Details of Drug-Drug Interaction
| Drug General Information (ID: DDIL0IO845) | |||||||||
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| Drug Name | Lofexidine | Drug Info | Ambrisentan | Drug Info | |||||
| Drug Type | Small molecule | Small molecule | |||||||
| Therapeutic Class | Antihypertensive Agents | Agents For Pulmonary Hypertension | |||||||
| Structure | |||||||||
| Mechanism of Lofexidine-Ambrisentan Interaction (Severity Level: Moderate) | |||||||||
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| Additive hypotensive effects Click to Show/Hide Mechanism Graph | |||||||||
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| Drug Name | Lofexidine | Ambrisentan | |||||||
| Mechanism |
Hypotensive effects Alpha-2 adrenergic receptor Agonist |
Antihypertensive agent Endothelin receptor Antagonist |
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| Key Mechanism Factor 1 | |||||||||
| Factor Name | Adrenergic receptor alpha-2 | Structure Sequence | |||||||
| Protein Family | G-protein coupled receptor 1 family | ||||||||
| Protein Function |
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol.
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| Key Mechanism Factor 2 | |||||||||
| Factor Name | Endothelin A receptor |
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Structure
Sequence
METLCLRASFWLALVGCVISDNPERYSTNLSNHVDDFTTFRGTELSFLVTTHQPTNLVLPSNGSMHNYCPQQTKITSAFKYINTVISCTIFIVGMVGNATLLRIIYQNKCMRNGPNALIASLALGDLIYVVIDLPINVFKLLAGRWPFDHNDFGVFLCKLFPFLQKSSVGITVLNLCALSVDRYRAVASWSRVQGIGIPLVTAIEIVSIWILSFILAIPEAIGFVMVPFEYRGEQHKTCMLNATSKFMEFYQDVKDWWLFGFYFCMPLVCTAIFYTLMTCEMLNRRNGSLRIALSEHLKQRREVAKTVFCLVVIFALCWFPLHLSRILKKTVYNEMDKNRCELLSFLLLMDYIGINLATMNSCINPIALYFVSKKFKNCFQSCLCCCCYQSKSLMTSVPMNGTSIQWKNHDQNNHNTDRSSHKDSMN
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| Gene Name | EDNRA | ||||||||
| Uniprot ID | EDNRA_HUMAN | ||||||||
| KEGG Pathway | hsa:1909 | ||||||||
| Protein Family | G-protein coupled receptor 1 family | ||||||||
| Protein Function |
Receptor for endothelin-1. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of binding affinities for ET-A is: ET1 > ET2 >> ET3.
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| Mechanism Description |
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| Recommended Action | |||||||||
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| Management | Hemodynamic responses should be monitored during coadministration of lofexidine with antihypertensive agents, especially during the first few weeks of therapy. | ||||||||