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効能
抗悪性腫瘍薬, 性腺刺激ホルモン放出ホルモン受容体作動薬
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説明
Decapeptyl is a modified (D-Trp6) LH-RH. Like recently marketed buserelin and
leuprolide (I), it is useful in achieving medical castration in the treatment of advanced prostate cancer.
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使用
Triptorelin is a GnRH agaonist shown to inhibit estradiol-induced cancer cell proliferation.
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定義
ChEBI: An oligopeptide comprising pyroglutamyl, histidyl, tryptophyl, seryl, tyrosyl, D-tryptophyl, leucyl, arginyl, prolyl and glycinamide residues joined in sequence. It is an agonist analogue of gonadotropin-releasing hormone.
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臨床応用
Triptorelin pamoate is another superagonist of GnRH, which like nafarelin acetate contains only
a single amino acid substitution (D-Trp6 for Gly6) when compared to the natural hormone. In the treatment of advanced prostate cancer, it is important to reduce serum
testosterone levels to very low levels, which can be achieved surgically by orchiectomy. When
this surgical method is unacceptable to the patient, an alternative approach is “chemical
castration,” which can be achieved by use of estrogen therapy, leuprolide,goserelin or histrelin acetates, and now, triptorelin pamoate. This product is available for IM
depot injection (monthly or every 3 months), wherein serum testosterone concentration drops to
a level generally seen in surgically castrated men.
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副作用
The side effects of Triptorelin: Painful or difficult urination, burning when you urinate, blood in the urine; bone pain; (in children) new or worsening signs of puberty; a seizure; chest pain or pressure, pain spreading to your jaw or shoulder; sudden numbness or weakness, slurred speech; increased pressure inside the skull - severe headaches, ringing in your ears, dizziness, nausea, vision problems, pain behind your eyes; loss of movement in any part of your body; high blood sugar - increased thirst, increased urination, hunger, dry mouth, fruity breath odor; or nerve problems - back pain, muscle weakness, problems with balance or coordination, severe numbness or tingling in your legs or feet, loss of bladder or bowel control.
