Testosterone undecanoate is a long-acting esterified form of the primary androgen testosterone, utilized clinically for the effective treatment of male hypogonadism and other conditions requiring sustained androgen replacement. The undecanoate ester is chemically attached to the parent testosterone molecule to significantly increase its lipid solubility, allowing for a prolonged, steady release and a much less frequent dosing schedule. It is currently available in both oral and injectable formulations, each offering distinct and predictable pharmacokinetic profiles.
Origin
This specific compound was developed in pharmaceutical chemistry to overcome the rapid metabolism and very short half-life of native, un-esterified testosterone, thereby providing a more convenient and pharmacokinetically stable therapeutic option. The use of long-chain fatty acid esters for creating a drug depot effect is a well-established and common principle in modern pharmacology.
Mechanism
Following administration, the testosterone undecanoate is stored in lipid depots, from which it is slowly and continuously released into the systemic circulation over an extended period. Plasma esterases then systematically hydrolyze the ester bond, cleaving the undecanoate chain and releasing active, bioidentical testosterone into the bloodstream. This slow, continuous release profile is designed to help maintain relatively stable serum testosterone concentrations, minimizing the supraphysiological peaks and profound troughs often seen with shorter-acting esters.
Combining oral hormones with fasting demands clinical precision to harmonize the metabolic benefits of fasting with the absorption needs of the therapy.
Fasting's impact on oral hormone absorption is molecule-specific, enhancing some like levothyroxine while inhibiting others like testosterone that require dietary fat.
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