Triptorelin Pamoate (2 brand names, 2 dosage forms, 1 route)
Available dosage forms: FOR SUSPENSION, EXTENDED RELEASE, INJECTABLE.
Routes of administration: INTRAMUSCULAR.
Brand Names
- TRELSTAR
- TRIPTODUR KIT
Indications and Usage
TRELSTAR is indicated for the treatment of advanced prostate cancer [see Clinical Studies (14) ].
Adverse Reactions
The following is discussed in more detail in other sections of the labeling: Hypersensitivity Reactions [see Warnings and Precautions (5.1)] Tumor Flare [see Warnings and Precautions (5.2)]. Metabolic Syndrome [see Warnings and Precautions (5.3)] Cardiovascular Diseases [see Warnings and Precautions (5.4)]. Convulsions [see Warnings and Precautions (5.5)]. Severe Cutaneous Adverse Reactions [see Warnings and Precautions (5.6)]. Effect of QT/QTc Interval [see Warnings and Precautions (5.7)].
Drug Interactions
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.
Mechanism of Action
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 125I-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.