What are some examples of GnRH antagonists?
Currently approved GnRH antagonists include the peptide molecules abarelix, cetrorelix, degarelix, and ganirelix and the small-molecule compounds elagolix and relugolix.
What drugs are GnRH agonists?
GnRH agonists (sold under the brand names Lupron, Zoladex, Trelstar, Viadur, Vantas, Eligard and Synarel – see Table below) are drugs that lower male hormones, which has the effect of shrinking prostate tumors or slowing the growth of prostate cancer. This therapy is known as Androgen Deprivation Therapy or ADT.
What are GnRH antagonist used for?
Gonadotropin-releasing hormone (GnRH) antagonists, which became commercially available from 1999, have been used for the prevention of premature luteinizing hormone (LH) surges in controlled ovarian stimulation for in vitro fertilization or intracytoplasmic sperm injection.
What is a GnRH analogue?
GnRH analogues are synthetic drugs similar to natural GnRH. There are two main types: agonists and antagonists. They are used in IVF in order to gain control of the reproductive cycle and to prevent undesired natural secretion of LH and, therefore, ovulation. GnRH analogues are ineffective if taken orally.
Does GnRH cause weight gain?
Suppressing sex hormone levels in premenopausal women with gonadotropin-releasing hormone (GnRH) agonist therapy also causes fat gain. For example, women treated for 16 weeks with a GnRH agonist gained 1.0 kg of fat, which equates to an energy excess of about 80 kcal per day.
What is GnRH used for?
| Gonadotropin-releasing hormone agonist | |
|---|---|
| Use | Fertility medicine; Prostate cancer; Breast cancer; Menorrhagia; Endometriosis; Uterine fibroids; Hyperandrogenism; Hirsutism; Precocious puberty; Transgender people; Chemical castration for paraphilias and sex offenders |
| Biological target | GnRH receptor |
| Chemical class | Peptides |
What does a GnRH analogue do when given to a woman?
GnRH agonists are a group of drugs that have been used to treat women with endometriosis for over 20 years [1]. They are modified versions of a naturally occurring hormone known as gonadotropin releasing hormone, which helps to control the menstrual cycle.
What are GnRH antagonist drugs?
Antagon® (ganirelix acetate) and Cetrotide® (cetrorelix) are GnRH antagonists (hormonal drugs) which are currently approved for enhancing response to ovulation inducing drugs, and specifically to prevent premature ovulation. GnRH antagonists have not been shown to cause major side effects in humans so far.
What is the side effect of GnRH?
Common side effects of the GnRH agonists and antagonists include symptoms of hypogonadism such as hot flashes, gynecomastia, fatigue, weight gain, fluid retention, erectile dysfunction and decreased libido. Long term therapy can result in metabolic abnormalities, weight gain, worsening of diabetes and osteoporosis.
Does GnRH cause weight loss?
Conclusion: Hypogonadism by GnRH agonist therapy induces lean mass loss, increased adiposity overall, and upper body fat accumulation.
How long does it take for GnRH to work?
You should notice an improvement in your symptoms within 4–8 weeks of beginning treatment, but some women will experience a temporary worsening of symptoms in the first 2 weeks.
How long can you take GnRH?
GnRH-a is given one of three ways: It can be injected into a muscle once a month. It is also available in a dose that lasts for 3 months. It can be injected under the skin of your belly once every 28 days.
Can a gonadotropin analogue replace a GnRH agonist?
This or similar drugs may eventually replace GnRH agonists in the treatment of ferret adrenal disease. Gonadotropin-releasing hormone analogues initially stimulate the pituitary gland, resulting in increased concentrations of luteinizing hormone and testosterone in men.
Are there any GnRH antagonists that are effective?
GnRH antagonists are being studied in people for treatment of the same diseases as are agonists. Theoretically, antagonists should be more effective than agonists at a much lower dosage. In human medicine, an antagonist called abarelix is being evaluated to determine its ability to inhibit the action of GnRH.
How are GnRH analogues different from histamine antagonists?
Due to the peptide nature of the synthetic analogues oral administration and potential gastrointestinal enzymatic degradation poor bioavailability results necessitating a parenteral delivery system. Some GnRH antagonists have been associated with significant histamine release, inhibiting their widespread use.
How are GnRH agonists and antagonists used in prostate cancer treatment?
The gonadotropin releasing hormone (GnRH) agonists and antagonists are short peptide analogues of GnRH that cause a profound inhibition of estrogen and androgen synthesis and are used predominantly as androgen deprivation therapy of advanced prostate cancer.