Leuprolide


Leuprolide

drugbox
IUPAC_name = "N"- [1- [1- [1- [1- [1- [1- [5-(diaminomethylideneamino)-1-
[2-(ethylcarbamoyl)pyrrolidin-1-yl] -1-oxo-pentan-2-
yl] carbamoyl] -3-methyl-butyl] carbamoyl] -3-methyl-
butyl] carbamoyl] -2-(4-hydroxyphenyl)ethyl]
carbamoyl] -2-hydroxy-ethyl] carbamoyl] -2-(1"H"-indol-3-
yl)ethyl] carbamoyl] -2-(3"H"-imidazol-4-yl)ethyl] -5-oxo-
pyrrolidine-2-carboxamide





width2 = 162
CAS_number = 53714-56-0
ATC_prefix = L02
ATC_suffix =AE02
PubChem = 441410
DrugBank = BTD00009
C = 59 | H = 84 | N = 16 | O = 12
molecular_weight = 1209.4 g/mol
elimination_half-life = 3 hours
excretion = Renal
pregnancy_category = X
legal_status = Rx-only
routes_of_administration = Implant / Injection

Leuprorelin (INN) or leuprolide acetate (USAN) is a gonadotropin-releasing hormone agonist (GnRH agonist).Proper Sequence: p-Glu-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt

Mode of action

By causing constant stimulation of the pituitary GnRH receptors, leuprolide initially causes stimulation (flare), but thereafter decreases pituitary secretion (downregulation) of the gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH).

Clinical usage

Like other GnRH agonists, leuprolide may be used in the treatment of: hormone-responsive cancers such as prostate cancer or breast cancer, estrogen-dependent conditions (such as endometriosis or uterine fibroids), to treat precocious puberty, and to control ovarian stimulation in In Vitro Fertilization (IVF). It is considered a possible treatment for paraphilias. [cite journal | author = Saleh F, Niel T, Fishman M | title = Treatment of paraphilia in young adults with leuprolide acetate: a preliminary case report series | journal = J Forensic Sci | volume = 49 | issue = 6 | pages = 1343–8 | year = 2004 | pmid = 15568711 | url = http://www.astm.org/cgi-bin/SoftCart.exe/JOURNALS/FORENSIC/PAGES/JFS2003035.htm?E+mystore | doi = 10.1520/JFS2003035]

A 2005 paper suggested it as a treatment for autism, [cite journal | author = Geier M, Geier D | title = The potential importance of steroids in the treatment of autistic spectrum disorders and other disorders involving mercury toxicity | journal = Med Hypotheses | volume = 64 | issue = 5 | pages = 946–54 | year = 2005 | pmid = 15780490 | doi = 10.1016/j.mehy.2004.11.018] the hypothetical method of action being the now defunct theory that autism is caused by mercury, with the additional assumption that mercury binds irreversibly to testosterone and therefore leuprolide can help cure autism by lowering the testosterone level and thereby the mercury level. [cite news |work=Slate |date=2007-05-28 |accessdate=2008-01-30 |url=http://www.slate.com/id/2166939/ |title= Thiomersal on trial: the theory that vaccines cause autism goes to court |author= Allen A] However, used on children or adolescents it could cause disastrous and irreversible damage to sexual functioning, and there is no scientifically valid or reliable research to show its effectiveness in treating autism. [cite web |url=http://www.researchautism.net/interventionitem.ikml?id=24 |accessdate=2007-08-19 |title= Testosterone regulation |date=2007-05-07 |publisher= Research Autism] Mark Geier, the proponent of the hypothesis, has frequently been barred from testifying in vaccine-autism related cases on the grounds of not being sufficiently expert in that particular issue. [" [http://www.ncmd.uscourts.gov/Opinions/Jul06/03cv669op.pdf John and Jane Doe v. Ortho-Clinical Diagnostics, Inc] ", US District Court for the Middle District of North Carolina, July 6, 2006] [" [http://www.casewatch.org/civil/geier.shtml Dr. Mark Geier Severely Criticized] ", Stephen Barrett, M.D., "Casewatch.org"]

Leuprolide is also under investigation for possible use in the treatment of mild to moderate Alzheimer's disease. [cite journal | author = Doraiswamy PM, Xiong GL. | title = Pharmacological strategies for the prevention of Alzheimer's disease | journal = Expert Opin Pharmacother | volume = 7 | issue = 1 | pages = 1–10 | year = 2006 pmid = 16370917 | doi = 10.1517/14656566.7.1.1 ]

Approvals

* Lupron Injection (5 mg/mL for daily subcutaneous injection) was first approved by the FDA for treatment of advanced prostate cancer on April 9, 1985.
* Lupron Depot (7.5 mg/vial for monthly intramuscular depot injection) was first approved by the FDA for palliative treatment of advanced prostate cancer on January 26, 1989, and subsequently in 22.5 mg/vial and 30 mg/vial for intramuscular depot injection every 3 and 4 months, respectively. 3.75 mg/vial and 11.25 mg/vial dosage forms were subsequently approved for subcutaneous depot injection every month and every 3 months, respectively for treatment of endometriosis or fibroids. 7.5 mg/vial, 11.25 mg/vial, and 15 mg/vial dosage forms were subsequently approved for subcutaneous depot injection for treatment of children with central precocious puberty.
* Viadur (72 mg yearly subcutaneous implant) was first approved by the FDA for palliative treatment of advanced prostate cancer on March 6, 2000.
* Eligard (7.5 mg for monthly subcutaneous depot injection) was first approved by the FDA for palliative treatment of advanced prostate cancer on January 24, 2002, and subsequently in 22.5 mg, 30 mg, and 45 mg doses for subcutaneous depot injection every 3, 4, and 6 months, respectively.

Leuprolide acetate is marketed by Bayer AG under the brand name Viadur, by Sanofi-Aventis under the brand name Eligard, and by TAP Pharmaceuticals under the brand name Lupron. It is available as a slow-release implant or subcutaneous/intramuscular injection.

In the UK, leuprorelin is marketed by Wyeth as Prostap SR(one month injection) and Prostap 3 (three month injection).

External links

* [http://www.tap.com/prd_ldep.asp Lupron Depot] (manufacturer's website)
* [http://pitap.abbott.com/showpi.asp?PI=luproninjection Lupron Injection] (package insert from abbott)
* [http://www.prescriptions.com.cn/catalog-L/Leuprolide_Acetate-description.htm Eligard] (professional information about the drug)
* [http://www.freewebs.com/adamshajnfeld/article.htm Reforming (purportedly) Non-Punitive Responses to Sexual Offending] (journal article discussing use of Lupron as a form of reforming sex offender law)
* [http://www.lupronvictimshub.com/ Lupron Victims Hub] website to serve consumers, healthcare workers & attorneys seeking information on Lupron (leuprolide) and its associated health risks.

References


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