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Goserelin- Indications, Dosage, Risks, and Interactions

Written by
Dr. Shikha
and medically reviewed by Dr. Nagaraj

Published on Aug 22, 2022 and last reviewed on Mar 30, 2023   -  23 min read

Abstract

Goserelin is a hormone therapy used in the treatment of breast cancer patients and prostate cancer patients. Refer to the article below for more details.

Overview:

The Goserelin implant is used to treat the symptoms of advanced prostate cancer and in conjunction with radiation therapy and other drugs to treat localized prostate cancer. In certain women, it is also used to treat severe breast cancer. Additionally, it is used to treat abnormal uterine bleeding as well as endometriosis, a condition in which the tissue which lines the uterus develops in other parts of the body such as ovaries, and fallopian tube causing pain, heavy or irregular menstruation, or periods, and other symptoms.

A group of drugs known as gonadotropin-releasing hormone (GnRH) agonists are included in the Goserelin implant. It functions by lowering the body's levels of specific hormones. It prevents testosterone production in men, which may encourage the development of cancerous cells. Goserelin reduces estradiol production in women to levels resembling the postmenopausal phase, which may inhibit the proliferation of cancer cells. Hormone levels return to normal after the drug is stopped.

Only brand-name medications are sold for Goserelin. There is no generic version available right now. An identical version of the active ingredient in a brand-name drug is a generic drug. The generic drug is thought to be equally secure and efficient as the brand-name medication. Generic medicines typically cost less than name-brand ones.

How Does Goserelin Work?

Our bodies produce molecules called hormones. Hormones serve as messengers and aid in regulating the function of cells and organs. Drugs used in hormonal therapy alter how hormones are produced or function in the body. Prostate cancer requires the hormone testosterone to spread. The testicles produce almost all of the testosterone in males.

Goserelin is a luteinizing hormone blocker, a form of hormone treatment. This indicates that it inhibits the pituitary gland's ability to release luteinizing hormone (LH). The male sex hormone, which is testosterone, is no longer produced by the testicles as a result. Hormone therapy for prostate cancer aims to lower or stop the body's production of testosterone, which slows down or stops the development of the tumor.

Indication for the Drug:

  1. Goserelin is indicated in prostatic carcinoma. It is recommended for the palliative treatment of advanced prostate cancer.

  2. Stage T2b-T4 (Stage B2-C) localized prostate cancer is approved for the use of Goserelin in combination with Flutamide. Flutamide and Goserelin should be administered for eight weeks before the start of radiation therapy and throughout radiation therapy.

  3. Goserelin is recommended as an endometrial-thinning medication prior to endometrial ablation for dysfunctional uterine bleeding.

  4. Goserelin is approved for the palliative treatment of progressed and advanced breast cancer in pre-and perimenopausal women. It may be possible to determine whether Goserelin medication will be effective by looking at the estrogen and progesterone receptor levels. The syringe's built-in automated safety mechanism helps to reduce the risk of needlestick injuries.

  5. Goserelin is prescribed to treat endometriosis, which includes reducing lesions and relieving pain throughout treatment. Women over the age of 18 who received treatment for endometriosis for six months had a successful experience with Goserelin.

What Are the Contraindications of the Drug?

a) Hypersensitivity

In the medical literature, anaphylactic responses to Goserelin have been documented. Patients with a known hypersensitivity to the gonadotropin-releasing hormone, gonadotropin-releasing hormone agonist analogs, or any of the components in Goserelin should not use the medication.

b) Pregnancy

Unless Goserelin is being taken for palliative treatment of advanced breast cancer, it is not advised to take the drug while pregnant. If Goserelin is given to a pregnant woman, the fetus could suffer injury. The patient should be informed of any potential risks to the fetus if this medication is used while pregnant. Due to anticipated hormone changes brought on by the medication, there is an elevated risk of miscarriage.

Dosage of the Drug:

Goserelin is available as an implant that a doctor or nurse will place in the stomach area using a syringe subcutaneously (under the skin) in a hospital or medical facility. Every four weeks, a 3.6 mg Goserelin implant is typically placed. Every 12 weeks, a 10.8 mg Goserelin implant is typically placed. The ailment being treated and how the patient reacts to the drug will determine how long they need to receive treatment. How long individuals should utilize the Goserelin implant is something their doctor will decide. In the initial weeks following implant installation, Goserelin may cause an increase in specific hormones. Throughout this period, the doctor will keep a close eye on the patient for any new or worsening symptoms.

  • Dosage for Endometriosis

    An implant containing 3.6 mg of Goserelin should be placed every 28 days for a maximum of six months for the treatment of endometriosis.

  • Dosage for Breast Cancer Palliative Care

    A 3.6-mg implant placed every 28 days is the normal prescribed Goserelin dosage for the palliative treatment of breast cancer.

  • Dosage for Uterine Bleeding

    One or two 3.6-mg implants of Goserelin are typically advised for treating uterine hemorrhage. Patients will normally have endometrial ablation four weeks after getting a single implant. During this treatment, the uterine lining is removed. If patients have two implants, the second one will be released four weeks after the first one. The endometrial ablation usually follows 2 to 4 weeks later.

  • Dosage for Prostate Cancer

    A 3.6-mg implant of Goserelin is typically advised for prostate cancer treatment. This should be followed by a 10.8 mg Goserelin implant after 28 days. This treatment will start eight weeks before radiation therapy.

  • Dosage for Treating Advanced Prostate Cancer With Palliative Care

    An implant containing 3.6 mg of Goserelin should be placed every 28 days as the standard suggested dosage for the palliative treatment of advanced prostate cancer. A 10.8-mg implant placed every 12 weeks is an alternative.

What if Patients Overdose?

Patients do not need to remember to take individual dosages because the Goserelin implant delivers the medication to their body over a predetermined period of time. There is no need to schedule an appointment to have the implant removed because it will dissolve over time. To continue the treatment, their doctor might wish to install another implant.

The Goserelin implant is made to continue dispensing the medication for a few days after the next dose is scheduled. Delaying the appointment for the subsequent Goserelin implant is not advised. Patients will nevertheless continue to receive the medication for a brief period if they choose. Patients should try as hard as they can to follow a 4-week or 12-week regimen, depending on their prescription dosage.

How Long Will Patients Have to Take This Medication?

Goserelin is designed to be used over an extended period of time. If patients and their doctors decide that taking Goserelin for a long time is safe and beneficial for them, they probably can continue using it.

Warnings and Precautions:

  1. Tumor Flare

    Similar to other GnRH (gonadotropin-releasing hormones) agonists, Goserelin initially induces brief elevations in serum levels of estrogen and testosterone in women with breast cancer. Occasionally, during the first few weeks of Goserelin treatment, symptoms may temporarily worsen, or new signs and symptoms of breast or prostate or breast cancer may appear. A small percentage of patients might have an increase in their bone pain that passes quickly and can be treated symptomatically. Similar to other GnRH agonists, patients with prostate cancer have experienced isolated incidences of ureteral blockage and spinal cord compression. If renal impairment brought on by ureteral blockage or spinal cord compression appears, the typical treatment for these complications is an urgent orchiectomy. It should be taken into consideration for patients with severe prostate cancer situations.

  2. Diabetes and Hyperglycemia

    Men taking GnRH (gonadotropin-releasing hormone) agonists have had hyperglycemia and an elevated chance of acquiring diabetes. Hyperglycemia may signal the onset of diabetes mellitus or a decline in the glycemic control of diabetic patients. Patients taking a GnRH agonist should routinely have their blood sugar and glycosylated hemoglobin (HbA1c) checked, and they should be managed according to standard procedures for treating hyperglycemia or diabetes.

  3. Hypersensitivity

    GnRH (gonadotropin-releasing hormone) agonist analogs have been linked to hypersensitivity, antibody production, and acute anaphylactic reactions. One patient revealed low-titer binding to Goserelin out of 115 women treated with the drug globally who were evaluated for the development of binding to Goserelin after treatment with the drug. The Goserelin binding component of this patient's plasma, which was collected after treatment, did not precipitate with rabbit anti-human immunoglobulin polyvalent sera, according to additional testing. These results imply the potential for antibody production.

  4. Pregnancy and Effect on Women of Childbearing Potential

    For women receiving Goserelin for benign gynecological disorders, pregnancy must be ruled out prior to beginning treatment. The prevention of pregnancy should be recommended for women who are capable of having children.

    All premenopausal women must utilize reliable non-hormonal contraception throughout their Goserelin treatment and for 12 weeks after stopping it. Goserelin typically prevents menstruation and slows ovulation when taken every 28 days, although pregnancy prevention is not guaranteed. Chronic administration is anticipated to have an impact on reproductive function due to the drug's anti-gonadotrophic effects.

    Goserelin can harm a fetus when given to a pregnant woman, according to its mechanism of action in humans and reports of increased pregnancy loss in animal studies. The patient should be informed of any potential risks to the fetus if this medication is used to treat breast cancer palliatively during pregnancy.

  5. Cervical Resistance

    Cervical resistance may rise as a result of Goserelin's pharmacologic effects on the uterus and cervix. As a result, caution is advised when dilatation of the cervix is necessary for endometrial ablation.

  6. Injection Site Injury

    Site Injury reports of Goserelin-related injection site injuries and vascular injuries, including discomfort, hematoma, bleeding, and hemorrhagic shock, necessitating blood transfusions and surgical intervention, have been made. Goserelin administration to patients with low BMI (body mass index) or those taking full-dose anticoagulation should be done with extra caution.

  7. Hypercalcemia

    In some prostate and breast cancer patients who started treatment with Goserelin and had bone metastases, hypercalcemia has been documented, just like with other GnRH (gonadotropin-releasing hormones) agonists or hormonal therapies (antiestrogens, estrogens, etc.). If hypercalcemia does occur, the proper treatments should be started right away.

  8. Cardiovascular Conditions

    The use of GnRH (gonadotropin-releasing hormone) agonists by men has been linked to an elevated risk of stroke, myocardial infarction, and sudden cardiac death. According to the provided odds ratios, the risk appears to be minimal, yet, it should be carefully considered, along with cardiovascular risk factors, when choosing a prostate cancer treatment. Patients receiving a GnRH agonist should be managed in accordance with current clinical practice and should be watched for symptoms and signs that indicate the onset of cardiovascular disease.

  9. Effect on the QT/QTc Interval

    The QT/QTc interval may be prolonged by androgen deprivation therapy. In patients with congenitally long QT syndrome, congestive heart failure, frequent electrolyte disorders, and individuals using medications known to lengthen the QT interval, healthcare providers should assess the advantages of androgen deprivation therapy against any potential dangers. Any abnormalities in the electrolyte should be treated. Think about routine electrolyte and ECG monitoring.

For Patients

What Is Prostate Cancer?

Cancer is a disease in which the body's cells proliferate unchecked. The prostate's cells are where prostate cancer first develops. The prostate gland is present in the male reproductive system. It is situated close to the bladder. It creates a fluid, which is a component of semen.

One of the most prevalent cancers is prostate cancer. It frequently develops quite slowly. It might not pose a major threat if it does not spread to other bodily regions. However, prostate cancer can occasionally develop quickly and disperse to other body regions. Prostate cancer of this type is dangerous.

What Causes Prostate Cancer?

Prostate cancer's exact cause is unknown to researchers. They are aware that it occurs when the genetic material is altered (DNA). These genetic alterations can occasionally be inherited, which means people are born with them. Additionally, there are some genetic alterations that can increase the risk of developing prostate cancer throughout the lifetime. But frequently, the precise reason for these genetic alterations is unknown.

What Are the Symptoms of Prostate Cancer?

Especially early on, prostate cancer symptoms are not usually present. If it does, potential symptoms include:

  • Issues with urinating, including a weak, difficult-to-start, or intermittent urine stream.

  • Having an urgent desire to urinate.

  • Frequent urination, especially during the night.

  • Urination that causes pain or burning.

  • Blood in the feces or urine.

  • Persistent pain in the pelvis, hips, or lower back.

  • Unpleasant ejaculation.

But many of these symptoms, including an enlarged prostate, may really be caused by more common prostate issues that are not cancer.

If any of the following mentioned below applies to an individual, they should talk to their doctor about their prostate health:

  • Possess potential prostate cancer symptoms.

  • Has a high risk of contracting prostate cancer.

  • A screening test revealed that they might have prostate cancer.

How Is Prostate Cancer Diagnosed?

Prostate cancer screening tests include:

Digital Rectal Examination (DRE): In this examination, the doctor presses a greased, gloved finger inside the patient's rectum to feel their prostate for lumps or anything strange.

Blood Test for Prostate-Specific Antigen (PSA): An elevated PSA blood level could indicate prostate cancer. High PSA levels might be brought on by numerous other factors as well.

Imaging Exams: These examinations could create images of the prostate using an MRI (magnetic resonance imaging) or an ultrasound.

The next step is typically a prostate biopsy if these tests indicate that one may have prostate cancer. The sure way to diagnose prostate cancer is through a biopsy. During a biopsy, a physician takes a sample of prostate tissue using a hollow needle. The organ is examined under a microscope to detect cancer cells.

How to Treat Prostate Cancer?

Age, overall health, and the severity of cancer all affect a patient's treatment options.

One or more of the following could be part of their treatment:

Observation is typically employed in older patients, those with prostate cancer that is not likely to spread quickly, and those who are asymptomatic or have other medical concerns. Their doctor will continue to monitor cancer over time to determine whether they may need to begin cancer treatment.

Two categories of observation exist:

The term "watchful waiting" refers to little to no testing. Patients will receive treatment to stop the onset or progression of symptoms, not to cure the malignancy.

Active surveillance entails routine examinations to check for changes in prostate cancer. Patients will receive treatment in an effort to treat cancer if the tests reveal that the cancer is growing or if patients start to experience symptoms. If cancer has not progressed beyond the prostate gland, one may be able to have surgery to remove the gland.

  • High energy is used in radiation therapy to either kill or stop the growth of cancer cells.

  • With hormone therapy, cancer cells are unable to obtain the hormones they require to proliferate. One can entail taking medication or having the testicles surgically removed.

  • Chemotherapy employs drugs to eradicate cancer cells, inhibit their growth, or prevent their spread.

  • Drugs or other compounds that target particular cancer cells are used in targeted therapy. The medications can be administered orally, intravenously, as a shot, as a cream, or via injection (by IV). Compared to radiation therapy or chemotherapy, this treatment does not destroy healthy cells as much.

  • Immunotherapy aids in the fight against cancer by your own immune system.

What Is Goserelin?

A hormone-like substance called Goserelin is present in the body. It decreases the body's production of sex hormones. While using this medication, both men and women will have decreased amounts of testosterone and estrogen. This medication is injected either once every month or once every 12 weeks into males to treat prostate cancer. Women with endometriosis, dysfunctional uterine hemorrhage, or advanced breast cancer are exclusively treated with a monthly injection.

What Should Patients Inform Their Doctor About Before Using This Medication?

If an individual has any of the following conditions, they need to inform their doctor about the same:

  • Bone issues.

  • Heart disease and diabetes.

  • Record of irregular heartbeat, unusual or allergic response to Goserelin, other medications, foods, colors, or preservatives

  • Pregnancy or trying to become pregnant.

  • Nursing a child.

How Should Patients Use This Medication?

This medication is intended for subcutaneous injection. It is administered by a medical expert in a hospital or clinic environment. Regarding the administration of this medication to children, consult a pediatrician. One might need to take extra care. If patients believe they have taken too much of this medication, call an emergency room or a poison control center right away. Patients should note that this medication is solely for them. Do not give this medication to anyone else.

What if Patients Miss a Dose?

It is crucial not to skip a dose. If patients are unable to keep a scheduled appointment, they should call their doctor or other healthcare providers.

What Other Drugs Might Interact With This Drug?

Take care not to combine this medication with any of the following drugs:

  • Cisapride

  • Dronedarone

  • Thioridazine

  • Pimozide

The following medicines or drugs may also interact with this drug:

  • Drugs which lengthen the QT period (an abnormal heart rhythm).

List all of the pharmaceuticals, herbs, over-the-counter remedies, and nutritional supplements patients take for their health to their doctor. Also, let them know whether you smoke, consume alcohol, or engage in illicit drug usage.

What Risks Should Patients Be Aware of While Taking This Medication?

Visit a physician or other healthcare professional to regularly monitor the progress. During the first few weeks of treatment, it is possible that the symptoms could seem to worsen. If the symptoms do not begin to improve or if they worsen following this period, notify your doctor or healthcare provider.

  • If patients use this medication for a long period, their bones could become weaker. Individuals run a greater risk of losing bone mass if they smoke or drink alcohol frequently. The risk of bone loss may also be increased by having a family history of the disease, using corticosteroids frequently, or using medications to treat seizures (convulsions). Consult your doctor for advice on maintaining bone health.

  • Women taking this medication should no longer experience monthly menstruation. If they continue to menstruate, they should let their doctor know. While using this medication and for 12 weeks after discontinuing it, women should not get pregnant.

  • If a woman wants to get pregnant or believes she might already be pregnant, she should tell her doctor. An unborn child could have major negative effects. For more information, patients should consult a physician or pharmacist. Breastfeeding a baby while taking this medication is not advised.

  • Men who want to father a kid should let their doctors know. This drug may reduce sperm counts. For more information, patients should consult a physician or pharmacist.

  • This medication may cause blood sugar to rise. If someone has diabetes, check with your healthcare provider to see if dietary or medication modifications are necessary.

What Negative Effects Could This Medication Have on Patients?

The following side effects should be reported as soon as possible to a physician or other healthcare provider:

  • Skin rashes, itching, hives, swelling of the face, lips, or tongue.

  • Bone discomfort due to allergic reactions.

  • Breathing difficulties.

  • Alterations to vision.

  • Chest discomfort.

  • Feeling dizzy or lightheaded.

  • Fever.

  • Chills.

  • Pain.

  • Swelling.

  • Numbness and tingling in the hands or feet.

The signs and symptoms of high blood sugar include feeling more thirsty or hungry than usual or an urge to urinate more frequently than usual. Additionally, one can have extreme fatigue or hazy vision as well as the warning signs and symptoms of decreased blood pressure, such as dizziness, feeling lightheaded or fainting, and very low energy levels.

Typically, the side effects listed below may not necessitate medical attention; however, if they persist or are unpleasant, patients should inform their doctor or other qualified healthcare providers.

  • Altered sex drive or behavior.

  • Both male and female breast size changes.

  • Mood or emotion changes.

  • Headache.

  • Hot flashes.

  • Irritation from the injection site.

  • Hunger loss.

  • Skin issues include dry skin and acne.

  • Vaginal dryness.

For Doctors

Chemical Taxonomy:

Kingdom- Organic compounds

Super Class- Organic acids and derivatives

Class- Carboxylic acids and derivatives

Subclass- Amino acids, peptides, and analogs

Direct Parent- Oligopeptides

Pharmacodynamics:

Males who first get Goserelin see an initial rise in serum levels of luteinizing hormone (LH), follicle-stimulating hormone (FSH), and testosterone, followed by subsequent rises in these hormones' levels. About 2 to 4 weeks after starting treatment, prolonged suppression of pituitary gonadotropins caused by chronic Goserelin injection causes serum testosterone levels to fall towards the range typically found in surgically castrated men. Regression of the accessory sex organ results from this. Castrate levels of serum testosterone have been suppressed for the duration of medication in clinical trials with follow-ups of more than two years.

In females, chronic exposure to Goserelin causes a similar down-regulation of the pituitary gland that suppresses gonadotropin secretion, lowers serum estradiol to rates comparable with the postmenopausal state, and would be expected to reduce ovarian size and function, shrink the uterus and mammary gland, and, if present, cause the regression of sex hormone-responsive tumors. Within three weeks of the initial treatment, serum estradiol is lowered to levels akin to those seen in postmenopausal women; nevertheless, once suppression was established, isolated increases of estradiol were noted in 10% of the patients involved in clinical trials.

Within four weeks of the drug's initial administration, serum luteinizing hormone (LH) and FSH (follicle stimulating hormone) are lowered to follicular phase levels, and with continuing usage of Goserelin, they are often maintained in that range. With the administration of a single depot injection, FSH and LH levels may not be suppressed to follicular phase levels on day 28 post-treatment in 5% or less of the women treated with Goserelin. Goserelin may not be able to suppress any of these hormones to these levels in some people. In all but a few rare instances, estradiol, LH, and FSH levels recover to pretreatment levels within 12 weeks of the final implant injection.

Mechanism of Action:

A synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH) is called Goserelin. If Goserelin is taken in its biodegradable version, it inhibits the release of pituitary gonadotropin. As a result, the levels of serum testosterone and LH are persistently suppressed. In both animal and in vitro investigations, Goserelin administration caused the hormonally sensitive rat mammary tumor and Dunning prostate tumor to regress or be inhibited in their growth.

Pharmacokinetics:

Goserelin's pharmacokinetics have been studied in healthy male and female volunteers as well as patients. In these investigations, Goserelin was given subcutaneously in doses of one 250 mcg (aqueous solution) dosage plus one or more 3.6 mg depot doses.

Absorption:

The blood levels of radiolabeled medication peaked between 0.5 and 1.0 hours after dosage due to fast absorption. Throughout the first eight days, Goserelin is released from the depot at a significantly slower pace; however, for the remaining 28 days of the dosage period, Goserelin is released more quickly and continuously. The treatment of Goserelin every 28 days caused testosterone levels to be lowered to and maintained in the range typically found in surgically castrated men, despite the fact that Goserelin's rate of release had changed. However, a few patients' minimal serum levels were raised throughout clinical trials. This range can be explained by interpatient variability.

Metabolism:

The primary method of clearance for Goserelin is by its metabolism, which is accomplished by hydrolyzing its C-terminal amino acids. One healthy male volunteer's urine contained the predominant component of 5-10 fragments, while the major component circulating in serum looked to be 1-7 fragments. Humans produce a restricted profile of metabolites from the metabolism of Goserelin that is similar to that of other species. Every human metabolite has also been discovered in toxicology species.

Distribution:

Following subcutaneous administration of a 250 mcg aqueous solution of Goserelin, the apparent volumes of distribution for males and females, respectively, were 44.1 and 20.3 liters. One sample of Goserelin was discovered to have a 27.3 percent plasma protein binding rate.

Excretion:

Goserelin has excreted relatively quickly after subcutaneous administration of the solution formulation, thanks to a combination of hepatic metabolism and urine excretion. Goserelin is eliminated in urine in excess of 90 % of a subcutaneous radiolabeled solution formulation dosage. Goserelin that has not been altered accounts for around 20 % of the dosage in urine. When given subcutaneously, Goserelin had a significantly higher total body clearance in females than in males.

Nonclinical Toxicology- Carcinogenesis, Mutagenesis, Impairment of Fertility

Carcinogenesis- An increased incidence of pituitary adenomas were seen in male and female rats given subcutaneous Goserelin implantation once every four weeks for a year and recovery for 23 weeks. Following subcutaneous Goserelin implant in rats over a period of 72 weeks in males and 101 weeks in females at identical dose levels, a higher incidence of pituitary adenomas was also noted. The rat pituitary adenomas' applicability to people has not been proven. Mice were given Goserelin subcutaneous implants every three weeks for two years, and this led to a rise in the incidence of histiocytic sarcomas of the vertebral column and femur. The available animal data could not be used to derive human dose or exposure multiples.

Mutagenesis- There is no proof of mutagenic potential according to experiments conducted on mammalian and bacterial systems for point mutations and cytogenetic effects.

Impairment of Fertility- Goserelin's endocrine activity caused modifications in both male and female rats that were consistent with gonadal inhibition. Weight loss and atrophic histological alterations in the testes, epididymis, seminal vesicle, and prostate gland were seen in male rats, and spermatogenesis was completely suppressed. When the ovarian activity was suppressed in female rats, the size and weight of the ovaries and secondary sex organs decreased; follicular growth was stopped at the antral stage, and the corpora lutea were smaller and lighter. Several weeks after the Goserelin dose was ceased, both males and females showed almost complete histologic reversal of these effects, with the exemption of the testes.

However, fertility and general reproductive performance were lowered in those who got pregnant after Goserelin dosing was stopped. Even though complete recovery of reproductive function might not have taken place prior to mating, fertile matings took place within two weeks of dosing cessation, and the ovulation rate, corresponding implantation rate, and the number of live fetuses decreased. When medication therapy ceased after continuous administration for a year, histological testing revealed that drug effects on reproductive organs in male and female dogs receiving Goserelin were reversible. The available animal data could not be used to derive human dose or exposure multiples.

Results From Clinical Studies:

  • Prostatic Cancer, Stage B2-C- In 466 individuals with bulky original tumors either restricted to the prostate (stage B2) or expanding outside the capsule (stage C), with or without pelvic node involvement, the effects of hormonal treatment in combination with radiation were examined. A considerably reduced percentage of local failure was observed in this multicenter, controlled trial when Goserelin and flutamide capsules were given prior to and during radiation treatment than when radiation alone was used. The incidence of distant metastases also showed a tendency to decline as a result of combination therapy. Those who had comprehensive hormone therapy together with radiation had a considerably longer median time without developing an illness than patients who only received radiation. Additionally, patients receiving the combination therapy experienced a significantly longer median disease-free life when normal PSA levels were added as a requirement for disease-free survival.

  • Endometriosis- Goserelin was demonstrated to be as effective as Danazol therapy in controlled clinical studies in reducing the size of endometrial lesions as evaluated by laparoscopy and alleviating clinical symptoms (dysmenorrhea, dyspareunia, and pelvic discomfort). In research that compared Goserelin with Danazol, 63 percent of Goserelin-treated patients and 42 percent of Danazol-treated patients experienced an extent of endometrial lesions that were less than or equal to 50 percent reduced. In the second research, which compared Goserelin with Danazol, 62 percent of Goserelin-treated patients and 51 percent of Danazol-treated patients had endometrial lesions that were less severe by more than or equivalent to 50 percent.

    Currently unknown are the clinical implications of a decline in endometriotic lesions, as well as the fact that the severity of symptoms is not always correlated with the laparoscopic staging of endometriosis. Within eight weeks of the first dose in these two investigations, Goserelin caused amenorrhea in all treated women. Menstruation frequently returns eight weeks after therapy is over. Clinical symptoms considerably decreased within four weeks of the medication's start administration, and by the time the course of therapy was complete, they had decreased by an average of 84 percent. Some women who start taking Goserelin for the first two months may develop vaginal bleeding of varying duration and severity. This bleeding most likely signals estrogen withdrawal bleeding and is anticipated to end on its own. There is no sufficient evidence to determine if Goserelin use increases or decreases pregnancy rates.

  • Breast Cancer- In premenopausal women with progesterone receptor positive or advanced estrogen receptor-positive breast cancer, a randomized clinical trial compared Goserelin with oophorectomy. For patients treated with Goserelin, the median time to treatment failure is 6.7 months, whereas for patients treated with oophorectomy, it is 5.5 months. 48 percent of the females in the Goserelin treatment group and 50 percent of the women in the oophorectomy group exhibited subjective responses based on measurements of pain control and performance status for both treatments. In uncontrolled clinical trials involving individuals with hormone receptor-positive and negative breast cancer, the results were comparable.

  • Prostate Cancer- Goserelin and orchiectomy both produced equivalent long-term endocrine responses and objective responses in controlled investigations of individuals with advanced prostatic cancer. In a comparison trial, the length of survival was comparable across the two treatment arms.

  • Thinning of the Endometrium- A prospective, randomized, parallel-group, double-blind study involving 358 premenopausal women with dysfunctional uterine hemorrhage was conducted. A randomization process was used to assign eligible patients to receive either two depot injections of Goserelin or two injections of a placebo four weeks apart. Approximately two weeks following the second injection, 155 individuals from each group had endometrial ablation using either a diathermy loop alone or in conjunction with a rollerball. A transvaginal ultrasound probe was used to measure the endometrial thickness prior to surgery. At 24 weeks following endometrial ablation, the incidence of amenorrhea was evaluated between Goserelin and placebo groups.

    When compared to the placebo group, the median endometrial thickness before surgery was considerably lower in the Goserelin therapy group. A single-center, open-label, randomized experiment was conducted on premenopausal women who had a dysfunctional uterine hemorrhage. In the trial, ablation with an Nd: YAG laser was performed four weeks following Goserelin administration to compare the effects of one depot and two depots of Goserelin that were administered four weeks apart.

    For the Goserelin therapy groups, a total of forty patients were randomly assigned. When compared to the group treated with one depot, the median endometrial thickness before surgery was considerably lower in comparison to the group treated with two depots. At 24 weeks, there was no difference in the prevalence of amenorrhea. Six months following surgery, 53% of the 74 patients who successfully completed the trial experienced hypomenorrhea, while 20% had normal menstrual cycles.

Interaction of Goserelin With Other Drugs:

There has not been any official research conducted on drug interactions. There have been no verified interactions between Goserelin and other medications reported. Pituitary-gonadal suppression is the outcome of administering Goserelin at therapeutic levels. Due to this suppression, diagnostic testing of pituitary-gonadotropic and gonadal activities performed throughout treatment and up until the resumption of menstruation may produce false results. Usually, 12 weeks after treatment is stopped, normal function returns.

Uses of Goserelin in Specific Populations:

Usage in Lactating Patients

Whether Goserelin is excreted in human milk is unknown. Rats that are lactating secrete Goserelin in their milk. Given that many medications are excreted in human milk and that the drug may have major negative effects in nursing infants, a choice should be taken regarding whether to stop breastfeeding or stop taking the medication while also considering how important the medication is to the mother.

Usage in Pregnant Patients

Pregnant people with advanced breast cancer fall into category D, and patients with endometriosis and thinned endometrium fall under pregnancy Category X.Unless Goserelin is being used for the palliative treatment of advanced breast cancer, it is not advised to take the drug while pregnant. The use of Goserelin in pregnant women has not been adequately and carefully studied. Goserelin can harm a fetus when given to a pregnant woman, according to its mechanism of action in humans and reports of increased pregnancy loss in animal studies.

The patient should be informed of any potential risks to the fetus if this medication is used while pregnant. Due to anticipated hormone changes brought on by the medication, there is an elevated risk of miscarriage.After being administered subcutaneously to rats and rabbits, Goserelin passes the placenta. Preimplantation loss and resorptions were enhanced when Goserelin was given to pregnant rabbits and rats during organogenesis. There was a dose-related increment in umbilical hernia in offspring when pregnant rats received Goserelin during gestation and lactation.

Usage in Patients With Renal Insufficiency

Male patients with impaired renal function in clinical trials with the solution formulation of Goserelin, as opposed to subjects with normal renal function, had a decreased total body clearance, an increased serum elimination half-life, and decreased creatinine clearance from the body. It is uncertain how decreased Goserelin clearance brought on by compromised renal function affects the efficacy and toxicity of medications in females. There is no evidence from pharmacokinetic investigations in patients with renal impairment that the dose should be adjusted when using the depot formulation.

Usage in Geriatric Patients

When giving Goserelin to male geriatric patients, there is no need to change the dosage. Women over 65 have not been investigated with Goserelin.

Usage in Pediatric Patients

Pediatric patients' safety and efficacy have not been confirmed.

Usage in Obese Patients

With each kilogram of body weight added, there was a roughly 1 to 2.5 percent drop in the AUC after the administration of a 10.8 mg depot. Testosterone levels in obese patients who have not shown a therapeutic response need to be closely watched.

Usage in Patients With Hepatic Insufficiency

When treated with a 250 mcg subcutaneous formulation of Goserelin, normal subjects and patients with mild hepatic impairment had comparable total body clearances and serum elimination half-lives. According to a pharmacokinetic study, people with somewhat impaired liver function do not require a dose change. Goserelin pharmacokinetic data in patients with severe hepatic insufficiency are lacking.

Overdose With Goserelin

Goserelin's pharmacologic characteristics make accidental or purposeful overdose improbable, as does the way it is administered. Overdosage has not been observed in clinical trials. Higher doses or more frequent administration did not result in a greater pharmacologic effect, according to animal studies. In rats and dogs, subcutaneous dosages of the drug up to 1 mg/kg/day, which is up to 250 times the anticipated daily dose for humans based on body surface area, did not result in any nonendocrine-related sequelae. Overdosage should be treated symptomatically if it happens.

Frequently Asked Questions


1.

What Are the Uses of Goserelin?

Goserelin is combined with other medications and radiation therapy to treat localized prostate cancer. Sometimes, it is used alone in treating advanced prostate cancer symptoms. Goserelin is used in women to treat breast cancer and uterine disorders (endometriosis).

2.

How Does Goserelin Work?

 
Goserelin is an injectable GnRH (gonadotropin-releasing hormone) agonist particularly used to treat prostate and breast cancer. Goserelin initially stimulates sex hormone (estrogen and testosterone) production in a non-physiological manner resulting in disruption of the hormonal feedback system and down-regulation of sex hormone production.

3.

Why Is Goserelin Used in the Treatment of Prostate Cancer?

Goserelin stops the release of testosterone from the testicles and reduces the testosterone levels in the body. The growth of prostate cancer depends on testosterone levels and the reduced testosterone results in a slowdown of cancer and its shrinkage.

4.

What Are the Benefits of Using Goserelin?

 
In males, Goserelin reduces the levels of testosterone hormones and prevents the growth and spread of prostate cancer. In females, it decreases estrogen levels and thus prevents the abnormal growth of uterine tissues.

5.

How Long Does Goserelin Take To Produce Its Effects?

Goserelin produces its effects on the human body after the first infection within two to three weeks. Therefore, it is usually administered monthly or every three months. The dose and schedule are finalized based on the patient's condition.

6.

What Are the Side Effects Associated With Goserelin?

Usually, the side effects seen in patients after using Goserelin are headache, blurred vision, swelling in the leg, redness and itching at the injection site, and weight gain. In females, irregular vaginal bleeding and abnormal menstrual cycle are also seen after Goserelin injection.

Last reviewed at:
30 Mar 2023  -  23 min read

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