Version May 2024
Assisted reproductive technologies, controlled ovarian hyperstimulation, adjunctive therapy: Decapeptyl [Canadian product]: 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).
Breast cancer, premenopausal ovarian suppression during adjuvant endocrine therapy (off-label use): IM: 3.75 mg once every 28 days ± 3 days (in combination with adjuvant endocrine therapy) for ~5 years; if receiving chemotherapy, begin ovarian suppression with the start of chemotherapy (Bellet 2016; Pagani 2014).
Breast cancer, premenopausal ovarian preservation during chemotherapy (off-label use): IM: 3.75 mg once every 28 days beginning at least 1 week prior to chemotherapy and continuing throughout chemotherapy (Lambertini 2015).
Breast cancer in male patients, hormone receptor–positive (off-label use): Note: Should be used in combination with an aromatase inhibitor (Ref).
Advanc ed or metastatic disease: IM: 3.75 mg once every 4 weeks (Ref). Endocrine therapy for males with advanced or metastatic, HR+, HER2-negative breast cancer may be sequenced as in females (Ref).
Endometrial stromal sarcoma (off-label use): IM: 3.75 mg once every 28 days for ~3 to 5 months (Jin 2015).
Endometriosis (off-label use):
Note: Hormonal add-back therapy (eg, estrogens or progestins) is recommended at the start of treatment to reduce bone mineral loss (Dunselman 2014; SOGC [Leyland 2010]).
IM: 3.75 mg once every 4 weeks for a total of 6 doses (Bergqvist 1998; Choktanasiri 1996) or 3.75 mg once every 6 weeks for a total of 4 doses (Tse 2000) or 11.25 mg once every 3 months (Donnez 2004). Duration of therapy is not well established (Dunselman 2014) but should be evaluated after 3 months (SOGC [Leyland 2010]); in general, use of GnRH agonists is limited to less than 6 or 12 months due to adverse events (Leone Roberti Maggiore 2014).
Paraphilia, males (off-label use):
Note: May cause an initial increase in androgen concentrations; concomitant antiandrogen therapy (eg, cyproterone, flutamide) is recommended starting 1 week before and continued for the first month after triptorelin initiation (Guay 2009; WFSBP [Thibaut 2020]). Avoid use in patients with severe osteoporosis (especially in patients with prior fracture) or active pituitary disease (WFSBP [Thibaut 2020]).
IM: 3.75 mg once monthly (Thibaut 1993; WFSBP [Thibaut 2020]) or 11.25 mg every 3 months (Ho 2012; WFSBP [Thibaut 2020]). If therapy is discontinued, rebound elevation in testosterone levels and recurrence of symptoms may occur; follow-on therapy with another agent is recommended (WFSBP [Thibaut 2020]).
Prostate cancer, advanced: Trelstar:
IM: 3.75 mg once every 4 weeks or
IM: 11.25 mg once every 12 weeks or
IM: 22.5 mg once every 24 weeks.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling. However, kidney impairment increases systemic exposure to triptorelin.
There are no dosage adjustments provided in the manufacturer's labeling. However, hepatic impairment increases systemic exposure to triptorelin.
Refer to adult dosing.
(For additional information see "Triptorelin: Pediatric drug information")
Central precocious puberty: Children ≥2 years: Triptodur: IM: 22.5 mg once every 24 weeks; discontinue therapy at appropriate age of onset of puberty.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling; however, in adult patients, renal impairment increased systemic exposure to triptorelin.
There are no dosage adjustments provided in the manufacturer's labeling; however, in adult patients, hepatic impairment increased systemic exposure to triptorelin.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
Central precocious puberty:
Reported adverse reactions are for children and adolescents.
>10%:
Local: Erythema at injection site, pain at injection site
Nervous system: Headache
Respiratory: Nasopharyngitis
1% to 10%:
Endocrine & metabolic: Hot flash, menstruation
Gastrointestinal: Gastroenteritis
Infection: Influenza
Local: Injection-site pruritus, swelling at injection site
Nervous system: Anxiety, mood changes
Otic: Otitis externa
Respiratory: Bronchitis, cough, pharyngitis, sinusitis, upper respiratory tract infection
Prostate cancer:
Reported adverse reactions are for adults.
>10%:
Endocrine & metabolic: Hot flash (59% to 73%), increased serum glucose
Hepatic: Increased serum alanine aminotransferase, increased serum aspartate aminotransferase, increased serum transaminases
Neuromuscular & skeletal: Skeletal pain (12% to 13%)
Renal: Increased blood urea nitrogen
1% to 10%:
Cardiovascular: Chest pain (2%), dependent edema (2%), hypertension (≤4%), lower extremity edema (6%), peripheral edema (1%)
Dermatologic: Pruritus (1%), skin rash (2%)
Endocrine & metabolic: Decreased libido (2%), gynecomastia (2%)
Gastrointestinal: Abdominal pain (1%), anorexia (2%), constipation (2%), diarrhea (1%), dyspepsia (2%), nausea (3%), vomiting (2%)
Genitourinary: Dysuria (5%), erectile dysfunction (2% to 10%), mastalgia (2%), testicular atrophy (8%), urinary retention (1%), urinary tract infection (1%)
Hematologic & oncologic: Anemia (1%)
Hepatic: Hepatic impairment (1%), increased serum alkaline phosphatase (≥2%)
Local: Pain at injection site (4%)
Nervous system: Asthenia (1%), dizziness (1% to 3%), emotional lability (1%), fatigue (2%), headache (2% to 7%), insomnia (≤2%), pain (2% to 3%)
Neuromuscular & skeletal: Arthralgia (≤2%), back pain (≤3%), lower extremity pain (2% to 5%), lower limb cramp (2%), myalgia (1%)
Ophthalmic: Conjunctivitis (1%), eye pain (1%)
Respiratory: Cough (2%), dyspnea (1%), pharyngitis (1%)
<1%: Neuromuscular & skeletal: Limb pain
Postmarketing (any indication):
Dermatologic: Urticaria
Hypersensitivity: Anaphylactic shock, angioedema, hypersensitivity reaction, nonimmune anaphylaxis
Nervous system: Aggressive behavior, depression, intracranial hypertension (idiopathic) (Tan 2019), irritability, outbursts of anger, seizure, suicidal ideation, suicidal tendencies
Ophthalmic: Visual disturbance, visual impairment
Miscellaneous: Crying
Hypersensitivity to triptorelin or any component of the formulation, other gonadotropin-releasing hormone (GnRH) agonists or GnRH; pregnancy.
Canadian labeling: Additional contraindications (not in the US labeling): Breastfeeding; undiagnosed abnormal vaginal bleeding (when used for endometriosis).
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.
• Decreased bone density: Use with caution in patients with risk factors for decreased bone mineral density; GnRH agonist therapy may increase risk for osteoporosis and bone fractures particularly with prolonged use.
• Hypersensitivity reactions: Angioedema and anaphylactic shock have occurred; discontinue use if severe reaction occurs.
• Metabolic syndrome: Metabolic changes (such as hyperglycemia, diabetes, hyperlipidemia) may occur; metabolic dysfunction associated steatotic liver disease, including cirrhosis, has also been reported. Hyperglycemia may manifest as diabetes or worsening of glycemic control in patients with diabetes.
• 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.
• Pseudotumor cerebri: Pseudotumor cerebri (idiopathic intracranial hypertension) has been reported in pediatric patients receiving GnRH agonists, including triptorelin.
• Psychiatric effects: Symptoms of emotional lability (eg, crying, irritability, anger, aggression, impatience) have been reported with GnRH agonists, including triptorelin; monitor for the development or worsening of psychiatric symptoms.
• Seizures: Seizures have been reported with GnRH agonists, including triptorelin in patients with or without a history of seizures or other conditions or concurrent medications associated with seizures.
• 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.
• Symptom flare: Transient initial increases in gonadotropins and sex steroids leading to a worsening of symptoms may be observed during the first few weeks of therapy or after subsequent doses. Testosterone levels increased above baseline and then decreased to castrate levels (<50 ng/dL) within 4 weeks. Patients with prostate cancer may experience new or increased bone pain, neuropathy, hematuria, or urethral or bladder outlet obstruction. Female patients with central precocious puberty may experience transient vaginal bleeding.
Disease-related concerns:
• Urinary tract obstruction: Observe patients with urinary tract obstruction closely during the first few weeks of treatment.
Dosage form specific issues:
• Polysorbate 80: Some dosage forms may contain polysorbate 80 (also known as Tweens). Hypersensitivity reactions, usually a delayed reaction, have been reported following exposure to pharmaceutical products containing polysorbate 80 in certain individuals (Isaksson 2002; Lucente 2000; Shelley 1995). Thrombocytopenia, ascites, pulmonary deterioration, and renal and hepatic failure have been reported in premature neonates after receiving parenteral products containing polysorbate 80 (Alade 1986; CDC 1984). See manufacturer's labeling.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Suspension Reconstituted, Intramuscular:
Trelstar Mixject: 11.25 mg (1 ea); 22.5 mg (1 ea) [contains polysorbate 80]
Suspension Reconstituted, Intramuscular [preservative free]:
Trelstar Mixject: 3.75 mg (1 ea); 11.25 mg (1 ea [DSC]); 22.5 mg (1 ea [DSC]) [contains polysorbate 80]
Suspension Reconstituted ER, Intramuscular:
Triptodur: 22.5 mg (1 ea) [contains polysorbate 80]
No
Suspension (reconstituted) (Trelstar Mixject Intramuscular)
3.75 mg (per each): $975.89
11.25 mg (per each): $2,927.66
22.5 mg (per each): $5,855.33
Suspension Reconstituted ER (Triptodur Intramuscular)
22.5 mg (per each): $23,832.91
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution Prefilled Syringe, Subcutaneous:
Decapeptyl: 0.1 mg/mL (1 mL)
Suspension Reconstituted, Intramuscular:
Trelstar: 3.75 mg (1 ea); 11.25 mg (1 ea); 22.5 mg (1 ea) [contains polysorbate 80]
IM: Administer by IM injection into the buttock at a 90° angle (Trelstar) or into the buttock or thigh (Triptodur); alternate injection sites. Ensure full amount is injected within 10 seconds without interruption (Trelstar). Prior to administration, perform at least 5 inversions with the syringe to resuspend the particles; do not prime the needle (Trelstar). Administer immediately (<2 minutes) after reconstitution. Must be administered by a health care provider.
SUBQ: Decapeptyl [Canadian product] is administered by SUBQ 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. Must administer under the supervision of a health care provider.
IM: Triptodur: Should only be administered by a health care professional; administer immediately after preparation; verify suspension appears milky and homogenous without aggregates before priming needle. Administer Triptodur by IM injection with a thin-walled 21-gauge needle into the buttock or thigh in a steady uninterrupted manner to prevent needle blockages; alternate injection sites.
Hazardous agent (NIOSH 2016 [group 1]).
Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2016; USP-NF 2020).
An FDA-approved patient medication guide, which is available with the product information and as follows, must be dispensed with this medication:
Triptodur: https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/208956s010lbl.pdf#page=12
Central precocious puberty: Triptodur: Treatment of central precocious puberty in patients 2 years and older.
Prostate cancer (advanced): Trelstar: Treatment of advanced prostate cancer.
Assisted reproductive technologies: Decapeptyl [Canadian product]: Adjunctive therapy in women undergoing controlled ovarian hyperstimulation for assisted reproductive technologies (ART).
Breast cancer, premenopausal ovarian suppression during adjuvant endocrine therapy; Breast cancer, premenopausal ovarian preservation during chemotherapy; Breast cancer in male patients, hormone receptor–positive; Endometrial stromal sarcoma; Endometriosis; Paraphilia, males
The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drugs that have a heightened risk of causing significant patient harm when used in error.
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Antidiabetic Agents: Hyperglycemia-Associated Agents may diminish the therapeutic effect of Antidiabetic Agents. Risk C: Monitor therapy
Choline C 11: Luteinizing Hormone-Releasing Hormone Analogs may diminish the therapeutic effect of Choline C 11. Risk C: Monitor therapy
Corifollitropin Alfa: Luteinizing Hormone-Releasing Hormone Analogs may enhance the therapeutic effect of Corifollitropin Alfa. Risk X: Avoid combination
Flotufolastat F18: Androgen Deprivation Therapy Agents may diminish the diagnostic effect of Flotufolastat F18. Management: Androgen deprivation therapy (ADT) may result in changes in the uptake of flotufolastat F18 in prostate cancer. The impact of ADT on the performance of flotufolastat F18 is unknown, but use of alternative agents should be considered. Risk D: Consider therapy modification
Gallium Ga 68 PSMA-11: Androgen Deprivation Therapy Agents may diminish the therapeutic effect of Gallium Ga 68 PSMA-11. Management: Androgen deprivation therapy (ADT) may result in changes in the uptake of gallium Ga 68 PSMA-11 (gozetotide) in prostate cancer. The impact of ADT on the performance of gallium Ga 68 PSMA-11 is unknown, but use of alternative agents should be considered. Risk D: Consider therapy modification
Hyperprolactinemic Agents: May diminish the therapeutic effect of Triptorelin. Risk X: Avoid combination
Indium 111 Capromab Pendetide: Luteinizing Hormone-Releasing Hormone Analogs may diminish the diagnostic effect of Indium 111 Capromab Pendetide. Risk X: Avoid combination
Piflufolastat F18: Androgen Deprivation Therapy Agents may diminish the diagnostic effect of Piflufolastat F18. Management: Androgen deprivation therapy (ADT) may result in changes in the uptake of piflufolastat F18 in prostate cancer. The impact of ADT on the performance of piflufolastat F18 is unknown, but use of alternative agents should be considered. Risk D: Consider therapy modification
QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor therapy
When used for assisted reproductive technologies (ART; not an approved use in the US), 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.
Based on the mechanism of action, may impair fertility in males of reproductive potential.
Based on the mechanism of action and data from animal reproduction studies, in utero exposure to triptorelin may cause fetal harm.
Hormonal changes that occur with therapy may increase the risk of pregnancy loss. Therefore, use is contraindicated during pregnancy. Outcome data following inadvertent exposure in early pregnancy are limited (Elefant 1995; Wu 2021).
It is not known if triptorelin is present in breast milk.
Due to the potential for adverse reactions in the breastfed infant, the manufacturer recommends that a decision be made to discontinue breastfeeding or to discontinue the drug, taking into account the importance of treatment to the mother.
Monitor blood glucose and/or HbA1c (periodically and as clinically necessary) and serum lipids. Consider periodic monitoring of electrocardiograms and electrolytes in patients at risk for QT prolongation. Monitor for signs/symptoms of emerging cardiovascular disease, hypersensitivity, or pseudotumor cerebri. Monitor for development/worsening of psychiatric symptoms.
Additional monitoring (per indication):
Treatment of precocious puberty: Monitor response to therapy with LH levels after a GnRH or GnRH agonist stimulation test, basal LH, or serum sex steroid levels beginning 1 to 2 months after initiation of therapy, during therapy, and with each subsequent dose; height every 3 to 6 months; bone age (periodically).
Prostate cancer: Serum testosterone levels, prostate-specific antigen; bone density. Monitor for signs/symptoms of tumor flare.
Cardiovascular monitoring for patients with prostate cancer: Comprehensive assessment prior to treatment including a history and physical examination, screening for cardiovascular disease risk factors such as hypertension, diabetes, dyslipidemia, obesity, and smoking; baseline and serial ECGs are recommended in patients at risk of QTc prolongation during androgen deprivation therapy (ADT); estimate 10-year cardiovascular disease risk in patients without cardiovascular disease at baseline; assess cardiovascular risk annually during ADT (ASCO [Armenian 2017]; ESC [Lyon 2022]).
Assisted reproductive technologies: 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).
Paraphilia, males (off-label use): 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); bone density (baseline and yearly) (Reilly 2000).
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 assisted reproductive technologies (ART), prevents premature LH surge in women undergoing controlled ovarian hyperstimulation.
Distribution: Vd: 30 to 33 L
Protein binding: None
Metabolism: Unknown; unlikely to involve CYP; no known metabolites
Half-life elimination: 2.8 ± 1.2 hours
Moderate to severe renal impairment: 6.6 to 7.7 hours
Hepatic impairment: 7.6 hours
Time to peak: Trelstar: 1 to 3 hours; Triptodur: 4 hours
Excretion: Urine (42% as intact peptide); hepatic
Altered kidney function: 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.
Older adult: Triptorelin clearance is partly correlated to total CrCl, which is well known to decrease with age.
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