How does this medication work? What will it do for me?

Triptorelin is a medication that has been designed to mimic the actions of gonadotropin releasing hormone (GnRH or luteinizing hormone releasing hormone, 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 in women, and the testicles in men, telling these organs to produce the sex hormones estrogen (in women) and testosterone (in men).

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 triptorelin does.

Triptorelin is used to treat advanced prostate cancer. It reduces the amount of testosterone in the blood, which can cause the prostate cancer to grow.

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 taking this medication, speak to your doctor. Do not stop taking 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 take this medication if their doctor has not prescribed it.

What form(s) does this medication come in?

Trelstar (1 month slow release) 3.75 mg triptorelin per vial

Each vial of sterile lyophilized microgranules contains triptorelin pamoate which is equivalent to triptorelin peptide base 3.75 mg. Nonmedicinal ingredients: poly-d,l-lactide-co-glycolide (170 mg), mannitol, USP (85 mg), carboxymethylcellulose sodium, USP (30 mg), and polysorbate 80 USP (2 mg). When 2 mL Sterile Water for Injection is added to the microgranules and mixed, a suspension is formed, which is intended as a single, monthly intramuscular injection.

Trelstar (3 month slow release) 11.25 mg triptorelin/vial

Each vial of sterile lyophilized microgranules contains triptorelin pamoate which is equivalent to triptorelin peptide base 11.25 mg. Nonmedicinal ingredients: poly-d,l-lactide-co-glycolide (145 mg), mannitol, USP (85 mg), carboxymethylcellulose sodium, USP (30 mg), and polysorbate 80 USP (2 mg). When 2 mL Sterile Water for Injection is added to the microgranules and mixed, a suspension is formed, which is intended as a single, 3 month intramuscular injection.

Trelstar (6 month slow release) 22.5 mg triptorelin/vial

Each vial of sterile lyophilized microgranules contains triptorelin pamoate which is equivalent to triptorelin peptide base 22.5 mg. Nonmedicinal ingredients: poly-d,l-lactide-co-glycolide, mannitol, USP, carboxymethylcellulose sodium, USP, and polysorbate 80, NF. When 2 mL Sterile Water for Injection is added to the microgranules and mixed, a suspension is formed, which is intended as a single, intramuscular injection administered every 6 months.

How should I use this medication?

Triptorelin is given as an intramuscular (into the muscle) injection by your doctor. When used to treat advanced prostate cancer, it may be given once every 28 days, every 3 months or every 6 months, depending on the dosage form used. 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.

It is important this medication be given exactly as prescribed by your doctor. Keeping a consistent schedule of injections is important. If you miss an appointment to receive triptorelin, contact your doctor as soon as possible to reschedule your appointment.

Triptorelin vials or dose delivery systems should be stored at room temperature and protected from light and freezing. Keep it 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 triptorelin if you:

  • are allergic to triptorelin or any ingredients of the medication
  • are allergic to medications called GnRH agonists or LHRH agonists (such as buserelin or goserelin)
  • are breast-feeding
  • are pregnant or may become pregnant while taking this medication

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 enlargement (for men)
  • constipation
  • coughing
  • diarrhea
  • difficulty getting or maintaining an erection
  • dizziness
  • fatigue or weakness
  • headache
  • hot flashes (sudden sweating and feeling of warmth)
  • increased blood pressure
  • nausea
  • pain, redness, swelling, or itching at the place of injection
  • reduced genital size
  • reduced sex drive
  • skin rash
  • trouble sleeping

Although most of the 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:

  • bone pain
  • breathing problems
  • difficult or painful urination
  • eye pain
  • leg cramps
  • loss of appetite
  • pain in the leg, back, breast, muscles, or joints
  • pain, swelling, numbness, or weakness of the limbs
  • signs of depression (e.g., poor concentration, changes in weight, changes in sleep, decreased interest in activities, thoughts of suicide)
  • swelling of the arms or legs
  • symptoms of high blood sugar (e.g., frequent urination, increased thirst, excessive eating, unexplained weight loss, poor wound healing, infections, fruity breath odour)
  • symptoms of liver problems (such as yellow eyes or skin, abdominal pain, loss of appetite, pale stools, itchy skin, or dark urine)
  • symptoms of a urinary tract infection (e.g. pain when urinating, urinating more often than usual, low back or flank pain)

Stop taking the medication and seek immediate medical attention if any of the following side effects occur:

  • chest pain
  • racing or abnormal heartbeat
  • symptoms of a serious allergic reaction (such as swelling of the face or throat, skin rash, hives, or difficulty breathing)

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: Triptorelin may cause low levels 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.

Your doctor will do blood tests regularly to monitor the number of specific types of blood cells, including red blood cells, in your blood.

Depression: GnRH medications have been known to cause 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. If you experience symptoms of depression such as poor concentration, changes in weight, changes in sleep, decreased interest in activities, or notice them in a family member who is taking this medication contact your doctor as soon as possible.

Diabetes: Triptorelin may cause an increase in blood sugar levels 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.

Drowsiness/reduced alertness: This medication may affect the mental or physical abilities needed to drive or operate machinery. Avoid driving, operating machinery, or performing other hazardous tasks until you have determined how this medication affects you.

Heart rhythm: Triptorelin can cause changes to the normal rhythm of the heart, as a result of reducing the testosterone in the body. An irregular heartbeat called QT prolongation is possible. QT prolongation is a serious life-threatening condition that can cause fainting, seizures, and sudden death. If you are at risk for heart rhythm problems (e.g., people with heart failure, angina, low potassium or magnesium levels, taking certain medications), 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.

Kidney function: Kidney disease or reduced kidney function may cause this medication to build up in the body, causing side effects. If you have reduced kidney function or kidney disease, 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 have reduced kidney or liver function, 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: Liver disease or reduced liver function may cause this medication to build up in the body, causing side effects. If you have liver problems, 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. Your doctor may want to test your liver function regularly with blood tests while you are taking this medication.

Men and the heart: There may be an increased risk of heart-related events (e.g., heart attacks, stroke, heart-related death) in 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: Triptorelin can cause your bones to lose thickness. If you are at risk for osteoporosis (thin bones) or are taking other medications that tend to thin bones, 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.

Short-term worsening of symptoms: When this medication is first used, an increase in testosterone occurs in the body. For some people, their symptoms may temporarily worsen during the first weeks of treatment with triptorelin. If your medical condition appears to worsen or you experience bone pain, numbness or tingling in the hands or feet, blood in the urine or difficulty urinating, contact your doctor as soon as possible.

Pregnancy: Triptorelin should not be used during pregnancy. A non-hormonal method of birth control (such as condoms, diaphragms, or IUDs) should be used during treatment. If you become pregnant during treatment, contact your doctor immediately.

Breast-feeding: It is not known if triptorelin passes into breast milk. Breast-feeding is not recommended for women taking this medication.

Children: The safety and effectiveness of using this medication have not been established for children.

What other drugs could interact with this medication?

There may be an interaction between triptorelin and any of the following:

  • antidiabetes medications (such as glyburide, glimepiride, metformin)
  • hyperprolactinemic drugs (such as risperidone, metoclopramide, verapamil)
  • medications that can thin the bones (such as prednisone)
  • testosterone and androgens

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 that 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.