Triptorelin

TRELSTAR is indicated for the treatment of advanced prostate cancer. TRELSTAR is a gonadotropin releasing hormone (GnRH) agonist indicated for the treatment of advanced prostate cancer.

Triptorelin is a synthetic decapeptide agonist analog of gonadotropin releasing hormone (GnRH). Comparative in vitro studies showed that triptorelin was 100-fold more active than native GnRH in stimulating luteinizing hormone release from monolayers of dispersed rat pituitary cells in culture and 20-fold more active than native GnRH in displacing 125 I-GnRH from pituitary receptor sites. In animal studies, triptorelin pamoate was found to have 13‑fold higher luteinizing hormone-releasing activity and 21-fold higher follicle-stimulating hormone-releasing activity compared to the native GnRH.

TRELSTAR is administered as a single intramuscular injection in either buttock. Due to different release characteristics, the dosage strengths are not additive and must be selected based upon the desired dosing schedule. 3.75 mg every 4 weeks. 11.25 mg every 12 weeks. 22.5 mg every 24 weeks. Trelstar injection kit

Known hypersensitivity to triptorelin or any other component of the product, or other GnRH agonists or GnRH. Hypersensitivity TRELSTAR is contraindicated in individuals with a known hypersensitivity to triptorelin or any other component of the product, or other GnRH agonists or GnRH.

Hypersensitivity: Anaphylactic shock, hypersensitivity, and angioedema have been reported. In the event of a reaction, discontinue TRELSTAR and initiate appropriate medical management. Tumor Flare: Transient increase in serum testosterone levels can occur within the first few weeks of treatment. This may worsen prostate cancer and result in spinal cord compression and urinary tract obstruction. Monitor patients at risk and manage as appropriate. Metabolic Syndrome: The use of GnRH agonists may lead to an increased risk of metabolic changes such as hyperglycemia, diabetes, hyperlipidemia, and non-alcoholic fatty liver disease. Monitor for signs and symptoms of metabolic syndrome including lipids, blood glucose level and/or HbA1c and manage according to institutional guidelines.

The following is discussed in more detail in other sections of the labeling: Hypersensitivity Reactions Tumor Flare. Metabolic Syndrome Cardiovascular Diseases. Convulsions. Severe Cutaneous Adverse Reactions. Effect of QT/QTc Interval. 3.75 mg: The most common adverse reactions (≥ 5%) during TRELSTAR 3.75 mg therapy included hot flushes, skeletal pain, impotence, and headache. 11.25 mg: The most common adverse reactions (≥ 5%) during TRELSTAR 11.25 mg therapy included hot flushes, skeletal pain, headache, edema in legs, and leg pain. 22.5 mg: The most common adverse reactions (≥ 5%) during TRELSTAR 22.5 mg therapy included hot flushes, erectile dysfunction, and testicular atrophy.

No drug-drug interaction studies involving TRELSTAR have been conducted. Human pharmacokinetic data with triptorelin suggest that C-terminal fragments produced by tissue degradation are either degraded completely within tissues, 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 TRELSTAR since hyperprolactinemia reduces the number of pituitary GnRH receptors.

Storage Store at 20-25°C (68-77°F). Do not freeze TRELSTAR.