leuprorelin

Action

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.

Availability

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.

➣ Endometriosis

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

Contraindications

• Hypersensitivity to drug, its components, GnRH, or other GnRH analogs

• Undiagnosed abnormal vaginal bleeding

• Pregnancy or breastfeeding

Precautions

Use cautiously in:

• renal, hepatic, or cardiac impairment.

Administration

• 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.

Adverse reactions

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

Interactions

Drug-diagnostic tests. Blood urea nitrogen, creatinine: increased levels

Pituitary-gonadal system tests: misleading results during and for up to 3 months after therapy

Patient monitoring

• 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.

Patient teaching

• 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.