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
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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

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

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  

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

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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, 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

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            Warnings

            Contraindications

            Hypersensitivity to GnRH or GnRH-agonist analogues

            Undiagnosed vaginal bleeding

            Pregnancy or women who may become pregnant

            Eligard not to be used in children

            Breastfeeding

            Cautions

            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

            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
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            Pregnancy & Lactation

            Pregnancy

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

            Based on findings in animal studies and mechanism of action, therapy may cause fetal harm when administered to a pregnant woman

            Advise pregnant patients and females of reproductive potential of the potential risk to the fetus

            Based on findings in animals and mechanism of action, therapy may impair fertility in males of reproductive potential

            Animal data

            • In animal developmental and reproductive toxicology studies, administration of a monthly formulation of leuprolide acetate on day 6 of pregnancy (sustained exposure was expected throughout the period of organogenesis) caused adverse embryo-fetal toxicity in animals at doses less than the human dose based on body surface area using an estimated daily dose

            Lactation

            The safety and efficacy of therapy have not been established in females; there is no information regarding presence of drug in human milk, the effects on breastfed child, or on milk production; because many drugs are excreted in human milk and because of potential for serious adverse reactions in a breastfed child from therapy, a decision should be made to discontinue breastfeeding or discontinue drug, taking into account importance of drug to 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.

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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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            Formulary

            FormularyPatient Discounts

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