Description

Simple

A medication used to treat early onset puberty in children and end-stage prostate cancer that is difficult to treat.

Clinical

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.

Overview

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.

Pharmacology

Indication

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.

Pharmacodynamic

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, t... Read more

Mechanism of action

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-s... Read more

Absorption

Following subcutaneous insertion of one histrelin implant as the product Vantas in advanced prostate cancer patients (n = 17), peak serum concentrations of 1.10 ± 0.375 ng/mL (mean ± SD) occurred at a median of 12 hours. Continuous subcutaneous release was evident, as serum levels were sustained... Read more

Protein binding

For the product Vantas, the fraction of drug unbound in plasma measured in vitro was 29.5% ± 8.9% (mean ± SD).

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 ± 7.86 L

Clearance

The apparent clearance following a 50 mg (as histrelin acetate) Vantas implant in 17 prostate cancer patients was 174 mL/min.

Half life

Information currently not available.

Route of elimination

Information currently not available.

Toxicity

Information currently not available.

Adverse Effects

Contraindications

  • Hypersensitivity:
    • Gonadotropin-Releasing Hormone
    • Gonadotropin-Releasing Hormone analogue
  • Regions: US
  • Regions: US
  • Patient Conditions:
      • Name: Pregnancy
      • Drugbank Id: DBCOND0018394

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
2,4-thiazolidinedione
The therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Histrelin.
Abexinostat
The risk or severity of QTc prolongation can be increased when Histrelin is combined with Abexinostat.
Acarbose
The therapeutic efficacy of Acarbose can be decreased when used in combination with Histrelin.
Acebutolol
The risk or severity of QTc prolongation can be increased when Histrelin is combined with Acebutolol.
Aceprometazine
The risk or severity of QTc prolongation can be increased when Histrelin is combined with Aceprometazine.
Acetohexamide
The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Histrelin.
Acetyldigoxin
The risk or severity of QTc prolongation can be increased when Histrelin is combined with Acetyldigoxin.
Acrivastine
The risk or severity of QTc prolongation can be increased when Histrelin is combined with Acrivastine.
Adenosine
The risk or severity of QTc prolongation can be increased when Histrelin is combined with Adenosine.
AICA ribonucleotide
The therapeutic efficacy of AICA ribonucleotide can be decreased when used in combination with Histrelin.
Ajmaline
The risk or severity of QTc prolongation can be increased when Ajmaline is combined with Histrelin.
Albiglutide
The therapeutic efficacy of Albiglutide can be decreased when used in combination with Histrelin.
Alfuzosin
The risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Histrelin.
Alimemazine
The risk or severity of QTc prolongation can be increased when Alimemazine is combined with Histrelin.
Allicin
The therapeutic efficacy of Allicin can be decreased when used in combination with Histrelin.
Alogliptin
The therapeutic efficacy of Alogliptin can be decreased when used in combination with Histrelin.
Amantadine
The risk or severity of QTc prolongation can be increased when Amantadine is combined with Histrelin.
AMG-222
The therapeutic efficacy of AMG-222 can be decreased when used in combination with Histrelin.
Amifampridine
The risk or severity of QTc prolongation can be increased when Histrelin is combined with Amifampridine.
Amiodarone
The risk or severity of QTc prolongation can be increased when Histrelin is combined with Amiodarone.
4 References
  1. 1 . Lewis KA, Eugster EA: Experience with the once-yearly histrelin (GnRHa) subcutaneous implant in the treatment of central precocious puberty. Drug Des Devel Ther. 2009 Sep 21;3:1-5.PubMed: 19920916
  2. 2 . Shore N, Cookson MS, Gittelman MC: Long-term efficacy and tolerability of once-yearly histrelin acetate subcutaneous implant in patients with advanced prostate cancer. BJU Int. 2012 Jan;109(2):226-32. doi: 10.1111/j.1464-410X.2011.10370.x. Epub 2011 Aug 18.PubMed: 21851539
  3. 3 . Djavan B, Schlegel P, Salomon G, Eckersberger E, Sadri H, Graefen M: Analysis of testosterone suppression in men receiving histrelin, a novel GnRH agonist for the treatment of prostate cancer. Can J Urol. 2010 Aug;17(4):5265-71.PubMed: 20735905
  4. 4 . Link Link