Lupron Depot

Lupron Depot is used to treat advanced prostate cancer, endometriosis, uterine fibroids, and central precocious puberty (CPP) (Lupron Depot-Ped only). It is a long-acting hormone injection given intramuscularly every 1, 3, 4, or 6 months, depending on the condition.

Lupron Depot works by suppressing the body's production of certain hormones through a process called "chemical castration" or "medical castration." When first administered, it briefly stimulates the pituitary gland to release luteinizing hormone (LH) and follicle-stimulating hormone (FSH). With continuous use, Lupron causes desensitization and down-regulation of GnRH receptors in the pituitary gland. The reduction in LH and FSH leads to significantly decreased production of sex hormones (testosterone in men, estrogen in women). Lupron belongs to the drug class called gonadotropin-releasing hormone (GnRH) agonists.

Lupron Depot (leuprolide acetate) first gained FDA approval on April 9, 1985. Lupron Depot-Ped was approved on April 16, 1993. There is no generic.

Lupron Depot is approved for:

• advanced prostate cancer
• endometriosis, to manage pain and reduce endometriotic lesions. May be used alone or in combination with norethindrone acetate (this is called add-back therapy) to reduce bone loss and hot flashes associated with Lupron depot use. The total duration of add-back therapy should not exceed 12 months.
• uterine leiomyomatas (fibroids), to improve anemia due to vaginal bleeding in combination with iron therapy in patients in whom 3 months of hormonal suppression is deemed necessary. The duration of treatment is limited to 3 months. The symptoms associated with fibroids will return after stopping therapy. Healthcare providers may consider a 1-month trial of iron alone, as some women will respond to iron alone. Lupron Depot may be added if the response to iron alone is inadequate.

Lupron Depot-Ped is approved for:

• central precocious puberty (CPP) in children aged 1 year and older.

Initially, Lupron Depot must be administered under the supervision of a healthcare provider, although some people can be taught how to self-administer it themselves.

• Lupron Depot is given into a muscle.
• The dosing schedule varies depending on the condition being treated, but it may be every 1, 3, 4, or 6 months.

Different brands or strengths of leuprolide are used to treat different conditions.

• Always check your medication to make sure you have received the correct brand and type prescribed by your doctor.

You may need frequent medical tests while using this medicine.

Keep all scheduled visits to the doctor. If a scheduled dose is missed, the person receiving Lupron Depot or Lupron Depot-Ped may start having symptoms or signs of puberty again.

• Your healthcare provider will do regular exams and blood tests.

Do not use Lupron Depot or Lupron Depot-Ped if you are allergic to leuprolide or similar medicines such as buserelin, goserelin, histrelin, or nafarelin; Lupron Depot, Lupron Depot-Ped, any of the inactive ingredients in the injection, or if you have abnormal vaginal bleeding that a doctor has not checked.

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

To make sure Lupron Depot is safe for you, tell your healthcare provider about all your medical conditions, including if you have ever had:

• depression, mental illness, or psychosis
• seizures or epilepsy
• a blood vessel disorder
• a brain tumor or spinal cord injury
• heart disease, congestive heart failure, long QT syndrome
• an electrolyte imbalance (such as low levels of potassium or magnesium in your blood) or
• risk factors for bone loss (personal or family history of osteoporosis, smoking, alcohol use, taking steroid or seizure medicines long term).

Call your doctor if your periods continue while you are being treated with this medicine.

Do not give this medicine to any child without medical advice.

Pregnancy and Breastfeeding

Lupron Depot usually causes women to stop ovulating or having menstrual periods. However, you may still be able to get pregnant. Leuprolide can cause birth defects and should not be used if you are pregnant. Use a condom or diaphragm with spermicide to prevent pregnancy because leuprolide can make hormonal birth control less effective. Tell your doctor right away if you inadvertently become pregnant.

You should not breastfeed while using leuprolide.

Leuprolide may cause infertility, although research shows full reversibility of fertility suppression when leuprolide is discontinued after continuous administration for up to 24 weeks. Lupron may be used to delay egg release for IVF treatment.

Common side effects

The most common side effects of Lupron Depot in prostate cancer are:

• general pain and joint problems
• hot flashes or body sweats
• gastrointestinal disturbances
• swelling and fluid build-up (edema)
• respiratory problems
• urinary problems
• injection site reactions, such as redness, swelling, or pain at the injection site
• shrinking of the testes
• weakness, lack of energy, or fatigue
• skin reactions.

The most common side effects of Lupron Depot in endometriosis or uterine fibroids are:

• hot flashes or body sweats
• headache or migraine
• vaginal inflammation with vaginal itching, discharge, or pain
• depression or mood swings
• general pain
• weight gain/loss
• nausea or vomiting
• decreased sex drive
• dizziness.

The most common side effects of Lupron Depot-Ped in central precocious puberty are:

• injection site reactions such as pain, swelling, and abscess
• weight gain
• pain throughout the body, including the upper stomach and chest
• headache
• acne or red, itchy rash, and white scales (seborrhea)
• serious skin rash (erythema multiforme)
• mood changes
• swelling of the vagina (vaginitis), vaginal bleeding, and vaginal discharge
• bleeding
• diarrhea
• nausea and vomiting
• fever
• ligament sprain
• fracture
• breast tenderness
• difficulty sleeping
• excessive sweating.

Serious side effects and warnings

Lupron Depot and Lupron Depot-Ped may cause the following serious side effects:

• Temporarily worse symptoms. Your symptoms may become temporarily worse during the first 2 to 4 weeks of treatment when you first start using Lupron Depot. In adults with prostate cancer, increases in serum testosterone of more than 50% above baseline may cause a tumor flare. Tell your healthcare provider immediately if you develop increased bone pain, nerve pain, blood in your urine, difficulty urinating, or spinal pain.

In women prescribed Lupron Depot for endometriosis or uterine fibroids, it may cause transient worsening of these symptoms for the first few weeks of treatment. In children, there may be a temporary increase in the clinical signs and symptoms of puberty, including vaginal bleeding. Tell your doctor if any increase in symptoms continues for longer than 2 months.

• Cardiovascular disease. There is an increased risk of serious cardiovascular problems, including heart attacks, sudden cardiac death, and strokes, in men receiving Lupron Depot. Your doctor will monitor your heart health more closely while you're on this medication. Tell your healthcare provider immediately if you experience chest pain or pressure, shortness of breath, or sudden weakness or numbness, especially on one side of the body.
• QT/QTc interval prolongation: Androgen deprivation therapy may prolong the QT interval. Your healthcare provider will weigh up your risks and benefits.
• Increased risk of seizures. The risk of seizures may be higher in people who have a history of seizures, a history of epilepsy, a history of brain or brain vessel (cerebrovascular) problems or tumors, or who are taking a medicine that has been connected to seizures, such as bupropion or selective serotonin reuptake inhibitors (SSRIs). Seizures have also happened in people without any of these problems. Call your healthcare provider right away if you, your child, or the person you are caring for has a seizure while taking Lupron Depot or Lupron Depot-Ped.
• Psychiatric events or mood changes, such as emotional lability (eg, crying, irritability, impatience, anger, and aggression) have been reported with Lupron Depot. Call your healthcare provider at once if you, your child, or someone you are caring for has unusual changes in mood or behavior.
• Increased pressure in the fluid around the brain (Pseudotumor Cerebri) can happen in people receiving GnRH agonist medicines such as Lupron Depot or Lupron Depot-Ped. Call your healthcare provider right away if you, your child, or the person you are caring for has any of the following symptoms during treatment: headache eye problems, including blurred vision, double vision, or decreased eyesight eye pain ringing in the ears dizziness nausea.
• Increased risk of diabetes and other metabolic conditions. People receiving GnRH agonists such as Lupron Depot have a higher risk of developing high blood sugar levels, diabetes, high cholesterol, and non-alcoholic fatty liver disease. Your doctor will monitor you for these.
• Allergic reactions. Get emergency medical help if you develop signs of an allergic reaction, such as hives, sweating, fast heartbeats, dizziness, difficulty breathing, or swelling in your face or throat.
• Serious skin reactions, including Stevens-Johnson syndrome/toxic epidermal necrolysis (SJS/TEN), have occurred in patients treated with Lupron Depot. Seek urgent medical attention if you develop a red or purple skin rash that spreads, blistering on your skin or inside your mouth or nose, or peeling skin that may be accompanied by fever.

Lupron Depot can harm an unborn baby or cause birth defects. Do not use it if you are pregnant or breastfeeding.

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 the FDA at 1-800-FDA-1088.

Dose of Lupron Depot for advanced prostate cancer:

Dose of Lupron Depot for endometriosis

Lupron Depot 3.75 mg administered as a single intramuscular (IM) injection once every month for up to six injections (6 months of therapy).

• May be administered alone or in combination with daily norethindrone acetate 5 mg (add-back treatment)
• If endometriosis symptoms recur after the initial course of therapy, retreatment for no more than six months may be considered, but only with the addition of norethindrone acetate add-back therapy. Do not re-treat with Lupron Depot 3.75 mg alone.

Dose of Lupron Depot for uterine fibroids

• Lupron Depot 3.75 mg is administered as a single intramuscular (IM) injection once every month for up to three injections (3 months of therapy).

Dose of Lupron Depot-Ped for central precocious puberty (CPP)

The dosage of Lupron Depot-Ped must be individualized for each child. Dosage recommendations are based on body weight.

• Adjust dosages as body weight changes.
• The dosage may be increased if adequate hormonal and clinical suppression is not achieved.
• Your healthcare provider will monitor your child's response to Lupron Depot-Ped.

Dosage Lupron Depot-Ped for 1-month administration

• Administer Lupron Depot-Ped 7.5 mg, 11.25 mg, or 15 mg for 1-month administration as a single-dose intramuscular injection once every month.

Dosage Lupron Depot-Ped for 3-month administration

• Administer Lupron Depot-Ped 11.25 mg or 30 mg for 3-month administration as a single-dose intramuscular injection once every 3 months (12 weeks).

Dosage Lupron Depot-Ped for 6-month administration

• Administer Lupron Depot-Ped 45 mg for 6-month administration as a single-dose intramuscular injection once every 6 months (24 weeks).

Call your doctor for instructions if you miss a dose.

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

Leuprolide can cause serious heart problems. Your risk may be higher if you also use certain other medicines for infections, asthma, heart problems, high blood pressure, depression, mental illness, cancer, malaria, or HIV.

Other drugs may interact with leuprolide, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell your doctor about all your current medicines and any medicine you start or stop using.

Store Lupron Depot and Lupron Depot-Ped in the original carton at room temperature, away from moisture and heat. Protect from light.

Keep out of reach of children.

Depot refers to the delivery system, which makes it long-lasting. The medication is suspended in microspheres that slowly break down over 1-6 months.

Lupron Depot 3.75 mg for 1-month administration

Active ingredients: leuprolide acetate 3.75 mg Inactive Ingredients: acetic acid, water for injection, polysorbate 80, mannitol, purified gelatin, carboxymethylcellulose sodium,

Lupron Depot 7.5mg for 1-month administration

Active ingredients: leuprolide acetate 7.5 mg

Inactive ingredients: purified gelatin, DL-lactic and glycolic acids copolymer, D-mannitol, carboxymethylcellulose sodium, polysorbate 80, water for injection, USP, glacial acetic acid, USP to control pH.

Lupron Depot 22.5 mg for 3-month administration

Active ingredients: leuprolide acetate 22.5 mg

Inactive ingredients: polylactic acid, D-mannitol, carboxymethylcellulose sodium, polysorbate 80, water for injection, USP, and glacial acetic acid, USP to control pH.

Lupron Depot 30 mg for 4-month administration

Active ingredients: leuprolide acetate 30 mg

Inactive ingredients: polylactic acid, D-mannitol, carboxymethylcellulose sodium, polysorbate 80, water for injection, USP, and glacial acetic acid, USP to control pH.

Lupron Depot 45 mg for 6-month administration

Active ingredients: leuprolide acetate 45 mg

Inactive ingredients: polylactic acid, D-mannitol, stearic acid, carboxymethylcellulose sodium, polysorbate 80, water for injection, USP, and glacial acetic acid, USP to control pH.

Lupron Depot-Ped ingredients

Lupron Depot-PED 7.5 mg, 11.25 mg, or 15 mg for 1-month administration: Active Ingredients: leuprolide acetate for depot suspension Inactive Ingredients: purified gelatin, DL-lactic and glycolic acids copolymer, D-mannitol, carboxymethylcellulose sodium, polysorbate 80, water for injection, USP, and glacial acetic acid, USP to control pH.

Lupron Depot-Ped 11.25 mg or 30 mg for 3-month administration: Active Ingredients: leuprolide acetate for depot suspension Inactive Ingredients: polylactic acid, D-mannitol, carboxymethylcellulose sodium, polysorbate 80, water for injection, USP, and glacial acetic acid, USP to control pH.

Lupron Depot-Ped 45 mg for 6-month administration: Active Ingredients: leuprolide acetate for depot suspension Inactive Ingredients: polylactic acid, D-mannitol, stearic acid, carboxymethylcellulose sodium, Dmannitol, polysorbate 80, water for injection, USP, and glacial acetic acid, USP to control pH.

AbbVie Inc. makes Lupron Depot and Lupron Depot-Ped. AbbVie is headquartered in North Chicago, Illinois, USA. It was formed in 2013 when AbbVie split off from Abbott Laboratories.