Gonadorelin Injection

Overview of Gonadorelin Injection

Dosage Strength of Gonadorelin Injection

1 mg/mL 5 mL Vial

General Information

Gonadorelin is a synthetic version of gonadotropin-releasing hormone (GnRH). A decapeptide that is created using solid-phase peptide synthesis, it causes the pituitary gland to synthesize and secrete follicle-stimulating hormone (FSH) and luteinizing hormone (LH), which are the two gonadotropins that the pituitary produces.12 Endogenous (naturally produced) GnRH is generated by neurons in the hypothalamus’ septum preoptic area and released into the pituitary portal blood, which ultimately causes the anterior pituitary gland to produce and release FSH and LH.3 LH and FSH regulate gonadal function in humans, contributing to child development as well as fertility in adults.45

The FDA had approved gonadorelin for human use, but it has since been discontinued. It was marketed under the brand names Factrel® (injections) and LutrePulse™ (subcutaneous pulsatile injections using OmniPod pump) but has since been discontinued in the United States.

Mechanism of Action

Gonadorelin behaves like naturally produced (endogenous) gonadotropin-releasing hormone (GnRH). It primarily signals the anterior pituitary gland to produce and secrete luteinizing hormone (LH). It also causes the production and release of follicle-stimulating hormone (FSH) by the anterior pituitary gland, though it does this to a lesser degree than with LH. However, in prepubescent girls and some people with gonadal function disorders, gonadorelin may cause more FSH to be produced than LH.1

Gonadorelin is often used to simulate the physiologic release of GnRH from the hypothalamus for patients with delayed puberty or fertility issues caused by hypogonadotropic hypogonadism (a lack of sex hormones due to a lack of a GnRH, FSH and/or LH). It is also sometimes used to induce ovulation for women with hypothalamic amenorrhea (absence of menstruation due to lack of GnRH). Gonadorelin administration leads to increased levels of LH and FSH, which then signal the testes or ovaries to create and secrete sex hormones.1

Pharmacokinetics

Gonadorelin behaves similarly to other hypothalamic peptide hormones that trigger or control physiological actions. Its pharmacokinetics appear to be similar in patients regardless of gender and whether or not they have hypothalamic hypogonadism. Its pharmacokinetics also appear to be similar whether administered via bolus injection or pulsatile pump.6

Gonadorelin is bioavailable at the anterior pituitary gland after pulsatile administration. It has a very short overall half-life when intravenously injected, however, with plasma concentration rising and falling rapidly.6 The initial half-life is about two to 10 minutes, and the terminal half-life is about 10 to 40 minutes.16 Despite the differences between intravenous and subcutaneous routes, dose-related increases in plasma gonadorelin concentrations as well as the observed release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) prove gonadorelin’s bioavailability from either route of administration. The body rapidly metabolizes it into biologically inactive peptide fragments before excreting it into the urine. This takes place primarily in the kidneys. Kidney dysfunction therefore prolongs the half-life and reduces the clearance of gonadorelin, whereas liver dysfunction does not.6

Contraindications/Precautions

If you know or suspect that you are allergic to gonadorelin, tell your doctor or pharmacist before using it. Even if you are not allergic to gonadorelin, this medication may contain inactive ingredients that can cause allergic reactions or other problems. Therefore, tell your doctor or pharmacist if you have any other allergies before using gonadorelin.7

It is also important to inform your doctor or pharmacist of your medical history before using gonadorelin, especially if you’ve had kidney disease, pituitary tumors (such as prolactinoma), ovarian cysts or cancer of the reproductive organs (breast, ovary, uterus, etc.).7

Tell your doctor or dentist about all of the medications and supplements you use (prescription medication; over-the-counter medication; vitamin, mineral or herbal supplements; etc.) before having surgery.7

Gonadorelin may cause multiple births (such as twins, triplets) in patients capable of becoming pregnant. It is important to discuss the risks and benefits of having such pregnancies with your healthcare provider. Gonadorelin may be used during the first trimester of pregnancy as directed by your healthcare provider. If you become pregnant or think you may be pregnant while using this medication, tell your doctor immediately.7

Ovarian hyperstimulation syndrome (OHSS) is a severe side effect that may happen to some patients with ovaries who use this drug. Talk to your healthcare provider immediately if you experience shortness of breath; very upset stomach, throwing up, or diarrhea; severe stomach pain or bloating; significant weight gain; or change in how much urine you pass when going to the bathroom.8

Though it is rare, patients who have been used gonadorelin to help them get pregnant have developed ovarian cancer. However, it is not clear if the medication led to these cases of ovarian cancer or not. Talk to your healthcare provider if you have questions or concerns about this.8

Pregnancy

Gonadorelin is not expected to be harmful to a human fetus. If you are pregnant or think that you may be pregnant, however, it is still important to talk to your doctor before taking this drug.9

Breastfeeding

It is not known if gonadorelin passes into breast milk. If you are breastfeeding, talk to your doctor before taking this medication.9

Adverse Reactions/Side Effects

Talk to your healthcare provider immediately if you experience any of the side effects listed below.

With Repeated Doses

  • Difficulty breathing
  • Flushing that lasts more than a short time
  • Rapid heartbeat10

Talk to your healthcare provider as soon as possible if you experience any of the side effects listed below.

With Single or Repeated Doses

  • Itching, pain, redness or swelling of skin where medication is injected
  • Skin rash where medication is injected or over entire body

With Repeated Doses

  • Hardening of skin where medication is injected
  • Hives10

Some side effects may not need medical attention. They may go away as your body adjusts to your gonadorelin medication. Your doctor may be able to tell you how to prevent or reduce some of these issues as well. Talk to your doctor if any of the side effects listed below continue or are bothersome, or if you have questions about them.

With Single Dose

  • Abdominal or stomach discomfort
  • Flushing that lasts a short time
  • Headaches
  • Lightheadedness
  • Nausea10

Some patients may experience side effects that are not listed above. Talk to your doctor if you experience other side effects.10

Storage

Refrigerate at 2°–8° C (36°–46° F) and away from heat, moisture and light. Keep all medicine out of the reach of children. Throw away any unused medicine after the beyond-use date. Do not flush unused medications or pour down a sink or drain.

  • 1. a. b. c. d. DrugBank Online [Internet]. [place unknown]: DrugBank Online. Gonadorelin; 2005 Jun 13 [updated 2022 Sep 6; cited 2022 Sep 7]. Available from: https://go.drugbank.com/drugs/DB00644
  • 2. PubChem [Internet]. Bethesda (MD): National Library of Medicine (US), National Center for Biotechnology Information; c 2004-2022. PubChem Compound Summary for CID 11980076, Gonadorelin acetate; [cited 2022 Sept. 12]. Available from: https://pubchem.ncbi.nlm.nih.gov/compound/Gonadorelin-acetate
  • 3. PubChem [Internet]. Bethesda (MD): National Library of Medicine (US), National Center for Biotechnology Information; 2004-. PubChem Compound Summary for CID 11980076, Gonadorelin acetate; [cited 2022 Sept. 12]. Available from: https://pubchem.ncbi.nlm.nih.gov/compound/Gonadorelin-acetate
  • 4. Hypertexts for Biomedical Sciences [Internet]. Fort Collins (CO): Colorado State University. Gonadotropins: luteinizing and follicle stimulating hormones; [updated 2018; cited 2022 Sep 12]. Available from: http://www.vivo.colostate.edu/hbooks/pathphys/endocrine/hypopit/lhfsh.html
  • 5. Mayo Clinic [Internet]. [place unknown]: IBM Watson Health; c 1998-2022. Gonadorelin (intravenous route, injection route); [updated 2022 Aug 1; cited 2022 Sep 7]. Available from: https://www.mayoclinic.org/drugs-supplements/gonadorelin-intravenous-route-injection-route/side-effects/drg-20067426?p=1
  • 6. a. b. c. d. Ferring Pharmaceuticals. Lutrepulse® [Internet]. North York (ON): Ferring Inc.; [revised 2016 May 17; cited 2022 Sep 12]. Available from: https://www.ferring.ca/media/1018/lutrepulse-pm-control-no-187199-32-mg-en_17may2016.pdf
  • 7. a. b. c. d. WebMD [Internet]. [place unknown]: First Databank, Inc. Gonadorelin acetate solution, reconstituted (recon soln) – uses, side effects, and more; [cited 2022 Sep 14]. Available from: https://www.webmd.com/drugs/2/drug-4210/gonadorelin-injection/details
  • 8. a. b. Memorial Sloan Kettering Cancer Center [Internet]. [place unknown]: UpToDate, Inc.; c2022. Gonadorelin; [updated 2022 Sep 14; cited 2022 Sep 14]. Available from: https://www.mskcc.org/cancer-care/patient-education/gonadorelin
  • 9. a. b. Drugs.com [Internet]. [place unknown]: Cerner Multum, Inc.; c1996-2022. Gonadorelin; [revised 2004 Jul 1; cited 2022 Sep 9]. Available from: https://www.drugs.com/mtm/gonadorelin-injectable.html
  • 10. a. b. c. d. Mayo Clinic [Internet]. [place unknown]: IBM Watson Health; c1998-2022. Gonadorelin (intravenous route, injection route); [updated 2022 Aug 1; cited 2022 Sep 7]. Available from: https://www.mayoclinic.org/drugs-supplements/gonadorelin-intravenous-route-injection-route/side-effects/drg-20067426?p=1

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