Drug information of Triptorelin

Mechanism of effect

Synthetic analog of gonadotropin-releasing hormone (GnRH) that acts as potent inhibitor of gonadotropin secretion

Pharmacodynamic

Synthetic analog of gonadotropin-releasing hormone (GnRH) that acts as potent inhibitor of gonadotropin secretion

Pharmacokinetics

C max is approximately 28.43 ng/mL, 38.5 ng/mL, and 44.1 ng/mL for triptorelin 3.75 mg, 11.25 mg, and 22.5 mg, respectively. T max is 1 to 3 h. Vd is 30 to 33 L (from an IV dose of 0.5 mg). There is no evidence of protein binding. No metabolites are found. Pharmacokinetic data suggest that C-terminal fragments produced by tissue degradation are either completely degraded in the tissues or are rapidly degraded further in plasma, or cleared by the kidneys Triptorelin is eliminated by both the liver and kidneys. 41.7% of a dose is excreted in urine. Time to peak effect occurs on day 4, days 2 to 3, or on day 3 for triptorelin 3.75 mg, 11.25 mg, or 22.5 mg, respectively. Duration of action is 4 wk for triptorelin 3.75 mg, and 3 to 4 wk for triptorelin 11.25 and 22.5 mg

Drug indications

Ovary cancer , Pancreatic Cancer , Palliative treatment of advanced prostate cancer , endometriosis , growth hormone deficiency

Dosage

Advanced Prostate Cancer Adults IM Dosing schedule depends on product strength selected. 3.75 mg once every 4 wk; 11.25 mg once every 12 wk; 22.5 mg once every 24 wk

Drug contraindications

Pregnancy , hypersensitivity to drug or its components.

Side effects

nausea , Headache , insomnia , chest pain , constipation , abdominal pain , dizziness , vomiting , fatigue , Angioedema , Hepatic dysfunction , rash , flushing , Diarrhea , Dyspnea , asthenia , pruritus , Hypertension , thrombocytopenia , neutropenia , lymphopenia , leukopenia , anemia , dyspepsia , Urinary tract infection , edema , Peripheral edema , Cough , impotence , myalgia , Flu-like symptoms , Injection-site reaction , anorexia , conjunctivitis , Gynecomastia , Arthralgia , pain in the extremities , back pain , bronchitis , Pain , Phosphate Alkaline increased , eye pain , urinary retention , Anaphylactic reaction , pharyngitis , dysuria , decreased libido

Interactions

Pimozide , Amitriptyline , Ranitidine , Cimetidine , Fluoxetine , Methyldopa , Verapamil , Glibenclamide , Toremifene , Dolasetron , vandetanib , sparfloxacin , Procainamide , Dofetilide , Inotuzumab‎ , Ganirelix , Arsenic trioxide , Halofantrine , Grepafloxacin , Paliperidone , Entrectinib , Bepridil , bedaquiline , Gemtuzumab , vemurafenib

Alerts

Monitor response to triptorelin by measuring serum levels of testosterone. 2-Closely observe patients with metastatic vertebral lesions and/or with upper or lower urinary tract obstruction during the first few weeks of therapy.

Points of recommendation

• For IM use only. • Reconstitute with sterile water; do not use any other diluent. • Administer triptorelin with a 21-guage needle immediately after reconstitution. • Advise patient, family, or caregiver that medication may temporarily worsen signs and symptoms of the disease (eg, bone pain, blood in urine, difficult or painful urination) but that these should improve in 3 to 4 wk. • Advise patient, family, or caregiver to immediately report any of the following to the health care provider: rash; itching or hives; swelling of the face, lips, eyes, or tongue; wheezing; shortness of breath; difficulty breathing; weakness or paralysis of legs; inability to urinate

Pregnancy level

X

Related drugs

Leuprolide acetate , Histrelin , Apalutamide