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LUPRODEX (LEUPROLIDE ACETATE) DEPOT INJECTION 11.25MG 1`S

Ksh 23,099

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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.

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.

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.

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.

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.

Storage

Store at room temperature (below 25°C). Keep in original packaging. Do not freeze. Reconstituted suspension must be administered immediately.

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.

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.

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.

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