Initially, triptorelin, like other LHRH agonists, causes a transient increase in serum testosterone levels. As a result, isolated cases of worsening of signs and symptoms of prostate cancer during the first weeks of treatment have been reported with LHRH agonists. Patients may experience worsening of symptoms or onset of new symptoms, including bone pain, neuropathy, hematuria, or urethral or bladder outlet obstruction. Cases of spinal cord compression, which may contribute to paralysis with or without fatal complications, have been reported with LHRH agonists.

If spinal cord compression or renal impairment develops, standard treatment of these complications should be instituted, and in extreme cases an immediate orchiectomy considered.

TRELSTAR^TM DEPOT should not be administered to individuals who are hypersensitive to triptorelin, other LHRH agonists, or LHRH. In the event of a hypersensitivity reaction, therapy with TRELSTAR^TM DEPOT should be discontinued immediately and the appropriate supportive and symptomatic care should be administered.

General: Patients with metastatic vertebral lesions and/or with upper or lower urinary tract obstruction should be closely observed during the first few weeks of therapy (see WARNINGS). Hypersensitivity and anaphylactic reactions have been reported with triptorelin as with other LHRH agonists (see CONTRAINDICATIONS and WARNINGS).

Laboratory Tests: Response to TRELSTAR^TM DEPOT should be monitored by measuring serum levels of testosterone and prostate-specific antigen.

Pregnancy, Teratogenic Effects: Pregnancy Category X (see CONTRAINDICATIONS). TRELSTAR^TM DEPOT is contraindicated in women who are or may become pregnant while receiving the drug. Studies in pregnant rats administered triptorelin at doses of 2, 10, and 100 µg/kg/day (approximately equivalent to 0.2, 0.8, and 8 times the recommended human therapeutic dose based on body surface area) during the period of organogenesis displayed maternal toxicity and embryotoxicity, but no fetotoxicity or teratogenicity. Similarly, no ter-atogenic effects were observed when mice were administered doses of 2, 20, and 200 µg/kg/day (approximately equivalent to 0.1, 0.7, and 7 times the recommended human therapeutic dose based on body surface area). If this drug is used during pregnancy or if the patient becomes pregnant while taking this drug, she should be apprised of the potential hazard to the fetus.

Carcinogenesis, Mutagenesis, Impairment of Fertility: In rats, doses of 120, 600, and 3000 µg/kg given every 28 days (approximately 0.3, 2.0, and 8 times the recommended human therapeutic dose based on body surface area) resulted in increased mortality with a drug treatment period of 13-19 months. The incidence of benign and malignant pituitary tumors and histiosarcomas were increased in a dose related manner. No oncogenic effect was observed in mice administered triptorelin for 18 months at doses up to 6000 µg/kg every 28 days (approximately 8 times the human therapeutic dose based on body surface area).

Mutagenicity studies performed with triptorelin using bacterial and mammalian systems (in vitro Ames test and chromosomal aberration test in CHO cells and an in vivo mouse micronucleus test) provided no evidence of mutagenic potential.

After 60 days of treatment followed by a minimum of four estrus cycles prior to mating, triptorelin, at doses of 2, 20, and 200 µg/kg/day in saline (approximately 0.2, 2.0, and 16 times the recommended human therapeutic dose based on body surface area) or 20 µg/kg/day in slow release microspheres, had no effect on the fertility or general reproductive performance of female rats. Treatment did not elicit embryotoxicity, teratogenicity, or any effects on the development of the offspring (F1 generation) or their reproductive performance.

No studies were conducted to assess the effect of triptorelin on male fertility.

Geriatric Use: Prostate cancer occurs primarily in an older patient population. Clinical studies with TRELSTAR^TM DEPOT have been conducted primarily in patients ≥65 years.

Nursing Mothers: It is not known whether TRELSTAR^TM DEPOT is excreted in human milk. Because many drugs are excreted in human milk, and because the effects of TRELSTAR^TM DEPOT on lactation and/or the breastfed child have not been determined, TRELSTAR^TM DEPOT should not be used by nursing mothers.

Pediatric Use: TRELSTAR^TM DEPOT has not been studied in pediatric patients.

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