dehydroepiandrosterone; prasterone (DHEA, Aslera, Intrarosa)
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Introduction
In females:
- derived largely from the adrenals (80%)
- 20% derived from ovaries
- theca cell systems is the source of ovarian androgens
30-50 mg/day is produced by zona fasciculata & zona reticularis of the adrenal cortex.
Quantitatively, the major secretory product of the adrenal gland. Adrenal production is regulated by ACTH. No known receptors for DHEA. Activity appears to be solely due to activity of its 2 metabolites, testosterone & estrone.
Concentrated in specific areas of the paleocortex in humans.
Pharmacology
prasterone. Tradenames: Aslera, Intrarosa
Indications
- treatment of lupus erythematosus (possibly)
- androgen replacement in women with adrenal insufficiency[5]
- metabolic syndrome X ?[6][7]
- dyspareunia in postmenopausal women (FDA-approved Nov 2016)[13]
- NO solid evidence to support popular uses:
- anti-aging factor
- appetite suppressant
- immune enhancer
- modulator of affect
- prevention of cardiovascular disease[8]
- no significant benefits on
- body composition, physical performance, insulin sensitivity, quality of life[10]
Dosage
Tabs: 200 mg (Aslera)
Once a day vaginal insert for dyspareunia (Intrarosa)
Pharmacokinetics
- inhibits cyt P450 3A4
- metabolized to testosterone & estradiol[6]
Monitor
Adverse effects
- concern derived from observation that DHEA is a precursor of testosterone & estradiol[6]
- women: weight gain, voice changes, facial hair, headaches
- males: gynecomastia, BPH,
- can lower HDL cholesterol
Drug interactions
- may increase serum levels of
- triazolam
- ketoconazole
- felodipine (other calcium channel blockers[12]?)
- simvastatin
- others
- sildenafil
Mechanism of action
- increases DHEA-sulfate levels
- may improve libido in women
- weak androgen
- activates PPAR-alpha (regulation of adipocyte physiology)
- may reduce abdominal fat (including visceral) in elderly [6][7]
- increases bone mineral density in elderly women with low pretreatment levels of DHEA[8]
More general terms
More specific terms
Additional terms
References
- ↑ Mayo Internal Medicine Board Review, 1998-99, Prakash UBS (ed) Lippincott-Raven, Philadelphia, 1998, pg 243
- ↑ Medical Knowledge Self Assessment Program (MKSAP) 11, American College of Physicians, Philadelphia 1998
- ↑ Prescriber's Letter 7(12):70 2000
- ↑ 4.0 4.1 Prescriber's Letter 8(8):48 2001
- ↑ 5.0 5.1 Solomon D. In: Intensive Course in Geriatric Medicine & Board Review, Marina Del Ray, CA, Sept 12-15, 2001
- ↑ 6.0 6.1 6.2 6.3 6.4 Prescriber's Letter 12(1): 2005 DHEA and Abdominal Obesity Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=210115&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 7.0 7.1 7.2 Villareal DT, Holloszy JO. Effect of DHEA on abdominal fat and insulin action in elderly women and men: a randomized controlled trial. JAMA. 2004 Nov 10;292(18):2243-8. PMID: https://www.ncbi.nlm.nih.gov/pubmed/15536111
- ↑ 8.0 8.1 8.2 Olech E & Merril JT, DHEA supplementation: The claims in perspective, Cleveland Clinic Journal of Medicine 72(11): 965, 2005
- ↑ 9.0 9.1 Nair KS et al DHEA in elderly women and DHEA or testosterone in elderly men. N Engl J Med 2006 Oct 19; 355:1647-59 PMID: https://www.ncbi.nlm.nih.gov/pubmed/17050889
Stewart PM. Aging and fountain-of-youth hormones. N Engl J Med 2006 Oct 19; 355:1724-6 PMID: https://www.ncbi.nlm.nih.gov/pubmed/17050897 - ↑ 10.0 10.1 Prescriber's Letter 13(12): 2006 Anti-aging effects of DHEA Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=221208&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Igwebuike A et al, Lack of dehydroepiandrosterone effect on a combined endurance and resistance exercise program in postmenopausal women. J Clin Endocrinol 2008, 93:534 PMID: https://www.ncbi.nlm.nih.gov/pubmed/18029465
- ↑ 12.0 12.1 Geriatric Review Syllabus, 8th edition (GRS8) Durso SC and Sullivan GN (eds) American Geriatrics Society, 2013
- ↑ 13.0 13.1 Brooks M FDA OKs Prasterone for Dyspareunia in Postmenopausal Women. Medscape. Nov 17, 2016 http://www.medscape.com/viewarticle/872022
FDA News Release. November 17, 2016 FDA approves Intrarosa for postmenopausal women experiencing pain during sex. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm529641.htm