Gonadorelin acetate

Stability

Gonadorelin acetate is stable for at least 12 months at 24 degrees Celsius and 50 per cent relative humidity and does not degrade even under accelerated storage conditions. Similarly, the lyophilised product has shown excellent stability when stored at 24 °C at 50% relative humidity for at least 18 months. The reconstituted gonadotropin acetate is stable for at least 45 days at 24 °C or 37 °C. The reconstituted gonadotropin acetate is stable for at least 12 months at 24 °C and 50% relative humidity.

Description

Gonadorelin acetate is a synthetic version of the naturally occurring gonadotropin-releasing hormone (GnRH). It’s a decapeptide (composed of 10 amino acids) that interacts primarily with the pituitary gland. When administered, it stimulates the pituitary’s gonadotrope cells to release two key reproductive hormones:
Luteinizing hormone (LH)；
Follicle-stimulating hormone (FSH)；
Due to its ability to influence reproductive hormone production, it’s used medically to treat various reproductive disorders. Gonadorelin acetate has multiple indications, including for males and females with congenital hypogonadotropic hypogonadism and females with functional HA. An example of functional HA is the “female athlete triad”, in which they lose their menses. Gonadorelin acetate is also used for women with infertility (idiopathic fertility or infertility related to PCOS) who do not respond to clomid or letrozole. At this point, patients can either do gonadotropin therapy with controlled ovarian hyperstimulation (“essentially IVF [in vitro fertilization]”) or undergo FSH therapy (ovulation induction therapy). However, some patients are deficient in LH, which is responsible for making estradiol. In this case, solo therapies such as Gonal-F? (follitropin alfa) or prominent FSH treatments are insufficient, and patients need to utilize combination FSH and hCG therapies or human menopausal gonadotropins (HMG, “which is the combined FSH and LH”) instead.

Uses

Luteinizing hormone releasing hormone human acetate salt has been used:

• for synchronization of the ovulations
• for pre-absorption of the anti-GnRH antibody in staining procedures
• to study pituitary sensitivity to GnRH in presence of endocrine disrupting compound

Application

Gonadorelin acetate is widely used in the diagnosis of central precocious puberty.

Biochem/physiol Actions

Hypothalamic peptide that stimulates release of gonadotrophins from anterior pituitary, thus regulating reproductive functions.

Side effects

Gonadorelin acetate is usually considered a safe medication. However, severe anaphylactic shock may occur after intravenous administration, manifested by loss of consciousness and tonic convulsions of the arms and legs; prompt treatment with epinephrine, diphenhydramine and fluids restores vital signs within 30 minutes. Therefore, it is recommended that these drugs be administered in an environment that is capable of handling systemic reactions.