Enantone L.P.

3.75 mg & 11.25 mg: Metastatic prostate cancer; locally advanced prostate cancer, as alternative to surgical castration. Adjuvant treatment to RT in patients w/ high-risk localized or locally advanced prostate cancer & to radical prostatectomy in patients w/ locally advanced prostate cancer at high risk of disease progression. Endometriosis at genital & extra-genital localization (from stage I-IV). Uterine fibroids (leiomyomata), when suppression of ovarian hormone production is indicated, as pre-op measure for vol reduction of individual fibroids in fibroid nucleation or hysterectomy. Central precocious puberty (girls <9 yr, boys <10 yr). Premenopausal breast cancer. 11.25 mg: Symptomatic laparoscopically confirmed endometriosis, when suppression of ovarian hormone production is indicated, provided the disease does not primarily require surgery; pre-op flattening of endometrium before planned operative hysteroscopic intervention eg, endometrium ablation or resection. 30 mg: Advanced prostate cancer.

SC/IM Prostate cancer Adult (including elderly) One 3.75-mg inj mthly or one 11.25-mg inj every 3 mth. Endometriosis One 3.75-mg inj mthly or one 11.25-mg inj every 3 mth. Start treatment during 1st 5 days of menstrual cycle. Management of endometriosis including pain relief & reduction of endometriosis lesions Duration: Up to 6 mth as monotherapy. 3.75-mg inj may be administered mthly for a period of 12 mth w/ concurrent HRT (norethindrone acetate 5 mg daily) & Ca supplementation. One 11.25-mg inj is administered to flatten endometrium before planned hysteroscopic operative interventions. Uterine fibroids Patient w/ heavy wt or markedly enlarged uterus One 3.75 mg inj mthly or one 11.25 mg inj every 3 mth initiated on 1st-5th day after the start of menstrual period. Duration: Up to 3 mth for 3.75-mg inj, 6 mth for 11.25-mg inj. Pre-op hematologic improvement of patients w/ anemia caused by uterine fibroids 11.25-mg inj + Fe. Premenopausal breast cancer Adult One 3.75-mg inj mthly or one 11.25-mg inj every 3 mth. Central precocious puberty 90-400 mcg/kg mthly or one 11.25-mg inj every 3 mth. May adjust dose according to patient's response. Advanced prostate cancer One 30-mg inj every 6 mth at 168-182 days (24-26 wk) interval. Inj sites may include abdominal skin, buttocks & upper thigh, changed every 6 mth.

3.75 mg & 11.25 mg: Hypersensitivity to leuprorelin acetate, other synthetic GnRH analogues or derivatives. Undiagnosed abnormal vag bleeding. Pregnancy & lactation. 30 mg: History of hypersensitivity to leuprorelin acetate or synthetic LH-RH or LH-RH derivatives.

W/draw treatment immediately if signs & symptoms of severe cutaneous reactions including SJS & TEN appear. Increased risk of depression; bone loss leading to osteoporosis & bone fracture in patients w/ additional risk factors. Seizures in adults & childn w/ or w/o history of epilepsy, seizure disorders or risk factors for seizures. Transient rise in testosterone, dihydrotestosterone & acid phosphatase levels in initial stages of therapy. Urinary tract obstruction & hematuria due to flare of primary carcinoma. May prolong QT interval. Patients w/ history of or risk factors for QT prolongation & those receiving concomitant medicinal products that might prolong QT interval. Administer anti-androgen 3 days prior to therapy & continue for the 1st 2-3 wk of treatment to reduce risk of flare. Carefully consider & closely supervise patients at risk of ureteric obstruction or spinal cord compression in the 1st few wk of treatment. Monitor patients at high risk for metabolic change or syndrome, or CV diseases. Frequently monitor blood glucose during treatment in diabetic patients. May influence ability to drive & use machines due to visual disturbances & dizziness. 3.75 mg & 11.25 mg: Permanently discontinue treatment if pseudotumor cerebri (PTC)/idiopathic intracranial HTN is confirmed. Increased uterine cervical resistance. Limited to 6 mth use. Persistent regular menstruation. Patients w/ major risk factors for decreased bone mineral content eg, chronic alcohol &/or tobacco use, strong family history of osteoporosis, or chronic use of drugs that can reduce bone mass eg, anticonvulsants or corticosteroid. Women w/ uterine fibroids. Males w/ urinary obstruction &/or metastatic vertebral lesions. Monitor patients for signs & symptoms of PTC including papilledema, headache, blurred vision, diplopia, loss of vision, pain behind eye or pain w/ eye movement, tinnitus, dizziness & nausea. Investigate undiagnosed abnormal vag bleeding. Confirm diagnosis of fibroids & exclude ovarian mass before initiating treatment. Instruct patients to prevent use of non-hormonal contraceptive methods during treatment. Not to be used during pregnancy & lactation. Childn w/ progressive brain tumors. Bone mineral density may decrease during therapy in childn w/ central precocious puberty. 11.25 mg: Discontinue administration if antitumor effect is not obtained & any tumor progression is observed. Not to be used when hormone receptor expression is -ve. Consider treatment discontinuation in girls w/ bone maturation >12 yr & boys w/ bone maturation >13 yr. Abnormal bleeding or pain in women w/ submucous fibroids. Transient aggravation of bone pain. Vag bleeding, spotting, discharge after 1st inj as sign of hormone w/drawal in girl w/ central precious puberty. Measure bone density before treatment of uterine fibroids in patients w/ major risk factors for decreased bone mineral contents & do not restart treatment when results are below normal range. Perform precise diagnosis of idiopathic &/or neurogenic central precocious puberty before therapy. Monitor hormonal parameters (testosterone, oestradiol) at 2-wk intervals in case of decreased absorption from depot; bone age at 6-12 mth intervals. Investigate vag bleeding beyond 1st or 2nd mth of therapy. 30 mg: Not indicated in case of hormone-independence of carcinoma. May cause reversible depression of fertility in men. Not intended to use in female & contraindicated during pregnancy & lactation.

Hot flush; headache; increased wt, decreased appetite; nausea; hyperhidrosis; muscular weakness; insomnia; testicular erectile dysfunction, testicular atrophy, decreased libido; inj site reaction (eg, induration, erythema, pain, abscess, swelling, nodules & necrosis), fatigue. Depression, mood changes (long term use); arthralgia; edema; dizziness; vomiting, diarrhea; abnormal hepatic function (including jaundice) & hepatic function test (usually transient); gynecomastia. 3.75 mg & 11.25 mg: Bone pain; vag hemorrhage, vulvovag dryness. Paresthesia; breast tenderness, vulvovaginitis, breast atrophy, vag discharge; visual impairment; palpitations; alopecia; abdominal pain; acne.

Concomitant use w/ medicinal products known to prolong QT interval or induce Torsades de Pointes eg, Class IA (eg, quinidine, disopyramide) or Class III (eg, amiodarone, sotalol, dofetilide, ibutilide) antiarrhythmics, methadone, moxifloxacin, antipsychotics.

Trophic Hormones & Related Synthetic Drugs / Cancer Hormone Therapy

L02AE02 - leuprorelin ; Belongs to the class of gonadotropin releasing hormone analogues. Used in endocrine therapy.

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