Gonadorelin Injection

• What It Is: Gonadorelin is a synthetic form of gonadotropin-releasing hormone (GnRH), a decapeptide created through solid-phase peptide synthesis. It stimulates the pituitary gland to produce and release follicle-stimulating hormone (FSH) and luteinizing hormone (LH).
• Function: GnRH is naturally produced by neurons in the hypothalamus and released into the pituitary portal blood. This triggers the anterior pituitary gland to release FSH and LH, which regulate gonadal function and contribute to child development and adult fertility.

• Approval: Gonadorelin was approved by the FDA for human use.
• Discontinued: It was marketed under the brand names Factrel® (injections) and LutrePulse™ (subcutaneous pulsatile injections using an OmniPod pump). Both have since been discontinued in the United States.

• Historical Use: Gonadorelin was used to assess pituitary function and to treat conditions related to GnRH deficiencies or dysfunctions.

• Mimicking Natural GnRH: Gonadorelin functions similarly to naturally produced (endogenous) gonadotropin-releasing hormone (GnRH). It primarily acts on the anterior pituitary gland, signaling it to produce and release luteinizing hormone (LH).
• FSH Production: In addition to stimulating LH production, gonadorelin also causes the production and release of follicle-stimulating hormone (FSH) by the anterior pituitary gland, though this effect is generally less pronounced than with LH. Interestingly, in prepubescent girls and certain individuals with gonadal function disorders, gonadorelin may induce more FSH production than LH.

• Delayed Puberty and Fertility Issues: Gonadorelin is often administered to simulate the physiological release of GnRH from the hypothalamus, particularly in patients experiencing delayed puberty or fertility issues due to hypogonadotropic hypogonadism (a condition characterized by a deficiency in sex hormones due to insufficient GnRH, FSH, and/or LH).
• Inducing Ovulation: It is also used to induce ovulation in women with hypothalamic amenorrhea, a condition where menstruation is absent due to insufficient GnRH production.

• Hormone Production: Administration of gonadorelin increases the levels of LH and FSH, which then signal the testes or ovaries to produce and secrete sex hormones, thereby aiding in the regulation of reproductive functions.

• Allergy to Gonadorelin: If you know or suspect that you are allergic to gonadorelin, it is crucial to inform your doctor or pharmacist before using this medication. Even if you do not have a known allergy to gonadorelin, this medication may contain inactive ingredients that could cause allergic reactions or other issues. Therefore, it is important to disclose any other allergies you have to your healthcare provider.

• Pre-Existing Conditions: Inform your doctor or pharmacist of your full medical history before using gonadorelin. Special attention should be given if you have a history of kidney disease, pituitary tumors (such as prolactinoma), ovarian cysts, or cancers of the reproductive organs (including breast, ovary, and uterus).

• Before Surgery: It is essential to inform your doctor or dentist about all the medications and supplements you are currently using, including prescription drugs, over-the-counter medications, vitamins, minerals, and herbal supplements, particularly before undergoing surgery.

• Multiple Births: Gonadorelin can increase the likelihood of multiple births (e.g., twins or triplets) in patients who are capable of becoming pregnant. It is important to discuss the potential risks and benefits of such pregnancies with your healthcare provider.
• Use During Pregnancy: Gonadorelin may be used during the first trimester of pregnancy as directed by your healthcare provider. If you become pregnant or suspect you may be pregnant while using this medication, inform your doctor immediately.

• Severe Side Effect: Gonadorelin may cause ovarian hyperstimulation syndrome (OHSS) in some patients with ovaries. This condition is serious and requires immediate medical attention if you experience symptoms such as shortness of breath, severe nausea or vomiting, diarrhea, severe stomach pain or bloating, significant weight gain, or changes in urine output.

• Possible Association: Though rare, there have been cases of ovarian cancer reported in patients who have used gonadorelin to assist with pregnancy. However, it is not clear if the medication directly caused these cases of ovarian cancer. If you have any questions or concerns about this risk, it is important to discuss them with your healthcare provider.

Contact your healthcare provider immediately if you experience any of the following side effects, especially with repeated doses:

• Difficulty Breathing
• Flushing that Lasts More Than a Short Time
• Rapid Heartbeat

Reach out to your healthcare provider if you experience any of these side effects:

• With Single or Repeated Doses:
  • Itching, pain, redness, or swelling of the skin where the medication is injected
  • Skin rash at the injection site or over the entire body
• With Repeated Doses:
  • Hardening of the skin where the medication is injected
  • Hives

Some side effects may not need medical attention and could resolve as your body adjusts to the medication. However, talk to your doctor if these side effects persist or are bothersome:

• With Single Dose:
  • Abdominal or stomach discomfort
  • Flushing that lasts a short time
  • Headaches
  • Lightheadedness
  • Nausea

Some patients may experience side effects not listed above. If you notice any other unusual symptoms, consult your doctor.

Gonadorelin is not expected to be harmful to a human fetus. However, if you are pregnant or think that you may be pregnant, it is important to consult your doctor before using this medication to ensure it is safe for your specific situation.

It is currently unknown if gonadorelin passes into breast milk. If you are breastfeeding or plan to breastfeed, you should discuss this with your doctor before starting the medication to understand any potential risks to your baby.

Store this medication at 68°F to 77°F (20°C to 25°C) 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.