ganirelix

Action and Spectrum

Mechanism of action

It is a GnRH antagonist that binds to GnRH receptors in the pituitary gland, preventing the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH). This results in the suppression of ovulation.

Spectrum

The spectrum of activity of ganirelix is limited to reproductive endocrinology. It is used primarily in assisted reproductive technologies (ART) to control follicle development and prevent premature luteinization in women undergoing controlled ovarian stimulation (COS). Ganirelix can also be used in the treatment of endometriosis and uterine fibroids.

Drug Interaction

Adverse Reaction

Frequency defined:

1-10%

Headache

Nausea

Vaginal bleeding

Abdominal pain

Injection site reaction

Pelvic pain

Ovarian hyperstimulation syndrome

<1%

Anaphylactoid reactions

Black Box Warning

Contraindication / Caution

Contraindications

• Pregnancy: It is not recommended for use during pregnancy as its safety in this population has not been established.
• Hypersensitivity to the drug: Individuals with a known hypersensitivity to ganirelix or any of its components should not use it.
• Liver disease should be used cautiously in patients with liver disease as it may cause liver damage.
• Cancer of the reproductive system: It should not be used in patients with cancer of the reproductive system as it may worsen the condition.

Caution

• Monitoring of treatment response: It should be used regularly to assess its effectiveness in controlling follicle development and preventing premature luteinization.
• Ovarian cysts may increase the risk of developing ovarian cysts, so close monitoring is recommended.
• Ovarian hyperstimulation syndrome (OHSS): OHSS is a rare but potentially severe complication of controlled ovarian stimulation, and ganirelix may increase the risk of OHSS.
• Interactions with other medications: It may interact with other medications, so you must inform your doctor of all medications you are taking.
• Monitoring of blood pressure: It may cause a decrease in blood pressure, so blood pressure should be regularly monitored during treatment.
• Possible side effects: Common side effects of ganirelix include abdominal pain, bloating, headaches, and hot flashes. In rare cases, serious side effects such as liver damage, decreased blood pressure, and anaphylaxis has been reported.

Pregnancy / Lactation

Pregnancy consideration: It is not recommended for use during pregnancy as its safety in this population has not been established

Lactation: Excretion of the drug in human breast milk is unknown

Pregnancy category:

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology

By blocking the release of luteinizing hormone-releasing hormone (LHRH) in the pituitary gland, ganirelix inhibits the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) and prevents ovulation until the follicles are of adequate size for use in assisted reproductive technologies (ART). This helps to control follicle development and prevent premature luteinization, ensuring that the follicles are ready for retrieval at the appropriate time.

Pharmacodynamics

By binding to GnRH receptors in the pituitary gland, ganirelix prevents the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH), which are essential for ovulation. This results in the suppression of ovulation and the prevention of premature luteinization in women undergoing controlled ovarian stimulation (COS) for assisted reproductive technologies (ART).

Regarding its effects on the reproductive system, ganirelix has been shown to effectively control follicle development and prevent premature luteinization in patients undergoing COS. This helps to ensure that the follicles are of adequate size for retrieval at the appropriate time, increasing the chances of successful ART procedures.

Pharmacokinetics

Absorption

It has an oral bioavailability of 91.1% after intravenous administration. The drug has a peak plasma concentration of 14.8 ng/mL after a single dose and 11.2 ng/mL after multiple doses. The peak plasma time is 1.1 hours, and the drug has a half-life of 12.8 hours after a single dose and 16.2 hours after multiple doses.

Distribution

It has a volume of distribution (Vd) of 43.7 L after intravenous administration and is highly protein bound (91.1%)

Metabolism:

The metabolism of ganirelix needs to be better understood.

Elimination/Excretion:

It is primarily eliminated through feces (75.1%) and urine (22.1%). The drug’s half-life is 12.8 hours after a single dose and 16.2 hours after multiple doses.

Adminstartion

Administration

Subcutaneous administration

• SC use only: It is recommended for subcutaneous use and should not be administered intravenously or intramuscularly.
• Injection sites: The recommended SC injection sites for the ganirelix are in the abdomen around the navel or upper thigh.
• Cleaning the injection site: The skin should be cleaned with soap and water for about 2 inches around the needle’s insertion area.
• Pinching up skin: A large area should be pinched between the finger and thumb.
• Insertion angle: The needle should be inserted at the base of the pinched-up skin at an angle of 45-90° to the skin surface.
• Correct needle placement: When correctly positioned, it won’t be easy to draw back on the plunger.
• Depressing plunger: Once the needle is correctly placed, the plunger should be depressed to administer the drug.
• Disposal: The syringe should be discarded after use.

Storage

• Temperature: It should be stored at a temperature between 20-25°C (68-77°F), with excursions allowed between 15-30°C (59-86°F).
• Protection from light: It should be protected from light

Patient Information Leaflet

Patient information leaflet

Generic Name: ganirelix

Pronounced: [ GA-ni-REL-ix ]

Why do we use ganirelix?

It is a gonadotropin-releasing hormone (GnRH) antagonist used in the medical treatment of infertility. It is used to prevent premature luteinizing hormone (LH) surges in women undergoing controlled ovarian hyperstimulation (COH) for in vitro fertilization (IVF) procedures.