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Lupron Depot: 7 things you should know

Medically reviewed by Carmen Fookes, BPharm. Last updated on Feb 17, 2022.

1. How it works

  • Lupron Depot is a brand (trade) name for leuprolide acetate which is a hormone deprivation treatment that may be used for the palliative care of advanced prostate cancer.
  • Leuprolide acetate is a gonadotropin-releasing hormone (GnRH) agonist. GnRH is produced by the hypothalamus and acts on the surface of gonadotropin cells in the pituitary gland stimulating the release of luteinizing hormone (LH) and follicular stimulating hormone (FSH), which stimulates the production and release of testosterone by the male testes. GnRH is typically released in pulses and is regulated by circulating levels of testosterone in men. Infusions of leuprolide acetate initially produce a transient increase in testosterone, but with continued non-pulsatile stimulation, LH and FSH synthesis are inhibited and testosterone levels decline. This causes a profound decrease in circulating testosterone, atrophy of the testes, and inhibition of the growth of hormone-dependent tumors, such as prostate cancer.
  • Lupron Depot belongs to the class of medications known as gonadotropin-releasing hormone agonists. Lupron Depot may also be known as androgen deprivation therapy.

2. Upsides

  • May be used for the palliative treatment of advanced prostate cancer.
  • Causes a profound inhibition of testosterone synthesis.
  • Slows tumor progression with a complete or partial response in most men.

3. Downsides

If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:

  • Hot flashes/sweats, general pain, gastrointestinal problems, urinary problems, edema, mood swings, and respiratory disorders are the most common side effects reported.
  • As a result of the physiologic effects of Lupron Depot, men may also experience a decrease in their libido, impotence, and testicular atrophy. May impair fertility in males with reproductive potential.
  • Changes in laboratory tests (such as low hemoglobin or increased cholesterol) have been reported but it is difficult to assess their relationship to Lupron Depot treatment.
  • Requires intramuscular injection once every 4 (7.5mg),12 (22.5mg), 16 (30mg), or 24 (45mg) weeks depending on the dosage.
  • Only available as a brand-name medication, not as a generic.
  • Must be administered by a healthcare professional.
  • The injection should be inspected before reconstitution and should not be used if caking or clumping is evident. A thin layer of powder on the wall of the syringe is considered normal before mixing. The diluent should be clear and colorless. See the product information for full reconstitution instructions.
  • The injection needs to be reconstituted before administration and the whole contents of the injection given as a single intramuscular injection within two hours of reconstitution or discarded because Lupron Depot does not contain a preservative. The injection should be administered at a 90-degree angle into the gluteal area, the anterior thigh, or deltoid. Rotate injection sites.
  • Rarely may cause pituitary apoplexy (a syndrome secondary to infarction of the pituitary gland) hypersensitivity reactions and anaphylaxis.
  • Initially causes an increase in serum testosterone levels to approximately 50% above baseline during the first few weeks of treatment with a transient worsening of symptoms including bone pain. This is known as a tumor flare. Rarely, ureteral obstruction and spinal cord compression have occurred which may contribute to paralysis. Monitor men with metastatic vertebral lesions or urinary tract obstruction during the first few weeks of therapy.
  • Men receiving Lupron Depot are at increased risk of developing diabetes or experiencing a worsening of their blood sugar control if they already have diabetes. Blood glucose and HbA1c levels should be monitored periodically.
  • Men receiving Lupron Depot are at increased risk of cardiovascular disease including myocardial infarction, sudden cardiac death, and stroke. Monitor for signs and symptoms of cardiovascular disease.
  • Androgen deprivation therapy may prolong the QT/QTc interval. Correct electrolyte abnormalities before treatment and weigh up risk vs benefits of Lupron Depot in men at higher risk for QT interval prolongation, such as those with congenital long QT syndrome, congestive heart failure, frequent electrolyte abnormalities, and taking other medications known to also prolong the QT interval.
  • May increase the risk of seizures. Risk is higher in those with a previous history of seizures or epilepsy, CNS anomalies or tumors, cerebrovascular disease, or taking other medications that also lower the seizure threshold such as bupropion or SSRIs.
  • Lupron Depot is only approved for use in men with advanced prostate cancer.

Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects

4. Bottom Line

Lupron Depot is a hormone deprivation treatment that may be used for the palliative care of advanced prostate cancer. The main side effects are hot flushes and general pain and it may cause impotence, loss of libido, and atrophy of the testes. It is effective at slowing tumor progression in the majority of men.

5. Tips

  • Lupron Depot is given once every four weeks, 12 weeks, 16, or 24 weeks depending on the dosage. Make sure you keep your appointments with your healthcare provider and get your injection on time. Lupron Depot is usually continued long-term, even if your cancer progresses.
  • Lupron Depot causes a profound decrease in testosterone levels it is common to experience a decrease in your libido, impotence, and testicular atrophy. Long-term use can also lower bone mineral density.
  • You may experience a "tumor flare" during the first few weeks of treatment. These should resolve with time. This may result in urinary symptoms and pain. Contact your doctor if new or worsened symptoms occur soon after starting Lupron Depot.
  • Mood swings, including depression, have also been reported. If you experience a low mood or have thoughts about suicide talk to your doctor or another trusted healthcare professional.
  • If you have diabetes, you may need to monitor your blood sugar levels more regularly while being treated with Lupron Depot.
  • Lupron Depot may affect your fertility. Talk to your doctor if you are planning to have a family in the future.
  • Lupron Depot may increase your risk for cardiovascular disease, including an increased risk of a heart attack. If you experience any chest pain or pain that radiates down your arm or up your neck, seek urgent medical attention.
  • See your doctor immediately if you develop any side effects of concern including shortness of breath or difficulty breathing, sudden headache, vomiting, visual changes, or confusion.

6. Response and effectiveness

  • After an initial rise, testosterone levels drop reaching castrate levels (lower than 50 ng/dL) within four weeks.
  • Numerous trials have reported the effectiveness of Lupron Depot. For example, for Lupron Depot 7.5mg given every month objective tumor response analysis showed a "no progression" (complete or partial response, or stable disease) in 77% (40/52) of patients at Week 12, and in 84% (42/50) of patients at Week 24. Local disease improved or remained stable in all (42) patients evaluated at Week 12 and in 98% (41/42) of patients elevated at Week 24. PAP normalized or decreased at Week 12 and/or 24 in the majority of patients with elevated baseline PAP. Results of trials have been consistent across all dosages studied.
  • Treatment is usually continued even if cancer metastasizes (spreads)
  • 80% of trial participants were at least 65 years old.

7. Interactions

Medicines that interact with Lupron Depot may either decrease its effect, affect how long it works for, increase side effects, or have less of an effect when taken with Lupron Depot. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.

There are over 250 medications that have major or moderate interactions with Lupron Depot. Some common medications that may interact with Lupron Depot include:

  • acid control treatments such as antacids, famotidine,
  • albuterol
  • antibiotics, such as cotrimoxazole, erythromycin, levofloxacin, or metronidazole
  • anticancer treatments such as doxorubicin
  • antidepressants, such as amitriptyline, citalopram, escitalopram, or venlafaxine
  • antidiarrheal medications, such as loperamide
  • antifungals, such as azithromycin
  • antihistamines, such as hydroxyzine
  • antipsychotics, such as aripiprazole, clozapine, haloperidol, thioridazine, or ziprasidone
  • bisacodyl
  • bupropion
  • chloroquine or hydroxychloroquine
  • cisapride
  • heart medications, such as amiodarone or flecainide
  • HIV medications, such as efavirenz or saquinavir
  • insulin and other antidiabetic medications such as glibenclamide, glyburide, or metformin
  • lactulose
  • lithium
  • magnesium salts
  • methadone
  • mineral oil
  • moxifloxacin
  • multiple sclerosis agents such as fingolimod or ozanimod
  • ondansetron
  • papaverine
  • pimozide
  • quinidine
  • salmeterol
  • senna
  • tamoxifen
  • tolbutamide
  • tramadol.

Lupron Depot suppresses the pituitary-gonadal system which will affect diagnostic tests of pituitary gonadotropic and gonadal functions conducted during treatment and for three months after discontinuation.

Note that this list is not all-inclusive and includes only some common medications that may interact with Lupron Depot. You should refer to the prescribing information for Lupron Depot for a complete list of interactions.


Further information

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

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Copyright 1996-2022 Revision date: February 16, 2022.