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<!--Pharmacokinetic data-->
<!--Pharmacokinetic data-->
| bioavailability = 50%<ref name="CuppTracy2002" />
| bioavailability = 50%<ref name="CuppTracy2002">{{cite book|author1=Melanie Johns Cupp|author2=Timothy S. Tracy|title=Dietary Supplements: Toxicology and Clinical Pharmacology|url=https://books.google.com/books?id=vuqPBAAAQBAJ&pg=PA135|date=10 December 2002|publisher=Springer Science & Business Media|isbn=978-1-59259-303-3|pages=135–}}</ref>
| metabolism = [[Liver|Hepatic]]<ref name="CuppTracy2002" />
| metabolism = [[Liver|Hepatic]]<ref name="CuppTracy2002" />
| metabolites = • [[Androsterone]]<ref name="CuppTracy2002" /><br />• [[Etiocholanolone]]<ref name="CuppTracy2002" /><br />• [[Dehydroepiandrosterone sulfate|{{abbr|DHEA|Dehydroepiandrosterone}} sulfate]]<ref name="CuppTracy2002" /><br />• [[Androstenedione]]<ref name="CuppTracy2002" /><br />• [[Androstenediol]]<ref name="CuppTracy2002" /><br />• [[Testosterone]]<ref name="CuppTracy2002" /><br />• [[Androstanediol]]<ref name="CuppTracy2002" />
| metabolites = • [[Androsterone]]<ref name="CuppTracy2002" /><br />• [[Etiocholanolone]]<ref name="CuppTracy2002" /><br />• [[Dehydroepiandrosterone sulfate|{{abbr|DHEA|Dehydroepiandrosterone}} sulfate]]<ref name="CuppTracy2002" /><br />• [[Androstenedione]]<ref name="CuppTracy2002" /><br />• [[Androstenediol]]<ref name="CuppTracy2002" /><br />• [[Testosterone]]<ref name="CuppTracy2002" /><br />• [[Androstanediol]]<ref name="CuppTracy2002" />
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Prasterone is used medically as the C3β [[ester]]s [[prasterone enanthate]] and [[prasterone sodium sulfate]].<ref name="Elks2014" /> Another derivative is [[fluasterone]] (16α-fluoro-DHEA).<ref name="pmid15177053" />
Prasterone is used medically as the C3β [[ester]]s [[prasterone enanthate]] and [[prasterone sodium sulfate]].<ref name="Elks2014" /> Another derivative is [[fluasterone]] (16α-fluoro-DHEA).<ref name="pmid15177053" />

==History==
Prasterone was discovered, via [[wikt:isolation|isolation]] from [[urine]], by [[Adolf Butenandt]] and [[:de:Hans Dannenbaum|Hans Dannenbaum]] in 1934.<ref name="CuppTracy2002">{{cite book|author1=Melanie Johns Cupp|author2=Timothy S. Tracy|title=Dietary Supplements: Toxicology and Clinical Pharmacology|url=https://books.google.com/books?id=vuqPBAAAQBAJ&pg=PA123|date=10 December 2002|publisher=Springer Science & Business Media|isbn=978-1-59259-303-3|pages=123–147}}</ref> Subsequently, [[prasterone sulfate]] was isolated from urine in 1944.<ref name="CuppTracy2002" /> An association between [[DHEA sulfate]] levels and aging was reported by De Nee and Vermeulen in 1965, and this lead to numerous studies assessing the relationship between DHEA and DHEA sulfate levels and the aging process.<ref name="CuppTracy2002" />

''Prasterone'', the proposed {{abbrlink|INN|International Nonproprietary Name}} and recommended {{abbr|INN|International Nonproprietary Name}} of the medication, were published in 1970 and 1978, respectively.<ref name="WHOChronicle1970">https://mednet-communities.net/inn/db/media/docs/p-innlist23.pdf</ref><ref name="WHOChronicle1978">https://mednet-communities.net/inn/db/media/docs/r-innlist18.pdf</ref> The combination of 4&nbsp;mg [[estradiol valerate]] and 200&nbsp;mg [[prasterone enanthate]] in an oil solution was introduced for use in menopausal hormone therapy by intramusuclar injection under the brand name Gynodian Depot in [[Europe]] by 1978.<ref name="pmid25506">{{cite journal | vauthors = Hoyme U, Baumueller A, Madsen PO | title = The influence of pH on antimicrobial substances in canine vaginal and urethral secretions | journal = Urol. Res. | volume = 6 | issue = 1 | pages = 35–42 | date = 1978 | pmid = 25506 | doi = | url = }}</ref><ref name="KoperaDhont1979">{{cite journal|last1=Kopera|first1=H.|last2=Dhont|first2=M.|last3=Dienstl|first3=F.|last4=Gambrell|first4=R. D.|last5=Gordan|first5=G. S.|last6=Heidenreich|first6=J.|last7=Lachnit-Fixon|first7=U.|last8=Lauritzen|first8=C.|last9=Lebech|first9=P. E.|last10=Sitruk-Ware|first10=R. L.|last11=Utian|first11=W. H.|title=Effects, side-effects, and dosage schemes of various sex hormones in the peri- and post-menopause|year=1979|pages=43–67|doi=10.1007/978-94-011-9720-5_6}}</ref><ref name="pmid6453267">{{cite journal | vauthors = Mattson LA, Cullberg G, Tangkeo P, Zador G, Samsioe G | title = Administration of dehydroepiandrosterone enanthate to oophorectomized women--effects on sex hormones and lipid metabolism | journal = Maturitas | volume = 2 | issue = 4 | pages = 301–9 | date = December 1980 | pmid = 6453267 | doi = | url = }}</ref><ref name="Muller1998">{{cite book|author=Muller|title=European Drug Index: European Drug Registrations, Fourth Edition|url=https://books.google.com/books?id=2HBPHmclMWIC&pg=PA566|date=19 June 1998|publisher=CRC Press|isbn=978-3-7692-2114-5|pages=566–}}</ref> In the early 1980s, prasterone was described as a miracle drug, with supposed anti-aging, anti-obesity, and anti-cancer benefits, and was available and widely sold [[over-the-counter]] in the [[United States]], primarily as a [[weight loss]] supplement, at this time.<ref name="CuppTracy2002" /><ref name="Randolph2010">{{cite book|author1=C.W. Randolph, Jr., M.D.|author2=Genie James|title=From Hormone Hell to Hormone Well: Straight Talk Women (and Men) Need to Know to Save Their Sanity, Health, and—Quite Possibly—Their Lives|url=https://books.google.com/books?id=dmGhAgAAQBAJ&pg=PA72|date=1 January 2010|publisher=Health Communications, Incorporated|isbn=978-0-7573-9759-2|pages=72–}}</ref> This continued until 1985, when the marketing of prasterone was banned by the [[Food and Drug Administration]] (FDA) due to the long-term risks of the compound being unknown.<ref name="CuppTracy2002" /><ref name="Randolph2010" /> Subsequently, prasterone became available over-the-counter in the United States once again as a dietary supplement following passage of the [[Dietary Supplement Health and Education Act of 1994]].<ref name="CuppTracy2002" /> Conversely, it remained banned in [[Canada]], the [[United Kingdom]], [[Australia]], and [[New Zealand]].<ref name="CuppTracy2002" /><ref name="DunfordDoyle2014">{{cite book|author1=Marie Dunford|author2=J. Andrew Doyle|title=Nutrition for Sport and Exercise|url=https://books.google.com/books?id=xRAeCgAAQBAJ&pg=PA442|date=7 February 2014|publisher=Cengage Learning|isbn=978-1-285-75249-5|pages=442–}}</ref>

In 2001, Genelabs submitted a [[New Drug Application]] of prasterone for the treatment of [[systemic lupus erythematosus]] (SLE) to the FDA.<ref name="CuppTracy2002" /><ref name="AdisInsight-3" /> It had the tentative brand names included Anastar, Aslera, and Prestara.<ref name="CuppTracy2002" /><ref name="BlauSchultz2009">{{cite book|author1=Sheldon Blau|author2=Dodi Schultz|title=Living With Lupus: The Complete Guide, 2nd Edition|url=https://books.google.com/books?id=ImpGzazIYN8C&pg=PT138|date=5 March 2009|publisher=Da Capo Press|isbn=978-0-7867-2985-2|pages=138–}}</ref><ref name="AdisInsight-3" /> However, this application was not approved, and while development of prasterone for SLE in both the United States and Europe continued until up to 2010, the medication was ultimately never approved for the treatment of this condition.<ref name="CuppTracy2002" /> In 2016, the [[Food and Drug Administration]] (FDA) in the [[United States]] approved prasterone in an intravaginal gel formulation for the treatment of painful sexual intercourse due to vulvovaginal atrophy under the brand name Intrarosa.<ref name="Voelker2017">{{cite journal|last1=Voelker|first1=Rebecca|title=Relief for Painful Intercourse|journal=JAMA|volume=317|issue=1|year=2017|pages=18|issn=0098-7484|doi=10.1001/jama.2016.19077}}</ref><ref name="JAMA2017">{{cite journal|title=Prasterone (Intrarosa) for Dyspareunia|journal=JAMA|volume=318|issue=16|year=2017|pages=1607|issn=0098-7484|doi=10.1001/jama.2017.14981}}</ref> This was the first prasterone-containing medication to be approved by the FDA in this country.<ref name="Voelker2017" />


==Society and culture==
==Society and culture==
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===Lupus===
===Lupus===
There is some evidence of short-term benefit in those with [[systemic lupus erythematosus]] but little evidence of long-term benefit or safety.<ref name="pmid17943841">{{cite journal|last=Crosbie|first=D|author2=Black, C|author3=McIntyre, L|author4=Royle, PL|author5=Thomas, S|title=Dehydroepiandrosterone for systemic lupus erythematosus|journal=Cochrane Database of Systematic Reviews|date=Oct 17, 2007|issue=4|page=CD005114|pmid=17943841|doi=10.1002/14651858.CD005114.pub2|editor1-last=Crosbie|editor1-first=David}}</ref> Prasterone was under development for the treatment of systemic lupus erythematosus in the [[United States]] and [[Europe]] in the late 2000s and reached [[Phases of clinical research#Phase III|phase III]] [[clinical trial]]s and [[New Drug Application|preregistration]] for this indication, respectively, but ultimately development was not continued past 2010.<ref name="AdisInsight-3">http://adisinsight.springer.com/drugs/800013229</ref>
There is some evidence of short-term benefit in those with SLE but little evidence of long-term benefit or safety.<ref name="pmid17943841">{{cite journal|last=Crosbie|first=D|author2=Black, C|author3=McIntyre, L|author4=Royle, PL|author5=Thomas, S|title=Dehydroepiandrosterone for systemic lupus erythematosus|journal=Cochrane Database of Systematic Reviews|date=Oct 17, 2007|issue=4|page=CD005114|pmid=17943841|doi=10.1002/14651858.CD005114.pub2|editor1-last=Crosbie|editor1-first=David}}</ref> Prasterone was under development for the treatment of systemic lupus erythematosus in the [[United States]] and [[Europe]] in the 1990s and 2000s and reached [[Phases of clinical research#Phase III|phase III]] [[clinical trial]]s and [[New Drug Application|preregistration]] for this indication, respectively, but ultimately development was not continued past 2010.<ref name="CuppTracy2002" /><ref name="AdisInsight-3">http://adisinsight.springer.com/drugs/800013229</ref>


===Memory===
===Memory===
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* {{cite journal | vauthors = Keppel Hesselink JM | title = [Prasterone (dihydroepiandrosterone): a modern source of eternal youth?] | language = Dutch; Flemish | journal = Ned Tijdschr Geneeskd | volume = 141 | issue = 51 | pages = 2484–7 | date = December 1997 | pmid = 9555138 | doi = | url = }}
* {{cite journal | vauthors = Keppel Hesselink JM | title = [Prasterone (dihydroepiandrosterone): a modern source of eternal youth?] | language = Dutch; Flemish | journal = Ned Tijdschr Geneeskd | volume = 141 | issue = 51 | pages = 2484–7 | date = December 1997 | pmid = 9555138 | doi = | url = }}
* {{cite journal | vauthors = Zelissen PM, Thijssen JH | title = [Role of prasterone (dehydroepiandrosterone) in substitution therapy for adrenocortical insufficiency] | language = Dutch; Flemish | journal = Ned Tijdschr Geneeskd | volume = 145 | issue = 42 | pages = 2018–22 | date = October 2001 | pmid = 11695098 | doi = | url = }}
* {{cite journal | vauthors = Zelissen PM, Thijssen JH | title = [Role of prasterone (dehydroepiandrosterone) in substitution therapy for adrenocortical insufficiency] | language = Dutch; Flemish | journal = Ned Tijdschr Geneeskd | volume = 145 | issue = 42 | pages = 2018–22 | date = October 2001 | pmid = 11695098 | doi = | url = }}
* {{cite journal|last1=Pope|first1=JE|last2=Cupp|first2=MJ|last3=Tracy|first3=TS|title=Dehydroepiandrosterone (DHEA) (Prasterone)|work=Dietary Supplements|year=2003|pages=123–147|publisher=Humana Press|location=Totowa, NJ|doi=10.1007/978-1-59259-303-3_8|url=https://books.google.com/books?id=vuqPBAAAQBAJ&pg=PA123}}
* {{cite journal | vauthors = Kocis P | title = Prasterone | journal = Am J Health Syst Pharm | volume = 63 | issue = 22 | pages = 2201–10 | date = November 2006 | pmid = 17090740 | doi = 10.2146/ajhp060100 | url = }}
* {{cite journal | vauthors = Kocis P | title = Prasterone | journal = Am J Health Syst Pharm | volume = 63 | issue = 22 | pages = 2201–10 | date = November 2006 | pmid = 17090740 | doi = 10.2146/ajhp060100 | url = }}
* {{cite journal | vauthors = Mendivil Dacal JM, Borges VM | title = [Dehydroepiandrosterone (DHEA), review of its efficiency in the managing of the libido decrease and other symtoms of aging] | language = Spanish; Castilian | journal = Actas Urol Esp | volume = 33 | issue = 4 | pages = 390–401 | date = April 2009 | pmid = 19579890 | doi = 10.4321/s0210-48062009000400009| url = }}
* {{cite journal | vauthors = Mendivil Dacal JM, Borges VM | title = [Dehydroepiandrosterone (DHEA), review of its efficiency in the managing of the libido decrease and other symtoms of aging] | language = Spanish; Castilian | journal = Actas Urol Esp | volume = 33 | issue = 4 | pages = 390–401 | date = April 2009 | pmid = 19579890 | doi = 10.4321/s0210-48062009000400009| url = }}

Revision as of 04:51, 4 March 2018

This article is about DHEA as a medication or supplement. For as a natural hormone, see DHEA.
Prasterone
Clinical data
Trade namesAstenile, Cetovister, 17-Chetovis, Dastonil S, Deandros, Diandrone, Fidelin™, Hormobago, 17-Hormoforin, Intrarosa, 17-Ketovis, Mentalormon, Psicosterone[1]
Other namesEL-10; GL-701; KYH-3102; Androst-5-en-3β-ol-17-one; 3β-Hydroxyandrost-5-en-17-one; 5,6-Didehydroepiandrosterone;[2] Dehydroisoepiandrosterone[1]
Routes of
administration		By mouth, vaginal (insert), intramuscular injection (as prasterone enanthate), injection (as prasterone sodium sulfate)
Drug classAndrogen; Anabolic steroid; Estrogen; Neurosteroid
ATCvet code
Legal status
Legal status
Pharmacokinetic data
Bioavailability50%[3]
MetabolismHepatic[3]
Metabolites• Androsterone[3]
• Etiocholanolone[3]
• DHEA sulfate[3]
• Androstenedione[3]
• Androstenediol[3]
• Testosterone[3]
• Androstanediol[3]
Elimination half-lifeDHEA: 25 minutes[4]
DHEA-S: 11 hours[4]
ExcretionUrine
Identifiers
  • (3S,8R,9S,10R,13S,14S)-3-hydroxy-10,13-dimethyl-1,2,3,4,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-17-one; (1S,2R,5S,10R,11S,15S)-5-Hydroxy-2,15-dimethyltetracyclo[8.7.0.02,7.011,15]heptadec-7-en-14-one
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
ChEBI
ChEMBL
Chemical and physical data
FormulaC19H28O2
Molar mass288.424 g/mol g·mol−1
3D model (JSmol)
Melting point148.5 °C (299.3 °F)
  • O=C3[C@]2(CC[C@@H]1[C@@]4(C(=C/C[C@H]1[C@@H]2CC3)\C[C@@H](O)CC4)C)C
  • InChI=1S/C19H28O2/c1-18-9-7-13(20)11-12(18)3-4-14-15-5-6-17(21)19(15,2)10-8-16(14)18/h3,13-16,20H,4-11H2,1-2H3/t13-,14-,15-,16-,18-,19-/m0/s1 checkY
  • Key:FMGSKLZLMKYGDP-USOAJAOKSA-N checkY
  (verify)

Prasterone, also known as dehydroepiandrosterone (DHEA), is a naturally occurring steroid which is used as a supplement and medication. It is an androstane derivative and a precursor of steroid hormones like testosterone and estradiol. Prasterone has weak androgenic activity, weak estrogenic activity, and neurosteroid activity, and acts as a prohormone of androgens and estrogens depending on its dosage and route of administration. As a medication, prasterone may be used to restore or increase DHEA levels in deficiency or old age, for menopausal women as a weak androgen or to treat vaginal atrophy, and, as prasterone sulfate, for cervical dilation during childbirth.

Medical uses

Deficiency

DHEA and DHEA sulfate are produced by the adrenal glands. In people with adrenal insufficiency such as in Addison's disease, there may be deficiency of DHEA and DHEA sulfate. In addition, levels of these steroids decrease throughout life and are 70 to 80% lower in the elderly relative to levels in young adults. Prasterone can be used to increase DHEA and DHEA sulfate levels in adrenal insufficiency and older age. Although there is deficiency of these steroids in such individuals, clinical benefits of supplementation, if any, are uncertain, and there is insufficient evidence at present to support the use of prasterone for such purposes.[5][6]

In clinical studies of prasterone supplementation, dosages have ranged from 20 to 1,600 mg per day.[7] In people with adrenal insufficiency, oral dosages of 20 to 50 mg/day prasterone have been found to restore DHEA and DHEA-S levels to normal ranges seen in healthy young adults.[7] Conversely, oral dosages of 100 to 200 mg/day prasterone have been found to result in supraphysiological levels of DHEA and DHEA-S.[7]

Menopause

See also: Prasterone enanthate

Prasterone is sometimes used as an androgen in menopausal hormone therapy.[8] In addition to prasterone itself, a long-lasting ester prodrug of prasterone, prasterone enanthate, is used in combination with estradiol valerate for the treatment of menopausal symptoms under the brand name Gynodian Depot.[9][10][11][12][13][14]

At a high dosage of 1,600 mg/day orally for 4 weeks, treatment of postmenopausal women with prasterone has been found to increase serum levels of DHEA by 15-fold, testosterone by 9-fold, DHEA-S, androstenedione (A4), and dihydrotestosterone (DHT) all by 20-fold, and estrone and estradiol both by 2-fold.[15][16]

Vaginal atrophy

Prasterone, under the brand name Intrarosa, is approved in the United States in a vaginal insert formulation for the treatment of atrophic vaginitis.[17][18] The mechanism of action of prasterone for this indication is unknown, though it may involve local metabolism of prasterone into androgens and estrogens.[18]

Childbirth

See also: Prasterone sodium sulfate

As the sodium salt of prasterone sulfate (brand names Astenile, Mylis, Teloin),[19][20] an ester prodrug of prasterone, prasterone is used in Japan as an injection for the treatment of insufficient cervical ripening and cervical dilation during childbirth.[1][21][22][23][24][25][26]

Side effects

Prasterone is produced naturally in the human body, but the long-term effects of its use are largely unknown.[27][28] In the short term, several studies have noted few adverse effects. In a study by Chang et al., prasterone was administered at a dose of 200 mg/day for 24 weeks with slight androgenic effects noted.[29] Another study utilized a dose up to 400 mg/day for 8 weeks with few adverse events reported.[30] A longer term study followed patients dosed with 50 mg of prasterone for 12 months with the number and severity of side effects reported to be small.[31] Another study delivered a dose of 50 mg of prasterone for 10 months with no serious adverse events reported.[32]

As a hormone precursor, there have been reports of side effects possibly caused by the hormone metabolites of prasterone.[28][33]

It is not known whether prasterone is safe for long-term use. Some researchers believe prasterone supplements might actually raise the risk of breast cancer, prostate cancer, heart disease, diabetes,[28] and stroke. Prasterone may stimulate tumor growth in types of cancer that are sensitive to hormones, such as some types of breast, uterine, and prostate cancer.[28] Prasterone may increase prostate swelling in men with benign prostatic hyperplasia (BPH), an enlarged prostate gland.[27]

Prasterone is a steroid hormone. High doses may cause aggressiveness, irritability, trouble sleeping, and the growth of body or facial hair on women.[27] It also may stop menstruation and lower the levels of HDL ("good" cholesterol), which could raise the risk of heart disease.[27] Other reported side effects include acne, heart rhythm problems, liver problems, hair loss (from the scalp), and oily skin. It may also alter the body's regulation of blood sugar.[27]

Prasterone may promote tamoxifen resistance.[27] Patients on hormone replacement therapy may have more estrogen-related side effects when taking prasterone. This supplement may also interfere with other medicines, and potential interactions between it and drugs and herbs are possible.[27]

Prasterone is possibly unsafe for individuals experiencing pregnancy, breastfeeding, hormone sensitive conditions, liver problems, diabetes, depression or mood disorders, polycystic ovarian syndrome (PCOS), or cholesterol problems.[34]

Chemistry

See also: List of androgens/anabolic steroids

Prasterone, also known as androst-5-en-3β-ol-17-one, is a naturally occurring androstane steroid and a 17-ketosteroid. It is closely related structurally to androstenediol (androst-5-ene-3β,17β-diol), androstenedione (androst-4-ene-3,17-dione), and testosterone (androst-4-en-17β-ol-3-one). Prasterone is the 5-dehydro analogue of epiandrosterone (5α-androstan-3β-ol-17-one) and is also known as 5-dehydroepiandrosterone or as δ5-epiandrosterone.

Derivatives

See also: List of androgen esters § Esters of other natural AAS

Prasterone is used medically as the C3β esters prasterone enanthate and prasterone sodium sulfate.[1] Another derivative is fluasterone (16α-fluoro-DHEA).[15]

History

Prasterone was discovered, via isolation from urine, by Adolf Butenandt and Hans Dannenbaum in 1934.[3] Subsequently, prasterone sulfate was isolated from urine in 1944.[3] An association between DHEA sulfate levels and aging was reported by De Nee and Vermeulen in 1965, and this lead to numerous studies assessing the relationship between DHEA and DHEA sulfate levels and the aging process.[3]

Prasterone, the proposed INNTooltip International Nonproprietary Name and recommended INN of the medication, were published in 1970 and 1978, respectively.[35][36] The combination of 4 mg estradiol valerate and 200 mg prasterone enanthate in an oil solution was introduced for use in menopausal hormone therapy by intramusuclar injection under the brand name Gynodian Depot in Europe by 1978.[37][38][39][40] In the early 1980s, prasterone was described as a miracle drug, with supposed anti-aging, anti-obesity, and anti-cancer benefits, and was available and widely sold over-the-counter in the United States, primarily as a weight loss supplement, at this time.[3][41] This continued until 1985, when the marketing of prasterone was banned by the Food and Drug Administration (FDA) due to the long-term risks of the compound being unknown.[3][41] Subsequently, prasterone became available over-the-counter in the United States once again as a dietary supplement following passage of the Dietary Supplement Health and Education Act of 1994.[3] Conversely, it remained banned in Canada, the United Kingdom, Australia, and New Zealand.[3][42]

In 2001, Genelabs submitted a New Drug Application of prasterone for the treatment of systemic lupus erythematosus (SLE) to the FDA.[3][43] It had the tentative brand names included Anastar, Aslera, and Prestara.[3][44][43] However, this application was not approved, and while development of prasterone for SLE in both the United States and Europe continued until up to 2010, the medication was ultimately never approved for the treatment of this condition.[3] In 2016, the Food and Drug Administration (FDA) in the United States approved prasterone in an intravaginal gel formulation for the treatment of painful sexual intercourse due to vulvovaginal atrophy under the brand name Intrarosa.[45][46] This was the first prasterone-containing medication to be approved by the FDA in this country.[45]

Society and culture

Generic names

Prasterone is the generic name of DHEA in English and Italian and its INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name, and DCITTooltip Denominazione Comune Italiana,[1][47][48][49] while its generic name is prasteronum in Latin, prastérone in French and its DCFTooltip Dénomination Commune Française, and prasteron in German.[48]

Marketing

In the United States, prasterone or prasterone sulfate have been advertised, under the names DHEA and DHEA-S, with claims that they may be beneficial for a wide variety of ailments. Prasterone and prasterone sulfate are readily available in the United States, where they are sold as over-the-counter dietary supplements.[50]

Regulation

United States

Prasterone is legal to sell in the United States as a dietary supplement. It is currently grandfathered in as an "Old Dietary Ingredient" being on sale prior to 1994. Prasterone is specifically exempted from the Anabolic Steroid Control Act of 1990 and 2004.[51] It is banned from use in athletic competition.

Canada

In Canada, prasterone is a Controlled Drug listed under Section 23 of Schedule IV of the Controlled Drugs and Substances Act[52] and as such is available by prescription only.

Australia

In Australia, a prescription is required to buy prasterone, where it is also comparatively expensive compared to off-the-shelf purchases in US supplement shops. Australian customs classify prasterone as an "anabolic steroid[s] or precursor[s]" and, as such, it is only possible to carry prasterone into the country through customs if one possesses an import permit which may be obtained if one has a valid prescription for the hormone.[53]

United Kingdom

Prasterone is listed as an anabolic steroid and is thus a class C controlled drug.

Sports and athletics

Prasterone is a prohibited substance under the World Anti-Doping Code of the World Anti-Doping Agency,[54] which manages drug testing for Olympics and other sports. In January 2011, NBA player O. J. Mayo was given a 10-game suspension after testing positive for prasterone. Mayo termed his use of prasterone as "an honest mistake," saying the prasterone was in an over-the-counter supplement and that he was unaware the supplement was banned by the NBA.[55] Mayo is the seventh player to test positive for performance-enhancing drugs since the league began testing in 1999. Rashard Lewis, then with the Orlando Magic, tested positive for prasterone and was suspended 10 games before the start of the 2009-10 season.[56] 2008 Olympic 400 meter champion Lashawn Merritt has also tested positive for prasterone and was banned from the sport for 21 months.[57] Yulia Efimova, who holds the world record pace for both the 50-meter and 200-meter breaststroke, and won the bronze medal in the 200-meter breaststroke in the 2012 London Olympic Games, tested positive for prasterone in an out-of-competition doping test.[58] In 2016 MMA fighter Fabio Maldonado revealed he was taking prasterone during his time with the UFC.[59]

Research

Anabolic uses

Body composition

A meta-analysis of intervention studies shows that prasterone supplementation in elderly men can induce a small but significant positive effect on body composition that is strictly dependent on prasterone conversion into its bioactive metabolites such as androgens or estrogens.[60]

Cancer

There is no evidence prasterone is of benefit in treating or preventing cancer.[27] Although prasterone is postulated as an inhibitor towards glucose-6-phosphate dehydrogenase (G6PD) and suppresses leukemia cell proliferation in vitro,[61][62] Prasterone may enhance G6PD mRNA expression, confounding its inhibitory effects.[63]

Cardiovascular disease

A review in 2003 found the then-extant evidence sufficient to suggest that low serum levels of DHEA-S may be associated with coronary heart disease in men, but insufficient to determine whether prasterone supplementation would have any cardiovascular benefit.[64]

Drug addiction

A double-blind, placebo-controlled study in adult polydrug users in a detoxification program showed the efficacy of prasterone treatment combined with psychosocial enrichment and after-care. Prasterone administration positively affected decision-making, mood and well-being as early as one month into treatment, and had a long-lasting preventive effect on relapse to drug use. In a 16-month follow-up, relapse rates of prasterone-treated subjects were only 11.5%. No adverse symptoms were found. These findings demonstrate the long-term effect of prasterone on drug relapse.[65]

Lupus

There is some evidence of short-term benefit in those with SLE but little evidence of long-term benefit or safety.[66] Prasterone was under development for the treatment of systemic lupus erythematosus in the United States and Europe in the 1990s and 2000s and reached phase III clinical trials and preregistration for this indication, respectively, but ultimately development was not continued past 2010.[3][43]

Memory

Prasterone supplementation has not been found to be useful for memory function in normal middle aged or older adults.[67] It has been studied as a treatment for Alzheimer's disease, but there is no evidence that it is effective.[68]

Mood

A few small, short term clinical studies have found that prasterone improves mood but its long-term efficacy and safety, and how it compares to antidepressants, was unknown as of 2015.[69][70]

Strength

Evidence is inconclusive in regards to the effect of prasterone on strength in the elderly.[71]

In middle-aged men, no significant effect of prasterone supplementation on lean body mass, strength, or testosterone levels was found in a randomized placebo-controlled trial.[72]

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Further reading

External links


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