Trelstar

— THERAPEUTIC CATEGORIES —
  • Prostate and other male cancers

Trelstar Generic Name & Formulations

General Description

Triptorelin pamoate 3.75mg, 11.25mg, 22.5mg; lyophilized microgranules for IM inj after reconstitution; contains mannitol.

Pharmacological Class

GnRH analogue.

How Supplied

MixJect system—1 (vial + vial adapter + prefilled syringe)

Mechanism of Action

Triptorelin is a synthetic decapeptide agonist analog of gonadotropin releasing hormone (GnRH). In animal studies, triptorelin pamoate was found to have 13‑fold higher luteinizing hormone-releasing activity and 21-fold higher follicle-stimulating hormone-releasing activity compared to the native GnRH.

Trelstar Indications

Indications

Treatment of advanced prostate cancer.

Trelstar Dosage and Administration

Adult

Give by IM inj in buttock (within 2mins after reconstitution); rotate inj site. 3.75mg every 4 weeks, or 11.25mg every 12 weeks, or 22.5mg every 24 weeks.

Children

Not established.

Trelstar Contraindications

Not Applicable

Trelstar Boxed Warnings

Not Applicable

Trelstar Warnings/Precautions

Warnings/Precautions

Not for use in women. Must administer under physician supervision. Discontinue if hypersensitivity occurs. Initial transient increase in serum testosterone may result in worsening of signs/symptoms including bone pain, neuropathy, hematuria, or urethral/bladder obstruction. Metastatic vertebral lesions and/or with urinary tract obstruction; monitor closely during the first few weeks of therapy. Spinal cord compression. Renal or hepatic impairment. May prolong QT/QTc interval in patients with congenital long QT syndrome, CHF, frequent electrolyte abnormalities. Correct any electrolyte abnormalities; monitor ECGs and electrolytes periodically. Metabolic changes (eg, hyperglycemia, diabetes, hyperlipidemia). Cardiovascular disease (eg, MI, sudden cardiac death, stroke). Monitor serum lipids, blood glucose and/or HbA1c periodically, and for signs/symptoms of cardiovascular disease. History of epilepsy. Intracranial tumors. Measure serum testosterone periodically. Embryo-fetal toxicity. Pregnancy. Nursing mothers: not recommended.

Trelstar Pharmacokinetics

Absorption

Mean peak serum concentrations of 28.4 ng/mL, 38.5 ng/mL, and 44.1 ng/mL occurred in 1–3 hours after the 3.75 mg, 11.25 mg, and 22.5 mg formulations, respectively.

Distribution

Volume of distribution: 30–33 L.

Elimination

Renal, fecal. Half-life: 3 hours (terminal).

Trelstar Interactions

Interactions

Concomitant hyperprolactinemic drugs: not recommended. Avoid concomitant drugs that are known to prolong the QT interval. May interfere with pituitary gonadotropic function tests.

Trelstar Adverse Reactions

Adverse Reactions

Inj site reactions, hot flushes, skeletal pain, impotence, headache, leg edema/pain, erectile dysfunction, testicular atrophy; convulsions.

Trelstar Clinical Trials

See Literature

Trelstar Note

Not Applicable

Trelstar Patient Counseling

See Literature