Trade Names:Supprelin LA- Implant 50 mg
Trade Names:Vantas- Implant 50 mg
Inhibits gonadotropin secretion.
C max is 1.1 ng/mL, occurring in 12 h. Bioavailability is 92%. Average rate of subcutaneous drug release is 56.7 mcg/day.
Vd following subcutaneous bolus of 500 mcg is 58 L. Unbound drug in plasma is 29.5%.
One single metabolite resulting from C-terminal dealkylation and possible fragments resulting from hydrolysis. Apparent Cl after a 50 mg subcutaneous implant is approximately 174 mL/min.
Terminal t ½ is 3.92 h.
Average serum histrelin concentrations are approximately 50% higher in patients with renal function impairment.Hepatic Function Impairment
Treatment of children with central precocious puberty.Vantas
Palliative treatment of advanced prostate cancer.
Women who are or may become pregnant while receiving this drug; patients hypersensitive to gonadotropin-releasing hormone (GnRH), GnRH agonist analogs, or any component of the product; women and children ( Vantas ).
Subcutaneous 1 implant (50 mg) for 12 mo. Implant must be removed after 12 mo, at which time another implant may be inserted to continue therapy.
Store implant in refrigerator (36° to 46°F). Protect from light. Do not freeze.
None well documented.
Results of diagnostic tests of pituitary gonadotropic and gonadal function may be affected.
Palpitations, ventricular extrasystoles (less than 2%).
Fatigue (10%); headache, insomnia (3%); decreased libido (2%); depression, dizziness, irritability, lethargy, malaise, tremor, weakness (less than 2%).
Contusion, hematoma, hypotrichosis, increased sweating, night sweats, pruritus (less than 2%).
Constipation (4%); abdominal discomfort, nausea (less than 2%).
Renal function impairment, testicular atrophy (5%); erectile dysfunction, gynecomastia (4%); aggravated gynecomastia, aggravated hematuria, aggravated renal failure, aggravated urinary frequency, breast pain, breast tenderness, dysuria, genital pruritus (male), renal calculus, sexual dysfunction, urinary frequency, urinary retention (less than 2%).
Anemia (less than 2%).
Hepatic disorder (less than 2%).
Increased AST, blood glucose, blood LDH, blood testosterone, and prostatic acid phosphatase, decreased CrCl (less than 2%).
Implant-site reactions (51%); keloid scar, scar, suture-related complication (6%); application-site pain, postprocedural pain (4%); wound infection.
Weight increase (2%); fluid retention, food craving, hypercalcemia, hypercholesterolemia, increased appetite, peripheral edema, weight decrease (less than 2%).
Aggravated back pain, arthralgia, back pain, bone pain, muscle twitching, myalgia, neck pain, pain in limb (less than 2%).
Exertional dyspnea (less than 2%).
Hot flashes (66%); exacerbated pain, feeling cold, flushing, pain, stent occlusion (less than 2%).
Monitor luteinizing hormone, follicle stimulating hormone, and estradiol or testosterone at 1 mo post implantation then every 6 mo thereafter. Assess height and bone age every 6 to 12 mo.Vantas
Ensure serum testosterone and prostate-specific antigen are periodically measured to monitor response to therapy, especially if anticipated clinical or biochemical response to therapy has not been achieved.
Category X .
Safety and efficacy not established in children younger than 2 yr of age.Vantas
Patients may experience worsening of symptoms or onset of new symptoms during the first week of treatment.
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