LEUPROLIDE ACETATE

(loo-proe'lide)

Eligard, Lupron, Lupron Depot, Lupron Depot-Ped, Viadur
Classifications: gonadotropin-releasing hormone (gnrh) analog;
Therapeutic:gnrh analog
Pregnancy Category: X

Availability

5 mg/mL injection; 3.75 mg, 7.5 mg, 11.25 mg, 15 mg, 22.5 mg, 30 mg microspheres for injection (depot formulations); 65 mg implant

Action

Occupies and desensitizes pituitary GnRH receptors, resulting initially in release of gonadotropins LH and FSH and stimulation of ovarian and testicular steroidogenesis.

Therapeutic Effect

Long-term administration suppresses both gonadotropin secretion and steroidogenesis and leads to prostatic and testicular atrophy. Antitumor effect: May inhibit growth of hormone-dependent tumors as indicated by reduction in concentrations of PSA and serum testosterone to levels equal to or less than pretreatment levels. Contraceptive effect: By inhibiting gonadotropin release, ovulation or spermatogenesis is suppressed. Has antitumor effect in males, and contraceptive effects in both males and females.

Uses

Palliative treatment of advanced prostatic carcinoma as alternative to orchiectomy or estrogen administration; endometriosis; anemia caused by leiomyomata.

Unlabeled Uses

Breast cancer; male contraceptive; delayed puberty.

Contraindications

Known hypersensitivity to benzyl alcohol, GnRH analog hypersensitivity; following orchiectomy or estrogen therapy; metastatic cerebral lesions; menstruation, abnormal vaginal bleeding, pregnancy (category X), lactation.

Cautious Use

Life-threatening carcinoma in which rapid symptomatic relief is necessary; osteoporosis; elderly.

Route & Dosage

Palliative Treatment for Prostate Cancer
Adult: SC 1 mg/d IM 7.5 mg/mo or 22.5 mg q3mo or 30 mg q4mo (depot preparation) Implant One implant q12mo

Endometriosis, Anemia
Adult: IM 3.75 mg qmo or 11.25 mg q3mo

Precocious Puberty
Child: IM Depot-Ped, 0.15–0.3 mg/kg q28d (min: 7.5 mg), titrate by 3.75-mg increments q4wk

Administration

Subcutaneous

Do not use Depot-Ped form for SC injection.
Rotate injection sites.

Intramuscular

Prepare solution for Depot-Ped injection using a 22-gauge needle (or syringe provided by manufacturer), withdraw 1.5 mL of diluent from the supplied ampule and inject it into the vial. Shake well to form a uniform suspension. Withdraw entire contents and administer immediately.
Do not administer parenteral drug formulation if particulate matter or discoloration is present.
Refrigerate unopened vials. Store vial in use at room temperature for several months with minimal loss of potency. Protect from light and freezing.

Adverse Effects (≥1%)

Body as a Whole: Disease flare (worsening of S&S of carcinoma), injection site irritation, asthenia, fatigue, fever, facial swelling. CNS: Dizziness, pain, headache, paresthesia. CV: Peripheral edema, cardiac arrhythmias, MI. Endocrine: Hot flushes, impotence, decreased libido, gynecomastia, breast tenderness, amenorrhea, vaginal bleeding, thyroid enlargement, hypoglycemia. GI: Nausea, vomiting, constipation, anorexia, sour taste, GI bleeding, diarrhea. Musculoskeletal: Increased bone pain, myalgia. Renal: Increased hematuria, dysuria, flank pain. Respiratory: Pleural rub, pulmonary fibrosis flare. Hematologic: Decreased Hct, Hgb. Skin: Pruritus, rash, hair loss.

Interactions

Drug: androgens, estrogens would counteract therapeutic effects.

Pharmacokinetics

Absorption: Readily absorbed from SC or IM sites. Metabolism: By enzymes in hypothalamus and anterior pituitary. Half-Life: 3 h.

Nursing Implications

Assessment & Drug Effects

Monitor PSA and testosterone levels in males with prostate cancer. A gradual rise in values after their decrease may signify treatment failure.
Inspect injection site. If local hypersensitivity reactions occur (erythema, induration), suspect sensitivity to benzyl alcohol. Report to physician.
Monitor I&O ratio and pattern. Report hematuria and decreased output. Carefully monitor voiding problems.

Patient & Family Education

When used for prostate cancer, bone pain and voiding problems (i.e., symptoms of tumor obstruction) usually increase during first several weeks of continuous treatment but are transient. Hot flushes also may be experienced.
Notify physician of neurologic S&S (paresthesia and weakness in lower limbs). Exercise caution when walking without assistance.
When used for endometriosis, continuous treatment may cause amenorrhea and other menstrual irregularities.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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