Details of Drug-Drug Interaction
| Drug General Information (ID: DDIBG4RO10) | |||||||||
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| Drug Name | Guanfacine | Drug Info | Dolutegravir | Drug Info | |||||
| Drug Type | Small molecule | Small molecule | |||||||
| Therapeutic Class | Antiadrenergic Agents | Antiviral Agents | |||||||
| Structure | |||||||||
| Mechanism of Guanfacine-Dolutegravir Interaction (Severity Level: Moderate) | |||||||||
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| Transporter inhibition Click to Show/Hide Mechanism Graph | |||||||||
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| Drug Name | Guanfacine | Dolutegravir | |||||||
| Mechanism | OCT2 substrate | OCT2 inhibitor | |||||||
| Key Mechanism Factor 1 | |||||||||
| Factor Name | Solute carrier family 22 member 2 |
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Structure
Sequence
MPTTVDDVLEHGGEFHFFQKQMFFLLALLSATFAPIYVGIVFLGFTPDHRCRSPGVAELSLRCGWSPAEELNYTVPGPGPAGEASPRQCRRYEVDWNQSTFDCVDPLASLDTNRSRLPLGPCRDGWVYETPGSSIVTEFNLVCANSWMLDLFQSSVNVGFFIGSMSIGYIADRFGRKLCLLTTVLINAAAGVLMAISPTYTWMLIFRLIQGLVSKAGWLIGYILITEFVGRRYRRTVGIFYQVAYTVGLLVLAGVAYALPHWRWLQFTVSLPNFFFLLYYWCIPESPRWLISQNKNAEAMRIIKHIAKKNGKSLPASLQRLRLEEETGKKLNPSFLDLVRTPQIRKHTMILMYNWFTSSVLYQGLIMHMGLAGDNIYLDFFYSALVEFPAAFMIILTIDRIGRRYPWAASNMVAGAACLASVFIPGDLQWLKIIISCLGRMGITMAYEIVCLVNAELYPTFIRNLGVHICSSMCDIGGIITPFLVYRLTNIWLELPLMVFGVLGLVAGGLVLLLPETKGKALPETIEEAENMQRPRKNKEKMIYLQVQKLDIPLN
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| 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.
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| Mechanism Description |
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| Recommended Action | |||||||||
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| Management | Caution is advised when dolutegravir is used with drugs that are substrates of OCT2, particularly those with a narrow therapeutic range such as metformin. Dosage adjustments as well as clinical and laboratory monitoring may be appropriate for some drugs whenever dolutegravir is added to or withdrawn from therapy. | ||||||||
| References | |||||||||||||||||||
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| 1 | Product Information. Lonsurf (tipiracil-trifluridine). Taiho Oncology, Inc., Princeton, NJ. | ||||||||||||||||||
| 2 | Product Information. Tivicay (dolutegravir). ViiV Healthcare, Research Triangle Park, NC. | ||||||||||||||||||