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Enzyme Inhibitors, Anticholinergic Drugs, When DDC is blocked, COMT will…

- - - - Dose reduction by 75 to 80%. AEs are reduced.
      - Decreased N/V and cardiac S/E
      - Prevent pyridoxine antagonism
    - - Increased central SE of L-dopa
      - Early development of long term SE possible
- - - - PK: Food decreases BA. Metabolised via glucuronidation. Half-life: 2-3 hours
      - S/E
        
        hepatotoxicity. May need discontinuation
        
        orthostatic hypotension
        
        CNS S/E as L-dopa
        
        GI effects: N/V/D, abdominal pain
        
        urine dicolouration
    - - PK: Metabolised via glucuronidation. 90% excreted in feces.
      - Decreases iron stores by chelation of iron
      - S/E
        
        urine dicolouration
        
        taste pervesion
        
        CNS S/E as L-dopa
        
        GI effects: N/V/D, abdominal pain
- - - - Reduce dopamine breakdown > reduce H2O2 formation, sparing nigral cells from damage by free radicals.
      - Prescribed early before L-dopa is began
      - Surviving striatal dopamine neurons accelerate dopamine synthesis, which then enhance H2O2 formation. Oxidative stress causes the remaining cells to die faster.
    - - Food increases BA by 3 to 4 times.
      - Extensive metabolism in gut / liver by CYP2B6 & CYP3A4
      - Major metabolites: N-desmethyl selegiline (active), L-amphetamine, L-methamphetamine
      - Excretion primarily in urine
    - - nausea, dizziness, hallucinations, confusion, depression, agitation, insomnia if taken at night
      - loss of balance, increase involuntary movements, bradykinesia
      - arrhythmia, orthostatic hypotension
- - - - GI: N/V/D, dyspepsia, dry mouth
      - CVS: palpitation, hypotension, tachycardia
      - CNS: hallucinations, delusions, confusion, dizziness