Seremax Forte Mechanism of Action

Pharmacology: Pregabalin binds to an auxiliary subunit (a₂-δprotein) voltage-gated Calcium channels in the central nervous system.
Mecobalamin: The exact mechanism of action is not yet elucidated, it is possible that mecobalamin is needed for the synthesis of melatonin, since the biosynthetic formation of melatonin requires the donation of a methyl group.
Alpha Lipoic Acid and its reduced metabolite, dihydrolipoic acid (DHLA), form a redox couple and may scavenge a wide range of reactive oxygen species.
Alpha lipoic acid has biological antioxidant activity, antioxidant recycling activity and activity in enhancing biological energy production.
Pharmacokinetics: Pregabalin is well absorbed after oral administration, is eliminated largely by renal excretion, and has an elimination half-life about 6 hours.
Absorption and Distribution: Following oral administration of seremax capsule under fasting conditions, peak plasma concentrations occur within 1.5 hours. Pregabalin oral bioavailability is ≥90% and is independent of dose. Following single (25-300mg) and multiple-dose (75 to 900 mg/day) administration, maximum plasma concentration (Cmax) and area under plasma concentration-time curve (AUC) values increase linearly. Following repeated administration, steady state is achieved within 24 to 28 hours. Multiple-dose pharmacokinetics can be predicted from single-dose data.
The rate of pregabalin absorption is decreased when given with food, resulting in decreasing in (max of approximately 25% to 30% and an increase in Tmax approximately 3 hours. However, administration of pregabalin with food has no clinically relevant effect on the total absorption of pregabalin. Therefore, pregabalin can be taken with or without food. Pregabalin does not bind to plasma protein. The apparent volume of distribution of pregabalin following oral distribution is approximately 0.5 L/kg.
Pregabalin is a substance for system L transporter for the transport of large amino acids across the blood brain barrier. Although there are no data in human, pregabalin has been shown to cross the blood brain barrier in mice, rats, and monkey. In addition, pregabalin has been shown to cross the placenta in rats and is presented in the milk of lactating rats.
Metabolism and Elimination: Pregabalin undergoes negligible metabolism in humans. Following a dose of radiolabeled pregabalin, approximately 90% of the administered dose recovered in the uterine as unchanged pregabalin. The N-methylated derivative of pregabalin, the major metabolite of pregabalin found in the urine, accounted for 0.9% of the dose. In preclinical studies, pregabalin (S-enantiomer) did not undergo racemisation to the R-enantiomer in mice, rats, rabbits, or monkeys.
Pregabalin is eliminated from the systemic circulation primarily by renal excretion as unchanged drug with a mean elimination half-life of 6.3 hours in subjects with normal renal function. Mean renal clearance was estimated to be 67.0 to 80.9 mL/min in young healthy subjects. Because pregabalin is not found to plasma proteins this clearance rate indicates that renal tubular reabsorption is involved. Pregabalin elimination is nearly proportional to creatinine clearance (ClCr).
Mecobalamin: Absorption of Mecobalamin following oral administration. The quantity of cobalamin detected following a small oral dose of mecobalamin but significantly more cobalamin accumulates in liver tissue following administration of mecobalamin. Human urinary excretion of mecobalamin is about one third, indicating substantially greater tissue retention.
Alpha Lipoic Acid: Alpha Lipoic Acid is absorbed from the small intestine and distributed to the liver via the portal circulation and to various tissues in the body via systemic circulation. Alpha lipoic acid readily crosses the blood-brain barrier. It is found, after its distribution to the various body tissues, intracellularly, intramitochondrialy and extracellularly.