Product Introduction:
Leuprosun is a sterile, long-acting depot formulation administered via intramuscular injection. It is primarily used in hormone-dependent cancers and disorders, where reduction in estrogen or testosterone levels is beneficial. The formulation allows for sustained drug release, ensuring efficacy over 1 to 3 months, depending on dosage.
Uses (Indications):
Leuprosun is used in the management of several hormone-responsive conditions:
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Advanced Prostate Cancer – To reduce testosterone levels and slow cancer progression
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Endometriosis – To relieve pelvic pain and reduce endometrial lesions
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Uterine Fibroids – Often used preoperatively to shrink fibroids and reduce bleeding
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Central Precocious Puberty (CPP) – In children with early puberty
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Breast Cancer (off-label) – In premenopausal women to suppress ovarian function
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Assisted Reproductive Technology (ART) – To control ovulation timing
Storage Instructions:
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Store the lyophilized vial below 25°C (77°F)
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Protect from light and moisture
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Once reconstituted, use immediately or within 30 minutes
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Do not freeze the diluent or reconstituted solution
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Keep out of reach of children and dispose of properly after use
How It Works (Mechanism of Action):
Leuprolide Acetate is a synthetic analogue of GnRH (gonadotropin-releasing hormone). Its action occurs in two phases:
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Initial Phase (Flare Effect): Stimulates the pituitary to release LH and FSH, temporarily increasing testosterone or estrogen levels.
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Chronic Phase (Downregulation): Continuous stimulation desensitizes GnRH receptors, leading to suppression of LH and FSH, which in turn lowers sex hormone levels (testosterone in males, estrogen in females) to castrate or menopausal levels.
This hormone suppression is beneficial in hormone-sensitive diseases like prostate or breast cancer.
Side Effects:
Common Side Effects:
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Hot flashes
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Fatigue or weakness
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Injection site reactions (pain, swelling)
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Headache or dizziness
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Night sweats
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Libido changes and erectile dysfunction in men
Severe Side Effects:
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Tumor flare reaction (initial worsening of symptoms in prostate cancer)
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Depression or mood disorders
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Osteoporosis with long-term use
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QT prolongation and arrhythmias
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Seizures (rare)
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Severe allergic reactions (anaphylaxis)
Dosage (Typical Recommended Dose):
For Prostate Cancer (Advanced):
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Leuprosun 11.25 mg IM every 3 months
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Leuprosun 22.5 mg IM every 6 months
For Endometriosis / Uterine Fibroids:
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3.75 mg IM monthly or
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11.25 mg IM every 3 months for up to 6 months
For Central Precocious Puberty (CPP):
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Dose is weight-based, typically 11.25 mg every 3 months
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Adjust based on hormone levels and response
Note: Always tailor the dosage based on the indication, age, weight, and clinical response.
Method of Administration:
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Administered as a deep intramuscular injection
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Reconstitute with the provided sterile diluent immediately before use
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Inject slowly into the gluteal muscle
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Administration must be done by a qualified healthcare provider
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Observe patient briefly for hypersensitivity reactions
Precautions:
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Tumor flare risk: Use with anti-androgens in prostate cancer initially
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Monitor bone density if used long-term (risk of osteoporosis)
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Not recommended in pregnancy – may cause fetal harm
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Use non-hormonal contraception during treatment
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Monitor for psychiatric symptoms (depression, mood changes)
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In children: Periodic assessment of growth and puberty progression is needed
Drug Interactions:
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QT-prolonging agents (e.g., amiodarone, methadone) – Increased risk of arrhythmias
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Anti-diabetic drugs – Leuprolide may affect glucose tolerance
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Corticosteroids – May worsen bone loss
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Hormonal therapies – May interfere with GnRH activity
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Caution when used with CNS depressants
Allergies (Warnings for Allergic Reactions):
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Contraindicated in patients with known hypersensitivity to Leuprolide, GnRH, or its analogues
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Symptoms of allergy may include rash, itching, difficulty breathing, or facial swelling
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Anaphylactic reactions, though rare, are potentially life-threatening
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Use should be discontinued immediately in the event of a severe allergic response
Overdose Information:
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Overdose is rare due to depot nature of formulation
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Symptoms may include hormonal imbalances, prolonged suppression, or injection site complications
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No specific antidote; treatment is symptomatic and supportive
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Immediate medical attention is advised if overdose is suspected
Missed Dose Instructions:
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If a dose is missed, administer as soon as possible
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Maintain strict scheduling for depot formulations
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Do not double up doses; consult physician for guidance
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Treatment efficacy depends on regular and timely dosing
Additional Notes:
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May cause a temporary worsening of symptoms before improvement is observed
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Long-term use requires bone health monitoring and possible supplementation
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Patients should be informed about possible sexual dysfunction and mood changes
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In women, therapy can induce menopausal symptoms
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Clinical evaluations including PSA, testosterone, or estradiol levels should be regularly performed to monitor treatment response
