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Triptorelin Acetate for Injection

Function and Efficacy

Triptorelin is a synthetic decapeptide that is an analog of natural GnRH (gonadotropin-releasing hormone). Animal and human studies have shown that after initial stimulation, long-term use of triptorelin can inhibit the secretion of gonadotropins, thereby inhibiting the function of the testicles and ovaries. Further studies on animals suggest another mechanism of action: direct gonadal inhibition by reducing the sensitivity of peripheral GnRH receptors. When triptorelin is injected into prostate cancer, the blood LH and FSH levels increase in the early stage, and then the blood testosterone level increases; after continuing the medication for 2 to 3 weeks, the blood LH and FSH levels decrease, and then the blood testosterone drops to castrate levels. At the same time, acid phosphatase increases transiently in the early stage of treatment. Treatment can improve symptoms. Precocious puberty In both sexes, triptorelin can inhibit the hypersecretion of pituitary gonadotropins, which is manifested as the inhibition of estradiol or testosterone secretion, the decrease of LH peak, and the increase of height age/bone age ratio. Initial gonadal stimulation may cause a small amount of vaginal bleeding, which needs to be treated with medroxyprogesterone acetate or cyproterone acetate. Endometriosis Continuous use of triptorelin can inhibit the secretion of estradiol, thereby keeping the ectopic endometrial tissue in a resting state. Infertility Triptorelin inhibits the secretion of gonadotropins (FSH and LH). This treatment ensures the suppression of the LH peak, thereby improving the quality of follicle production and increasing the number of follicles. Uterine fibroid studies have shown that the size of some uterine fibroids has been significantly reduced, which is most obvious in the third month of treatment. Most patients develop amenorrhea after the first month of treatment and need to correct anemia caused by menorrhagia or uterine bleeding. Animal toxicology studies have not shown any special toxicity of the drug molecule. The observed effects are related to the pharmacological properties of the drug on the endocrine system. It is completely absorbed 40 to 45 days after administration.

Ingredients

Triptorelin (I) (Decapeptyl)

Name Description Content CAS NO. Manufacturer
TriptorelinIngredients

Triptorelin is a synthetic decapeptide and an analog of natural GnRH. After initial stimulation, long-term use can inhibit the secretion of gonadotropin, thereby inhibiting testicular and ovarian function. Direct gonadal inhibition is produced by reducing the sensitivity of peripheral GnRH receptors. In the treatment of prostate cancer, blood LH and FSH levels increase in the early stage, and then blood testosterone levels increase; after continuing to use the drug for 2 to 3 weeks, blood LH and FSH levels decrease, and blood testosterone drops to castration levels. At the same time, acid phosphatase increases transiently in the early stage of treatment, and symptoms improve. For patients with precocious puberty, triptorelin can inhibit the hypersecretion of pituitary gonadotropin, which is manifested as inhibition of estradiol or testosterone secretion, decreased LH peak, and increased height age/bone age ratio. In the treatment of endometriosis, continuous medication can inhibit estradiol secretion and keep ectopic endometrial tissue in a resting state. In the treatment of infertility, triptorelin can inhibit the secretion of gonadotropins (FSH and LH), ensuring the suppression of the LH peak, thereby improving the quality of follicle formation and increasing the number of follicles. Studies on uterine fibroids have shown that the size of some uterine fibroids has been significantly reduced, which is most obvious in the third month of treatment. Most patients experience amenorrhea after the first month of treatment, and anemia caused by menorrhagia or uterine bleeding needs to be corrected.

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Appearance

This product is almost white lyophilized substance or powder.

Indication

In vitro fertilization can also be used for hormone-dependent prostate cancer, endometriosis and uterine fibroids.

Usage and Dosage

Closely monitor the serum level of sex hormones during treatment. 1. Controlled-release agent: intramuscular injection of 3.75 mg/4 weeks, the treatment period for women should not exceed 6 months. 2. Injection: 500 μg/time, once/day, subcutaneous injection, for 7 consecutive days, then maintain with 100 μg/time subcutaneous injection daily. 3. In vitro fertilization 500 μg/time/day subcutaneous injection, 100 μg/time/day after 7-10 days.

Adverse Reactions

Male: At the beginning of treatment, with the transient increase in blood testosterone levels, some patients may experience aggravation of urinary tract symptoms, bone pain caused by bone metastasis, and spinal cord compression caused by vertebral metastasis. These symptoms will disappear after 1-2 weeks. During treatment, the most commonly reported adverse reactions (hot flashes, decreased libido, and impotence) are related to decreased plasma testosterone, which is the result of the pharmacological action of the drug and is similar to the adverse reactions observed with other GnRH analogs. Female: At the beginning of treatment, due to the transient increase in plasma estradiol levels, endometriosis symptoms (pelvic pain, dysmenorrhea) may be aggravated, which disappears after 1-2 weeks. Uterine bleeding may occur within one month after the first injection. When this drug is used to treat female infertility, the combined use of gonadotropins can cause ovarian stimulation, which may cause ovarian hypertrophy, pelvic pain and/or abdominal pain. During treatment, the most commonly reported adverse reactions such as hot flashes, vaginal dryness, decreased libido, and dyspareunia are related to pituitary-ovarian blockade. Headaches, joint pain, and muscle pain have been reported rarely. Male and female: Allergic reactions such as urticaria, rash, and itching have been reported. Rarely, Quincke's edema has occurred. Some patients have experienced nausea, vomiting, weight gain, hypertension, mood disorders, fever, abnormal vision, and pain at the injection site. Long-term use of GnRH analogs can cause bone loss and is at risk of osteoporosis. Children: Initial ovarian stimulation may cause a small amount of vaginal bleeding in girls. As in adults, children have also been reported to experience allergic reactions such as urticaria, rash, itching, and rarely Quincke's edema. Some children have experienced nausea, vomiting, weight gain, hypertension, mood disorders, fever, abnormal vision, and pain at the injection site. The above adverse reactions may occur even when the treatment is satisfactory. If the patient experiences the above adverse reactions or adverse reactions not listed in this manual, please notify the doctor immediately.

Precautions

It is contraindicated for those who are allergic to GnRH, GnRH analogs or any of the ingredients of the drug. Pregnancy, if in doubt, please consult your doctor.

Drug Interactions

Not yet clear.

Storage

Store below 25℃.

Validity Period

24 months.

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