CAPSULE Presentation

Each hard gelatin capsule contains:
Methylcobalamin JP 750 mcg
Pregabalin IP              75 mg


Pregabalin is structurally similar to gamma-aminobutyric acid (GABA) - an inhibitory neurotransmitter. It may be used to manage neuropathic pain, postherpetic neuralgia, and fibromyalgia among other conditions. Methylcobalamin, the activated form of vitamin B12, has protection by promoting regeneration of injured nerves and antagonizing glutamate-induced neurotoxicity.been used to treat some nutritional diseases and other diseases in clinic. It exerts neuronal

Indications

  • Neuropathic Pain
  • Diabetic Peripheral Neuropathic Pain (DPN)
  • Effectively supports brain and nerve function
  • Treatment of fibromyalgia

Mechanism of action

Pregabalin is structural analogue of gamma-aminobutyric acid (GABA), it does not bind to GABA receptors. Instead, it binds the alpha2-delta subunit of presynaptic voltage-gated calcium channels in the central nervous system. By binding presynaptically to the alpha2-delta subunit of voltage-gated calcium channels in the central nervous system, pregabalin modulates the release of several excitatory neurotransmitters including glutamate, substance-P, norepinephrine, and calcitonin gene related peptide. In addition, pregabalin prevents the alpha2-delta subunit from being trafficked from the dorsal root ganglia to the spinal dorsal horn, which may also contribute to the mechanism of action Pregabalin does not modulate dopamine receptors, serotonin receptors, opiate receptors, sodium channels or cyclooxygenase activity.

Vitamin B12 or Methylcobalamin deficiency has been associated with significant neurological pathology, especially peripheral neuropathy. Cyanocobalamin is the principal form used in vitamin supplements, while methylcobalamin is a coenzyme form that acts as an important co-factor in the activities of vitamin B12-dependent methyltransferases. It is required for integrity of myelin, neuronal function, proper red blood cell formation and DNA synthesis. Methylcobalamin helps in the synthesis of neuronal lipids, regeneration of axonal nerves and has neuroprotective activity, which promote neurons to function in proper way.

Pharmacokinetics of Pregabalin

Absorption: Pregabalin is rapidly absorbed from GIT
Bioavailability is about 90%
Volume of Distribution: Volume of Distribution is approximately 0.56 L/kg
It is not bound to plasma proteins
Metabolism: Negligible amount is metabolised
Excretion: Excreted unchanged mainly from urine

Pharmacokinetics of Mecobalamin

Absorption: Peak plasma concentrations after 3 hours
Excretion: Majorly excreted in urine

Side Effects

  • Dizziness
  • Drowsiness
  • Dry mouth
  • Constipation
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