Drug General Information (ID: DDITOEQULZ)
  Drug Name Mecamylamine Drug Info Lofexidine Drug Info
  Drug Type Small molecule Small molecule
  Therapeutic Class Antihypertensive Agents Antihypertensive Agents
  Structure

 Mechanism of Mecamylamine-Lofexidine Interaction (Severity Level: Moderate)
     Additive hypotensive effects Click to Show/Hide Mechanism Graph
Could Not Find 2D Structure
      Drug Name Mecamylamine Lofexidine
      Mechanism Hypotensive effects
Neuronal acetylcholine receptor  Antagonist
Hypotensive effects
Alpha-2 adrenergic receptor  Agonist
      Key Mechanism Factor 1
Factor Name Neuronal acetylcholine receptor Structure Sequence
Protein Family Ligand-gated ion channel (TC 1.A.9) family
Protein Function
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
    Click to Show/Hide
      Key Mechanism Factor 2
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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      Mechanism Description
  • Additive hypotensive effects by the combination of Mecamylamine and Lofexidine 

Recommended Action
      Management Hemodynamic responses should be monitored during coadministration of lofexidine with antihypertensive agents, especially during the first few weeks of therapy.

References
1 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
2 Product Information. Lucemyra (lofexidine). US WorldMeds LLC, Louisville , KY.
3 Warrington SJ, Ankier SI, Turner P "Evaluation of possible interactions between ethanol and trazodone or amitriptyline." Neuropsychobiology 15 (1986): 31-7. [PMID: 3725002]