Leuprolide

FDA label

Read the full label on DailyMed ↗

Renal Undefined

Hepatic Undefined

These formulations are not indicated in children (see LUPRON DEPOT-PED labeling).

Instructions

• Must be administered by a healthcare provider.
• Strengths are not additive; select by desired dosing schedule. No fractional doses or combinations of doses of this or any depot formulation.
• Reconstitute prefilled dual-chamber syringe; give as a single IM injection (gluteal, anterior thigh, or deltoid); alternate sites.
• No preservative: inject immediately or discard if not used within two hours. Do not use if clumping/caking or powder not in suspension.
• Treatment is usually continued upon development of non-metastatic and metastatic castration-resistant prostate cancer.

Available strengths

• inj 3.75, 7.5, 11.25, 15, 21, 22.5, 30, 42, 45 mg

Contraindications

• Known hypersensitivity to GnRH, GnRH agonists or any excipient (anaphylactic reactions to GnRH agonists reported)

Cautions

• Tumor flare: testosterone ~50% above baseline in first weeks (bone pain, neuropathy, hematuria, urinary obstruction, spinal cord compression)
• Metabolic syndrome (hyperglycemia/diabetes, hyperlipidemia, NAFLD)
• Cardiovascular disease (MI, sudden cardiac death, stroke)
• QT/QTc prolongation
• Convulsions
• Severe cutaneous adverse reactions (SJS/TEN, DRESS, AGEP)
• Laboratory tests: monitor serum testosterone (castrate < 50 ng/dL)
• Embryo-fetal toxicity

Adverse reactions

• Hot flashes/sweats
• General pain
• Injection site reaction/pain
• GI disorders
• Urinary disorders
• Edema
• Respiratory disorder
• Upper respiratory infection
• Joint disorders
• Testicular atrophy
• Asthenia/fatigue
• Headache

Pregnancy May cause fetal harm (animal data and mechanism of action); no data in pregnant women. Safety/efficacy not established in females.

Lactation No information on presence in human milk or effects on breastfed child; safety/efficacy not established in females — discontinue breastfeeding or the drug.