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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

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

Eligard

  • 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
more...

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

Monitoring

  • 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

Endometriosis

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

Administration

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
more...

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 

Administration

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 

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Interactions

Interaction Checker

leuprolide and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Hot flashes (57%)

            Cardiovascular changes or ischemia (19%)

            Fatigue (18%)

            Pain (13%)

            Peripheral edema (12%)

            1-10%

            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

            Convulsion

            Depression

            Neuropathy

            Decreased bone density

            Hematuria

            Obstruction of ureter or bladder

            Impotence

            Sweating

            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

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

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            Warnings

            Contraindications

            Hypersensitivity to GnRH or GnRH-agonist analogues

            Undiagnosed vaginal bleeding

            Pregnancy

            Eligard not to be used in children

            Breastfeeding

            Cautions

            Urinary tract obstruction, vertebral metastases, or psychiatric disorder may occur

            May cause development or worsening of depression

            Females treated for precocious puberty may experience abnormal menses; inform healthcare provider if bleeding continues

            Decrease in bone density reported when drug used for >6 months

            Worsening of endometriosis or uterine leiomyomata symptoms with therapy reported initially

            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, ureteralobstruction, or spinal cord compression; monitor patients at risk closely and manage as appropriate

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            Pregnancy & Lactation

            Pregnancy category: X

            Lactation: Contraindicated; not known if drug is excreted in breast milk; make decision to either discontinue nursing or discontinue drug, taking into account risk and benefits to the mother

            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.

            more...
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            Pharmacology

            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

            Absorption

            Bioavailability: SC, 80-94%

            Distribution

            Protein bound: 43-49%

            Vd: Males, 27 L

            Metabolism

            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

            Elimination

            Half-life: 3 hr

            Clearance: 8.34 L/hr

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

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            Images

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            Formulary

            FormularyPatient Discounts

            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.
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            • 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.
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