Histrelin: Difference between revisions

Latest revision as of 11:08, 23 March 2025

A gonadotropin-releasing hormone agonist used in hormone therapy

Histrelin is a gonadotropin-releasing hormone (GnRH) agonist used primarily in the treatment of hormone-sensitive conditions such as prostate cancer and central precocious puberty. It is a synthetic analog of the naturally occurring GnRH, which plays a crucial role in the regulation of the pituitary gland and the release of gonadotropins.

Mechanism of Action[edit]

Histrelin functions by initially stimulating the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the pituitary gland. However, with continuous administration, it leads to downregulation of the GnRH receptors in the pituitary, resulting in decreased secretion of LH and FSH. This ultimately reduces the production of testosterone in males and estrogen in females, which is beneficial in conditions like prostate cancer and precocious puberty where hormone suppression is desired.

Medical Uses[edit]

Histrelin is primarily used in the following conditions:

Prostate Cancer[edit]

In the treatment of prostate cancer, histrelin is used to lower testosterone levels, which can help slow the growth of hormone-sensitive tumors. It is often part of androgen deprivation therapy (ADT).

Central Precocious Puberty[edit]

For children with central precocious puberty, histrelin helps delay the onset of puberty by suppressing the premature release of sex hormones. This can help in achieving a more typical timing of puberty and normal adult height.

Administration[edit]

Histrelin is administered as a subcutaneous implant, which provides a continuous release of the drug over a period of time, typically 12 months. This method of delivery ensures consistent hormone suppression without the need for daily medication.

Side Effects[edit]

Common side effects of histrelin include hot flashes, decreased libido, and mood changes. In children, it may cause temporary local reactions at the site of the implant. Long-term use can lead to decreased bone density, so monitoring is recommended.

Related Pages[edit]

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-{{intro}}
+{{Short description|A gonadotropin-releasing hormone agonist used in hormone therapy}}
-Histrelin is a gonadotropin releasing hormone (GnRH) agonist that is a potent inhibitor of production of testosterone (in men) and estrogen (in women) and is used predominantly to treat advanced [[prostate cancer]].
-{{livtox}}
-Histrelin is associated with a low rate of transient serum enzyme elevations during therapy, but has not been linked convincingly to cases of clinically apparent acute [[liver injury]].
-{{moa}}
+[[File:Histrelin.svg|thumb|right|Chemical structure of Histrelin]]
-Histrelin (his trel' in) is a nonapeptide analogue of gonadotropin releasing hormone that acts on the pituitary to cause the synthesis and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH), two gonadotropins that act on the male testes to stimulate the production of testosterone and on the female ovaries to induce synthesis of estrogen.  Histrelin and other GnRH agonists cause an initial surge of gonadotropin release, but then lead to down-regulation of their synthesis and secretion which results in a decline in testosterone and estrogen production.  Histrelin, alone or in combination with other antiandrogens, has been found to be palliative in advanced prostate cancer and as effective as surgical castration.
-{{fda}}
+'''Histrelin''' is a [[gonadotropin-releasing hormone]] (GnRH) [[agonist]] used primarily in the treatment of hormone-sensitive conditions such as [[prostate cancer]] and [[central precocious puberty]]. It is a synthetic analog of the naturally occurring GnRH, which plays a crucial role in the regulation of the [[pituitary gland]] and the release of [[gonadotropins]].
-Histrelin was approved for use in the United States in 1991 and as a once-yearly implant formulation in 2004.  The major indications for histrelin are advanced prostate cancer and precocious puberty.
-{{brand}}
+==Mechanism of Action==
-Histrelin is available generically and under the brand names Supprelin (for precocious puberty) and Vantas (for prostate cancer) in solution as implants of 50 mg, which are inserted subcutaneously in the inner aspect of the upper arm at 12 month intervals.
+Histrelin functions by initially stimulating the release of [[luteinizing hormone]] (LH) and [[follicle-stimulating hormone]] (FSH) from the pituitary gland. However, with continuous administration, it leads to downregulation of the GnRH receptors in the pituitary, resulting in decreased secretion of LH and FSH. This ultimately reduces the production of [[testosterone]] in males and [[estrogen]] in females, which is beneficial in conditions like prostate cancer and precocious puberty where hormone suppression is desired.
-{{se}}
+==Medical Uses==
-Histrelin and the other GnRH analogues cause a profound hypogonadism ("chemical castration") and its common [[side effects]] are typical of androgen deprivation, including hot flashes, loss of libido, erectile dysfunction, depression, [[nausea]], [[diarrhea]], weight gain and fluid retention.  Rare, but potentially severe adverse events include hypersensitivity reactions and transient tumor flare with the first injection.
+Histrelin is primarily used in the following conditions:
-{{cancer drugs}}
+===Prostate Cancer===
-{{coststubd}}
+In the treatment of [[prostate cancer]], histrelin is used to lower testosterone levels, which can help slow the growth of hormone-sensitive tumors. It is often part of [[androgen deprivation therapy]] (ADT).
-<gallery>
+===Central Precocious Puberty===
-File:Histrelin.svg|Histrelin
+For children with [[central precocious puberty]], histrelin helps delay the onset of puberty by suppressing the premature release of sex hormones. This can help in achieving a more typical timing of puberty and normal adult height.
-</gallery>
-<gallery>
+==Administration==
-File:Histrelin.svg|Histrelin
+Histrelin is administered as a subcutaneous implant, which provides a continuous release of the drug over a period of time, typically 12 months. This method of delivery ensures consistent hormone suppression without the need for daily medication.
-</gallery>
+==Side Effects==
+Common side effects of histrelin include hot flashes, decreased libido, and mood changes. In children, it may cause temporary local reactions at the site of the implant. Long-term use can lead to decreased bone density, so monitoring is recommended.
+==Related Pages==
+* [[Gonadotropin-releasing hormone]]
+* [[Prostate cancer]]
+* [[Central precocious puberty]]
+* [[Androgen deprivation therapy]]
+[[Category:Hormonal antineoplastic agents]]
+[[Category:GnRH agonists]]