticoagulant effect of warfarin. Because warfarin has a narrow therapeutic index, patients taking warfarin should be cautioned to avoid use of ubiquinone and advised to consult their health care provider before using dietary supplements.

Ubiquinone Adverse Reactions

Rare side effects include epigastric discomfort, loss of appetite, nausea and diarrhea. Use is not recommended in pregnancy and lactation and in people with demonstrated hypersensitivity.

Toxicology

Research reveals little or no information regarding toxiclology with the use of this product.

History

The first ubiquinone was isolated in 1957. Since that time, ubiquinones have been extensively studied in Japan, Russia, and Europe with research in the US having begun more recently. Lay press accounts claim that roughly 12 million Japanese now use ubiquinones as the medication of choice for management of cardiovascular diseases supplying the demand for more than 250 commercially available preparations. Ubiquinone is touted as an effective treatment of congestive heart failure (CHF), cardiac arrhythmias and hypertension, and in the reduction of hypoxic injury to the myocardium. Other claimed effects include the increase of exercise tolerance, stimulation of the immune system, and counteracting of the aging process. Clinical uses have included the treatment of diabetes, obesity, and periodontal disease. Ubiquinone has not been approved for therapeutic use in the US, but it is available as a food supplement.

Chemistry

Ubiquinones are a class of lipid-soluble benzoquinones that are involved in mitochondrial electron transport. They are found in the majority of aerobic organisms, from bacteria to mammals, hence the name “ubiquinone” (“ubiquitous quinone”). Studies in rats have shown that levels of ubiquinone and cytochrome C reductase increase adaptively during endurance exercise training. This increase occurs in red quadriceps and soleus muscle but not in white cardiac or quadriceps muscle. The increase in red muscle levels represents a positive adaptation to training. 9 Experiments have shown that ubiquinones participate in oxidation-reduction reactions in the mitochondrial respiratory chain. They also have properties of hydrogen carriers, thus providing a coupling of proton translocation to respiration by means of a chemiosmotic mechanism. 10

Structurally ubiquinones are analogous to vitamin K. The basic molecule is 2,3-dimethoxy-5-methylbenzoquinone, to which are attached variable terpenoid side chains containing 1 to 10 monounsaturated trans-isoprenoid units. The 6- to 10-unit chain forms (Q-6 to Q-10) are found in animals, with Q-10 being exclusive to humans. All of the ubiquinones have been synthesized in the laboratory. 11 Studies with deuterated analogs of Q-10 have demonstrated that Q-10 occurs in a mobile environment within the cell, physically separate from the orientational constraints of bilayer lipid chains. This suggests that the bulk of the long-chain ubiquinones are not directly involved functionally in electron transport. Q-10 may represent only a small fraction of total ubiquinone. 12

HPLC of ubiquinone-10 has been performed, 13 as has sodium lauryl sulfate use in hexane extraction of ubiquinone-10 from plasma samples. 14

Ubiquinone Uses and Pharmacology

Biomedical evidence provides the rationale for the use of ubiquinone in cardiovascular diseases. Endogenous forms function as essential cofactors in several metabolic pathways, especially in oxidative respiration. Supraphysiologic doses of ubiquinone may benefit tissues that have been rendered ischemic and then reperfused. Ubiquinone appears to function in such tissues as a free-radical scavenger, membrane stabilizer, or both. 15 Ubiquinone as a mobile component in mitochondrial membrane and its role in electron transfer has been reported. 16 It may have applications in treating ischemic heart disease, CHF, toxin-induced cardiopathy and possibly hypertension. It protects ischemic myocardium during surgery. 15

Experiments with rabbit hearts measured the effects of Q-10 during hypoxia and following reoxygenation. In untreated hearts, reoxygenation was followed by a release of ATP metabolites and creatine phosphokinase. Pretreatment of the hearts with Q-10 eliminated these releases. This suggests that Q-10 retards the breakdown of ATP metabolites, providing a pool from which ATP can be constructed by a salvage process during reoxygenation. 17 , 18 Coenzyme Q-10 also provides a protective effect when used on rat mitochondria. 19

Q-10 has also been shown to eliminate biochemical derangements (reductions of norepinephrine and ATP) in thyrotoxic rabbit hearts. 20 In beef hearts, Q-10 protected mitochondria from oxidative damage to lipid membranes induced by treatment with an adriamycin-iron complex. In these experiments, it reduced the inactivation of NADPH and succinate oxidases. 21 In transplantation experiments, rats receiving livers subjected to prior warm ischemic damage did not survive more than 2 days. Pretreatment of the donors with Q-10 significantly increased the duration of survival, decreased AST and ALT levels and increased total protein to the normal range without affecting total bilirubin or hepatic histology. Thus, ubiquinone had a protective effect on donated livers subjected to heat-induced ischemia before transplantation. 22

Ubiquinone's role in cardiac treatment using human subjects is promising. In geriatric patients, Q-10 treatment improved both symptoms and clinical conditions of all 34 patients with CHF. 23 It was also effective for symptomatic mitral valve prolapse and improved stress-induced cardiac dysfunction in 400 pediatric patients. 24 Activity tolerance improvements were observed in a double-blind study of 19 patients with chronic myocardial disease given oral ubiquinone-10. 25 In advanced heart failure, 12 patients given 100 mg daily of the drug showed marked clinical improvement. 26 Immune system effects were enhanced in myocardial failure in another report, when Q-10 was used in conjunction with other drugs. 27 Aiding defective myocardial supply, ubiquinone's role in oxidative phosphorylation offers positive results in adjunctive treatment, clinical outcomes, symptoms, and quality of life in these cardiac patients. 28

Q-10 actions on lipids have also been reported. The mechanism may be membrane phospholipid protection against phospholipase attack. 29 In its reduced form, ubiquinone's presence in all cellular membrane, blood serum, and serum lipoproteins, allows protection from lipid peroxidation. 30 Its ability to remain stable in hypercholesterolemia patients has been studied. 31 , 32 Ubiquinol can also sustain vitamin E's antioxidant effects by regenerating the vitamin from its oxidized form. 30 , 33

One report describes ubiquinone and its role in human nutrition. 34 A case report uses ubiquinone to treat drug-induced rhabdomyolysis and hepatotoxicity. 35

Dosage

Ubiquinone has been studied in clinical trials at doses of 90 to 200 mg/day for heart failure, cirrhosis, and antioxidant properties. 1 , 2 , 3 , 4 , 5 , 6 , 7 , 8

Pregnancy/Lactation

Information regarding safety and efficacy in pregnancy and lactation is lacking.

Interactions

Ubiquinone (coenzyme Q10) ingestion may decrease the anticoagulant effect of warfarin. A decrease in the international normalized ratio (INR) occurred in 3 patients taking warfarin after they started taking ubiquinone. 36 Two patients had been receiving warfarin for several years before taking ubiquinone. The INR increased when ubiquinone was discontinued. In a placebo-controlled, double-blind, crossover study, in patients on long-term warfarin, coenzyme Q10 did not influence the anticoagulant response (INR) of warfarin. 37

Adverse Reactions

No serious side effects have been associated with the use of ubiquinone. Use of the substance is contraindicated in people with demonstrated hypersensitivity. Use during pregnancy or lactation is not recommended, because studies have not demonstrated the safety of ubiquinone for fetuses and infants. Rare side effects have included epigastric discomfort, loss of appetite, nausea and diarrhea, affecting fewer than 1% of more than 5000 individuals in one study.

Toxicology

Research reveals little or no information regarding toxiclology with the use of this product.

Bibliography

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