Trelstar (triptorelin pamoate)

Dosage of triptorelin pamoate is expressed in terms of the base.

No dosing information is available for this tab.

No dosing information is available for this tab.

In vitro, triptorelin does not inhibit cytochrome P-450 (CYP) isoenzymes 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, or 3A4/5 at clinically relevant concentrations. Triptorelin does not induce CYP isoenzymes 1A2 or 3A4/5.

Triptorelin is a poor substrate of P-glycoprotein (P-gp). In vitro, triptorelin does not inhibit P-gp.

There are no contraindication interactions for this drug.

There are no severe interactions for this drug.

There are no moderate interactions for this drug.

Known hypersensitivity to triptorelin or any other ingredient in the formulation, other gonadotropin-releasing hormone (GnRH) agonists, or GnRH. Known or suspected pregnancy. (See Fetal/Neonatal Morbidity and Mortality under Cautions: Warnings/Precautions.)

• Pregnancy

• Chronic heart failure
• Congenital long QT syndrome
• Hypokalemia
• Hypomagnesemia
• Lower seizure threshold
• Prolonged QT interval
• Seizure disorder

• Acute myocardial infarction
• Anemia
• Cerebrovascular accident
• Depression
• Diabetes mellitus
• Disease of liver
• Hypercholesterolemia
• Hypertension
• Kidney disease with reduction in glomerular filtration rate (GFr)
• Obesity
• Tobacco smoker
• Urinary tract obstruction
• Vertebral metastases

Initial (usually during the first week of therapy with the 3.75-, 11.25-, or 22.5-mg formulation of Trelstar(R)) transient increases in serum testosterone concentrations occur in most adults receiving triptorelin for prostate cancer and may be associated with temporary worsening of disease manifestations. (See Endocrine Effects under Cautions: Warnings/Precautions.) At least 10% of adults receiving the 11.25-mg formulation of triptorelin (Trelstar(R)) experienced abnormalities in laboratory values including decreased hemoglobin and erythrocyte count and increased serum concentrations of glucose, BUN, AST (SGOT), ALT (SGPT), and alkaline phosphatase. At least 10% of adults receiving the 22.5-mg formulation of triptorelin (Trelstar(R)) experienced abnormalities in laboratory values including decreased hemoglobin concentration, increased serum glucose concentrations, and increased serum hepatic aminotransferase (transaminase) concentrations.

Adverse effects occurring in 1% or more of adults receiving either the 3.75- or 11.25-mg formulation (Trelstar(R)) include hot flushes (flashes), skeletal pain, headache, impotence, pain at injection site, hypertension, leg pain, generalized pain, insomnia, fatigue, dizziness, diarrhea, and urinary retention. Additional adverse effects occurring in 1% or more of adults include vomiting, anemia, pruritus, urinary tract infection, and emotional lability in those receiving the 3.75-mg formulation.

Additional adverse effects occurring in 1% or more of adults receiving the 11.25-mg formulation (Trelstar(R)) include leg edema, dysuria, back pain, nausea, dependent edema, breast pain, arthralgia, decreased libido, chest pain, leg cramps, gynecomastia, constipation, dyspepsia, increased alkaline phosphatase, anorexia, coughing, rash, asthenia, peripheral edema, abdominal pain, abnormal hepatic function, myalgia, dyspnea, pharyngitis, eye pain, and conjunctivitis.

Adverse effects occurring in 5% or more of adults receiving the 22.5-mg formulation (Trelstar(R)) include hot flushes (flashes), influenza, hypertension, urinary tract infection, back pain, erectile dysfunction, arthralgia, headache, pain in extremity, testicular atrophy, bronchitis, diabetes mellitus or hyperglycemia, insomnia, peripheral edema, and urinary retention.

Adverse effects occurring in 5% or more of pediatric patients receiving the 22.5-mg formulation (Triptodur(R)) include injection site reactions, vaginal bleeding, hot flush, headache, cough, and infection (i.e., bronchitis, gastroenteritis, influenza, nasopharyngitis, otitis externa, pharyngitis, sinusitis, upper respiratory infection).

More Frequent

• Hypertension

Less Frequent

• Anemia
• Chest pain
• Transient testosterone increase in male
• Urinary retention
• Urinary tract infection

Rare or Very Rare

• Acute generalized exanthematous pustulosis
• Acute myocardial infarction
• Anaphylaxis
• Angioedema
• Cancer-related spinal cord compression
• Cerebrovascular accident
• Deep venous thrombosis
• Diabetes mellitus
• DRESS syndrome
• Hematuria
• Idiopathic intracranial hypertension
• Interstitial lung disease
• Pituitary apoplexy
• Pulmonary thromboembolism
• Seizure disorder
• Steatosis of liver
• Stevens-johnson syndrome
• Suicidal
• Suicidal ideation
• Thromboembolic disorder
• Toxic epidermal necrolysis
• Transient cerebral ischemia

More Frequent

• Bone pain
• Erectile dysfunction
• Injection site erythema
• Injection site pain
• Leg pain
• Testicular atrophy

Less Frequent

• Abnormal hepatic function tests
• Abnormal vaginal bleeding
• Acute abdominal pain
• Anorexia
• Arthralgia
• Back pain
• Bronchitis
• Conjunctivitis
• Constipation
• Cough
• Cramps in legs
• Diarrhea
• Dizziness
• Drug-induced hot flash
• Dyspepsia
• Dyspnea
• Fatigue
• General weakness
• Gynecomastia
• Headache disorder
• Hyperglycemia
• Injection site inflammation
• Insomnia
• Mastalgia
• Mood changes
• Myalgia
• Ocular pain
• Pain
• Pain in extremities
• Peripheral edema
• Pharyngitis
• Pruritus of skin
• Skin rash
• Symptoms of anxiety
• Vomiting

Rare or Very Rare

• Aggressive behavior
• Bullous dermatitis
• Depression
• Erythema multiforme
• Exfoliative dermatitis
• Irritability
• Thrombophlebitis
• Visual changes

No enhanced messaging available.

Safety and efficacy of triptorelin pamoate have not been established in pediatric patients younger than 2 years of age. Safety and efficacy of triptorelin pamoate in pediatric patients with central precocious puberty (CPP) have been established in an open-label, noncomparative study that included 44 pediatric patients 2-9 years of age.

Triptorelin may cause fetal harm if administered to pregnant women based on its mechanism of action and animal findings. (See Fetal/Neonatal Morbidity and Mortality under Cautions: Warnings/Precautions.)

It is not known whether triptorelin is distributed into human milk or if the drug has any effect on milk production or the nursing infant. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for triptorelin and any potential adverse effects on the breastfed infant from triptorelin or from the underlying maternal condition.

Clinical studies evaluating triptorelin pamoate in patients with prostate cancer have been conducted principally in patients 65 years of age and older since prostate cancer occurs mainly in an older patient population.