Details of Drug Interaction

Details of Drug-Drug Interaction

 Drug General Information (ID: DDITAVLH2R)
  Drug Name Ranolazine Drug Info Varenicline Drug Info
  Drug Type Small molecule Small molecule
  Therapeutic Class Analgesics Smoking Cessation Agents
  Structure

 Mechanism of Ranolazine-Varenicline Interaction (Severity Level: Moderate)
     Transporter inhibition Click to Show/Hide Mechanism Graph
Could Not Find 2D Structure
      Drug Name Ranolazine Varenicline
      Mechanism OCT2 inhibitor OCT2 substrate
      Key Mechanism Factor 1
Factor Name Solute carrier family 22 member 2
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Structure Sequence
MPTTVDDVLEHGGEFHFFQKQMFFLLALLSATFAPIYVGIVFLGFTPDHRCRSPGVAELSLRCGWSPAEELNYTVPGPGPAGEASPRQCRRYEVDWNQSTFDCVDPLASLDTNRSRLPLGPCRDGWVYETPGSSIVTEFNLVCANSWMLDLFQSSVNVGFFIGSMSIGYIADRFGRKLCLLTTVLINAAAGVLMAISPTYTWMLIFRLIQGLVSKAGWLIGYILITEFVGRRYRRTVGIFYQVAYTVGLLVLAGVAYALPHWRWLQFTVSLPNFFFLLYYWCIPESPRWLISQNKNAEAMRIIKHIAKKNGKSLPASLQRLRLEEETGKKLNPSFLDLVRTPQIRKHTMILMYNWFTSSVLYQGLIMHMGLAGDNIYLDFFYSALVEFPAAFMIILTIDRIGRRYPWAASNMVAGAACLASVFIPGDLQWLKIIISCLGRMGITMAYEIVCLVNAELYPTFIRNLGVHICSSMCDIGGIITPFLVYRLTNIWLELPLMVFGVLGLVAGGLVLLLPETKGKALPETIEEAENMQRPRKNKEKMIYLQVQKLDIPLN
Gene Name 44836
Uniprot ID S22A2_HUMAN
KEGG Pathway hsa:6582
Protein Family Major facilitator (TC 2.A.1) superfamily
Protein Function
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamine, creatinine, amantadine, memantine, acriflavine, 4-[4-(dimethylamino)-styryl]-N-methylpyridinium ASP, amiloride, metformin, N-1-methylnicotinamide (NMN), tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, cisplatin and oxaliplatin. Cisplatin may develop a nephrotoxic action. Transport of creatinine is inhibited by fluoroquinolones such as DX-619 and LVFX. This transporter is a major determinant of the anticancer activity of oxaliplatin and may contribute to antitumor specificity.
    Click to Show/Hide
      Mechanism Description
  • Decreased clearance of Varenicline due to the transporter inhibition by Ranolazine 

Recommended Action
      Management It may be advisable to monitor patients for altered efficacy and safety if ranolazine must be used with an OCT2 substrate.

References
1 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
2 Product Information. Ranexa (ranolazine). Calmoseptine Inc, Huntington Beach, CA.
3 FDA. U.S. Food and Drug Administration "Drug Safety Communications: FDA updates label for stop smoking drug Chantix (varenicline) to include potential alcohol interaction, rare risk of seizures, and studies of side effects on mood, behavior, and thinking. Safety announcement." .