User:Mr. Ibrahem/Eplerenone

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Mr. Ibrahem/Eplerenone
Clinical data
Pronunciation/ɛpˈlɛrənoʊn/
Trade namesInspra, Epnone, Dosterep, others
Other namesSC-66110; CGP-30083; 9-11α-Epoxymexrenone; 9,11α-Epoxy-7α-methoxycarbonyl-3-oxo-17α-pregn-4-ene-21,17-carbolactone
AHFS/Drugs.comMonograph
MedlinePlusa603004
Pregnancy
category
  • AU: B3
Routes of
administration		By mouth (tablets)
Drug classAldosterone antagonist, potassium-sparing diuretic[1]
Legal status
Legal status
Pharmacokinetic data
Bioavailability~70%[2]
Protein binding~50% (33–60%) (primarily to α1-acid glycoprotein)[2][3]
MetabolismLiver (CYP3A4)[2][3]
Metabolites6β-OH-EPL, 6β,21-OH-EPL, 21-OH-EPL, 3α,6β-OH-EPL[2] (All inactive)[2]
Onset of actionWithin 2 weeks[4]
Elimination half-life4–6 hours[5]
ExcretionUrine (67%), feces (32%)[6]
Identifiers
  • methyl (4aS,4bR,5aR,6aS,7R,9aS,9bR,10R)-4a,6a-dimethyl-2,5'-dioxo-2,4,4',4a,5',5a,6,6a,8,9,9a,9b,10,11-tetradecahydro-3H,3'H-spiro[cyclopenta[7,8]phenanthro[4b,5-b]oxirene-7,2'-furan]-10-carboxylate
Chemical and physical data
FormulaC24H30O6
Molar mass414.498 g·mol−1
3D model (JSmol)
  • COC(=O)[C@@H]4C\C1=C\C(=O)CC[C@]1(C)[C@@]65O[C@@H]6C[C@@]3(C)[C@@H](CC[C@]23CCC(=O)O2)[C@H]45
  • InChI=1S/C24H30O6/c1-21-7-4-14(25)10-13(21)11-15(20(27)28-3)19-16-5-8-23(9-6-18(26)30-23)22(16,2)12-17-24(19,21)29-17/h10,15-17,19H,4-9,11-12H2,1-3H3/t15-,16+,17-,19+,21+,22+,23-,24-/m1/s1 checkY
  • Key:JUKPWJGBANNWMW-VWBFHTRKSA-N checkY
  (verify)

Eplerenone, sold under the brand name Inspra among others, is a medication used to treat heart failure and high blood pressure.[4] For high blood pressure it is a second line treatment.[4] It is taken by mouth.[4] Effects generally occur within 2 weeks.[4]

Common side effects include high blood potassium, diarrhea, breast enlargement, and abdominal pain.[4] Other side effects may include arrhythmias, angioedema, and low blood pressure with standing.[1] It is a aldosterone antagonist and a potassium-sparing diuretic.[1]

Eplerenone was approved for medical use in the United States in 2002.[4] It is available as a generic medication.[1] In the United Kingdom a month of medication costs the NHS about £25.[1] This amount in the United States costs about 19 USD as of 2021.[7]

References[edit]

  1. ^ a b c d e BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 206. ISBN 978-0-85711-369-6.{{cite book}}: CS1 maint: date format (link)
  2. ^ a b c d e Lemke TL, Williams DA (24 January 2012). Foye's Principles of Medicinal Chemistry. Lippincott Williams & Wilkins. pp. 743–. ISBN 978-1-60913-345-0. Archived from the original on 1 August 2020. Retrieved 6 July 2021.
  3. ^ a b Sica DA (January 2005). "Pharmacokinetics and pharmacodynamics of mineralocorticoid blocking agents and their effects on potassium homeostasis". Heart Failure Reviews. 10 (1): 23–9. doi:10.1007/s10741-005-2345-1. PMID 15947888. S2CID 21437788.
  4. ^ a b c d e f g h i "Eplerenone Monograph for Professionals". Drugs.com. Archived from the original on 19 August 2020. Retrieved 23 July 2021.
  5. ^ Struthers A, Krum H, Williams GH (April 2008). "A comparison of the aldosterone-blocking agents eplerenone and spironolactone". Clinical Cardiology. 31 (4): 153–8. doi:10.1002/clc.20324. PMC 6652937. PMID 18404673.
  6. ^ Frishman WH, Cheng-Lai A, Nawarskas J (4 January 2005). Current Cardiovascular Drugs. Springer Science & Business Media. pp. 246–. ISBN 978-1-57340-221-7. Archived from the original on 1 August 2020. Retrieved 6 July 2021.
  7. ^ "Eplerenone Prices, Coupons & Savings Tips - GoodRx". GoodRx. Archived from the original on 17 January 2021. Retrieved 23 July 2021.
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