Leuprolide Acetate

A to Z Drug Facts

Actions A synthetic luteinizing hormone-releasing hormone (LHRH) agonist of greater potency than naturally occurring gonadotropin-releasing hormone (GnRH). Occupies pituitary GnRH receptors and thus desensitizes them, inhibiting gonadotropin secretion required for gonadal production of testosterone and estrogen.

 Indications Palliative treatment of advanced prostatic cancer (alone or in combination with flutamide); management of endometriosis in women > 18 yr (depot preparation); treatment of children with central precocious puberty (CPP [pediatric injection or depot pediatric]); uterine leiomyomata (depot preparation).

Breast and ovarian carcinoma.

 Contraindications Pregnancy; lactation; hypersensitivity to GnRH, GnRH agonist analogs, or product components; undiagnosed vaginal bleeding.

 Route/Dosage

Advanced Prostate Cancer

ADULTS: SC 1 mg/day. IM 7.5 mg q mo (depot preparation).

Central Precocious Puberty (CPP)

ADULTS: SC Starting dose: 50 mcg/kg/day as single injection. Individualize dosage and titrate to response.

ADULTS: IM Starting dose: 0.3 mg/kg q 4 wk (min 7.5 mg) as single injection (depot preparation). Must be administered by health care provider or designated health care provider.

Endometriosis

ADULTS: IM 3.75 mg as single monthly injection or 11.25 mg IM q 3 mo (depot preparation).

Uterine Leiomyomata

ADULTS: IM 3.75 mg as a single monthly injection or 11.25 mg IM q 3 mo.

Interactions None well documented.

Lab Test Interferences Diagnostic tests of pituitary gonadotropic and gonadal functions during treatment and up to 12 wk after discontinuing depot preparation may be misleading.

 Adverse Reactions

CARDIOVASCULAR: Arrhythmias; edema; angina or hypertension rarely. CNS: Mental depression; headache; decreased libido. DERMATOLOGIC: Erythema; ecchymosis; irritation at injection site; acne. ENDOCRINE: Hot flashes; gynecomastia. GU: Vaginitis; vaginal dryness; impotence; testicular atrophy; amenorrhea; infertility. MUSCULOSKELETAL: Decreased bone density; symptom flare, manifested by increased bone pain during first 1 to 2 wk of therapy in patients with bone metastases.

 Precautions

Pregnancy: Category X. Use a nonhormonal method of contraception. Lactation: Undetermined. Children: Safety and efficacy of injection not established; recommended depot preparation for CPP. Bone density changes: Use of depot preparation may result in decreased bone density. Decreased bone mineral content risk factors may cause additional bone loss with long-term use. Hypersensitivity: Injection contains benzyl alcohol, which can cause local hypersensitivity reactions. Depot preparation is preservative-free.

 Administration/Storage

• Use syringes included in the kit or low-dose insulin syringes (SC). Do not use needles smaller than 22-gauge (IM). Rotate injection sites.
• Reconstitute depot form only with diluent provided. Reconstituted suspension will appear milky. Suspension is stable for 24 hr after reconstitution.
• Store unreconstituted depot form at room temperature.
• Refrigerate injection (nondepot form) until used for first dose. May then be stored at room temperature until contents of vial have been administered. Protect from light.
• Store implant at room temperature.

 Assessment/Interventions

• Obtain patient history, including drug history and any known allergies.
• Ensure that baseline laboratory tests (eg, testosterone, acid phosphase) have been obtained before beginning therapy and monitor periodically thereafter.
• Monitor I&O carefully and assess for bladder distention with prostate cancer. Transient exacerbation of symptoms (eg, urinary obstruction, hematuria) occurs in many patients during first week of therapy.

 Patient/Family Education

• Caution patient that depot preparation must not be taken during pregnancy or when pregnancy is possible. Advise patient to use reliable form of birth control while taking this drug.
• Advise patient/family to follow prescribed regimen. Do not alter dose or discontinue therapy without consulting health care provider.
• Instruct patient on proper injection technique and have patient perform return demonstration.
• Advise patient to use nonhormonal forms of birth control because menstrual irregularities may occur.
• Inform patient that burning, itching, or swelling may develop at injection site, and to notify health care provider if these symptoms worsen.
• Advise patient that increased bone pain and difficulty urinating may occur in early treatment of prostate cancer.
• With patients receiving drug for CPP, inform family that menses or spotting may occur initially but to notify health care provider if symptoms continue beyond second month.
• Inform patients receiving drug for endometriosis/uterine leiomyomata that menstruation should stop and to notify health care provider if it persists.

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Copyright © 2003 Facts and Comparisons
David S. Tatro
A to Z Drug Facts