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).

Adv. Reactions/Side Effects ⬆ ⬇

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)

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.

Availability ⬆ ⬇

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

Route/Dosage ⬆ ⬇

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.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

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.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: hormones

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.

Patient/Family Teaching ⬆ ⬇

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.

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Indications ⬇

Contraind./Precautions ⬆ ⬇