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 injection).

Excretion
Half life: 7.5 hours.

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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 injection site may occur. Prostate cancer: During first few weeks, 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.

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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.

Decrease in LHRH receptors in pituitary with hyperprolactinaemic drugs antagonises effects of triptorelin.

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Intramuscular
Uterine fibroids
Adult: 3 or 3.75 mg by IM injection every 4 weeks for up to 6 months. Begin treatment during the 1st 5 days of the menstrual cycle.

Intramuscular
Endometriosis
Adult: 3 or 3.75 mg by IM injection every 4 weeks for up to 6 month. 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 injection starting from the 2nd day of the menstrual cycle for 10-12 days.

Parenteral
Prostate cancer
Adult: 3 or 3.75 mg by IM injection every 4 weeks using 1 month depot preparation. The 1st dose may be preceded with 0.1 mg daily for 7 days by SC injection. Alternatively, 11.25 mg IM every 12 weeks using the 3 months depot formulation.

Parenteral
Precocious puberty
Child: 50 mcg/kg, using the 3 mg depot preparation by IM injection every 4 weeks. 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 injection; first 3 doses to be given at 14 day intervals with further doses given every 4 weeks.

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Contraindicated in pregnancy

Category X: Studies in animals or human beings have demonstrated foetal abnormalities or there is evidence of foetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.

Contraindicated in lactation

Safety and efficacy not established

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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.

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Suppression of pituitary-gonadal axis may lead to misleading results of pituitary-gonadal function tests if conducted during treatment and after cessation of therapy.