Drug General Information (ID: DDIKYX3AQN)
  Drug Name Zaleplon Drug Info Lofexidine Drug Info
  Drug Type Small molecule Small molecule
  Therapeutic Class Anxiolytics/Sedatives/Hypnotics Antihypertensive Agents
  Structure

 Mechanism of Zaleplon-Lofexidine Interaction (Severity Level: Moderate)
     Additive hypotensive effects Click to Show/Hide Mechanism Graph
Could Not Find 2D Structure
      Drug Name Zaleplon Lofexidine
      Mechanism 1 Antihypertensive agent Hypotensive effects
Alpha-2 adrenergic receptor  Agonist
      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.
    Click to Show/Hide
      Mechanism Description
  • Additive hypotensive effects by the combination of Zaleplon and Lofexidine 
      Mechanism 2 Hypotensive effects Hypotensive effects
Alpha-2 adrenergic receptor  Agonist
      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.
    Click to Show/Hide
      Mechanism Description
  • Additive hypotensive effects by the combination of Zaleplon and Lofexidine 

Recommended Action
      Management Caution and close monitoring for development of hypotension is advised during coadministration of these agents. Avoid alcohol in patients receiving vasodilating antihypertensive drugs. Patients should be advised to avoid rising abruptly from a sitting or recumbent position and to notify their physician if they experience dizziness, lightheadedness, syncope, orthostasis, or tachycardia.

References
1 Ellison JM, Milofsky JE, Ely E "Fluoxetine-induced bradycardia and syncope in two patients." J Clin Psychiatry 51 (1990): 385-6. [PMID: 2211552]
2 Feder R "Bradycardia and syncope induced by fluoxetine." J Clin Psychiatry 52 (1991): 139. [PMID: 2005082]
3 Sternbach H "Fluoxetine-associated potentiation of calcium-channel blockers." J Clin Psychopharmacol 11 (1991): 390-1. [PMID: 1770159]