Triptorelin: Difference between revisions

Revision as of 11:54, 9 February 2025

A synthetic hormone used in medicine

Triptorelin is a gonadotropin-releasing hormone agonist (GnRH agonist) used in the treatment of hormone-sensitive conditions. It is a synthetic decapeptide analog of the natural gonadotropin-releasing hormone (GnRH). Triptorelin is primarily used in the management of prostate cancer, endometriosis, and precocious puberty.

Medical uses

Triptorelin is used in the treatment of several medical conditions:

Prostate cancer: Triptorelin is used as part of androgen deprivation therapy to reduce the levels of testosterone in the body, which can help slow the growth of prostate cancer cells.

Endometriosis: By suppressing the production of estrogen, triptorelin can help alleviate the symptoms of endometriosis, a condition where tissue similar to the lining inside the uterus grows outside the uterus.

Precocious puberty: Triptorelin is used to delay early onset puberty in children by suppressing the release of gonadotropins.

Mechanism of action

Triptorelin acts as an agonist of the gonadotropin-releasing hormone receptor (GnRHR). Initially, it stimulates the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to a temporary increase in sex hormone levels. However, with continuous administration, it causes downregulation of the GnRHR, resulting in decreased production of LH and FSH, and subsequently, a reduction in sex hormone levels.

Side effects

Common side effects of triptorelin include hot flashes, decreased libido, and mood changes. Long-term use can lead to osteoporosis due to decreased bone density.

Chemistry

Triptorelin is a decapeptide with the sequence pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2. It is available in various formulations, including depot injections that provide sustained release of the drug over time.

History

Triptorelin was first synthesized in the 1970s and has been used clinically since the 1980s. It is marketed under various brand names, including Decapeptyl and Trelstar.

Related pages

References

@@ Line 1: / Line 1: @@
+{{Short description|A synthetic hormone used in medicine}}
+{{Use dmy dates|date=October 2023}}
-{{intro}}
+[[File:Triptorelin.svg|thumb|Chemical structure of triptorelin]]
-Triptorelin is a gonadotropin releasing hormone (GnRH) agonist that is a potent inhibitor of the synthesis of testosterone (in men) and estrogen (in women) and is used to treat advanced prostate cancer.
+'''Triptorelin''' is a [[gonadotropin-releasing hormone agonist]] (GnRH agonist) used in the treatment of hormone-sensitive conditions. It is a synthetic decapeptide analog of the natural [[gonadotropin-releasing hormone]] (GnRH). Triptorelin is primarily used in the management of [[prostate cancer]], [[endometriosis]], and [[precocious puberty]].
-{{livtox}}
+==Medical uses==
-Triptorelin 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]].
+Triptorelin is used in the treatment of several medical conditions:
-{{moa}}
-Triptorelin (trip" toe rel' in) is a decapeptide analogue of gonadotropin releasing hormone (GnRH) 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.  Triptorelin 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.  Triptorelin, alone or in combination with other antiandrogens, has been found to be palliative in advanced prostate cancer and as effective as surgical castration.
-{{fda}}
+* '''Prostate cancer''': Triptorelin is used as part of [[androgen deprivation therapy]] to reduce the levels of [[testosterone]] in the body, which can help slow the growth of prostate cancer cells.
-Triptorelin was approved for use in the United States for prostate cancer in 2000 and is still widely used, being considered a first line [[treatment]] of this hormone responsive malignancy.  Triptorelin is available generically and under the brand name Trelstar in an injectable suspension for intramuscular depot administration every 4 weeks (3.75 mg), 12 weeks (11.25 mg) or 24 weeks (22.5 mg).  Triptorelin and the other GnRH analogues cause a profound hypogonadism ("chemical castration").
-{{se}}
+* '''Endometriosis''': By suppressing the production of [[estrogen]], triptorelin can help alleviate the symptoms of endometriosis, a condition where tissue similar to the lining inside the uterus grows outside the uterus.
-The 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 can include immediate hypersensitivity reactions, pituitary apoplexy and, with long term use, weight gain, metabolic changes, diabetes and osteoporosis.
-{{cancer drugs}}
+* '''Precocious puberty''': Triptorelin is used to delay early onset puberty in children by suppressing the release of [[gonadotropins]].
-{{coststubd}}
+==Mechanism of action==
+Triptorelin acts as an agonist of the [[gonadotropin-releasing hormone receptor]] (GnRHR). Initially, it stimulates the release of [[luteinizing hormone]] (LH) and [[follicle-stimulating hormone]] (FSH), leading to a temporary increase in [[sex hormone]] levels. However, with continuous administration, it causes downregulation of the GnRHR, resulting in decreased production of LH and FSH, and subsequently, a reduction in sex hormone levels.
+==Side effects==
+Common side effects of triptorelin include hot flashes, decreased libido, and mood changes. Long-term use can lead to [[osteoporosis]] due to decreased [[bone density]].
+==Chemistry==
+Triptorelin is a decapeptide with the sequence pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2. It is available in various formulations, including depot injections that provide sustained release of the drug over time.
+==History==
+Triptorelin was first synthesized in the 1970s and has been used clinically since the 1980s. It is marketed under various brand names, including Decapeptyl and Trelstar.
+==Related pages==
+* [[Gonadotropin-releasing hormone]]
+* [[Prostate cancer]]
+* [[Endometriosis]]
+* [[Precocious puberty]]
+==References==
+{{Reflist}}
+[[Category:Hormones]]
+[[Category:Peptides]]
+[[Category:Prostate cancer treatments]]
+[[Category:Endometriosis]]
+[[Category:Puberty]]