Histrelin

Histrelin Uses, Dosage, Side Effects, Food Interaction and all others data.

Histrelin is a gonadotropin releasing hormone (GnRH) agonist that acts as a potent inhibitor of gonadotropin when administered as an implant that delivers continuous therapeutic doses. Following an initial stimulatory phase with increased circulating levels of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to a transient increase in concentration of gonadal steroids (testosterone and dihydrotestosterone in males), continuous administration of histrelin acetate results in decreased levels of LH and FSH due to a reversible down-regulation of the GnRH receptors in the pituitary gland and desensitization of the pituitary gonadotropes.

As the product Supprelin LA (FDA), histrelin is indicated for the treatment of children with central precocious puberty (CPP). As the product Vantas (FDA), histrelin is indicated for the palliative treatment of advanced prostate cancer.

Long-term treatment with histrelin acetate suppresses the LH response to GnRH causing LH levels to decrease to prepubertal levels within 1 month of treatment. As a result, serum concentrations of sex steroids (estrogen or testosterone) also decrease. In the treatment of Central Precocious Puberty, this is relevant as secondary sexual development ceases to progress in most patients. Additionally, linear growth velocity is slowed which improves the chance of attaining predicted adult height.

Histrelin
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Histrelin
Availability	Prescription only
Generic	Histrelin
Histrelin Other Names	Histrelin, histrelina, histreline, histrelinum
Related Drugs	Triptodur, Supprelin LA, estradiol, tamoxifen, Premarin, Lupron, Xtandi, leuprolide, Casodex, Zytiga
Weight	50mg
Type	Subcutaneous, Subcutaneous Implant, Implant
Formula	C₇₀H₉₄N₁₈O₁₆
Weight	Average: 1443.632 Monoisotopic: 1442.709519019
Protein binding	For the product Vantas, the fraction of drug unbound in plasma measured in vitro was 29.5% Â± 8.9% (mean Â± SD).
Groups	Approved
Therapeutic Class
Manufacturer
Available Country	United States
Last Updated:	September 19, 2023 at 7:00 am

Uses

Histrelin is a GnRH agonist found in subcutaneous implants used for the treatment of pediatric patients with central precocious puberty and the palliative treatment of advanced prostate cancer.

Histrelin is also used to associated treatment for these conditions: Advanced Prostate Cancer, Central Precocious Puberty (CPP)

How Histrelin works

Food Interaction

No interactions found.

Histrelin Drug Interaction

Moderate: formoterol, formoterolUnknown: pemetrexed, pemetrexed, benzoyl peroxide / clindamycin topical, benzoyl peroxide / clindamycin topical, iodine i 131 tositumomab, iodine i 131 tositumomab, mesalamine, mesalamine, duloxetine, duloxetine, cytomegalovirus immune globulin, cytomegalovirus immune globulin, tamsulosin, tamsulosin, mycophenolic acid, mycophenolic acid, cyclosporine, cyclosporine

Volume of Distribution

The apparent volume of distribution of histrelin following a subcutaneous bolus dose of histrelin as the product Vantas (500 mcg) in healthy volunteers was 58.4 Â± 7.86 L

Elimination Route

Following subcutaneous insertion of one histrelin implant as the product Vantas in advanced prostate cancer patients (n = 17), peak serum concentrations of 1.10 Â± 0.375 ng/mL (mean Â± SD) occurred at a median of 12 hours. Continuous subcutaneous release was evident, as serum levels were sustained throughout the 52 week dosing period (see Figure 1). The mean serum histrelin concentration at the end of the 52 week treatment duration was 0.13 Â± 0.065 ng/mL.