Overview of Coenzyme Q10 (Ubiquinone) Injection
Dosage Strength of Coenzyme Q10 Injection
20 mg/mL 10 mL Vial
Coenzyme Q10 (CoQ10) is found in all cells across all domains of life.12 It is a redox-active lipid biosynthesized in the mitochondria by the conjugation of a benzoquinone ring with a 10-unit isoprenoid chain.234 It is essential in the production of cellular energy in the form of adenosine triphosphate (ATP).56 It is a significant antioxidant and therefore prevents free radical generation and modifications of DNA, proteins, and lipids.56 It can also help in the regeneration of other antioxidants, such as vitamin E.7 CoQ10 is also naturally found in some foods, such as meat, nuts, fruits, and vegetables.8 However, the average daily dietary intake of CoQ10 is very low, about three to six milligrams, and earlier studies show that dietary intake of CoQ10 does not appear to increase CoQ10 tissue levels above normal.89
Subnormal serum levels of Coenzyme Q10 have been observed in patients with advanced heart failure; type 2 diabetes (insulin resistance and high blood glucose levels); neurodegenerative disease, including Parkinson’s disease; metabolic syndrome; hypertension; preeclampsia; certain types of cancer, like breast cancer and melanoma, and more.10111213141516171819 This data has led researchers to investigate exogenous CoQ10 supplementation as a potential treatment for these conditions. However, research so far is inconclusive or contradictory as to whether exogenous CoQ10 supplementation can help treat or manage symptoms of these conditions.20212223242526
Coenzyme Q10 is one of the most commonly used dietary supplements.2728 CoQ10 is not FDA-approved for the treatment of any medical condition and there is little data on the safety and efficacy of long-term use of coenzyme Q10.29 However, the FDA granted orphan status to an oral coenzymeQ10 drug, called UbiQGel, for its use in clinical trials on patients diagnosed with mitochondrial cytopathies (MC).3031
CoQ10 deficiency is a known cause of mitochondrial disease. The evidence to date shows promise that CoenzymeQ10 may be a potential treatment of mitochondrial disorders. However, further research is needed to determine the appropriate dosage.32
CoQ10 injections should only be taken under the supervision of a physician.
Mechanism of Action
Coenzyme Q10 is an essential cofactor of intra-complex electron transportation in adenosine triphosphate (ATP) synthesis, also referred to as oxidative phosphorylation.336 It is vital to the health of all cells, and therefore all tissues and organs, in the body. Cells constantly use ATP as an energy source to conduct biological reactions.
CoQ10 is an antioxidant and therefore prevents free radical generation and modifications of DNA, proteins, and lipids.5
CoQ10 is an endogenous inhibitor of platelets.34 Exogenous CoQ10 is an upregulator of the cAMP/PKA pathway, an activator of the A2A adenosine receptor, an inhibitor of phosphodiesterase 3A phosphorylation, and a significant inhibitor of vitronectin-receptor (CD51/CD61) expression.343536
Coenzyme Q10 can be administered orally, intramuscularly, intravenously, and even intrastriatally.25434445 There is very limited data on the pharmacokinetics of exogenous coenzyme Q10 in the form of intramuscular or intravenous injection. A study performed on rats observed that CoQ10, when administered intravenously, crosses the blood-brain barrier and accumulates in the brain.46
Coenzyme Q10 has a large molecular weight and is lipophilic. Oral CoQ10 supplementation has low bioavailability and limited uptake.47 Absorption and bioavailability studies show that intestinal absorption of exogenous CoQ10 is highly variable.484950 Intestinal absorption of CoQ10 is three times faster when taken with food.51
Low doses of CoQ10, following intestinal absorption in rats, appears in the lysosomes of the liver and in plasma lipoproteins. It does not however appear in other organs such as the heart and/or kidneys, and uptake in the whole body was only two to three percent of the total dose.52 Another study involving rats reports that with higher supplementation of 150 mg/day, CoQ10 appears in heart and skeletal muscle, as well as their mitochondria.53
The half-life of oral exogenous Coenzyme Q10 is approximately 33 hours.49
Pharmacokinetic studies suggest that exogenous CoQ10 does not influence endogenous biosynthesis of CoQ10. They also suggest that exogenous CoQ10 does not accumulate in plasma or tissues after ceasing supplementation.55
There is no data on the indications of coenzyme Q10 intramuscular injections. Oral coenzyme Q10 has low bioavailability. Taking CoQ10 capsules with food has been shown to increase intestinal absorption of CoQ10 threefold.51
One study found that oral doses of CoQ10 of 100 mg or higher can cause mild insomnia in some individuals.26 Some patients may benefit from taking CoQ10 in the morning.
There is no established optimum dose of exogenous coenzyme Q10 supplementation. The suggested daily dose for healthy adults is typically between 30 mg to 100 mg per day. Adults diagnosed with a medical condition may choose to take up to 60 mg to 1,200 mg per day.49 A risk assessment of oral exogenous CoQ supplementation reports the observed safe level (OSL) or highest observed intake (HOI) for oral CoQ10 as up to 1,200 mg per day for adults and up to 10 mg/day in children.11565758
There is very little data on the safety and efficacy of CoQ10 supplementation in children.
Contraindications / Precautions
Patients with a known allergy to Coenzyme Q10 should not take this product.
The literature is contradictory as to whether coenzyme Q10 has antihypertensive properties.23 In some clinical trials, coenzyme Q10 lowered both systolic and diastolic blood pressure.5929 Patients with low blood pressure should use precaution when taking CoQ10.
As an antioxidant, CoQ10 is contraindicated in patients undergoing chemotherapy and/or radiation therapy. CoQ10, and other antioxidants, may increase the risk of recurrence in cancer patients undergoing treatment.266061
Pregnancy / Breastfeeding
The safety and efficacy of CoQ-10 injections in pregnancy and breastfeeding have not been established. As such, it is difficult to determine a drug-associated risk of adverse developmental outcomes. Women who are pregnant or breast-feeding should avoid using this product.
CoQ-10 is a natural component found in human breast milk.6263 Currently, there is no data available regarding the effects of exogenous synthetic CoQ-10 on CoQ-10 concentrations in breast milk.64 Additionally, there is no data on how exogenous synthetic CoQ-10 affects milk production or its effects on the breastfed infant.
Initial studies show that oral exogenous synthetic CoQ10 may reduce the risk of developing preeclampsia during pregnancy, when administered daily to pregnant women with an increased risk for preeclampsia, starting at 20 weeks gestation.65
Coenzyme Q10 is similar in chemical structure to vitamin K.5 Research is contradictory as to whether vitamin K, and therefore coenzyme Q10, counteract the anticoagulant effects of warfarin.68697071727374 Coenzyme Q10 may increase the rate of metabolism of warfarin by selective interaction with cytochrome p450 enzymes, reducing International Normalized Ratio (INR).1036727576 One study observed an increased risk of bleeding in patients with concomitant administration of CoQ10 and warfarin.77
Early research shows a link between CoQ10 intake and reduced platelet size.36 A more recent study also shows that CoQ10 inhibits platelet aggregation.34 CoQ10 may increase the risk of bleeding in patients taking platelet agglutination inhibitor drugs, such as acetylsalicylic acid (ASAs), like aspirin; clopidogrel (Plavix); prasugrel (Effient); and ticagrelor (Brilinta).29367879
The evidence is contradictory as to whether CoQ10 improves β-cell function, enhances insulin sensitivity, and decreases blood glucose levels in patients with type 2 diabetes.2180 CoQ10 may augment the effects of other blood glucose-lowering agents, such as biguanides and sulfonylureas, and metformins in people with diabetes, and increase the risk of hypoglycemia.81
One study found that CoQ10 decreases blood glucose in individuals diagnosed with type 2 diabetes.82 CoQ10 may augment the effect of insulin and other blood glucose-lowering agents, such as sulfonylureas and metformin.83
The literature is contradictory as to whether coenzyme Q10 has antihypertensive properties.23 In some clinical trials, coenzyme Q10 lowered both systolic and diastolic blood pressure.5929 CoQ10 may augment the effects of antihypertensive medication and is therefore contraindicated in patients taking antihypertensive medication and patients with low blood pressure.
As an antioxidant, CoQ10 is contraindicated in patients undergoing chemotherapy and/or radiation therapy. CoQ10, and other antioxidants, may increase the risk of recurrence in cancer patients undergoing treatment.266061
Adverse Reactions / Side Effects
Limited research on the safety and efficacy of CoQ10 signifies that not all side effects are known. So far, major side effects of oral coenzyme Q10 supplementation have not been reported. There is no data on the side effects of intramuscular or intravenous injection of CoQ10.
Recorded side effects of oral CoQ10 supplementation in adults include rash, epigastric pain, nausea, headache, fatigue, heartburn, increased involuntary movements, anorexia, vomiting, diarrhea, pain in the upper abdomen, dizziness, irritability, sensitivity to light, and elevated liver enzymes.25298485
In children diagnosed with a mitochondrial disorder, oral CoQ10 supplementation has caused mild side effects, including nausea, diarrhea, heartburn, and less commonly reported are headache, dizziness, irritability, and agitation.81
There is no data on the short-term or long-term side effects associated with intravenous and intramuscular injection of CoQ10 in humans. There is little data on the long-term effects of oral CoQ10 supplementation. A review of clinical studies reveals that no serious or frequent side effects were observed in adults with oral administration of CoQ10 when taking 200 mg/day for up to 12 months or 100 mg/day for up to 6 years. However, the review also notes that these studies were not designed to examine side effects and therefore suggests that monitoring side effects was not a priority during these studies.86 One study saw impairments in cognitive and sensory function in mice after prolonged administration of high levels of CoQ10.87
The literature is contradictory as to whether coenzyme Q10 lowers blood pressure.2359 In some clinical trials, coenzyme Q10 lowered both systolic and diastolic blood pressure levels.2959 Coenzyme Q10 supplementation is contraindicated for patients who are taking anti‐hypertensive medication. Patients with low blood pressure should use precaution when taking CoQ10.
Store this medication at 68°F to 77°F (20°C to 25°C) and away from heat, moisture and light. Keep all medicine out of the reach of children. Throw away any unused medicine after the beyond use date. Do not flush unused medications or pour down a sink or drain.
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