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Pronunciation:

(loo PROE lide)

U.S. Brand Names:

Eligard®; Lupron®; Lupron Depot®; Lupron Depot-Ped®; Viadur®

Synonyms:

Abbott-43818; Leuprolide Acetate; Leuprorelin Acetate; NSC-377526; TAP-144

Generic Available:

Yes: Injection (solution)

Canadian Brand Names:

Lupron®; Lupron® Depot®; Viadur®

Use:

Palliative treatment of advanced prostate carcinoma; management of endometriosis as initial treatment and/or treatment of recurrent symptoms; preoperative treatment of anemia caused by uterine leiomyomata (fibroids); central precocious puberty

Use - Unlabeled/Investigational:

Treatment of breast, ovarian, and endometrial cancer; infertility; prostatic hyperplasia

Pregnancy Risk Factor:

Pregnancy Implications:

Pregnancy must be excluded prior to the start of treatment. Although leuprolide usually inhibits ovulation and stops menstruation, contraception is not ensured and a nonhormonal contraceptive should be used. Fetal abnormalities and increased fetal mortality have been noted in animal studies.

Lactation:

Excretion in breast milk unknown/contraindicated

Contraindications:

Hypersensitivity to leuprolide, GnRH, GnRH-agonist analogs, or any component of the formulation; spinal cord compression (orchiectomy suggested); undiagnosed abnormal vaginal bleeding; pregnancy; breast-feeding

Warnings/Precautions:

Transient increases in testosterone serum levels occur at the start of treatment. Tumor flare, bone pain, urinary tract obstruction or spinal cord compression have been reported when used for prostate cancer; closely observe patients for weakness, paresthesias, and urinary tract obstruction in first few weeks of therapy. Observe patients with metastatic vertebral lesions or urinary obstruction closely. Exacerbation of endometriosis or uterine leiomyomata may occur initially. Decreased bone density has been reported when used for 6 months. Use caution in patients with a history of psychiatric illness; alteration in mood, memory impairment, and depression have been associated with use.

Adverse Reactions:

Children:

1% to 10%

Central nervous system: Pain (2%)

Dermatologic: Acne (2%), rash (2%), seborrhea (2%)

Genitourinary: Vaginitis (2%), vaginal bleeding (2%), vaginal discharge (2%)

Local: Injection site reaction (5%)

<1%: Alopecia, cervix disorder, dysphagia, emotional lability, epistaxis, fever, gingivitis, gynecomastia, headache, nausea, nervousness, peripheral edema, personality disorder, sexual maturity accelerated, skin striae, somnolence, syncope, urinary incontinence, vasodilation, vomiting, weight gain

Adults (frequency dependent upon formulation and indication):

Cardiovascular: Angina, atrial fibrillation, CHF, deep vein thrombosis, edema, hot flashes, hypertension, MI, tachycardia

Central nervous system: Abnormal thinking, agitation, amnesia, confusion, convulsion, dementia, depression, dizziness, fever, headache, insomnia, pain, vertigo

Dermatologic: Alopecia, bruising, cellulitis

Endocrine & metabolic: Breast enlargement, breast tenderness, dehydration, hyperglycemia, hyperlipidemia, hyperphosphatemia, libido decreased, menstrual disorders, potassium decreased

Gastrointestinal: Anorexia, appetite increased, diarrhea, dysphagia, eructation, GI hemorrhage, gingivitis, gum hemorrhage, intestinal obstruction, nausea, peptic ulcer

Genitourinary: Balanitis, impotence, testicular atrophy, urinary disorder, vaginitis

Hematologic: Platelets decreased, PT prolonged, WBC increased

Hepatic: Hepatomegaly, liver function tests abnormal

Local: Abscess, injection site reaction

Neuromuscular & skeletal: Leg cramps, myalgia, paresthesia, weakness

Renal: BUN increased

Respiratory: Allergic reaction, emphysema, hemoptysis, hypoxia, lung edema, pulmonary embolism

Miscellaneous: Body odor, flu-like syndrome, neoplasm, voice alteration

Children and Adults: Postmarketing/case reports: Anaphylactic reactions, asthmatic reactions, bone density decreased; fibromyalgia-like symptoms (arthralgia/myalgia, headaches, GI distress); hypotension, induration at the injection site, peripheral neuropathy, photosensitivity, prostate pain, rash, spinal fracture/paralysis, tenosynovitis-like symptoms, urticaria, WBC decreased

Overdosage/Toxicology:

Treatment is supportive.

Stability:

Lupron®: Store unopened vials of injection in refrigerator, vial in use can be kept at room temperature of 30°C (86°F) for several months with minimal loss of potency. Protect from light and store vial in carton until use. Do not freeze.

Eligard®: Store at 2°C to 8°C (36°F to 46°C). Allow to reach room temperature prior to using; once mixed, must be administered within 30 minutes.

Lupron Depot® may be stored at room temperature of 25°C, excursions permitted to 15°C to 30°C (59°F to 86°F). Upon reconstitution, the suspension does not contain a preservative and should be used immediately.

Viadur® may be stored at room temperature of 15°C to 30°C (59°F and 86°F).

Mechanism of Action:

Potent inhibitor of gonadotropin secretion; continuous daily administration results in suppression of ovarian and testicular steroidogenesis due to decreased levels of LH and FSH with subsequent decrease in testosterone (male) and estrogen (female) levels. Leuprolide may also have a direct inhibitory effect on the testes, and act by a different mechanism not directly related to reduction in serum testosterone.

Pharmacodynamics/Kinetics:

Onset of action: Following transient increase, testosterone suppression occurs in ~2-4 weeks of continued therapy

Distribution: Males: Vd: 27 L

Protein binding: 43% to 49%

Metabolism: Not well defined; forms smaller, inactive peptides and metabolites

Bioavailability: Oral: None; SubQ: 94%

Half-life elimination: 3 hours

Excretion: Urine (<5% as parent and major metabolite)

Dosage:

Children: Precocious puberty (consider discontinuing by age 11 for females and by age 12 for males):

SubQ (Lupron®): 20-45 mcg/kg/day; titrate dose upward by 10 mcg/kg/day if down-regulation is not achieved

I.M. (Lupron Depot-Ped®): 0.3 mg/kg/dose given every 28 days (minimum dose: 7.5 mg)

25 kg: 7.5 mg

>25-37.5 kg: 11.25 mg

>37.5 kg: 15 mg

Titrate dose upward in 3.75 mg every 4 weeks if down-regulation is not achieved.

Adults:

Advanced prostatic carcinoma:

SubQ:

Eligard®: 7.5 mg monthly or 22.5 mg every 3 months or 30 mg every 4 months

Lupron®: 1 mg/day

Viadur®: 65 mg implanted subcutaneously every 12 months

I.M.:

Lupron Depot®: 7.5 mg/dose given monthly (every 28-33 days) or

Lupron Depot-3®: 22.5 mg every 3 months or

Lupron Depot-4®: 30 mg every 4 months

Endometriosis: I.M.: Initial therapy may be with leuprolide alone or in combination with norethindrone; if retreatment for an additional 6 months is necessary, norethindrone should be used. Retreatment is not recommended for longer than one additional 6-month course.

Lupron Depot®: 3.75 mg/month for up to 6 months or

Lupron Depot-3®: 11.25 mg every 3 months for up to 2 doses (6 months total duration of treatment)

Uterine leiomyomata (fibroids): I.M. (in combination with iron):

Lupron Depot®: 3.75 mg/month for up to 3 months or

Lupron Depot-3®: 11.25 mg as a single injection

Administration:

Eligard®: Packaged in two syringes; one contains the Atrigel® polymer system, and the second contains leuprolide acetate powder; follow instructions for mixing; must be administered within 30 minutes of mixing

Lupron Depot®: Do not use needles smaller than 22 gauge; reconstitute only with diluent provided

Viadur® implant: Requires surgical implantation and removal at 12-month intervals

Monitoring Parameters:

Bone mineral density

Precocious puberty: GnRH testing (blood LH and FSH levels), measurement of bone age every 6-12 months, testosterone in males and estradiol in females; Tanner staging

Prostatic cancer: LH and FSH levels, serum testosterone (2-4 weeks after initiation of therapy), PSA; weakness, paresthesias, and urinary tract obstruction in first few weeks of therapy

Test Interactions:

Interferes with pituitary gonadotropic and gonadal function tests during and up to 3 months after therapy

Patient Education:

Use as directed. Do not discontinue without consulting prescriber. You may experience disease flare (increased bone pain) and urinary retention during early treatment (usually resolves); dizziness, headache, lethargy, or faintness (use caution when driving or engaging in tasks that require alertness until response to drug is known); nausea or vomiting (small, frequent meals or analgesics may help); hot flashes, flushing, or redness (cold clothes and cool environment may help); breast swelling or tenderness; or decreased libido. Report irregular or rapid heartbeat, palpitations, chest pain; inability to void or changes in urinary pattern; unresolved nausea or vomiting; numbness of extremities; breast swelling or pain, respiratory difficulty, or redness, swelling or pain at injection sites. Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Do not get pregnant. Consult prescriber for appropriate barrier contraceptive use during and for a time following therapy. Do not breast-feed.

Additional Information:

Eligard® Atrigel®: A nongelatin-based, biodegradable, polymer matrix

Viadur®: Leuprolide acetate implant containing 72 mg of leuprolide acetate, equivalent to 65 mg leuprolide free base. One Viadur® implant delivers 120 mcg of leuprolide/day over 12 months.

Anesthesia and Critical Care Concerns/Other Considerations:

Eligard® is a nongelatin-based, biodegradable, polymer matrix.

Viadur® is a leuprolide acetate implant containing 72 mg of leuprolide acetate, equivalent to 65 mg leuprolide free base. One Viadur® implant delivers 120 mcg of leuprolide/day over 12 months.

Dental Health: Effects on Dental Treatment:

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

No information available to require special precautions

Mental Health: Effects on Mental Status:

Depression is common; may cause drowsiness, dizziness, or insomnia

Mental Health: Effects on Psychiatric Treatment:

None reported

Oncology: Emetic Potential:

Very low (<10%)

Oncology: Vesicant:

Dosage Forms:

Implant (Viadur®): 65 mg [released over 12 months; packaged with administration kit]

Injection, solution, as acetate (Lupron®): 5 mg/mL (2.8 mL) [contains benzyl alcohol; packaged with syringes and alcohol swabs]

Injection, powder for reconstitution, as acetate [depot formulation; prefilled syringe]:

Eligard®:

7.5 mg [released over 1 month]

22.5 mg [released over 3 months]

30 mg [released over 4 months]

Lupron Depot®: 3.75 mg, 7.5 mg [released over 1 month; contains polysorbate 80]

Lupron Depot®-3 Month: 11.25 mg, 22.5 mg [released over 3 months; contains polysorbate 80]

Lupron Depot®-4 Month: 30 mg [released over 4 months; contains polysorbate 80]

Lupron Depot-Ped®: 7.5 mg, 11.25 mg, 15 mg [released over 1 month; contains polysorbate 80]

International Brand Names:

Lupron® (CA); Lupron® Depot® (CA); Viadur® (CA)

References

Adjei AL and Hsu L, "Leuprolide and Other LH-RH Analogues,"Pharm Biotechnol, 1993, 5:159-99.

Chrisp P and Sorkin EM, "Leuprorelin. A Review of Its Pharmacology and Therapeutic Use in Prostatic Disorders,"Drugs Aging, 1991, 1(6):487-509.

Crawford ED, Eisenberger MA, McLeod DG, et al, "A Controlled Trial of Leuprolide With and Without Flutamide in Prostatic Carcinoma,"N Engl J Med, 1989, 321(7):419-24.

Kappy MS, Stuart T, and Perelman A, "Efficacy of Leuprolide Therapy in Children With Central Precocious Puberty,"Am J Dis Child, 1988, 142(10):1061-4.

Kavanagh JJ, Roberts W, Townsend P, et al, "Leuprolide Acetate in the Treatment of Refractory or Persistent Epithelial Ovarian Cancer,"J Clin Oncol, 1989, 7(1):115-8.

Lee PA and Page JG, "Effects of Leuprolide in the Treatment of Central Precocious Puberty,"J Pediatr, 1989, 114(2):321-4.

Plosker GL and Brogden RN, "Leuprorelin. A Review of Its Pharmacology and Therapeutic Use in Prostate Cancer, Endometriosis and Other Sex Hormone-Related Disorders,"Drugs, 1994, 48(6):930-67.

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