Ganirelix

Ganirelix is injected under the skin. You may be shown how to use injections at home. Do not self-inject this medicine if you do not fully understand how to give the injection and properly dispose of used needles and syringes.

Ganirelix is usually given once daily for several days in a row during certain phases of your fertility treatment cycle. Follow your doctor's instructions and try not to miss any doses.

Each single use vial (bottle) of this medicine is for one use only. Throw away after one use, even if there is still some medicine left in it after injecting your dose.

Use each disposable needle only one time. Throw away used needles in a puncture-proof container (ask your pharmacist where you can get one and how to dispose of it). Keep this container out of the reach of children and pets.

During your treatment with ganirelix, your blood may need to be tested often. Visit your doctor regularly. You must remain under the care of your doctor while using ganirelix.

Store the prefilled syringe at room temperature, away from heat, moisture and light.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Call your doctor for instructions if you miss a dose.

Ganirelix is a prescription medication used during certain fertility treatments in women called ovarian stimulation to help ensure that women's eggs can develop properly. 

Ganirelix belongs to a group of medications called gonadotropin-releasing hormone antagonists. These work by decreasing the production of certain hormones in the body order to prevent ovulation from occurring at the wrong time and to allow additional fertility treatments to promote ovulation at the right time.

Ganirelix is available in an injectable form to be given directly under the skin.

Common side effects of ganirelix include headache, abdominal pain, and vaginal bleeding.

Medications can interact with certain foods. In some cases, this may be harmful and your doctor may advise you to avoid certain foods. In the case of ganirelix, there are no specific foods that you must exclude from your diet when receiving this medication.

Tell your doctor if you are breastfeeding or plan to breastfeed.

It is not known if ganirelix crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication. Your doctor and you will decide if the benefits outweigh the risk of using ganirelix.

Call your doctor for instructions if you miss a dose.

Follow your doctor's instructions about any restrictions on food, beverages, or activity.

• Tell all of your health care providers that you take this medicine. This includes your doctors, nurses, pharmacists, and dentists.
• If you have a latex allergy, talk with your doctor.
• Have blood work checked as you have been told by the doctor. Talk with the doctor.
• Talk with your doctor before you drink alcohol.
• Limit working out while undergoing ovarian stimulation. Talk with your doctor.
• A pregnancy test will be done to show that you are NOT pregnant before starting ganirelix. If you get pregnant while taking this medicine, call your doctor right away.

The pulsatile release of GnRH stimulates the synthesis and secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). The frequency of LH pulses in the mid and late follicular phase is approximately 1 pulse per hour. These pulses can be detected as transient rises in serum LH. At midcycle, a large increase in GnRH release results in an LH surge. The midcycle LH surge initiates several physiologic actions including: ovulation, resumption of meiosis in the oocyte, and luteinization. Luteinization results in a rise in serum progesterone with an accompanying decrease in estradiol levels.

Ganirelix Acetate acts by competitively blocking the GnRH receptors on the pituitary gonadotroph and subsequent transduction pathway. It induces a rapid, reversible suppression of gonadotropin secretion. The suppression of pituitary LH secretion by Ganirelix Acetate is more pronounced than that of FSH. An initial release of endogenous gonadotropins has not been detected with Ganirelix Acetate, which is consistent with an antagonist effect. Upon discontinuation of Ganirelix Acetate, pituitary LH and FSH levels are fully recovered within 48 hours.

Pharmacokinetics

The pharmacokinetic parameters of single and multiple injections of Ganirelix Acetate Injection in healthy adult females are summarized in Table I. Steady-state serum concentrations are reached after 3 days of treatment. The pharmacokinetics of Ganirelix Acetate are dose-proportional in the dose range of 125 to 500 mcg.

Ganirelix Acetate is rapidly absorbed following subcutaneous injection with maximum serum concentrations reached approximately one hour after dosing. The mean absolute bioavailability of Ganirelix Acetate following a single 250 mcg subcutaneous injection to healthy female volunteers is 91.1%.

The mean (SD) volume of distribution of Ganirelix Acetate in healthy females following intravenous administration of a single 250-mcg dose is 43.7 (11.4) liters (L). In vitro protein binding to human plasma is 81.9%.

Following single-dose intravenous administration of radiolabeled Ganirelix Acetate to healthy female volunteers, Ganirelix Acetate is the major compound present in the plasma (50–70% of total radioactivity in the plasma) up to 4 hours and urine (17.1–18.4% of administered dose) up to 24 hours. Ganirelix Acetate is not found in the feces. The 1–4 peptide and 1–6 peptide of Ganirelix Acetate are the primary metabolites observed in the feces.

On average, 97.2% of the total radiolabeled Ganirelix Acetate dose is recovered in the feces and urine (75.1% and 22.1%, respectively) over 288 h following intravenous single dose administration of 1 mg [14C]-Ganirelix Acetate. Urinary excretion is virtually complete in 24 h, whereas fecal excretion starts to plateau 192 h after dosing.

Special Populations

The pharmacokinetics of Ganirelix Acetate Injection have not been determined in special populations such as geriatric, pediatric, renally impaired and hepatically impaired patients (see PRECAUTIONS).

Formal in vivo or in vitro drug-drug interaction studies have not been conducted (see PRECAUTIONS). Since Ganirelix Acetate can suppress the secretion of pituitary gonadotropins, dose adjustments of exogenous gonadotropins may be necessary when used during controlled ovarian hyperstimulation (COH).

• Antagon
• Ganirelix Acetate

Administer SubQ in abdomen (around navel) or upper thigh; rotate injection site.

Indium 111 Capromab Pendetide: Antigonadotropic Agents may diminish the diagnostic effect of Indium 111 Capromab Pendetide. Avoid combination

Concerns related to adverse effects:

• Hypersensitivity: Hypersensitivity reactions, including anaphylactoid reactions, have been reported; may occur with the first dose; use is not recommended in women with severe allergic conditions. Use with caution in women with signs and symptoms of other allergic conditions.

Special populations:

• Pregnancy: Exclude pregnancy before beginning treatment.

Dosage form specific issues:

• Latex: The packaging may contain natural rubber latex.

Other warnings/precautions:

• Experienced specialists: Should only be prescribed by fertility specialists.