Pinaka

Uses

Mecobalamin is used for-

• Peripheral Neuropathies
• Diabetic Neuropathy
• Verteberal Syndrome
• Nerve Compression Syndrome
• Multiple sclerosis
• Amyotrophic lateral sclerosis
• Parkinson’s disease
• Alzheimer’s disease
• Diabetic retinopathy
• Entrapment neuropathy
• Drug induced neuropathy
• Megaloblastic anemia due to Vitamin B12 deficiency

HMG CoA reductase inhibitors mediated decreased level of Coenzyme Q10 in blood, Drug induced Myopathy, Protects body against free radical damage with its antioxidant property, Adjuvant therapy in cardiovascular disease especially in angina and congestive heart failure, Immune system depression, Cognitive decline, Useful in the management of Periodontal Disease

Pinaka is also used to associated treatment for these conditions: Vitamin B12 Deficiency, Nutritional supplementationMigraine

How Pinaka works

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.

Dosage

Pinaka dosage

Tablet: The usual adult dosage is one 500 mcg tablet three times daily. The dosage should be adjusted according to the age of patient and the severity of symptoms.

Injection:

• Peripheral neuropathies: The usual adult dosage is one ampoule equivalent to 500 mcg of Mecobalamin, administered intramuscularly or intravenously three times a week.The dosage should be adjusted according to the age of patient and the severity of symptoms.
• Megaloblastic anemia: The usual adult dosage is one ampoule equivalent to 500 mcg of Mecobalamin, administered intramuscularly or intravenously three times a week. After about two months of administration, dosage should be changed to one ampoule equivalent to 500 mcg of Mecobalamin every one to three months as maintenance therapy

The recommended dose of Co-enzyme Q10 is:

For Co-enzyme Q10 deficiency:150 mg daily.

For mitochondrial disorders:150-160 mg, or 2 mg/kg/day.

For heart failure in adults:100 mg per day divided into 2 or 3 doses.

For recent myocardial infarction:120 mg daily in 2 divided doses.

For high blood pressure:120-200 mg per day divided into 2 doses.

For isolated systolic hypertension:60 mg twice daily.

For preventing migraine headache:100 mg three times daily.

For Parkinsons disease:300 mg, 600 mg, 1200 mg and 2400 mg per day in 3-4 divided doses.

For infertility in men:200-300 mg per day.

For muscular dystrophy:100 mg per day.

Dividing the total daily dose by taking smaller amounts two or three times a day instead of a large amount all at once can help to reduce side effects.

Side Effects

Generally Mecobalamin is well tolerated. However, a few side effects like GI discomfort (including anorexia, nausea or diarrhea) & rash may be seen after administration of Mecobalamin.

Coenzyme Q10 is well tolerated and having no significant side effects. Mild gastrointestinal symptoms such as nausea, diarrhea and epigastric distress have been reported.

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.

Precaution

The medicine should not be used for months if there is no response at all after its use for a certain period of time.

Supplemental Coenzyme Q10 may improve beta-cell function and glycemic control in type II diabetics. Therefore, those diabetic patients who do use supplemental Coenzyme Q10 should determine by appropriate monitoring if they need to make any adjustments in their diabetic medications.

Interaction

Decreased GI tract absorption with neomycin, aminosalicylic acid, H2-blockers and colchicine. Reduced serum concentrations with oral contraceptives. Reduced effects in anaemia with parenteral chloramphenicol.

Warfarin: Supplemental Coenzyme Q10 may decrease the effectiveness of Warfarin.

Statins: The statin drugs are known to decrease Coenzyme Q10 levels in humans.

Doxorubicin: Coenzyme Q10 may increase the cardiotoxicity of doxorubicin.

Antidiabetic medications: Coenzyme Q10 may improve glycemic control in some type II diabetics. If this were to occur, antidiabetic medications might need appropriate adjusting

Volume of Distribution

Ubidecarenone is distributed to the various tissues of the body and it is able to enter the brain. 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.

Elimination Route

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. 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.

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.

Elimination Route

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. In the urine, ubidecarenone is bound to saposin B protein and represents only 8.3% of the total administered dose.

Pregnancy & Breastfeeding use

Not recommended during pregnancy & lactation.

Because of lack of information on long-term safety, pregnant women and nursing mothers should avoid Coenzyme Q10.

Contraindication

Hypersensitivity to any component of this product.

Patients with a known hypersensitivity to any component of this product

Special Warning

Use in children: Not recommended.

Storage Condition

Oral: Store at room temperature. Protect from moisture and light.

Parenteral: Store at room temperature. Do not expose to direct light.

Store in a cool & dry place, protect from light & moisture. Keep out of the reach of children.

Innovators Monograph

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