Triptorelin Acetate
Indications
Triptorelin Acetate is used for:
Uterine fibroids, Female infertility, Endometriosis, Prostate cancer
Adult Dose
Parenteral
Prostate cancer
Adult: 22.5 mg IM q6Months, OR
11.25 mg IM q3Months, OR
3.75 mg IM qMonth
Intramuscular
Endometriosis; 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.
Child Dose
<18 years: Safety and efficacy not established
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.
Renal Dose
Administration
Contra Indications
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.
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.
Pregnancy-Lactation
Interactions
Decrease in LHRH receptors in pituitary with hyperprolactinaemic drugs antagonises effects of triptorelin.
Adverse Effects
Side effects of Triptorelin Acetate :
>10%
Hot flushes (82%),Skeletal pain (17%)
1-10%
Impotence (10%),Headache (7%),Hypertension (5%),Injection site pain (5%),Generalized pain (3%),Vomiting (3%),Fatigue (3%),Insomnia (3%),UTI (3%),Diarrhea (2%),Pruitus (2%),UTI (2%),Spinal cord compression (rare)
Potentially Fatal: Anaphylactic shock.
Mechanism of Action
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.