Which Drugs Are Use For Destroy the Sex?

Use in Cancer

Goserelin acetate is approved to treat:

  • Breast cancer is advanced. It is used as palliative treatment in premenopausal and perimenopausal women.
  • Prostate cancer. It is used with flutamide and radiation therapy in localized prostate cancer. It is also used as palliative treatment in advanced prostate cancer.

Goserelin acetate is also being studied in conditions related to cancer.

Contraindications

  • Goserelin is contraindicated in patients with hypersensitivity to goserelin, GnRH, or with Gonadotropin-Releasing Hormone (GnRH) Analogs hypersensitivity; anaphylactic reactions to synthetic GnRH or GnRH agonist analogs have been reported.
  • cancer metastasis to bone
  • diabetes
  • high cholesterol
  • low amount of magnesium in the blood
  • low amount of calcium in the blood
  • high amount of calcium in the blood
  • low amount of potassium in the blood
  • overweight
  • high blood pressure
  • a heart attack
  • prolonged QT interval on EKG
  • chronic heart failure
  • abnormal EKG with QT changes from birth
  • a stroke
  • pregnancy
  • obstruction of any part of the urinary tract
  • tobacco smoking

Dosage

Prostate Cancer

For the palliative treatment of advanced carcinoma of the prostate:

  • 3.6 mg or 10.8 mg subcutaneously into the upper abdominal wall once
  • The 3.6 mg dosage may be repeated every 28 days.
  • The 10.8 mg dosage may be repeated every 12 weeks.
  • Intended for long-term administration unless clinically inappropriate.
  • Prostate cancer, stage B2 to C (in combination with an antiandrogen and radiotherapy; begin 8 weeks prior to radiotherapy): Males: SubQ:
  • Combination 28-day/12-week implant: 3.6 mg implant, followed in 28 days by 10.8 mg implant

OR

  • 28-day implant (alternate dosing): 3.6 mg; repeated every 28 days for a total of 4 doses (2 depots preceding and 2 during radiotherapy)
  • In combination with flutamide for the management of locally confined Stage T2b-T4 (Stage B2-C) carcinoma of the prostate. Treatment should start 8 weeks prior to radiation therapy and continue during radiation.
  • For the palliative treatment of advanced carcinoma of the prostate.

Endometriosis

  • 3.6 mg subcutaneously into the upper abdominal wall once; repeat every 28 days. The recommended duration of therapy is 6 months.
  • For the management of endometriosis, including pain relief and reduction of endometriotic lesions.

Breast Cancer–Palliative

  • For use in the palliative treatment of advanced breast cancer: 3.6 mg subcutaneously into the upper abdominal wall once; repeat every 28 days
  • Intended for long-term administration unless clinically inappropriate.
  • For the palliative treatment of advanced breast cancer in pre-and perimenopausal women

Dose for Bleeding

  • 1 or 2 of the 3.6 mg subcutaneous depot injections (with each depot given 4 weeks apart). When 1 depot is administered, surgery should be performed at 4 weeks.
  • When 2 depots are administered, surgery should be performed within 2 to 4 weeks following the administration of the second depot.

Administration Technique

The proper method of administration of ZOLADEX is described in the instructions that follow.

  • Put the patient in a comfortable position with the upper part of the body slightly raised. Prepare an area of the anterior abdominal wall below the navel line with an alcohol swab.
    NOTE: Caution should be taken while injecting ZOLADEX into the anterior abdominal wall due to the proximity of the underlying inferior epigastric artery and its branches.
  • Examine the foil pouch and syringe for damage. Remove the syringe from the opened foil pouch and hold the syringe at a slight angle to the light. Check that at least part of the ZOLADEX implant is visible.
  • Grasp the red plastic safety tab and pull away from the syringe, and discard. Remove the needle cover. Unlike liquid injections, there is no need to remove air bubbles as attempts to do so may displace the ZOLADEX implant.
  • Holding the syringe around the protective sleeve, using an aseptic technique, pinch the skin of the patient’s anterior abdominal wall below the navel line. With the bevel of the needle facing up, insert the needle at a 30 to 45-degree angle to the skin in one continuous deliberate motion until the protective sleeve touches the patient’s skin.
    NOTE: The ZOLADEX syringe cannot be used for aspiration. If the hypodermic needle penetrates a large vessel, blood will be seen instantly in the syringe chamber. If a vessel is penetrated, withdraw the needle and inject it with a new syringe elsewhere. Monitor patients for signs or symptoms of abdominal hemorrhage. Use extra care when administering ZOLADEX to patients with a low BMI and/or to patients receiving full-dose anticoagulation.
  • Do not penetrate into muscle or peritoneum.
  • To administer the ZOLADEX implant and to activate the protective sleeve, grasp the barrel at the finger grip and depress the plunger until you cannot depress it any further. If the plunger is not depressed fully, the protective sleeve will NOT activate. When the protective sleeve ‘clicks’, the protective sleeve will automatically begin to slide to cover the needle.
    NOTE: The needle does not retract.
  • Withdraw the needle and allow the protective sleeve to slide and cover the needle. Dispose of the syringe in an approved sharps collector.

Side Effects

The Most Common

  • headache
  • hot flashes (a sudden wave of mild or intense body heat)
  • sweating
  • sudden reddening of the face, neck, or upper chest
  • lack of energy
  • loss of appetite
  • breast pain or change in breast size in women
  • decreased sexual desire or ability
  • painful sexual intercourse
  • vaginal discharge, dryness, or itching
  • menstruation (periods)
  • swelling of the hands, feet, ankles, or lower legs
  • depression
  • nervousness
  • unable to control emotions and frequent mood changes
  • difficulty falling asleep or staying asleep
  • pain, itching, swelling, or redness at the place where the implant was inserted
  • hives
  • rash
  • itching
  • difficulty breathing or swallowing
  • chest pain
  • pain in the arms, back, neck, or jaw
  • unusual weight gain
  • slow or difficult speech
  • dizziness or fainting
  • weakness or numbness of an arm or leg
  • bone pain
  • not able to move legs
  • painful or difficult urination
  • frequent urination
  • extreme thirst
  • weakness
  • blurred vision
  • dry mouth
  • nausea
  • vomiting
  • breath that smells fruity
  • decreased consciousness

More Common

  • Fast or irregular heartbeat
  • Bone, muscle, or joint pain
  • changes in the skin color of the face
  • fainting
  • fast or irregular breathing
  • numbness or tingling of the hands or feet
  • puffiness or swelling of the eyelids or around the eyes
  • skin rash, hives, or itching
  • sudden, severe decrease in blood pressure and collapse
  • tightness in the chest
  • troubled breathing
  • pain, bruising, swelling, redness, oozing, or bleeding where the implant was injected;
  • dizziness, trouble breathing, feeling light-headed (like you might pass out);
  • high blood sugar – increased thirst, increased urination, dry mouth, fruity breath odor;
  • high calcium levels – confusion, tiredness, nausea, vomiting, loss of appetite, constipation, increased thirst or urination, weight loss;
  • heart attack symptoms – chest pain or pressure, pain spreading to your jaw or shoulder, nausea, sweating; or
  • signs of a blood clot – sudden numbness or weakness on one side of the body, chest pain, problems with vision or speech, pain or swelling in one leg.

RARE

  • Anxiety
  • deepening of voice
  • increased hair growth
  • mental depression
  • mood changes
  • Pain in the chest
  • pain in the groin or legs (especially in the calves of the legs)
  • Sudden sweating and feelings of warmth (also called hot flashes)
  • Blurred vision
  • burning, itching, redness, or swelling at the place of injection
  • decreased interest in sexual intercourse
  • dizziness
  • headache
  • nausea or vomiting
  • swelling and increased tenderness of the breasts
  • swelling of the feet or lower legs
  • trouble sleeping
  • weight gain
  • Light, irregular vaginal bleeding
  • stopping of menstrual periods
  • Burning, dryness, or itching of the vagina
  • pelvic pain
  • Bone pain
  • constipation
  • decreased size of the testicles
  • inability to have or keep an erection

Drug Interactions

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Pregnancy and Lactation

AU TGA pregnancy category: D
US FDA pregnancy category:

Pregnancy

This drug is contraindicated during pregnancy unless it is being used for the palliative treatment of advanced breast cancer. This drug can harm a developing fetus. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential harm to the fetus. There is an increased risk of pregnancy loss due to hormone changes caused by this drug. Verify negative pregnancy status in females of reproductive potential prior to initiating therapy.

Lactation

A decision should be made to either discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother; some experts consider use to be contraindicated.

How should this medicine be used?

Goserelin comes as an implant to be inserted with a syringe subcutaneously (under the skin) in your stomach area by a doctor or nurse in a medical office or clinic. An implant with 3.6 mg of goserelin is usually inserted every 4 weeks. An implant with 10.8 mg of goserelin is usually inserted every 12 weeks. The length of your treatment depends on the condition being treated and your response to the medication. Your doctor will determine how long you should use the goserelin implant.

Goserelin may cause an increase in certain hormones in the first few weeks after insertion of the implant. Your doctor will monitor you carefully for any new or worsening symptoms during this time.

What special precautions should I follow?

Before receiving a goserelin implant,

  • tell your doctor and pharmacist if you are allergic to goserelin, histrelin (Supprelin LA, Vantas), leuprolide (Eligard, Lupron), nafarelin (Synarel), triptorelin (Trelstar), any other medications, or any of the ingredients in goserelin implant. Ask your pharmacist for a list of the ingredients.
  • tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: medications for seizures or oral steroids such as dexamethasone (Decadron, Dexpak), methylprednisolone (Medrol), and prednisone (Sterapred). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
  • tell your doctor if you have a history of drinking alcohol or using tobacco products for a long period of time, or if you or anyone in your family has or has ever had osteoporosis (a condition in which the bones become thin and weak and break easily), or if you have or have ever had a compressed spinal cord, diabetes, unusual vaginal bleeding, urinary obstruction in men (blockage that causes difficulty urinating), or heart or liver disease.
  • tell your doctor if you are pregnant or plan to become pregnant. Goserelin implants should not be used in pregnant women, except for the treatment of advanced breast cancer. Call your doctor right away if you think you have become pregnant during your treatment. Goserelin implant may harm the fetus. You should not plan to become pregnant while using a goserelin implant or for 12 weeks after your treatment. Your doctor may perform a pregnancy test or tell you to begin your treatment during your menstrual period to be sure that you are not pregnant when you begin using the goserelin implant. You will need to use a reliable nonhormonal method of birth control to prevent pregnancy while you are using a goserelin implant and for 12 weeks after your treatment. Talk to your doctor about the types of birth control that are right for you, and continue to use birth control even though you should not have regular menstrual periods during your treatment. tell your doctor if you are breastfeeding. You should not breastfeed during your treatment with a goserelin implant.

References

  1. https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019726s050s051s052lbl.pdf
  2. https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019726s059,020578s037lbl.pdf
  3. https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/020578s034,020578s035lbl.pdf
  4. https://www.accessdata.fda.gov/drugsatfda_docs/psg/Goserelin_Acetate_impSQ_20578_19726_RC10-08.pdf
  5. https://pubchem.ncbi.nlm.nih.gov/compound/Fertilan
  6. https://www.drugs.com/zoladex.html
  7. https://go.drugbank.com/drugs/DB00014
  8. https://medlineplus.gov/druginfo/meds/a601002.html
  9. https://en.wikipedia.org/wiki/Goserelin
  10. https://www.mayoclinic.org/drugs-supplements/goserelin-subcutaneous-route/side-effects/drg-20067310
  11. https://www.webmd.com/drugs/2/drug-7104/goserelin-subcutaneous/details/list-contraindications
  12. NCI Thesaurus Tree
  13. NORMAN Suspect List Exchange Classification
  14. PubChem
  15. Antineoplastic Agents, Hormonal
  16. Anatomical Therapeutic Chemical (ATC) classification
    Target-based classification of drugs