Triptorelin

Contraindications

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What is the most important information I should know about Triptorelin?

You should not use this medication if you are allergic to Triptorelin or similar drugs such as leuprolide (Lupron, Viadur, Eligard) or goserelin (Zoladex).

Before using Triptorelin, tell your doctor if you have any type of cancer that has spread to your spine, a bladder obstruction or problems with urination, diabetes, heart disease, high blood pressure, high cholesterol, a history of stroke or heart attack, or if you smoke.

After your injection, your prostate cancer symptoms may get worse for a short time because Triptorelin raises your testosterone levels. These side effects should get better within 3 or 4 weeks. Call your doctor if your symptoms do not improve, or if they get worse while using Triptorelin.

Some of the side effects of Triptorelin are symptoms of prostate cancer that may occur because the medicine raises your testosterone levels. Call your doctor at once if you have pain or burning when you urinate, blood in your urine, bone pain, numbness, tingling, muscle weakness, or loss of movement in any part of your body.

Although Triptorelin is not for use by women, this medication can cause birth defects and should not be used by a woman who is pregnant or who may become pregnant.

Undesirable effects

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What are the possible side effects of Triptorelin?

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in practice.

The safety of the three Triptorelin formulations was evaluated in clinical trials involving patients with advanced prostate cancer. Mean testosterone levels increased above baseline during the first week following the initial injection, declining thereafter to baseline levels or below by the end of the second week of treatment. The transient increase in testosterone levels may be associated with temporary worsening of disease signs and symptoms, including bone pain, neuropathy, hematuria, and urethral or bladder outlet obstruction. Isolated cases of spinal cord compression with weakness or paralysis of the lower extremities have occurred.

Adverse reactions reported for each of the three Triptorelin formulations in the clinical trials, are presented in Table 2, Table 3, and Table 4. Often, causality is difficult to assess in patients with metastatic prostate cancer. The majority of adverse reactions related to Triptorelin are a result of its pharmacological action, i.e., the induced variation in serum testosterone levels, either an increase in testosterone at the initiation of treatment, or a decrease in testosterone once castration is achieved. Local reactions at the injection site or allergic reactions may occur.

The following adverse reactions were reported to have a possible or probable relationship to therapy as ascribed by the treating physician in at least 1% of patients receiving Triptorelin 3.75 mg.

Table 2: Triptorelin 3.75 mg: Treatment-Related Adverse Reactions Reported by 1% or More of Patients During Treatment

The following adverse reactions were reported to have a possible or probable relationship to therapy as ascribed by the treating physician in at least 1% of patients receiving Triptorelin 11.25 mg.

Table 3: Triptorelin 11.25 mg: Treatment-Related Adverse Reactions Reported by 1% or More of Patients During Treatment

The following adverse reactions occurred in at least 5% of patients receiving Triptorelin 22.5 mg. The table includes all reactions whether or not they were ascribed to Triptorelin by the treating physician. The table also includes the incidence of these adverse reactions that were considered by the treating physician to have a reasonable causal relationship or for which the relationship could not be assessed.

Table 4: Triptorelin 22.5 mg: Adverse Reactions Reported by 5% or More of Patients During Treatment

The following abnormalities in laboratory values not present at baseline were observed in 10% or more of patients:

Triptorelin 3.75 mg: There were no clinically meaningful changes in laboratory values detected during therapy.

Triptorelin 11.25 mg: Decreased hemoglobin and RBC count and increased glucose, BUN, SGOT, SGPT, and alkaline phosphatase at the Day 253 visit.

Triptorelin 22.5 mg: Decreased hemoglobin and increased glucose and hepatic transaminases were detected during the study. The majority of the changes were mild to moderate.

The following adverse reactions have been identified during post approval use of gonadotropin releasing hormone agonists. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

During postmarketing surveillance, rare cases of pituitary apoplexy (a clinical syndrome secondary to infarction of the pituitary gland) have been reported after the administration of gonadotropin-releasing hormone agonists. In a majority of these cases, a pituitary adenoma was diagnosed with a majority of pituitary apoplexy cases occurring within 2 weeks of the first dose, and some within the first hour. In these cases, pituitary apoplexy has presented as sudden headache, vomiting, visual changes, ophthalmoplegia, altered mental status, and sometimes cardiovascular collapse. Immediate medical attention has been required.

During postmarketing experience, convulsions, and thromboembolic events including, but not limited to, pulmonary emboli, cerebrovascular accident, myocardial infarction, deep venous thrombosis, transient ischemic attack, and thrombophlebitis have been reported.

Therapeutic indications

Prostate Cancer: Treatment of locally advanced prostate cancer alone or as concomitant and adjuvant to radiotherapy and metastatic prostate cancer.

A favourable effect of the treatment is all the more pronounced and more frequent if the patient has not previously received any other hormone treatment.

Genital and Extragenital Endometriosis (Stage I-IV): Treatment should not be administered ≥6 months. It is not recommended to undertake a second course of treatment by Triptorelin or by another GnRH analogue.

Diphereline P.R. (1M): Precocious Puberty (before the age of 8 years in girls and 10 years in boys).

Female Infertility: Complementary treatment in association with the gonadotrophins [human menopausal gonadotrophin (hMG), FSH, human chorionic gonadotrophin (hCG)] in the course of ovulation induction in view of in vitro fertilization and embryo transfer (IVFET).

Treatment of Uterine Fibromyomas Prior to Surgery: Associated with anemia (hemoglobin ≤8 g/dL), when a reduction in the size of the fibromyoma is necessary to facilitate or modify the surgical technique: Endoscopic surgery, transvaginal surgery. The treatment of duration is restricted to 3 months.

Triptorelin is a man-made form of a hormone that regulates many processes in the body. Triptorelin overstimulates the body's own production of certain hormones, which causes that production to shut down temporarily.

The Triptorelin brand of Triptorelin is used in men to treat the symptoms of prostate cancer. Triptorelin treats only the symptoms of prostate cancer and does not treat the cancer itself.

The Triptodur brand of Triptorelin is used to treat precocious puberty in boys and girls who are at least 2 years old.

Triptorelin may also be used for purposes not listed in this medication guide.

Name of the medicinal product

Qualitative and quantitative composition

Depot Injection: Each disposable syringe contains injectable amount of Triptorelin (D-Trp6-LHRH) 3.75 mg encapsulated in a biodegradable polymer, poly(DL-lactide-co-glycolide). Each syringe of suspension medium contains polysorbate 80, dextran 70, sodium chloride, sodium dihydrogen phosphate dihydrate, sodium hydroxide solution to adjust the pH, and water for injection 1 mL.

Daily Injection: Each 0.1 mg/mL injectable solution contains Triptorelin acetate 105 mcg equivalent to Triptorelin 95.6 mcg, in a pH-adjusted aqueous sodium chloride solution.

Special warnings and precautions for use

Triptorelin is usually given once every 4, 12, or 24 weeks. Your dose schedule will depend on the strength of Triptorelin you are using. Follow all directions on your prescription label. Do not use this medicine in larger or smaller amounts or for longer than recommended.

Triptorelin is injected into a muscle. You may be shown how to use injections at home. Do not self-inject this medicine if you do not understand how to give the injection and properly dispose of used needles and syringes.

Triptorelin is a powder medicine that must be mixed with a liquid (diluent) before using it. If you are using the injections at home, be sure you understand how to properly mix and store the medicine.

Do not shake the mixed medicine or it may foam. Prepare your dose only when you are ready to give an injection. Do not use if the medicine has changed colors or has particles in it. Call your pharmacist for new medicine.

After your injection, your prostate cancer symptoms may get worse for a short time because Triptorelin raises your testosterone levels. These side effects should get better within 3 or 4 weeks. Call your doctor if your symptoms do not improve, or if they get worse while using Triptorelin.

While using Triptorelin, you may need frequent blood tests.

Each single use vial (bottle) of this medicine is for one use only. Throw away after one use, even if there is still some medicine left in it after injecting your dose.

Use a disposable needle only once, then throw away in a puncture-proof container (ask your pharmacist where you can get one and how to dispose of it). Keep this container out of the reach of children and pets.

Store vials and prefilled syringes at room temperature away from moisture, heat, and light. Do not freeze.

Central precocious puberty: Triptodur: Treatment of central precocious puberty in patients 2 years and older

Prostate cancer (advanced): Triptorelin: Palliative treatment of advanced prostate cancer

Assisted reproductive technologies: Triptorelin [Canadian product]: Adjunctive therapy in women undergoing controlled ovarian hyperstimulation for assisted reproductive technologies (ART)

Data from a limited number of case reports and clinical experience suggest Triptorelin may be beneficial in the treatment of endometrial stromal sarcoma.

Based on The World Federation of Societies of Biological Psychiatry (WFSBP) Guidelines for the Biological Treatment of Paraphilias, Triptorelin given for paraphilia/hypersexuality is an effective and recommended treatment option in the management of this condition.

Dosage (Posology) and method of administration

Triptorelin must be administered under the supervision of a physician.

Triptorelin is administered by a single intramuscular injection in either buttock. Dosing schedule depends on the product strength selected (Table 1). The lyophilized microgranules are to be reconstituted in sterile water. No other diluent should be used.

Table 1: Triptorelin Recommended Dosing

Wash your hands with soap and hot water and put on gloves immediately prior to preparing the injection. Place the sealed tray on a clean, flat surface that is covered with a sterile pad or cloth. Peel the cover away from the tray and remove the MIXJECT components and the Triptorelin vial. Remove the Flip-Off button from the top of the vial, revealing the rubber stopper. Place the vial in a standing upright position on the prepared surface. Disinfect the rubber stopper with the alcohol wipe. Discard the alcohol wipe and allow the stopper to dry. Proceed to MIXJECT Activation.

Injectable suspension: 3.75 mg, 11.25 mg, 22.5 mg.

Triptorelin is supplied in a single dose vial with a Flip-Off seal containing sterile lyophilized Triptorelin pamoate microgranules incorporated in a biodegradable copolymer of lactic and glycolic acids.

Triptorelin is also supplied in the Triptorelin MIXJECT single-dose delivery system consisting of a vial with a Flip-Off seal containing sterile lyophilized Triptorelin pamoate microgranules incorporated in a biodegradable copolymer of lactic and glycolic acids, a MIXJECT vial adapter, and a pre-filled syringe containing sterile water for injection, USP, 2 mL, pH 6 to 8.5.

Triptorelin 3.75 mg – NDC 52544-153-02 (single dose vial) and NDC 52544-189-76 (Triptorelin 3.75 mg with MIXJECT single-dose delivery system)

Triptorelin 11.25 mg – NDC 52544-154-02 (single dose vial) and NDC 52544-188-76 (Triptorelin 11.25 mg with MIXJECT single-dose delivery system)

Triptorelin 22.5 mg – NDC 52544-156-02 (single dose vial) and NDC 52544-092-76 (Triptorelin 22.5 mg with MIXJECT single-dose delivery system)

Store at 20-25°C (68-77°F). Do not freeze Triptorelin with MIXJECT.

Distributed By: Actavis Pharma, Inc., Parsippany, NJ 07054 USA. Manufactured By: Debio RP, CH-1920 Martigny, Switzerland. MIXJECT is manufactured by: Medimop Medical Projects Ltd., Ra'anana, Israel. The pre-filled syringe containing sterile water for injection is manufactured by: Abbott Biologicals BV, Olst, The Netherlands. For all medical inquiries contact: ACTAVIS Medical Communications, Parsippany, NJ 07054 USA. 800-272-5525. Revised: July 2014.

Interaction with other medicinal products and other forms of interaction

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What other drugs will affect Triptorelin?

No drug-drug interaction studies involving Triptorelin have been conducted.

Human pharmacokinetic data with Triptorelin suggest that C-terminal fragments produced by tissue degradation are either degraded completely within tissues or are rapidly degraded further in plasma, or cleared by the kidneys. Therefore, hepatic microsomal enzymes are unlikely to be involved in Triptorelin metabolism. However, in the absence of relevant data and as a precaution, hyperprolactinemic drugs should not be used concomitantly with Triptorelin since hyperprolactinemia reduces the number of pituitary GnRH receptors.