UBIDECARENONE
THIS COMPOUND BELONGS TO THE CLASS OF ORGANIC COMPOUNDS KNOWN AS UBIQUINONES. THESE ARE COENZYME Q DERIVATIVES CONTAINING A 5, 6-DIMETHOXY-3-METHYL(1,4-BENZOQUINONE) MOIETY TO WHICH AN ISOPRENYL GROUP IS ATTACHED AT RING POSITION 2(OR 6).
DESCRIPTION
UBIDECARENONE, ALSO CALLED COENZYME Q10, IS A 1,4-BENZOQUINONE. FROM HIS NAME (Q10), THE Q REFERS TO THE CONSTITUTIVE QUINONE GROUP, AND 10 IS RELATED TO THE NUMBER OF ISOPRENYL SUBUNITS IN ITS TAIL. IT IS A POWERFUL ANTIOXIDANT, A LIPID-SOLUBLE AND ESSENTIAL COFACTOR IN MITOCHONDRIAL OXIDATIVE PHOSPHORYLATION. THE UBIDECARENONE IS THE COENZYME DESTINED FOR MITOCHONDRIAL ENZYME COMPLEXES INVOLVED IN OXIDATIVE PHOSPHORYLATION IN THE PRODUCTION OF ATP. IT IS FUNDAMENTAL FOR CELLS THAT HAVE A HIGH METABOLIC DEMAND. UBIDECARENONE IS SOLD AS A DIETARY SUPPLEMENT AND IS NOT FDA APPROVED AS A DRUG THUS, IT IS NOT MEANT TO TREAT, CURE OR PREVENT ANY DISEASE. FDA DOES NOT APPROVE THIS DIETARY SUPPLEMENTS BEFORE SOLD NOR REGULATE THE MANUFACTURING PROCESS.
PHARMACOLOGY
INDICATION
THE DIET SUPPLEMENTS CONTAINING UBIDECARENONE ARE INDICATED, AS STATED IN THE PRODUCT LABEL, TO ASSIST INDIVIDUALS WITH CARDIOVASCULAR COMPLAINTS INCLUDING CONGESTIVE HEART FAILURE AND SYSTOLIC HYPERTENSION. IN THE PRODUCT, UBIDECARENONE IS USED TO INCREASE THE CARDIAC INPUT AS WELL AS FOR THE PREVENTION OF SEVERAL OTHER DISEASES LIKE PARKINSON, FIBROMYALGIA, MIGRAINE, PERIODONTAL DISEASE AND DIABETES, BASED ON PRECLINICAL STUDIES. IT IS IMPORTANT TO HIGHLIGHT THAT THESE PRODUCTS ARE NOT FDA APPROVED AND IT IS RECOMMENDED TO USE UNDER DISCRETION.
ASSOCIATED CONDITIONS
Β· MIGRAINE
PHARMACODYNAMICS
UBIDECARENON HAS ROLES IN MANY PRYSIOLOGICAL PROCESS INCLUDING SULFIDE OXIDATION, REGULATION OF MITOCHONDRIAL PERMEABILITY TRANSITION PORE AND TRANSLOCATION OF PROTONS AND CALCIUM IONS ACCROSS BIOLOGICAL MEMBRANES. STUDIES HAVE SHOWN ITS BENEFITIAL EFFECT IN TREATING CANCER, STATIN MYOPATHY, CONGESTIVE HEART FAILURE AND HYPERTENSION.
MECHANISM OF ACTION
UBIDECARENONE IS AN ESSENTIAL COFACTOR IN THE MITOCHONDRIAL ELECTRON TRANSPORT CHAIN. ITS FUNCTIONS ARE THE ACCEPTANCE OF ELECTRONS FROM THE COMPLEX I AND II AND THIS ACTIVITY IS VITAL FOR THE PRODUCTION OF ATP. IT ACTS AS A MOBILE REDOX AGENT SHUTTLING ELECTRONS AND PROTONS IN THE ELECTRON TRANSPORT CHAIN. UBIDECARENONE ALSO PRESENTS ANTIOXIDANT ACTIVITY IN MITOCHONDRIA AND CELLULAR MEMBRANES, PROTECTING AGAINST PEROXIDATION OF LIPID MEMBRANES AS WELL AS INHIBITING OXIDATION OF LDL-CHOLESTEROL.10
ABSORPTION
UBIDECARENONE IS ABSORBED FROM THE SMALL INTESTINE INTO THE LYMPHATICS AND THEN IT CAN ENTER THE BLOOD. THE HYDROPHOBICITY AND LARGE MOLECULAR WEIGHT LIMIT ITS ABSORPTION MAKING IT VERY POOR AND VARIABLE DEPENDING ON THE FOOD INTAKE AND THE NUMBER OF LIPIDS PRESENTED IN THE FOOD. THE ABSORPTION IS LOWER IN THE PRESENCE OF AN EMPTY STOMACH AND GREATER IN PRESENCE OF HIGH LIPID FOOD DIET. THE DAILY DOSAGE OF UBIDECARENONE PRESENTS THE REACH OF MAXIMAL SERUM CONCENTRATION BY REACHING A PLATEAU AFTER THREE WEEKS.10 THE PHARMACOKINETIC PROPERTIES MAY VARY BETWEEN DIFFERENT BRANDS BUT STUDIES HAVE REPORTED AN AUC OF 11.51 MCG H/ML AND A CMAX OF 0.32 MCG/ML AT A TIME OF 7.9 H.
VOLUME OF DISTRIBUTION
UBIDECARENONE IS DISTRIBUTED TO THE VARIOUS TISSUES OF THE BODY AND IT IS ABLE TO ENTER THE BRAIN.10 IN PRECLINICAL STUDIES WITH INTRAVENOUS ADMINISTRATION OF UBIDECARENONE, IT IS REPORTED A VOLUME OF DISTRIBUTION OF 20.4 L/KG WHICH REFLECTS ITS ABILITY TO PENETRATE EXTENSIVELY INTO ORGANS AND TISSUES. AS A GENERAL RULE, TISSUES WITH HIGH-ENERGY REQUIREMENTS OR METABOLIC ACTIVITY TEND TO PRESENTS HIGHER AMOUNTS OF UBIDECARENONE, THESE ORGANS CAN BE HEART, KIDNEY, LIVER AND MUSCLE.
PROTEIN BINDING
IN THE BLOOD, UBIDECARENONE IS SPLIT INTO THE VARIOUS LIPOPROTEIN PARTICLES INCLUDING LDL AND VLDL.10 THE PLASMA CONCENTRATION OF UBIDECARENONE IS HIGHLY DEPENDENT ON THE PRESENCE OF PLASMA LIPOPROTEINS AND ABOUT 95% OF THE ADMINISTERED FORM IS FOUND IN THE REDUCED FORM.
METABOLISM
STUDIES INDICATE THAT THERE IS NO SATURATION PROCESS DURING THE METABOLISM OF UBIDECARENONE. IT IS METABOLIZED IN ALL TISSUES BY THE PHOSPHORYLATION IN THE CELLS AND TRANSPORTATION TO THE KIDNEYS FOR FURTHER EXCRETION BY THE URINE.11 AFTER EXERTING ITS ACTION, UBIDECARENONE IS REDUCED AND FORMS HYDROQUINONE WHICH IS CAPABLE OF RECYCLING AND REGENERATES OTHER ANTIOXIDANTS SUCH AS TOCOPHEROL AND ASCORBATE. THE LATER METABOLISM OF HYDROQUINONE GENERATES THE FORMATION OF Q ACID I AND Q ACID II IN FREE AND CONJUGATED FORMS.
ROUTE OF ELIMINATION
THE MAIN ELIMINATION ROUTE OF UBIDECARENONE IS THROUGH THE BILE. AFTER ITS ORAL ADMINISTRATION, OVER 60% OF THE DOSE IS EXCRETED IN THE FECES IN THE FORM OF UNCHANGED UBIDECARENONE AND A SMALL FRACTION OF THE METABOLITES.10 , IN THE URINE, UBIDECARENONE IS BOUND TO SAPOSIN B PROTEIN AND REPRESENTS ONLY 8.3% OF THE TOTAL ADMINISTERED DOSE.
HALF LIFE
THE PHARMACOKINETIC PROPERTIES MAY VARY BETWEEN DIFFERENT BRANDS BUT STUDIES HAVE REPORTED A HALF-LIFE OF UBIDECARENONE OF 21.7 H.
CLEARANCE
IN PRECLINICAL STUDIES WITH INTRAVENOUS ADMINISTRATION OF UBIDECARENONE, IT IS REPORTED A TOTAL CLEARANCE OF 1.18 ML H/KG WHICH WAS INDICATIVE OF A PROLONGED ELIMINATION.
TOXICITY
THERE HAVE NOT BEEN REPORTS OF ADVERSE EVENTS OF DIET SUPPLEMENTATION WITH UBIDECARENONE. THE NORMAL SIDE EFFECTS REPORTED IN HUMANS ARE RELATED TO THE GASTROINTESTINAL TRACT.
(R)-WARFARIN THE THERAPEUTIC EFFICACY OF (R)-WARFARIN CAN BE DECREASED WHEN USED IN COMBINATION WITH UBIDECARENONE.
(S)-WARFARIN THE THERAPEUTIC EFFICACY OF (S)-WARFARIN CAN BE DECREASED WHEN USED IN COMBINATION WITH UBIDECARENONE.
2,4-THIAZOLIDINEDIONE THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH 2,4-THIAZOLIDINEDIONE.
4-HYDROXYCOUMARIN THE THERAPEUTIC EFFICACY OF 4-HYDROXYCOUMARIN CAN BE DECREASED WHEN USED IN COMBINATION WITH UBIDECARENONE.
ACARBOSE THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN ACARBOSE IS COMBINED WITH UBIDECARENONE.
ACENOCOUMAROL THE THERAPEUTIC EFFICACY OF ACENOCOUMAROL CAN BE DECREASED WHEN USED IN COMBINATION WITH UBIDECARENONE.
ACETOHEXAMIDE THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH ACETOHEXAMIDE.
ACIPIMOX THE RISK OR SEVERITY OF MYOPATHY, RHABDOMYOLYSIS, AND MYOGLOBINURIA CAN BE INCREASED WHEN ACIPIMOX IS COMBINED WITH UBIDECARENONE.
AICA RIBONUCLEOTIDE THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH AICA RIBONUCLEOTIDE.
ALAPROCLATE THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH ALAPROCLATE.
ALBIGLUTIDE THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH ALBIGLUTIDE.
ALENDRONIC ACID THE RISK OR SEVERITY OF MYOPATHY, RHABDOMYOLYSIS, AND MYOGLOBINURIA CAN BE INCREASED WHEN ALENDRONIC ACID IS COMBINED WITH UBIDECARENONE.
ALLICIN THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH ALLICIN.
ALOGLIPTIN THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH ALOGLIPTIN.
ALUMINIUM CLOFIBRATE THE RISK OR SEVERITY OF MYOPATHY, RHABDOMYOLYSIS, AND MYOGLOBINURIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH ALUMINIUM CLOFIBRATE.
AMG-222 THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH AMG-222.
AMIODARONE THE RISK OR SEVERITY OF MYOPATHY, RHABDOMYOLYSIS, AND MYOGLOBINURIA CAN BE INCREASED WHEN AMIODARONE IS COMBINED WITH UBIDECARENONE.
AMPHOTERICIN B THE RISK OR SEVERITY OF MYOPATHY, RHABDOMYOLYSIS, AND MYOGLOBINURIA CAN BE INCREASED WHEN AMPHOTERICIN B IS COMBINED WITH UBIDECARENONE.
ANAGLIPTIN THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH ANAGLIPTIN.
ATORVASTATIN THE RISK OR SEVERITY OF MYOPATHY AND RHABDOMYOLYSIS CAN BE DECREASED WHEN UBIDECARENONE IS COMBINED WITH ATORVASTATIN.
BACLOFEN THE RISK OR SEVERITY OF MYOPATHY, RHABDOMYOLYSIS, AND MYOGLOBINURIA CAN BE INCREASED WHEN BACLOFEN IS COMBINED WITH UBIDECARENONE.
BALAGLITAZONE THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH BALAGLITAZONE.
BENFLUOREX THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH BENFLUOREX.
BETAMETHASONE THE RISK OR SEVERITY OF MYOPATHY, RHABDOMYOLYSIS, AND MYOGLOBINURIA CAN BE INCREASED WHEN BETAMETHASONE IS COMBINED WITH UBIDECARENONE.
BEZAFIBRATE THE RISK OR SEVERITY OF MYOPATHY, RHABDOMYOLYSIS, AND MYOGLOBINURIA CAN BE INCREASED WHEN BEZAFIBRATE IS COMBINED WITH UBIDECARENONE.
BISEGLIPTIN THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH BISEGLIPTIN.
BROMOCRIPTINE THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH BROMOCRIPTINE.
BUFORMIN THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH BUFORMIN.
BUMETANIDE THE RISK OR SEVERITY OF MYOPATHY, RHABDOMYOLYSIS, AND MYOGLOBINURIA CAN BE INCREASED WHEN BUMETANIDE IS COMBINED WITH UBIDECARENONE.
CANAGLIFLOZIN THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH CANAGLIFLOZIN.
CAPTOPRIL THE RISK OR SEVERITY OF MYOPATHY, RHABDOMYOLYSIS, AND MYOGLOBINURIA CAN BE INCREASED WHEN CAPTOPRIL IS COMBINED WITH UBIDECARENONE.
CARBIMAZOLE THE RISK OR SEVERITY OF MYOPATHY, RHABDOMYOLYSIS, AND MYOGLOBINURIA CAN BE INCREASED WHEN CARBIMAZOLE IS COMBINED WITH UBIDECARENONE.
CARBUTAMIDE THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH CARBUTAMIDE.
CARMEGLIPTIN THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH CARMEGLIPTIN.
CERIVASTATIN THE RISK OR SEVERITY OF MYOPATHY AND RHABDOMYOLYSIS CAN BE DECREASED WHEN UBIDECARENONE IS COMBINED WITH CERIVASTATIN.
CHLOROQUINE THE RISK OR SEVERITY OF MYOPATHY, RHABDOMYOLYSIS, AND MYOGLOBINURIA CAN BE INCREASED WHEN CHLOROQUINE IS COMBINED WITH UBIDECARENONE.
CHLORPROPAMIDE THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN CHLORPROPAMIDE IS COMBINED WITH UBIDECARENONE.
CIBENZOLINE THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH CIBENZOLINE.
CIGLITAZONE THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH CIGLITAZONE.
CIMETIDINE THE RISK OR SEVERITY OF MYOPATHY, RHABDOMYOLYSIS, AND MYOGLOBINURIA CAN BE INCREASED WHEN CIMETIDINE IS COMBINED WITH UBIDECARENONE.
CIPROFIBRATE THE RISK OR SEVERITY OF MYOPATHY, RHABDOMYOLYSIS, AND MYOGLOBINURIA CAN BE INCREASED WHEN CIPROFIBRATE IS COMBINED WITH UBIDECARENONE.
CIPROFLOXACIN THE RISK OR SEVERITY OF MYOPATHY, RHABDOMYOLYSIS, AND MYOGLOBINURIA CAN BE INCREASED WHEN CIPROFLOXACIN IS COMBINED WITH UBIDECARENONE.
CITALOPRAM THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN CITALOPRAM IS COMBINED WITH UBIDECARENONE.
CLADRIBINE THE RISK OR SEVERITY OF MYOPATHY, RHABDOMYOLYSIS, AND MYOGLOBINURIA CAN BE INCREASED WHEN CLADRIBINE IS COMBINED WITH UBIDECARENONE.
CLINAFLOXACIN THE RISK OR SEVERITY OF HYPOGLYCEMIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH CLINAFLOXACIN.
CLOFIBRATE THE RISK OR SEVERITY OF MYOPATHY, RHABDOMYOLYSIS, AND MYOGLOBINURIA CAN BE INCREASED WHEN CLOFIBRATE IS COMBINED WITH UBIDECARENONE.
CLOFIBRIDE THE RISK OR SEVERITY OF MYOPATHY, RHABDOMYOLYSIS, AND MYOGLOBINURIA CAN BE INCREASED WHEN UBIDECARENONE IS COMBINED WITH CLOFIBRIDE.
CLORINDIONE THE THERAPEUTIC EFFICACY OF CLORINDIONE CAN BE DECREASED WHEN USED IN COMBINATION WITH UBIDECARENONE.
COLCHICINE THE RISK OR SEVERITY OF MYOPATHY, RHABDOMYOLYSIS, AND MYOGLOBINURIA CAN BE INCREASED WHEN COLCHICINE IS COMBINED WITH UBIDECARENONE.
COUMARIN THE THERAPEUTIC EFFICACY OF COUMARIN CAN BE DECREASED WHEN USED IN COMBINATION WITH UBIDECARENONE.