Pronunciation: TRIP-toe-REL-in PAM-oh-ate
Class: Gonadotropin-releasing hormone
- Injection, lyophilized microgranules for suspension 3.75 mg
- Injection, lyophilized microgranules for suspension 11.25 mg
- Injection, lyophilized microgranules for suspension 22.5 mg
Synthetic analog of gonadotropin-releasing hormone (GnRH) that acts as potent inhibitor of gonadotropin secretion.
C max is approximately 28.43 ng/mL, 38.5 ng/mL, and 44.1 ng/mL for triptorelin 3.75 mg, 11.25 mg, and 22.5 mg, respectively. T max is 1 to 3 h.
Vd is 30 to 33 L (from an IV dose of 0.5 mg). There is no evidence of protein binding.
No metabolites are found. Pharmacokinetic data suggest that C-terminal fragments produced by tissue degradation are either completely degraded in the tissues or are rapidly degraded further in plasma, or cleared by the kidneys.
Triptorelin is eliminated by both the liver and kidneys. 41.7% of a dose is excreted in urine.
Time to peak effect occurs on day 4, days 2 to 3, or on day 3 for triptorelin 3.75 mg, 11.25 mg, or 22.5 mg, respectively.
Duration of action is 4 wk for triptorelin 3.75 mg, and 3 to 4 wk for triptorelin 11.25 and 22.5 mg.
Special PopulationsRenal Function Impairment
There is a decrease in total Cl proportional to decrease in CrCl and increased Vd and half-life. Patients with renal impairment had 2- to 4-fold higher exposure (AUC) values than younger healthy men.Hepatic Function Impairment
The decrease in triptorelin Cl is more pronounced. Triptorelin half-life increase is similar to renal impairment. Patients with hepatic impairment had 2- to 4-fold higher exposure (AUC) values than younger healthy men.Elderly
Triptorelin clearance is partly correlated to total CrCl, which is well known to decrease with age.Children
Not evaluated in patients younger than 18 y of age.Race
The effects of race have not been systematically studied.
Indications and Usage
Palliative treatment of advanced prostate cancer.
Treatment of ovarian cancer, pancreatic carcinoma, endometriosis, hyperandrogenism, growth hormone deficiency, in vitro fertilization, uterine leiomyomata, central precocious puberty.
Hypersensitivity to triptorelin or any component of product, or other GnRH agonists or GnRH; pregnancy.
Dosage and AdministrationAdvanced Prostate Cancer
IM Dosing schedule depends on product strength selected. 3.75 mg once every 4 wk; 11.25 mg once every 12 wk; 22.5 mg once every 24 wk.
- For IM use only.
- Because of different release characteristics, dosage strengths are not additive and must be selected based upon the desired dosing schedule.
- Reconstitute with sterile water; do not use any other diluent.
- Administer triptorelin with a 21-guage needle immediately after reconstitution.
- Inject into either buttock; rotate injection sites.
Store at 68° to 77°F. Do not freeze.
Drug InteractionsHyperprolactinemic drugs
Do not coadminister with triptorelin because hyperprolactinemia reduces the number of pituitary GnRH receptors.
Laboratory Test Interactions
Because chronic or continuous administration of triptorelin suppresses pituitary-gonadal axis, diagnostic tests of the pituitary-gonadal function performed during triptorelin treatment or after cessation of therapy may be misleading.
Headache (8%); insomnia (5%); dizziness (3%); fatigue (2%); emotional lability, asthenia (1%).
Rash (2%); pruritus (1%).
Conjunctivitis, eye pain (1%).
Nausea (3%); anorexia, constipation, dyspepsia, vomiting (2%); abdominal pain, diarrhea (1%).
UTI (12%); erectile dysfunction (10%); testicular atrophy (8%); impotence (7%); dysuria, urinary retention (5%); breast pain, decreased libido, gynecomastia (2%).
Decreased hemoglobin and red blood cell count, increased glucose, BUN, AST, ALT, and alkaline phosphatase (10% or more).
Leg edema (6%); diabetes mellitus/hyperglycemia, peripheral edema (5%); dependent edema (2%).
Skeletal pain (13%); back pain (11%); arthralgia, pain in extremity (8%); leg pain (5%); leg cramps (2%); myalgia (1%).
Bronchitis (5%); coughing (2%); dyspnea, pharyngitis (1%).
Hot flushes (73%); influenza (16%); hypertension (14%); injection-site pain (4%); pain (3%); chest pain (2%); abnormal hepatic function, anemia (1%); pituitary apoplexy (postmarketing).
Monitor response to triptorelin by measuring serum levels of testosterone. Closely observe patients with metastatic vertebral lesions and/or with upper or lower urinary tract obstruction during the first few weeks of therapy.
Category X .
Safety and efficacy not established.
Anaphylactic reactions reported.
Worsening of signs and symptoms
Initial transient increase in testosterone may lead to worsening of signs and symptoms of prostate cancer (eg, bone pain, urethral or bladder outlet obstruction) during first few weeks of treatment. Cases of spinal cord compression have been reported with GnRH agonists.
- Advise patient, family, or caregiver that medication will be prepared and administered by a health care provider in a health care setting.
- Educate patient, family, or caregiver of importance of returning as scheduled for additional injections in order to achieve maximal benefits from the medication.
- Advise patient, family, or caregiver that medication may temporarily worsen signs and symptoms of the disease (eg, bone pain, blood in urine, difficult or painful urination) but that these should improve in 3 to 4 wk.
- Advise patient, family, or caregiver to immediately report any of the following to the health care provider: rash; itching or hives; swelling of the face, lips, eyes, or tongue; wheezing; shortness of breath; difficulty breathing; weakness or paralysis of legs; inability to urinate.
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