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User:Mr. Ibrahem/Riociguat

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Mr. Ibrahem/Riociguat
Skeletal formula of riociguat
Ball-and-stick model of riociguat
Clinical data
Trade namesAdempas
Other namesBAY 63-2521
AHFS/Drugs.comMonograph
License data
Pregnancy
category
  • AU: X (High risk)
Routes of
administration
By mouth
Drug classSoluble guanylate cyclase (sGC) stimulator[1]
Legal status
Legal status
  • AU: S4 (Prescription only)
  • US: ℞-only
  • EU: Rx-only
Pharmacokinetic data
Bioavailability94%
Protein binding95%
MetabolismCYP1A1, CYP3A4, CYP2C8, CYP2J2
MetabolitesN-desmethylriociguat (active), glucuronide (inactive)
Elimination half-life5–10 h
Excretion33–45% Kidney,
48–59% Bile duct
Identifiers
  • Methyl N-[4,6-Diamino-2-[1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-pyrimidinyl]-N-methyl-carbaminate
Chemical and physical data
FormulaC20H19FN8O2
Molar mass422.424 g·mol−1
3D model (JSmol)
  • c14ncccc4c(-c(nc2N)nc(N)c2N(C)C(=O)OC)nn1Cc3ccccc3F
  • InChI=1S/C20H19FN8O2/c1-28(20(30)31-2)15-16(22)25-18(26-17(15)23)14-12-7-5-9-24-19(12)29(27-14)10-11-6-3-4-8-13(11)21/h3-9H,10H2,1-2H3,(H4,22,23,25,26) ☒N
  • Key:WXXSNCNJFUAIDG-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Riociguat, sold under the brand name Adempas is a medication used to treat two forms of pulmonary hypertension (PH): chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension (PAH).[1] It is a second line treatment.[1] It is taken by mouth.[1]

Common side effects include headache, upset stomach, nausea, and diarrhea.[1] Other side effects may include bleeding and low blood pressure.[1] Use in pregnancy may harm the baby.[1] It is a stimulator of soluble guanylate cyclase (sGC).[1]

Riociguat was approved for medical use in the United States in 2013.[1] In the United Kingdom it costs the NHS about £2,000 for 4 weeks as of 2021.[2] This amount in the United States costs about 9,500 USD.[3]

References[edit]

  1. ^ a b c d e f g h i j k "Riociguat Monograph for Professionals". Drugs.com. Archived from the original on 30 January 2021. Retrieved 17 October 2021.
  2. ^ a b BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 197. ISBN 978-0-85711-369-6.{{cite book}}: CS1 maint: date format (link)
  3. ^ "Adempas Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 10 August 2020. Retrieved 17 October 2021.