1 What is this medicine
and what is it used for?
Leuprolide acetate is a synthetic GnRH
(gonadotrophin-releasing hormone) agonist. When given continuously (as a depot
formulation), it initially causes a transient surge in LH and FSH — and
therefore testosterone/oestrogen — followed by profound and sustained
suppression of gonadal hormone production. This is called 'medical castration'
or androgen/oestrogen deprivation therapy (ADT/EDT).
The 11.25 mg depot formulation provides 3 months
(approximately 84 days) of continuous GnRH agonist activity from a single
injection. It is used for:
• Prostate cancer — androgen
deprivation therapy in hormone-sensitive advanced or metastatic prostate
cancer; and adjuvant therapy with radiation.
• Endometriosis — treatment of pelvic
pain, dysmenorrhoea, and dyspareunia associated with endometriosis.
• Uterine fibroids (leiomyomata) —
pre-operative shrinkage of fibroids.
• Central precocious puberty — to delay
premature puberty in children.
2 How this medicine is
given
The Luprodex 11.25 mg depot is given as a single deep
intramuscular (IM) or subcutaneous (SC) injection by a healthcare professional
every 3 months (12-weekly). It must be reconstituted immediately before
injection — the powder is combined with the provided diluent in the syringe and
administered without delay after reconstitution. Injection sites (typically
gluteal, deltoid, or anterior thigh) should be rotated.
|
The 3-month depot replaces monthly injections —
convenience is a key benefit. TESTOSTERONE FLARE (Prostate Cancer): During
the first 1–2 weeks, leuprolide causes a temporary rise in testosterone
before it drops. This 'flare' can temporarily worsen bone pain or urinary
symptoms. Anti-androgen cover (e.g. bicalutamide) is usually given for the
first 4 weeks to block the effects of the testosterone surge. |
3 Possible side effects
|
Frequency |
Side Effect |
What to Do |
|
Very Common (>10%) |
Hot flushes |
Breathable clothing;
cooling fans; discuss pharmacological options (e.g. venlafaxine) with doctor. |
|
Very Common (>10%) |
Decreased libido /
sexual dysfunction |
Expected effect of
hormone suppression. Counsel patients. |
|
Very Common (>10%) |
Fatigue |
Regular gentle
exercise; rest as needed. |
|
Very Common (>10%) |
Decreased bone mineral
density (osteoporosis risk) |
Calcium + Vitamin D
supplementation; DEXA scan; consider bone protection
(bisphosphonates/denosumab). |
|
Common (1–10%) |
Testosterone flare
(prostate cancer — first 2 weeks) |
Cover with
anti-androgen for first 4 weeks; monitor for worsening symptoms. |
|
Common (1–10%) |
Injection site
reactions |
Rotate sites; warm
compress post-injection. |
|
Common (1–10%) |
Mood changes /
depression |
Monitor mood; refer
for psychological support if needed. |
|
Common (1–10%) |
Gynaecomastia
(prostate cancer) |
Usually mild; discuss
options with oncologist. |
|
Common (1–10%) |
Cardiovascular risk
(metabolic syndrome, diabetes) |
Monitor glucose,
lipids, blood pressure; lifestyle optimisation. |
4 Contraindications
Leuprolide is contraindicated in: pregnancy (can cause foetal
harm — category X); undiagnosed vaginal bleeding (gynaecological indications);
known hypersensitivity to GnRH agonists or excipients.
Use with caution in: patients with cardiovascular disease
(increased risk of MI, sudden cardiac death described in androgen deprivation
therapy — monitor carefully); patients with prior osteoporosis; and patients
with a history of depression.
5 Drug interactions
• QT-prolonging agents: GnRH agonists
prolong QT interval — additive risk. Monitor ECG.
• Antidiabetics: androgen deprivation
reduces insulin sensitivity — monitor and adjust antidiabetic doses.
• Anticoagulants: INR changes possible
during hormonal treatment — monitor warfarin patients.
6 Storage
Store at room temperature (below 25°C). Keep in original
packaging. Do not freeze. Reconstituted suspension must be administered
immediately.
7 Prescription
requirement
|
PRESCRIPTION ONLY MEDICINE (POM) —
Oncology/urology (prostate cancer) or gynaecology (endometriosis/fibroids)
specialist prescription. Monitoring (prostate cancer): PSA, testosterone
levels, bone density (DEXA), cardiovascular risk factors, glucose/lipids. |
8 Guidance for patients
& caregivers
For prostate cancer patients: in the first 2 weeks after your
first injection, testosterone temporarily rises before it falls. This 'flare'
can briefly worsen symptoms (bone pain, urinary difficulties). Your doctor will
prescribe an anti-androgen tablet to take during this period to block the
effects of the flare.
Long-term androgen deprivation reduces bone density. It is
very important to take calcium and vitamin D daily, to do weight-bearing
exercise regularly, and to have bone density scans as scheduled.
The hot flushes and sexual side effects are expected and are
due to hormone suppression. Various management strategies are available —
discuss with your specialist team.
9 Pharmacist &
prescriber notes
Luprodex 11.25 mg = 3-month depot formulation (vs 3.75 mg =
1-month). The testosterone flare in the first 7–10 days requires concurrent
anti-androgen cover (bicalutamide 50 mg/day or cyproterone acetate for 4 weeks
starting 3 days before first injection).
This is especially important in patients with spinal
metastases or severe obstructive uropathy — the flare in these patients can
precipitate spinal cord compression or acute urinary retention.
QT prolongation: baseline and periodic ECG monitoring
recommended, particularly in patients on other QT-prolonging drugs.
Cardiovascular events: FDA/EMA warning — increased risk of MI, sudden cardiac
death, and stroke with GnRH agonists. Screen and optimise CV risk factors
before starting.
10 Frequently asked
questions
Will I lose my sex drive permanently?
Libido is suppressed while your testosterone levels are low
during treatment. If treatment is eventually stopped, testosterone levels
typically recover — though this takes several months and is not guaranteed in
all patients, especially after long-term therapy.
What about my bones?
Long-term testosterone suppression reduces bone mineral
density (osteoporosis). Calcium (1000–1200 mg/day) and vitamin D (800–1000
IU/day) supplements are important. A bone density scan (DEXA) is recommended at
baseline and every 1–2 years.
Can leuprolide affect my heart?
There is evidence that androgen deprivation therapy modestly
increases cardiovascular risk over time. Regular monitoring of blood pressure,
blood glucose, and cholesterol is important. Report any chest pain, shortness
of breath, or palpitations immediately.
What is the difference between this and tablets like
relugolix?
Luprodex is an injection given every 3 months. Relugolix
(Orgovyx) is an oral daily tablet. Both reduce testosterone but work
differently: leuprolide is a GnRH agonist (initial flare then suppression);
relugolix is a GnRH antagonist (immediate suppression, no flare). Your
urologist/oncologist will choose the most appropriate option.
Can I still drive and work normally?
Yes, in general. Fatigue and mood changes may affect some
patients. Discuss any specific occupational concerns with your doctor.