MEGALIN

Each hard gelatin capsule contains:

(Pregabalin IP 75 mg / 150 mg )

Capsule for Oral Use

Although Pregabalin is a structural derivative of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), it does not bind directly to GABA or benzodiazepine receptors. 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.

PHARM

Absorption: After oral dosing administered in the fasted state, Pregabalin absorption is rapid, and extensive. Pregabalin oral bioavailability is reported to be ≥90% regardless of the dose. Cmax is attained within 1.5 hours after single or multiple doses, and steady state is attained within 24-48 hours with repeated administration. Both Cmax and AUC appear to be dose proportional.

Distribution: After oral administration of Pregabalin, the reported apparent volume of distribution is roughly 0.5 L/kg. Although Pregabalin is not very lipophilic, it is able to cross the blood brain barrier (BBB). Pregabalin is not plasma protein bound.

Metabolism & Excretion: Less than 2% of Pregabalin is metabolized and it is excreted virtually unchanged in the urine.

Half Life: The elimination half- life of Pregabalin is 6.3 hours.

ACOKINETICS

• Diabetic Peripheral Neuropathic Pain
• Post herpetic Neuralgia
• Fibromyalgia
• Adjunctive therapy in Partial Onset Seizure
• Neuropathic Pain with Spinal Cord Injury

ADVERSE REACTION:

The most common side effects of this drug are drowsiness and dizziness. Other less common side effects experienced may be dry mouth, diarrhea, constipation and nausea

DOSAGE AND ADMINISTRATION: 150 mg to 300 mg per day in 2 to 3 divided dose.

CONTRAINDICATIONS:

• Hypersensitivity to any ingredients of formulation

WARNINGS AND PRECAUTIONS:

• This medicine has been associated with dizziness and somnolence, which could increase the occurrence of accidental injury (fall) in elderly patients.
• This medicine may cause blurring or loss of vision, or other changes in eyesight, many of which are temporary.
• Some patients with diabetes who gain weight while taking Pregabalin may need an alteration in their diabetic medicines.
• There have been reports of kidney failure in some patients when taking this medicine. If while taking this medicine you notice decreased urination, you should tell your doctor as stopping the medicine may improve this.
• It is advised not to drink alcohol while taking this medicine
• Do not take more medicine than prescribed.
• There have been reports of convulsions when taking this medicine or shortly after stopping this medicine. If you experience a convulsion, contact your doctor immediately.
• Contact your doctor if you experience trouble breathing or shallow breaths.