Decaquinon

Ubidecarenone.

Each tablet also contains the following excipients: FD&C Yellow No. 6 (sunset yellow FCF), carnauba wax, hydrated silicon dioxide, microcrystalline cellulose, titanium oxide, stearic acid, calcium stearate, talc, precipitated calcium carbonate, corn starch, lactose hydrate, white shellac, hydroxypropylcellulose, pullulan, povidone and macrogol 6000.
Ubidecarenone is (2E, 6E, 10E, 14E, 18E, 22E, 26E, 30E, 34E, 38E)-2-(3, 7, 11, 15, 19, 23, 27, 31, 35, 39-Decamethyltetraconta-2, 6, 10, 14, 18, 22, 26, 30, 34, 38-decaen-1-yl)-5, 6-dimethoxy-3-methyl-1, 4-benzoquinone.
Molecular Formula: C₅₉H₉₀O₄. Molecular Weight: 863.34.
Ubidecarenone occurs as a yellow to orange, crystalline powder. It is odorless and tasteless. It is freely soluble in diethylether, very slightly soluble in ethanol (99.5) and practically insoluble in water. It is gradually decomposed by light and darkens.
Melting Point: Approximately 48°C.
Ubidecarenone (Coenzyme Q₁₀, Ubiquinone 50), the active ingredient of Decaquinon, was 1st isolated in 1957 as fat-soluble crystals from the bovine heart muscle. Later, Cooly and Folkers and their colleagues demonstrated that ubidecarenone activity is low in the myocardium of patients with heart disease. Ubidecarenone (CoQ₁₀), administered orally, is absorbed via the lymphatic system and is incorporated into intracellular mitochondria. It has now been confirmed that CoQ₁₀ acts directly on ischemic myocardium and improves the efficiency of oxygen utilization. These actions of CoQ₁₀ enable the heart muscle to maintain high levels of energy-producing functions, even under ischemic conditions, thus reducing ischemia-induced myocardial damage. Clinically, the effect of CoQ₁₀ on myocardial disorders was studied observing electrocardiograms at rest and with exercise loading, and it was confirmed that CoQ₁₀ administration normalized the depressed cardiac function. Furthermore, double-blind controlled clinical trials have demonstrated the efficacy of Decaquinon in improving the symptoms of congestive heart failure associated with decreased left ventricular function due to chronically ischemic heart or hypertensive heart disease.

Pharmacology: Improvement of Oxygen Utilization Efficiency in Ischemic Myocardium: In an experiment using guinea pig ventricular papillary muscle, ubidecarenone improved impaired myocardial contractility which occurred under hypoxic perfusion.
Stimulation of ATP Production in Heart Muscle: In rabbits, heart muscle pretreated with ubidecarenone intraperitoneally, the decrease in ATP production in heart muscle seen after post-ischemic reperfusion was inhibited, so that post-ischemic reperfusion-induced myocardial cell injury was only slight.
Improvement of Diminished Cardiac Function: When ubidecarenone was administered orally from the stage of myocardial injury to the stage of cardiac hypertrophy in models of cardiomyopathy (hamsters with cardiomyopathy), diminished myocardial contractility and expansibility were a lesser extent in the treated animals than in the untreated group or digoxin-treated group.
In the rat models of myocardial infarction, ubidecarenone slightly inhibited a post-infarction decrease in cardiac function. When the effect of ubidecarenone on the post-infarction prognosis was determined in rat models of myocardial infarction, the long-term survival rate was higher for the treated group than for the untreated group.
Anti-aldosterone Effect: Ubidecarenone inhibited the secretion of aldosterone and antagonized Na⁺ retention brought about by the aldosterone in rats, resulting in the acceleration of Na⁺ diuresis. However, ubidecarenone has no effect on K⁺ excretion.
Clinical Studies: Clinical Efficacy: In double-blind clinical trials and open-labeled clinical trials, Decaquinon has been demonstrated to be useful for treating objective and subjective symptoms (edema, pulmonary congestion, hepatic enlargement, anginal symptoms and others) associated with congestive heart failure due to ischemic heart disease, hypertension or rheumatic heart disease and others.
Pharmacokinetics: Blood Concentration of Decaquinon Uncoated Tablets 10 mg and Decaquinon Sugar-Coated Tablets 10 mg: Ten (10) tablets of Decaquinon uncoated tablets 10 mg or of Decaquinon sugar-coated tablets 10 mg were administered orally to healthy adult male volunteers at a single dose (ubidecarenone 100 mg) in a crossover design, and changes in the plasma concentration were compared. For both dosage forms, the time to reach peak plasma concentration (about 0.5 mcg/mL of exogenous CoQ₁₀) was 6 hrs after administration and thereafter, the plasma concentration gradually declined. There was no statistically significant difference between the 2 different dosage forms. (See figure and table.)

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Click on icon to see table/diagram/image

Symptoms associated with mild and moderate congestive heart failure in patients under standard treatment.

Adults: 1 tab (ubidecarenone 10 mg) orally 3 times a day after meals.

There is no experience to date with deliberate overdose.
No specific antidote is known.

There are no known contraindications to Decaquinon.

Use in pregnancy & lactation: Teratogenicity of Decaquinon has not been reported. Clinically, safety of Decaquinon during pregnancy and lactation has not been established.

Use in pregnancy & lactation: Teratogenicity of Decaquinon has not been reported. Clinically, safety of Decaquinon during pregnancy and lactation has not been established.

Adverse reactions were reported in 78 of 5350 patients (1.46%). (At the end of the investigation for incidence of adverse reactions.)
Gastrointestinal: >5%, ≥0.1%: Stomach discomfort, anorexia, nausea and diarrhea.
Hypersensitivity*: >5%, ≥0.1%: Rash.
*In the event of such symptoms, appropriate measures eg, discontinuation of Decaquinon should be taken.

There are no reports that Decaquinon caused clinically significant drug interactions with other drugs.
Incompatibility: Incompatibility is not known yet.

Store at room temperature not exceeding 30°C. Preserve in light-resistant containers. Protect from moisture.

Other Cardiovascular Drugs

C01EB09 - ubidecarenone ; Belongs to the class of other cardiac preparations.

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