Gonadorelin
Gonadorelin is synthetic gonadotropin-releasing hormone (GnRH), an approved pharmaceutical. Given in pulses it stimulates pituitary release of LH and FSH; it has been used diagnostically to test pituitary function and therapeutically (via pump) for hypothalamic infertility. In hormone-replacement circles it is used to maintain testicular function, though hCG is more commonly chosen for that role.
01 Overview
Gonadorelin is identical to endogenous GnRH, the decapeptide that drives pituitary gonadotropin secretion. Because the axis responds to pulsatile rather than continuous GnRH, its clinical use reflects this: pulsatile pump administration can restore fertility in hypothalamic hypogonadism, while a single dose is used to assess pituitary responsiveness. This is a genuinely approved, well-characterised drug.
In testosterone-replacement and post-cycle contexts it is used off-label to keep the testes stimulated. Its extremely short half-life means bolus subcutaneous dosing produces only brief LH/FSH pulses, and continuous exposure paradoxically suppresses the axis (the basis for GnRH-agonist therapies), so dosing schedule matters greatly.
02 Mechanism
Acts as GnRH at pituitary gonadotroph receptors; pulsatile administration stimulates LH and FSH release, whereas continuous or high-dose exposure downregulates receptors and suppresses gonadotropins.
03 Dosing
| Tier | Dose | Route | Notes |
|---|---|---|---|
| Off-label HPTA support | 100–200 mcg | SubQ | Off-label bolus dosing, often 2-3 times weekly or daily; pulsatile pump protocols differ. Diagnostic dose ~100 mcg. |
04 Effects
| Effect | Magnitude | Evidence | |
|---|---|---|---|
| Stimulates LH and FSH releasePulsatile administration reliably triggers pituitary LH/FSH secretion. | Reproducible gonadotropin pulse | Clinical | |
| Maintains testicular function (off-label)Used to preserve testicular size/function on TRT, though hCG is better established for this. | Variable | Observational |
05 Side effects
| Effect | Severity | Frequency | Evidence | Countermeasures |
|---|---|---|---|---|
| Injection-site and hypersensitivity reactionsLocal reactions and rare hypersensitivity have been reported with clinical use. | Mild | Occasional | Clinical | |
| Axis suppression with continuous dosingNon-pulsatile or excessive dosing downregulates the axis and suppresses gonadotropins. | Moderate | Schedule-dependent | Clinical |