Reprocetar (Lyophilisate) Instructions for Use

Marketing Authorization Holder

Pharmasintez-Tyumen, LLC (Russia)

Manufactured By

Pharmasintez, JSC (Russia)

Or

Pharmasintez-Tyumen, LLC (Russia)

ATC Code

H01CC02 (Cetrorelix)

Active Substance

Cetrorelix (Rec.INN registered by WHO)

Dosage Form

Reprocetar

Lyophilizate for the preparation of solution for subcutaneous administration 0.25 mg

Dosage Form, Packaging, and Composition

Lyophilizate for the preparation of solution for subcutaneous administration

0.25 mg – vials – carton packs – By prescription
0.25 mg – vials (7 pcs.) – carton packs – By prescription

Clinical-Pharmacological Group

Gonadotropin-releasing hormone antagonist

Pharmacotherapeutic Group

Pituitary and hypothalamic hormones and their analogues; hypothalamic hormones; antigonadotropin-releasing hormones

Pharmacological Action

GnRH antagonist. It has a competitive effect on the binding of endogenous GnRH to the receptors of pituitary cell membranes. Due to this, Cetrorelix controls the secretion of gonadotropins (LH and FSH). It causes a dose-dependent inhibition of LH and FSH secretion by the pituitary gland. In the absence of prior stimulation, the onset of inhibition of pituitary secretory function occurs almost immediately after the administration of cetrorelix. In women, it causes a delay in the rise in LH levels and, consequently, ovulation.

The duration of action depends on the magnitude of the dose used.

The effect of cetrorelix is completely reversible after discontinuation of treatment.

Pharmacokinetics

Cetrorelix is rapidly absorbed after s/c injection, the absolute bioavailability is about 85%. Pharmacokinetic parameters after a single s/c administration of 0.25 mg and multiple administration (for 14 days), respectively: C_max – 4.17-5.92 ng/ml and 5.18-7.96 ng/ml; T_max – 0.5-1.5 h and 0.5-2 h; AUC – 23.4-42 ng/h/ml and 36.7-54.2 ng/h/ml. V_d is 1.1 l/kg. T_1/2 is 2.4-48.8 h and 4.1-179.3 h after single and multiple (for 14 days) s/c administration of a 0.25 mg dose, respectively. Cetrorelix is excreted by the kidneys.

Indications

Prevention of premature ovulation in patients during treatment aimed at achieving controlled ovarian stimulation, followed by oocyte retrieval and assisted reproductive procedures.

ICD codes

Dosage Regimen

Administer subcutaneously in the abdominal region. Rotate injection sites daily.

Reconstitute the 0.25 mg lyophilisate immediately before use with 1 ml of Sodium Chloride 0.9% solution. Gently swirl the vial until the solution is clear; do not shake. Inspect the solution for particulate matter and discoloration prior to administration. Discard any unused solution.

Initiate treatment on day 5, 6, or 7 of ovarian stimulation with gonadotropins. Alternatively, follow the fixed or flexible protocol as directed by the fertility specialist.

Inject one vial of 0.25 mg daily. Continue daily administration until adequate follicular development is confirmed by ultrasound and serum estradiol levels, typically culminating in the day of final oocyte maturation trigger.

Adhere strictly to the prescribed treatment schedule. The timing of the daily injection is critical for efficacy. Do not discontinue treatment prematurely.

In the event of a missed dose, contact the treating physician immediately for guidance. The risk of a premature LH surge increases significantly with delayed or missed doses.

Adverse Reactions

Immune system disorders: uncommon – systemic allergic or pseudoallergic reaction, including life-threatening anaphylaxis.

Nervous system disorders: uncommon – headache.

Gastrointestinal disorders: uncommon – nausea.

Reproductive system and breast disorders: common – mild or moderate ovarian hyperstimulation syndrome (OHSS) – grade I-II according to WHO classification; uncommon – severe OHSS – grade III according to WHO classification.

Local reactions common – redness, swelling, itching at the injection site, usually transient and mild.

Contraindications

Hypersensitivity to cetrorelix or exogenous peptide hormones; moderate or severe renal failure, moderate or severe hepatic failure; postmenopausal period; pregnancy, lactation (breastfeeding).

With caution

In the presence of signs and symptoms of an active allergic process or a history of predisposition to allergies.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and breastfeeding.

Use in Hepatic Impairment

Contraindicated in moderate or severe hepatic impairment.

Use in Renal Impairment

Contraindicated in moderate or severe renal impairment.

Special Precautions

In case of OHSS development, symptomatic therapy should be carried out (including rest, intravenous administration of electrolytes or colloid solutions, heparin therapy).

Luteal phase support should be carried out in accordance with the generally accepted practice of reproductive procedures.

Caution should be exercised when using cetrorelix in the presence of signs and symptoms of an active allergic process or a history of predisposition to allergies; in women with severe allergic conditions, the use of cetrorelix should be avoided.

To date, experience with repeated ovarian stimulation using cetrorelix is limited. For repeated courses of treatment, Cetrorelix should be used after assessing the degree of potential risk and treatment effectiveness.

Drug Interactions

A low probability of drug interactions has been demonstrated with the simultaneous administration of cetrorelix with drugs whose metabolism involves cytochrome P450, or which undergo glucuronidation or any other conjugation. Although there is no evidence of interaction with other widely used drugs, in particular, with gonadotropins and drugs that potentially induce histamine release in patients with a predisposition to allergies, the possibility of drug interaction with their simultaneous use with cetrorelix cannot be completely excluded.

Storage Conditions

Store at 2°C (36°F) to 8°C (46°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.