Read the summary and the most important questions on HNH-23306

• L1 general introduction; terms and definitions

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• What is a drug?

  • Medicines
    
  • bio-actives
  • chemicals

• L2 Molecular Pharmacodynamics and receptor pharmacology

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• Different classes of receptors (4)

  • Ligand-gated ion channels 
    
  • G-protein-coupled receptors 
  • protein kinases
  • transcription factors 

• What is asthma (in brief)

  Recurrent and reversible airway obstruction 
  
  

  • inflammatory changes in the airways
  • bronchial hyper-responsiveness
  • attack in two phases 

• What are examples for pharmacology of asthma

  • Beta 2 - adrenergic agonists relax smooth muscle 
    
  • short acting (salbutamol) or long acting (salmeterol)
  • usually given as local formation 
  • use depends on type of asthma, often combined with glucocorticoids 
  • sometimes: muscarinic receptor antagonist 

  
  
  - not that common anymore: PDE inhibitors 

• The general principles of drug action: receptor models

  Hangt ervan af of het een agonist of antagonist is en of het occupation governed by affinity (L->R)of activation governed by efficacy (B->O) is

• L3 Pharmacokinetics deel 1

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• How do compounds cross the intestinal epithelium?

  • Paracellular transport 
    
  • transcellular transport 
  • active or carrier mediated 

• The expression/activity of cytochrome P450 (CYP450) is dependent on:

  • Genetics 
    
  • gender
  • age 
  • diet
  • smoking 
  • environment 
  • diseases
  • medicines etc 

  
  
  geen grapefruit eten want dan wordt P450 geblokkeerd!

• Where can ion trapping be used for?

  Ion trapping can be used to distribute drugs into the urinary compartment to increase/decrease the urinary excretion of poisons/drugs etc 
  
  

  • arlkalinization of the urine (by administration of sodium bicarbonate) to increase urinary excretion of acetyl salicylic acid
  • idem to reduce urine levels of illicit drugs with basic properties (cocaine, amphetamine, morphine...)

• How many liter water is in your total body

  60-70%
  
  30-40 liters 

• L4 Pharmocokinetics deel 2

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• What does it mean when your Vd is 0,2 L/kg; 0,55 L/kg; >1 L/kg

  Vd 0.2 L/kg 
  

  • total extracellular volume 
  • polar / very hydrophilic compounds 
  • e.g. Vecuronium, gentamicin, carbenicillin, many biopharmacuticals 

  
  
  
  Vd 0.55 L/kg
  

  • total body water 
  • e.g. Ethanol, phenytoin 

  
  
  Vd > 1 L/kg
  

  • lipophylic compounds
  • for example compounds acting in the CNS
  • diazepam 
  • mianserin 
  • trimipramine