A synthetic peptide analogue of gonadotropin-releasing hormone used to treat prostate cancer, endometriosis, and advanced breast cancer.
[Blend of gonadorelin (from GONADO(TROPIN-)REL(EASING HORMONE) + –IN) and SERINE.]
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Results for goserelin
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A synthetic peptide analogue of gonadotropin-releasing hormone used to treat prostate cancer, endometriosis, and advanced breast cancer.
[Blend of gonadorelin (from GONADO(TROPIN-)REL(EASING HORMONE) + –IN) and SERINE.]
Brand names: Zoladex®
Goserelin injection
What are goserelin implants?
GOSERELIN (Zoladex® 3.6 mg Implant, Zoladex® 3-month Implant) is a man-made protein that is like a hormone in the body called gonadotropin-releasing hormone (GnRH). Regular injections of goserelin decrease the levels of testosterone in men and estrogen in women. Goserelin can be used for the relief of endometriosis, or for the treatment of prostate cancer and breast cancer. Women receive the Zoladex® 3.6 mg implant only, and injections are given every 4 weeks. Men may receive the Zoladex® 3.6 mg implant every 4 weeks, or may receive a Zoladex® 3-month implant instead. Generic goserelin implants are not yet available.What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions (some only apply to women):How should I use this medicine?
Goserelin implant is for injection subcutaneously (injection under the skin) into the upper abdominal wall. It is only administered under the supervision of a health care professional. You will need one injection a month, or one injection every three months (for men only) depending on the strength of implant used.What if I miss a dose?
It is important not to miss a dose. Call your prescriber or health care professional if you are unable to keep an appointment. You should receive your dosage within the specified time (every 4 weeks or every 3 months, depending on the implant strength)What drug(s) may interact with goserelin?
cimetidineWhat should I watch for while taking goserelin?
Visit your prescriber or health care professional for regular checks on your progress. During the first week your symptoms may get worse; check with your prescriber or health care professional if they do not improve after 2 weeks.What side effects may I notice from receiving goserelin?
Side effects that you should report to your prescriber or health care professional as soon as possible (some only apply to women):Where can I keep my medicine?
This does not apply. You will receive goserelin in a hospital or clinic setting by a trained health care professional and will not usually need to store this medication at home.Last updated: 7/1/2002
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
A synthetic peptide analogue of gonadotropin-releasing hormone used to treat endometriosis and some forms of cancer.
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Goserelin
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| Systematic (IUPAC) name | |
| N-[1-[[1-[[1-[[1-[[1-[[1-[[1-[2- [(carbamoylamino)carbamoyl]pyrrolidin-1-yl]- 5-(diaminomethylideneamino)-1-oxo -pentan-2-yl]carbamoyl]-3-methyl- butyl]carbamoyl]-2-tert-butoxy- ethyl]carbamoyl]-2-(4-hydroxyphenyl) ethyl]carbamoyl]-2-hydroxy-ethyl] carbamoyl]-2-(1H-indol-3-yl)ethyl] carbamoyl]-2-(3H-imidazol-4-yl)ethyl]- 5-oxo-pyrrolidine-2-carboxamide |
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| Identifiers | |
| CAS number | |
| ATC code | L02 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C59H84N18O14 |
| Mol. mass | 1269.410 g/mol |
| Synonyms | D-Ser(But)6Azgly10LHRH |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Protein binding | 27.3% |
| Metabolism | ? |
| Half life | 4-5 hours |
| Excretion | renal |
| Therapeutic considerations | |
| Pregnancy cat. |
D (3.6mg) / X (10.8mg) (USA) |
| Legal status |
℞ Prescription only |
| Routes | implant |
Goserelin is an injectable gonadotropin releasing hormone super-agonist (GnRH agonist). It stops the production of sex hormones (testosterone and oestrogen).
Goserelin is marketed by AstraZeneca with the brand name Zoladex.[1] It was first launched in 1987 and is currently the second-largest selling GnRH analogue in the world. It is currently available in more than one hundred markets.
Zoladex 3.6 mg subcutaneous monthly biodegradable implant was first approved by the FDA on November 3, 1989[2] for treatment of prostate cancer, a 10.8 mg subcutaneous 3-month biodegradable implant and other indications were subsequently approved.
Goserelin is an GnRH analogue. It is chemically similar to the body's natural GnRH though it has a greatly extended half-life. After administration, peak serum concentrations are reached in about two hours. It rapidly binds to the GnRH receptor cells in the pituitary gland 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. 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.[3]
Goserelin is used to treat hormone-sensitive cancers of the prostate and breast (in pre-/perimenopausal women) 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. Both depots are used for the treatment of prostate cancer, endometriosis and uterine fibroids but only the 1-month depot is approved for breast cancer, endometrial thinning and assisted reproduction.
Goserelin causes an increase in bone pain and symptoms of prostatic cancer during the first few weeks of treatment. As the body adjusts to the medication, the symptoms will disappear. Goserelin may cause hot flushes, headache, stomach upset, difficulty urinating, weight gain, swelling and tenderness of breasts, decreased erections, reduced sexual desire.
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