User:Mr. Ibrahem/Ambrisentan

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Mr. Ibrahem/Ambrisentan
Clinical data
Trade namesLetairis, Volibris, Pulmonext, others
AHFS/Drugs.comMonograph
MedlinePlusa612023
License data
Pregnancy
category
  • AU: X (High risk)
Routes of
administration
Oral
Drug classEndothelin receptor antagonist[1]
Legal status
Legal status
  • AU: S4 (Prescription only)
  • CA: ℞-only
  • UK: POM (Prescription only)
  • US: ℞-only
  • EU: Rx-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
BioavailabilityUndetermined
Protein binding99%
Elimination half-life15 hours (terminal)
Identifiers
  • (2S)-2-[(4,6-dimethylpyrimidin-2-yl)oxy]-3-methoxy-3,3-diphenylpropanoic acid
Chemical and physical data
FormulaC22H22N2O4
Molar mass378.428 g·mol−1
3D model (JSmol)
  • O=C(O)[C@@H](Oc1nc(cc(n1)C)C)C(OC)(c2ccccc2)c3ccccc3
  • InChI=1S/C22H22N2O4/c1-15-14-16(2)24-21(23-15)28-19(20(25)26)22(27-3,17-10-6-4-7-11-17)18-12-8-5-9-13-18/h4-14,19H,1-3H3,(H,25,26)/t19-/m1/s1 checkY
  • Key:OUJTZYPIHDYQMC-LJQANCHMSA-N checkY
  (verify)

Ambrisentan, sold under the brand name Letairis among others, is a medication used for pulmonary hypertension.[2] It improved the ability to exercise and slows worsening.[2] It is not useful in those with pulmonary fibrosis.[2] It is taken by mouth.[2]

Common side effects include swelling, palpitations, headache, and constipation.[2] Other side effects may include anemia, flushing, ringing in the ears, and liver problems.[3] Use in pregnancy may harm the baby.[3] It works by blocking the endothelin receptor, specifically the type A endothelin receptor (ETA).[1]

Ambrisentan was approved for medical use in the United States in 2007 and Europe in 2008.[2][4] In the United Kingdom it costs the NHS about £1,600 per month.[3] In the United States this amount costs about 5,100 USD as of 2021.[5]

References[edit]

  1. ^ a b Vatter H, Seifert V (2006). "Ambrisentan, a non-peptide endothelin receptor antagonist". Cardiovasc Drug Rev. 24 (1): 63–76. doi:10.1111/j.1527-3466.2006.00063.x. PMID 16939634.
  2. ^ a b c d e f g h "Ambrisentan Monograph for Professionals". Drugs.com. Archived from the original on 4 July 2021. Retrieved 21 July 2021.
  3. ^ a b c BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 195. ISBN 978-0-85711-369-6.
  4. ^ "Volibris". Archived from the original on 23 July 2021. Retrieved 21 July 2021.
  5. ^ "Ambrisentan Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 10 April 2021. Retrieved 21 July 2021.