Triptorelin

Indications
 Parenteral
Prostate cancer
Adult: 3 or 3.75 mg by IM Inj every 4 wk using 1 mth depot preparation. The 1st dose may be preceded with 0.1 mg daily for 7 days by SC inj. Alternatively, 11.25 mg IM every 12 wk using the 3 mth depot formulation.
Intramuscular
Endometriosis
Adult: 3 or 3.75 mg by IM Inj every 4 wk for up to 6 mth. Begin treatment during the 1st 5 days of the menstrual cycle.
Intramuscular
Uterine fibroids
Adult: 3 or 3.75 mg by IM Inj every 4 wk for up to 6 mth. Begin treatment during the 1st 5 days of the menstrual cycle.
Subcutaneous
Female infertility
Adult: In conjunction with gonadotrophins, 0.1 mg daily by SC Inj starting from the 2nd day of the menstrual cycle for 10-12 days.
Parenteral
Precocious puberty
Child: 50 mcg/kg, using the 3 mg depot preparation by IM Inj every 4 wk. Alternatively, using the 3.75 mg depot preparation, <20 kg 1.875 mg, 20-30 kg 2.5 mg, >30 kg 3.75 mg by IM or SC inj; first 3 doses to be given at 14 day intervals with further doses given every 4 wk.
Contraindications
 Hypersensitivity to triptorelin and other luteinising hormone-releasing hormone (LHRH) or LHRH agonists; as sole treatment in prostate cancer patients with spinal cord compression or evidence of spinal metastases; progressive brain tumours in children. Pregnancy; lactation.
Warnings / Precautions
 Patients with pituitary adenoma; weight-related amenorrhoea until weight corrected; polycystic ovary disease or endometriotic cysts; metabolic bone disease. Monitor closely as there may be initial worsening of signs and symptoms during first few wk of therapy. Contraceptive measures to be taken to protect against unwanted ovulation in females.
Adverse Reactions
 Hot flushes, weight gain, sleep disturbances, headache, hypertension, weight gain, decreased libido, abnormal vision, mood disorders, nausea, abdominal pain or discomfort, rash and impotence. Transient pain, redness or local inflammation at the inj site may occur. Prostate cancer: During first few wk, bone pain, worsening of urinary obstruction symptoms and/or worsening of neurological signs of vertebral metastases (back pain, weakness or paresthesia of the lower limbs). Gynaecomastia, vertigo and dizziness. Endometriosis: Initial worsening of pelvic pain, dysmenorrhoea with heavy menstrual bleeding or spotting. Sweating, vaginal dryness, dyspareunia, breast pain, hair loss, small loss in bone density. Precocious puberty: Mild or moderate withdrawal bleeding in the first mth of treatment.
Potentially Fatal: Anaphylactic shock.
Drug Interactions
 Decrease in LHRH receptors in pituitary with hyperprolactinaemic drugs antagonises effects of triptorelin.
See Below for More triptorelin Drug Interactions
Lab Interactions
 Suppression of pituitary-gonadal axis may lead to misleading results of pituitary-gonadal function tests if conducted during treatment and after cessation of therapy.
Mechanism of Actions
 Triptorelin is a synthetic analogue of natural gonadotropin-releasing hormone. Initial admin stimulates the release of pituitary gonadotrophins with a transient increase in testosterone levels in men and in oestradiol levels in women, leading to an initial worsening of symptoms during the first wk. Prolonged admin leads to a suppression of gonadotrophins and a decrease in plasma testosterone or oestradiol after approximately 20 days, which is maintained for as long as triptorelin is admin.
Absorption: Rapidly absorbed with peak plasma concentrations after 40 minutes (subcutaneous inj).
Excretion: Half life: 7.5 hr.
ATC Classification
 L02AE04 - triptorelin ; Belongs to the class of gonadotropin releasing hormone analogues. Used in endocrine therapy.
Available As
  • Triptorelin 0.1 mg
  • Triptorelin 0.5 mg
  • Triptorelin 3.75 mg

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