histrelin

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histrelin

[his-trel´in]

a synthetic preparation of gonadotropin-releasing hormone, used as the acetate ester in treatment of precocious puberty.

histrelin

(hiss-tre-lin) ,

Supprelin LA

(trade name),

Vantas

(trade name)

Classification

Therapeutic: hormones
Pharmacologic: gonadotropin releasing hormones

Pregnancy Category: X

Indications

Palliative treatment of advanced prostate cancer (Vantas).Central precocious puberty (Supprelin LA).

Action

Continuous administration decreases production of gonadotropins.

Therapeutic effects

Suppression of testosterone production.

Prevention of disease progression.

Pharmacokinetics

Absorption: Highly absorbed (92%) from implant. Peak absorption occurs at 12 hours, and continues over 1–year period.

Distribution: Unknown.

Protein Binding: 29%.

Metabolism and Excretion: Unknown.

Half-life: 3.92 hours.

Time/action profile (↓ in LH, FSH, and sex-steroid levels)

ROUTE	ONSET	PEAK	DURATION
Subcut	unknown	12 hr	52 wk

Contraindications/Precautions

Contraindicated in: Hypersensitivity to any component of the product, GnRH, or GnRH agonist analogs; Women.

Use Cautiously in: Patients with metastatic vertebral lesions or urinary tract obstruction (initial transient ↑ in testosterone may worsen symptoms); Pediatric: Children <2 yr (safety not established) (Supprelin LA).

Adverse Reactions/Side Effects

Central nervous system

stroke (life-threatening)
headache (most frequent)
anxiety
depression
dizziness
insomnia
irritability
lethargy
malaise
seizures

Ear, Eye, Nose, Throat

visual disturbances

Respiratory

dyspnea

Cardiovascular

Myocardial infarction (life-threatening)
vasodilation (most frequent)
edema
palpitations
tachycardia

Gastrointestinal

hepatotoxicity (life-threatening)
abdominal discomfort
constipation
nausea
vomiting

Genitourinary

dysuria
hematuria
polyuria
urinary retention

Dermatologic

acne
↑ sweating
pruritis
rash

Endocrinologic

breast discharge
breast pain
genital pruritis
↑ breast size

Hematologic

anemia

Local

itching, erythema, and swelling at implantation site (most frequent)

Metabolic

hypercalcemia
hyperglycemia
hyperlipidemia

Musculoskeletal

arthralgia
bone pain
joint stiffness
muscle cramps
muscle stiffness
myalgia

Neurologic

tremor

Miscellaneous

allergic reactions including angioedema (life-threatening)
hot flashes (most frequent)
↑ appetite
↑ pain

Interactions

Drug-Drug interaction

Unknown.

Route/Dosage

Prostate Cancer

Subcutaneous (Adults) 50 mg implant inserted every 12 mo.

Central Precocious Puberty

Subcutaneous (Children ≥2 yr) 50 mg implant inserted every 12 mo.

Availability

Injection: 50 mg/implant

Nursing implications

Nursing assessment

Obtain a complete physical and endocrinologic examination, including height, weight, before starting, after 3 mo and every 6–12 mo during therapy.
Assess for signs of disease progression periodically throughout therapy.
Monitor patient for signs of hypersensitivity (angioedema, urticaria, hypotension, tachycardia, loss of consciousness, bronchospasm, dyspnea, flushing, pruritus). Discontinue therapy if any of these symptoms occur.
Lab Test Considerations: Monitor LD, FSH, estradiol, or testosterone at 1 mo after implantation and every 6 mo thereafter.
- May cause ↑ AST and LDH; usually reversible with removal of implant.

Potential Nursing Diagnoses

Sexual dysfunction (Indications)
Deficient knowledge, related to medication regimen (Patient/Family Teaching)

Implementation

Subcutaneous: Histrelin is given as a single yearly subcutaneous implant. The implant must be removed after 12 mo of therapy. Subsequent implantation may be used to continue therapy.

Patient/Family Teaching

Instruct patient to not to get arm wet for 24 hrs and to avoid strenuous lifting for 7 days after insertion.
Inform patient and family that if implants are not given yearly, disease may progress.
Advise patient and family that during initial agonistic phase (1–3 wk) the patient may have transient symptom worsening or onset of new symptoms, including bone pain, neuropathy, hematuria, or urinary tract obstruction.
Inform patient and family that redness or swelling may occur at the implantation site, especially after initial implantation or implant removal. Notify health care professional if this reaction is severe or does not go away.
Instruct patient and family to contact health care professional at the first sign of skin rash, urticaria, rapid heartbeat, difficulty swallowing or breathing, or any swelling that may suggest angioedema.

Evaluation/Desired Outcomes

Palliation of signs and symptoms associated with prostate cancer.
Delay of early onset of puberty.

Mentioned in ?

References in periodicals archive ?

Subcutaneous histrelin implants (Vantas[R]) are used in the treatment of prostate cancer and would not improve incontinence symptoms.

Getting Ready for Certification: Urinary Incontinence

LHRH analogs include; leuprolide (Lupron, Eligard), goserelin (Zoladex), triptorelin (Trelstar), and histrelin (Vantas).

Testosterone and Prostate Cancer: Who is Right?

Time to menarche and final height after histrelin implant treatment for central precocious puberty.

A Critical Appraisal of the Effect of Gonadotropin-Releasing Hormon Analog Treatment on Adult Height of Girls with Central Precocious Puberty

Treatment with a gonadotropin-releasing hormone agonist such as leuprolide or histrelin can be initiated for adolescents in Tanner Stage 2, assessed by hormone levels, as well as breast, testicle, and pubic hair development (childgrowthfoundation.org/CMS/FILES/ Puberty_and_the_Tanner_Stages.pdf), to suppress ongoing puberty.

Transgender patients: providing sensitive care

The GnRH agonists used for pubertal suppression in GD include two of those approved for the treatment of precocious puberty: leuprolide by monthly intramuscular injection, and histrelin, a subcutaneous implant with yearly dosing.

Gender dysphoria in children and suppression of debate

Lack of correlation between fertility and sperm numbers in male rats treated with histrelin, a potent LHRH agonist.

Pig spermatozoa defect in acrosome formation caused poor motion parameters and fertilization failure through artificial insemination and in vitro fertilization

Cyclosporine, Cycloserine, Eflornithine, Everolimus, Histrelin,

Repurposing - finding new uses for old (and patented) drugs: bridging the "Valley of Death," to translate academic research into new medicines

Commercial examples include histrelin implants for the palliative treatment of prostate cancer and uterine fibroids, and early puberty in children, levonorgestrel and etonogestrel implants for family planning, and buprenorphine for the treatment of opioid addiction (pending FDA approval).

Implantable drug delivery devices--an overview

GnRH analogs used for pubertal delay include leuprolide (Lupron[R] [subcutaneous injection; 50 mcg/kg/day, may increase by 10 mcg/kg/day as needed] and Lupron[R] Depot [intramuscular injection; 15 mg every 4 weeks in children more than 37.5 kg or 22.5 mg IM every 3 months]) and histrelin (Supprelin[R] LA and Vantas[R] [yearly subcutaneous implant]) (Milazzo, 2008; Skidmore-Roth, 2007).

Care of the child with the desire to change gender--Part I

"A review of the pharmacokinetic and pharmacological properties of a once-yearly administered histrelin acetate implant in the treatment of prostate cancer," BJU International 103(s2): 7-13.

Recent publications

The Food and Drug Administration approved Supprelin LA (histrelin acetate subcutaneous implant) 50 mg for treatment of central precocious puberty in children.

Supprelin LA, Xyzal tablets

* Recommended Dosage: The once-yearly implant continuously releases approximately 65 mcg/day of the go nadotropin-releasing hormone analog histrelin. The implant is inserted in the upper aspect of the arm.