Central precocious puberty. Prostate cancer, Palliative treatment, advanced disease. Used with radiotherapy and continued after to treat high-risk localized or locally advanced prostate cancer.<20240708>
藥理
Triptorelin is an agonist analog of gonadotropin releasing hormone (GnRH) and causes suppression of ovarian and testicular steroidogenesis due to decreased levels of LH and FSH with subsequent decrease in testosterone (male) and estrogen (female) levels. After chronic and continuous administration, usually 2 to 4 weeks after initiation, a sustained decrease in LH and FSH secretion occurs. When used for ART, prevents premature LH surge in women undergoing controlled ovarian hyperstimulation.(UTD)
藥動學
Distribution:
Vd, healthy young men: 0.4 L/kg
Vd, hepatic impairment: 0.49 L/kg
Vd, renal insufficiency: 0.58 to 0.68 L/kg
Metabolism:
CYP450 metabolism unlikely
Excretion:
Renal: 41.7% (healthy men) ; 62% (hepatic impairment); 5% to 17% (renal impairment)
Elimination Half Life:
Healthy men: 2.81 hours
Hepatic impairment, 7.58 hours
Moderate and severe renal impairment: 6.56 and 7.65 hours .
禁忌症
Hypersensitivity to triptorelin or any other component of the product .
Hypersensitivity to other gonadotropin-releasing hormone (GnRH) agonists or to GnRH .
Existing or potential for pregnancy.
懷孕分類
X (FDA)
哺乳分類
Infant risk cannot be ruled out.(MDX)
副作用
Common:
Cardiovascular: Hypertension (3.6% to 14.2% ), Peripheral edema (1.1% to 6.3% )
Dermatologic: Injection site pain (Adults, 3.6% to 4% ; pediatrics, 45% )
Endocrine metabolic: Hot sweats (58.6% to 73% ; pediatrics, 4.5% )
Gastrointestinal: Gastroenteritis (6.8% ), Nausea (2.9% ), Vomiting (2.1% )
Musculoskeletal: Arthralgia (2.3% to 7.5% ), Backache (2.9% to 10.8% ), Bone pain (12.1% to 13.2% ), Pain in limb (2.1% to 7.5% )
Neurologic: Dizziness (1.4% to 2.9% ), Headache (Adults, 6.9% to 7.5% ; pediatrics, 13.6% ), Insomnia (1.7% to 5% )
Renal: Dysuria (4.6% ), Urinary retention (1.1% to 5% ), Urinary tract infectious disease (1.4% to 11.6% )
Reproductive: Atrophy of testis (7.5% ), Erectile dysfunction (10% ), Erectile dysfunction (2.3% to 7.1% ), Pain of breast (2.3% ), Reduced libido (2.3% )
Respiratory: Nasopharyngitis (13.6% ), Upper respiratory infection (9.1% )
Other: Fatigue (2.1% to 2.3% ), Influenza (Adults, 15.8% ; pediatrics, 4.5% ), Pain (2.1% to 3.4% )
Serious:
Endocrine metabolic: Pituitary apoplexy
Immunologic: Anaphylaxis, Hypersensitivity reaction, Sepsis
Neurologic: Seizure
Psychiatric: Psychiatric symptom
Reproductive: Disorder of puberty
Other: Angioedema, Tumor flare (8% )
劑量和給藥方法
Prostate cancer, Palliative treatment, advanced disease:
3.75 mg IM every 4 wk
11.25 mg IM every 12 wk
22.5 mg IM every 24 wk
小兒調整劑量
Central precocious puberty:(2 years or older) 22.5 mg IM every 24 weeks.