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leuprolide acetate (leuprorelin (UK))
Pharmacologic class: Gonadotropin-releasing hormone (GnRH) analog
Therapeutic class: Antineoplastic
Pregnancy risk category X
Inhibits and desensitizes GnRH receptors, thus inhibiting gonadotropin secretion when given continuously. This inhibition causes initial increase and then profound decrease in luteinizing hormone and follicle-stimulating hormone levels and, ultimately, reduces testosterone and estrogen sex hormones.
Eligard Depot: 7.5 mg, 22.5 mg, 30 mg, 45 mg
Injection: 1 mg/0.2 ml
Lupron Depot injection: 3.75 mg/ml, 7.5 mg/ml
Lupron Depot-3 month injection: 11.25 mg, 22.5 mg
Lupron Depot-4 month injection: 30 mg
Lupron Depot-Ped injection: 7.5 mg, 11.25 mg, 15 mg
Indications and dosages
➣ Advanced prostate cancer
Adults: 1 mg subcutaneously daily (1 mg/0.2-ml formulation). For Lupron Depot formulation, 7.5 mg I.M. monthly, 22.5 mg I.M. q 3 months, or 30 mg I.M. q 4 months. For Eligard formulation, 7.5 mg subcutaneously monthly, 22.5 mg subcutaneously q 3 months, 30 mg subcutaneously q 4 months, or 45 mg subcutaneously q 6 months.
Adults: 3.75 mg I.M. (depot injection) as a single injection once monthly, or 11.25 mg I.M. q 3 months. Duration is up to 6 months.
➣ Adjunct to iron therapy in anemia caused by uterine leiomyomas
Adults: 3.75 mg I.M. monthly or 11.25 mg I.M. q 3 months as a single dose. Recommended duration is 6 months or less.
➣ Central precocious puberty
Children: 50 mcg/kg/day subcutaneously as a single injection, increased in increments of 10 mcg/kg/day as needed
Children weighing more than 37.5 kg (82.5 lb): Initially, 15 mg of Depot-Ped I.M. q 4 weeks, increased in increments of 3.75 mg q 4 weeks as needed
Children weighing 25 to 37.5 kg (55 to 82.5 lb): Initially, 11.25 mg of Depot-Ped I.M. q 4 weeks, increased in increments of 3.75 mg q 4 weeks as needed
Children weighing less than 25 kg (55 lb): Initially, 7.5 mg of Depot-Ped I.M. q 4 weeks, increased in increments of 3.75 mg q 4 weeks as needed
• Hypersensitivity to drug, its components, GnRH, or other GnRH analogs
• Undiagnosed abnormal vaginal bleeding
• Pregnancy or breastfeeding
Use cautiously in:
• renal, hepatic, or cardiac impairment.
• Give Eligard within 30 minutes of mixing. After this time, discard.
• Administer Lupron injection immediately after mixing. Otherwise, discard.
• Administer Lupron Depot-Ped only under prescriber's supervision.
CNS: anxiety, depression, dizziness, drowsiness, asthenia, fatigue, headache, vertigo, syncope, mood changes
CV: palpitations, angina, arrhythmias, myocardial infarction
EENT: blurred vision
GI: nausea, vomiting, diarrhea, constipation, abdominal pain, dyspepsia, anorexia
GU: urinary frequency, hematuria, decreased testes size, erectile dysfunction, decreased libido, gynecomastia
Hematologic: anemia, thrombocytopenia
Respiratory: dyspnea, pleural rub, worsening of pulmonary fibrosis, pulmonary embolism
Skin: alopecia, pruritus, rash, diaphoresis
Other: sour taste, edema, hot flashes, anaphylaxis
Drug-diagnostic tests. Blood urea nitrogen, creatinine: increased levels
Pituitary-gonadal system tests: misleading results during and for up to 3 months after therapy
• Observe injection site for local reactions.
☞ Monitor cardiovascular and respiratory status carefully to detect serious adverse reactions.
• Evaluate neurologic status. Institute safety measures as needed to prevent injury.
• Periodically monitor serum testosterone and prostate-specific antigen levels.
• Inform patient that localized reaction may occur at injection site. Tell him to contact prescriber if symptoms don't resolve.
• Advise patient and family to watch for and report signs or symptoms of depression.
• Tell patient drug may cause libido changes or erectile dysfunction. Encourage him to discuss these problems with prescriber.
• Teach patient to minimize GI upset by eating small, frequent servings of food and drinking plenty of fluids.
☞ Instruct female of childbearing age to use reliable contraception during therapy. Tell her to stop drug immediately and contact prescriber if she suspects pregnancy.
☞ Tell female patient not to breastfeed.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the tests mentioned above.