Drug General Information (ID: DDIDJHC0Z4)
  Drug Name Bisoprolol Drug Info Guanethidine Drug Info
  Drug Type Small molecule Small molecule
  Therapeutic Class Antihypertensive Agents Antihypertensive Agents
  Structure

 Mechanism of Bisoprolol-Guanethidine Interaction (Severity Level: Moderate)
     Additive hypotensive effects Click to Show/Hide Mechanism Graph
Could Not Find 2D Structure
      Drug Name Bisoprolol Guanethidine
      Mechanism 1 Antihypertensive agent
Beta-1 adrenergic receptor  Antagonist
Antihypertensive agent
Noradrenaline transporter  Inducer
      Key Mechanism Factor 1
Factor Name Adrenergic receptor beta-1
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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 Norepinephrine transporter
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Structure Sequence
MLLARMNPQVQPENNGADTGPEQPLRARKTAELLVVKERNGVQCLLAPRDGDAQPRETWGKKIDFLLSVVGFAVDLANVWRFPYLCYKNGGGAFLIPYTLFLIIAGMPLFYMELALGQYNREGAATVWKICPFFKGVGYAVILIALYVGFYYNVIIAWSLYYLFSSFTLNLPWTDCGHTWNSPNCTDPKLLNGSVLGNHTKYSKYKFTPAAEFYERGVLHLHESSGIHDIGLPQWQLLLCLMVVVIVLYFSLWKGVKTSGKVVWITATLPYFVLFVLLVHGVTLPGASNGINAYLHIDFYRLKEATVWIDAATQIFFSLGAGFGVLIAFASYNKFDNNCYRDALLTSSINCITSFVSGFAIFSILGYMAHEHKVNIEDVATEGAGLVFILYPEAISTLSGSTFWAVVFFVMLLALGLDSSMGGMEAVITGLADDFQVLKRHRKLFTFGVTFSTFLLALFCITKGGIYVLTLLDTFAAGTSILFAVLMEAIGVSWFYGVDRFSNDIQQMMGFRPGLYWRLCWKFVSPAFLLFVVVVSIINFKPLTYDDYIFPPWANWVGWGIALSSMVLVPIYVIYKFLSTQGSLWERLAYGITPENEHHLVAQRDIRQFQLQHWLAI
Gene Name SLC6A2
Uniprot ID SC6A2_HUMAN
KEGG Pathway hsa:6530
Protein Family Sodium:neurotransmitter symporter (SNF) (TC 2.A.22) family
Protein Function
Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
    Click to Show/Hide
      Mechanism Description
  • Additive hypotensive effects by the combination of Bisoprolol and Guanethidine 
     Increased risk of bradycardia Click to Show/Hide Mechanism Graph
Could Not Find 2D Structure
      Drug Name Bisoprolol Guanethidine
      Mechanism 2 Bradycardia
Beta adrenergic receptor  Antagonist
Potentiate the bradycardia effect of beta blocker
      Key Mechanism Factor 3
Factor Name Adrenergic receptor beta Structure Sequence
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
      Mechanism Description
  • Increased risk of bradycardia by the combination of Bisoprolol and Guanethidine 
      Mechanism 3 Bradycardia
Beta-1 adrenergic receptor  Antagonist
Potentiate the bradycardia effect of beta blocker
      Key Mechanism Factor 4
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
      Mechanism Description
  • Increased risk of bradycardia by the combination of Bisoprolol and Guanethidine 

Recommended Action
      Management Caution is advised if beta-blockers, including ophthalmic formulations, are prescribed in combination with sympathetic ganglion-blocking or catecholamine-depleting agents. Patients should contact their doctor if they experience dizziness, lightheadedness, syncope, bradycardia, shortness of breath, difficulty breathing, edema, and/or chest pain.

References
1 Kronig MH, Roose SP, Walsh BT, Woodring S, Glassman AH "Blood pressure effects of phenelzine." J Clin Psychopharmacol 3 (1983): 307-10. [PMID: 6630590]
2 Product Information. Marplan (isocarboxazid) Roche Laboratories, Nutley, NJ.
3 Product Information. Matulane (procarbazine). Roche Laboratories, Nutley, NJ.