Summary Class notes - HNH-23306

- HNH-23306
- Renger Witkamp
- 2019 - 2020
- Wageningen University (Wageningen University, Wageningen)
- Voeding en Gezondheid
277 Flashcards & Notes
2 Students
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Summary - Class notes - HNH-23306

  • 1572217200 L1 general introduction; terms and definitions

  • The definition of pharmacology
    The study of the effects of drugs on living systems, aiming to improve their functioning
  • What is a drug?
    • Medicines
    • bio-actives
    • chemicals
  • Waar wordt naproxennatrium voor/bij gebruikt?
    Bij koorts en bij pijn
  • Wat wordt er met OTC bedoeld
    OTC = over the counter 

    dus je kan hem zonder recept halen bij bijvoorbeeld de kruitvat.
  • Legal definitions of drug ('medicine')
    'Any substance or combination of substances which may be administered to human beings with a view to making a medical diagnosis or to restoring, correcting or modifying physiological functions in human beings' [engels]

    substantie of smanestelling van substanties, welke is bestemd te worden gebruikt of op enigerlei wijze wordt aangeduid of aanbevolen als zijnde geschikt voor:
    1. het genezen, leningen of voorkomen van enige aandoening, ziekte, ziekteverschijnsel, pijn, verwonding of gebrek bij de mens
    2. het herstellen, verbeteren of wijzigen van het functioneren van organellen bij de mens, 
    3. het stellen van een medische diagnose door toediening aan of aanwending bij de mens;  


    interpreteer dat wat hierboven staat! (is het een drug treatment)
  • De definitie van indications
    The reason to use the drug.

    The officially, legal approved where the drug can be used for.
  • Wat zijn de 'indications' van naproxennatrium
    • Headaches
    • toothaches
    • menstrual cramps
    • muscular pains
    • backache (lumbago)
    • for relief of the signs and pain in influenza and after vaccination 
  • Medicines need approval by national authorities (= CBG in NL) or European (EMA)
  • Welke soorten registratie codes zijn er waar je een medicine aan kan herkennen
    • Nationally approved: RVG code
    • Homeopathic medicines: RVH code
    • European registration: EU code 
  •  Waar staat de afkorting NSAID voor
    Nonsteroidal anti-inflammatory drug
  • Analgesic = pijnstiller 
    antipyretic = koorts verlagend
  • Non-steroidal anti-inflammatory drugs bind to cycle-oxygenase [= prostaglandin endperoxide H synthase (PGHS)]
  • What are cycle-oxygenases and what are they doing?
    Zie de afbeelding; de stuctuur wordt zo veranderd dat er isomeren kunnen worden gemaakt waardoor het door het hele lichaam een functie heeft
  • Er zijn twee vormen van COX welke twee zijn dat en wat doen ze
    COX 1 en COX 2 

    • gastro-protective prostaglandins PGE PGI

    COX 2 
    • inflammatory prostaglandins 

    Je zou COX2 willen remmen maar je remt ze allebei waardoor je GI-tract? Niet meer zo goed wordt beschermd 
  • Bekijk de afbeelding goed!

    waarom kan je beter naproxen nemen dan rofecoxib
  • Pharmaceutical phase --> formulation, administration desintegration, dissolution etc. 

    pharmacokinetic phase --> absorption, distribution, metabolism and excretion 

    pharmacodynamic phase --> interactions with molecular targets 
  • What are the routes of application?
    Zie de afbeelding 

    tussen lever en blood zit nog een biotransformatie stap dus er kunnen nog verandering optreden 
  • Basics of oral drug absorption (6)
    • Mostly in duodenum 
    • drug should be in dissolved state 
    • often by passive diffusion (...polarity, pKa etc)
    • sometimes active transport involved 
    • lipid soluble compounds (partly) with lipids
    • metabolism in intestinal wall can be considerable
  • Een belangrijk plaatje
  • Biotransformation =
    Omzetting, conjugates
  • 1572303600 L2 Molecular Pharmacodynamics and receptor pharmacology

  • Acetyl salicylic acid =
  • What kind of claims are there?
    • Nutrition claims 
    • health claims 
      • function claims 
  • Pharmaceutical phase -->
    Formulation, administration desintegration, dissolution etc
  • Pharmacokinetic phase -->
    Absorption, distribution, metabolism and excretion
  • Pharmacodynamic phase -->
    Interactions with molecular targets
  • Some basic principles of pharmacodynamics (5)
    • The molecular action of a drug / bioactive can often be explained by-, and predicted from a receptor concept 
    • receptors: macromolecules including enzymes, transporters, structures on cell membranes, transcription factors, nucleotides etc. 
    • receptors are mostly normal regulatory structures playing a role in the physiology of the organism 
    • natural ligands: neurotransmitters, hormones or other signaling molecules
    • drugs just bind by coincidence or by design to these receptors 
  • What are the 'real' receptors?
    • agonist 
    • antagonist 

    ion channels 
    • blockers 
    • modulators 
  • Ligand-gated ion channels; also: ionotropticw receptors
    Multi-subunit ion channels 

    location: cell surface transmembrane 

    examples of ligands:
  • GABA is the major inhibitory neurotransmitter in the central nervous system. Wat heeft effect op de GABA?
    • Benzodiazepines enhance the response to GABA
    • they act allosterically on the receptor 
    • examples:
      • diazepam 
      • oxazepam 
      • lorazepam 
  • G-protein-coupled receptors
    Location: cell surface transmembrane 

    examples of ligands:
    alfa- and beta-adrenergic 
  • Protein kinases
    Location: cell surface transmembrane 

    examples of ligands
    growth factors, insulin 
    peptide hormones 
  • Transcription factors
    Location: cytoplasm 

    examples of ligands:
    steroid hormones 
    thyroid hormone 
    vitamine D
  • Different classes of receptors (4)
    • Ligand-gated ion channels 
    • G-protein-coupled receptors 
    • protein kinases
    • transcription factors 
  • G- protein coupled receptors (GPCRs) wat weet je ervan?
    • One of most important targets for today's drugs 
    • very large family of regulatory proteins 
    • 7TM (trans-membrane) receptor structure 
    • central mechanism: GTP-GDP reaction 
    • five different key targets for G-proteins that translate the signal:
      • adenylate cyclase /cAMP
      • phospholipase 
      • ion channels 
      • Pho kinase 
      • mitogen-activated protein kinase 
  • Bekijk goed het plaatje, de start zit links boven
  • 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 
  • Target enzymes can be bi-directionally controlled by a Gs and Gi protein
  • Making our own 'endocannabinoids'
    • We have our own endocannabinoid system (ECS)
    • the ECS is a highly important regulation system in our body 
    • endocannabinoids are formed from fatty acids 
    • the ECS offers many opportunities for disease management and prevention 
  • De CB1 moet niet geblokkeerd worden, je gelukshormoon komt daar bij kijken en zal dus leiden tot depressie
  • 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
  • Benzodiazepines stimuleren de binding van GABA maar hierdoor wordt je heel relaxed en slaperig
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Alpha 2 antagonist
Available as food supplement yohimbine. Herbal viagra, was many side effects
Alpha 2 agonist
Used to decrease blood pressure. For exempel clonidine. Clinically not first choice therapy
Alpha 1 antagonist
Used to prevent urinary retention or to lower blood pressure via peripheral vasocilation. Can als be used for Raynaud's syndrome
Alpha 1 agonist
Used for local effect as anti-congestive in the nose. Swollen muces tissue in nose is decreased by vasoconstriction. More space to breath but not enough blood supply
Beta 1 antagonist
Beta blockers

beta blockers = used to calm down the heart, it decreases blood pressure and cardiac output. In case of angina pectoris or hypertension 
Beta 1 agonist
Used after a shock to increase the blood volume
The most predominant action of drugs that belong to the class of the ACE-inhibitors is:
Alfa-1 edrenergic antagonists can be used as drugs for the following indications:
To procent urinary retention in benige prostaten hypertrophy
Hen two drug formulations are bio-equivalent, this means that:
Thee have the same area under the curve (AUC), tmax and Cmax
Which of the following approaches can provide good targets for pharmacological modulation of appetite and/or food-intake?
The use of GLP-1 analogues