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Leuprolide acetate
Leuprolide acetate (Lupron)
Leuprolide acetate
(loo-PROH-lyd)
Pregnancy Category: X Lupron Lupron/Lupron Depot Lupron/Lupron Depot 7.5 mg/22.5 mg Lupron Depot 3.75 mg Lupron Depot Lupron Depot--3 Month Lupron Depot--4 Month Lupron Depot-Ped Lupron for Pediatric Use (Rx)

Classification: Antineoplastic agent, hormonal

See Also: See also Antineoplastic Agents.

Action/Kinetics: Related to the naturally occurring GnRH. By desensitizing GnRH receptors, gonadotropin secretion is inhibited. Initially, however, LH and FSH levels increase, leading to increases of sex hormones. However, decreases in these hormones will be observed within 2-4 weeks. Peak plasma levels: 4 hr for various doses. t1/2: 3 hr. Chronic use results in a measureable increase in body length, return to prepubertal state of reproductive organs, and cessation of menses (if present).

Uses: Palliative treatment in advanced prostatic cancer when orchiectomy or estrogen treatment are not appropriate. Endometriosis (use depot form). Central precocious puberty (use depot-PED form). In combination with iron supplements for the presurgical treatment of anemia caused by uterine fibroid tumors (use depot form). Investigational: With flutamide for metastatic prostatic cancer.

Contraindications: Pregnancy, in women who may become pregnant while receiving the drug, and during lactation. Sensitivity to benzyl alcohol (found in leuprolide injection). Undiagnosed abnormal vaginal bleeding. Hypersensitivity to GnRH or GnRH agonist analogs. The 30-mg depot in women.

Special Concerns: Safety and efficacy have not been determined in children (except depot-PED). May cause increased bone pain and difficulty in urination during the first few weeks of therapy for prostatic cancer.

Side Effects: Injection and Depot. GI: N&V;, anorexia, diarrhea, constipation, taste disorders/perversion, gingivitis, dysphagia, hepatic dysfunction. CNS: Pain, depression, emotional lability, insomnia, headache, dizziness, nervousness, paresthesias, anxiety, memory disorder, syncope, personality disorder, somnolence, spinal fracture/paralysis. CV: Peripheral edema, angina, cardiac arrhythmias, TIA/stroke hypotension, vasodilation. GU: Hematuria, urinary frequency or urgency, dysuria, testicular pain, incontinence, cervix disorder, penile swelling, prostate pain. Respiratory: Dyspnea, hemoptysis, pneumonia, epistaxis, pulmonary infiltrates. Endocrine: Gynecomastia, breast tenderness, impotency, hot flashes, sweating, decreased testicular size, increased or decreased libido. Musculoskeletal: Myalgia, bone pain, pelvic fibrosis, ankylosing spondylosis. Dermatologic: Dermatitis, skin reactions, acne, seborrhea, hair growth, ecchymosis, hair loss, skin striae, erythema multiforme and other rashes, androgen-like effects. Ophthalmic: Ophthalmic disorder, abnormal vision. Other: Asthenia, diabetes, fever, chills, tinnitus, infection, body odor, hard nodule in throat, accelerated sexual maturation, hearing disorder, peripheral neuropathy.
Injection. CV: MI, pulmonary emboli. GI: GI bleeding rectal polyps, peptic ulcer. CNS: Lethargy, mood swings, numbness, blackouts, fatigue. Respiratory: Cough, pulmonary fibrosis pleural rub. Dermatologic: Carcinoma of the skin/ear, itching, dry skin, pigmentation, skin lesions. GU: Bladder spasms, urinary obstruction. Miscellaneous: Enlarged thyroid, inflammation, temporal bone swelling, blurred vision.

Laboratory Test Alterations: Injection and Depot. Calcium. WBC. Hypoproteinemia. Injection: BUN, creatinine. Depot: LDH, alkaline phosphatase, AST, uric acid, cholesterol, LDL, triglycerides, PT, PTT, glucose, WBC. Platelets, potassium. Hyperphosphatemia, abnormal LFTs. Misleading results from tests of pituitary gonadotropic and gonadal function up to 4-8 weeks after discontinuing depot therapy.

How Supplied: Injection: 5 mg/mL; Kit: 5 mg/mL, 7.5 mg, 11.25 mg, 15 mg, 22.5 mg; Powder for injection: 3.75 mg, 7.5 mg. 11.5 mg, 15 mg, 30 mg

Dosage
•Depot, Injection Advanced prostatic cancer.
Injection: 1 mg/day SC using the syringes provided. Depot (IM): 7.5 mg monthly, 22.5 mg q 3 months, or 30 mg q 4 months.
Central precocious puberty.
Injection: Initial: 50 mcg/kg/day SC as a single dose. Dose may increased by 10 mcg/kg/day, which is the maintenance dose. Depot-Ped: Initial: 0.3 mg/kg/4 weeks (minimum 7.5 mg) as a single IM dose.
Endometriosis, uterine fibroids.
3.75 mg IM once a month for at least 6 months for endometriosis and 3 months or less for uterine fibroids. If further treatment is contemplated, assess bone density prior to beginning therapy.