Trelstar
(triptorelin)Dosage & Administration
TRELSTAR is administered as a single intramuscular injection in either buttock. Due to different release characteristics, the dosage strengths are not additive and must be selected based upon the desired dosing schedule. ( 2.1)
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Trelstar Prescribing Information
TRELSTAR is indicated for the treatment of advanced prostate cancer [see Clinical Studies (14)].
2.1 Dosing Information
TRELSTAR must be administered under the supervision of a physician.
TRELSTAR is administered by a single intramuscular injection in either buttock. Dosing schedule depends on the product strength selected (Table 1). The lyophilized microgranules are to be reconstituted in sterile water. No other diluent should be used.
| Dosage | 3.75 mg | 11.25 mg | 22.5 mg |
| Recommended dose | 1 injection every 4 weeks | 1 injection every 12 weeks | 1 injection every 24 weeks |
Due to different release characteristics, the dosage strengths are not additive and must be selected based upon the desired dosing schedule.
The suspension should be administered within 2 minutes after reconstitution.
As with other drugs administered by intramuscular injection, the injection site should be alternated periodically.
Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
Reconstitution Instructions for TRELSTAR
Important: Please read the instructions completely and prepare the patient before you begin the injection kit activation and drug administration procedure.
*The strength indicated on the vial in the figure above is for representative purposes only. All three strengths of the Trelstar vial have their individual strengths indicated on the label. Users will see either 3.75 mg, 11.25 mg or 22.5 mg, with the corresponding duration of treatment (4, 12 or 24 weeks respectively).
Preparation and Activation
Check that you are using the prescribed strength/dose (3.75 mg, 11.25 mg, or 22.5 mg) and that the expiry date has not passed, before preparation and activation.
Wash your hands with soap and hot water and put on gloves immediately prior to preparing the injection. Place the sealed tray on a clean, flat surface that is covered with a sterile pad or cloth. Peel the cover away from the tray and remove the injection kit components and TRELSTAR vial.
General Instructions and Recommendations
The product is a suspension of microgranules that can settle in the diluent. The final product to be administered is a suspension of microgranules with a milky, homogeneous appearance. If the product settles in the vial, shake it again to resuspend the microgranules.
If the microgranules settle in the syringe, this will block the needle during administration. It is very important to inject the product within 2 minutes following reconstitution in the vial. If the product settles in the syringe, draw some air back into the syringe, shake it again, and expel the air (without priming the needle) before administering it.
 | STEP 1 – PREPARE VIAL Remove the flip-off button cap from the vial, revealing the rubber stopper. |
 | STEP 2 – APPLY VIAL ADAPTER Peel the cover away from the blister pack containing the vial adapter. Do not remove the vial adapter from the blister pack. |
 | STEP 3 – PREPARE SYRINGE AND CONNECT TO VIAL ADAPTER (a) Grasp the plastic ‘spin lock’ collar on the syringe barrel with index finger and thumb. Unscrew and discard the gray rubber cap from the syringe barrel. (b) Maintaining your grip on the spin lock, attach the syringe to the vial adapter by screwing the spin lock clockwise onto the vial adapter luer lock. Gently twist the spin lock until it stops turning to ensure a tight connection. |
 | STEP 4 – TRANSFER DILUENT TO VIAL Holding the vial and adapter with one hand, slowly push the plunger rod with the other hand and transfer all of the diluent into the vial. |
  | STEP 5 – MIX TRELSTAR SUSPENSION Gripping the vial and vial adapter firmly, shake vigorously for 30 seconds to mix the contents thoroughly. This will ensure complete mixing of TRELSTAR and the sterile water diluent. Check the appearance of the suspension through the bottom of the vial. The suspension should appear homogeneous and milky. In order to avoid separation of the suspension, proceed to the next steps without delay. The product must be injected within less than 2 minutes from reconstitution.
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   | STEP 6 – LOAD THE SYRINGE WITH TRELSTAR (a) Immediately invert the system so that the vial is at the top and the syringe is at the bottom. Pull back the plunger rod slowly to draw the reconstituted TRELSTAR into the syringe while maintaining pressure on the plunger rod to ensure it does not pull back too far. (b) Remove air bubbles by expelling air into the vial but do not propel the suspension beyond the luer lock. Note: If the product settles in the syringe, draw some air back into the syringe, shake it again, and expel the air (without priming the needle) before administering it. |
 | STEP 7 – DISCONNECT VIAL ADAPTER AND CONNECT NEEDLE (a) Hold the barrel and spin lock firmly. |
 | STEP 8 – PREPARE FOR INJECTION Make sure that the patient is ready for the administration. |
 | STEP 9 – ADMINISTRATION Administer the injection by inserting the needle at a 90-degree angle into the large gluteal muscle. Ensure that the full amount of the product is injected within 10 seconds without interruption. Injection sites should be alternated. |
 | STEP 10 – SAFETY LOCK AFTER INJECTION After administering the injection, immediately activate the safety mechanism by centering your thumb or forefinger on the textured finger pad area of the safety cover and pushing it forward over the needle until you hear or feel it lock in place. Use the one-handed technique and activate the mechanism away from yourself and others. Immediately discard the syringe into a sharps container after a single use. |
For injectable suspension: 3.75 mg, 11.25 mg, 22.5 mg of slightly yellow lyophilized microgranules in a single-dose vial for reconstitution with an injection kit containing one syringe filled with sterile water for injection, a vial adapter to help with reconstitution, and one needle (see figure in section 2.2).
8.1 Pregnancy
Risk Summary
Based on findings in animal studies and mechanism of action, TRELSTAR can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology (12.1)]. Expected hormonal changes that occur with TRELSTAR treatment increase the risk for pregnancy loss. In animal developmental and reproductive toxicology studies, daily administration of triptorelin to pregnant rats during the period of organogenesis caused maternal toxicity and embryo-fetal toxicities, including loss of pregnancy, at doses as low as 0.2, 0.8, and 8 times the estimated human daily dose based on body surface area. Advise pregnant patients and females of reproductive potential of the potential risk to the fetus.
Data
Animal Data
Studies in pregnant rats administered triptorelin at doses of 2, 10, and 100 mcg/kg/day (approximately equivalent to 0.2, 0.8, and 8 times the estimated human daily dose based on body surface area) during the period of organogenesis demonstrated maternal toxicity and embryo-fetal toxicities. Embryo-fetal toxicities consisted of pre-implantation loss, increased resorption, and reduced mean number of viable fetuses at the high dose. Teratogenic effects were not observed in viable fetuses in rats or mice. Doses administered to mice were 2, 20, and 200 mcg/kg/day (approximately equivalent to 0.1, 0.7, and 7 times the estimated human daily dose based on body surface area).
8.2 Lactation
The safety and efficacy of TRELSTAR have not been established in females. There are no data on the presence of triptorelin in human milk, the effects of the drug on milk production, or the effects of the drug on the breastfed child. Because of the potential for serious adverse reactions in a breastfed child from TRELSTAR, a decision should be made to either discontinue breastfeeding, or discontinue the drug taking into account the importance of the drug to the mother.
8.3 Females and Males of Reproductive Potential
Infertility
Males
Based on mechanism of action, TRELSTAR may impair fertility in males of reproductive potential [see Clinical Pharmacology ].
8.4 Pediatric Use
The safety and effectiveness of TRELSTAR in pediatric patients have not been established.
8.5 Geriatric Use
Prostate cancer occurs primarily in an older population. Clinical studies with TRELSTAR have been conducted primarily in patients ≥ 65 years [see Clinical Pharmacology (12.3) and Clinical Studies (14)].
8.6 Renal Impairment
Subjects with renal impairment had higher exposure than young healthy males [see Clinical Pharmacology (12.3)].
8.7 Hepatic Impairment
Subjects with hepatic impairment had higher exposure than young healthy males [see Clinical Pharmacology (12.3)].
4.1 Hypersensitivity
TRELSTAR is contraindicated in individuals with a known hypersensitivity to triptorelin or any other component of the product, or other GnRH agonists or GnRH [see Warnings and Precautions (5.1)].
5.1 Hypersensitivity Reactions
Anaphylactic shock, hypersensitivity, and angioedema related to TRELSTAR administration have been reported. In the event of a hypersensitivity reaction, discontinue TRELSTAR immediately and administer the appropriate supportive and symptomatic care.
5.2 Tumor Flare
Initially, triptorelin (TRELSTAR), like other GnRH agonists, causes a transient increase in serum testosterone levels [see Clinical Pharmacology (12.2) ]. As a result, worsening signs and symptoms of prostate cancer during the first weeks of treatment have been reported with GnRH agonists. Patients may experience worsening of symptoms or onset of new symptoms, including bone pain, neuropathy, hematuria, or urethral or bladder outlet obstruction.
Closely monitor patients with metastatic vertebral lesions and/or with urinary tract obstruction during the first few weeks of therapy.
5.3 Metabolic Syndrome
The use of GnRH agonists (including TRELSTAR) may lead to metabolic changes such as hyperglycemia, diabetes mellitus, and hyperlipidemia. Non-alcoholic fatty liver disease, including cirrhosis, occurred in the post-marketing setting. Hyperglycemia may represent new-onset of diabetes mellitus or worsening of glycemic control in patients with pre-existing diabetes. Monitor for changes in serum lipids, blood glucose and/or glycosylated hemoglobin (HbA1c) periodically in patients receiving TRELSTAR and manage according to institutional guidelines.
5.4 Cardiovascular Diseases
Increased risk of developing myocardial infarction, sudden cardiac death and stroke has been reported in association with the use of GnRH agonists (including TRELSTAR) in men. The risk appears low based on the reported odds ratios and should be evaluated carefully along with cardiovascular risk factors when determining a treatment for patients with prostate cancer. Monitor patients receiving TRELSTAR for symptoms and signs suggestive of development of cardiovascular disease and manage according to current institutional guidelines.
Convulsions
Convulsions have occurred in patients treated with GnRH analog (including TRELSTAR). These events included patients with risk factors for seizures such as a history of epilepsy, intracranial tumors or co-medication with other drugs known to present a risk of seizure reactions. Convulsions have also been reported in patients in the absence of known risk factors. Manage patients receiving TRELSTAR who experience convulsion according to institutional guidelines.
Effect on QT/QTc Interval
Androgen deprivation therapy with TRELSTAR may prolong the QT/QTc interval. Providers should consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients with congenital long QT syndrome, congestive heart failure, frequent electrolyte abnormalities, and in patients taking drugs known to prolong the QT interval. Electrolyte abnormalities should be corrected. Consider periodic monitoring of electrocardiograms and electrolytes.
Laboratory Tests
Monitor serum levels of testosterone following injection of TRELSTAR. In the majority of patients, testosterone levels increased above baseline, and then declined thereafter to castrate levels (< 50 ng/dL) within four weeks [see Clinical Studies and Adverse Reactions ].
Laboratory Test Interactions
Chronic or continuous administration of TRELSTAR in therapeutic doses results in suppression of pituitary-gonadal axis. Diagnostic tests of the pituitary-gonadal function conducted during treatment and after cessation of therapy may therefore be misleading.
Embryo-Fetal Toxicity
Based on findings from animal studies and mechanism of action, TRELSTAR can cause fetal harm when administered to a pregnant woman [ Clinical Pharmacology (12.1)]. In animal developmental and reproductive toxicology studies, daily administration of triptorelin to pregnant rats during the period of organogenesis caused maternal toxicity and embryo-fetal toxicities, including loss of pregnancy, at doses as low as 0.2, 0.8, and 8 times the estimated human daily dose based on body surface area. Advise pregnant patients and females of reproductive potential of the potential risk to the fetus [see Use in Specific Populations (8.1)].