Camelon 4/Camelon 8 Mechanism of Action

Pharmacology: Camelon 4: Pharmacodynamics: Naturally occurring glucocorticoids (Hydrocortisone), which also have salt-retaining properties, are used as replacement therapy in adrenocortical deficiency states. Their synthetic analogs are primarily used for their potent anti-inflammatory effects in disorder of many organ systems. It has greater anti-inflammatory potency than Prednisolone to induce sodium and water retention. The relative potency of Methylprednisolone to Hydrocortisone is at least four to one. Glucocorticoids cause profound and varied metabolic effects. In addition, they modify the body's immune responses to diverse stimuli.
Pharmacokinetics: Absorption: Methylprednisolone is rapidly absorbed and the maximum plasma Methylprednisolone concentration is achieved around 1.5 to 2.3 hours across doses following oral administration in normal healthy adults. The absolute bioavailability of Methylprednisolone in normal healthy subjects is generally high (82% to 89%) following oral administration.
Distribution: Methylprednisolone is widely distributed into the tissues, crosses the blood-brain barrier, and is secreted in breast milk. Its apparent volume of distribution is approximately 1.4 L/kg. The plasma protein binding of Methylprednisolone in humans is approximately 77%.
Metabolism: In humans, Methylprednisolone is metabolized in the liver to inactive metabolites, the major ones are 20β-hydroxymethylprednisolone and 20β-hydroxymethylprednisolone. Metabolism in the liver occurs primarily via the CYP3A4 enzyme. For a list of drug interactions based on CYP3A4-mediated metabolism see INTERACTIONS.
Methylprednisolone, like many CYP3A4 substrates, may also be a substrate for the ATP-binding cassette (ABC) transport protein p-glycoprotein, influencing tissue distribution and interactions with other medicines.
Elimination: The mean elimination half-life for total Methylprednisolone is in the range of 1.8 to 5.2 hours. Methylprednisolone clearance is altered by concurrent administration of Troleandomycin, Erythromycin, Rifampicin, Anticonvulsants and Theophylline. No dosing adjustments are necessary in renal failure.
(Pharmacodynamic and pharmacokinetic data are obtained from the clinical data of the innovator product, MEDROL Tablet).
Camelon 8: Methylprednisolone, a semisynthetic derivative of the natural renal cortex hormone, cortisol.
Methylprednisolone has glucocorticoid actions.
In common with other glucocorticoids, Methylprednisolone influences the metabolism in almost all tissues. These effects are vital to maintain the body's homeostasis and to regulate the activities of the immune system.