Triptorelin


Generic Medicine Info
Indications and Dosage
Intramuscular
Hormone sensitive locally advanced prostate cancer, Hormone sensitive metastatic prostate cancer
Adult: As triptorelin embonate 3.75 mg depot preparation: 3.75 mg once every 4 weeks. As triptorelin embonate 11.25 mg depot preparation: 11.25 mg once every 12 weeks. All doses are given via IM inj.

Intramuscular
Locally advanced prostate cancer
Adult: Alternative to surgical castration; adjuvant treatment to radiotherapy in patients with high-risk cases; neoadjuvant treatment before radiotherapy in patients with high-risk cases; adjuvant treatment to radical prostatectomy in patients with cases at high risk of disease progression: As triptorelin acetate 3 mg sustained-release depot preparation: 3 mg once every 4 weeks. As triptorelin pamoate 11.25 mg sustained-release depot preparation: 11.25 mg once every 12 weeks. As triptorelin pamoate 22.5 mg sustained-release depot preparation: 22.5 mg every 24 weeks. All doses are given via IM inj.

Intramuscular
Adjuvant treatment of hormone-responsive early stage breast cancer in premenopausal women
Adult: In combination with tamoxifen or an aromatase inhibitor in patients at high risk of recurrence: As triptorelin acetate 3 mg sustained-release depot preparation: 3 mg every 4 weeks given via deep IM inj. Initiate treatment at least 6-8 weeks (equivalent to at least 2 doses) before starting the aromatase inhibitor. Thereafter, do not interrupt triptorelin treatment to avoid rebound increases in estrogen levels. Recommended treatment duration: 5 years.

Intramuscular
Endometriosis
Adult: As triptorelin acetate 3 mg sustained-release depot preparation: 3 mg once every 4 weeks. As triptorelin pamoate 11.25 mg sustained-release depot preparation: 11.25 mg every 3 months. Initiate treatment during the 1st 5 days of the menstrual cycle. Max treatment duration: 6 months. All doses are given via IM inj.

Intramuscular
Central precocious puberty
Child: As triptorelin pamoate 11.25 mg sustained-release depot preparation: Onset in girls before 8 years; in boys before 10 years 11.25 mg every 3 months. As triptorelin embonate 22.5 mg depot preparation: ≥2 years with onset in girls before 8 years; in boys before 10 years 22.5 mg once every 24 weeks. Discontinue treatment around the physiological age of puberty in girls and boys, and in girls with bone maturation of >12 years. All doses are given via IM inj.

Intramuscular
Metastatic prostate cancer
Adult: As triptorelin acetate 3 mg sustained-release depot preparation: 3 mg once every 4 weeks. As triptorelin pamoate 11.25 mg sustained-release depot preparation: 11.25 mg once every 12 weeks. As triptorelin pamoate 22.5 mg sustained-release depot preparation: 22.5 mg every 24 weeks. All doses are given via IM inj. Continue treatment upon the development of castrate-resistant prostate cancer (refer to local treatment guidelines).

Intramuscular
Palliative treatment of advanced prostate cancer
Adult: As triptorelin pamoate 3.75 mg depot preparation: 3.75 mg every 4 weeks via IM inj into the buttock.

Intramuscular
Uterine fibroids
Adult: Treatment of cases prior to surgery or when surgery is inappropriate: As triptorelin acetate 3 mg sustained-release depot preparation: 3 mg once every 4 weeks given via deep IM inj for at least 3 months. Initiate treatment during the 1st 5 days of the menstrual cycle. Max treatment duration: 6 months.

Intramuscular
Libido in severe hypersexuality or sexual deviation
Adult: For the reduction of sex drive in men with severe sexual deviations: In combination with psychotherapy: As triptorelin embonate prolonged-release depot preparation: 11.25 mg every 12 weeks. Consider the addition of anti-androgen when initiating therapy to counteract transient rise in serum testosterone levels, and when stopping the treatment due to increased risk of sensitivity to restored testosterone.

Parenteral
Hormone sensitive locally advanced prostate cancer, Hormone sensitive metastatic prostate cancer
Adult: As triptorelin acetate 3.75 mg prolonged-release depot preparation: 3.75 mg once every 4 weeks given via deep IM or SC inj. Alternatively in some countries, the treatment regimen may initially use 0.1 mg once daily (triptorelin acetate 0.1 mg immediate-release preparation) given via SC inj for 7 days; followed by 3.75 mg on day 8 (triptorelin acetate 3.75 mg prolonged-release depot preparation) given via IM inj, repeated every 4 weeks. Dosage administration may vary among individual product formulation and between countries (refer to specific product guideline).

Parenteral
Endometriosis, Uterine fibroids
Adult: As triptorelin acetate 3.75 mg prolonged-release depot preparation: 3.75 mg once every 4 weeks given via deep IM or SC inj. Initiate treatment during the 1st 5 days of the menstrual cycle. Max treatment duration: 6 months (for endometriosis); 3 or 6 months (for uterine fibroids). Dosage administration may vary among individual product formulation and between countries (refer to specific product guideline).

Parenteral
Central precocious puberty
Child: As triptorelin acetate 3.75 mg prolonged-release depot preparation: Onset in girls before 9 years; in boys before 10 years <20 kg: 1.875 mg; 20-30 kg: 2.5 mg; >30 kg: 3.75 mg. Give the 1st 3 doses on days 0, 14, and 28 via IM or SC inj. Thereafter, further doses are administered once every 4 weeks, then may be increased to once every 3 weeks if necessary. Discontinue treatment if a bone maturation of >12 years in girls or >13 years in boys is achieved.
Reconstitution
Refer to individual product-specific recommendations for respective methods of reconstitution.
Contraindications
Undiagnosed vaginal bleeding; severe osteoporosis (for use in severe sexual deviation in men). Pregnancy and lactation.
Special Precautions
Patient with history of QTc prolongation, heart failure, congenital long QT syndrome, frequent electrolyte abnormalities; risk factors for osteoporosis or decreased bone mineral density (e.g. family history of osteoporosis, prolonged use of agents that reduce bone mineral density, malnutrition, smoking, chronic alcohol abuse); known or history of depression, history of seizures, epilepsy, CNS anomalies or tumours, cerebrovascular disorders, upper or lower urinary tract obstruction, metastatic vertebral lesions; at high risk for metabolic or CV diseases. Treatment guidelines may vary among individual products (refer to product-specific recommendations). Children (particularly those with progressive brain tumours).
Adverse Reactions
Significant: QT/QTc interval prolongation, reduced bone mineral density with prolonged use (e.g. osteoporosis, bone fractures), hyperglycaemia, diabetes, hypertension, seizures, psychiatric effects (e.g. depression, mood changes, crying, irritability, aggression, impatience, anger), urethral obstruction, tumour flare, transiently increased serum testosterone levels, increased lymphocyte count, hypersensitivity reactions (e.g. angioedema, anaphylactic shock). Rarely, ovarian hyperstimulation syndrome (OHSS), pituitary apoplexy (secondary to pituitary adenoma).
Gastrointestinal disorders: Nausea, abdominal pain or discomfort, dry mouth.
General disorders and administration site conditions: Asthenia, fatigue, irritability, oedema, inj site reactions (e.g. pain, erythema, inflammation).
Investigations: Increased weight.
Musculoskeletal and connective tissue disorders: Bone pain, back pain, pain in the extremity, myalgia, arthralgia, muscle spasms.
Nervous system disorders: Headache, paraesthesia, dizziness.
Psychiatric disorders: Sleep disorder, insomnia, nervousness.
Renal and urinary disorders: Dysuria, urinary incontinence.
Reproductive system and breast disorders: Erectile dysfunction, loss of libido, decreased libido, gynaecomastia, impotence, vaginal haemorrhage, vulvovaginal dryness, dysmenorrhoea, pelvic pain, dyspareunia, ovarian hypertrophy, breast pain or disorder, vaginal bleeding.
Skin and subcutaneous tissue disorders: Hyperhidrosis, acne, seborrhoea.
Vascular disorders: Hot flushes, embolism.
Potentially Fatal: MI, sudden cardiac death, stroke, spinal cord compression.
IM/Parenteral/SC: X
MonitoringParameters
Prior to treatment initiation: Confirm pregnancy status, premenopausal status following chemotherapy (irrespective of menstrual status), ovarian suppression by low blood concentrations of FSH and estradiol, bone mineral density. Monitor blood glucose levels and HbA1c periodically; blood pressure, electrolytes and ECG regularly in at-risk patients; signs and symptoms of hypersensitivity reactions, emerging CV disease, and worsening/developing psychiatric symptoms. For treatment of prostate cancer, monitor serum testosterone levels and prostate-specific antigen.
Drug Interactions
May increase risk of QT interval prolongation with agents known to induce torsades de pointes or prolong QT interval (e.g. quinidine, disopyramide, sotalol, amiodarone, methadone, moxifloxacin, antipsychotics). May reduce the level of GnRH receptors in the pituitary with drugs known to increase prolactin levels.
Lab Interference
May cause a misleading pituitary-gonadal diagnostic test result when conducted during or after treatment discontinuation; chronic use may suppress pituitary-gonadal function and for up to 8 weeks after stopping the therapy.
Action
Description: Triptorelin is a synthetic decapeptide agonist analogue of natural gonadotropin-releasing hormone (GnRH). It stimulates the pituitary to secrete more LH and FSH which will initially result in increased serum testosterone levels in men or serum estrogen concentrations in women. After chronic administration, triptorelin causes the inhibition of pituitary LH- and FSH-secretion, thereby decreasing testicular and ovarian steroidogenesis by which the serum testosterone levels and serum estradiol concentrations fall to within the castrate or postmenopausal range, respectively.
Pharmacokinetics:
Absorption: Rapidly absorbed following SC inj.
Distribution: Volume of distribution: 30-33 L.
Excretion: Via urine (42% as intact peptides). Elimination half-life: 2.8 ± 1.2 hours.
Chemical Structure

Chemical Structure Image
Triptorelin

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 25074470, Triptorelin. https://pubchem.ncbi.nlm.nih.gov/compound/Triptorelin. Accessed Mar. 26, 2021.

Storage
Store between 2-8°C or below 25°C. Protect from light. Do not freeze. Storage recommendations may vary among countries or individual products (refer to specific product guidelines).
ATC Classification
L02AE04 - triptorelin ; Belongs to the class of gonadotropin releasing hormone analogues. Used in endocrine therapy.
References
Anon. Triptorelin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 26/11/2020.

Buckingham R (ed). Triptorelin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 26/11/2020.

Decapeptyl 0.1 mg Injection (Ferring Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 26/11/2020.

Decapeptyl SR 11.25 mg, Powder and Solvent for Suspension for Injection (Ipsen Limited). MHRA. https://products.mhra.gov.uk. Accessed 26/11/2020.

Decapeptyl SR 22.5 mg Powder and Solvent for Suspension for Injection (Ipsen Limited). MHRA. https://products.mhra.gov.uk. Accessed 26/11/2020.

Decapeptyl SR 3 mg, Powder for Suspension for Injection (Ipsen Limited). MHRA. https://products.mhra.gov.uk. Accessed 26/11/2020.

Diphereline PR 3.75 mg (IPSEN Pharma [Hong Kong]). MIMS Hong Kong. http://www.mims.com/hongkong. Accessed 26/11/2020.

Gonapeptyl Depot 3.75mg, Powder and Solvent for Suspension for Injection (Ferring Pharmaceuticals Ltd). MHRA. https://products.mhra.gov.uk. Accessed 26/11/2020.

Joint Formulary Committee. Triptorelin. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 26/11/2020.

Pamorelin 11.25 mg Powder for Suspension for Injection (Orient Europharma [M] Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 26/11/2020.

Pamorelin 22.5 mg Powder for Suspension for Injection (Orient Europharma [M] Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 26/11/2020.

Pamorelin 3.75 mg Powder for Suspension for Injection (Orient Europharma [M] Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 26/11/2020.

Salvacyl, 11.25 mg Powder and Solvent for Prolonged-Release Suspension for Injection (Ipsen Limited). MHRA. https://products.mhra.gov.uk. Accessed 26/11/2020.

Trelstar (Verity Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 26/11/2020.

Triptodur (Arbor Pharmaceuticals, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 26/11/2020.

Disclaimer: This information is independently developed by MIMS based on Triptorelin from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 MIMS. All rights reserved. Powered by MIMS.com
  • Diphereline/Diphereline P.R.
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