loo-PROE-lide

• Advanced prostate cancer in patients who are unable to tolerate orchiectomy or estrogen therapy (may be used in combination with flutamide or bicalutamide).
• Central precocious puberty (CPP).
• Endometriosis (as monotherapy or in combination with norethindrone).
• Uterine fibroids (in combination with iron).

• A synthetic analogue of luteinizing hormone–releasing hormone (LHRH).
• Initially causes a transient increase in testosterone; however, with continuous administration, testosterone levels are decreased.
• Reduces gonadotropins, testosterone, and estradiol.

• Decreased testosterone levels and resultant decrease in spread of prostate cancer.
• Reduction of pain/lesions in endometriosis.
• Decreased growth of fibroids.
• Delayed puberty.

Absorption: Rapidly and almost completely absorbed following subcut administration. More slowly absorbed following IM administration of depot form.

Distribution: Unknown.

Metabolism/Excretion: Unknown.

Half-life: 3 hr.

Contraindicated in:

• Hypersensitivity to synthetic analogues of LHRH (GnRH) or GnRH agonists
• OB: Pregnancy (may cause fetal harm)
• Lactation: Lactation.

Use Cautiously in:

• Hypersensitivity to benzyl alcohol (results in induration and erythema at subcut site)
• Congenital long QT syndrome, HF, electrolyte abnormalities, or concurrent use of other drugs known to prolong the QT interval
• Seizures, cerebrovascular disorders, CNS tumor, or concurrent use of bupropion or selective serotonin reuptake inhibitors.
• Rep: Women of reproductive potential.

CV: MI, angina, arrhythmias.
Depot: QT interval prolongation, vasodilation.

Derm: Depot: hair growth, rash.
Subcut: dry skin, hair loss, pigmentation, skin cancer, skin lesions.

EENT: blurred vision.
Subcut: hearing disorder.

Endo: breast swelling, breast tenderness, hyperglycemia.

F and E: hypercalcemia, lower extremity edema.

GI: anorexia, diarrhea, dysphagia, nausea, vomiting.
Depot: HEPATOTOXICITY, gingivitis.
Subcut: GI BLEEDING, hepatic impairment, peptic ulcer, rectal polyps, taste disorders.

GU: ↓fertility (males), ↓ testicular size, dysuria, incontinence, testicular pain.
Depot: cervix disorder.
Subcut: bladder spasm, penile swelling, prostate pain, urinary obstruction.

Local: burning, itching, swelling at injection site.

Metab: Depot: hyperuricemia, ↓ bone density.

MS: fibromyalgia, transient ↑ in bone pain (prostate cancer only).
Subcut: ankylosing spondylitis, joint pain, pelvic fibrosis, temporal bone pain.

Neuro: Subcut: peripheral neuropathy , SEIZURES, STROKE, aggression, anger, dizziness, headache, impatience, irritability, syncope.
Depot: depression, drowsiness, personality disorder.
Subcut: anxiety, blurred vision, lethargy, memory disorder, mood swings.

Resp: PULMONARY EMBOLISM, hemoptysis.
Depot: epistaxis, throat nodules.
Subcut: cough, pleural rub, pulmonary fibrosis, pulmonary infiltrate.

Misc: hot flashes, chills, ↓ libido, fever.
Depot: body odor, epistaxis.

Drug-Drug:

• ↑antineoplastic effects with antiandrogens (megestrol, flutamide).
• Concurrent use with bupropion or SSRIs may ↑ risk of seizures.
• QT interval prolonging drugs may ↑ risk of QT interval prolongation.

Advanced Prostate Cancer

• SC (Adults): Leuprolide acetate — 1 mg/day; Eligard — 7.5 mg once monthly, 22.5 mg every 3 mo, 30 mg every 4 mo, or 45 mg every 6 mo. Camcevi — 42 mg every 6 mo.
• IM (Adults): Lupron Depot — 7.5 mg once monthly or 22.5 mg every 3 mo or 30 mg every 4 mo or 45 mg every 6 mo.

Endometriosis

• IM (Adults): Lupron Depot — 3.75 mg once monthly for up to 6 mo or 11.25 mg every 3 mo for up to 2 doses; if symptoms recur after initial course of therapy, may administer a 2nd course of therapy.

Uterine Fibroids (with iron therapy)

• IM (Adults): Lupron Depot — 3.75 mg once monthly for up to 3 mo or 11.25 mg single injection.

Central Precocious Puberty

• SC (Children 2 yr): Leuprolide acetate — 50 mcg/kg/day, may ↑ by 10 mcg/kg/day as required. Fensolvi — 45 mg every 6 mo.
• IM (Children 2 yr and >37.5 kg): Lupron Depot-Ped — 15 mg every 4 wk; may ↑ by 3.75 mg every 4 wk as required.
• IM (Children 2 yr and 26–37.5 kg): Lupron Depot-Ped — 11.25 mg every 4 wk; may ↑ by 3.75 mg every 4 wk as required.
• IM (Children 2 yr and 25 kg): Lupron Depot-Ped — 7.5 mg every 4 wk; may ↑ by 3.75 mg every 4 wk as required.
• IM (Children 2 yr): Lupron Depot-Ped — 11.25 or 30 mg every 3 mo.

• Do not confuse Lupron Depot with Lupron Depot-Ped.
  • Norethindrone acetate 5 mg daily may be used to prevent bone density loss from leuprolide.
  • Correct electrolyte abnormalities before starting therapy.
• SC
  • Camcevi: Must be administered by a health care professional. Allow prefilled syringe to stand at room temperature for 30 min before injection. Wear gloves during preparation and administration. Inject into upper- or mid-abdominal area with sufficient soft or loose subcutaneous tissue that has not recently been used. Clean the injection site with an alcohol swab. Do NOT inject in areas with brawny or fibrous subcutaneous tissue or locations that can be rubbed or compressed (with a belt or clothing waistband). Avoid applying heat directly to the site of injection. Pinch skin and inject at 90° angle, release skin and inject full contents of syringe.
  • Eligard subcut formulation: Bring to room temperature before mixing. Reconstitution: Assemble the Eligard kit and reconstitute solution using syringes provided, as directed by manufacturer. Wearing gloves, mix in syringes as directed by manufacturer, do not shake. Solution must reach room temperature before administration and must be administered within 30 min of mixing, or be discarded. Solution is light tan to tan in color. Inject into abdomen, upper buttocks, or anywhere that has adequate amounts of subcut tissue without excessive pigment, nodules, lesions, or hair. Vary site with each injection. Store in refrigerator; may also be stored at room temperature in original packing for up to 8 wk before mixing.
  • Fensolvi:Must be administered by a health care professional. Allow to reach room temperature before reconstitution. Reconstitution: Follow manufacturer's instructions for assembling syringes and mixing.Concentration: 45 mg/0.375 mL. Administer within 30 min or discard. Inject into abdomen or upper buttocks. Avoid areas that have excessive pigment, nodules, lesions, or hair. Pinch skin and inject at 90° angle. Release skin and inject slowly. Rotate injection sites.
• IM: Use syringe supplied by manufacturer. Rotate sites.
  • Leuprolide depot is only for IM injection.
  • Lupron Depot formulation:Lupron Depot-Ped must be administered by a health care professional. Reconstitution: To prepare for injection screw white plunger into end stopper until stopper begins to turn. Hold syringe upright; release diluent by slowly pushing, over 6–8 sec, until the first stopper is at the blue line in the middle of the barrel. Keep syringe upright. Mix microspheres by shaking syringe until power forms a unified suspension. Tap syringe if caking or clumping occurs. Do not combine syringes or partial syringes to arrive at a dose of Lupron Depot-Ped. Suspension will appear milky. Do not use if powder does not go into suspension. Keep syringe upright, remove cap and expel air. Inject at 90° angle in gluteal area, anterior thigh, or deltoid, aspirate and discard if blood in syringe. Suspension settles very quickly; mix and administer immediately. Administer within 2 hr or discard. Rotate injection sites.

Camcevi, Eligard, Fensolvi, Lupron, Lupron Depot, Lupron Depot-Ped

Lupron, Zeulide Depot

Therapeutic Classification: antineoplastics

Pharmacologic Classification: hormones, gonadotropin releasing hormones

(Generic available)

• Emulsion for injection (Camcevi) (prefilled syringe): 42 mg/syringe;
• Lyophilized microspheres for depot injection (Lupron Depot): 3.75 mg; 7.5 mg; 11.25 mg; 22.5 mg; 30 mg; 45 mg;
• Lyophilized microspheres for depot injection (Lupron Depot-Ped): 7.5 mg; 11.25 mg; 15 mg; 30 mg;
• Lyophilized powder for injection (Fensolvi): 45 mg/vial;
• Polymeric matrix injectable formulation for injection (Eligard): 7.5 mg; 22.5 mg; 30 mg; 45 mg;
• Solution for injection (leuprolide acetate): 1 mg/0.2 mL;

(effect on hormone levels)

†Initial transient ↑ in testosterone and estradiol levels.

†Maximum decline in testosterone and estradiol levels.

iRestoration of normal pituitary–gonadal function; in amenorrheic patients, normal menses usually returns 60–90 days after treatment is discontinued.

• Monitor ECG periodically in patients at risk for QT interval prolongation.
• Prostate Cancer: Assess for an increase in bone pain, especially during the first few wk of therapy. Monitor patients with vertebral metastases for increased back pain and decreased sensory/motor function.
  • Monitor intake and output ratios; assess for bladder distention in patients with urinary tract obstruction during initiation of therapy.
• Fibroids: Assess for severity of symptoms (bloating, pelvic pain, pressure, excessive vaginal bleeding) periodically during therapy.
• Endometriosis: Assess for endometrial pain prior to and periodically during therapy.
• CPP: Prior to therapy, diagnosis of CPP should be confirmed by onset of secondary sex characteristics in girls <8 yr or boys <9 yr; a complete physical and endocrinologic examination, including height, weight, hand and wrist x-ray; total sex steroid level (estradiol or testosterone); adrenal steroid level; beta human chorionic gonadotropin level; GnRH stimulation test; and computerized tomography of the head must be performed. These parameters are monitored after 1–2 mo and every 3–6 mo during therapy.
  • Assess for signs of precocious puberty (menses, breast development, testicular growth) periodically during therapy. Dose is increased until no progression of the disease is noted either clinically or by lab test parameters, then usually maintained throughout therapy. Discontinuation of therapy should be considered before age 11 in girls and age 12 in boys.

• Verify negative pregnancy test before starting therapy.Initially ↑, then ↓ luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This leads to castration levels of testosterone in boys 2–4 wk after initial increase in concentrations.
  • Monitor testosterone, prostatic acid phosphate, and prostate-specific antigen (PSA) levels to evaluate response to therapy. Transient ↑ in levels may occur during the 1st mo of therapy for prostate cancer.
  • Monitor electrolytes before starting and periodically during therapy. May cause ↑ BUN, serum calcium, uric acid, hypoproteinemia, LDH, alkaline phosphatase, AST, hyperglycemia, hyperlipidemia, hyperphosphatemia, WBC, PT, or aPTT. May also cause ↓ platelets and serum potassium.
  • Monitor blood sugar and glycosylated hemoglobin periodically during therapy.

• Advise patient that medication may cause hot flashes. Notify health care professional if these become bothersome.
• Leuprolide depot usually causes a temporary discontinuation of menstruation. Advise patient to notify health care professional if menstruation persists or if intermittent bleeding occurs.
• Inform patient of the possibility of the development or worsening of depression and occurrence of memory disorders.
• Rep: May cause fetal harm. Advise females of reproductive potential to use effective contraception during therapy. Advise patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Advise patient that leuprolide may impair fertility.
• Prostate Cancer: Instruct patient and family on subcut injection technique. Review patient insert provided with leuprolide patient-administration kit.
  • Instruct patient to take medication exactly as directed. Take missed doses as soon as remembered unless not remembered until next day.
  • Inform patient that bone pain may increase at initiation of therapy, but will resolve with time. Advise patient to discuss use of analgesics to control pain with health care professional.
  • Instruct patient to notify health care professional promptly if difficulty urinating, weakness, or numbness occurs.
• Endometriosis: Advise patient to use a form of contraception other than oral contraceptives during therapy. Inform patient that amenorrhea is expected but does not guarantee contraception. Advise patient that breast feeding should be avoided during therapy.
• Central Precocious Puberty: Instruct patient and family on the proper technique for subcut injection. Emphasize the importance of administering the medication at the same time each day. Rotate injection sites periodically.
  • Inform patient and parents that if injections are not given daily, pubertal process may be reactivated.
  • Advise patient and parents that during the first 2 mo of therapy patient may experience a light menstrual flow or spotting. Health care professional should be notified if this continues beyond 2nd mo.
  • Instruct patient and parents to notify health care professional immediately if irritation at the injection site or unusual signs or symptoms occur.

• Decrease in the spread of prostate cancer.
• Decrease in lesions and pain in endometriosis.
• Resolution of the signs of CPP.
• Improvement in preoperative hematologic parameters in patients with anemia from uterine fibroids.

NDC Code^*

• 0074- AbbVie Inc.
  • 0074-2108- Lupron Depot-PED
    • 0074-2108-03- 1 KIT in 1 CARTON (0074-2108-03) * 1 mL in 1 SYRINGE * 1 SWAB in 1 PACKET

• 0074- AbbVie Inc.
  • 0074-2282- Lupron Depot-PED
    • 0074-2282-03- 1 KIT in 1 CARTON (0074-2282-03) * 1 mL in 1 SYRINGE * 1 SWAB in 1 PACKET

• 0074- AbbVie Inc.
  • 0074-2440- Lupron Depot-PED
    • 0074-2440-03- 1 KIT in 1 CARTON (0074-2440-03) * 1 mL in 1 SYRINGE * 1 SWAB in 1 PACKET

• 0074- AbbVie Inc.
  • 0074-3346- Lupron Depot
    • 0074-3346-03- 1 KIT in 1 CARTON (0074-3346-03) * 1.5 mL in 1 SYRINGE * 1 SWAB in 1 PACKET

• 0074- AbbVie Inc.
  • 0074-3473- Lupron Depot
    • 0074-3473-03- 1 KIT in 1 CARTON (0074-3473-03) * 1.5 mL in 1 SYRINGE * 1 SWAB in 1 PACKET

• 0074- AbbVie Inc.
  • 0074-3641- Lupron Depot
    • 0074-3641-03- 1 KIT in 1 CARTON (0074-3641-03) * 1 mL in 1 PACKET * 1 mL in 1 SYRINGE

• 0074- AbbVie Inc.
  • 0074-3641- Lupron Depot
    • 0074-3641-71- 1 KIT in 1 CARTON (0074-3641-71) * 1 mL in 1 PACKET * 1 mL in 1 SYRINGE

• 0074- AbbVie Inc.
  • 0074-3642- Lupron Depot
    • 0074-3642-03- 1 KIT in 1 CARTON (0074-3642-03) * 1 mL in 1 SYRINGE * 1 SWAB in 1 PACKET

• 0074- AbbVie Inc.
  • 0074-3663- Lupron Depot
    • 0074-3663-03- 1 KIT in 1 CARTON (0074-3663-03) * 1 mL in 1 PACKET * 1.5 mL in 1 SYRINGE

• 0074- AbbVie Inc.
  • 0074-3683- Lupron Depot
    • 0074-3683-03- 1 KIT in 1 CARTON (0074-3683-03) * 1.5 mL in 1 SYRINGE * 1 SWAB in 1 PACKET

• 0074- AbbVie Inc.
  • 0074-3779- Lupron Depot-PED
    • 0074-3779-03- 1 KIT in 1 CARTON (0074-3779-03) * 1.5 mL in 1 SYRINGE * 1 SWAB in 1 PACKET

• 0074- AbbVie Inc.
  • 0074-9694- Lupron Depot-PED
    • 0074-9694-03- 1 KIT in 1 CARTON (0074-9694-03) * 1.5 mL in 1 SYRINGE * 1 SWAB in 1 PACKET

• 0781- Sandoz Inc
  • 0781-4003- Leuprolide Acetate
    • 0781-4003-32- 1 KIT in 1 CARTON (0781-4003-32) * 1 VIAL, MULTI-DOSE in 1 CARTON (0781-3006-42) > 2.8 mL in 1 VIAL, MULTI-DOSE * 1 mL in 1 PACKET

• 47335- Sun Pharmaceutical Industries, Inc.
  • 47335-936- leuprolide acetate
    • 47335-936-40- 1 KIT in 1 CARTON (47335-936-40) * 1 mL in 1 PACKET * 1 VIAL, MULTI-DOSE in 1 CARTON > 2.8 mL in 1 VIAL, MULTI-DOSE

• 62935- TOLMAR PHARMACEUTICALS INC.
  • 62935-223- ELIGARD
    • 62935-223-05- 1 KIT in 1 CARTON (62935-223-05) *.375 mL in 1 SYRINGE (62935-224-05) *.375 mL in 1 SYRINGE (62935-221-04)

• 62935- TOLMAR PHARMACEUTICALS INC.
  • 62935-303- ELIGARD
    • 62935-303-30- 1 KIT in 1 CARTON (62935-303-30) *.5 mL in 1 SYRINGE (62935-305-29) *.5 mL in 1 SYRINGE (62935-304-30)

• 62935- TOLMAR PHARMACEUTICALS INC.
  • 62935-453- ELIGARD
    • 62935-453-45- 1 KIT in 1 CARTON (62935-453-45) *.375 mL in 1 SYRINGE (62935-455-45) *.375 mL in 1 SYRINGE (62935-454-44)

• 62935- TOLMAR PHARMACEUTICALS INC.
  • 62935-753- ELIGARD
    • 62935-753-75- 1 KIT in 1 CARTON (62935-753-75) *.25 mL in 1 SYRINGE (62935-755-75) *.25 mL in 1 SYRINGE (62935-154-50)