Zoladex, sustained release subcutaneous capsule 10.8mg syringe applicator

Composition

1 depot capsule for subcutaneous administration of prolonged action contains:

Active ingredient

goserelin (in the form of acetate) 10.8 mg.

Auxiliary substances:

low-molecular-weight lactide-glycolide copolymer (95:5) and high-molecular-weight lactide-glycolide copolymer (95:5) in a ratio of 3:1,

glacial acetic acid (removed during production).

Pharmacological action

Zoladex is a synthetic analog of the natural luteinizing hormone releasing hormone (LHRH).

With constant use, Zoladex inhibits the release of LH by the pituitary gland, which leads to a decrease in serum testosterone concentrations in men and serum estradiol concentrations in women. This effect is reversible after discontinuation of therapy. At the initial stage, Zoladex, like other LHRH agonists, can cause a temporary increase in the concentration of testosterone in the blood serum in men and the concentration of estradiol in the blood serum in women. In the early stages of Zoladex therapy, some women may experience vaginal bleeding of varying duration and intensity.

In men, by about 21 days after the first capsule is administered, testosterone concentrations are reduced to post-castration levels and continue to be reduced with continuous treatment every 28 days. Such a decrease in testosterone concentration in most patients leads to regression of the prostate tumor and to symptomatic improvement.

In women, the serum estradiol concentration also decreases by about 21 days after the first capsule is administered and, with regular administration of the drug every 28 days, remains reduced to a level comparable to that observed in menopausal women. This reduction leads to a positive effect in hormone-dependent forms of breast cancer, endometriosis, uterine fibroids and suppression of follicle development in the ovaries. It also causes thinning of the endometrium and is the cause of amenorrhea in most patients.

Zoladex in combination with iron preparations has been shown to cause amenorrhea and an increase in hemoglobin levels and corresponding hematological parameters in women with uterine fibroids and concomitant anemia.

While taking LHRH agonists, women may experience menopause. Rarely, some women do not recover from menstruation after the end of therapy.

Pharmacokinetics

The introduction of a capsule every 4 weeks ensures the maintenance of effective concentrations. Accumulation in the tissues does not occur.

Binding to plasma proteins is low. In patients with normal renal function, T _1/2 from the blood serum is 2-4 hours

. Pharmacokinetics in special clinical cases

In patients with impaired renal function, T _1/2 increases. When Zoladex 10.8 mg is administered every 12 weeks, this change will not have significant consequences, so it is not necessary to change the dose for this category of patients.

No significant changes in pharmacokinetics are observed in patients with hepatic insufficiency.

Indications

• Prostate cancer that is sensitive to hormonal effects.
• Endometriosis.
• Uterine fibroids (as an auxiliary agent in combination with surgical treatment).

Use during pregnancy and lactation

It is contraindicated during pregnancy and lactation.

Use in children

Contraindicated in childhood.

Contraindications

• Hypersensitivity to goserelin or other LHRH analogues.
• Pregnancy.
• Lactation (breastfeeding).
• Children’s age.

Side effects

From the cardiovascular system

Hypotension or hypertension may occur (usually transient, disappeared either during Zoladex therapy or after it was discontinued; in rare cases, medical intervention was required, including discontinuation of Zoladex).

From the central nervous system and peripheral nervous system

Non-specific paresthesias are possible.

Musculoskeletal disorders

Possible arthralgia.

Allergic reactions

Rarely-hypersensitivity reactions, including some manifestations of anaphylaxis.

Dermatological reactions

Possible skin rash (usually moderate; often disappeared without discontinuation of therapy).

For men

Hot flashes, sweating, decreased potency are possible (rarely discontinuation of therapy is required).

Sometimes-swelling and soreness of the mammary glands.

At the beginning of treatment, patients with prostate cancer may have a temporary increase in bone pain (treatment is symptomatic).

In some cases – violation of the patency of the ureters and compression of the spinal cord. The use of GnRH analogues can cause a loss of bone mineral density.

For women

Hot flashes, increased sweating, changes in libido are possible (rarely discontinuation of therapy is required).

Sometimes-headaches, mood swings, including depression, dryness of the vaginal mucosa and changes in the size of the mammary glands.

In women with uterine fibroma, degeneration of fibromatous nodes is possible. As with other GnRH agonists, ovarian cysts have been reported.

How to take, course of administration and dosage

Subcutaneous injection into the anterior abdominal wall, every 12 weeks.

For malignant neoplasms

The drug is used for a long time.

For benign gynecological diseases

The drug is used for no more than 6 months.

Use in special clinical cases

Elderly patients, patients with renal or hepatic insufficiency do not need to adjust the dose.

Overdose

• Symptoms: The experience of overdose in humans is limited.
• No clinically significant adverse events were observed in the case of unintentional administration of Zoladex earlier or at a higher dose.
• There are no data on overdose in humans.
• Treatment: (in case of overdose) — symptomatic therapy.

Special instructions

Caution should be exercised when prescribing Zoladex 10.8 mg to men who are particularly at risk of developing ureteral obstruction or spinal cord compression. This category of patients should be closely monitored during the first month of therapy. In the event that compression of the spinal cord or renal failure due to ureteral obstruction is observed or develops, standard treatment should be prescribed for these complications.

In women, Zoladex 10.8 mg is indicated only for the treatment of endometriosis and uterine fibroids.

During treatment and before the restoration of menstruation, non-hormonal methods of contraception should be used.

The use of GnRH analogues in women can cause a decrease in bone mineral density. The results of the study of Zoladex 3.6 mg show that after the end of treatment, some recovery of bone mineral density occurs; separate data on this with the use of Zoladex 10.8 mg are currently not available.

Currently, there is no experience of using hormone replacement therapy in the treatment of Zoladex 10.8 mg.

The resumption of menstruation after the end of treatment with Zoladex 10.8 mg may be delayed in some patients.

The use of Zoldex 10.8 mg may lead to increased cervical resistance, and caution should be exercised when dilating the cervix.

There are no data on the effectiveness of Zoladex 10.8 mg therapy lasting more than 6 months for benign gynecological diseases.

Influence on the ability to drive motor vehicles and manage mechanisms

There is no evidence that Zoladex 10.8 mg impairs the ability to drive vehicles and work with mechanisms.

Form of production

Zoladex is a syringe for subcutaneous administration of prolonged action.

Storage conditions

Store at temperatures below 25°C. Keep out of reach of children.

Shelf

life is 3 years.

Active ingredient

Goserelin

Conditions of release from pharmacies

By prescription

Dosage form

of the capsule

Description

Adults on doctor’s prescription

Weight

Weight: 43 gr.