Cetrotide 250 mcg/vial

INDICATIONS

Cetrorelix Acetate is indicated for the treatment of infertility in females. It restricts eggs to release directly and prevents premature ovulation. In Female infertility, Cetrorelix Acetate prevents release of premature eggs during a process called ovulation in females. This helps in normal development ... Read moreCetrorelix Acetate is indicated for the treatment of infertility in females. It restricts eggs to release directly and prevents premature ovulation. In Female infertility, Cetrorelix Acetate prevents release of premature eggs during a process called ovulation in females. This helps in normal development of an egg in a woman's ovary (female reproductive organ), and stimulates the release of a healthy, matured egg. This helps to treat infertility in women and increases the chance of a successful pregnancy.

PHARMACOLOGY

Cetrorelix Acetate is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity. Cetrorelix Acetate blocks the effects of GnRH. GnRH controls the secretion of luteinizing hormone (LH), which induces ovulation during the menstrual cycle. During hormone treatment for ovarian stimulation, premature ovulation may lead to eggs that are not suitable for fertilization. Cetrorelix Acetate blocks such undesirable premature ovulation. GnRH induces the production and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) from the gonadotropic cells of the anterior pituitary. Due to a positive estradiol (E2) feedback at midcycle, GnRH liberation is enhanced resulting in an LH-surge. This LH-surge induces the ovulation of the dominant follicle, resumption of oocyte meiosis and subsequently luteinization as indicated by rising progesterone levels. Cetrorelix Acetate competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner. The onset of LH suppression is approximately two hours with the 0.25 mg dose. This suppression is maintained by continuous treatment and there is a more pronounced effect on LH than on FSH. An initial release of endogenous gonadotropins has not been detected with Cetrorelix injection, which is consistent with an antagonist effect. The effects of Cetrorelix Acetate on LH and FSH are reversible after discontinuation of treatment. In women, Cetrorelix Acetate delays the LH-surge, and consequently ovulation, in a dose dependent fashion. FSH levels are not affected at the doses used during controlled ovarian stimulation. A dose of Cetrorelix Acetate 0.25 mg every 24 hours has been shown to maintain the effect.

DOSAGE

Cetrorelix Acetate administered subcutaneously once daily (0.25 mg dose) at 24 hour intervals, either in the morning or in the evening as part of the multiple dose protocol during the early-to mid-follicular phase (Day 5/6 to Day11). It is for subcutaneous injection into the lower abdominal wall. The first administration of Cetrorelix Acetate 0.25 mg should be performed under the supervision of a physician. The reconstituted product is to be administered subcutaneously. Use immediately after reconstitution.

INTERACTION

No formal drug-drug interaction studies have been performed with Cetrorelix Acetate. In vitro investigations have shown that interactions are unlikely with medicinal products that are metabolized by cytochrome P450 or glucuronised or conjugated in some other way. However, the possibility of interactions with gonadotropins or medicinal products that may induce histamine release in susceptible individuals, cannot be totally excluded.

SIDE EFFECTS

The most commonly reported adverse effects are local injection site reactions such as erythema, swelling and pruritus that are usually transient in nature and mild in intensity. Mild to moderate ovarian hyperstimulation syndrome (OHSS) (WHO grade I or II) have been commonly reported and should be considered as an intrinsic risk of the stimulation procedure.

PREGNANCY & LACTATION

Cetrorelix Acetate is not intended to be used during pregnancy and lactation.

PRECAUTIONS & WARNINGS

This medicinal product must be allowed to reach room temperature prior to injection. It should be removed from the refrigerator approximately 30 minutes before use.
Do not use if the reconstituted solution contains particles or if the solution is not clear.
The solution should be used immediately after reconstitution.

THERAPEUTIC CLASS

Drugs affecting (inhibiting) gonadotrophin

STORAGE CONDITIONS

To be used immediately after reconstitution. Store in a refrigerator (2°C to 8°C temperature). Do not freeze. Keep away from light & wet place. Keep out of reach of children.