For the use of a Registered Medical Practitioner, Hospital or Laboratory only.
1. Description
Costead contains ubiquinol (CoQH2), the reduced form of coenzyme Q10 (CoQ10), which acts as an active antioxidant that prevents the initiation and propagation of lipid peroxidation in biological membranes and human low-density lipoprotein (LDL). It plays an essential role in maintaining cellular defence against oxidative damage and also sustains the effects of vitamin E by regenerating the vitamin from the tocopheroxyl radical.
2. Composition
Each hard gelatin capsule contains:
- Ubiquinol Acetate (Bioavailable CoQ10) – 100 mg
- Excipients – q.s.
Approved colours used in empty capsule shells.
3. Dosage Form
Hard gelatin capsule
4. Pharmacology
Pharmacodynamics
Pharmacological class: Antioxidant; mitochondrial electron transport chain cofactor (Ubiquinol/Coenzyme Q10).
Mechanism of Action
Ubiquinol is the reduced, active form of Coenzyme Q10 and functions as an essential cofactor in the mitochondrial electron transport chain, facilitating electron transfer between Complex I/II and Complex III to support ATP production.
It acts as a potent lipid-soluble antioxidant, scavenging reactive oxygen species (ROS) and preventing lipid peroxidation of cellular and mitochondrial membranes.
Ubiquinol regenerates oxidized vitamin E (α-tocopherol), thereby enhancing endogenous antioxidant defenses.
It helps preserve mitochondrial membrane integrity, improves cellular energy metabolism, and reduces oxidative stress associated with aging and chronic diseases.
In patients with chronic kidney disease (CKD), supplementation may help reduce oxidative stress and support renal and cardiovascular health as an adjunct to standard therapy.
Clinical background: CoQ10 deficiency has been reported in congestive heart failure,9,10 Type 2 diabetes,11,12 hepatitis,13 liver cirrhosis,13 hepatocellular carcinomas,13 ALS,14 Alzheimer’s disease,15 juvenile fibromyalgia16 and Down’s syndrome.17 Statin drugs inhibit the endogenous production of CoQ10, which has been implicated in fatigue and myalgia; Ubiquinol replenishes CoQ10 stores in these patients.18,19 Supplementation with Ubiquinol improves dyslipidaemia-related endothelial function and increases serum nitric oxide levels.20,21
Pharmacokinetics
Absorption
Ubiquinol is administered orally.
Being highly lipophilic, it is absorbed through the gastrointestinal tract along with dietary lipids.
Following absorption, it is incorporated into chylomicrons, enters the lymphatic system, and subsequently reaches the systemic circulation.
Time to maximum plasma concentration (Tmax): Approximately 6.5 hours.
Distribution
In circulation, Ubiquinol is transported mainly by VLDL and LDL, with smaller amounts associated with HDL.
Approximately 95% of circulating CoQ10 exists in the reduced (ubiquinol) form.
It is widely distributed to tissues with high energy requirements, including the heart, kidneys, liver, and skeletal muscle.
Metabolism
Ubiquinol undergoes reversible oxidation to ubiquinone as part of the mitochondrial redox cycle and participates continuously in cellular energy production and antioxidant defense.
Elimination
CoQ10 is eliminated mainly via the biliary route in the faeces; only small amounts are excreted in the urine.
Elimination half-life (t½): Approximately 33 hours.
Chronic administration produces a dose-dependent increase in plasma CoQ10 concentrations. Compared with ubiquinone, ubiquinol achieves higher plasma levels because of its greater bioavailability.
5. Indications
Supplementation with Ubiquinol replenishes depleted levels and circumvents CoQ10 deficiency.1,2,7-8
6. Contraindications
None
7. Precautions
None
Pregnancy and Lactation: There are no adequate and well-controlled studies in pregnant or lactating women to establish safety.
8. Drug Interactions
Because of its structural similarity to vitamin K, it has been suggested that CoQ10 may have procoagulant activity and interfere with warfarin. While there are reports of individual case studies showing the interaction of CoQ10 and warfarin,22,23 other case studies involving highly monitored patients on warfarin specifically noted no interactions with CoQ10.9 A randomized, double-blind, placebo-controlled study designed to assess the effect of CoQ10 on warfarin also showed no effect.24 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.25
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 changes to the diet, 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.26
9. Adverse Effects
Costead is generally well tolerated. As with any dietary supplement, some gastrointestinal discomfort may be experienced.
10. 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
Administration: Oral administration
Capsule should be swallowed whole and not opened, chewed or crushed.
11. Overdosage
No data available.
12. Storage
Store in a dry place at a temperature not exceeding 30°C. Protect from light. Keep the medicine out of reach of children.
Additional Information
Key Benefits
- Costead helps reduce oxidative stress
- Ubiquinol is the reduced, active antioxidant form of Coenzyme Q10.
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.
Additional pharmacokinetic information
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.3,4 A major portion of CoQ10 in tissues is in the reduced form as Ubiquinol.5
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.6
13. Presentation
10 Capsules in a strip, 1 strip in a box.