Goserelin-long (Implant) Instructions for Use

Marketing Authorization Holder

Pharmstandard-Ufimsky Vitaminny Zavod OJSC (Russia)

Manufactured By

Nativa, LLC (Russia)

Or

Pharmstandard-UfaVITA OJSC (Russia)

ATC Code

L02AE03 (Goserelin)

Active Substance

Goserelin (Rec.INN registered by WHO)

Dosage Form

Goserelin-long

Implant 3.6 mg: syringe-applicators

Dosage Form, Packaging, and Composition

Implant in a syringe-applicator – white or almost white pieces of a solid polymer material of cylindrical shape; inclusions are allowed.

Excipients: D,L-lactic and glycolic acids copolymer – up to 18 mg.

3.6 mg – syringes (1) – bags (1) – cardboard packs.

Clinical-Pharmacological Group

Gonadotropin-releasing hormone analogue – depot form

Pharmacotherapeutic Group

Antineoplastic hormonal preparations and hormone antagonists, hormones and related compounds, gonadotropin-releasing hormone analogues

Pharmacological Action

Synthetic analogue of natural GnRH. With continuous use, it inhibits the pituitary gland’s secretion of LH and FSH, which leads to a decrease in the blood concentrations of testosterone in men and estradiol in women.

At the beginning of treatment, a temporary increase in the concentrations of these hormones is possible. By approximately the 21st day after the injection of the first depot, hormone concentrations decrease: in men – to castration levels; in women – to levels comparable to those observed in the postmenopausal period.

Hormone concentrations continue to remain suppressed with continuous treatment. At the same time, most men experience regression of the prostate tumor and symptomatic improvement; in women – a positive response of hormone-dependent forms of breast cancer, endometriosis, and uterine fibroids.

Pharmacokinetics

When using the depot form (3.6 mg), absorption in the first 8 days after administration is slower than in the following days (with an interval between injections of 28 days).

C_max in blood plasma is 2.5 ng/ml. T_1/2 is 4.2 hours.

In patients with severe renal impairment, T_1/2 is somewhat prolonged (dose adjustment is not required in this case).

Indications

Hormone-sensitive prostate cancer (including as part of combination therapy with bicalutamide); breast cancer (in premenopausal and menopausal periods). Endometriosis; uterine fibroids (as an auxiliary agent in combination with surgical treatment).

ICD codes

Dosage Regimen

It is used as a depot form of 3.6 mg every 28 days or 10.8 mg every 12 weeks.

Treatment of benign gynecological diseases should be carried out for only 6 months. Repeated courses are not recommended due to the risk of developing partial loss of mineral components and decreased bone density.

It is administered subcutaneously into the anterior abdominal wall. If necessary, local anesthesia can be performed.

No dose adjustment is required when used in patients with impaired renal or hepatic function, or in the elderly.

Adverse Reactions

In men: hot flashes and decreased potency; rarely – swelling and tenderness of the mammary glands; at the beginning of treatment – temporary increase in bone pain; in some cases – impaired ureteral patency and spinal cord compression.

In women: hot flashes, increased sweating and changes in libido, headaches, depression, dryness of the vaginal mucosa; at the beginning of treatment, a temporary increase in the symptoms of the disease is possible; rarely – change in breast size, demineralization of bone tissue, irreversible menopause.

In both men and women, skin rash is possible; rarely, in patients with bone metastases, hypercalcemia may occur after the start of therapy.

Contraindications

Pregnancy, lactation, childhood, hypersensitivity to goserelin or other GnRH analogues.

Use in Pregnancy and Lactation

Goserelin is contraindicated for use during pregnancy and lactation.

When using goserelin for the treatment of gynecological pathology in women of childbearing age, possible pregnancy should be excluded before starting treatment; during therapy, non-hormonal methods of contraception should be used until menstruation resumes.

Use in Hepatic Impairment

No dose adjustment is required when used in patients with impaired hepatic function.

Use in Renal Impairment

No dose adjustment is required when used in patients with impaired renal function.

Pediatric Use

Contraindicated in childhood.

Geriatric Use

No dose adjustment is required when used in elderly patients.

Special Precautions

Goserelin 10.8 mg is not indicated for use in women.

Goserelin should be used with caution in men at high risk of developing ureteral obstruction or spinal cord compression. In this case, strict medical supervision is necessary during the first month of therapy.

Changes in blood pressure are noted during the use of goserelin.

Goserelin 3.6 mg is also used for pituitary desensitization in preparation for superovulation stimulation as part of an in vitro fertilization program.

Drug Interactions

Drug interactions of goserelin have not been described.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°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.