leuprolide (Rx)

Brand and Other Names:Lupron, Lupron Depot, more...Lupron Depot 3 Month, Lupron Depot 4 Month, Lupron Depot 6 Month, Lupron Depot-Ped, Eligard
  • Print

Dosing & Uses


Dosage Forms & Strengths


  • 7.5mg (monthly)
  • 22.5mg (3 months)
  • 30mg (4 months)
  • 45mg (6 months)

Lupron Depot

  • 3.75mg (monthly)
  • 7.5mg (monthly)
  • 11.25mg (3 months)
  • 22.5mg (3 months)
  • 30mg (4 months)
  • 45mg (6 months)

Leuprolide acetate

  • 5mg/mL

Advanced Prostate Cancer

Lupron: 7.5 mg IM monthly, 22.5 mg IM every 3 months, 30 mg IM every 4 months, or 45 mg IM every 6 months

Eligard: 7.5 mg SC monthly, 22.5 mg SC every 3 months, 30 mg SC every 4 months, 45 mg SC every 6 months

Leuprolide acetate: 1 mg/0.2 mL/day SC


  • Measure prostate-specific antigen (PSA) in first few weeks of therapy; measure luteinizing hormone (LH) and follicle-stimulating hormone (FSH) levels and serum testosterone after 4 weeks of therapy


3.75 mg IM monthly for up to 6 months or 11.25 mg IM every 3 months for 2 doses (6 months total)

Recommended duration of treatment is 6 months; may treat again for additional 6 months, but with concomitant administration of norethindrone

Uterine Leiomyomata (Fibroids)

3.75 mg IM monthly for up to 3 months or 11.25 mg IM once

Use concomitant iron treatment

Breast Cancer in Premenopausal Ovarian Ablation (Off-label)

3.75 mg IM every 28 days or 11.25 mg IM every 3 months for up to 24 months


Do not use a combination of syringes to achieve a particular dose or length of therapy

Evaluate cardiovascular risk before initiating therapy and routinely thereafter

Routinely check for diabetes (blood glucose and Hb A1C) before initiating therapy and during treatment

Rotate SC injection sites frequently

In men, recommend calcium, vitamin D, exercise to prevent osteoporosis

Monitor serum PSA, testosterone, prostatic acid phosphatase (PAP)

Dosage Forms & Strengths

Lupron Depot-Ped

  • 7.5mg (monthly)
  • 11.25mg (monthly)
  • 15mg (monthly)
  • 11.25mg (3 months)
  • 30mg (3 months)

Leuprolide acetate

  • 5mg/mL

Central Precocious Puberty

Indicated when signs of sexual maturity begin to develop in girls <8 years old and boys <9 years old; may be discontinued at appropriate age of onset of puberty (eg, 11 years in females and 12 years in males), at physician's discretion

<2 years old: Safety and efficacy not established

Lupron Depot-Ped (monthly dose)

  • <25 kg: 7.5 mg IM monthly
  • >25 kg to 37.5 kg: 11.25 mg IM monthly
  • >37.5 kg: 15 mg IM monthly
  • Assess response 1-2 months after initial injection; if adequate hormonal and clinical suppression not achieved with starting doses, increase next monthly dose to the next higher level

Lupron Depot-Ped (3-month dose)

  • 11.25 mg or 30 mg as single IM injection every 3 months (dose not based on weight)
  • Regardless of dose chosen, goals are to suppress pituitary gonadotropins and peripheral sex steroids and to arrest progression of secondary sexual characteristics
  • Assess response 2-3 months after initial injection and 6 months after injection

Leuprolide acetate

  • 50 mcg/kg/day SC; may be titrated upward by 10 mcg/kg/day if downregulation not achieved  


Do not use partial syringes or combination of syringes to achieve particular dose

Vary injection site periodically

Monitor response with gonadotropin-releasing hormone (GnRH) stimulation test; measure testosterone in males and estradiol in females, Tanner staging

Check height and bone age every 6-12 months while using Lupron Depot-Ped

Measure bone mineral density



Interaction Checker

and leuprolide

No Results

     activity indicator 
    No Interactions Found
    Interactions Found


      Serious - Use Alternative

        Significant - Monitor Closely


            All Interactions Sort By:
             activity indicator 

            Adverse Effects


            Hot flashes (57%)

            Cardiovascular changes or ischemia (19%)

            Fatigue (18%)

            Pain (13%)

            Peripheral edema (12%)


            Asthenia (10%)

            Gynocomastia (7%)

            Headache (7%)

            Testicular atrophy (7%)

            Anorexia (6%)

            Anemia (5%)

            Bone pain (5%)

            Constipation (7%)

            Urinary frequency (6%)

            Dermatitis (5%)

            Dizziness (5%)

            Nausea and vomiting (5%)

            Gastroenteritis (3%)

            Myalgia (3%)

            UTI (3%)

            Dyspnea (2%)

            Frequency Not Defined




            Decreased bone density


            Obstruction of ureter or bladder



            Implant site reactions (pain, bruising, edema)

            Spinal cord compression (rare)

            Postmarketing Reports

            Anaphylactoid or asthmatic reaction

            Rash, urticaria, photosensitivity reactions

            Localized reactions (eg, induration, abscess)

            Mood swings, including depression; rare reports of suicidal ideation and attempts (many, but not all, of these patients had history of depression)

            Fibromyalgia (eg, joint and muscle pain, headaches, sleep disorder, GI distress, shortness of breath)

            Reduced WBC count

            Hepatobiliary: Serious liver injury (rare)

            Injury/poisoning/procedural complications: Spinal fracture

            Musculoskeletal/connective tissue: Tenosynovitislike symptoms

            Neurologic: Convulsion, peripheral neuropathy, paralysis

            Cardiovascular: Hypotension, myocardial infarction, pulmonary embolism

            Pituitary apoplexy: Symptoms include sudden headache, vomiting, visual changes, ophthalmoplegia, altered mental status, cardiovascular collapse; immediate medical attention required

            Respiratory system: Interstitial lung disease

            Urogenital system: Prostate pain




            Hypersensitivity to GnRH or other GnRH-agonist analogues

            Undiagnosed vaginal bleeding


            Children (Eligard)


            Urinary tract obstruction or vertebral metastases may occur

            May cause development or worsening of depression

            Females treated for precocious puberty may experience abnormal menses or spotting for first 2 months; notify healthcare provider if bleeding continues after second month

            Decrease in bone density reported when drug used for >6 months; use caution if there are additional risk factors for bone loss, including corticosteroid therapy or chronic alcohol use

            Worsening of endometriosis or uterine leiomyomata symptoms with therapy reported initially

            Rare cases of pituitary apoplexy, frequently secondary to pituitary adenoma reported (onset 1hr to usually <2 weeks): may present as sudden headache, vomiting, visual or mental status changes and cardiovascular collapse (rare), requiring immediate medical attention

            Worsening of glycemic control reported in men receiving GnRH agonists; monitor blood glucose and/or glycosylated hemoglobin (HbA1c) periodically in patients receiving a GnRH agonist and manage with current practice for treatment of hyperglycemia or diabetes

            Prostate cancer symptoms may worsen during initial treatment period

            Convulsions reported

            Androgen deprivation therapy may prolong the QT/QTc interval; consider whether benefits of androgen deprivation outweighs potential risks in patients with congenital long QT syndrome, congestive heart failure, frequent electrolyte abnormalities, and patients taking drugs known to prolong the QT interval; correct electrolyte abnormalities and monitor ECG and electrolytes periodically

            Men receiving GnRH agonists for prostate cancer have slightly increased risk of diabetes, heart attack, stroke, and sudden death

            In women, duration of treatment with GnRH agonists not to exceed 1 year, except in treatment of breast cancer

            Transient increase in serum levels of testosterone during treatment may result in worsening of symptoms or onset of new signs and symptoms during first few weeks of treatment, including bone pain, neuropathy, hematuria, bladder outlet obstruction, or ureteralobstruction; monitor patients at risk closely and manage as appropriate

            Psychiatric adverse events or emotional lability, including crying, irritability, impatience, anger, and aggression, reported; many, but not all, patients had a history of psychiatric illness or other comorbidities with an increased risk of depression

            Spinal cord compression reported; observe patients closely for weakness and paresthesias in first few weeks of therapy; observe patients with metastatic vertebral lesions closely

            Postmarketing reports of convulsions reported, including patients with or without a history of seizures, epilepsy, cerebrovascular disorders, central nervous system anomalies, and patients on concomitant medications associated with convulsions such as bupropion and SSRIs

            Tumor flare resulting from transient increases in testosterone, leading to bone pain, hematuria, bladder outlet obstruction, and neuropathy in prostate cancer patients reported during first few weeks of therapy

            Closely observe patients for urinary tract obstruction and hematuria in first few weeks of therapy

            Orchiectomy or luteinizing hormone agonists recommended as initial treatment for androgen deprivation in patients with advanced androgen sensitive prostate cancer

            Duration of treatment is limited by risk of loss of bone mineral density

            When using drug for management of endometriosis, combination use of norethindrone acetate (add-back therapy) is effective in reducing loss of BMD that occurs with leuprolide acetate; do not retreat with drug without combination norethindrone acetate; assess BMD before retreatment

            Therapy for hormone receptor-positive breast cancer

            • Ovarian suppression recommended, in addition to adjuvant endocrine therapy, for premenopausal women with higher-risk disease; lower risk patients should not
            • Ovarian suppression, addition to adjuvant chemotherapy recommended for premenopausal women with stage II or stage III breast cancers
            • Ovarian suppression, in addition to endocine therapy, recommended in women with stage I or II breast cancers at higher risk of recurrence, who might consider chemotherapy
            • Women with stage I disease, which does not require chemotherapy should receive endocrine therapy but not ovarian suppression
            • Women with node-negative cancers <1 cm (T!A< T!B) should receive endocrine therapy, but not ovarian suppression

            Pregnancy & Lactation


            There are no available data in pregnant women to inform the drug-associated risk

            Treatment may cause fetal harm based on findings from animal studies and drug’s mechanism of action; there are limited human data on the use in pregnant women

            Exclude pregnancy in women of reproductive potential prior to initiating

            Drug may cause embryo-fetal harm when administered during pregnancy; drug is not a contraceptive; if contraception is indicated, advise females of reproductive potential to use a non-hormonal method of contraception during treatment


            • Based on pharmacodynamic effects of decreasing secretion of gonadal steroids, fertility is expected to be decreased while on treatment; clinical and pharmacologic studies in adults (>18 years) have shown reversibility of fertility suppression when drug is discontinued after continuous administration for periods of up to 24 weeks
            • There is no evidence that pregnancy rates are affected following discontinuation of therapy
            • Animal studies (prepubertal and adult rats and monkeys) with leuprolide acetate and other GnRH analogs have shown functional recovery of fertility suppression

            Animal data

            • Based on animal reproduction studies, drug may be associated with an increased risk of pregnancy complications, including early pregnancy loss and fetal harm
            • In animal reproduction studies, subcutaneous administration of drug to rabbits during period of organogenesis caused embryo-fetal toxicity, decreased fetal weights and a dose-dependent increase in major fetal abnormalities in animals at doses less than the recommended human dose based on body surface area using an estimated daily dose
            • A similar rat study also showed increased fetal mortality and decreased fetal weights but no major fetal abnormalities at doses less than the recommended human dose based on body surface area using an estimated daily dose


            There are no data on presence of drug in either animal or human milk, effects on breastfed infants, or on milk production

            Developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant from treatment or from underlying maternal condition

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.



            Mechanism of Action

            Agonist analogue of luteinizing hormone-releasing hormone (LHRH)

            When administered continuously, decreases LH and FSH levels by acting as potent inhibitor of gonadotropin secretion; decrease in LH and FSH levels followed by suppression of ovarian and testicular steroidogenesis; testosterone levels reduced to below castrated levels in males


            Bioavailability: SC, 80-94%


            Protein bound: 43-49%

            Vd: Males, 27 L


            Metabolized to smaller inactive peptides, a pentapeptide (metabolite I), tripeptides (metabolites II and III), and a dipeptide (metabolite IV); these fragments may be further catabolized


            Half-life: 3 hr

            Clearance: 8.34 L/hr

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





            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
            Additional Offers
            Email to Patient



            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Email Forms to Patient



            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.