(trip toe REL in)
- Triptorelin Embonate
- Triptorelin Pamoate
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Suspension Reconstituted, Intramuscular:
Trelstar: 3.75 mg (1 ea [DSC]); 11.25 mg (1 ea [DSC]) [contains polysorbate 80]
Trelstar Mixject: 3.75 mg (1 ea); 11.25 mg (1 ea); 22.5 mg (1 ea) [contains polysorbate 80]
Brand Names: U.S.
- Trelstar Mixject
- Trelstar [DSC]
- Gonadotropin Releasing Hormone Agonist
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.
Vd: 30 to 33 L
Unknown; unlikely to involve CYP; no known metabolites
Urine (42% as intact peptide); hepatic
Time to Peak
1 to 3 hours
2.8 ± 1.2 hours
Moderate-to-severe renal impairment: 6.6 to 7.7 hours
Hepatic impairment: 7.6 hours
Special Populations: Renal 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.
Special Populations: 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.
Special Populations: Elderly
Triptorelin clearance is partly correlated to total CrCl, which is well known to decrease with age.
Use: Labeled Indications
Advanced prostate cancer: Palliative treatment of advanced prostate cancer
Assisted reproductive technologies: Decapeptyl [Canadian product]: Adjunctive therapy in women undergoing controlled ovarian hyperstimulation for assisted reproductive technologies (ART)
Off Label Uses
Based on The World Federation of Societies of Biological Psychiatry (WFSBP) Guidelines for the Biological Treatment of Paraphilias, triptorelin given for paraphilia/hypersexuality is an effective and recommended treatment option in the management of this condition.
Additional Off-Label Uses
Endometriosis; In vitro fertilization; Precocious puberty; Uterine sarcoma
Hypersensitivity to triptorelin or any component of the formulation, other GnRH agonists or GnRH; pregnancy
Canadian labeling: Additional contraindications (not in US labeling): Breast-feeding women
Advanced prostate carcinoma: IM:
3.75 mg once every 4 weeks or
11.25 mg once every 12 weeks or
22.5 mg once every 24 weeks
Controlled ovarian hyperstimulation for assisted reproductive technologies (ART) (adjunctive therapy): Decapeptyl [Canadian product]): Females: SubQ: Usual dose: 0.1 mg once daily initiated on day 2 or 3 or days 21 to 23 of menstrual cycle (or 5 to 7 days prior to expected onset of menses). Dose may be adjusted according to ovarian response as measured by ovarian ultrasound with or without serum estradiol levels. Treatment is continued until follicles achieve suitable size (typically 4 to 7 weeks).
Treatment of paraphilia/hypersexuality (off-label use; Guay, 2009; Thibaut, 1993): Males:
Note: May cause an initial increase in androgen concentrations which may be treated with an antiandrogen (eg, flutamide, cyproterone) for 1 to 2 months (Guay, 2009). Avoid use in patients with osteoporosis or active pituitary pathology.
SubQ: Test dose: 1 mg (observe for hypersensitivity)
IM: 3.75 mg monthly
Refer to adult dosing.
Dosing: Renal Impairment
There are no dosage adjustments provided in the manufacturer’s labeling. However, renal impairment increases systemic exposure to triptorelin.
Dosing: Hepatic Impairment
There are no dosage adjustments provided in the manufacturer’s labeling. However, hepatic impairment increases systemic exposure to triptorelin.
Trelstar: Reconstitute with 2 mL sterile water for injection. Shake well to obtain a uniform suspension. Solution will appear milky. Administer immediately after reconstitution.
MIXJECT System: Follow manufacturer's instructions for mixing prior to use.
Administer by IM injection into the buttock; alternate injection sites. Administer immediately after reconstitution.
Decapeptyl [Canadian product] is administered by subcutaneous injection into the lower abdomen; alternate injection sites. If a dose is missed, it can be administered on the same day; however, do not double doses.
Trelstar: Store at 20°C to 25°C (68°F to 77°F). Do not freeze MIXJECT system. Administer immediately after reconstitution.
Decapeptyl [Canadian product]: Store at 2°C to 8°C (36°F to 46°F); do not freeze. Protect from light.
Antidiabetic Agents: Hyperglycemia-Associated Agents may diminish the therapeutic effect of Antidiabetic Agents. Monitor therapy
Choline C 11: Luteinizing Hormone-Releasing Hormone Analogs may diminish the therapeutic effect of Choline C 11. Monitor therapy
Corifollitropin Alfa: Luteinizing Hormone-Releasing Hormone Analogs may enhance the therapeutic effect of Corifollitropin Alfa. Avoid combination
Highest Risk QTc-Prolonging Agents: QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying) may enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Management: Avoid such combinations when possible. Use should be accompanied by close monitoring for evidence of QT prolongation or other alterations of cardiac rhythm. Consider therapy modification
Indium 111 Capromab Pendetide: Luteinizing Hormone-Releasing Hormone Analogs may diminish the diagnostic effect of Indium 111 Capromab Pendetide. Avoid combination
MiFEPRIStone: May enhance the QTc-prolonging effect of QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying). Management: Though the drugs listed here have uncertain QT-prolonging effects, they all have some possible association with QT prolongation and should generally be avoided when possible. Consider therapy modification
Moderate Risk QTc-Prolonging Agents: QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying) may enhance the QTc-prolonging effect of Moderate Risk QTc-Prolonging Agents. Monitor therapy
Pituitary-gonadal function may be suppressed with chronic administration and for up to 8 weeks after triptorelin therapy has been discontinued.
Prostate cancer: As reported with all strengths; frequency of effect may vary by strength:
Endocrine & metabolic: Hot flash (59% to 72%), increased serum glucose, increased testosterone (peak: days 2-4; decline to low levels by weeks 3-4)
Hematologic & oncologic: Decreased hemoglobin, decreased red blood cells
Hepatic: Increased serum alkaline phosphatase (2% to >10%), increased serum ALT, increased serum AST
Neuromuscular & skeletal: Musculoskeletal pain (12% to 13%)
Renal: Increased blood urea nitrogen
1% to 10%:
Cardiovascular: Lower extremity edema (6%), hypertension (≤4%), chest pain (2%), dependent edema (2%), peripheral edema (≤1%)
Central nervous system: Headache (2% to 7%), pain (2% to 3%), dizziness (1% to 3%), fatigue (2%), insomnia (1% to ≤2%), emotional lability (1%)
Dermatologic: Skin rash (2%), pruritus (1%)
Endocrine & metabolic: Decreased libido (2%), gynecomastia (2%)
Gastrointestinal: Nausea (3%), anorexia (2%), constipation (2%), dyspepsia (2%), mastalgia (2%), vomiting (2%), abdominal pain (1%), diarrhea (1%)
Genitourinary: Erectile dysfunction (10%), testicular atrophy (8%), impotence (2% to 7%), dysuria (5%), urinary retention (≤1%), urinary tract infection (≤1%)
Hematologic & oncologic: Anemia (1%)
Local: Pain at injection site (4%)
Neuromuscular & skeletal: Leg pain (2% to 5%), back pain (≤3%), leg cramps (2%), arthralgia (≤2%), myalgia (1%), weakness (1%)
Ophthalmic: Conjunctivitis (1%), eye pain (1%)
Respiratory: Cough (2%), dyspnea (1%), pharyngitis (1%)
Central nervous system: Headache (4% to 27%)
Gastrointestinal: Abdominal pain (9% to 15%)
Genitourinary: Vaginal hemorrhage (2% to 24%)
Local: Inflammation at injection site (10% to 12%)
1% to 10%:
Cardiovascular: Flushing (4%)
Central nervous system: Dizziness (4% to 5%), fatigue (3% to 4%), malaise (2%)
Endocrine & metabolic: Spontaneous abortion (7%), dysmenorrhea (2% to 6%), ovarian hyperstimulation syndrome (3%), hot flash (2%), ovarian cyst (1%)
Gastrointestinal: Nausea (3% to 10%), vomiting (3%), abdominal distension (2%), diarrhea (2%)
Genitourinary: Pelvic pain (6%), gynecological pain (adnexa uteri, 2%), leukorrhea (2%)
Local: Pain at injection site (4% to 7%), bruising at injection site (3%), injection site reaction (2% to 3%)
Neuromuscular & skeletal: Postoperative pain (3% to 4%), back pain (3%)
Respiratory: Upper respiratory tract infection (4%), flu-like symptoms (3%), pharyngitis (3%), dyspnea (2%), rhinitis (2%)
Postmarketing and/or case reports (all indications; limited to important or life-threatening): Anaphylactic shock, anaphylaxis, angioedema, bladder outflow obstruction, blurred vision, cerebrovascular accident, circulatory shock, deep vein thrombosis, dyspareunia, exacerbation of depression, hematuria, hypersensitivity reaction, increased appetite, myocardial infarction, neuropathy, pituitary apoplexy, prolonged Q-T interval on ECG, pulmonary embolism, renal insufficiency, seizure, sleep disorder, spinal cord compression, thrombophlebitis, tissue necrosis at injection site, transient ischemic attacks, tumor flare, urethral obstruction, vaginal dryness
Concerns related to adverse effects:
• Cardiovascular effects: Androgen-deprivation therapy (ADT) may increase the risk for cardiovascular disease (Levine, 2010). Myocardial infarction, sudden cardiac death and stroke have been reported in men receiving GnRH agonists. ADT may prolong the QT/QTc interval; consider the benefits of ADT versus the risk for QT prolongation in patients with a history of QTc prolongation, congenital long QT syndrome, heart failure, frequent electrolyte abnormalities, and in patients with medications known to prolong the QT interval. Consider periodic monitoring of electrocardiograms and electrolytes in at-risk patients.
• Decreased bone density: Use with caution in patients with risk factors for decreased bone mineral density; may increase risk for osteoporosis and bone fractures particularly with prolonged use.
• Hyperglycemia: Hyperglycemia and an increased risk of developing diabetes has been reported with therapy and may manifest as diabetes or worsening of glycemic control in patients with diabetes. Monitor blood glucose and/or glycosylated hemoglobin (HbA1c) as clinically necessary.
• Hypersensitivity reactions: Angioedema and anaphylactic shock have occurred; discontinue use if severe reaction occurs.
• Ovarian hyperstimulation syndrome: Decapeptyl [Canadian product]: Ovarian hyperstimulation syndrome (OHSS) is a rare exaggerated response to ovulation induction therapy (Corbett 2014; Fiedler 2012). This syndrome may begin within 24 hours of treatment but may become most severe 7 to 10 days after therapy (Corbett 2014). Symptoms of mild/moderate OHSS may include abdominal distention/discomfort, diarrhea, nausea, and/or vomiting. Severe OHSS symptoms may include severe abdominal pain, anuria/oliguria, ascites, severe dyspnea, hypotension, or nausea/vomiting (intractable). Decreased creatinine clearance, hemoconcentration, hypoproteinemia, elevated liver enzymes, elevated WBC, and electrolyte imbalances may also be present (ASRM 2016; Corbett 2014; Fiedler 2012). Treatment is primarily symptomatic and includes fluid and electrolyte management, analgesics, and prevention of thromboembolic complications (ASRM 2016; SOGC-CFAS 2011). Therapy with gonadotropins should be stopped.
• Pituitary apoplexy: Rare cases of pituitary apoplexy (frequently secondary to pituitary adenoma) have been observed with GnRH agonist administration (onset from 1 hour to usually <2 weeks); may present as sudden headache, vomiting, visual or mental status changes, and infrequently cardiovascular collapse; immediate medical attention required.
• Spinal cord compression: Cases of spinal cord compression, which may contribute to weakness or paralysis (possible fatal complications), have been reported; observe patients with metastatic vertebral lesions closely during the first few weeks of treatment.
• Tumor flare: Transient initial increases in testosterone can lead to worsening symptoms (bone pain, hematuria, urethra/bladder outlet obstruction, neuropathy) of prostate cancer during the first few weeks of therapy.
• Urinary tract obstruction: Observe patients with urinary tract obstruction closely during the first few weeks of treatment.
Serum testosterone levels, prostate-specific antigen, glucose and HbA1c (periodically), bone density, signs and symptoms of emerging cardiovascular disease; consider periodic monitoring of electrocardiograms and electrolytes.
Decapeptyl [Canadian product]: Negative pregnancy test prior to initiation of therapy; signs/symptoms of allergic reaction for 30 minutes after administration; ultrasound and/or estradiol levels to assess follicle development; ultrasound to assess number and size of follicles
OHSS: Monitoring of hospitalized patients should include abdominal circumference, albumin, cardiorespiratory status, electrolytes, fluid balance, hematocrit, hemoglobin, serum creatinine, urine output, urine specific gravity, vital signs, weight (daily or as necessary) and liver enzymes (weekly) (SOGC-CFAS 2011).
Treatment of paraphilia/hypersexuality (off-label use): The following monitoring has been recommended for other GnRH agonists: CBC (baseline, monthly for 4 months then every 6 months); serum testosterone (baseline, monthly for 4 months then every 6 months); serum LH (baseline and every 6 months), FSH (baseline), serum BUN and creatinine (baseline and every 6 months); bone density (baseline and yearly); ECG (baseline) (Reilly 2000)
Pregnancy Risk Factor
Use is contraindicated in pregnant women. When used for ART, pregnancy must be ruled out prior to therapy and nonhormonal contraception should be used until menses occurs. Due to the short half-life of triptorelin (formulations used for ART), it is not expected to be present in the maternal serum at the time of embryo transfer. In case reports, spontaneous abortion, congenital anomalies, and other adverse events have been reported following triptorelin (Decapeptyl) exposure during pregnancy.
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience sexual dysfunction, loss of libido, hot flashes, or insomnia. Have patient report immediately to prescriber signs of pituitary apoplexy (sudden headache, vomiting, passing out, mood changes, eye weakness, unable to move eyes, or change in eyesight), signs of high blood sugar (confusion, feeling sleepy, more thirst, hunger, passing urine more often, flushing, fast breathing, or breath that smells like fruit), signs of DVT (edema, warmth, numbness, change in color, or pain in the extremities), signs of severe cerebrovascular disease (change in strength on one side is greater than the other, trouble speaking or thinking, change in balance, or change in eyesight), shortness of breath, excessive weight gain, swelling of arms or legs, difficult urination, severe headache, severe dizziness, passing out, back pain, hematuria, dark urine, breast pain, burning or numbness feeling, tachycardia, arrhythmia, chills, pharyngitis, mood changes, painful urination, severe muscle pain, severe joint pain, leg cramps, severe loss of strength and energy, angina, or bone pain (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
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- Drug class: gonadotropin releasing hormones