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Endocrine Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Triptorelin (as the acetate) is administered in the form of an aqueous copolymer microsphere suspension (i.e., Decapeptyl SRTM) by intramuscular or subcutaneous injection. It produces similar side effects to those associated with the other GnRH agonist analogues described in this section.
Uterine Cancer
Published in Pat Price, Karol Sikora, Treatment of Cancer, 2020
Claudia von Arx, Hani Gabra, Christina Fotopoulou
Megestrol acetate (160 mg/day) and medroxy progesterone acetate are the two progestins used for medical treatment. Both oral and parenteral routes for progestin therapy appear to be effective, although the optimal dose and duration of therapy are unknown. The minimum duration of progestin therapy appears to be 3 months, but some women will require a longer course.18 After induction of response, a periodic withdrawal of progestins is usually recommended. Other modalities, such as IUDs and gonadotropin releasing hormone agonists (e.g., triptorelin), should not be routinely used outside the setting of clinical trials.110
Hormonal Regulation in the Treatment of Fibroids
Published in John C. Petrozza, Uterine Fibroids, 2020
Victoria Fitz, Steven L. Young
Investigators have also attempted to target estrogen action using an aromatase inhibitor (letrozole) to partially block estrogen synthesis. Since fibroids may, themselves, produce estrogen via aromatase expression [25], such an approach could reduce autocrine/intracrine estrogen action as well as the endocrine action of ovarian estrogens inhibited by GnRHa medications. Furthermore, these agents may be helpful for treating postmenopausal fibroids that may be maintained mainly by endogenous estrogen production. Encouragingly, small trials have suggested a similar effect of aromatase inhibitors to that of a GnRHa, triptorelin, but with a greatly reduced incidence of vasomotor symptoms [26].
Triptorelin nanoparticle-loaded microneedles for use in assisted reproductive technology
Published in Drug Delivery, 2023
Xiaoyan Lu, Yiying Sun, Meishan Han, Daoyuan Chen, Xiaoyan He, Siqi Wang, Kaoxiang Sun
Triptorelin has been administered in three regimens for ART: a long protocol utilizing the downregulation effect, a short protocol utilizing the flare-up effect and downregulation effect, and an ultrashort protocol utilizing the flare-up effect (Siristatidis et al., 2015). Triptorelin is commonly marketed as a long-acting injection suspension. However, in long protocols the detrimental effects of treatment depots on embryos in early pregnancy must be considered (Eftekhar et al., 2013). Therefore, a short-acting formulation of triptorelin (0.1 mg) has been developed for the clinical regime of daily subcutaneous administration for ART. Daily injections administered by clinical staff in different regimens over 2–15 days impose severe psychological and physical burdens on women receiving ART. In addition, peptides administered by subcutaneous injection can be degraded by enzymes in the skin, resulting in reduced amounts of effective drug entering the bloodstream (Ito et al., 2011), thereby exposing women receiving ART to the potential risks posed by greater-than-effective amounts of highly active drugs in their skin.
Effects of water-soluble additive on the release profile and pharmacodynamics of triptorelin loaded in PLGA microspheres
Published in Drug Development and Industrial Pharmacy, 2023
Xiaoyan He, Jiwei Liu, Tao Song, Yiying Sun, Xiaoyan Lu, Nuannuan Li, Kaoxiang Sun
Male Sprague Dawley (SD) rats were selected to evaluate the pharmacodynamics of triptorelin in different formulations. The SD rats were randomly divided into several groups, one of which was castrated group (n = 6). For castrated group, normal rats were anesthetized with 10% chloral hydrate (0.36 ml/100g). A small incision was made on the ventral skin above the pubic symphysis. The testicle located in the scrotum was gently pushed into the abdominal cavity. Then, the abdominal wall was opened, testicle and epididymis were pulled out and removed using small scissors. Finally, the incision was sutured with surgical thread. The microspheres were administrated after the surgical wound healing. Before administration, the microspheres were reconstituted with diluent containing 0.5% carboxymethylcellulose sodium (CMC-Na) and 0.1% tween 80. Then, the drug suspension was administered by intramuscular injection at a dose of 0.3 mg/kg. At predetermined time intervals, blood samples were taken from the oculi chorioideae vein and transferred into blood collection tubes containing heparin sodium. After shaking, the tubes were centrifuged at 3,500 rpm for 10 min to gain plasma samples. Then, the samples were placed in the refrigerator before further analysis.
Evaluating triptorelin as a treatment option for breast cancer
Published in Expert Opinion on Pharmacotherapy, 2019
Emanuela Ferraro, Dario Trapani, Eleonora Marrucci, Giuseppe Curigliano
Several studies have demonstrated that triptorelin is able to induce menopausal status, with a decrease in serum estrogens. According to these evidences, triptorelin is approved in association with AI and tamoxifen in early breast cancer for premenopausal women. The use of LH-RHa is mandatory in combination with agents which are active only in a menopausal status such as fulvestrant, AI with or without CDK 4/6 inhibitors in advanced setting, in order to induce OFS. In addition, triptorelin is suggested to preserve ovarian function for women with the desire of motherhood during chemotherapy treatment regardless of the HR status. For male breast cancer, LH-RHas are recommended in combination with AI to suppress testis function; the principle is analog to the medical castration used in the treatment of prostate cancer.