Zoladex 10.8 mg, syringe applicators

Zoladex is a synthetic analogue of the naturally occurring 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 serum testosterone concentrations in men and serum estradiol concentrations in women. In the early stages of therapy with Zoladex, some women may experience vaginal bleeding of varying duration and intensity.

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

In women, 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 the development of follicles in the ovaries. It also causes thinning of the endometrium and is the cause of amenorrhea in most patients.

It has been shown that Zoladex in combination with iron preparations causes amenorrhea and an increase in hemoglobin and relevant hematological parameters in women with uterine fibroids and concomitant anemia.

Against the background of taking LHRH agonists in women, the onset of menopause may occur. Rarely, some women do not return to menstruation after the end of therapy.

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

Plasma protein binding is low. In patients with normal renal function T 1/2 from blood serum is 2-4 hours.

Pharmacokinetics in special clinical situations

In patients with impaired renal function T 1/2 increases. With the introduction of Zoladex 10.8 mg every 12 weeks, this change will not have significant consequences, so changing the dose for this category of patients is not required.

In patients with hepatic insufficiency, significant changes in pharmacokinetics are not observed.

Composition

1 depot capsule for s / c administration of prolonged action contains:

Active substance

Goserelin (as acetate) 10.8 mg.  

Excipients:

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

glacial acetic acid (removed during production).

Indications

Use during pregnancy and lactation

Contraindications

Side effects

How to take, course of administration and dosage

Overdose

Special Instructions