Lupron Depot 11.25

Last updated on RxList: 8/4/2021
Lupron Depot 11.25 Side Effects Center

What Is Lupron Depot 11.25?

Lupron Depot 11.25 mg (leuprolide acetate for depot suspension) 3-Month Formulation is a man-made form of a hormone that regulates many processes in the body used in men to treat the symptoms of prostate cancer. Lupron Depot 11.25 mg is used in women to treat symptoms of endometriosis (overgrowth of uterine lining outside of the uterus) or uterine fibroids, and is also used to treat precocious (early-onset) puberty in both male and female children.

What Are Side Effects of Lupron Depot 11.25?

Common side effects of Lupron Depot 11.25 mg include:

  • hot flashes (flushing),
  • increased sweating,
  • night sweats,
  • chills,
  • clammy skin,
  • tiredness,
  • headache,
  • upset stomach or stomach pain,
  • nausea,
  • diarrhea,
  • constipation,
  • breast swelling or tenderness,
  • acne,
  • joint or muscle aches or pain,
  • trouble sleeping (insomnia),
  • reduced sexual interest,
  • impotence,
  • vaginal discomfort or dryness,
  • vaginal itching or discharge,
  • abnormal vaginal bleeding (in girls),
  • swelling of the ankles or feet,
  • dizziness,
  • increased growth of facial hair,
  • weakness,
  • skin redness/itching/scaling,
  • testicle pain,
  • depression,
  • memory problems, or
  • injection site reactions (burning, pain, bruising, redness, stinging).

Dosage for Lupron Depot 11.25

When Lupron Depot 11.25 mg is used regularly, it is expected menstrual periods will stop (or decrease to light bleeding/spotting). Menstrual periods usually return within 3 months after treatment with Lupron Depot 11.25 mg is stopped. Tell your doctor if you have serious side effects of Lupron Depot 11.25 mg including:

  • mental/mood changes (e.g., new or worsening depression, thoughts of suicide, mood swings, memory problems, aggression in children),
  • bone pain (in adults), or
  • easily broken bones (in adults).

Lupron Depot 11.25 mg is given in a single dose. Treatment duration depends on the condition being treated.

What Drugs, Substances, or Supplements Interact with Lupron Depot 11.25?

Other drugs may interact with Lupron Depot. Tell your doctor all prescription and over-the-counter medications and supplements you use.

Lupron Depot 11.25 During Pregnancy and Breastfeeding

Lupron Depot must not be used during pregnancy. It may harm a fetus. If you become pregnant or think you may be pregnant, inform your doctor. Consult your doctor to discuss birth control. Non-hormonal birth control methods (e.g., condoms, diaphragm with spermicide) are recommended during treatment. It is unknown if this drug passes into breast milk. Because the effects of on a nursing infant are unknown, breastfeeding is not recommended.

Additional Information

Our Lupron Depot 11.25 mg (leuprolide acetate) Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.

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.

SLIDESHOW

What Is Endometriosis? Symptoms, Causes, Treatment See Slideshow
Lupron Depot 11.25 Consumer Information

Get emergency medical help if you have signs of an allergic reaction (hives, sweating, fast heartbeats, dizziness, difficult breathing, swelling in your face or throat) or a severe skin reaction (fever, sore throat, burning in your eyes, skin pain, red or purple skin rash that spreads and causes blistering and peeling).

Call your doctor at once if you have:

  • problems with your pituitary gland--sudden severe headache, vomiting, problems with your eyes or vision, changes in mood or behavior;
  • bone pain, loss of movement in any part of your body;
  • swelling, rapid weight gain;
  • a seizure;
  • unusual changes in mood or behavior (crying spells, anger, feeling irritable);
  • sudden chest pain or discomfort, wheezing, dry cough or hack;
  • painful or difficult urination; or
  • high blood sugar--increased thirst, increased urination, hunger, dry mouth, fruity breath odor.

Rare but serious side effects may occur. Call your doctor if you have:

  • pain or unusual sensations in your back, numbness, weakness, or tingly feeling in your legs or feet;
  • muscle weakness or loss of use, loss of bowel or bladder control;
  • heart attack symptoms--chest pain or pressure, pain spreading to your jaw or shoulder, nausea, sweating; or
  • signs of a stroke--sudden numbness or weakness (especially on one side of the body), sudden severe headache, slurred speech.

Common side effects may include:

  • pituitary gland problems;
  • cold symptoms such as stuffy nose, sneezing, sore throat, cough with or without mucus;
  • fever, tiredness, not feeling well;
  • stomach pain, nausea, vomiting, constipation;
  • wheezing, chest tightness, trouble breathing;
  • hot flashes, sweating;
  • dizziness, mood changes;
  • headache, general pain;
  • vaginal swelling, itching, or discharge;
  • weight changes;
  • decreased testicle size;
  • decreased interest in sex; or
  • redness, pain, swelling, or oozing 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 entire detailed patient monograph for Lupron Depot 11.25 (Leuprolide Acetate for Depot Suspension)

QUESTION

Endometriosis occurs deep inside the uterus. See Answer
Lupron Depot 11.25 Professional Information

SIDE EFFECTS

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.

LUPRON DEPOT (Monotherapy)

The safety of LUPRON DEPOT 11.25 mg for the endometriosis and fibroids indications was established based on adequate and well-controlled adult studies of LUPRON DEPOT 3.75 mg for 1-month administration and on a single trial of LUPRON DEPOT 11.25 mg. The safety of LUPRON DEPOT 3.75 mg was evaluated in six clinical studies in which a total of 332 women were treated for up to six months. Women were treated with monthly IM injections of LUPRON DEPOT 3.75 mg. The population age range was 18 to 53 years old.

Adverse Reactions (>1%) Leading To Study Discontinuation

In the six studies 1.8% of patients treated with LUPRON DEPOT 3.75 mg discontinued prematurely due to hot flashes.

Common Adverse Reactions

LUPRON DEPOT 3.75 mg was utilized in controlled clinical trials that studied the drug in 166 endometriosis and 166 uterine fibroids patients. Adverse reactions reported in ≥ 5% of patients in either of these populations are noted in the following tables.

Table 2: Adverse Reactions Reported in ≥ 5% of Patients Taking LUPRON DEPOT-Endometriosis (2 Studies)

  LUPRON DEPOT 3.75 mg
N=166
%
Danazol
N=136
%
Placebo
N=31
%
Hot flashes/sweats* 84 57 29
Headache* 32 22 6
Vaginitis* 28 17 0
Depression/emotional lability* 22 20 3
General pain 19 16 3
Weight gain/loss 13 26 0
Nausea/vomiting 13 13 3
Decreased libido* 11 4 0
Dizziness 11 3 0
Acne 10 20 0
Skin reactions 10 15 3
Joint disorder* 8 8 0
Edema 7 13 3
Paresthesias 7 8 0
GI disturbances* 7 6 3
Neuromuscular disorders* 7 13 0
Breast changes/tenderness/pain* 6 9 0
Nervousness* 5 8 0
In these same studies, symptoms reported in < 5% of patients included: Body as a Whole -Injection site reactions; Cardiovascular System -Palpitations, Syncope, Tachycardia; Digestive System -Appetite changes, Dry mouth, Thirst; Endocrine System -Androgen-like effects; Hemic and Lymphatic System -Ecchymosis; Nervous System -Anxiety*, Insomnia/Sleep disorders*, Delusions, Memory disorder, Personality disorder; Skin and Appendages -Alopecia, Hair disorder; Special Senses -Ophthalmologic disorders*; Urogenital System -Dysuria*, Lactation.
* = Possible effect of decreased estrogen.

Table 3: Adverse Reactions Reported in ≥ 5% of Patients -Uterine Fibroids (4 Studies)

  LUPRON DEPOT 3.75 mg
N=166
%
Placebo
N=163
%
Hot flashes/sweats* 73 18
Headache* 26 18
Vaginitis* 11 2
Depression/emotional lability* 11 4
Asthenia 8 5
General pain 8 6
Joint disorder* 8 3
Edema 5 1
Nausea/vomiting 5 4
Nervousness* 5 1
In these same studies, symptoms reported in < 5% of patients included: Body as a Whole -Body odor, Flu syndrome, Injection site reactions; Cardiovascular System -Tachycardia; Digestive System -Appetite changes, Dry mouth; Endocrine System -Androgen-like effects; Nervous System -Anxiety*, Insomnia/Sleep disorders*; Respiratory System -Rhinitis; Skin and Appendages -Nail disorder; Special Senses -Conjunctivitis, Taste perversion; Urogenital System -Menstrual disorders.
* = Possible effect of decreased estrogen.

In one controlled clinical trial utilizing the monthly formulation of LUPRON DEPOT, patients diagnosed with uterine fibroids received a higher dose (7.5 mg) of LUPRON DEPOT. Adverse reactions seen with this dose that were not seen at the lower dose included galactorrhea, pyelonephritis, and urinary incontinence. Generally, a higher incidence of hypoestrogenic effects was observed at the higher dose.

In a pharmacokinetic trial involving 20 healthy female subjects receiving LUPRON DEPOT 11.25 mg, a few adverse reactions were reported with this formulation that were not reported previously, including face edema.

In a phase 4 study involving endometriosis patients receiving LUPRON DEPOT 3.75 mg (N=20) or LUPRON DEPOT 11.25 mg (N=21), similar adverse reactions were reported by the two groups of patients. In general the safety profiles of the two formulations were comparable in this study.

LUPRON DEPOT With Norethindrone Acetate Add-back Therapy

The safety of co-administering LUPRON DEPOT and norethindrone acetate was evaluated in two clinical studies in which a total of 242 women with endometriosis were treated for up to one year. Women were treated with monthly IM injections of leuprolide acetate 3.75 mg (13 injections) alone or monthly IM injections of leuprolide acetate 3.75 mg (13 injections) plus 5 mg norethindrone acetate daily. The population age range was 17-43 years old. The majority of patients were Caucasian (87%).

One study was a controlled clinical trial in which 106 women were randomized to one year of treatment with LUPRON DEPOT alone or with LUPRON DEPOT and norethindrone acetate. The other study was an open-label single arm clinical study in 136 women of one year of treatment with LUPRON DEPOT plus norethindrone acetate, with follow-up for up to 12 months after completing treatment.

Adverse Reactions (>1%) Leading To Study Discontinuation

In the controlled study, 18% of patients treated monthly with LUPRON DEPOT and 18% of patients treated monthly with LUPRON DEPOT plus norethindrone acetate discontinued therapy due to adverse reactions, most commonly hot flashes (6%) and insomnia (4%) in the LUPRON DEPOT alone group and hot flashes and emotional lability (4% each) in the LUPRON DEPOT plus norethindrone group.

In the open label study, 13% of patients treated monthly with LUPRON DEPOT plus norethindrone acetate discontinued therapy due to adverse reactions, most commonly depression (4%) and acne (2%).

Common Adverse Reactions

Table 4 lists the adverse reactions observed in at least 5% of patients in any treatment group, during the first 6 months of treatment in the two add-back clinical studies, in which patients were treated with monthly LUPRON DEPOT 3.75 mg with or without norethindrone acetate co-treatment. The most frequently-occurring adverse reactions observed in these studies were hot flashes and headaches.

Table 4: Adverse Reactions Occurring in the First Six Months of Treatment in ≥ 5% of Patients with Endometriosis

Adverse Reactions Controlled Study Open Label Study
LD-Only*
N=51
%
LD/N†
N=55
%
LD/N†
N=136
%
Any Adverse Reaction 98 96 93
Hot flashes/Sweats 98 87 57
Headache/Migraine 65 51 46
Depression/Emotional Lability 31 27 34
Insomnia/Sleep Disorder 31 13 15
Nausea/Vomiting 25 29 13
Pain 24 29 21
Vaginitis 20 15 8
Asthenia 18 18 11
Dizziness/Vertigo 16 11 7
Altered Bowel Function (constipation, diarrhea) 14 15 10
Weight Gain 12 13 4
Decreased Libido 10 4 7
Nervousness/Anxiety 8 4 11
Breast Changes/Pain/Tenderness 6 13 8
Memory Disorder 6 2 4
Skin/Mucous Membrane Reaction 4 9 11
GI Disturbance (dyspepsia, flatulence) 4 7 4
Androgen-Like Effects (acne, alopecia) 4 5 18
Changes in Appetite 4 0 6
Injection Site Reaction 2 9 3
Neuromuscular Disorder (leg cramps, paresthesia) 2 9 3
Menstrual Disorders 2 0 5
Edema 0 9 7
* LD-Only = LUPRON DEPOT 3.75 mg
† LD/N = LUPRON DEPOT 3.75 mg plus norethindrone acetate 5 mg

In the controlled clinical trial, 50 of 51 (98%) patients in the LUPRON DEPOT 3.75 mg arm and 48 of 55 (87%) patients in the LUPRON DEPOT 3.75 mg plus norethindrone acetate arm reported experiencing hot flashes on one or more occasions during treatment.

Table 5 presents hot flash data in the last month of treatment.

Table 5: Hot Flashes in the Month Prior to the Assessment Visit (Controlled Study)

Assessment Visit Treatment Group Number of Patients Reporting Hot Flashes Number of Days with Hot Flashes Maximum Number Hot Flashes in 24 Hours
N (%) N2 Mean N2 Mean
Week 24 LD-Only* 32/37 86 37 19 36 5.8
LD/N† 22/38 581 38 71 38 1.91
* LD-Only = LUPRON DEPOT 3.75 mg
† LD/N = LUPRON DEPOT 3.75 mg plus norethindrone acetate 5 mg
1Statistically significantly less than the LD-Only group (p<0.01)
2Number of patients assessed.

Serious Adverse Reactions

Urinary tract infection, renal calculus, depression

Changes In Laboratory Values during Treatment

Liver Enzymes

Three percent of uterine fibroid patients treated with LUPRON DEPOT 3.75 mg for 1-month administration, manifested post-treatment transaminase values that were at least twice the baseline value and above the upper limit of the normal range. None of the laboratory increases were associated with clinical symptoms.

In the two clinical trials of women with endometriosis, 4 of 191 patients receiving leuprolide acetate plus norethindrone acetate for up to 12 months developed an elevated (at least twice the upper limit of normal) SGPT and 2 of 136 developed an elevated GGT. Five of the 6 increases were observed beyond 6 months of treatment. None was associated with an elevated bilirubin concentration.

Lipids

Triglycerides were increased above the upper limit of normal in 12% of the endometriosis patients who received LUPRON DEPOT 3.75 mg and in 32% of the subjects receiving LUPRON DEPOT 11.25 mg.

Of those endometriosis and uterine fibroid patients whose pretreatment cholesterol values were in the normal range, mean change following therapy was +16 mg/dL to +17 mg/dL in endometriosis patients and +11 mg/dL to +29 mg/dL in uterine fibroid patients. In the endometriosis patients, increases from the pretreatment values were statistically significant (p<0.03). There was essentially no increase in the LDL/HDL ratio in patients from either population receiving LUPRON DEPOT 3.75 mg.

Percent changes from baseline for serum lipids and percentages of patients with serum lipid values outside of the normal range in the two studies of leuprolide acetate and norethindrone acetate are summarized in the tables below. The major impact of adding norethindrone acetate to treatment with LUPRON DEPOT was a decrease in serum HDL cholesterol and an increase in the LDL/HDL ratio.

Table 6: Serum Lipids: Mean Percent Changes From Baseline Values at Treatment Week 24

  LUPRON DEPOT 3.75 mg LUPRON DEPOT 3.75 mg plus norethindrone acetate 5 mg daily
Controlled Study
(n=39)
Controlled Study
(n=41)
Open Label Study
(n=117)
Baseline Value* Wk 24 % Change Baseline Value* Wk 24 % Change Baseline Value* Wk 24 % Change
Total Cholesterol 170.5 9.2% 179.3 0.2% 181.2 2.8%
HDL Cholesterol 52.4 7.4% 51.8 -18.8% 51.0 -14.6%
LDL Cholesterol 96.6 10.9% 101.5 14.1% 109.1 13.1%
LDL/HDL Ratio 2.0† 5.0% 2.1† 43.4% 2.3† 39.4%
Triglycerides 107.8 17.5% 130.2 9.5% 105.4 13.8%
* mg/dL
† ratio

Changes from baseline tended to be greater at Week 52. After treatment, mean serum lipid levels from patients with follow up data returned to pretreatment values.

Table 7: Percentage of Patients with Serum Lipids Values Outside of the Normal Range

LUPRON DEPOT 3.75 mg LUPRON DEPOT 3.75 mg plus norethindrone acetate 5 mg daily
Controlled Study
(n=39)
Controlled Study
(n=41)
Open Label Study
(n=117)
Wk 0 Wk 24* Wk 0 Wk 24* Wk 0 Wk 24*
Total Cholesterol (>240 mg/dL) 15% 23% 15% 20% 6% 7%
HDL Cholesterol (<40 mg/dL) 15% 10% 15% 44% 15% 41%
LDL Cholesterol (>160 mg/dL) 0% 8% 5% 7% 9% 11%
LDL/HDL Ratio (>4.0) 0% 3% 2% 15% 7% 21%
Triglycerides (>200 mg/dL) 13% 13% 12% 10% 5% 9%
* Includes all patients regardless of baseline value.

Postmarketing Experience

The following adverse reactions have been identified during post-approval use of LUPRON DEPOT monotherapy or LUPRON DEPOT with norethindrone acetate add-back therapy. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

During postmarketing surveillance with other dosage forms and in the same or different populations, the following adverse reactions were reported:

  • Allergic reactions (anaphylactic, rash, urticaria, and photosensitivity reactions)
  • Mood swings, including depression
  • Suicidal ideation and attempt
  • Symptoms consistent with an anaphylactoid or asthmatic process
  • Localized reactions including induration and abscess at the site of injection
  • Symptoms consistent with fibromyalgia (e.g., joint and muscle pain, headaches, sleep disorders, gastrointestinal distress, and shortness of breath), individually and collectively

Other adverse reactions reported are:

Hepato-biliary disorder -Serious liver injury

Injury, poisoning and procedural complications -Spinal fracture

Investigations -Decreased white blood count

Musculoskeletal and connective tissue disorder -Tenosynovitis-like symptoms

Nervous System disorder -Convulsion, peripheral neuropathy, paralysis

Vascular disorder -Hypotension, Hypertension

Serious venous and arterial thrombotic and thromboembolic reactions have been reported, including deep vein thrombosis, pulmonary embolism, myocardial infarction, stroke, and transient ischemic attack

Pituitary Apoplexy

During post-marketing surveillance, cases of pituitary apoplexy (a clinical syndrome secondary to infarction of the pituitary gland) have been reported after the administration of leuprolide acetate and other GnRH 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 entire FDA prescribing information for Lupron Depot 11.25 (Leuprolide Acetate for Depot Suspension)

© Lupron Depot 11.25 Patient Information is supplied by Cerner Multum, Inc. and Lupron Depot 11.25 Consumer information is supplied by First Databank, Inc., used under license and subject to their respective copyrights.

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