Leuprorelin


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : IM/SC Palliative treatment of advanced prostate cancer 1 mg/day as single dose via SC inj. Depot: In the UK: 3.75 mg every mth via IM/SC inj, or 11.25 mg every 3 mth via SC inj; in the US: 7.5 mg every mth, or 22.5 mg every 3 mth, or 30 mg every 4 mth via IM/SC inj; or 45 mg every 6 mth via SC inj. Endometriosis, Uterine fibroids Depot: 3.75 mg every mth via IM/SC inj or 11.25 mg every 3 mth as IM inj. Duration: Usually up to 3 mth (for anaemia due to uterine fibroids) or 6 mth (for endometriosis). Endometrial prep prior to intrauterine surgery 3.75 mg as a single inj via IM/SC given 5-6 wk before procedure; initiated during days 3-5 of menstrual cycle.
Dosage Details
Parenteral
Palliative treatment of advanced prostate cancer
Adult: 1 mg as single daily dose by SC inj. Depot preparations may be given by IM or SC route, dosage and route may differ between different brands and countries. In the UK: As depot preparations: 3.75 mg every mth as single IM/SC inj; or 11.25 mg every 3 mth via SC inj. In the US: As depot preparations: 7.5 mg every mth, or 22.5 mg every 3 mth, or 30 mg every 4 mth via IM/SC inj depending on the preparations; or 45 mg every 6 mth via SC inj.

Parenteral
Endometriosis
Adult: As depot preparations: 3.75 mg every mth given as a single IM/SC inj or 11.25 mg every 3 mth as IM depot Inj. Initiate treatment during the 1st 5 days of menstrual cycle up to 6 mth. May be used with norethindrone acetate 5 mg daily for initial management of endometriosis and for management of recurrence symptoms. Duration of retreatment: Should not exceed one additional 6 mth course.

Parenteral
Uterine fibroids
Adult: As depot preparations: In combination with iron therapy for women with anaemia due to uterine fibroids, 3.75 mg every month given as a single IM/SC inj or 11.25 mg every 3 months as IM Inj. Treatment duration: Usually up to 3 months. Max: 6 months.

Parenteral
Precocious puberty
Child: As aqueous soln inj: Initial: 50 mcg/kg daily by SC inj, may be titrated upwards by 10 mcg/kg/day if total down-regulation is not achieved. As depot preparations: Initial: 0.3 mg/kg/dose (minimum dose: 7.5 mg) given every 4 wk via IM inj; which equates to children ≤25 kg: 7.5 mg; >25-37.5 kg: 11.25 mg and >37.5 kg: 15 mg given every 4 wk. Maintenance: May titrate dose upwards in steps of 3.75 mg every 4 wk if down-regulation is not achieved. Consider discontinuing therapy before age 11 (females) and age 12 (males).

Parenteral
Preparation for intrauterine surgery
Adult: Endometrial preparation prior to intrauterine surgery: As depot preparations: 3.75 mg as a single inj via IM/SC given 5-6 wk before the procedure; therapy should be initiated during days 3-5 of the menstrual cycle.
Contraindications
Pregnancy, lactation; hypersensitivity to GnRH, GnRH agonist analogs or product excipients; undiagnosed abnormal vaginal bleeding.
Special Precautions
Vary inj site periodically. May cause transient elevation of testosterone levels during the first 1-2 wk, which may lead to worsening or onset of new symptoms (e.g. bone pain, neuropathy, haematuria) in prostate cancer patients. Ureteral obstruction and spinal cord compression have been reported; closely monitor patients with urinary obstruction and/or metastatic vertebral lesion. Leuprorelin is associated with increased risk of diabetes and certain CV diseases (heart attack, sudden cardiac death, stroke) when used in men for treatment of prostate cancer. For prostate cancer, monitor response by testosterone and prostate-specific antigen (PSA) levels. For precocious puberty in children, monitor response by GnRH stimulation test sex steroid levels 1-2 month after treatment initiation. Leuprorelin usually inhibits ovulation and stops menstruation in women, but does not incur contraception, non-hormonal contraception should be used as pregnancy is contraindicated. May cause adverse reactions associated with hypoestrogenism and loss in bone density.
Adverse Reactions
Inj site reactions. Treatment of precocious puberty: General pain, headache, acne, rash, seborrhoea, emotional lability, vaginitis, vaginal bleeding vaginal discharge. Treatment of prostate cancer: Transient worsening of signs and symptoms (usually increase in bone pain), ECG changes, high blood pressure, peripheral oedema, anorexia, constipation, nausea, vomiting, anaemia, myalgia, dizziness, general pain, headache, insomnia or sleep disorder, sinus congestion, urinary frequency/urgency, haematuria, UTI, asthaenia, physiological effects of decreased testosterone (e.g. gynaecomastia, breast tenderness, decreased testicular size, hot flashes, impotence). Treatment of endometriosis and uterine fibroids treatment: General pain, headache, asthaenia, nausea, vomiting, oedema, weight changes, acne, hirsutism, dizziness, insomnia, sleep disturbance, paraesthesias, skin reactions, effects of hypoestrogenism such as hot flashes, joint disorder, myalgia, decreased libido, depression, emotional lability, nervousness, breast tenderness, vaginitis.
Potentially Fatal: Anaphylactic reactions.
IM/Parenteral/SC: X
Lab Interference
As Leuprorelin suppresses the pituitary-gonadal system, treatment may interfere with diagnostic tests of pituitary gonadotropic and gonadal functions during treatment and up to 12 wk after discontinuing leuprorelin depot.
Action
Description: Leuprorelin is a gonadotropin-releasing hormone (GnRH) analogue. Following an initial stimulation of gonadotrophins, continuous admin of Leuprorelin leads to down regulation of GnRH receptors and subsequently reduces pituitary gonadotrophin secretion. Reduced gonadotrophin levels lead to inhibition of sex hormone (testosterone and oestrogen) production. Within 2-4 wk after treatment initiation, testosterone levels in male may be reduced to below castrate threshold.
Pharmacokinetics:
Absorption: Not active when given orally.
Distribution: Protein binding: 43-49%. Vd: 27 L (following IV bolus dose).
Metabolism: Major metabolite: Pentapeptide.
Excretion: Elimination half-life: 3 hr (following 1 mg IV bolus admin).
Disclaimer: This information is independently developed by MIMS based on Leuprorelin from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
  • Lucrin PDS
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