Details of Drug Interaction | MecDDI

Drug General Information (ID: DDIAS5R4EQ)
Drug Name			Esmolol		Drug Info		Sildenafil		Drug Info
Drug Type		Small molecule				Small molecule
Therapeutic Class		Antihypertensive Agents				Impotence Agents/Agents For Pulmonary Hypertension
Structure

Mechanism of Esmolol-Sildenafil Interaction (Severity Level: Moderate)
Additive hypotensive effects Click to Show/Hide Mechanism Graph

Drug Name		Esmolol				Sildenafil
Mechanism		Antihypertensive agent Beta-1 adrenergic receptor Antagonist				Hypotensive effects Prostacyclin receptor Agonist
Key Mechanism Factor 1
		Factor Name		Adrenergic receptor beta-1				× Structure Sequence MGAGVLVLGASEPGNLSSAAPLPDGAATAARLLVPASPPASLLPPASESPEPLSQQWTAGMGLLMALIVLLIVAGNVLVIVAIAKTPRLQTLTNLFIMSLASADLVMGLLVVPFGATIVVWGRWEYGSFFCELWTSVDVLCVTASIETLCVIALDRYLAITSPFRYQSLLTRARARGLVCTVWAISALVSFLPILMHWWRAESDEARRCYNDPKCCDFVTNRAYAIASSVVSFYVPLCIMAFVYLRVFREAQKQVKKIDSCERRFLGGPARPPSPSPSPVPAPAPPPGPPRPAAAAATAPLANGRAGKRRPSRLVALREQKALKTLGIIMGVFTLCWLPFFLANVVKAFHRELVPDRLFVFFNWLGYANSAFNPIIYCRSPDFRKAFQRLLCCARRAARRRHATHGDRPRASGCLARPGPPPSPGAASDDDDDDVVGATPPARLLEPWAGCNGGAAADSDSSLDEPCRPGFASESKV
		Gene Name		ADRB1
		Uniprot ID		ADRB1_HUMAN
		KEGG Pathway		hsa:153
		Protein Family		G-protein coupled receptor 1 family
		Protein Function		Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity. Mediates Ras activation through G(s)-alpha- and cAMP-mediated signaling. Involved in the regulation of sleep/wake behaviors (PubMed:31473062). Click to Show/Hide
Key Mechanism Factor 2
		Factor Name		Prostacyclin receptor				× Structure Sequence MADSCRNLTYVRGSVGPATSTLMFVAGVVGNGLALGILSARRPARPSAFAVLVTGLAATDLLGTSFLSPAVFVAYARNSSLLGLARGGPALCDAFAFAMTFFGLASMLILFAMAVERCLALSHPYLYAQLDGPRCARLALPAIYAFCVLFCALPLLGLGQHQQYCPGSWCFLRMRWAQPGGAAFSLAYAGLVALLVAAIFLCNGSVTLSLCRMYRQQKRHQGSLGPRPRTGEDEVDHLILLALMTVVMAVCSLPLTIRCFTQAVAPDSSSEMGDLLAFRFYAFNPILDPWVFILFRKAVFQRLKLWVCCLCLGPAHGDSQTPLSQLASGRRDPRAPSAPVGKEGSCVPLSAWGEGQVEPLPPTQQSSGSAVGTSSKAEASVACSLC
		Gene Name		PTGIR
		Uniprot ID		PI2R_HUMAN
		KEGG Pathway		hsa:5739
		Protein Family		G-protein coupled receptor 1 family
		Protein Function		Receptor for prostacyclin (prostaglandin I2 or PGI2). The activity of this receptor is mediated by G(s) proteins which activate adenylate cyclase. Click to Show/Hide
Mechanism Description		Additive hypotensive effects by the combination of Esmolol and Sildenafil

Recommended Action
Management		Caution is advised if PDE5 inhibitors are prescribed in combination with antihypertensive agents. Patients receiving the combination should be advised to avoid rising abruptly from a sitting or recumbent position, especially following treatment initiation or a dosage increase, and to contact their doctor if they experience symptoms of hypotension such as dizziness, lightheadedness, fainting, or tachycardia.

References
1	Product Information. Levitra (vardenafil). Bayer, West Haven, CT.
2	Product Information. Stendra (avanafil). Vivus Inc, Mountain View, CA.
3	Product Information. Viagra (sildenafil). Pfizer US Pharmaceuticals, New York, NY.