Zoladex capsule n/k.vv.prol.d th 3.6mg-syringe applicator

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

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

In men, approximately by day 21 after the first capsule of testosterone concentration is reduced to post-castration levels and continues to be reduced at a constant treatment conducted every 28 days. This reduction in testosterone levels in most patients results in a regression of prostate cancer and symptomatic improvement.

In women, estradiol serum concentration is also reduced by about 21 days after the first capsule and, at regular administration of the drug every 28 days, is reduced to a level comparable to that seen in postmenopausal women. This reduction leads to a positive effect in hormone-dependent forms of breast cancer, endometriosis, uterine fibroid disease and suppression of follicular development in the ovary. It also causes thinning of the endometrium is the cause of amenorrhea in the majority of patients.

It is shown that Zoladex in combination with iron preparations amenorrhea and cause an increase in hemoglobin and related hematological parameters in women with fibroids and related anemia.

While taking LHRH agonists in women may occur menopause. Rarely, some women, there is no recovery of menses after cessation of therapy.

pharmacokinetics

Introduction capsules every 4 weeks maintains effective concentrations. Accumulation in the tissues at the same time 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 situations

In patients with impaired renal function T _1/2 is increased. With the introduction of Zoladex 10.8 mg every 12 weeks this change will not have a significant impact, so to change the dose for these patients is not required.

In patients with hepatic insufficiency significant changes in the pharmacokinetics was observed.

Active substance:
Goserelin

Manufacturer

AstraZeneca, UK

Prescribing

Adults are prescribed by a doctor

Composition

In one depot capsule for p / to the introduction of the prolonged action contained:

The active substance

goserelin (as acetate) 10.8 mg.

Excipients:

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

glacial acetic acid (removed in the manufacturing process).

Indications

• Prostate cancer is sensitive to hormonal influences.


• Endometriosis.


• uterine fibroids (as an adjuvant in combination with surgical treatment).

Contraindications

• Increased sensitivity to goserelin or other LHRH analogs.


• Pregnancy.


• lactation (breastfeeding).


• Children’s age.

Side effects

Cardio-vascular system

Possible hypotension or hypertension (usually transient, disappearing or Zoladex during therapy or after its termination; rarely required medical intervention, including cancellation Zoladex).

On the part of the central nervous system and peripheral nervous system

Possible nonspecific paresthesias.

On the part of the musculoskeletal system

Possible arthralgia.

allergic reactions

Rarely – hypersensitivity reactions, including some manifestations of anaphylaxis.

dermatological reactions

Possible skin rash (usually moderately expressed, often disappear without treatment discontinuation).

men

Possible hot flushes, sweating, reducing potency (cancel therapy is rarely necessary).

Sometimes – swelling and breast tenderness.

At the beginning of treatment in patients with prostate cancer may be a temporary strengthening of bone pain (symptomatic treatment).

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

Among women

Vzmozhno hot flashes, sweating, changes in libido (abolition of therapy is rarely necessary).

Sometimes – headaches, mood changes, including depression, dryness of the vaginal mucosa and changes in breast size.

Women with uterine fibroids is possible degeneration fibromatous nodes. As with other GnRH agonists, reported on the formation of ovarian cysts.

How to accept, acceptance rate and dosage

N / k in the anterior abdominal wall, every 12 weeks.

Of malignancy

The drug is used for a long time.

In benign gynecological diseases

The drug used is not more than 6 months.

Use of a special clinical cases

Elderly patients, patients with renal or hepatic insufficiency, to effect adjustments in the dose is not necessary.

Storage conditions

At temperatures below 25 ° C

Active substance

Goserelin

Interaction

Store at a temperature below 25 ° C.

Keep out of the reach of children.

Special conditions

Should be used with caution Zoladex 10.8 mg men are at particular risk for ureteral obstruction or compression of the spinal cord. In these patients should be monitored closely during the first month of therapy. In the event that there are, or are developing spinal cord compression or renal impairment due to ureteric obstruction, should be given the standard treatment for these complications.

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

During treatment and until recovery of menstruation should use non-hormonal methods of contraception.

The use of GnRH analogues in women can cause a reduction in bone mineral density. Results of the study 3.6 mg Zoladex show that after treatment there is a bone mineral density reduction, certain data about the application Zoladex 10.8 mg are not available at present.

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

Resumption of menses after treatment Zoladex 10.8 mg in some patients may be delayed.

Application Zoldeksa 10.8 mg may increase the resistance of the cervical, care must be taken in cervical dilation.

No data on the efficacy of therapy Zoladex 10.8 mg of more than 6 months for benign gynecological diseases.

Effects on ability to drive vehicles and management mechanisms

There is no evidence that Zoladex 10.8 mg impairs the ability to drive vehicles and operate machinery.

Pregnancy and lactation

Contraindicated during pregnancy and breastfeeding.

Use in children

Is contraindicated in children.

Overdose

• Symptoms: the experience of overdose in humans is limited. In the case of unintentional administration Zoladex earlier time or at a higher dose were noted clinically significant adverse events.
  


• Data regarding overdosage in humans is not available.


• Treatment: (in case of overdose) – symptomatic therapy

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