Name | Triptorelin acetate |
Synonyms | OvuGel BIM 21003C Decapeptyl-Depot Triptelin Acetate Triptorelin acetate Triptorelin Acetate OR Triptorelin PaMoate 6-D-Tryptophan Luteinizing HorMone-Releasing Factor (Pig) Acetate 6-D-Tryptophan Luteinizing HorMone-Releasing Factor (Swine) Acetate 5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-tryptophyl-L-leucyl-L-arginyl-L-prolylglycinamide Glycinamide, 5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-tryptophyl-L-leucyl-L-arginyl-L-prolyl- |
CAS | 140194-24-7 |
InChI | InChI=1/C64H82N18O13/c1-34(2)23-46(56(88)75-45(13-7-21-69-64(66)67)63(95)82-22-8-14-52(82)62(94)72-31-53(65)85)76-58(90)48(25-36-28-70-42-11-5-3-9-40(36)42)78-57(89)47(24-35-15-17-39(84)18-16-35)77-61(93)51(32-83)81-59(91)49(26-37-29-71-43-12-6-4-10-41(37)43)79-60(92)50(27-38-30-68-33-73-38)80-55(87)44-19-20-54(86)74-44/h3-6,9-12,15-18,28-30,33-34,44-52,70-71,83-84H,7-8,13-14,19-27,31-32H2,1-2H3,(H2,65,85)(H,68,73)(H,72,94)(H,74,86)(H,75,88)(H,76,90)(H,77,93)(H,78,89)(H,79,92)(H,80,87)(H,81,91)(H4,66,67,69)/t44-,45-,46-,47-,48+,49-,50-,51-,52-/m0/s1 |
Molecular Formula | C64H82N18O13.C2H4O2 |
Molar Mass | 1371.52 |
Density | 1.52g/cm3 |
Refractive Index | 1.723 |
Use | Hormonal down-regulation required for infertility treatment |
Overview | triptorelin acetate is the acetate of triptorelin, the active ingredient is triptorelin, triptorelin is a synthetic and highly effective agonist analog, which was first marketed in Germany in 1986. In order to improve the bioavailability of general drugs, many salt formation increases the solubility and then improves the bioavailability. Therefore, the pharmacological effects and adverse reactions of the two are consistent. Triptorelin acetate injection and sustained and controlled release preparation of two dosage forms. Triptorelin acetate is 5-oxoprolyl-L-group Aminoacyl-L-seryl-L-tyrosyl-D-Seryl-L-leucyl-L-arginyl-L-prolyl-L-glycinamide acetate, formula C64H82N18O13.XC2H4O2, molecular weight 1311.46.X60.02. Based on the calculation of water-free and acetic acid-free, the content of C64H82N18O13 shall be 97.0% ~ 103.0%. |
pharmacological action | the active ingredient of triptorelin acetate is a synthetic analog of gonadotropin-releasing hormone, the structural improvement is that the sixth L-glycine in the natural molecular structure is replaced by d-tryptophan, so that its effect is more significant and the half-time of plasma is longer. After injection, the drug initially stimulates the pituitary gland to release luteinizing hormone and ovalbumin. When the pituitary gland is chronically stimulated to enter a refractory period, the release of gonadotropins is reduced, thereby reducing sex steroids to castrate levels. The effects are reversible. The drug was absorbed rapidly by subcutaneous administration, and the plasma concentration reached the peak value in 15-60 min and reached the maximum effect in 1 h. Intramuscular injection of sustained-release preparation could maintain the curative effect for more than 28d. |
indications | triptorelin acetate is mainly used for the treatment of endometriosis, hormone-dependent prostate cancer, breast cancer, and true precocious puberty in children, it can also be used in assisted reproductive technology. Injection: the usual amount is 500 μg once a day for 7 consecutive days, then 100 μg once a day, subcutaneous injection as a maintenance amount. Controlled release agent: 3.75mg is injected subcutaneously or intramuscularly every 4 weeks, and each injection should be carried out in different parts of the body. In vitro fertilization: 1 times a day, each time 500 μg, subcutaneous injection, 7~10 days, 1 times a day, each time 100 μg. |