Drug reference

Triptorelin

GnRH Analogue · Hormonal Antineoplastic / Endocrine Modifier

Also known as Triptorelin acetate, Triptorelin embonate, DECAPEPTYL SR

GnRH AnalogueHormonal Antineoplastic / Endocrine ModifierATC null

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Avoid.

FDA category + note

Top interactionssee all 12 →

AmiodaroneSevereDatabaseDDInter
AmisulprideSevereDatabaseDDInter
AnagrelideSevereDatabaseDDInter
Arsenic TrioxideSevereDatabaseDDInter

Mechanism

Administration of gonadorelin analogues produces an initial phase of stimulation; continued administration is followed by down-regulation of gonadotrophin-releasing hormone receptors, thereby reducing the release of gonadotrophins (follicle stimulating hormone and luteinising hormone) which in turn leads to inhibition of androgen and oestrogen production.

Indications

Advanced prostate cancerEndometriosisAdjuvant treatment of endocrine responsive early stage breast cancer (in combination with tamoxifen or an aromatase inhibitor, in premenopausal women at high risk of recurrence after chemotherapy)Adjuvant treatment to radiotherapy and neoadjuvant treatment prior to radiotherapy in high-risk localised or locally advanced prostate cancerReduction of uterine volume and fibroid size (pre-operative, in conjunction with iron supplementation for associated anaemia)Androgen deprivation therapy (ADT) for all forms of advanced prostate cancerProstate cancer in conjunction with radiation therapy or in some cases following surgical removal of the prostate gland (for localized intermediate- to high-risk)Adjuvant treatment of breast cancer or metastatic disease for premenopausal women (in combination with tamoxifen or AIs)Suppression of ovarian estrogen and progesterone production in pre- and perimenopausal womenFemale infertility (short term)Carcinoma prostate (long term)Endometriosis (long term)Precocious puberty (long term)Uterine leiomyoma (long term)Assisted reproduction

Dosing

Adult: For advanced prostate cancer: 11.25 mg intramuscular injection every 3 months; or 22.5 mg intramuscular injection every 6 months; or 3 mg intramuscular injection every 4 weeks.…
Pediatric: For precocious puberty: 50 µg/kg i.m. of depot inj. every 4 weeks

Pharmacokinetics

Onset

Initial rise in LH and FSH levels, followed by sustained decrease in serum LH and estrogen (women) or testosterone (men) after 14 to 21 days. Castrate testosterone levels achieved within 3 to 4 weeks in men.

Contraindications

Pregnancy
Breastfeeding
Pregnant women

Side effects

Common

Increased testosterone production (initial stage, in prostate cancer, leading to tumour flare)Paraesthesia (with subcutaneous use, frequency not known)Bone disorder (with subcutaneous use, frequency not known)Breast pain (with subcutaneous use, frequency not known)Memory loss (with subcutaneous use, frequency not known)Hot flashesDecreased bone densityVaginal dryness (women)Vaginal atrophy (women)Erectile dysfunction (men)Vasomotor symptoms (hot flashes)Vaginal drynessDecreased libidoOsteoporosisAmenorrheaDyspareuniaVasomotor instabilityImpotenceGynecomastiaFatigueAnemiaWeight gainDecreased insulin sensitivityAltered lipid profilesFracturesLoss of muscle massLoss of libidoEmotional lability

Serious

Spinal cord compression (due to tumour flare in prostate cancer)
Ureteric obstruction (due to tumour flare in prostate cancer)
Increased pain (due to tumour flare in prostate cancer)
Testosterone flare (transient rise in testosterone leading to acute stimulation of prostate cancer growth and symptoms, typically lasting 2 to 3 weeks)
Increased risk of diabetes
Increased risk of coronary heart disease