A systematic approach to the therapeutic administration of peptides, involving periods of use followed by periods of cessation or reduced dosage. This strategy is employed to maximize the desired physiological effects while mitigating potential risks, such as receptor downregulation, desensitization, or suppression of endogenous hormone production. The goal of cycling is to maintain optimal receptor sensitivity and promote a more physiological, pulsatile signaling pattern.
Origin
The practice of ‘cycling’ originated in bodybuilding and sports medicine with anabolic steroids, but the principle was adapted for peptide therapeutics based on fundamental endocrinology principles. The term acknowledges that continuous supra-physiological stimulation of hormone receptors often leads to a diminished response. This clinical approach aims to mimic the body’s natural intermittent or pulsatile hormone release.
Mechanism
Continuous exposure to a peptide ligand can cause target cell receptors to be internalized or chemically modified, leading to functional desensitization. By introducing a ‘rest’ period during the cycle, the target cell has time to restore the number and sensitivity of its receptors on the cell surface. This periodic withdrawal and reintroduction helps to preserve the efficacy of the therapeutic peptide and prevent negative feedback on the body’s own endocrine axes.
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