Zoladex - Instructions For Use Of The Drug, Reviews, Analogs, Price

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Zoladex

Zoladex: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Drug interactions
14. 14. Analogs
15. 15. Terms and conditions of storage
16. 16. Terms of dispensing from pharmacies
17. 17. Reviews
18. 18. Price in pharmacies

Latin name: Zoladex

ATX code: L02AE03

Active ingredient: Goserelin acetate (Goserelin Acetate)

Manufacturer: AstraZeneca (UK)

Description and photo update: 2019-06-08

Prices in pharmacies: from 3739 rubles.

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Zoladex is a synthetic analogue of natural gonadotropin-releasing hormone (GnRH).

Release form and composition

Dosage form - capsules for subcutaneous administration of prolonged action, which are cylindrical pieces of solid polymeric material, free or almost free of visible inclusions, white or cream in color (in syringe applicators with a protective mechanism (Safety Glide safe administration system), 1 syringe per aluminum laminated envelopes, in a cardboard box 1 envelope).

Active ingredient: goserelin (in the form of acetate), in 1 capsule - 3.6 or 10.8 mg.

Additional substances of 3.6 mg capsules: glacial acetic acid, glycolic and lactic acid copolymer (50:50).

Additional substances of capsules 10.8 mg: copolymer of lactic and glycolic acids, low molecular weight (95: 5) and high molecular weight (95: 5).

Pharmacological properties

Pharmacodynamics

With constant use, Zoladex inhibits the release of luteinizing hormone by the pituitary gland, which leads to a decrease in the serum concentration of estradiol in women and testosterone in men. After discontinuation of the drug, this effect disappears. In the initial stage, goserelin, like other GnRH agonists, can temporarily increase the serum estradiol concentration in women and the serum testosterone concentration in men. Also, in the early stages of drug treatment, some women develop vaginal bleeding of varying intensity and duration.

In men, the testosterone concentration decreases to castration levels by about 21 days after the first administration of the Zoladex capsule and remains reduced with constant therapy, carried out every 28 days (when using 3.6 mg capsules) or every 3 months (when using 10.8 mg capsules) … With such a decrease in testosterone concentration in most patients, prostate tumor regression occurs and symptomatic improvement is observed.

The concentration of estradiol when using the drug in women also decreases by about 21 days after the administration of the first capsule of Zoladex 3.6 mg and remains reduced (at the level observed during menopause) with regular therapy carried out every 28 days. Such a decrease in the concentration of estradiol leads to a positive effect in endometriosis, hormone-dependent forms of breast cancer, suppression of the development of follicles in the ovaries and uterine fibroids. Thinning of the endometrium occurs, and most women develop amenorrhea.

After the introduction of 10.8 mg capsules, the serum concentration of estradiol in women decreases within 4 weeks after the introduction of the first capsule of the drug and remains reduced throughout the treatment. When switching to Zoladex 10.8 mg from other GnRH analogs, the suppression of estradiol concentration is preserved. The therapeutic effect of reducing the level of estradiol is manifested in uterine fibroids and endometriosis.

Zoladex 3.6 mg when combined with iron preparations causes amenorrhea, as well as an increase in the level of hematological parameters and hemoglobin in patients with concomitant anemia and uterine fibroids.

Menopause is possible during treatment with GnRH agonists. In some women (rarely), menstruation does not recover after treatment ends.

Pharmacokinetics

Maintaining effective drug concentrations is achieved by administering Zoladex 3.6 mg every 4 weeks and Zoladex 10.8 mg every 12 weeks. The drug does not accumulate in tissues.

Goserelin poorly binds to plasma proteins. In patients with normal renal function, the serum half-life of the drug is 2–4 hours (with impaired renal function, this indicator increases). With the monthly introduction of capsules 3.6 mg or 10.8 mg, such a change does not have significant consequences, therefore, dose adjustment is not required for patients with impaired renal function.

In case of impaired liver function, the pharmacokinetics of the drug changes slightly.

Indications for use

For capsules 3.6 and 10.8 mg:

• Fibroma of the uterus;
• Endometriosis;
• Prostate cancer.

For 3.6 mg capsules only:

• Mammary cancer;
• In vitro fertilization (to desensitize the pituitary gland);
• Planned operations on the endometrium (for its thinning).

Contraindications

Absolute:

• Childhood;
• Pregnancy and lactation;
• Individual hypersensitivity to the drug or other GnRH analogues.

Zoladex should be used with caution in the treatment of men who are at risk of developing spinal cord compression or ureteral obstruction, as well as when performing in vitro fertilization (IVF) in women with polycystic ovary syndrome.

Instructions for the use of Zoladex: method and dosage

3.6 mg capsules

Zoladex is injected subcutaneously into the anterior abdominal wall, 1 pc. every 28 days.

In malignant neoplasms, the drug is used for a long time. In benign gynecological diseases, therapy lasts up to 6 months (there is no data on the safety and effectiveness of longer treatment).

To thin the endometrium during planned operations, Zoladex is administered 2 times at 4-week intervals. In this case, the ablation of the uterus is performed in the first 2 weeks after the introduction of the second dose.

In IVF, Zoladex is used to desensitize the pituitary gland, which is determined by the level of estradiol in the blood serum. As a rule, the required concentration of estradiol, which corresponds to that in the early follicular phase of the cycle (about 150 pmol / l), is reached between 7 and 21 days. After the onset of desensitization with the help of gonadotropin, superovulation is stimulated. The desensitization of the pituitary gland caused by the use of Zoladex may be more persistent, as a result of which an increase in the need for gonadotropin is possible. Its administration is stopped at the appropriate stage of follicle development, then human chorionic gonadotropin (hCG) is administered to induce ovulation.

Capsules 10.8 mg

Zoladex is injected subcutaneously into the anterior abdominal wall:

• Men: every 3 months;
• Women: every 12 weeks.

Side effects

• Immune system: infrequently - hypersensitivity reactions; in rare cases - anaphylactic reactions;
• Metabolic disorders: often - decreased glucose tolerance (in men); infrequently - hypercalcemia (in women);
• Endocrine system: very rarely - hemorrhage in the pituitary gland;
• Cardiovascular system: very often - hot flashes; often - heart failure and myocardial infarction (in men), hypertension or hypotension;
• Nervous system and psyche: very often - decreased libido; often - depression and headache (in women), spinal cord compression (in men), decreased mood, paresthesia; very rarely - psychotic disorders;
• Musculoskeletal system: often - bone pain (in men), arthralgia (in women); infrequently - arthralgia (in men);
• Genitourinary system: very often - an increase in the size of the mammary glands and dryness of the vaginal mucosa (in women), erectile dysfunction (in men); often - gynecomastia (in men); infrequently - obstruction of the ureters and breast tenderness (in men); in rare cases - ovarian cyst (in women), ovarian hyperstimulation syndrome (in women to whom Zoladex is prescribed simultaneously with gonadotropins); frequency unknown - vaginal bleeding (in women);
• Skin and subcutaneous tissue: very often - increased sweating; often - alopecia (in women), rash; frequency unknown - alopecia (in men);
• Neoplasms: very rarely - a pituitary tumor; frequency unknown - degeneration of fibromatous nodes in women with uterine fibroids;
• Others: very often - reactions at the injection site of the capsule (in women); often - a temporary increase in the symptoms of the disease at the beginning of treatment for women with breast cancer, reactions at the injection site (in men);
• Laboratory tests: often - an increase in body weight, a decrease in bone mineral density.

Overdose

Data on Zoladex overdose are limited. With the unintentional introduction of capsules ahead of time or the use of the drug in higher doses, clinically significant side effects did not develop.

Overdose treatment is symptomatic.

special instructions

The resumption of the menstrual cycle after the end of the course of treatment may be delayed in some women. Before menstruation is restored, women undergoing treatment with Zoladex should use non-hormonal methods of contraception. In rare cases, menopause may occur without the restoration of menstruation after discontinuation of the drug.

When goserelin is used in combination with gonadotropin, ovarian hyperstimulation syndrome (OHSS) may develop. For this reason, it is necessary to carefully monitor the process of stimulating the cycle in order to identify the risk of developing OHSS in time. If necessary, the administration of hCG should be discontinued.

According to the instructions, Zoladex can lead to an increase in cervical resistance, and therefore, care must be taken when dilating the cervix.

During IVF, the drug should be used only in a specialized medical institution under the supervision of a doctor with experience in this field.

GnRH analogues can cause a decrease in bone mineral density. Reducing the loss of bone mineral density and the manifestation of vasomotor symptoms in women receiving Zoladex for the treatment of endometriosis allows the simultaneous administration of hormone replacement therapy with daily use of estrogen and progestogen drugs. In men, the loss of bone mineral density, according to preliminary data, reduces the simultaneous use of bisphosphonate.

Since GnRH agonists can reduce glucose tolerance in men, it is recommended that they regularly monitor blood glucose levels.

There were no reports of the negative effect of Zoladex on the reaction rate and ability to concentrate.

Application during pregnancy and lactation

Zoladex is contraindicated in pregnant and lactating women.

Pediatric use

The drug is not used in children and adolescents.

With impaired renal function

Patients with impaired renal function do not require dose adjustment of Zoladex.

For violations of liver function

Patients with impaired liver function do not require dose adjustment of Zoladex.

Drug interactions

There is no information on the interaction of Zoladex with other drugs.

Analogs

Analogs of Zoladex are: Decapeptyl, Decapeptyl Depot, Dipherelin, Leiprorelin Sandoz, Lukrin Depot, Lupride Depot, Eligard.

Terms and conditions of storage

Store at temperatures up to 25 ° C out of reach of children.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Zoladex

There are reports of the frequent occurrence of adverse reactions. According to reviews, Zoladex regularly causes sleep disturbances, headaches and frequent menstruation. Despite this, the drug is effective, as evidenced by the positive characteristics of this drug.

The price of Zoladex in pharmacies

Capsules for subcutaneous administration of prolonged action at a dosage of 3.6 mg (1 pc. In a package) can be bought in pharmacies at a price of 7873 rubles.

The price for Zoladex 10.6 mg (1 pc. In a package) is from 22 297 rubles.

Zoladex: prices in online pharmacies

Drug name Price Pharmacy

Zoladex 3.6 mg capsule for subcutaneous administration of prolonged action 1 pc. 3739 RUB Buy

Zoladex 10.8 mg capsule for subcutaneous administration of prolonged action 1 pc. 12 699 RUB Buy

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!