acetate belongs to a super-agonist class of drugs and is an injectible gonadotropin releasing hormone
drug. It is also known as a lutenizing hormone-releasing hormone (LHRH). It is used to suppress the production of sex hormones
estrogen and testosterone.
Goserelin Acetate, or marketed under the trade name Zoladex by the pharmaceutical company AstraZeneca, is indicated for the treatment of conditions like advanced breast cancer
in women and prostate cancer
in males. Its main action is to suppress the production of the sex hormones testosterone and estrogen, as some cancers are hormone dependent.
Goserelin, or zoladex is administered subcutaneously at a dosage of 10.8 mg. It should be taken every 12 weeks into the anterior abdominal walls below the navel line.
The drug is supplied as 10.mg sterile, biodegradable product. The implant contains an equivalent of 10.8 mg goserelin acetate. They are also available at implants with an equivalent of 3.6 mg of goserelin acetate, designed for an administration every 28 days.
The drug has been reported to be well tolerated in most clinical trials. The reported side effects were very rare and were unlikely to happen. The most common of these side effects were the changes brought by reduction of hormones.
There are very rare cases of non-threatening side effects such as allergic reactions
to the drug (rashes, hives
, pain at the injection site) reported with the use of the drug. Some side effects of the drug include allergic reactions such as hives, swelling
of the face, lips
and injection sites. Pain in the injection sites, numbness, redness and swelling of the skin and difficulty in breathing may also be some of the side effects of the drug.
Similarly with other hormonal therapies, hypercalcemia (elevated calcium
levels) was reported as side effects of the drug. Most of the side effects commonly reported were physiological effects of the decrease in hormones – hot flashes, sexual dysfunction, and a decrease in erections.
There have been no known drug interactions conducted with the use of Zoladex. There were no confirmed interaction between zoladex and other drugs.
The drug Goserelin is contraindicated in patients with a known hypersensitivity to the drug, or its known components. It is also contraindicated in patients suffering from severely low levels of testosterone and estrogen. Pregnant patients, or patients who wish to become pregnant, are not advised to use the drug. Aspiring fathers are also not advised to use the drug.
Caution is to be exercised when administering the drug to patients with pre-existing conditions of diabetes
, as the use of the drug is known to reduce glucose tolerance
. Patients with a particular risk of developing urethral obstruction or compression of the spinal cord
should be examined closely when taking the product.
It is not known whether goserelin has adverse effects to the fetus. However, the use of the drug in pregnant women should always be consulted with the doctor. Nursing mothers, or women planning to breastfeed must first consult their doctor prior to the usage of the drug. The potential benefits of the drug must always be weighed against its risks to the nursing mother and infant.
• Molecular formula of goserelin is C59H84N18O14
• Chemical IUPAC Name is 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
• Molecular weight is 1269.41 g/mol
• Goserelin available : 10,8mg tablets