Drug General Information (ID: DDI9E8LAY0)
  Drug Name Apraclonidine Drug Info Safinamide Drug Info
  Drug Type Small molecule Small molecule
  Therapeutic Class Ophthalmic Glaucoma Agents Dopaminergic Antiparkinsonism Agents
  Structure

 Mechanism of Apraclonidine-Safinamide Interaction (Severity Level: Major)
     Additive hypertensive effects Click to Show/Hide Mechanism Graph
Could Not Find 2D Structure
      Drug Name Apraclonidine Safinamide
      Mechanism Hypertensive effects
Alpha-1 adrenergic receptor  Agonist
Hypertensive effects
Monoamine oxidase non-selective  Inhibitor
      Key Mechanism Factor 1
Factor Name Adrenergic receptor alpha-1 Structure Sequence
Protein Family G-protein coupled receptor 1 family
Protein Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
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      Key Mechanism Factor 2
Factor Name Monoamine oxidase Structure Sequence
Protein Family Flavin monoamine oxidase family
Protein Function
Catalyzes the oxidative deamination of primary and some secondary amine such as neurotransmitters, with concomitant reduction of oxygen to hydrogen peroxide and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues (PubMed:20493079, PubMed:8316221, PubMed:18391214, PubMed:24169519). Preferentially oxidizes serotonin (PubMed:20493079, PubMed:24169519). Also catalyzes the oxidative deamination of kynuramine to 3-(2-aminophenyl)-3-oxopropanal that can spontaneously condense to 4-hydroxyquinoline (By similarity).
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      Mechanism Description
  • Additive hypertensive effects by the combination of Apraclonidine and Safinamide 

Recommended Action
      Management The use of apraclonidine ophthalmic solution with MAOIs is considered contraindicated. At least 14 days should elapse between discontinuation of MAOI therapy and initiation of treatment with apraclonidine.

References
1 De Vita VT, Hahn MA, Oliverio VT "Monoamine oxidase inhibition by a new carcinostatic agent, n-isopropyl-a-(2-methylhydrazino)-p-toluamide (MIH). (30590)." Proc Soc Exp Biol Med 120 (1965): 561-5. [PMID: 4379192]
2 Product Information. Iopidine (apraclonidine). Alcon Laboratories Inc, Fort Worth, TX.
3 Schulz R, Antonin KH, Hoffmann E, et al "Tyramine kinetics and pressor sensitivity during monoamine oxidase inhibition by selegiline." Clin Pharmacol Ther 46 (1989): 528-36. [PMID: 2510962]