Leuprolide
Also known as: Eligard, Leuprolide, Leuprolide acetate, Leuprorelin, Lupron, Lupron Depot, TAP-144, Viadur
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Summary
Leuprolide acetate is a synthetic GnRH analog used to suppress sex hormone secretion in conditions such as prostate cancer, endometriosis, uterine fibroids, central precocious puberty, and for assisted reproduction protocols.
Mechanism of Action
Continuous activation of pituitary GnRH receptors causes an initial surge of LH/FSH followed by receptor down‑regulation, leading to profound suppression of gonadal steroid production.
Routes of Administration
Goals & Uses
- Central precocious puberty (CPP)Pediatric EndocrinologyHigh
- Assisted reproduction (controlled ovarian hyperstimulation)ReproductiveModerate
- Prostate cancer (hormone-sensitive, advanced)OncologyHigh
- Prostate cancerOncologyHigh
- Central precocious pubertyPediatric EndocrinologyHigh
- Uterine fibroidsGynecologyModerate
- Uterine fibroids (leiomyomata)GynecologyHigh
- Assisted reproduction (controlled ovarian stimulation)Reproductive MedicineModerate
- Gender-affirming hormone therapy (puberty suppression)EndocrinologyModerate
- EndometriosisGynecologyHigh
Contraindications
- Undiagnosed vaginal bleedingGynecologicalHigh
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
- BreastfeedingPopulationHighPotential transfer into breast milk or insufficient safety data
- Hypersensitivity to GnRH analogues or excipientsImmunologicHigh
- Spinal cord compression risk (prostate cancer)OncologyHigh
- Known hypersensitivity to leuprolide or formulation excipientsGeneralModerate
Adverse Effects
- Hot flashes / vasomotor symptomsAutonomic / ThermoregulatoryCommon
- Mood changesPsychiatricUncommon
- Testosterone/estrogen flare (initial)EndocrineCommon
- Injection site reactionsLocalCommon
- Injection site painLocalCommonPain at the injection site
- Sexual dysfunction (decreased libido, erectile dysfunction)Sexual HealthCommon
- Decreased libidoSexual / EndocrineCommon
- Hot flashesEndocrine / VasomotorCommon
- Bone mineral density loss / osteoporosisMusculoskeletalCommon
- QT/QTc prolongationCardiovascularUncommon
- Bone mineral density lossSkeletalUncommon
Drug Interactions
- CYP3A4 inhibitors (e.g., ketoconazole)Low
- Estrogen replacement therapyModerate
- Antidiabetic agents (insulin, sulfonylureas)Moderate
- QT-prolonging agents (e.g., antiarrhythmics, antipsychotics)High
- Anticoagulants (warfarin)Moderate
Population Constraints
- Elderly patients with osteoporosisComorbidityRelative
- Pediatric patients (outside CPP indication)AgeRelative
- Patients with osteoporosis or high fracture riskMusculoskeletalRelative
- Patients with pre-existing cardiovascular diseaseCardiovascularRelative
- Patients with depression or psychiatric disordersPsychiatricRelative
- Pediatric patients <2 yearsAgeRelative
Regulatory Status
- European UnionApprovedApproved: Prostate cancer, Endometriosis, Uterine fibroids, Central precocious pubertyEMA‑approved; marketed under multiple brand names.
- United StatesApprovedApproved: Prostate cancer, Endometriosis, Uterine fibroids, Central precocious puberty, Assisted reproductionFDA‑approved; prescription only.
- United KingdomApprovedApproved: Prostate cancer, Endometriosis, Uterine fibroids, Central precocious pubertyMHRA‑approved; prescription required.
Approved by FDA (US), EMA (EU) and MHRA (UK) for multiple endocrine‑related indications.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Leuprolide?
Leuprolide acetate is a synthetic GnRH analog used to suppress sex hormone secretion in conditions such as prostate cancer, endometriosis, uterine fibroids, central precocious puberty, and for assisted reproduction protocols.
What is Leuprolide used for?
Leuprolide is educationally associated with: Central precocious puberty (CPP), Assisted reproduction (controlled ovarian hyperstimulation), Prostate cancer (hormone-sensitive, advanced), Prostate cancer, Central precocious puberty, Uterine fibroids, Uterine fibroids (leiomyomata), Assisted reproduction (controlled ovarian stimulation), Gender-affirming hormone therapy (puberty suppression), Endometriosis. Educational only — not medical advice.
How is Leuprolide administered?
Recorded routes of administration: Intramuscular, Subcutaneous, Subcutaneous Implant.
What are the potential side effects of Leuprolide?
Reported adverse effects include: Hot flashes / vasomotor symptoms, Mood changes, Testosterone/estrogen flare (initial), Injection site reactions, Injection site pain, Sexual dysfunction (decreased libido, erectile dysfunction), Decreased libido, Hot flashes, Bone mineral density loss / osteoporosis, QT/QTc prolongation, Bone mineral density loss. This list is not exhaustive — consult a qualified clinician.
Who should avoid Leuprolide?
Recorded contraindications: Undiagnosed vaginal bleeding, Pregnancy, Breastfeeding, Hypersensitivity to GnRH analogues or excipients, Spinal cord compression risk (prostate cancer), Known hypersensitivity to leuprolide or formulation excipients. Consult a qualified clinician before use.