Histrelin (Supprelin LA, Vantas) is a GnRH analog that acts on the gonadotropin-releasing cells of the anterior pituitary and inhibits the secretion of LH and FSH. It is indicated for the treatment of precocious puberty and advanced prostatic carcinoma.

Histrelin Uses:

• Central precocious puberty (Supprelin LA):

  • It is used to treat central precocious puberty in children.

• Advanced prostate cancer (Vantas):

  • It is indicated as a palliative treatment of advanced prostate cancer

Histrelin (Vantas) Dose in Adults

Histrelin (Vantas) Dose in the treatment of advanced Prostate cancer:

• Subcutaneous: 50 mg, as surgical implant every 12 months

Histrelin (Vantas) Dose in Childrens

Histrelin (Supprelin LA, Vantas) Dose in the treatment of central precocious puberty:

• Children ≥2 years:

  • Supprelin LA: Subcutaneous: 50 mg, as surgical implant every 12 months

Pregnancy Risk Factor X

• It is not recommended during pregnancy.
• It can cause fetal harm and spontaneous abortion.

Histrelin use during breastfeeding:

• It is unknown if breast milk contains histrelin.
• These products are not recommended for postpubertal women.

Dose in Kidney disease:

• Vantas: CrCl ≥15 mL/minute: No dose adjustment required.
• Supprelin LA: Manufacturer has not provided dose adjustment.

Dose in Liver disease:

The manufacturer has not provided dose adjustment in labeling.

Common Side Effects of Histrelin (Supprelin LA, Vantas):

• Dermatologic:

  • Dermatological Reaction

Less Common Side Effects Of Histrelin (Supprelin LA, Vantas):

• Central Nervous System:

  • Emotional Lability
  • Headache
  • Migraine
  • Sensation Of Cold

• Dermatologic:

  • Scarring
  • Pruritus

• Endocrine & Metabolic:

  • Gynecomastia
  • Hypermenorrhea
  • Weight Gain

• Genitourinary:

  • Uterine Hemorrhage
  • Breast Tenderness
  • Dysmenorrhea
  • Precocious Puberty

• Hematologic & Oncologic:

  • Pituitary Neoplasm

• Infection:

  • Localized Infection

• Local:

  • Application Site Pain

• Neuromuscular & Skeletal:

  • Keloid-Like Scar

• Respiratory:

  • Epistaxis
  • Flu-Like Symptoms

• Miscellaneous:

  • Procedural Complications
  • Postoperative Pain

Frequency of Side effects Not Defined:

• Endocrine & Metabolic:

  • Altered Hormone Levels

Prostate Cancer:

Common Side Effects Of Histrelin (Supprelin LA, Vantas):

• Dermatologic:

  • Dermatological Reaction

• Endocrine & Metabolic:

  • Hot Flash

Less Common Side Effects Of Histrelin (Supprelin LA, Vantas):

• Cardiovascular:

  • Flushing
  • Palpitations
  • Peripheral Edema
  • Ventricular Premature Contractions

• Central Nervous System:

  • Fatigue
  • Headache
  • Insomnia
  • Depression
  • Dizziness
  • Irritability
  • Lethargy
  • Malaise
  • Pain
  • Sensation Of Cold

• Dermatologic:

  • Diaphoresis
  • Genital Pruritus
  • Hypotrichosis
  • Night Sweats
  • Pruritus

• Endocrine & Metabolic:

  • Gynecomastia
  • Decreased Libido
  • Weight Gain
  • Fluid Retention
  • Hypercalcemia
  • Hypercholesterolemia
  • Increased Lactate Dehydrogenase
  • Increased Prostatic Acid Phosphatase
  • Increased Serum Glucose
  • Weight Loss

• Gastrointestinal:

  • Constipation
  • Abdominal Distress
  • Food Cravings
  • Increased Appetite
  • Nausea

• Genitourinary:

  • Testicular Atrophy
  • Erectile Dysfunction
  • Breast Tenderness
  • Dysuria
  • Exacerbation Of Gynecomastia
  • Exacerbation Of Hematuria
  • Exacerbation Of Urinary Frequency
  • Hematuria
  • Mastalgia
  • Urinary Frequency
  • Urinary Retention

• Hematologic & Oncologic:

  • Anemia
  • Bruise
  • Hematoma

• Hepatic:

  • Hepatic Disease
  • Increased Serum AST

• Local:

  • Bruising At Injection Site
  • Pain At Injection Site
  • Tenderness At Injection Site
  • Erythema At Injection Site
  • Inflammation At Injection Site
  • Injection Site Infection

• Neuromuscular & Skeletal:

  • Arthralgia
  • Back Pain
  • Exacerbation Of Back Pain
  • Limb Pain
  • Muscle Twitching
  • Myalgia
  • Neck Pain
  • Ostealgia
  • Tremor
  • Weakness

• Renal:

  • Renal Insufficiency
  • Decreased Creatinine Clearance
  • Exacerbation Of Renal Failure
  • Nephrolithiasis

• Respiratory:

  • Dyspnea On Exertion

• Miscellaneous:

  • Stent Occlusion

Contraindications to Histrelin (Supprelin LA, Vantas):

• Hypersensitivity to any component of histrelin, Gonadotropin-releasing hormone (GnRH), or GnRH-agonist analogs
• Females who may or are pregnant

Warnings and precautions

• Cardiovascular effects

  • Androgen-deprivation treatment (ADT), has the potential to increase your risk of cardiovascular events such as stroke, MI, and sudden cardiac deaths.
  • ADT can prolong the QT interval. Patients with preexisting conditions that could cause QT prolongation should weigh the risks and benefits of ADT.
  • Regular monitoring of electrolytes and ECG is recommended.

• Hyperglycemia:

  • Hyperglycemia may occur with androgen-deprivation therapy (in prostate carcinoma).
  • This can lead to new-onset diabetes, or worsening glycemic control for pre-diabetic people.
  • Keep an eye on your blood sugar levels.

• Pituitary apoplexy

  • GnRH agonists can cause pituitary apoplexy in rare cases (onset between 1 hour and 2 weeks).
  • It can present as a sudden headache, vomiting or visual state change.

• Psychiatric events

  • GnRH agonists can cause aggression, emotional liability, impotence and irritability.
  • For psychiatric symptoms, monitoring is recommended.

• Seizures:

  • GnRH agonists, including histrelin, may cause a seizure
  • These conditions can be caused by known conditions or patients who have not yet been diagnosed.

• Compression of the spinal cord:

  • It has been reported that it can cause paralysis.
  • Monitoring is recommended for weakness and paresthesias in patients suffering from metastatic vertebral diseases, especially at the beginning of therapy.

• Tumor flare:

  • It can temporarily raise serum testosterone and worsen symptoms such as bone pain, neuropathy and hematuria.

• Occlusion of the urinary tract:

  • It is possible to have a urinary tract obstruction if it is being used for prostate cancer Ureteral
  • Monitor your urinary tract for obstruction.

• Worsening symptoms

  • When central precious puberty is being used, there may be a temporary increase in the serum estradiol and testosterone levels in females.
  • However, puberty symptoms should diminish within four weeks.

Monitoring parameters:

Central precocious puberty (CPP):

• LH, FSH, estradiol, or testosterone (after 1 month then every 6 months)
• Height,
• Bone age (every 6 to 12 months)
• Tanner staging
• Monitor for clinical evidence of suppression of CPP manifestations
• Monitor for psychiatric symptoms, including depression.

Prostate cancer:

• Serum testosterone levels
• prostate-specific antigen (PSA)
• Bone mineral density
• Weakness
• Paresthesias, and urinary tract obstruction (especially during the first few weeks of therapy)
• Blood sugars
• Monitor for symptoms associated with cardiovascular disease
• ECG and electrolytes frequently.

How to administer Histrelin (Supprelin LA, Vantas)?

It is inserted subcutaneously: Surgical implantation into the inner portion of the upper arm (non-dominant) with implantation device. Do not bend or pinch the implant;

The site on arm:

• implant halfway between the shoulder and the elbow at the crease between the tricep and the bicep

Implant Removal:

• It should be removed after ~12 months. Palpate to locate implant for removal. If not palpable, ultrasound, CT, or MRI may be used to locate the implant; plain films are not helpful because the implant is not radiopaque

Refer to the manufacturer's labeling for full insertion and removal details.

Mechanism of action of Histrelin (Supprelin LA, Vantas):

• It acts as a powerful inhibitor of gonadotropin production.
• Continuous administration causes a decrease in testosterone and dihydrotestosterone (males), and an increase in estrone, estradiol (premenopausal women).
• Within 2 - 4 Weeks, it reduces testosterone levels castration in males treated for prostate cancer.
• The linear growth velocity in central precocious puberty is slower, which increases the likelihood of reaching predicted adult height.

The beginning of action:

• Prostate cancer: In 2 to 4 weeks, chemical castration.
• CPP: The progression of sexual development is stopped and growth is slowed within a month

Time:

• 12 Months (plus a few weeks of histrelin-release)

Protein binding

• Adults: 70% +- 9 %

Metabolism:

• Hepatic via Cterminal dealkylation, hydrolysis

Bioavailability:

• Adults: Subcutaneous: 92%

Half-life elimination:

• Terminal for Adults: 4 Hours

Time to reach the peak

• Serum: Adults: 12 Hours

International Brand Names of Histrelin:

• Supprelin LA
• Vantas
• Vantasse
• Vantus

Histrelin Brand Names in Pakistan:

No Brands Available in Pakistan.