Ganirelix (Orgalutran) is a competitive GnRH (gonadotrophin-releasing hormone) receptor antagonist that is used to suppress premature ovulation in patients undergoing controlled ovarian hyperstimulation syndrome.

Ganirelix (Orgalutran) Uses:

• As an adjunct to controlled ovarian hyperstimulation:

  • It inhibits the premature LH (luteinizing hormone) surge in patients who are undergoing controlled ovarian hyperstimulation.

Ganirelix (Orgalutran) dose in Adults

Ganirelix (Orgalutran) dose as an adjunct to controlled ovarian hyperstimulation:

• 250 mcg subQ once a day.
• Follicle-stimulating hormone is started on days 2 or 3 of the cycle, followed by the beginning of the treatment during the mid- or late phase.
• Up until the day that chorionic gonadotropins are administered, the treatment is continued.

Ganirelix (Orgalutran) Use in Children:

Not indicated

Ganirelix (Orgalutran) Pregnancy Risk Category: X

•  

• Animal studies have shown that fetal abnormalities can be observed, including fetal loss. 
• Hormonal changes that cause fetal loss could lead to fetal resorption.
• Pregnant women should not use it.
• It is used to treat infertility among women. Pregnancy should be ruled out before you start the therapy.

Ganirelix use during breastfeeding:

• It is unknown if the drug will be excreted into breastmilk.
• Manufacturers recommend that you avoid the drug while breastfeeding.

Ganirelix (Orgalutran) Dose in Kidney disease:

• It has not been studied in severe kidney disease.
• The manufacturer has not provided any recommendations regarding dose adjustments in patients with kidney disease.

Ganirelix (Orgalutran) Dose in Liver disease:

• It has not been studied in severe liver disease.
• The manufacturer has not provided any recommendations regarding dose adjustments in patients with liver disease.

Side Effects of Ganirelix (Orgalutran):

• Central Nervous System:

  • Headache

• Endocrine & Metabolic:

  • Ovarian Hyperstimulation Syndrome

• Gastrointestinal:

  • Abdominal Pain
  • Nausea

• Genitourinary:

  • Pelvic Pain
  • Vaginal Hemorrhage

• Local:

  • Injection Site Reaction

Contraindications to Ganirelix (Orgalutran):

• You may have severe allergic reactions to any ingredient of the drug.
• Allergy reactions to GnRH and any other GnRH analogues
• Pregnancy
• Moderate to severe kidney disease
• Moderate to severe liver disease

Warnings and precautions

• Hypersensitivity

  • There have been reports of allergic reactions, including anaphylaxis or anaphylactoid reactions.
  • After the first dose, allergic reactions can occur. 
  • Patients with symptoms or signs of allergic reactions should not use this medication. In severe cases, it must be stopped immediately.

Ganirelix: Drug Interaction

Monitoring parameters:

Assess follicle size via an ultrasound.

How to administer Ganirelix (Orgalutran)?

• It is administered as a subcutaneous injection into the anterior abdomen or upper thighs.
• The injection sites should be rotated.

Mechanism of action of Ganirelix (Orgalutran):

• By inhibiting the GnRH (gonadotropin-releasing hormone receptors located in the anterior pituitary), it inhibits the release of gonadotropin hormones (luteinizing hormone) from the anterior pituitary.
• It prevents ovulation until the size of the follicles is sufficient.

Duration:

• Less than 48 hours

Absorption:

• Rapid after SubQ administration.

Protein binding:

• 81.9%

Metabolism:

• The liver converts it into two main metabolites (1-4 and 1-6 peptide)

Bioavailability:

• 91.1% after subQ administration.

Half-life elimination:

• Single dose: 12.8 hours;
• Multiple dosing: 16.2 hours

Time to peak levels:

• 1.1 hours

Excretion:

• Feces (75%) within 288 hours;
• urine (22%) within 24 hours

International Brands of Ganirelix:

• Orgalutran
• Fyremadel
• Ganilever
• Ganirest

Ganirelix Brands Names in Pakistan: