triptorelin

REMS

Trelstar

Palliative treatment of advanced prostate cancer when orchiectomy or estrogen administration are contraindicated or unacceptable.

Triptodur

Central precocious puberty (CPP).

Action ⬆ ⬇

A synthetic analogue of luteinizing hormone-releasing hormone (LHRH) Initially causes a transient increase in testosterone; however, with continuous administration, testosterone levels are decreased Reduces gonadotropins, testosterone, and estradiol.

Therapeutic effects:

Decreased testosterone levels and resultant decrease in spread of prostate cancer.
Decreased or reversal of progression of clinical signs of puberty

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed following IM administration.

Distribution: Unknown.

Metabolism/Excretion: Excreted by liver and kidneys.

Half-Life: 3 hr.

Time/Action Profile ⬆ ⬇

(effects on hormone levels)

ROUTE	ONSET	PEAK	DURATION
IM	unknown	1 hr‡	4 wk
IM-ER	unknown	4 hr‡	4 wk

‡Blood level of triptorelin.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity to triptorelin or similar agents;
OB: Pregnancy (may cause fetal harm);
Lactation: Lactation.

Use Cautiously in:

History of seizures, CNS tumors, or use of medications that lower seizure threshold;
Metastatic vertebral lesions and/or upper or lower urinary tract obstruction (symptoms may transiently worsen following initiation of therapy);
Renal or hepatic impairment (may need dosage adjustment);
Congenital long QT syndrome, HF, electrolyte abnormalities, or concurrent use of other drugs known to prolong the QT interval (for depot);
Pedi: Children 2 yr (for CPP) (safety and effectiveness not established).

Adv. Reactions/Side Effects ⬆ ⬇

CV: MYOCARDIAL INFARCTION, hypertension, QT interval prolongation

Derm: flushing, pruritus

GI: diarrhea, vomiting

GU: erectile dysfunction, ↓fertility (males), testicular atrophy, urinary retention, urinary tract infection, vaginal bleeding

Hemat: anemia

Neuro: SEIZURES, STROKE, headache, anxiety, dizziness, emotional lability, fatigue, insomnia

Resp: cough

Local: injection site pain

Metab: hyperglycemia

MS: musculoskeletal pain

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA), injection site reactions

Interactions ⬆ ⬇

Drug-drug:

Concurrent use of hyperprolactinemic drugs should be avoided (may ↓ number of drug receptor sites).
Concurrent use with bupropion or SSRIs may ↑ risk of seizures.

Route/Dosage ⬆ ⬇

Prostate Cancer

Central Precocious Puberty

IM (Adults ): 3.75 mg monthly or 11.25 mg every 3 mo or 22.5 mg every 6 mo.
IM (Children ≥2 yr): Extended-release injection—22.5 mg every 24 wk. Discontinue at the appropriate age of puberty onset.

Availability ⬆ ⬇

Suspension for injection: 3.75 mg/vial; 11.25 mg/vial; 22.5 mg/vial
Extended—release suspension for injection: 22.5 mg/vial

Assessment ⬆ ⬇

Monitor patient for signs and symptoms of hypersensitivity reactions (dyspnea, rash, laryngeal edema) following each dose. Have diphenhydramine, epinephrine, and resuscitation equipment readily available.
Prostate Cancer: Assess patient for symptoms of prostate cancer prior to and throughout therapy. Symptoms may worsen or onset of new symptoms (bone pain, neuropathy, hematuria, urethral or bladder outlet obstruction) may occur during first few wk of treatment.
CPP: Monitor height (for calculation of growth rate) every 3-6 mos and monitor bone age periodically.

Lab Test Considerations:

Monitor blood glucose and/or glycosylated hemoglobin (A1c) periodically during therapy; may cause hyperglycemia.
- Prostate Cancer: Monitor response by measuring serum testosterone and prostate-specific antigen levels periodically during therapy.
- CPP
  Monitor response with LH levels after a GnRH or GnRH agonist stimulation test, basal LH, or serum concentration of sex steroid levels starting 1 to 2 mos after starting therapy, during therapy as necessary to confirm maintenance of efficacy, and with each subsequent dose.

Implementation ⬆ ⬇

Triptorelin must be administered under the supervision of a physician.
IM: Prostate cancer: Reconstitute by withdrawing 2 mL of sterile water for injection into a syringe with a 20-gauge needle and inject into vial. Shake well to obtain a uniform suspension and thoroughly disperse particles. Suspension will appear milky; do not administer solutions that are discolored of contain particulate matter. Withdraw entire contents of reconstituted suspension and inject immediately. Discard suspension if not used immediately after reconstitution. Follow manufacture's instructions for use of Mixject system. Inject immediately after reconstitution in the ventrogluteal site.
- CPP: Use diluent in syringe provided. Follow manufacturer's instructions for preparation. Solution is milky and homogenous; do not administer if solution is discolored or contains aggregates or precipitates. Remove air from syringe and administer immediately. Inject in ventrogluteal site or thigh relatively rapidly and in a steady and uninterrupted manner to avoid potential blockage of the needle.
- Rotate injection sites periodically.

Patient/Family Teaching ⬆ ⬇

Explain the purpose of triptorelin to patient and family. Advise patients with CPP to read Medication Guide before starting therapy and with each Rx refill in case of changes.
May cause dizziness. Caution patient not to drive or other activities requiring alertness until response to medication is known.
Advise patient to notify health care professional immediately if signs and symptoms of hypersensitivity reactions (skin rashes, redness, or swelling; severe itching; hives; trouble breathing or swallowing; fast heart beat; sweating; throat tightness, hoarseness; swelling of face, mouth, and tongue; dizziness; fainting) occur.
Inform patient of increased risk of developing diabetes, myocardial infarction, sudden cardiac death and stroke.
Advise patient being treated for prostate cancer that triptorelin may cause impotence.
Rep: May be teratogenic. Advise females of reproductive potential to use effective contraception and to avoid breastfeeding during therapy. May impair male fertility.
Emphasize the importance of routine examinations to monitor for side effects and assess response.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇