Methylcobalamin is the neurologically active form of vitamin B12. Vitamin B12 comes in several kinds including hydroxy, cyano, and adenosyl, but only the methyl and adenosyl forms are active within the body. Methylcobalamin donates methyl groups to the myelin sheath that insulates nerve fibres and regenerates damaged neurons. In a B12 deficiency, toxic fatty acids destroy the myelin sheath but high enough doses of B12 can repair it. Animal studies have shown that high doses of Methylcobalamin are effective in neuron regeneration and that there is no known toxicity at these doses.
It has been demonstrated by recent studies that combination of Pregabalin and Methylcobalamin shows significantly better symptoms relief with the modest improvement of nervous system, chronic pain, perioperative pain, migraine and enhances immune system function.
Indications and Usage:
● It is used for neuropathic pain associated with spinal cord injury.
● Diabetic peripheral neuropathy.
● Treatment of fibromyalgia.
● It is also used for treatment of chronic pain, perioperative pain, and migraine.
● Supports the nervous system
● Helps memory and learning
● Boosts energy
● Helps control homocysteine levels
● Promotes a healthy cardiovascular system
● Enhances immune system function
● Effectively supports brain and nerve function.
Drug Interactions:
BEFORE TAKING THIS MEDICINE TELL THE DOCTOR ABOUT ANY MEDICAL PROBLEMS AN ALLERGIES THAT PATIENT HAS NOW OR HAS HAD.
Usually drug interactions occur when it is taken with another drug or with food. Before you take a medication for a particular ailment, you should inform the health expert about intake of any other medications including non-prescription medications.
Mechanism of action:
Combination of Pregabalin and Methylcobalamin not only decreases the release of neurotransmitters but also helps in regeneration of the myelin sheath. Pregabalin also has got analgesic activity which reduces the pain associated with neuropathy. Thus the combination of Pregabalin and Methylcobalamin is useful for arresting the progress of diabetic neuropathy and also helps in relieving the pain associated with neuropathy. Methylcobalamin is a co-factor of methionine synthase, an enzyme that transfers methyl groups to homocysteine to regenerate methionine. Elevated homocysteine levels are a risk factor for coronary artery disease. Methionine can be transformed to S-adenoxylmethionine (SAM) that is involved in a variety of methylation reactions in the body, one of which is alleviating depression.
Pharmacodynamics:
It binds to the α2δ (alpha2delta) subunit of the voltage-dependent calcium channel in the central nervous system. It help to decreases the release of neurotransmitters including glutamate, norepinephrine, substance P and calcitonin gene-related peptide. However, unlike anxiolytic compounds (e.g., benzodiazepines) which exert their therapeutic effects through binding to GABA, and benzodiazepine receptors. It neither binds directly to these receptors nor augments GABA currents or affects GABA metabolism. The half life for pregabalin is 6.3 hours.
Pharmacokinetics of Pregabalin:
Absorption:Pregabalin is rapidly absorbed when administered on an empty stomach, with peak plasma concentrations occurring within one hour. Pregabalin oral bioavailability is estimated to be greater than or equal to 90% and is independent of dose. The rate of pregabalin absorption is decreased when given with food resulting in a decrease in Cmax by approximately 25 to 30% and a delay in Tmax to approximately 2.5 hours. Administration with food, however, has no clinically significant effect on the extent of absorption.
Distribution:In humans, the volume of distribution of pregabalin for an orally administered dose is approximately 0.56 L/kg and is not bound to plasma proteins.
Metabolism: Pregabalin undergoes negligible metabolism in humans. Approximately 98% of the radioactivity recovered in the urine was unchanged pregabalin. The major metabolite is N-methyl pregabalin.
Excretion:Pregabalin is eliminated from the systemic circulation primarily by renal excretion as unchanged drug. Renal clearance of pregabalin is 73 mL/minute.
Pharmacokinetics of Methylcobalamin:
Mecobalamin is the neurologically active form of vitamin B12 and occurs as a water-soluble vitamin in the body. It is a cofactor in the enzyme methionine synthase, which functions to transfer methyl groups for the regeneration of methionine from homocysteine. In anaemia, it increases erythrocyte production by promoting nucleic acid synthesis in the bone marrow and by promoting maturation and division of erythrocytes.
Absorption: Peak plasma concentrations after 3 hr (oral); 0.9 hr (IM); 3 min (IV).
Excretion: Via urine.
Side Effects:
● Dizziness
● Drowsiness
● Dry mouth
● Constipation
Conclusion:
From the above discussion, it can be concluded that Pregabalin and Methylcobalamin tablet could improve the quality of life with improvement of nervous system, chronic pain, perioperative pain, migraine and enhances immune system function and responsible for healthy cardiovascular system.
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Contraindications:
Pregabalin is contraindicated in patients with known hypersensitivity to pregabalin or any of its components. Vitamin B12 supplementation is generally regarded as safe during pregnancy and lactation.
Storage:
Store at room temperature, 15-30° C (59-86°F). Keep away from moisture.