Diphereline PR

Triptorelin

3.75 mg-, 11.25 mg-, & 22.5 mg-vial: Locally advanced or metastatic prostate cancer. 3.75 mg- & 11.25 mg-vial: Genital & extragenital endometriosis (Stage I-IV). 3.75 mg-vial only: High-risk localised or locally advanced prostate cancer in combination w/ RT. Central precocious puberty (before 8 yr in girls & 10 yr in boys). Uterine fibromyomas prior to surgery, associated w/ anaemia (Hb ≤8 g/dL), when a reduction in the size of fibromyoma is necessary to facilitate or modify the surgical techniques: endoscopic surgery, transvaginal surgery. Complementary treatment in association w/ gonadotrophins (hMG, FSH, hCG) in the course of ovulation induction in view of in vitro fertilisation & embryo transfer (I.V.F.E.T.). Adjuvant treatment in combination w/ tamoxifen or an aromatase inhibitor, of endocrine responsive early stage breast cancer in women at high risk of recurrence who are confirmed as pre-menopausal after chemotherapy completion.

IM 3.75-mg vial Prostate cancer 1 inj every 4 wk. Alternatively, 1 SC inj of immediate release Diphereline 0.1 mg for 7 days, then 1 IM inj of Diphereline PR 3.75 mg on day 8, repeated every 4 wk. Duration: 2-3 yr in patients w/ high-risk localised or locally advanced prostate cancer receiving RT. Central precocious puberty Childn >30 kg 1 inj every 4 wk (28 days), 20-30 kg ⅔ dose every 4 wk (28 days), <20 kg ½ dose every 4 wk (28 days). Endometriosis 1 inj every 4 wk (start in the 1st 5 days of the menstrual cycle). Max duration: 6 mth. Treatment of uterine fibromyoma prior to surgery 1 inj every 4 wk (start in the 1st 5 days of the menstrual cycle). Max duration: 3 mth. Female infertility 1 inj on the 2nd day of the cycle. Breast cancer 1 inj every 4 wk in combination w/ tamoxifen or an aromatase inhibitor, initiated at least 6-8 wk prior to aromatase inhibitor treatment. Min of 2 triptorelin inj (w/ 4 wk interval between inj) should be administered before commencement of aromatase inhibitor treatment. Duration: Up to 5 yr for adjuvant treatment in combination w/ other hormonotherapy. 11.25-mg vial Prostate cancer 1 inj every 3 mth. Endometriosis 1 inj every 3 mth (start in the 1st 5 days of the menstrual cycle) for at least 3 mth. Max duration: 6 mth. 22.5-mg vial Locally advanced or metastatic, hormone-dependent prostate cancer 1 inj every 6 mth.

Hypersensitivity to GnRH & its analogues. Pregnancy & lactation. In breast cancer treatment in pre-menopausal women: Initiation of aromatase inhibitor treatment before adequate ovarian suppression w/ triptorelin has been achieved.

Avoid inadvertent intravascular inj. May reduce bone mineral density, increasing the risk of osteoporosis. Rarely, treatment w/ GnRH analogues may reveal previously unrecognised presence of pituitary gonadotroph adenoma. Increased risk of depression (potentially severe) in patients treated w/ GnRH agonists; monitor patients who suffer from depression during treatment. Potential risk of haematoma; caution in patients treated w/ anticoagulants. May impair the ability to drive & use machines. In men: May cause transient increase in serum testosterone levels & transient worsening of signs & symptoms of prostate cancer during the 1st wk of treatment. Isolated cases of spinal cord compression or urethral obstruction. Risk of QT interval prolongation; anaemia; suppression of pituitary gonadotropin system; transient increase in acid phosphatases. Carefully assess before treatment initiation & monitor during treatment patients at high risk for metabolic or CV diseases. In women: Female infertility: Follicular recruitment induced by triptorelin inj associated w/ gonadotrophins may increase significantly in some predisposed patients, particularly in cases of polycystic ovary. Induced ovulation should only be carried out under close medical supervision w/ strict & regular biological & clinical tests: plasma oestrogen assay & ultrasonography. Endometriosis & pre-surgery treatment of uterine fibroids: Not recommended in patients <18 yr. Occurrence of constant hypogonadotropic amenorrhoea. Check plasma oestradiol levels in case of metrorrhagia; if <50 pg/mL, possible associated organic lesions should be investigated. A non-hormonal method of contraception should be used throughout treatment up to 1 mth after last inj. Regularly check the size of fibroid during uterine fibroid treatment. Few cases of bleeding have been reported in patients w/ submucosal fibroids. Breast cancer: Ensure adequate ovarian suppression following chemotherapy & before commencing triptorelin treatment; confirm adequate ovarian suppression following commencement of triptorelin treatment. Patients who discontinue triptorelin treatment should also discontinue aromatase inhibitors w/in 1 mth of last triptorelin administration (28-day formulation). Risk of musculoskeletal disorders when combined w/ an aromatase inhibitor or tamoxifen. Reports of HTN, hyperglycemia & diabetes in premenopausal women w/ breast cancer receiving triptorelin in combination w/ either exemestane or tamoxifen. Ped: Central precocious puberty: Childn w/ progressive brain tumours. Precocious pseudopuberty & gonadotropin-independent precocious puberty should be excluded. Mild to moderate vag bleeding during the 1st mth. Slipped capital femoral epiphysis can occur after treatment discontinuation.

Men: Decreased libido; paraesthesia in lower limbs; hot flushes; hyperhidrosis; back pain; erectile dysfunction (including ejaculation failure & disorder); asthenia. Anaemia; hypersensitivity; depression, libido loss, mood changes; dizziness, headache; HTN; dry mouth, nausea; musculoskeletal pain, pain in extremity; pelvic pain; inj site reaction (including erythema, inflammation & pain), oedema; increased wt. Women: Sleep disorders (including insomnia), mood disorder, decreased libido; headache; hot flushes; acne, hyperhidrosis, seborrhoea; breast disorder, dyspareunia, genital bleeding (including vag bleeding, w/drawal bleeding), ovarian hyperstimulation syndrome, ovarian enlargement, pelvic pain, vulvovag dryness; asthenia. Hypersensitivity; depression, nervousness; dizziness; nausea, abdominal pain & discomfort; arthralgia, muscle spasm, pain in limb; breast pain; inj site reaction (including pain, swelling, erythema & inflammation), peripheral oedema; increased wt. Childn: Genital bleeding (including vag haemorrhage, spotting), w/drawal bleeding, uterine haemorrhage, vag discharge. Hypersensitivity; headache; hot flushes; abdominal pain; acne; inj site reaction (including inj site pain, erythema & inflammation); increased wt. Breast cancer: Insomnia, decreased libido, depression; hot flushes, HTN; nausea; hyperhidrosis; musculoskeletal disorder, osteoporosis; urinary incontinence; dyspareunia, vulvovag dryness; fatigue. Hypersensitivity; diabetes (glucose intolerance), hyperglycaemia; embolism; fracture; inj site reaction.

Careful monitoring w/ hormone assays when triptorelin is used in combination w/ drugs that modify pituitary gonadotropins secretion. Potential additive effect on QT interval w/ drugs known to prolong QT interval or induce torsades de pointes eg, class IA antiarrhythmics (eg, quinidine, disopyramide) or class III antiarrhythmics (eg, amiodarone, sotalol, dofetilide, ibutilide), methadone, moxifloxacin, antipsychotics.

Cancer Hormone Therapy / Trophic Hormones & Related Synthetic Drugs

L02AE04 - triptorelin ; Belongs to the class of gonadotropin releasing hormone analogues. Used in endocrine therapy.

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