Definition
Like goserelin, triptorelin, buserelin and leuprorelin (Raja 2022), histrelin is a gonadotropin-releasing hormone agonist (GnRH) (Herold 2022).
Histrelin has been on the market since 2007 (Raja 2022). In the same year, it was approved for use in children with pubertas praecox (Olson- Kennedy 2021).
Pharmacodynamics
Histrelin inhibits the release of LH and FSH, which in turn reduces the testosterone concentration and thus inhibits hormone-dependent tumor growth. The bioavailability is 92 % and the plasma half-life is up to 4 h (Nabieva 2024).
When used s. c. as a 50 mg implant in pubertas praecox, there is a strong suppression of the hypothalamic-pituitary-gonadal axis (HPG) after approx. one month (Eugster 2016).
Indication
- Advanced prostate carcinoma as part of palliative therapy with chemical castration (Nabieva 2024 / Freissmuth 2012)
- Central pubertas praecox (Eugster 2015)
- On the suppression of puberty in transgender people (Olson- Kennedy 2021)
- Endometriosis
- Certain forms of breast carcinoma
- Uterus myomatosus
- Myomas (Freissmuth 2012)
Dosage and type of application
Histrelin is used as an implant (Nabieva 2024). It is effective for 12 months (Raja 2022).
Undesirable effects
- Hot flushes
- Headaches, joint and bone pain
- depression
- insomnia
- Respiratory diseases
- Liver diseases
- Local reactions at the site of application
- Gynecomastia
- Neuropathies
- dizziness
- dyspnea
- Nausea
- Constipation (Nabieva 2024)
- Removal of the implant in pubertas praecox has an approx. 25 % rupture rate (Eugster 2015)
Contraindication
Hypersensitivity to GnRH analogs (Nabieva 2024)
Preparations
Vantas®