Leuprorelin

When ATH:
L02AE02

Characteristic.

The antitumor agent, synthetic analog of gonadotropin releasing hormone. Available in the form of acetate, molecular weight 1269,47.

Pharmacological action.
Antigonadotropnoe, anti-androgenic, antiestrogens, antitumor.

Application.

Progressive hormone-dependent prostate cancer (symptomatic treatment, as an alternative to orchiectomy or estrogenterapii). Uterine fibroids (preoperatively or alternatively surgery), endometriosis (confirmed by laparoscopy).

Contraindications.

Hypersensitivity (incl. analogs of gonadotropin-releasing hormone), hormone-prostate cancer, metastases to the spine or urinary tract obstruction (for the treatment of prostate cancer), uterine bleeding of unknown etiology.

Pregnancy and breast-feeding.

Contraindicated during pregnancy and lactation (unknown, Do penetrates into breast milk). Leuprorelin can cause adverse fetal effects when administered to pregnant women. Fetal disorders after administration of leuprolide acetate during pregnancy were observed in rabbits, but not in rats. Increased mortality and body weight were observed and fruits rabbits, in rats and. Causes, causing fetal mortality, are a consequence of the hormonal effects of leuprorelin. Suggest, that when using leuprorelin during pregnancy, there is a risk of spontaneous miscarriage.

In women of childbearing age before treatment should be deleted pregnancy, use non-hormonal methods for contraception.

Side effects.

From the nervous system and sensory organs: headache, dizziness, depression, anxiety, nervousness, fatigue, sleep disturbance, fainting, paresthesia, hallucinations, stupor, personality changes, memory impairment, hearing and visual impairment, noise in ears, conjunctivitis.

Cardio-vascular system and blood (hematopoiesis, hemostasis): heartbeat, tachycardia, chest tightness, ECG changes.

From the digestive tract: change in appetite, taste, dry mouth or hypersalivation, thirst, nausea, vomiting, diarrhea or constipation, increase or reduction of body weight, increased activity of alkaline phosphatase and hepatic transaminases.

Allergic reactions: dermatitis, itching, rash.

Other: swelling of the face and legs, tides (sudden sweating or warmth), decreased libido; in women - androgenic effects (lowering the timbre of the voice, hirsutism), amenorrhea, vaginal dryness, vaginitis, white, acne, reduction in bone density and bone mass, increase plasma cholesterol; in men - angina pectoris and myocardial infarction (chest pain), pulmonary embolism (sudden shortness of breath), tromboflebit (pain in the groin or leg, especially in the calf muscles), impotence, gynecomastia, decrease in testicular.

Local reactions - pain and redness at the injection site.

At the beginning of treatment - transient effects: increased symptoms of the disease / additional symptoms of the underlying disease, incl. joint pain (males); increased symptoms of the disease in patients with metastases in the spine, urinary tract obstruction or hematuria may result in neurological problems, such as temporary weakness of the lower limbs, paresthesias and weighting of urological symptoms.

Cooperation.

Alcohol potentiates the reduction in the rate of psychomotor reactions.

Overdose.

Symptoms: increased side effects.

Treatment: symptomatic.

Dosing and Administration.

/ M or n / a (injection is prepared time) 1 every 1-3 months (depot): with prostate cancer - 3,75 or 7,5 mg; with uterine fibroids and endometriosis - 3,75 mg; women of childbearing age the first injection is carried out on the third day of menstruation; course - no more 6 Months.

Precautions.

Patients with increased risk of complications should be under medical supervision for 7 days after the first injection. During treatment it is necessary to control the level of LDH, hepatic transaminases, and before the start of re-rate to determine bone density. During the treatment of endometriosis there is a risk of bone density reduction of the gain in trabecular spine (It may be irreversible); 6-month period of treatment is reduction in the density slightly, except in patients with risk factors (a history of osteoporosis e.g.).

In the treatment of prostate cancer in order to prevent the symptoms, associated with the increase in the plasma concentration of testosterone, should be prescribed anti-androgens. In the case of metastasis to the spine in prostate cancer symptoms may increase during the first few weeks of treatment with leuprorelin risk of neurological complications, including paralysis.

In men, the suppression of secretion of testosterone leads to impaired fertility. Although it is not known, whether to restore fertility after the abolition of leuprolide, after the cancellation of similar analogues restore fertility occurred.

It will be appreciated, that after 6 months of treatment leuprorelin endometriosis menstruation resumes 3 Months. Reduces the speed of psychomotor reactions, and during treatment is not recommended to engage in potentially dangerous activities.

Place of introduction should be changed every month (buttocks, hip).