Eligard (Leuprolide Acetate)
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Eligard (Leuprolide Acetate)

ELIGARD
(leuprolide acetate) Suspension for Subcutaneous Injection

DRUG DESCRIPTION

ELIGARD (leuprolide acetate) ® is a sterile polymeric matrix formulation of leuprolide acetate, a GnRH agonist, for subcutaneous injection. It is designed to deliver leuprolide acetate at a controlled rate over a one-, three-, four- or six-month therapeutic period.

Leuprolide acetate is a synthetic nonapeptide analog of naturally occurring gonadotropin releasing hormone (GnRH) that, when given continuously, inhibits pituitary gonadotropin secretion and suppresses testicular and ovarian steroidogenesis. The analog possesses greater potency than the natural hormone. The chemical name is 5-oxo-L-prolyl-L-histidyl-Ltryptophyl-L-seryl-L-tyrosyl-D-leucyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide acetate (salt) with the following structural formula:

ELIGARD (leuprolide acetate) Structural Formula Illustration

ELIGARD (leuprolide acetate) ® is prefilled and supplied in two separate, sterile syringes whose contents are mixed immediately prior to administration. The two syringes are joined and the single dose product is mixed until it is homogenous. ELIGARD (leuprolide acetate) ® is administered subcutaneously, where it forms a solid drug delivery depot.

One syringe contains the ATRIGEL® Delivery System and the other contains leuprolide acetate. ATRIGEL® is a polymeric (non-gelatin containing) delivery system consisting of a biodegradable poly (DL-lactide-co-glycolide) (PLGH or PLG) polymer formulation dissolved in a biocompatible solvent, N-methyl-2-pyrrolidone (NMP).

Refer to Table 5 for the delivery system composition and constituted product formulation for each ELIGARD (leuprolide acetate) ® product.

Table 5: ELIGARD (leuprolide acetate) ® Delivery System Composition and Constituted Product Formulation

    ELIGARD® 7.5 mg ELIGARD® 22.5 mg ELIGARD® 30 mg ELIGARD® 45 mg
ATRIGEL® Delivery System Syringe Polymer PLGH PLG PLG PLG
Polymer description Copolymer containing carboxyl endgroups Copolymer with hexanediol Copolymer with hexanediol Copolymer with hexanediol
Polymer DL­lactide to Glycolide Molar Ratio 50:50 75:25 75:25 85:15
Constituted Product Polymer delivered 82.5 mg 158.6 mg 211.5 mg 165 mg
NMP delivered 160.0 mg 193.9 mg 258.5 mg 165 mg
Leuprolide acetate delivered 7.5 mg 22.5 mg 30 mg 45 mg
Approximate Leuprolide free base equivalent 7.0 mg 21 mg 28 mg 42 mg
Approximate administered formulation weight 250 mg 375 mg 500 mg 375 mg
Approximate injection volume 0.25 mL 0.375 mL 0.5 mL 0.375 mL

What are the possible side effects of leuprolide (Eligard, Lupron, Lupron Depot, Lupron Depot-Gyn, Lupron Depot-Ped)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have a serious side effect such as:

  • bone pain, loss of movement in any part of your body;
  • swelling, rapid weight gain;
  • pain, burning, stinging, bruising, or redness where the medication was injected;
  • feeling like you might pass out;
  • painful or difficult urination;
  • urinating more...

Read All Potential Side Effects and See Pictures of Eligard »

What are the precautions when taking leuprolide acetate (Eligard)?

Before using leuprolide, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: diabetes, heart disease (such as heart attack), stroke, high cholesterol, family history of sudden cardiac death.

Leuprolide may weaken your bones and increase your risk for bone loss (osteoporosis) if used for a long time. Before using this medication, tell your doctor or pharmacist if you have osteoporosis or if you have any of the following risk factors for osteoporosis: long-term alcohol use, smoking, family history...

Read All Potential Precautions of Eligard »

Last reviewed on RxList: 3/3/2011
This monograph has been modified to include the generic and brand name in many instances.

INDICATIONS

ELIGARD (leuprolide acetate) ® is indicated for the palliative treatment of advanced prostate cancer.

DOSAGE AND ADMINISTRATION

ELIGARD (leuprolide acetate) ® is administered subcutaneously and provides continuous release of leuprolide acetate over a one-, three-, four-, or six-month treatment period (Table 1). The injection delivers the dose of leuprolide acetate incorporated in a polymer formulation.

Table 1: ELIGARD (leuprolide acetate) ® Recommended Dosing

Dosage 7.5 mg 22.5 mg 30 mg 45 mg
Recommended Dose 1 injection every month 1 injection every 3 months 1 injection every 4 months 1 injection every 6 months

Once mixed, ELIGARD (leuprolide acetate) ® should be discarded if not administered within 30 minutes.

As with other drugs administered by subcutaneous injection, the injection site should vary periodically. The specific injection location chosen should be an area with sufficient soft or loose subcutaneous tissue. In clinical trials, the injection was administered in the upper- or mid-abdominal area. Avoid areas with brawny or fibrous subcutaneous tissue or locations that could be rubbed or compressed (i.e., with a belt or clothing waistband).

Mixing Procedure

IMPORTANT: Allow the product to reach room temperature before using. Once mixed, the product must be administered within 30 minutes.

Follow the instructions as directed to ensure proper preparation of ELIGARD (leuprolide acetate) ® prior to administration:

ELIGARD (leuprolide acetate) ® is packaged in either thermoformed trays or pouches. Each carton contains:

  • One sterile Syringe A pre-filled with the ATRIGEL® Delivery System
  • One Syringe B pre-filled with leuprolide acetate powder
  • One long white plunger rod for use with Syringe B
  • One sterile needle
  • Desiccant pack(s)

1. On a clean field, open all of the packages and remove the contents. Discard the desiccant pack(s).

Figure 1

Mixing Procedure - Illustration 1

Figure 2

Mixing Procedure - Illustration 2

2. Pull out the blue-tipped short plunger rod and attached stopper from Syringe B and discard (Figure 1). Gently insert the long, white replacement plunger rod into the gray primary stopper remaining in Syringe B by twisting it in place (Figure 2).

Figure 3

Mixing Procedure - Illustration 3

Figure 4

Mixing Procedure - Illustration 4

3. Unscrew the clear cap from Syringe A (Figure 3). Remove the gray rubber cap from Syringe B (Figure 4).

Figure 5

Mixing Procedure - Illustration 5

4. Join the two syringes together by pushing in and twisting until secure (Figure 5).

Figure 6

Mixing Procedure - Illustration 6

5. Inject the liquid contents of Syringe A into Syringe B containing the leuprolide acetate. Thoroughly mix the product by pushing the contents of both syringes back and forth between syringes (approximately 45 seconds) to obtain a uniform suspension (Figure 6). When thoroughly mixed, the suspension will appear light tan to tan (ELIGARD (leuprolide acetate) ® 7.5 mg) or colorless to pale yellow (ELIGARD (leuprolide acetate) ®, 22.5 mg, 30 mg and 45 mg) in color. Please Note: Product must be mixed as described; shaking will not provide adequate mixing of the product.

Figure 7

Mixing Procedure - Illustration 7

6. Hold the syringes vertically with Syringe B on the bottom. The syringes should remain securely coupled. Draw the entire mixed product into Syringe B (short, wide syringe) by depressing the Syringe A plunger and slightly withdrawing the Syringe B plunger. Uncouple Syringe A while continuing to push down on the Syringe A plunger (Figure 7). Note: Small air bubbles will remain in the formulation – this is acceptable.

Figure 8

Mixing Procedure - Illustration 8

Figure 9

Mixing Procedure - Illustration 9

Figure 10

Mixing Procedure - Illustration 10

7. Hold Syringe B upright. Remove the cap on the bottom of the sterile needle cartridge by twisting it (Figure 8). Attach the needle cartridge to the end of Syringe B (Figure 9) by pushing in and turning the needle until it is firmly seated. Do not twist the needle onto the syringe until it is stripped. Pull off the clear needle cartridge cover prior to administration (Figure 10).

Administration Procedure

IMPORTANT: Allow the product to reach room temperature before using. Once mixed, the product must be administered within 30 minutes.

1. Choose an injection site on the abdomen, upper buttocks, or anywhere with adequate amounts of subcutaneous tissue that does not have excessive pigment, nodules, lesions, or hair. Since you can vary the injection site with a subcutaneous injection, choose an area that hasn't recently been used.

2. Cleanse the injection-site area with an alcohol swab.

3. Using the thumb and forefinger of your non-dominant hand, grab and bunch the area of skin around the injection site.

Administration Procedure -  Illustration 1

4. Using your dominant hand, insert the needle quickly at a 90° angle. The approximate angle you use will depend on the amount and fullness of the subcutaneous tissue and the length of the needle. After the needle is inserted, release the skin with your nondominant hand.

Administration Procedure -   Illustration 2

5. Inject the drug using a slow, steady push. Press down on the plunger until the syringe is empty.

6. Withdraw the needle quickly at the same angle used for insertion.

7. Discard all components safely in an appropriate biohazard container.

HOW SUPPLIED

Dosage Forms And Strengths

ELIGARD® is an injectable suspension of leuprolide acetate available in a single use kit. The kit consists of a two-syringe mixing system, a sterile needle (Table 2), a silicone desiccant pouch to control moisture uptake, and a package insert for constitution and administration procedures. Each syringe is individually packaged. One contains the ATRIGEL® Delivery System and the other contains leuprolide acetate. When constituted, ELIGARD (leuprolide acetate) ® is administered as a single dose.

Table 2: ELIGARD (leuprolide acetate) ® Needle specifications

ELIGARD® formulation Gauge Length
7.5 mg 20-gauge ½-inch
22.5 mg 20-gauge ½-inch
30 mg 20-gauge 5/8-inch
45 mg 18-gauge 5/8-inch

ELIGARD (leuprolide acetate) ® is available in a single use kit of a two syringe-mixing system in the following strengths:

ELIGARD (leuprolide acetate) ® 7.5 mg – NDC 0024-0793-75
ELIGARD (leuprolide acetate) ® 22.5 mg – NDC 0024-0222-05
ELIGARD (leuprolide acetate) ® 30 mg – NDC 0024-0610-30
ELIGARD (leuprolide acetate) ® 45 mg – NDC 0024-0605-45

Storage

Store at 2 - 8 °C (35.6 – 46.4 °F)

Manufactured by: Tolmar, Inc Fort Collins, CO 80526 for: TOLMAR Therapeutics, Inc. Fort Collins, CO 80526. Distributed by: sanofi-aventis U.S. LLC Bridgewater, NJ 08807

Last reviewed on RxList: 3/3/2011
This monograph has been modified to include the generic and brand name in many instances.

SIDE EFFECTS

Clinical Trial Experience

The safety of all ELIGARD (leuprolide acetate) ® formulations was evaluated in clinical trials involving patients with advanced prostate cancer. In addition, the safety of ELIGARD (leuprolide acetate) ® 7.5 mg was evaluated in 8 surgically castrated males (Table 4). ELIGARD (leuprolide acetate) ®, like other GnRH analogs, caused a transient increase in serum testosterone concentrations during the first one to two weeks of treatment. Therefore, potential exacerbations of signs and symptoms of the disease during the first weeks of treatment are of concern in patients with vertebral metastases and/or urinary obstruction or hematuria. If these conditions are aggravated, it may lead to neurological problems such as weakness and/or paresthesia of the lower limbs or worsening of urinary symptoms [see WARNINGS AND PRECAUTIONS].

During the clinical trials, injection sites were closely monitored. Refer to Table 3 for a summary of reported injection site events.

Table 3: Reported Injection Site Adverse Events

  7.5 mg 22.5 mg 30 mg 45 mg
Study Number AGL9904 AGL9909 AGL0001 AGL0205
Number of patients 120 117 90 111
Treatment 1 injection every month up to 6 months 1 injection every 3 months up to 6 months 1 injection every 4 months up to 8 months 1 injection every 6 months up to 12 months
Number of injections 716 230 175 217
Transient burning/stinging 248 (34.6%)
injections;84% reported as mild
50 (21.7%)
injections; 86% reported as mild
35 (20%)
injections; 100% reported as mild
35 (16%)
injections; 91.4% reported as mild3
Pain (generally brief and mild) 4.3% of injections
(18.3% of patients)
3.5% of injections
(6.0% of patients)
2.3% of injections2
(3.3% of patients)
4.6% of injections4
Erythema (generally brief and mild) 2.6% of injections
(12.5% of patients)
0.9% of injections1
(1.7% of patients)
1.1% of injections
(2.2% of patients)
 
Bruising (Mild) 2.5% of injections
(11.7% of patients)
1.7% of injections
(3.4% of patients)
  2.3% of injections5
Pruritis 1.4% of injections
(9.2% of patients)
0.4% of injections
(0.9% of patients)
   
Induration 0.4% of injections
(2.5% of patients)
     
Ulceration 0.1% of injections
( > 0.8% of patients)
     
1 Erythema was reported following 2 injections of ELIGARD (leuprolide acetate) ® 22.5 mg. One report characterized the erythema as mild and it resolved within 7 days. The other report characterized the erythema as moderate and it resolved within 15 days. Neither patient experienced erythema at multiple injections.
2 A single event reported as moderate pain resolved within two minutes and all 3 mild pain events resolved within several days following injection of ELIGARD (leuprolide acetate) ® 30 mg.
3 Following injection of ELIGARD (leuprolide acetate) ® 30 mg, three of the 35 burning/stinging events were reported as moderate.
4 Transient pain was reported as mild in intensity in nine of ten (90%) events and moderate in intensity in one of ten (10%) events following injection of ELIGARD (leuprolide acetate) ® 45 mg.
5 Mild bruising was reported following 5 (2.3%) study injections and moderate bruising was reported following 2 ( < 1%) study injections of ELIGARD (leuprolide acetate) ® 45 mg.

These localized adverse events were non-recurrent over time. No patient discontinued therapy due to an injection site adverse event.

The following possibly or probably related systemic adverse events occurred during clinical trials with ELIGARD (leuprolide acetate) ®, and were reported in > 2% of patients (Table 7). Often, causality is difficult to assess in patients with metastatic prostate cancer. Reactions considered not drug-related are excluded.

Table 4: Summary of Possible or Probably Related Systemic Adverse Events Reported by > 2% of Patients treated with ELIGARD (leuprolide acetate) ®

    7.5 mg 7.5 mg 22.5 mg 30 mg 45 mg
Study Number   AGL9904 AGL9802 AGL9909 AGL0001 AGL0205
Number of patients   120 8 117 90 111
Treatment   1 injection every month up to 6 months 1 injection (surgically castrated patients) 1 injection every 3 months up to 6 months 1 injection every 4 months upto 8 months 1 injection every 6 months up to 12 months
Body System Adverse Event   Number (Percent)    
Body as a Malaise and Fatigue 21 (17.5 %)   7 (6.0%) 12 (13.3%) 13 (11.7%)
Whole Weakness         4 (3.6%)
Nervous System Dizziness 4 (3.3%)     4 (4.4%)  
Vascular Hot flashes/sweats 68
(56.7%)*
2
(25.0%)*
66
(56.4%)*
66
(73.3%)*
64
(57.7%)*
Renal/Urinary Urinary frequency     3 (2.6%) 2 (2.2%)  
Nocturia       2 (2.2%)  
Gastrointestinal Nausea     4 (3.4%) 2 (2.2%)  
Gastroenteritis/colitis 3 (2.5%)        
Skin Pruritis     3 (2.6%)    
Clamminess       4 (4.4%)*  
Night sweats       3 (3.3%)* 3 (2.7%)*
Alopecia       2 (2.2%)  
Musculoskeletal Arthralgia     4 (3.4%)    
Myalgia       2 (2.2%) 5 (4.5%)
Pain in limb         3 (2.7%)
Reproductive Testicular atrophy 6 (5.0%)     4 (4.4%)* 8 (7.2%)*
Gynecomastia       2 (2.2%)* 4 (3.6%)*
Testicular pain       2 (2.2%)  
Psychiatric Decreased libido       3 (3.3%)*  
*Expected pharmacological consequences of testosterone suppression.
In the patient populations studied with ELIGARD (leuprolide acetate) ® 7.5 mg, a total of 86 hot flashes/sweats adverse events were reported in 70 patients. Of these, 71 events (83%) were mild; 14 (16%) were moderate; 1 (1%) was severe.
In the patient population studied with ELIGARD (leuprolide acetate) ® 22.5 mg, a total of 84 hot flashes/sweats adverse events were reported in 66 patients. Of these, 73 events (87%) were mild; 11 (13%) were moderate; none were severe.
In the patient population studied with ELIGARD (leuprolide acetate) ® 30 mg, a total of 75 hot flash adverse events were reported in 66 patients. Of these, 57 events (76%) were mild; 16 (21%) were moderate; 2 (3%) were severe.
In the patient population studied with ELIGARD (leuprolide acetate) ® 45 mg, a total of 89 hot flash adverse events were reported in 64 patients. Of these, 62 events (70%) were mild; 27 (30%) were moderate; none were severe.

In addition, the following possibly or probably related systemic adverse events were reported by < 2% of the patients treated with ELIGARD (leuprolide acetate) ® in these clinical studies.

Body System Adverse Event
General Sweating, insomnia, syncope, rigors, weakness, lethargy
Gastrointestinal Flatulence, constipation, dyspepsia
Hematologic Decreased red blood cell count, hematocrit and hemoglobin
Metabolic Weight gain
Musculoskeletal Tremor, backache, joint pain, muscle atrophy, limb pain
Nervous Disturbance of smell and taste, depression, vertigo
Psychiatric Insomnia, depression, loss of libido*
Renal/Urinary Difficulties with urination, pain on urination, scanty urination, bladder spasm, blood in urine, urinary retention, urinary urgency, incontinence, nocturia, nocturia aggravated
Reproductive/ Urogenital: Testicular soreness/pain, impotence*, decreased libido*, gynecomastia*, breast soreness/tenderness*, testicular atrophy*, erectile dysfunction, penile disorder*, reduced penis size
Skin Alopecia, clamminess, night sweats*, sweating increased*
Vascular Hypertension, hypotension
* Expected pharmacological consequences of testosterone suppression.

Changes in Bone Density

Decreased bone density has been reported in the medical literature in men who have had orchiectomy or who have been treated with a GnRH agonist analog. It can be anticipated that long periods of medical castration in men will have effects on bone density.

Postmarketing Experience

During post-marketing surveillance, rare cases of pituitary apoplexy (a clinical syndrome secondary to infarction of the pituitary gland) have been reported after the administration of gonadotropin-releasing hormone agonists. In a majority of these cases, a pituitary adenoma was diagnosed with a majority of pituitary apoplexy cases occurring within 2 weeks of the first dose, and some within the first hour. In these cases, pituitary apoplexy has presented as sudden headache, vomiting, visual changes, ophthalmoplegia, altered mental status, and sometimes cardiovascular collapse. Immediate medical attention has been required.

Read the Eligard (leuprolide acetate) Side Effects Center for a complete guide to possible side effects »

DRUG INTERACTIONS

No pharmacokinetic drug-drug interaction studies were conducted with ELIGARD (leuprolide acetate) ®.

Last reviewed on RxList: 3/3/2011
This monograph has been modified to include the generic and brand name in many instances.

WARNINGS

Included as part of the PRECAUTIONS section.

PRECAUTIONS

Tumor Flare

ELIGARD (leuprolide acetate) ® 7.5 mg 22.5 mg 30 mg, like other GnRH agonists, causes a transient increase in serum concentrations of testosterone during the first week of treatment. ELIGARD (leuprolide acetate) ® 45 mg causes a transient increase in serum concentrations of testosterone during the first two weeks of treatment. Patients may experience worsening of symptoms or onset of new signs and symptoms during the first few weeks of treatment, including bone pain, neuropathy, hematuria, or bladder outlet obstruction.

Cases of ureteral obstruction and/or spinal cord compression, which may contribute to paralysis with or without fatal complications, have been observed in the palliative treatment of advanced prostate cancer using GnRH agonists.

Patients with metastatic vertebral lesions and/or with urinary tract obstruction should be closely observed during the first few weeks of therapy. If spinal cord compression or ureteral obstruction develops, standard treatment of these complications should be instituted.

Laboratory Tests

Response to ELIGARD (leuprolide acetate) ® should be monitored by measuring serum concentrations of testosterone and prostate specific antigen periodically.

In the majority of patients, testosterone levels increased above Baseline during the first week, declining thereafter to Baseline levels or below by the end of the second or third week. Castrate levels were generally reached within two to four weeks.

Castrate testosterone levels were maintained for the duration of the treatment with ELIGARD (leuprolide acetate) ® 7.5 mg. No increases to above the castrate level occurred in any of the patients.

Castrate levels were generally maintained for the duration of treatment with ELIGARD (leuprolide acetate) ® 22.5 mg.

Once castrate levels were achieved with ELIGARD (leuprolide acetate) ® 30 mg, most (86/89) patients remained suppressed throughout the study.

Once castrate levels were achieved with ELIGARD (leuprolide acetate) ® 45 mg, only one patient ( < 1%) experienced a breakthrough, with testosterone levels > 50 ng/dL.

Results of testosterone determinations are dependent on assay methodology. It is advisable to be aware of the type and precision of the assay methodology to make appropriate clinical and therapeutic decisions.

Drug/Laboratory Test Interactions

Therapy with leuprolide acetate results in suppression of the pituitary-gonadal system. Results of diagnostic tests of pituitary gonadotropic and gonadal functions conducted during and after leuprolide therapy may be affected.

Hyperglycemia and Diabetes

Hyperglycemia and an increased risk of developing diabetes have been reported in men receiving GnRH agonists. Hyperglycemia may represent development of diabetes mellitus or worsening of glycemic control in patients with diabetes. 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.

Cardiovascular Diseases

Increased risk of developing myocardial infarction, sudden cardiac death and stroke has been reported in association with use of GnRH agonists in men. The risk appears low based on the reported odds ratios, and should be evaluated carefully along with cardiovascular risk factors when determining a treatment for patients with prostate cancer. Patients receiving a GnRH agonist should be monitored for symptoms and signs suggestive of development of cardiovascular disease and be managed according to current clinical practice.

Nonclinical toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

Two-year carcinogenicity studies were conducted with leuprolide acetate in rats and mice. In rats, a dose-related increase of benign pituitary hyperplasia and benign pituitary adenomas was noted at 24 months when the drug was administered subcutaneously at high daily doses (0.6 to 4 mg/kg). There was a significant but not dose-related increase of pancreatic islet-cell adenomas in females and of testicular interstitial cell adenomas in males (highest incidence in the low dose group). In mice, no leuprolide acetate-induced tumors or pituitary abnormalities were observed at a dose as high as 60 mg/kg for two years. Patients have been treated with leuprolide acetate for up to three years with doses as high as 10 mg/day and for two years with doses as high as 20 mg/day without demonstrable pituitary abnormalities. No carcinogenicity studies have been conducted with ELIGARD (leuprolide acetate) ®.

Mutagenicity studies have been performed with leuprolide acetate using bacterial and mammalian systems and with ELIGARD (leuprolide acetate) ® 7.5 mg in bacterial systems. These studies provided no evidence of a mutagenic potential.

Use In Specific Populations

Pregnancy

Pregnancy category X

[See ‘CONTRAINDICATIONS' section]

ELIGARD (leuprolide acetate) ® is contraindicated in women who are or may become pregnant while receiving the drug. Expected hormonal changes that occur with ELIGARD (leuprolide acetate) ® treatment increase the risk for pregnancy loss. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus and the potential risk for pregnancy loss.

In non-clinical studies in rats, major fetal abnormalities were observed after administration of leuprolide acetate throughout gestation. There were increased fetal mortality and decreased fetal weights in rats and rabbits. The effects of fetal mortality are expected consequences of the alterations in hormonal levels brought about by this drug. The possibility exists that spontaneous abortion may occur.

Nursing Mothers

ELIGARD (leuprolide acetate) ® is not indicated for use in women [see INDICATIONS AND USAGE]. It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from ELIGARD (leuprolide acetate) ®, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use

The safety and effectiveness of ELIGARD (leuprolide acetate) ® in pediatric patients have not been established.

Geriatric Use

The majority of the patients (approximately 70%) studied in the clinical trials were age 70 and older.

Last reviewed on RxList: 3/3/2011
This monograph has been modified to include the generic and brand name in many instances.

OVERDOSE

In clinical trials using daily subcutaneous injections of leuprolide acetate in patients with prostate cancer, doses as high as 20 mg/day for up to two years caused no adverse effects differing from those observed with the 1 mg/day dose.

CONTRAINDICATIONS

Hypersensitivity

ELIGARD (leuprolide acetate) ® is contraindicated in patients with hypersensitivity to GnRH, GnRH agonist analogs or any of the components of ELIGARD (leuprolide acetate) ®. Anaphylactic reactions to synthetic GnRH or GnRH agonist analogs have been reported in the literature.

Pregnancy

ELIGARD (leuprolide acetate) may cause fetal harm when administered to a pregnant woman. Expected hormonal changes that occur with ELIGARD (leuprolide acetate) treatment increase the risk for pregnancy loss and fetal harm when administered to a pregnant women [see Use in Specific Populations]. ELIGARD (leuprolide acetate) is contraindicated in women who are or may become pregnant. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus.

Last reviewed on RxList: 3/3/2011
This monograph has been modified to include the generic and brand name in many instances.

CLINICAL PHARMACOLOGY

Mechanism of Action

Leuprolide acetate, a gonadotropin releasing hormone (GnRH) agonist, acts as a potent inhibitor of gonadotropin secretion when given continuously in therapeutic doses. Animal and human studies indicate that after an initial stimulation, chronic administration of leuprolide acetate results in suppression of testicular and ovarian steroidogenesis. This effect is reversible upon discontinuation of drug therapy.

In humans, administration of leuprolide acetate results in an initial increase in circulating levels of luteinizing hormone (LH) and follicle stimulating hormone (FSH), leading to a transient increase in levels of the gonadal steroids (testosterone and dihydrotestosterone in males, and estrone and estradiol in premenopausal females). However, continuous administration of leuprolide acetate results in decreased levels of LH and FSH. In males, testosterone is reduced to below castrate threshold ( ≤ 50 ng/dL). These decreases occur within two to four weeks after initiation of treatment. Long-term studies have shown that continuation of therapy with leuprolide acetate maintains testosterone below the castrate level for up to seven years.

Pharmacodynamics

Following the first dose of ELIGARD (leuprolide acetate) ®, mean serum testosterone concentrations transiently increased, then fell to below castrate threshold ( ≤ 50 ng/dL) within three weeks for all ELIGARD (leuprolide acetate) ® concentrations.

Continued monthly treatment with ELIGARD (leuprolide acetate) ® 7.5 mg maintained castrate testosterone suppression throughout the study. No breakthrough of testosterone concentrations above castrate threshold ( > 50 ng/dL) occurred at any time during the study once castrate suppression was achieved (Figure 11).

One patient received less than a full dose of ELIGARD (leuprolide acetate) ® 22.5 mg at baseline, never suppressed and withdrew from the study at Day 73. Of the 116 patients remaining in the study, 115 (99%) had serum testosterone levels below the castrate threshold by Month 1 (Day 28). By Day 35, 116 (100%) had serum testosterone levels below the castrate threshold. Once testosterone suppression was achieved, one patient ( < 1%) demonstrated breakthrough (concentrations > 50 ng/dL after achieving castrate levels) following the initial injection; that patient remained below the castrate threshold following the second injection (Figure 12).

One patient withdrew from the ELIGARD (leuprolide acetate) ® 30 mg study at Day 14. Of the 89 patients remaining in the study, 85 (96%) had serum testosterone levels below the castrate threshold by Month 1 (Day 28). By Day 42, 89 (100%) of patients attained castrate testosterone suppression. Once castrate testosterone suppression was achieved, three patients (3%) demonstrated breakthrough (concentrations > 50 ng/dL after achieving castrate levels) (Figure 13).

One patient at Day 1 and another patient at Day 29 were withdrawn from the ELIGARD (leuprolide acetate) ® 45 mg study. Of the 109 patients remaining in the study, 108 (99.1%) had serum testosterone levels below the castrate threshold by Month 1 (Day 28). One patient did not achieve castrate suppression and was withdrawn from the study at Day 85. Once castrate testosterone suppression was achieved, one patient ( < 1%) demonstrated breakthrough (concentrations > 50 ng/dL after achieving castrate levels) (Figure 14).

Leuprolide acetate is not active when given orally.

Pharmacokinetics

Absorption

ELIGARD (leuprolide acetate) ® 7.5 mg

The pharmacokinetics/pharmacodynamics observed during three once-monthly injections in 20 patients with advanced prostate cancer is shown in Figure 11. Mean serum leuprolide concentrations following the initial injection rose to 25.3 ng/mL (Cmax) at approximately 5 hours after injection. After the initial increase following each injection, serum concentrations remained relatively constant (0.28 – 2.00 ng/mL).

Figure 11: Pharmacokinetic/Pharmacodynamic Response (N=20) to ELIGARD (leuprolide acetate) ® 7.5 mg – Patients Dosed Initially and at Months 1 and 2

Pharmacokinetic/Pharmacodynamic Response - Illustration

A reduced number of sampling timepoints resulted in the apparent decrease in Cmax values with the second and third doses of ELIGARD (leuprolide acetate) ® 7.5 mg (Figure 11).

ELIGARD (leuprolide acetate) ® 22.5 mg

The pharmacokinetics/pharmacodynamics observed during two injections every three months (ELIGARD (leuprolide acetate) ® 22.5 mg) in 22 patients with advanced prostate cancer is shown in Figure 12. Mean serum leuprolide concentrations rose to 127 ng/mL and 107 ng/mL at approximately 5 hours following the initial and second injections, respectively. After the initial increase following each injection, serum concentrations remained relatively constant (0.2 – 2.0 ng/mL).

Figure 12: Pharmacokinetic/Pharmacodynamic Response (N=22) to ELIGARD (leuprolide acetate) ® 22.5 mg – Patients Dosed Initially and at Month 3

Pharmacokinetic/Pharmacodynamic Response (N=22) to ELIGARD® 22.5 mg - Illustration

ELIGARD (leuprolide acetate) ® 30 mg

The pharmacokinetics/pharmacodynamics observed during injections administered initially and at four months (ELIGARD (leuprolide acetate) ® 30 mg ) in 24 patients with advanced prostate cancer is shown in Figure 13. Mean serum leuprolide concentrations following the initial injection rose rapidly to 150 ng/mL (Cmax) at approximately 3.3 hours after injection. After the initial increase following each injection, mean serum concentrations remained relatively constant (0.1 – 1.0 ng/mL).

Figure 13: Pharmacokinetic/Pharmacodynamic Response (N=24) to ELIGARD (leuprolide acetate) ® 30 mg – Patients Dosed Initially and at Month 4

Pharmacokinetic/Pharmacodynamic Response (N=24) to ELIGARD® 30 mg - Illustration

ELIGARD (leuprolide acetate) ® 45 mg

The pharmacokinetics/pharmacodynamics observed during injections administered initially and at six months (ELIGARD (leuprolide acetate) ® 45 mg) in 27 patients with advanced prostate cancer is shown in Figure 14. Mean serum leuprolide concentrations rose to 82 ng/mL and 102 ng/mL (Cmax) at approximately 4.5 hours following the initial and second injections, respectively. After the initial increase following each injection, mean serum concentrations remained relatively constant (0.2 – 2.0 ng/mL).

Figure 14: Pharmacokinetic/Pharmacodynamic Response (N=27) to ELIGARD (leuprolide acetate) ® 45 mg - Patients Dosed Initially and at Month 6

Pharmacokinetic/Pharmacodynamic Response (N=27) to ELIGARD® 45 mg - Illustration

There was no evidence of significant accumulation during repeated dosing. Non-detectable leuprolide plasma concentrations have been occasionally observed during ELIGARD (leuprolide acetate) ® administration, but testosterone levels were maintained at castrate levels.

Distribution

The mean steady-state volume of distribution of leuprolide following intravenous bolus administration to healthy male volunteers was 27 L. In vitro binding to human plasma proteins ranged from 43% to 49%.

Metabolism

In healthy male volunteers, a 1-mg bolus of leuprolide administered intravenously revealed that the mean systemic clearance was 8.34 L/h, with a terminal elimination half-life of approximately 3 hours based on a two compartment model.

No drug metabolism study was conducted with ELIGARD®. Upon administration with different leuprolide acetate formulations, the major metabolite of leuprolide acetate is a pentapeptide (M1) metabolite.

Excretion

No drug excretion study was conducted with ELIGARD (leuprolide acetate) ®.

Geriatrics

[see Use In Special Populations]

Race

In patients studied, mean serum leuprolide concentrations were similar regardless of race. Refer to Table 6 for distribution of study patients by race.

Table 6: Race Characterization of Study Patients

Race ELIGARD® 7.5 mg ELIGARD® 22.5 mg ELIGARD® 30 mg ELIGARD® 45 mg
White 26 19 18 17
Black - 4 4 7
Hispanic 2 2 2 3

Renal and Hepatic Insufficiency

The pharmacokinetics of ELIGARD (leuprolide acetate) ® in hepatically and renally impaired patients have not been determined.

Clinical Studies

One open-label, multicenter study was conducted with each ELIGARD (leuprolide acetate) ® formulation (7.5 mg, 22.5 mg, 30 mg, and 45 mg) in patients with Jewett stage A though D prostate cancer who were treated with at least a single injection of study drug (Table 7). These studies evaluated the achievement and maintenance of castrate serum testosterone suppression over the duration of therapy (Figures 15-18).

During the AGL9904 study using ELIGARD (leuprolide acetate) ® 7.5 mg, once testosterone suppression was achieved, no patients (0%) demonstrated breakthrough (concentration > 50 ng/dL) at any time in the study.

During the AGL9909 study using ELIGARD (leuprolide acetate) ® 22.5 mg, once testosterone suppression was achieved, only one patient ( < 1%) demonstrated breakthrough following the initial injection; that patient remained below the castrate threshold following the second injection.

During the AGL0001 study using ELIGARD (leuprolide acetate) ® 30 mg, once testosterone suppression was achieved, three patients (3%) demonstrated breakthrough. In the first of these patients, a single serum testosterone concentration of 53 ng/dL was reported on the day after the second injection. In this patient, castrate suppression was reported for all other timepoints. In the second patient, a serum testosterone concentration of 66 ng/dL was reported immediately prior to the second injection. This rose to a maximum concentration of 147 ng/dL on the second day after the second injection. In this patient, castrate suppression was again reached on the seventh day after the second injection and was maintained thereafter. In the final patient, serum testosterone concentrations > 50 ng/dL were reported at 2 and at 8 hours after the second injection. Serum testosterone concentration rose to a maximum of 110 ng/dL on the third day after the second injection. In this patient, castrate suppression was again reached eighteen days after the second injection and was maintained until the final day of the study, when a single serum testosterone concentration of 55 ng/dL was reported.

During the AGL0205 study using ELIGARD (leuprolide acetate) ® 45 mg, once testosterone suppression was achieved, one patient ( < 1%) demonstrated breakthrough. This patient reached castrate suppression at Day 21 and remained suppressed until Day 308 when his testosterone level rose to 112 ng/dL. At Month 12 (Day 336), his testosterone was 210 ng/dL.

Table 7: Summary of ELIGARD (leuprolide acetate) ® Clinical Studies

    7.5 mg 22.5 mg 30 mg 45 mg
Study number   AGL9904 AGL9909 AGL0001 AGL0205
Total Number of patients   120 (117 completed) 1172 (111 completed3) 90 (82 completed4) 111 (103 completed5)
Jewett Stages Stage A - 2 2 5
Stage B - 19 38 43
Stage C 89 60 16 19
Stage D 31 36 34 44
Treatment   6 monthly injections 1 injection (4 patients) 1 injection (5 patients) 1 injection (5 patients)
      2 injections, one every three months (113 patients) 2 injections, one every four months (85 patients) 2 injections, one every six months (106 patients)
Duration of therapy 6 months 6 months 8 months 12 months
Mean testosterone concentration (ng/dL) Baseline 361.3 367.1 385.5 367.7
Day 2 574.6 (Day 3) 588.0 610.0 588.6
Day 14 Below Baseline (Day 10) Below Baseline Below Baseline Below Baseline
Day 28 21.8 27.7 (Day 21) 17.2 16.7
Conclusion 6.1 10.1 12.4 12.6
Number of patients castrate threshold ( ≤ 50 ng/dL) Day 28 112 of 119 115 of 116 85 of 89 (96%) 108 of 109
below (94.1%) (99%)   (99.1%)
Day 35 - 116 (100%) - ­
Day 42 119 (100%) - 89 (100%) -
Conclusion 1171 (100%) 111 (100%) 81 (99%) 102 (99%)
1 Two patients withdrew for reasons unrelated to drug.
2 One patient received less than a full dose at Baseline, never suppressed, and was withdrawn at Day 73 and given an alternate treatment.
3 All non-evaluable patients who attained castration by Day 28 maintained castration at each timepoint up to and including the time of withdrawal.
4 One patient withdrew on Day 14. All 7 non-evaluable patients who had achieved castration by Day 28 maintained castration at each timepoint, up to and including the time of withdrawal.
5 Two patients were withdrawn prior to the Month 1 blood draw. One patient did not achieve castration and was withdrawn on Day 85. All 5 non-evaluable patients who attained castration by Day 28, maintained castration at each timepoint up to and including the time of withdrawal.

Figure 15: ELIGARD (leuprolide acetate) ® 7.5 mg Mean Serum Testosterone Concentrations (n=117)

ELIGARD® 7.5 mg Mean Serum Testosterone Concentrations - Illustration

Figure 16: ELIGARD (leuprolide acetate) ® 22.5 mg Mean Serum Testosterone Concentrations (n=111)

ELIGARD® 22.5 mg Mean Serum Testosterone Concentrations -  Illustration

Figure 17: ELIGARD (leuprolide acetate) ® 30 mg Mean Serum Testosterone Concentrations (n=90)

ELIGARD® 30 mg Mean Serum Testosterone Concentrations - Illustration

Figure 18: ELIGARD (leuprolide acetate) ® 45 mg Mean Serum Testosterone Concentrations (n=103)

ELIGARD® 45 mg Mean Serum Testosterone Concentrations - Illustration

Serum PSA decreased in all patients in all studies whose Baseline values were elevated above the normal limit. Refer to Table 8 for a summary of the effectiveness of ELIGARD (leuprolide acetate) ® in reducing serum PSA values.

Table 8: Effect of ELIGARD (leuprolide acetate) ® on Patient Serum PSA Values

ELIGARD® 7.5 mg 22.5 mg 30 mg 45 mg
Mean PSA Reduction at Study Conclusion 94% 98% 86% 97%
Patients with Normal PSA at Study Conclusion* 94% 91% 93% 95%
*Among patients who presented with elevated levels at Baseline

Other secondary efficacy endpoints evaluated included WHO performance status, bone pain, urinary pain and urinary signs and symptoms. Refer to Table 9 for a summary of these endpoints.

Table 9: Secondary Efficacy Endpoints

    ELIGARD® 7.5 mg ELIGARD® 22.5 mg ELIGARD® 30 mg ELIGARD® 45 mg
Baseline WHO Status = 01 88% 94% 90% 90%
  WHO Status = 12 11% 6% 10% 7%
WHO Status = 23       3%
Mean Bone Pain4(range) 1.22 (1-9) 1.20 (1-9) 1.20 (1-7) 1.38 (1-7)
Mean Urinary Pain (range) 1.12 (1-5) 1.02 (1-2) 1.01 (1-2) 1.22 (1-8)
Mean Urinary Signs and Symptoms (range) Low 1.09 (1-4) Low Low
Number of Patients with ProstateAbnormalities 102 (85%) 96 (82%) 66 (73%) 89 (80%)
    Month 6 Month 6 Month 8 Month 12
Follow-up WHO Status = 0 Unchanged 96% 87% 94%
WHO Status = 1 Unchanged 4% 12% 5%
WHO Status = 2     1% 1%
Mean Bone Pain (range) 1.26 (1-7) 1.22 (1-5) 1.19 (1-8) 1.31 (1-8)
Mean Urinary Pain (range) 1.07 (1-8) 1.10 (1-8) 1.00 (1-1) 1.07 (1-5)
Mean Urinary Signs and Symptoms (range) Modestly Decreased 1.18 (1-7) Modestly Decreased Modestly Decreased
Number of Patients with Prostate Abnormalities 77 (64%) 76 (65%) 54 (60%) 60 (58%)
1 WHO Status = 0 classified as “fully active.”
2 WHO Status = 1 classified as “restricted in strenuous activity but ambulatory and able to carry out work of a light or sedentary nature.”
3 WHO Status = 2 classified as “ambulatory but unable to carry out work activities.”
4 Pain score scale: 1 (no pain) to 10 (worst pain possible).

Last reviewed on RxList: 3/3/2011
This monograph has been modified to include the generic and brand name in many instances.

PATIENT INFORMATION

As with other GnRH agonists, patients may experience hot flashes. During the first few weeks of treatment, patients may also experience increased bone pain, increased difficulty in urinating, and the onset or aggravation of weakness or paralysis. Patients should notify their doctor if they develop new or worsened symptoms after beginning ELIGARD (leuprolide acetate) ® treatment. Patients should be told about the injection site related adverse reactions, such as transient burning/stinging, pain, bruising, and redness. These injection site reactions are usually mild and reversible. If they do not resolve, patients should tell their doctor. If the patient experiences an allergic reaction, they should contact their doctor immediately.

Last reviewed on RxList: 3/3/2011
This monograph has been modified to include the generic and brand name in many instances.

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PATIENT INFORMATION

As with other GnRH agonists, patients may experience hot flashes. During the first few weeks of treatment, patients may also experience increased bone pain, increased difficulty in urinating, and the onset or aggravation of weakness or paralysis. Patients should notify their doctor if they develop new or worsened symptoms after beginning ELIGARD (leuprolide acetate) ® treatment. Patients should be told about the injection site related adverse reactions, such as transient burning/stinging, pain, bruising, and redness. These injection site reactions are usually mild and reversible. If they do not resolve, patients should tell their doctor. If the patient experiences an allergic reaction, they should contact their doctor immediately.

Last reviewed on RxList: 3/3/2011
This monograph has been modified to include the generic and brand name in many instances.

Disclaimer

Eligard Consumer

IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

LEUPROLIDE MONTHLY (7.5 MG) - SUBCUTANEOUS INJECTION

(LEW-pro-lide)

COMMON BRAND NAME(S): Eligard

USES: Leuprolide is used to treat advanced prostate cancer in men. It is not a cure. Most types of prostate cancer need the male hormone testosterone to grow and spread. Leuprolide works by reducing the amount of testosterone that the body makes. This helps slow or stop the growth of cancer cells and helps relieve symptoms such as painful/difficult urination. Talk to your doctor about the risks and benefits of treatment.

OTHER USES: This section contains uses of this drug that are not listed in the approved professional labeling for the drug but that may be prescribed by your health care professional. Use this drug for a condition that is listed in this section only if it has been so prescribed by your health care professional.

Other leuprolide products may also be used to treat disorders of the uterus (e.g., endometriosis, fibroids). In females, leuprolide reduces the amount of estrogen that the body makes. Leuprolide may also be used to stop early puberty in children.

HOW TO USE: This medication is given as an injection under the skin (subcutaneously), usually once a month or as directed by your doctor. This product slowly releases the medication into your blood over a 1-month period.

If you are directed to inject this medication yourself, learn all preparation and usage instructions in the product package. If any of the information is unclear, consult your doctor or pharmacist.

Remove the product from the refrigerator and allow it to come to room temperature. Wash your hands and properly mix the medication. Before using, check this product visually for particles or discoloration. If either is present, do not use the liquid. Clean the injection site with an alcohol swab. Change the location of the injection site each time to avoid problem areas under the skin. Give each dose within 30 minutes of mixing. If more than 30 minutes have passed since mixing, throw out the product and prepare another syringe/dose.

Learn how to store and discard needles and medical supplies safely. Consult your pharmacist.

Use this medication regularly to get the most benefit from it. To help you remember, mark your calendar to keep track of when to schedule the next dose.

Disclaimer

Eligard Consumer (continued)

SIDE EFFECTS: Hot flashes (flushing), increased sweating, night sweats, tiredness, swelling of the ankles/feet, increased urination at night, dizziness, or mild burning/pain/bruising at the injection site may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

Infrequently, shrinking of the testicles, breast tenderness/swelling, and reduced sexual interest/ability may also occur as a result of lowered testosterone levels. Talk to your doctor if these effects occur.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

During the first few weeks of treatment, your level of testosterone will actually increase before it decreases. This is a normal response by your body to this drug. This may sometimes result in new or worsening symptoms for a few weeks. If you have prostate cancer that has spread to the spine or caused urinary blockage, you may require closer monitoring by your doctor, especially when you first start treatment. Tell your doctor immediately if you experience any of the following serious side effects: bone pain, numbness/tingling/weakness of the arms/legs, blood in the urine, painful/difficult urination, unusual weakness, inability to move.

Tell your doctor immediately if any of these unlikely but serious side effects occur: new/worsening bone pain, easily broken bones, increased thirst/urination, mental/mood changes (such as depression, thoughts of suicide, mood swings, aggression in children).

Get medical help right away if any of these rare but serious side effects occur: chest/jaw/left arm pain, irregular heartbeat, weakness on one side of the body, slurred speech.

Rarely, a very serious problem with your pituitary gland (pituitary apoplexy) may occur, usually in the first hour to 2 weeks after your first injection. Seek immediate medical attention if any of these very serious side effects occur: sudden severe headache, sudden severe mental/mood changes (e.g., severe confusion, difficulty concentrating), vision changes, severe vomiting, fainting.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US -

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Read the Eligard (leuprolide acetate) Side Effects Center for a complete guide to possible side effects »

PRECAUTIONS: Before using leuprolide, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: diabetes, heart disease (such as heart attack), stroke, high cholesterol, family history of sudden cardiac death.

Leuprolide may weaken your bones and increase your risk for bone loss (osteoporosis) if used for a long time. Before using this medication, tell your doctor or pharmacist if you have osteoporosis or if you have any of the following risk factors for osteoporosis: long-term alcohol use, smoking, family history of osteoporosis and broken bones, use of certain medications (e.g., corticosteroids such as prednisone, certain anti-seizure drugs such as phenytoin).

This drug may make you dizzy. Do not drive, use machinery, or do any activity that requires alertness until you are sure you can perform such activities safely. Limit alcoholic beverages.

Leuprolide must not be used during pregnancy. It may harm an unborn baby. If you become pregnant or think you may be pregnant, inform your doctor immediately. Consult your doctor for more details and to discuss reliable forms of birth control. Non-hormonal birth control methods are recommended during treatment with leuprolide.

It is not known if leuprolide passes into breast milk. Because the effects of leuprolide on a nursing infant are unknown, breast-feeding is not recommended. Consult your doctor before breast-feeding.

Disclaimer

Eligard Consumer (continued)

DRUG INTERACTIONS: Your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor or pharmacist first.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use.

Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

OVERDOSE: If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US National Poison Hotline at 1-800-222-1222. Canada residents can call a provincial poison control center.

NOTES: Do not share this medication with others.

Laboratory and/or medical tests (e.g., blood testosterone level, PSA blood test, blood glucose) should be performed periodically to monitor your progress. Consult your doctor for more details.

MISSED DOSE: It is very important that you do not miss any doses. However, if you do miss a dose, contact your doctor promptly to establish a new schedule.

STORAGE: Refrigerate between 36-46 degrees F (2-8 degrees C). Do not freeze. Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-800-854-1166 (USA) or 1-800-668-1507 (Canada).

Information last revised February 2012. Copyright(c) 2012 First Databank, Inc.

Eligard Patient Information Including Side Effects

Brand Names: Eligard, Lupron, Lupron Depot, Lupron Depot-Gyn, Lupron Depot-Ped

Generic Name: leuprolide (Pronunciation: LOO proe lide)

What is leuprolide (Eligard)?

Leuprolide is a man-made form of a hormone that regulates many processes in the body. Leuprolide overstimulates the body's own production of certain hormones, which causes that production to shut down temporarily. Leuprolide reduces the amount of testosterone in men or estrogen in women.

Leuprolide is used in men to treat the symptoms of prostate cancer. Leuprolide treats only the symptoms of prostate cancer and does not treat the cancer itself. Use any other medications your doctor has prescribed to best treat your condition.

Leuprolide is used in women to treat symptoms of endometriosis (overgrowth of uterine lining outside of the uterus) or uterine fibroids.

Leuprolide is also used to treat precocious (early-onset) puberty in both male and female children.

Leuprolide may also be used for purposes not listed in this medication guide.

What are the possible side effects of leuprolide (Eligard)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have a serious side effect such as:

  • bone pain, loss of movement in any part of your body;
  • swelling, rapid weight gain;
  • pain, burning, stinging, bruising, or redness where the medication was injected;
  • feeling like you might pass out;
  • painful or difficult urination;
  • urinating more often than usual;
  • high blood sugar (increased thirst, increased urination, hunger, dry mouth, fruity breath odor, drowsiness, dry skin, blurred vision, weight loss);
  • sudden numbness or weakness (especially on one side of the body), problems with speech or balance;
  • sudden headache with vision problems, vomiting, confusion, slow heart rate, weak pulse, fainting, or slow breathing; or
  • chest pain or heavy feeling, pain spreading to the arm or shoulder, nausea, sweating, general ill feeling.

Rare but serious side effects may include:

  • pain or unusual sensations in your back;
  • numbness, weakness, or tingly feeling in your legs or feet;
  • muscle weakness or loss of use; and
  • loss of bowel or bladder control.

Less serious side effects may include:

  • acne, increased growth of facial hair;
  • breakthrough bleeding in a female child during the first 2 months of leuprolide treatment;
  • dizziness, weakness, tired feeling;
  • hot flashes, night sweats, chills, clammy skin;
  • nausea, diarrhea, constipation, stomach pain;
  • skin redness, itching, or scaling;
  • joint or muscle pain;
  • vaginal itching or discharge
  • breast swelling or tenderness;
  • testicle pain;
  • impotence, loss of interest in sex;
  • depression, sleep problems (insomnia), memory problems; or
  • redness, burning, stinging, or pain where the shot was given.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Read the Eligard (leuprolide acetate) Side Effects Center for a complete guide to possible side effects »

What is the most important information I should know about leuprolide (Eligard)?

You should not breast-feed while you are using leuprolide.

You should not use this medication if you are allergic to leuprolide or similar medications such as buserelin (Suprefact, Suprecor), goserelin (Zoladex), histrelin (Supprelin), or nafarelin (Synarel).

You should not use leuprolide if you have abnormal vaginal bleeding that has not been diagnosed by a doctor.

Before using leuprolide, tell your doctor if you have epilepsy, asthma, migraines, heart or kidney disease, a history of depression, osteoporosis, bone cancer affecting your spine, blood in your urine, or if you are unable to urinate.

Tell your doctor if you have a personal or family history of osteoporosis, or if you have any risk factors for bone loss such as smoking, alcohol use, or taking steroid or seizure medications long term. Long-term use of this medication may decrease bone density, possibly leading to osteoporosis.

Certain brands or strengths of leuprolide are used to treat only men and should not be used in women or children. Always check your medication to make sure you have received the correct brand and strength prescribed by your doctor.

Eligard Patient Information including How Should I Take

What should I discuss with my healthcare provider before using leuprolide (Eligard)?

Certain brands or strengths of leuprolide are used to treat only men and should not be used in women or children. Always check your medication to make sure you have received the correct brand and strength prescribed by your doctor. Ask the pharmacist if you have any questions about the medicine you receive at the pharmacy.

You should not use this medication if you are allergic to leuprolide or similar medications such as buserelin (Suprefact, Suprecor), goserelin (Zoladex), histrelin (Supprelin), nafarelin (Synarel), or if you have:

  • abnormal vaginal bleeding that has not been diagnosed by a doctor; or
  • if you are pregnant or breast-feeding.

Do not breast-feed a baby while using leuprolide.

To make sure you can safely use leuprolide, tell your doctor if you have any of these other conditions:

  • a personal or family history of osteoporosis;
  • risk factors for bone loss such as smoking, alcohol use, or taking steroid or seizure medications long term;
  • diabetes, heart disease, high blood pressure, recent weight gain, high cholesterol (especially in men);
  • epilepsy;
  • asthma;
  • migraines;
  • kidney disease;
  • a history of depression;
  • bone cancer affecting your spine;
  • blood in your urine; or
  • if you are unable to urinate.

FDA pregnancy category X. This medication can cause birth defects. Do not use leuprolide if you are pregnant. Tell your doctor right away if you become pregnant during treatment.

Leuprolide usually causes women to stop ovulating or having menstrual periods. However, you may still be able to get pregnant. Use an effective barrier form of birth control (such as a condom or diaphragm with spermicide gel or inserts). Hormonal forms of contraception (such as birth control pills, injections, implants, skin patches, and vaginal rings) may not be effective in preventing pregnancy while you are using leuprolide.

Because leuprolide is expected to cause your menstrual periods to stop, contact your doctor if your periods continue while you are being treated with this medication.

Long-term use of this medication may decrease bone density, possibly leading to osteoporosis. Talk with your doctor about your possible risk for osteoporosis. You may need to receive a bone scan if you ever need to be re-treated with leuprolide in the future.

How should I use leuprolide (Eligard)?

Leuprolide is injected under the skin or into a muscle. You may be shown how to use injections at home. Do not self-inject this medicine if you do not fully understand how to give the injection and properly dispose of used needles and syringes.

This medication comes with patient instructions for safe and effective use. Follow these directions carefully. Ask your doctor or pharmacist if you have any questions.

Leuprolide may be given once every month or once every 3 to 6 months. How often you receive this medication will depend on the condition being treated. Follow your doctor's instructions.

Because different brands or strengths of leuprolide are used to treat different conditions, it is very important that you receive exactly the brand and strength your doctor has prescribed. If you self-inject this medication at home, always check your medication to make sure you have received the correct brand and type prescribed by your doctor.

Your symptoms may become temporarily worse as your hormones adjust when you first start using this medication. For best results, keep using the medication as instructed by your doctor. Your condition should eventually improve with continued use of leuprolide.

To be sure this medication is helping your condition, your blood may need to be tested often. This will help your doctor determine how long to treat you with leuprolide. You may still need blood tests for up to 3 months after you stop using leuprolide to check your hormone levels and pituitary gland function. Do not miss any scheduled appointments.

Store Lupron in the original carton at room temperature, away from moisture and heat.

Store Eligard in the refrigerator. Do not freeze. You may take the medicine out and allow it to reach room temperature before mixing and injecting your dose. After the dose is mixed, you must use the injection within 30 minutes.

Use a disposable needle only once. Throw away used needles in a puncture-proof container (ask your pharmacist where you can get one and how to dispose of it). Keep this container out of the reach of children and pets.

Eligard Patient Information including If I Miss a Dose

What happens if I miss a dose (Eligard)?

Call your doctor for instructions if you miss a dose.

Women who miss more than one leuprolide dose may have breakthrough bleeding. Children who miss more than one dose may have a return of pubertal symptoms such as breast development, growth in the testicles, or menstrual periods.

What happens if I overdose (Eligard)?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Overdose symptoms may include weakness, or irritation where the leuprolide shot was given.

What should I avoid while using leuprolide (Eligard)?

Follow your doctor's instructions about any restrictions on food, beverages, or activity.

What other drugs will affect leuprolide (Eligard)?

There may be other drugs that can interact with leuprolide. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.

Where can I get more information?

Your pharmacist can provide more information about leuprolide.


Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

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