Pronunciation: loo-pron dep-oh
Generic name: leuprolide acetate for depot suspension
Other brand names of leuprolide acetate for depot suspension include: Lupron Depot, Lupron Depot-Ped
Dosage form: injectable injection
Drug classes: Gonadotropin releasing hormones , Hormones / antineoplastics
What is Lupron Depot?
Lupron Depot is a long-acting, prescription hormonal injection used to treat various hormone-related conditions, such as advanced prostate cancer, endometriosis, uterine fibroids, and central precocious puberty (CPP) in children (Lupron Depot-Ped only).
- Lupron Depot and Lupron Depot-Ped are given by injection every 1, 3, 4, or 6 months depending on the condition.
- Lupron Depot-Ped is only for CPP.
- “Depot” refers to the delivery system. The medication is suspended in microspheres that slowly break down over 1-6 months.
Lupron Depot (leuprolide acetate) first gained FDA approval on April 9, 1985. There is no generic.
FDA approvals and indications
Lupron Depot is approved for advanced prostate cancer, endometriosis, and uterine fibroids.
Advanced prostate cancer
The treatment of advanced prostate cancer.
Endometriosis
The management of endometriosis, including pain relief and reduction of endometriotic lesions.
- May be used alone or in combination with norethindrone acetate (add-back therapy) to reduce bone loss and hot flashes associated with Lupron depot use.
- The total duration of treatment should not exceed 12 months.
Uterine Fibroids
To improve anemia due to vaginal bleeding from uterine fibroids (uterine leiomyomata) 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.
Central Precocious Puberty
Lupron Depot-Ped is approved to treat children aged at least 1 year with central precocious puberty (CPP).
Side effects
Prostate Cancer
The most common side effects of Lupron Depot 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.
Endometriosis or Uterine Fibroids
The most common side effects of Lupron Depot 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.
Central Precocious Puberty
The most common side effects of Lupron Depot-Ped are:
- injection site reactions such as pain, swelling, and abscess
- weight gain
- pain throughout body
- 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.
When Lupron Depot-Ped is administered once every 6 months, other common side effects include upper stomach pain, bleeding, diarrhea, nausea and vomiting, fever, itching, pain, rash, ligament sprain, fracture, breast tenderness, difficulty sleeping, chest pain, and excessive sweating.
Serious side effects and warnings
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 adults or children prescribed Lupron Depot for other conditions this may cause transient worsening of symptoms, including the signs and symptoms of endometriosis or uterine fibroids during 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.
May be associated with an increased risk of seizures. The risk of seizures may be higher in people who have a history of seizures, have a history of epilepsy, have a history of brain or brain vessel (cerebrovascular) problems or tumors, 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.
May increase the risk of psychiatric events or mood changes, such as emotional lability (eg, crying, irritability, impatience, anger, and aggression). 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.
There is an increased risk of developing diabetes in people receiving GnRH agonists such as Lupron Depot. Your doctor will monitor your blood glucose level and manage any changes according to guidelines.
Lupron Depot can harm an unborn baby or cause birth defects. Do not use it if you are pregnant or breastfeeding.
Lupron Depot or Lupron Depot-Ped may cause an allergic reaction. Get emergency medical help if you develop signs of an allergic reaction such as hives, sweating, fast heartbeats, dizziness, difficulty breathing, swelling in your face or throat, or a severe skin reaction which may include a red or purple skin rash that spreads and causes blistering and peeling.
Also, call your healthcare provider at once if you have:
- A sudden severe headache
- A wheezing, dry cough, or hack
- Bone pain
- Heart attack symptoms – chest pain or pressure, pain spreading to your jaw or shoulder, nausea, sweating; or
- High blood sugar, symptoms may include increased thirst, increased urination, hunger, dry mouth, or fruity breath odor
- Loss of movement in any part of your body
- Muscle weakness or loss of use, loss of bowel or bladder control
- Pain or unusual sensations in your back, numbness, weakness, or tingly feeling in your legs or feet
- Painful or difficult urination
- Problems with your eyes or vision
- Rapid weight gain
- Signs of a stroke – sudden numbness or weakness (especially on one side of the body), sudden severe headache, slurred speech
- Sudden chest pain or discomfort
- Swelling
- Unusual changes in mood or behavior (crying spells, anger, feeling irritable)
- Vomiting.
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.
How does Lupron Depot work?
Lupron Depot (leuprolide acetate) works by suppressing the body’s production of certain hormones through a process called “chemical castration” or “medical castration.” This creates a temporary state of low sex hormones, which can be beneficial for treating conditions that are stimulated or worsened by these hormones.
Mechanism of Action: Lupron is a gonadotropin-releasing hormone (GnRH) agonist. When first administered, it briefly stimulates the pituitary gland to release luteinizing hormone (LH) and follicle-stimulating hormone (FSH).
Down-regulation: With continuous use, Lupron causes desensitization and down-regulation of GnRH receptors in the pituitary gland. This leads to a dramatic decrease in the production of LH and FSH.
Hormone Suppression: The reduction in LH and FSH leads to significantly decreased production of sex hormones (testosterone in men, estrogen in women).
- In men: Testosterone levels drop significantly
- In women: Estrogen levels decrease substantially.
Before taking this medicine
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.
How is Lupron administered?
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 Depote-Ped may start having symptoms or signs of puberty again.
- Your healthcare provider will do regular exams and blood tests.
Lupron Depot Dosage
Lupron Depot dosage for advanced prostate cancer:
| Lupron Depot Recommended Dosing for Advanced Prostate Cancer | ||||
| Dosage | 7.5 mg for 1-Month Administration | 22.5 mg for 3-Month Administration | 30 mg for 4-Month Administration | 45 mg for 6-Month Administration |
| Recommended dose | 1 injection every 4 weeks | 1 injection every 12 weeks | 1 injection every 16 weeks | 1 injection every 24 weeks |
Lupron Depot dosage 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.
Lupron Depot dosage 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).
Lupron Depot-Ped dosage 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.
| Body Weight | Once Monthly Lupron Depot-Ped Dosage |
| Less than or equal to 25 kg | 7.5 mg |
| Greater than 25 kg up to 37.5 kg | 11.25 mg |
| Greater than 37.5 kg | 15 mg |
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).
What happens if I miss a dose?
Call your doctor for instructions if you miss a dose.
What should I avoid while using Lupron Depot?
Follow your doctor’s instructions about any restrictions on food, beverages, or activity.
What other drugs will affect Lupron Depot?
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.
Storage
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.
Ingredients
Lupron Depot ingredients
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, and stearic acid, carboxymethylcellulose sodium, Dmannitol, polysorbate 80, water for injection, USP, and glacial acetic acid, USP to control pH.
Who makes Lupron Depot and Lupron Depot-Ped?
AbbVie Inc. makes Lupron Depot and Lupron Depot-Ped. AbbVie is headquartered in North Chicago, Illinois, USA. It was formed in 2013 when it split off from Abbott Laboratories as an independent biopharmaceutical company.
