Goserelin
Encyclopedia
Goserelin acetate is an injectable gonadotropin releasing hormone superagonist
(GnRH agonist), also known as a luteinizing hormone releasing hormone (LHRH) agonist
. Structurally, it is a decapeptide. Goserelin acetate is used to suppress production of the sex hormones (testosterone
and oestrogen), particularly in the treatment of breast and prostate cancer.
Goserelin acetate stimulates the production of the sex hormones testosterone and oestrogen in a non-pulsatile (non-physiological) manner. This causes the disruption of the endogenous hormonal feedback systems, resulting in the down-regulation of testosterone and oestrogen production.
Zoladex approved by the U.S. Food and Drug Administration in 1989 for treatment of prostate cancer.
thus leading to an initial increase in production of luteinizing hormone
and thus leading to an initial increase in the production of corresponding sex hormones. This initial flare may be treated by co-prescribing/co-administering Casodex (Bicalutamide) or similar medication. Eventually, after a period of about 14–21 days, production of LH is greatly reduced due to receptor downregulation, and sex hormones are generally reduced to castrate levels.
Goserelin Acetate is used to treat hormone-sensitive cancers of the breast
(in pre- and peri- menopausal women) and prostate
, and some benign gynaecological disorders (endometriosis
, uterine fibroids and endometrial thinning). In addition, goserelin is used in assisted reproduction and in the treatment of precocious puberty
. It is available as a 1-month depot and a long-acting 3-month depot.
production, before the receptors are desensitised and hormonal production is inhibited. The symptoms will disappear, with hormonal inhibition. It is therefore advisable to co-treat with an antiandrogen
during the first 2-3 weeks of Gosrelin treatment, particularly in patients with pre-existing bone symptoms. Goserelin may cause bone pain
, hot flushes, headache
, stomach upset
, depression
, difficulty urinating
(isolated cases), weight gain
, swelling and tenderness of breasts (infrequent), decreased erections
and reduced sexual desire. Bone pain can be managed symptomatically, and decreased libido can be treated by Levitra (Vardenafil
) or other similar oral therapies.
Memory loss may be severe and may not return to normal levels.
Superagonist
An irreversible agonist is a type of agonist that binds permanently to a receptor in such a manner that the receptor is permanently activated. It is distinct from a mere agonist in that the association of an agonist to a receptor is reversible, whereas the binding of an irreversible agonist to a...
(GnRH agonist), also known as a luteinizing hormone releasing hormone (LHRH) agonist
Agonist
An agonist is a chemical that binds to a receptor of a cell and triggers a response by that cell. Agonists often mimic the action of a naturally occurring substance...
. Structurally, it is a decapeptide. Goserelin acetate is used to suppress production of the sex hormones (testosterone
Testosterone
Testosterone is a steroid hormone from the androgen group and is found in mammals, reptiles, birds, and other vertebrates. In mammals, testosterone is primarily secreted in the testes of males and the ovaries of females, although small amounts are also secreted by the adrenal glands...
and oestrogen), particularly in the treatment of breast and prostate cancer.
Goserelin acetate stimulates the production of the sex hormones testosterone and oestrogen in a non-pulsatile (non-physiological) manner. This causes the disruption of the endogenous hormonal feedback systems, resulting in the down-regulation of testosterone and oestrogen production.
Zoladex approved by the U.S. Food and Drug Administration in 1989 for treatment of prostate cancer.
Pharmacokinetics
Goserelin is a synthetic analogue of a naturally occurring luteinising-hormone releasing hormone (LHRH). Bioavailability is almost complete. Goserelin is poorly protein bound and has a serum elimination half-life of two to four hours in patients with normal renal function. The half-life increases with patients with impaired renal function. There is no significant change in pharmacokinetics in subjects with hepatic failure. After administration, peak serum concentrations are reached in about two hours. It rapidly binds to the LHRH receptor cells in the pituitary glandPituitary gland
In vertebrate anatomy the pituitary gland, or hypophysis, is an endocrine gland about the size of a pea and weighing 0.5 g , in humans. It is a protrusion off the bottom of the hypothalamus at the base of the brain, and rests in a small, bony cavity covered by a dural fold...
thus leading to an initial increase in production of luteinizing hormone
Luteinizing hormone
Luteinizing hormone is a hormone produced by the anterior pituitary gland. In females, an acute rise of LH called the LH surge triggers ovulation and development of the corpus luteum. In males, where LH had also been called interstitial cell-stimulating hormone , it stimulates Leydig cell...
and thus leading to an initial increase in the production of corresponding sex hormones. This initial flare may be treated by co-prescribing/co-administering Casodex (Bicalutamide) or similar medication. Eventually, after a period of about 14–21 days, production of LH is greatly reduced due to receptor downregulation, and sex hormones are generally reduced to castrate levels.
Indications
Breast cancer
Breast cancer is cancer originating from breast tissue, most commonly from the inner lining of milk ducts or the lobules that supply the ducts with milk. Cancers originating from ducts are known as ductal carcinomas; those originating from lobules are known as lobular carcinomas...
(in pre- and peri- menopausal women) and prostate
Prostate cancer
Prostate cancer is a form of cancer that develops in the prostate, a gland in the male reproductive system. Most prostate cancers are slow growing; however, there are cases of aggressive prostate cancers. The cancer cells may metastasize from the prostate to other parts of the body, particularly...
, and some benign gynaecological disorders (endometriosis
Endometriosis
Endometriosis is a gynecological medical condition in which cells from the lining of the uterus appear and flourish outside the uterine cavity, most commonly on the ovaries. The uterine cavity is lined by endometrial cells, which are under the influence of female hormones...
, uterine fibroids and endometrial thinning). In addition, goserelin is used in assisted reproduction and in the treatment of precocious puberty
Precocious puberty
As a medical term, precocious puberty describes puberty occurring at an unusually early age. In most of these children, the process is normal in every respect except the unusually early age, and simply represents a variation of normal development. In a minority of children, the early development is...
. It is available as a 1-month depot and a long-acting 3-month depot.
Side effects
Goserelin Acetate may cause a temporary increase in bone pain and symptoms of prostatic cancer during the first few weeks of treatment. This is known as the tumour flare effect, and is the result of an initial increase in luteinizing hormoneLuteinizing hormone
Luteinizing hormone is a hormone produced by the anterior pituitary gland. In females, an acute rise of LH called the LH surge triggers ovulation and development of the corpus luteum. In males, where LH had also been called interstitial cell-stimulating hormone , it stimulates Leydig cell...
production, before the receptors are desensitised and hormonal production is inhibited. The symptoms will disappear, with hormonal inhibition. It is therefore advisable to co-treat with an antiandrogen
Antiandrogen
Antiandrogens, or androgen antagonists, first discovered in the 1960s, prevent androgens from expressing their biological effects on responsive tissues. Antiandrogens alter the androgen pathway by blocking the appropriate receptors, competing for binding sites on the cell's surface, or affecting...
during the first 2-3 weeks of Gosrelin treatment, particularly in patients with pre-existing bone symptoms. Goserelin may cause bone pain
Bone pain
Bone pain is a debilitating form of pain emanating from the bone tissue. It occurs as a result of a wide range of diseases and/or physical conditions and may severely impair the quality of life for patients who suffer from it...
, hot flushes, headache
Headache
A headache or cephalalgia is pain anywhere in the region of the head or neck. It can be a symptom of a number of different conditions of the head and neck. The brain tissue itself is not sensitive to pain because it lacks pain receptors. Rather, the pain is caused by disturbance of the...
, stomach upset
Abdominal pain
Abdominal pain can be one of the symptoms associated with transient disorders or serious disease. Making a definitive diagnosis of the cause of abdominal pain can be difficult, because many diseases can result in this symptom. Abdominal pain is a common problem...
, depression
Depression (mood)
Depression is a state of low mood and aversion to activity that can affect a person's thoughts, behaviour, feelings and physical well-being. Depressed people may feel sad, anxious, empty, hopeless, helpless, worthless, guilty, irritable, or restless...
, difficulty urinating
Urinary retention
Urinary retention, also known as ischuria, is a lack of ability to urinate. It is a common complication of benign prostatic hyperplasia , although it can also be caused by nerve dysfunction, constipation, infection, or medications...
(isolated cases), weight gain
Weight gain
Weight gain is an increase in body weight. This can be either an increase in muscle mass, fat deposits, or excess fluids such as water.-Description:...
, swelling and tenderness of breasts (infrequent), decreased erections
Erectile dysfunction
Erectile dysfunction is sexual dysfunction characterized by the inability to develop or maintain an erection of the penis during sexual performance....
and reduced sexual desire. Bone pain can be managed symptomatically, and decreased libido can be treated by Levitra (Vardenafil
Vardenafil
Vardenafil is a PDE5 inhibitor used for treating erectile dysfunction that is sold under the trade names Levitra and Staxyn.-History:...
) or other similar oral therapies.
Memory loss may be severe and may not return to normal levels.
External links
- One man's experience of prostate cancer treatment using goserelin - BBC NewsBBC NewsBBC News is the department of the British Broadcasting Corporation responsible for the gathering and broadcasting of news and current affairs. The department is the world's largest broadcast news organisation and generates about 120 hours of radio and television output each day, as well as online...