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    / Astellas


    Active Ingredient
    Leuprorelin Acetate 7.5, 22.5, 45 mg

    Status in Israel
    RX

    Presentation and Status in Health Basket

    Presentation Basket Yarpa Pharmasoft

    Pre-filled Syringe

    1 X 22.5 mg

    partial basket chart 51301

    Pre-filled Syringe

    1 X 45 mg

    partial basket chart 51303

    Related information


    Dosage

    Leuprorelin should be administered under the direction of a healthcare professional having available the appropriate expertise for monitoring the response to treatment.
    Leuprorelin 7.5 mg is administered as a single subcutaneous injection every month. The injected solution forms a solid medicinal product delivery depot and provides continuous release of leuprorelin acetate for one month.
    Leuprorelin 22.5mg  is administered as a single subcutaneous injection every three months. The injected solution forms a solid medicinal product delivery depot and provides continuous release of leuprorelin acetate over a three-month period.
    Leuprorelin 45mg is administered as a single subcutaneous injection every six months. The injected solution forms a solid medicinal product delivery depot and provides continuous release of leuprorelin acetate over a six-month period. As a rule, therapy of advanced prostate cancer with Leuprorelin entails long-term treatment and therapy should not be discontinued when remission or improvement occurs. Response to Leuprorelin should be monitored by clinical parameters and by measuring prostate specific antigen (PSA) serum levels. Clinical studies have shown that testosterone levels increased during the first 3 days of treatment in the majority of non-orchiectomised patients and then decreased to below medical castration levels within 3 – 4 weeks. Once attained, castrate levels were maintained as long as medicinal product therapy continued (<1.0% testosterone breakthroughs). In case the patient’s response appears to be sub-optimal, it should be confirmed that serum testosterone levels have reached or are remaining at castrate levels. As lack of efficacy may result from incorrect preparation, reconstitution, or administration, testosterone levels should be evaluated in cases of suspected or known handling errors.


    Indications

    Treatment of hormone dependent advanced prostate cancer.


    Contra-Indications

    Contraindicated in women. Paediatric  patients. Hypersensitivity to leuprorelin acetate, to other GnRH agonists or to any of the excipients. In patients who previously underwent orchiectomy (as with other GnRH agonists, Leuprorelin does not result in further decrease of serum testosterone in case of surgical castration). As sole treatment in prostate cancer patients with spinal cord compression or evidence of spinal metastases.


    Special Precautions

    Lack of clinical efficacy may occur due to incorrect reconstitution of the product. for the instructions for preparation and administration of the product and for evaluation of testosterone levels in cases of suspected or known handling errors. Androgen deprivation therapy may prolong the QT interval. In patients with a history of or risk factors for QT prolongation and in patients receiving concomitant medicinal products that might prolong the QT interval physicians should assess the benefit risk ratio including the potential for Torsade de pointes prior to initiating Leuprorelin Acetate. Leuprorelin acetate, like other GnRH agonists, causes a transient increase in serum concentrations of testosterone, dihydrotestosterone and acid phosphatase during the first week of treatment. Patients may experience worsening of symptoms or onset of new symptoms, including bone pain, neuropathy, haematuria, or ureteral or bladder outlet obstruction. These symptoms usually subside on continuation of therapy. Additional administration of an appropriate antiandrogen should be considered beginning 3 days prior to leuprorelin therapy and continuing for the first two to three weeks of treatment. This has been reported to prevent the sequelae of an initial rise in serum testosterone. Following surgical castration, Leuprorelin Acetate does not lead to a further decrease in serum testosterone levels in male patients. Cases of ureteral obstruction and spinal cord compression, which may contribute to paralysis with or without fatal complications, have been reported with GnRH agonists. If spinal cord compression or renal impairment develops, standard treatment of these complications should be instituted. Patients with vertebral and/or brain metastases as well as patients with urinary tract obstruction should be closely monitored during the first few weeks of therapy. A proportion of patients will have tumors which are not sensitive to hormone manipulation. Absence of clinical improvement despite adequate testosterone suppression is diagnostic of this condition, which will not benefit from further therapy with Leuprorelin Acetate. Decreased bone density has been reported in the medical literature in men who have had orchiectomy or who have been treated with a GnRH agonist. Antiandrogen therapy significantly increases the risk for fractures owing to osteoporosis. Only limited data is available on this issue. Fractures owing to osteoporosis were observed in 5% of patients following 22 months of pharmacological androgen deprivation therapy and in 4% of patients following 5 to 10 years of treatment. The risk for fractures owing to osteoporosis is generally higher than the risk for pathological fractures. Apart from long lasting testosterone deficiency, increased age, smoking and consumption of alcoholic beverages, obesity and insufficient exercise may have an influence on the development of osteoporosis. During post-marketing surveillance, rare cases of pituitary apoplexy (a clinical syndrome secondary to infarction of the pituitary gland) have been reported after the administration of GnRH-agonists, with a majority occurring within 2 weeks of the first dose, and some within the first hour. In these cases, pituitary apoplexy was presented as sudden headache, vomiting, visual changes, ophthalmoplegia, altered mental status, and sometimes cardiovascular collapse. Immediate medical attention is required. Hyperglycemia and diabetes: Hyperglycemia and an increased risk of developing diabetes have been reported in men receiving GnRH agonists. Hyperglycemia may represent development of diabetes mellitus or worsening of glycemic control in patients with diabetes. Monitor blood glucose and/or glycosylated hemoglobin (HbA1c) periodically in patients receiving a GnRH agonist and manage with current practice for treatment of hyperglycemia or diabetes. Cardiovascular diseases: Increased risk of developing myocardial infarction, sudden cardiac death and stroke has been reported in association with use of GnRH agonists in men. The risk appears low based on the reported odds ratios, and should be evaluated carefully along with cardiovascular risk factors when determining a treatment for patients with prostate cancer. Patients receiving GnRH agonists should be monitored for symptoms and signs suggestive of development of cardiovascular disease and be managed according to current clinical practice.


    Side Effects

    Nasopharyngitis, nausea, diarrhea, ecchymoses, erythema, pruritus, night sweats, arthralgia, limb pain, myalgia, urinary infrequency, difficulty in micturation, dysuria, nocturia, oliguria, breast tenderness, testicular atrophy, testicular pain, infertility, breast hypertrophy,fatigue, injection site burning, injection site paraesthesia. Malaise, injection site pain, injection site bruising, injection site stinging , rigors, weakness, hot flashes, hypertension, hypotension.
    See prescribing information for full details.


    Drug interactions

    No pharmacokinetic drug-drug interaction studies have been performed with this drug.  There have been no reports of any interactions of leuprorelin acetate with other medicinal products. Since androgen deprivation treatment may prolong the QT interval, the concomitant use of this drug  with medicinal products known to prolong the QT interval or medicinal products able to induce Torsade de pointes such as class IA (e.g. quinidine, disopyramide) or class III (e.g. amiodarone, sotalol, dofetilide, ibutilide) antiarrhythmic medicinal products, methadone, moxifloxacin, antipsychotics, etc. should be carefully evaluated.


    Pregnancy and Lactation

    Contraindicated in women.
    See prescribing information for full details.


    Overdose

    Leuprorelin does not have the potential for abuse, and deliberate overdose is unlikely. There are no reports of abuse or overdose having occurred in clinical practice with leuprorelin acetate, but in the event that excessive exposure becomes a reality, observation and symptomatic supportive treatment are recommended.


    Important notes

    Compatibility: The leuprorelin present in syringe B must only be mixed with the solvent in syringe A and must not be mixed with other medicinal products.
    Storage: Store at 2-8°C.
    Effects on ability to drive and use machines: The ability to drive and operate machines may be impaired due to fatigue, dizziness and visual disturbances being possible side effects of treatment or resulting from the underlying disease.


    Manufacturer
    Astellas Pharma Europe BV, The Netherlands
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