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

Pregnancy Based on findings in animal studies and mechanism of action, therapy can cause fetal harm when administered to a pregnant woman; expected hormonal changes that occur with treatment increase risk for pregnancy loss; in animal developmental and reproductive toxicology studies, daily administration of drug to pregnant rats during period of organogenesis caused maternal toxicity and embryo-fetal toxicities, including loss of pregnancy, at doses as low as 0.2, 0.8, and 8 times estimated human daily dose based on body surface area; advise pregnant patients and females of reproductive potential of potential risk to fetus Based on mechanism of action, treatment may impair fertility in males of reproductive potential Lactation The safety and efficacy not established in females; there are no data on presence of drug in human milk, effects of drug on milk production, or on breastfed child; because of potential for serious adverse reactions in a breastfed child from treatment, a decision should be made to either discontinue breastfeeding, or discontinue drug taking into account importance of drug to mother

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.