Drug General Information (ID: DDIKW94N1B)
  Drug Name Vardenafil Drug Info Riociguat Drug Info
  Drug Type Small molecule Small molecule
  Therapeutic Class Impotence Agents Vasodilator Agents
  Structure

 Mechanism of Vardenafil-Riociguat Interaction (Severity Level: Major)
     Additive hypotensive effects Click to Show/Hide Mechanism Graph
Could Not Find 2D Structure
      Drug Name Vardenafil Riociguat
      Mechanism Hypotensive effects
Phosphodiesterase 5A  Inhibitor
Hypotensive effects
Soluble guanylyl cyclase  Agonist
      Key Mechanism Factor 1
Factor Name Phosphodiesterase 5A
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Structure Sequence
MERAGPSFGQQRQQQQPQQQKQQQRDQDSVEAWLDDHWDFTFSYFVRKATREMVNAWFAERVHTIPVCKEGIRGHTESCSCPLQQSPRADNSAPGTPTRKISASEFDRPLRPIVVKDSEGTVSFLSDSEKKEQMPLTPPRFDHDEGDQCSRLLELVKDISSHLDVTALCHKIFLHIHGLISADRYSLFLVCEDSSNDKFLISRLFDVAEGSTLEEVSNNCIRLEWNKGIVGHVAALGEPLNIKDAYEDPRFNAEVDQITGYKTQSILCMPIKNHREEVVGVAQAINKKSGNGGTFTEKDEKDFAAYLAFCGIVLHNAQLYETSLLENKRNQVLLDLASLIFEEQQSLEVILKKIAATIISFMQVQKCTIFIVDEDCSDSFSSVFHMECEELEKSSDTLTREHDANKINYMYAQYVKNTMEPLNIPDVSKDKRFPWTTENTGNVNQQCIRSLLCTPIKNGKKNKVIGVCQLVNKMEENTGKVKPFNRNDEQFLEAFVIFCGLGIQNTQMYEAVERAMAKQMVTLEVLSYHASAAEEETRELQSLAAAVVPSAQTLKITDFSFSDFELSDLETALCTIRMFTDLNLVQNFQMKHEVLCRWILSVKKNYRKNVAYHNWRHAFNTAQCMFAALKAGKIQNKLTDLEILALLIAALSHDLDHRGVNNSYIQRSEHPLAQLYCHSIMEHHHFDQCLMILNSPGNQILSGLSIEEYKTTLKIIKQAILATDLALYIKRRGEFFELIRKNQFNLEDPHQKELFLAMLMTACDLSAITKPWPIQQRIAELVATEFFDQGDRERKELNIEPTDLMNREKKNKIPSMQVGFIDAICLQLYEALTHVSEDCFPLLDGCRKNRQKWQALAEQQEKMLINGESGQAKRN
Gene Name PDE5A
Uniprot ID PDE5A_HUMAN
KEGG Pathway hsa:8654
Protein Family Cyclic nucleotide phosphodiesterase family
Protein Function
Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. This phosphodiesterase catalyzes the specific hydrolysis of cGMP to 5'-GMP (PubMed:9714779, PubMed:15489334). Specifically regulates nitric-oxide-generated cGMP (PubMed:15489334).
    Click to Show/Hide
      Key Mechanism Factor 2
Factor Name Guanylate cyclase soluble Structure Sequence
Protein Family Adenylyl cyclase class-4/guanylyl cyclase family
Protein Function
Mediates responses to nitric oxide (NO) by catalyzing the biosynthesis of the signaling molecule cGMP.
    Click to Show/Hide
      Mechanism Description
  • Additive hypotensive effects by the combination of Vardenafil and Riociguat 

Recommended Action
      Management Concomitant use of riociguat with PDE inhibitors, including specific PDE-5 inhibitors (e.g., avanafil, sildenafil, tadalafil, vardenafil) or nonspecific PDE inhibitors (e.g., dipyridamole, theophylline), is considered contraindicated. Riociguat should be discontinued at least 24 hours before administering a PDE-5 inhibitor, and avoidance of riociguat administration within 24 hours after sildenafil or within 48 hours after tadalafil is recommended. Limited data exists for other PDE inhibitors.

References
1 Cerner Multum, Inc. "Australian Product Information.".
2 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
3 Product Information. Adempas (riociguat). Bayer Pharmaceutical Inc, West Haven, CT.