| LEUPROLIDE ACETATE
Eligard, Lupron, Lupron Depot, Lupron Depot-Ped, Viadur
Classifications: gonadotropin-releasing hormone (gnrh) analog; Therapeutic:gnrh analog
Pregnancy Category: X
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
Occupies and desensitizes pituitary GnRH receptors, resulting initially in release of gonadotropins LH and FSH and stimulation
of ovarian and testicular steroidogenesis.
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.
Palliative treatment of advanced prostatic carcinoma as alternative to orchiectomy or estrogen administration; endometriosis;
anemia caused by leiomyomata.
Breast cancer; male contraceptive; delayed puberty.
Known hypersensitivity to benzyl alcohol, GnRH analog hypersensitivity; following orchiectomy or estrogen therapy; metastatic
cerebral lesions; menstruation, abnormal vaginal bleeding, pregnancy (category X), lactation.
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
Adult: IM 3.75 mg qmo or 11.25 mg q3mo
Child: IM Depot-Ped, 0.150.3 mg/kg q28d (min: 7.5 mg), titrate by 3.75-mg increments q4wk
- Do not use Depot-Ped form for SC injection.
- Rotate injection sites.
- 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
Nausea, vomiting, constipation
, anorexia, sour taste, GI bleeding, diarrhea
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.
would counteract therapeutic effects.
Readily absorbed from SC or IM sites. Metabolism:
By enzymes in hypothalamus and anterior pituitary. Half-Life:
Assessment & Drug Effects
- Monitor PSA and testosterone levels in males with prostate cancer. A gradual rise in values after their decrease may signify
- 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.