How does this medication work? What will it do for me?
Leuprolide is a medication that has been designed to mimic the actions of gonadotropin releasing hormone (GnRH or LHRH), the hormone released from the hypothalamus gland in the brain. The hypothalamus uses GnRH to send messages to the pituitary gland in the brain, which then sends messages to the ovaries or the testicles, telling these organs to produce the sex hormones estrogen (ovaries) and testosterone (testicles). Normally, GnRH comes from the hypothalamus in pulses, leading to the production of estrogen or testosterone. If GnRH came from the hypothalamus all of the time (rather than in "pulses"), it would have the opposite effect and "turn off" hormone production. This is what leuprolide does.
When given to boys or men, leuprolide reduces the amount of testosterone produced in the body. This medication is used to treat prostate cancer because prostate cancer cells need testosterone in order to grow and reproduce.
When given to girls or women, leuprolide reduces the amount of estrogen the body produces. It is used to treat endometriosis because reduced levels of estrogen help to relieve the symptoms of this condition. It may also be used with iron supplementation to improve anemia before surgery to remove uterine fibroids.
This medication is also used to help slow down the development of the genital areas for boys (under the age of 9) and girls (under the age of 8) who are experiencing early puberty. As soon as the child stops using the medication, normal development will continue.
This medication may be available under multiple brand names and/or in several different forms. Any specific brand name of this medication may not be available in all of the forms or approved for all of the conditions discussed here. As well, some forms of this medication may not be used for all of the conditions discussed here.
Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are being given this medication, speak to your doctor. Do not stop using this medication without consulting your doctor.
Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to use this medication if their doctor has not prescribed it.
What form(s) does this medication come in?
5 mg vial
Each mL contains 5 mg of leuprolide acetate. Nonmedicinal ingredients: acetic acid, benzyl alcohol, sodium chloride, sodium hydroxide, and sterile water for injection USP.
How should I use this medication?
The recommended dose of leuprolide depends on the condition being treated and the frequency of injection that is most convenient for your condition.
Leuprolide is available as a daily injection (under the skin) or as a long-acting injection (into the muscle every 1, 3, or 4 months).
If you are giving yourself or your child daily injections, it is very important to follow the directions as printed on the package insert.
Be sure to check the solution for discolouration and particle matter before each use. Presterilized disposable syringes are supplied and the usual sites of injection are indicated in the package insert. To avoid damage to your skin and tissues, it is important to change the injection site on your body from time to time as recommended by your doctor.
The long-acting form of this medication (depot) is injected into your muscle by your doctor at the appropriate intervals. It is very important to receive this medication at the correct times. If you miss your appointment for an injection, make a new one as soon as possible.
It is important that this medication be administered exactly as prescribed by your doctor. If you are using the daily injections and miss a dose, administer it as soon as possible and continue with your regular schedule. If it is almost time for your next dose, skip the missed dose and continue with your regular dosing schedule. Do not administer a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.
Many things can affect the dose and schedule of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose or schedule different from the ones listed here, do not change the way that you are using the medication without consulting your doctor.
Check the packaging instructions to find out whether to store this medication in the refrigerator or at room temperature, as different brands have different requirements. Once mixed, the suspension should be used immediately or discarded. Protect from freezing and keep out of the reach of children.
Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.
Who should NOT take this medication?
Do not use leuprolide if you:
- are allergic to leuprolide acetate or any ingredients of the medication
- are breast-feeding
- are or may become pregnant
- have undiagnosed abnormal vaginal bleeding
What side effects are possible with this medication?
Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.
The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.
The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.
Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.
- breast tenderness
- flu-like symptoms (e.g., muscle aches, sudden lack of energy, fever, cough, sore throat)
- hot flashes
- increased sweating (adult women)
- light, irregular vaginal bleeding
- menstrual cramps
- sleeping problems
- stopping of menstrual periods (adult women)
- weight changes
Although most of these side effects listed below don't happen very often, they could lead to serious problems if you do not check with your doctor or seek medical attention.
Check with your doctor as soon as possible if any of the following side effects occur:
- burning, itching, redness, or swelling at site of injection
- decreased testicle size (adult men)
- difficulty urinating
- erectile dysfunction or decreased libido (adults)
- itchy skin rash
- mood swings (children; crying, irritability, restlessness, aggressive behaviour)
- muscle or joint pain
- numbness or swelling of the arms or legs
- severe bone pain
- signs of depression (e.g., poor concentration, changes in weight, changes in sleep, decreased interest in activities, thoughts of suicide)
- swelling of feet or legs, fluid retention
- symptoms of liver problems (e.g., nausea, vomiting, diarrhea, loss of appetite, weight loss, yellowing of the skin or whites of the eyes, dark urine, pale stools)
- tendon inflammation and pain
- vaginal burning, dryness, itching, or discharge
- vision changes
- symptoms of lung inflammation (e.g., shortness of breath, dry cough with exertion)
Stop taking the medication and seek immediate medical attention if any of the following occur:
- pituitary apoplexy (e.g., sudden headache, vomiting, changes to vision, eye muscle movement problems, confusion or loss of consciousness or sudden, severe decrease in blood pressure and collapse)
- severe chest or abdominal pain
- severe muscle or joint pain
- signs of a heart attack (e.g., chest pain or pressure, pain extending through shoulder and arm, nausea and vomiting, sweating)
- signs of a serious allergic reaction (e.g., abdominal cramps, difficulty breathing, nausea and vomiting, or swelling of the face and throat)
Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.
Are there any other precautions or warnings for this medication?
Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.
Anemia: Leuprolide acetate may cause a decreased level of red blood cells. If you experience symptoms of reduced red blood cell count (anemia) such as shortness of breath, feeling unusually tired, or pale skin, contact your doctor as soon as possible.
Cholesterol: Leuprolide acetate can cause increased levels of cholesterol. If you are at risk of developing high cholesterol or you have high cholesterol levels before starting this medication, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.
Depression: Sex hormones influence mood swings and symptoms of depression. If you have depression or a history of depression, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.
Diabetes: Leuprolide may cause a loss of blood glucose control, and glucose tolerance may change. People with diabetes may find it necessary to monitor their blood sugar more frequently while using this medication. If you have diabetes or are at risk for developing diabetes, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.
Heart rhythm: Leuprolide acetate can cause changes to the normal rhythm of the heart, including an irregular heartbeat called QT prolongation. QT prolongation is a serious life-threatening condition that can cause fainting, seizures, and sudden death. If you have a history of heart disease or a heart condition called long QT syndrome, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.
Liver function: In rare cases, leuprolide has been reported to cause liver failure or inflammation of the liver. If you experience symptoms of liver problems such as fatigue, feeling unwell, loss of appetite, nausea, yellowing of the skin or whites of the eyes, dark urine, pale stools, abdominal pain or swelling, and itchy skin, contact your doctor immediately.
Men and heart-related conditions: There may be an increased risk of heart-related events (e.g., heart attacks, stroke, heart-related death) for men being treated for prostate cancer with GnRH medications. Before you start treatment, tell your doctor if you have diabetes, heart disease, had a previous heart attack or stroke, or have cardiovascular risk factors (e.g., high blood pressure, smoking, or cholesterol). If you have any of these conditions, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.
Osteoporosis: Over time, leuprolide can cause the bones to lose thickness. People who are at risk for osteoporosis, such as those with a family history of osteoporosis, long-term alcohol or tobacco use, or who are taking other medications that tend to thin bones, such as seizure medications or long-term use of corticosteroids, are more likely to experience this loss of bone. If you have any of these conditions, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.
Seizures: People using leuprolide have reported experiencing seizures. People who have a history of epilepsy, medical conditions that increase the risk of seizures, and are taking medications that increase the risk of seizures may be more likely to experience this effect, however people with none of these conditions have also reported seizures. If you have a history of seizures, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.
If you experience a seizure, get emergency medical help.
Starting treatment: During the first few weeks of treatment with leuprolide, you may notice that your signs and symptoms temporarily get worse. This is due to a sudden increase in hormones that will normalize once the right dose for you has been found.
Urinary problems: People with problems urinating due to blockage or narrowing along the urinary tract (obstructive uropathy) may find that starting this medication makes this symptom worse initially. If you have problems with urination, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.
Pregnancy: Leuprolide should not be used during pregnancy. A non-hormonal method of birth control (e.g., condom, diaphragm, IUD) should be used during treatment. If you become pregnant during treatment, notify your doctor as soon as possible.
Breast-feeding: It is not known if leuprolide passes into breast milk. If you are breast-feeding and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.
What other drugs could interact with this medication?
There may be an interaction between leuprolide and any of the following:
- antiarrhythmics (e.g., amiodarone, disopyramide, dronedarone, procainamide, propafenone, quinidine)
- antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
- "azole" antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- beta 2-agonists (e.g., formoterol, indacaterol, olodaterol, salbutamol, salmeterol)
- diabetes medications (e.g., canagliflozin, glyburide, linagliptin, lixisenatide, insulin, metformin, rosiglitazone)
- macrolide antibiotics (e.g., clarithromycin, erythromycin)
- selective serotonin reuptake inhibitors (SSRIs, e.g., citalopram, fluoxetine, paroxetine, sertraline)
- serotonin antagonists (anti-emetic medications; e.g., granisetron, ondansetron)
- tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:
- stop taking one of the medications,
- change one of the medications to another,
- change how you are taking one or both of the medications, or
- leave everything as is.
An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.
Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.
All material copyright MediResource Inc. 1996 – 2024. Terms and conditions of use. The contents herein are for informational purposes only. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition. Source: www.medbroadcast.com/drug/getdrug/Lupron