Triptorelin (Decapeptyl) is a gonadotrophin-releasing hormone (GnRH) analog that reduces the production of estrogens and testosterone by decreasing the FSH and LH.

Indications of Triptorelin (Decapeptyl):

• Central precocious puberty:

  • Triptodur: It is used for treating central precocious puberty in patients 2 years and older.

• Advanced Prostate cancer:

  • Trelstar: It is indicated for palliative treatment of advanced prostate cancer.

• Assisted reproductive technologies:

  • Decapeptyl [Canadian product]: It is given as an adjunct therapy in women undergoing controlled ovarian hyperstimulation for assisted reproductive technologies (ART)

• Off Label Use of Triptorelin in Adults:

  • Endometrial stromal sarcoma;
  • Endometriosis;
  • Paraphilia/hypersexuality

Triptorelin (Decapeptyl) dose in Adults:

Triptorelin (Decapeptyl) dose in the treatment of advanced Prostate cancer:

• Trelstar: An intramuscular dose of

  • 75 mg once every 4 weeks or
  • 25 mg once every 12 weeks or
  • 5 mg once every 24 weeks

Triptorelin (Decapeptyl) dose in the adjunctive therapy of Controlled ovarian hyperstimulation for assisted reproductive technologies (ART):

Decapeptyl (Canadian product):

• Usual dose: 0.1 mg once daily subcutaneous initiated on day 2 or 3 or days 21 to 23 of the menstrual cycle (or 5 to 7 days before menses).
• The dose may be adjusted according to ovarian response as measured by ovarian ultrasound with or without serum estradiol levels.
• Treatment is continued until follicles achieve a suitable size (typically 4 to 7 weeks).

Triptorelin (Decapeptyl) dose in the treatment of Endometrial stromal sarcoma (off-label):

• 3.75 mg intramuscular once every 28 days for 3 to 5 months.

Triptorelin (Decapeptyl) dose in the treatment of Endometriosis (off-label):

• 3.75 mg intramuscular once every 4 weeks for a total of 6 doses or
• 3.75 mg once every 6 weeks for a total of 4 doses or
• 11.25 mg once every 3 months
• To prevent bone damage, hormonal add on therapy such as estrogens/progestins is given at the start of treatment.
• Due to side effects, GnRH-agonists use is limited to less than 6 or 12 months.

Triptorelin (Decapeptyl) dose in the treatment of paraphilia/ hypersexuality (off-label):

Note:

An initial increase in androgen concentrations can be controlled by antiandrogen such as flutamide, cyproterone) for 1 to 2 months.

It should be avoided in patients with osteoporosis or active pituitary pathology.

• Test dose: 1 mg subcutaneous(observe for hypersensitivity); if tolerated, follow with monthly intramuscular injections
• 3.75 mg  intramuscular monthly

Triptorelin (Decapeptyl) dose in Childrens

Triptorelin (Decapeptyl) dose for the treatment of Central precocious puberty:

• Children ≥2 years:

  • Triptodur: 22.5 mg intramuscular once every 24 weeks;
  • discontinue therapy at appropriate age of onset of puberty.

Pregnancy Risk Category: X

• Studies on animal reproduction showed that fetal harm was evident.
• Pregnancy is not a good time to take triptorelin.
• Triptorelin, which is a short-lived hormone, should not be found in the maternal serum during embryo transfer.
• It can lead to impaired fertility in men.

Triptorelin use during breastfeeding:

• It is not known if triptorelin is excreted in breast milk.
• According to the manufacturer, the decision to stop breastfeeding or discontinue using the drug is based on the mother's need for it.

Dose adjustment in renal disease:

There are no dosage adjustments provided in the manufacturer's labeling. However, renal impairment increases systemic exposure to triptorelin.

Dose adjustment in liver disease:

There are no dosage adjustments provided in the manufacturer's labeling. However, hepatic impairment increases systemic exposure to triptorelin. 

Common Side Effects of Triptorelin (Decapeptyl):

• Central Nervous System:

  • Headache

• Endocrine & Metabolic:

  • Hot Flash
  • Increased Serum Glucose

• Hematologic & Oncologic:

  • Decreased Hemoglobin
  • Decreased Red Blood Cells

• Hepatic:

  • Increased Serum Alanine Aminotransferase
  • Increased Serum Aspartate Aminotransferase
  • Increased Serum Transaminases

• Local:

  • Pain At Injection Site
  • Erythema At Injection Site

• Neuromuscular & Skeletal:

  • Skeletal Pain

• Renal:

  • Increased Blood Urea Nitrogen

• Respiratory:

  • Nasopharyngitis

Rare Side Effects of Triptorelin (Decapeptyl):

• Cardiovascular:

  • Lower Extremity Edema
  • Hypertension
  • Chest Pain
  • Peripheral Edema

• Central Nervous System:

  • Pain
  • Dizziness
  • Anxiety
  • Fatigue
  • Mood Changes
  • Insomnia
  • Emotional Lability

• Dermatologic:

  • Injection Site Pruritus
  • Skin Rash
  • Pruritus

• Endocrine & Metabolic:

  • Decreased Libido
  • Dependent Edema
  • Gynecomastia

• Gastrointestinal:

  • Gastroenteritis
  • Nausea
  • Anorexia
  • Constipation
  • Dyspepsia
  • Vomiting
  • Abdominal Pain
  • Diarrhea

• Genitourinary:

  • Erectile Dysfunction
  • Menstruation
  • Testicular Atrophy
  • Impotence
  • Dysuria
  • Mastalgia
  • Urinary Retention
  • Urinary Tract Infection

• Hematologic & Oncologic:

  • Anemia

• Hepatic:

  • Increased Serum Alkaline Phosphatase
  • Hepatic Insufficiency

• Infection:

  • Influenza

• Local:

  • Swelling At Injection Site

• Neuromuscular & Skeletal:

  • Lower Extremity Pain
  • Back Pain
  • Lower Limb Cramps
  • Arthralgia
  • Asthenia
  • Myalgia

• Ophthalmic:

  • Conjunctivitis
  • Eye Pain

• Otic:

  • Otitis Externa

• Respiratory:

  • Upper Respiratory Tract Infection
  • Cough
  • Bronchitis
  • Pharyngitis
  • Sinusitis
  • Dyspnea

• Miscellaneous:

  • Postoperative Pain
  • Missed Abortion

Frequency of Side effects Not Defined:

• Endocrine & Metabolic:

  • Increased Testosterone Level

Contraindications to Triptorelin (Decapeptyl):

• Hypersensitivity to triptorelin, any component of the formulation, or any other GnRH antagonists or GnRH
• pregnancy
• Breastfeeding women

Warnings and precautions

• Cardiovascular effects

  • There are several possible causes of sudden cardiac death, including myocardial injury, QT/QTc prolongation, stroke, and prolonged QT/QTc interval.
  • High-risk cases require monitoring of electrolytes and ECG.

• Reduced bone density

  • Long term GnRH agonist therapy may increase the risk of osteoporosisand bone fractures.

• Hyperglycemia:

  • This can cause hyperglycemia and new-onset DM.
  • Therefore, it is important to monitor blood glucose levels and glycosylated hemoglobin.

• Hypersensitivity reactions

  • In angioedema or anaphylaxis, it is best to avoid.

• Ovarian hyperstimulation syndrome:

  • Decapeptyl [Canadian Product]Ovarian hyperstimulation syndrome can present as severe dyspnea, hypotension, abdominal pain, nausea/vomiting and diarrhea.
  • It indicates a higher WBC, deranged liver enzymes, electrolytes, decreased creatinine clearing, hemoconcentration and hypoproteinemia.
  • The treatment involves the cessation of drug, hydration and analgesics as well as electrolyte management.

• Pituitary apoplexy

  • Pituitary apoplexy can cause sudden headaches, vomiting, changes in visual or mental status, and sometimes even cardiovascular collapse.

• Psychiatric effects

  • Triptorelin can cause emotional lability symptoms such as anger, crying, irritability and aggression.

• Seizures:

  • Single-agent seizures can also be caused by concurrent medication.

• Compression of the spinal cord:

  • There are cases of spinal cord compression that can lead to paralysis or weakness.

• Symptom flare:

  • Patients diagnosed with prostate cancer might experience increased bone pain, neuropathy or hematuria.
  • Transient vaginal bleeding may occur in female patients with central precocious sperm.

Triptorelin: Drug Interaction

Monitoring parameters:

• Blood glucose and glycosylated hemoglobin
• ECG
• signs and symptoms of emerging cardiovascular disease
• development/worsening of psychiatric symptoms.

Additional monitoring (per indication):

• Treatment of precocious puberty:

  • Leutinizing hormone levels at baseline, or serum sex steroid levels beginning 1 to 2 months after starting, during therapy, and with each subsequent dose; height every 3 to 6 months
  • bone age monthly

• Prostate cancer:

  • Serum testosterone levels
  • prostate-specific antigen
  • bone density.

• Assisted reproductive technologies: Decapeptyl [Canadian product]:

  • Rule out for pregnancy
  • signs/symptoms of an allergic reaction during therapy
  • ultrasound/ estradiol levels to assess follicle development

• Ovarian hyperstimulation syndrome:

  • Weight /vitals
  • Hb/hematocrit
  • Monitoring of abdominal circumference,
  • Serum electrolytes/albumin
  • Renal function test/Liver function tests
  • urine output/urine specific gravity
  • cardiorespiratory status

• Treatment of paraphilia/hypersexuality (off-label use):

  • CBC
  • serum BUN and creatinine
  • Serum FSH and LH
  • testosterone
  • ECG
  • bone density

How to administer Triptorelin (Decapeptyl)?

IM:

• Intramuscular injection into the buttock (Trelstar) or thigh (Triptodur);
• It should be given under the supervision of a health care provider.

SubQ:

• Decapeptyl [Canadian product] is administered by subcutaneous injection into the lower abdomen.
• If a dose is missed, it can be administered on the same day; however, do not double doses.
• It must be administered under the supervision of a health care provider.

Mechanism of action of Triptorelin (Decapeptyl):

• Triptorelin is a gonadotrophin-releasing hormone analog that decreases FSH, LH with using for 2-4 weeks resulting in suppression of ovarian and steroidal gonadogenesis thereby reducing the production of estrogens and testosterone.
• It prevents premature LH surge in women who are subject to controlled ovarian stimulation when assisted reproductive techniques are used.

Protein binding: None

Metabolism: Unknown; unlikely to involve CYP; no known metabolites

Half-life elimination: 2.8 ± 1.2 hours Moderate-to-severe renal impairment: 6.6 to 7.7 hours Hepatic impairment: 7.6 hours

Time to peak:

• Trelstar: 1 to 3 hours
• Triptodur: 4 hours

Excretion: Occurs in urine (42% as an intact peptide) or liver 

International Brands of Triptorelin (Decapeptyl):

• Trelstar Mixject
• Trelstar
• Triptodur
• Decapeptyl
• Arvekap
• Decapeptyl
• Decapeptyl CR
• Decapeptyl Daily
• Decapeptyl Depot
• Decapeptyl LA
• Decapeptyl LP
• Decapeptyl Retard
• Decapeptyl SR
• Decapetyl
• Diphereline
• Diphereline PR
• Fertipeptil
• Gonapeptyl
• Gonapeptyl CR
• Gonapeptyl Daily
• Gonapeptyl Depot
• Gonapeptyl,CR
• GonapeptylCR
• Neo Decapeptyl
• Neo-Decapeptyl CR
• Pamorelin
• Salvacyl

Triptorelin Brand Names in Pakistan: