User:Mr. Ibrahem/Apremilast

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Mr. Ibrahem/Apremilast
Clinical data
Pronunciation/əˈprɛmɪlæst/ ə-PREM-i-last
Trade namesOtezla, Aplex, others
Other namesCC-10004
AHFS/Drugs.comMonograph
MedlinePlusa614022
License data
Pregnancy
category
  • AU: B3
Routes of
administration		By mouth (tablets)
Drug classPhosphodiesterase 4 (PDE4) inhibitor[1]
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)[2]
  • US: ℞-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability73%;[3] Tmax = ~2.5 hours
Protein bindingc. 68%[3]
MetabolismLiver (CYP3A4, with minor contributions from CYP2A6, CYP1A2)[3]
MetabolitesO-desmethylapremilast glucuronide (and others)[4]
Elimination half-life6–9 hours[3]
ExcretionUrine (58%), faeces (39%)[3]
Identifiers
  • N-{2-[(1S)-1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl}acetamide
Chemical and physical data
FormulaC22H24N2O7S
Molar mass460.50 g·mol−1
3D model (JSmol)
  • O=S(=O)(C)C[C@H](c1ccc(OC)c(OCC)c1)N3C(=O)c2cccc(c2C3=O)NC(=O)C
  • InChI=1S/C22H24N2O7S/c1-5-31-19-11-14(9-10-18(19)30-3)17(12-32(4,28)29)24-21(26)15-7-6-8-16(23-13(2)25)20(15)22(24)27/h6-11,17H,5,12H2,1-4H3,(H,23,25)/t17-/m1/s1
  • Key:IMOZEMNVLZVGJZ-QGZVFWFLSA-N

Apremilast, sold under the brand name Otezla among others, is a medication used to treat plaque psoriasis, psoriatic arthritis, and Behçet's disease.[1][5] It is used when other treatments are not effective.[1] It is taken by mouth.[7]

Common side effects include diarrhea, nausea, the common cold, and headaches.[1] Other side effects may include depression and weight loss.[5] Safety in pregnancy is unclear, with evidence of harm in other animals.[8] It is an inhibitor of the enzyme phosphodiesterase 4 (PDE4) which results in a decrease in cytokins.[1]

Apremilast was approved for medical use in the United States in 2014 and Europe in 2015.[5][1] In the United Kingdom 4 weeks of treatment costs the NHS about £550 as of 2021.[7] In the United States this amount costs about 4,100 USD.[9]

References[edit]

  1. ^ a b c d e f g h "Otezla". Archived from the original on 3 March 2020. Retrieved 15 January 2022.
  2. ^ "Otezla 30 mg Film-Coated Tablets - Summary of Product Characteristics (SmPC)". (emc). 15 April 2020. Archived from the original on 15 January 2021. Retrieved 19 April 2020.
  3. ^ a b c d e "Otezla (aprelimast) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Archived from the original on 17 October 2014. Retrieved 28 March 2014.
  4. ^ Haberfeld H, ed. (2015). Austria-Codex (in German). Vienna: Österreichischer Apothekerverlag.
  5. ^ a b c d "DailyMed - OTEZLA- apremilast tablet, film coated". dailymed.nlm.nih.gov. Archived from the original on 15 January 2022. Retrieved 15 January 2022.
  6. ^ "Apremilast (Otezla) Use During Pregnancy". Drugs.com. 27 September 2019. Archived from the original on 4 December 2020. Retrieved 19 April 2020.
  7. ^ a b BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 1165. ISBN 978-0857114105.
  8. ^ "Apremilast (Otezla) Use During Pregnancy". Drugs.com. Archived from the original on 4 December 2020. Retrieved 15 January 2022.
  9. ^ "Otezla Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 25 May 2016. Retrieved 15 January 2022.
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