Leuprorelin parenteral
- Drugs List
- Therapeutic Indications
- Dosage
- Administration
- Contraindications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
- Monograph
Presentation
Injections of leuprorelin.
Drugs List
Therapeutic Indications
Uses
Breast cancer
Carcinoma - prostate
Endometrial preparation before intrauterine surgery
Endometriosis
Gonadotrophin-dependent precocious puberty
Preservation of ovarian function
Treatment of uterine fibroids prior to surgery
Metastatic prostate cancer.
Locally advanced prostate cancer, as an alternative to surgical castration.
As an adjuvant treatment to radiotherapy in patients with high-risk localised or locally advanced prostate cancer.
As an adjuvant treatment to radical prostatectomy in patients with locally advanced prostate cancer at high risk of disease progression.
Neo-adjuvant treatment prior to radiotherapy in patients with high-risk localised or locally advanced prostate cancer.
Management of endometriosis, including pain relief and reduction of endometriotic lesions.
Endometrial preparation before intrauterine surgery, including endometrial ablation or resection.
Reduction in size of uterine fibroids prior to surgery, and of associated bleeding.
Preservation of ovarian function in pre-menopausal women with neoplastic disease undergoing chemotherapy treatment that can cause premature ovarian insufficiency.
Treatment in pre and perimenopausal women with advanced breast cancer suitable for hormonal control.
Endocrine responsive early stage breast cancer in pre and perimenopausal women at higher risk of disease recurrence, as an adjunctive treatment in combination with tamoxifen or an aromatase inhibitor.
Treatment of central precocious puberty (girls under 9 years of age, boys under 10 years of age)
Dosage
Adults
Prostatic cancer
3.75mg by subcutaneous or intramuscular injection every 4 weeks.
Or
11.25mg by subcutaneous injection every 3 months.
Monitor the response by measuring clinical parameters and testosterone serum levels and/or prostate-specific antigen (PSA). If a patient has a suboptimal response it is recommended to confirm serum testosterone levels have reached or are remaining at castrate levels.
Endometriosis
3.75mg by subcutaneous or intramuscular injection every 4 weeks for a maximum of 6 months, starting during first 5 days of the menstrual cycle.
Or
11.25mg by intramuscular injection every 3 months for a maximum of 6 months, starting during first 5 days of the menstrual cycle.
If considered necessary to reduce bone mineral density loss and vasomotor symptoms, hormone replacement therapy (HRT) can be co-administered with leuprorelin providing the risks and benefits of this action has been taken into account.
Endometrial preparation for intrauterine surgery
3.75mg by subcutaneous or intramuscular injection 5 to 6 weeks before surgery, starting during days 3 to 5 of the menstrual cycle.
Preoperative management of uterine fibroids and associated bleeding
3.75mg by subcutaneous or intramuscular injection every 4 weeks, usually for 3 to 4 months up to a maximum of 6 months.
Preservation of ovarian function
3.75mg by subcutaneous or intramuscular injection 2 weeks before starting chemotherapy and every 4 weeks thereafter for the duration of chemotherapy.
Advanced Breast cancer
3.75mg by subcutaneous injection every month.
Or
11.25mg by subcutaneous injection every 3 months.
Early Breast cancer
3.75mg by subcutaneous injection every month in combination with tamoxifen or an aromatase inhibitor.
Or
11.25mg by subcutaneous injection every 3 months in combination with tamoxifen or an aromatase inhibitor.
Women receiving chemotherapy should start leuprorelin therapy after completion of chemotherapy, once pre-menopausal status has been confirmed.
The recommended duration of combination therapy is up to 5 years.
Children
Gonadotrophin-dependent precocious puberty:
Child with body weight of 20kg or greater:
3.75mg by subcutaneous injection every 4 weeks.
Or
11.25mg by subcutaneous injection every 3 months.
Child with body weight of less than 20kg:
1.88mg by subcutaneous injection every 4 weeks.
Or
5.625mg by subcutaneous injection every 3 months.
Doses may need to be increased if inadequate suppression at starting dose. Minimal effective monthly dose should be determined by means of LHRH test.
Manufacturer recommends dosing interval of 30 (+/- 2) days should be maintained to prevent recurrence of symptoms.
Additional Dosage Information
In combination with aromatase inhibitor for advanced and early breast cancer
Leuprorelin treatment should be initiated 6-8 weeks before starting aromatase inhibitor treatment.
Two 3.75mg injections with an interval of 4 weeks should be administered before aromatase inhibitor treatment.
Or
One 11.25mg injection should be administered before aromatase inhibitor treatment.
Administration
For subcutaneous or intramuscular injection after reconstitution.
If repeated injections are required, then the site of administration should be varied.
Contraindications
Breastfeeding
Long QT syndrome
Pregnancy
Torsade de pointes
Undiagnosed gynaecological haemorrhage
Precautions and Warnings
Children under 18 years
Family history of long QT syndrome
Major risk factors for decreased bone mineral content
Predisposition to diabetes mellitus
Predisposition to seizures
Tobacco smoking
Cardiovascular disorder
Chronic alcoholism
Depression
Diabetes mellitus
Electrolyte imbalance
Epileptic disorder
History of depression
History of seizures
History of torsade de pointes
Urinary obstruction
Vertebral metastases
Correct electrolyte disorders before treatment
Advise ability to drive/operate machinery may be affected by side effects
Not all available brands are licensed for all age groups
Not all available brands are licensed for all indications
Not all available strengths are licensed for all indications
Prostate cancer: Prophylaxis of flare with anti-androgen is recommended
Administer reconstituted solution immediately
Do not discontinue on remission or improvement
Vary injection site during prolonged therapy
Exclude pregnancy prior to initiation of treatment
Measure bone density in at risk patients prior to therapy
Children: Monitor bone age at 6-12 month intervals
Consider monitoring ECG in patients at risk of QT prolongation
If spinal cord compression present/develops,use specific standard treatment
Monitor blood glucose closely in patients with diabetes mellitus
Monitor closely patient at risk of cardiovascular disorders
Monitor hepatic function
Monitor patient for signs and symptoms of depression
Monitor patients at risk of spinal cord compression or urinary obstruction
Monitor patients with metabolic disorders
Monitor serum electrolytes
Monitor testosterone level in event of injection site abscess
Advise patient to report any new or worsening depression/suicidal ideation
Disease flare may occur at beginning of treatment
May increase uterine cervical resistance
Advise patient to seek advice at first indications of pregnancy
Female: Barrier or non-hormonal contraception advised during treatment
Advise patient that abnormal bleeding and pain may occur
Advise patient to report regular menstruation if it persists during therapy
Menstruation stops during treatment
An initial rise in sex steroids may occur, leading to worsening clinical signs and symptoms, with continued treatment this should dissipate.
In women it is advised to confirm diagnosis of fibroids and exclude ovarian mass before treatment.
Sterile abscess at injection site has occurred during leuprorelin treatment (mainly after intramuscular injection at higher than recommended dosage) which may decrease the absorption of leuprorelin from the depot. In cases of abscess hormonal parameters (testosterone, oestradiol) should be monitored at 2 week intervals.
Pregnancy and Lactation
Pregnancy
Leuprorelin is contraindicated during pregnancy.
The manufacturers recommend excluding pregnancy before starting leuprorelin. Human data suggests an increase in foetal malformations when leuprorelin is used during pregnancy.
Lactation
Leuprorelin is contraindicated during breastfeeding.
The manufacturers recommend that leuprorelin should not be used during breastfeeding.
Side Effects
Abdominal pain
Acne
Altered glucose tolerance
Altered hormone levels
Altered liver function tests
Anaphylactic reaction
Anorexia
Arthralgia
Blood lipid changes
Blurred vision
Breast tenderness
Changes in breast size
Changes in libido
Chills
Decrease in bone mineral density
Decrease in trabecular bone density
Depression
Diarrhoea
Dizziness
Emotional lability
Epiphysiolysis at the site of the hip joint
Facial oedema
Fatigue
Fever
Gynaecomastia
Hair loss
Headache
Hepatic disorders
Hot flushes
Hypersensitivity reactions
Hypertension
Hypotension
Impotence
Increased uterine cervical resistance
Insomnia
Interstitial pneumonitis
Irritation (injection site)
Jaundice
Leucopenia
Menstrual disturbances
Mood changes
Muscle weakness
Myalgia
Nausea
Palpitations
Paraesthesia
Paralysis
Peripheral oedema
Pituitary apoplexy
Prolongation of QT interval
Pruritus
Pulmonary embolism
Rash
Seizures
Spinal fracture
Sweating
Testicular atrophy
Thrombocytopenia
Tumour flare
Urinary obstruction
Urticaria
Vaginal bleeding
Vaginal dryness
Visual disturbances
Vomiting
Weight changes
Wheezing
Worsening depression
Overdosage
It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.
The following number will direct the caller to the relevant local centre (0844) 892 0111
Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Further Information
Last Full Review Date: June 2019
Reference Sources
Summary of Product Characteristics: Prostap SR DCS. Takeda UK ltd. Revised May 2019.
Summary of Product Characteristics: Prostap 3 DCS. Takeda UK ltd. Revised August 2019.
NICE Evidence Services Available at: www.nice.org.uk Last accessed: 19 June 2019
Medscape UK | Univadis prescription drug monographs & interactions are based on FDB Multilex Content
FDB Disclaimer : FDB Multilex is intended for the use of healthcare professionals and is provided on the basis that the healthcare professionals will retain FULL and SOLE responsibility for deciding what treatment to prescribe or dispense for any particular patient or circumstance.