triptorelin

trip-to-REL-in

Therapeutic Classification: antineoplastics

Pharmacologic Classification: hormones

High Alert

TrelstarPalliative treatment of advanced prostate cancer when orchiectomy or estrogen administration are contraindicated or unacceptable.
TriptodurCentral precocious puberty.

A synthetic analogue of luteinizing hormone-releasing hormone. 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.

Absorption: Well absorbed following IM administration.

Distribution: Unknown.

Metabolism/Excretion: Excreted by liver and kidneys.

Half-Life: 3 hr.

(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.

Contraindicated in:

Hypersensitivity to triptorelin or similar agents;
OB: Pregnancy;
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 central precocious puberty) (safety and effectiveness not established).

CV: hypertension, MI, QT interval prolongation

Derm: flushing, pruritus

Endo: hyperglycemia

GI: cirrhosis, diarrhea, nonalcoholic fatty liver disease, vomiting

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

Hemat: anemia

Local: injection site reactions

Metab: hyperlipidemia

MS: musculoskeletal pain

Neuro: headache, anxiety, dizziness, emotional lability, fatigue, insomnia, intracranial hypertension (children), SEIZURES, STROKE

Resp: cough

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)

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.

Prostate Cancer

IM (Adults ): 3.75 mg monthly or 11.25 mg every 3 mo or 22.5 mg every 6 mo.

Central Precocious Puberty

IM (Children ≥2 yr): Extended-release injection: 22.5 mg every 24 wk. Discontinue at the appropriate age of puberty onset.

Suspension for injection (Trelstar): 3.75 mg/vial; 11.25 mg/vial; 22.5 mg/vial
Extended-release suspension for injection (Triptodur): 22.5 mg/vial

Monitor patient for signs and symptoms of hypersensitivity reactions (dyspnea, rash, laryngeal edema) following each dose. Have diphenhydramine, epinephrine, and resuscitation equipment readily available.
Obtain ECG at start of therapy; prolonged QT/QTc interval may occur. Closely monitor patients with congenital long QT syndrome, HF, frequent electrolyte abnormalities, and those concomitantly taking drugs known to prolong the QT interval.
Monitor patients for signs and symptoms of emerging cardiovascular disease such as MI (chest pain, dyspnea, diaphoresis, dizziness, nausea) and stroke (weakness, slurred speech, confusion, dizziness); sudden cardiac death can occur, especially in men.
Monitor for seizures and institute seizure precautions; ↑ risk with history of seizures, epilepsy, intracranial tumors, or concomitant use of other drugs known to present a risk of seizure reactions.
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.
Central Precocious Puberty: Monitor height (for calculation of growth rate) every 3–6 mo and monitor bone age periodically. Gonadotropin and sex steroid levels may ↑ above baseline and cause a transient ↑ in clinical signs and symptoms of puberty, including vaginal bleeding, during the first wks of therapy.
Pedi: Monitor children for signs and symptoms of pseudotumor cerebri (headache, papilledema, blurred vision, diplopia, loss of vision, pain behind the eye or pain with eye movement, tinnitus, dizziness, nausea).

Lab Test Considerations:

Verify negative pregnancy test before starting therapy.
- Monitor blood glucose, A1c, and lipids periodically during therapy; may cause hyperglycemia and hyperlipidemia.
- Prostate Cancer: Monitor response by measuring serum testosterone and prostate-specific antigen levels periodically during therapy. Serum testosterone levels may transiently ↑ during first few wks of therapy.
- Central Precocious PubertyMonitor response with LH levels after a GnRH or GnRH agonist stimulation test, basal LH, or serum concentration of sex steroid levels starting 1–2 mo after starting therapy, during therapy as necessary to confirm maintenance of efficacy, and with each subsequent dose.

Triptorelin must be administered under the supervision of a health care provider.
Use double gloves and a protective gown to prepare and administer. If possible, prepare in a biological safety cabinet or a compounding aseptic containment isolator; eye, face, and respiratory protection may be needed. Prepare and administer in a closed-system drug-transfer device. During administration, if there is a potential that the substance could splash or if the patient may resist, use eye and face protection.
IM: Prostate cancer: Use diluent in syringe provided. Follow manufacturer's instructions for use of vial adapter. Shake reconstituted suspension well to obtain a uniform suspension and thoroughly disperse particles. Suspension will appear milky; do not administer solutions that are discolored or contain particulate matter. Withdraw entire contents of reconstituted suspension and inject immediately. Discard suspension if not used immediately after reconstitution. Inject immediately (within 2 min) after reconstitution in the ventrogluteal site.
- Central Precocious Puberty: 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 (within 2 min). 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.

Explain the purpose and side effects of triptorelin to patient and family. Do not stop receiving drug without consulting health care professional. If an appointment is missed, contact health care professional as soon as possible to reschedule. Advise patient and family to read Medication Guide before starting and periodically during therapy and with each Rx refill in case of changes.
Emphasize the importance of routine examinations to monitor for side effects and assess response.
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 rash, redness, or swelling; severe itching; hives; trouble breathing or swallowing; fast heartbeat; sweating; throat tightness; hoarseness; swelling of face, mouth, and tongue; dizziness; fainting) occur.
Inform patient of ↑ risk of developing seizures, diabetes, heart attack, sudden cardiac death, and stroke.
Advise patient being treated for prostate cancer that triptorelin may cause impotence.
Advise patient and family of patient being treated for central precocious puberty that a transient ↑ in the clinical signs and symptoms of puberty, including vaginal bleeding, may occur during the first wks of therapy.
Rep: May cause fetal harm. Advise women of reproductive potential to use effective contraception and to avoid breastfeeding during therapy. May impair male fertility.

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

Trelstar, Triptodur

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Route/Dosage ⬆ ⬇

Availability ⬆ ⬇

Assessment ⬆ ⬇

Implementation ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Evaluation/Desired Outcomes ⬆ ⬇

US Brand Names ⬆