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Samenvatting Farmacologie partim I $18.86
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  7. Farmacologie (1028GENGE2)

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Samenvatting Farmacologie partim I

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  • Course
  • Farmacologie (1028GENGE2)
  • Institution
  • Universiteit Antwerpen (UA)

Samenvatting van het volledige eerste deel van farmacologie. Dit deel wordt gegeven door professor Guns, samen met de studierichtingen farmacie en biomedische. Op de eerste 2 pagina's is de inhoudstafel terug te vinden. Op het einde van het document zitten zowel de voorbeeldvragen als antwoorden di...

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Document information

  • August 30, 2024
  • 61
  • 2023/2024
  • Summary

Subjects

  • farmacologie
  • partim i
  • farmacodynamiek
  • farmacokinetiek
  • gm response
  • chemische transmissie
  • autonoom zenuwstelsel
  • cholinerg systeem
  • mediatoren
  • lokale hormonen
  • aller
  • noradrenerge neurotransmissie

Written for

  • Universiteit Antwerpen (UA)
  • Geneeskunde
  • Farmacologie (1028GENGE2)
All documents for this subject (22)

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Inhoudsopgave

= geneesmiddelenleer ............................................................................................................................................................... 3

1. Farmacodynamiek................................................................................................................................................................. 3
PK & PD bepalen biologisch effect.................................................................................................................................................. 3
Geneesmiddelen ............................................................................................................................................................................. 3
Aangrijpingspunten van geneesmiddelen ...................................................................................................................................... 3
Receptoren ..................................................................................................................................................................................... 4
Verschillende klassen ................................................................................................................................................................ 5
Basisprincipes van receptor interacties .......................................................................................................................................... 6
Agonist binding .......................................................................................................................................................................... 6
Antagonisten ............................................................................................................................................................................. 8

2. Farmacokinetiek ................................................................................................................................................................. 11
Passage door membranen............................................................................................................................................................ 11
ADME ........................................................................................................................................................................................... 13
Farmacokinetische analyse en modellen ...................................................................................................................................... 18
Herhaalde toediening ................................................................................................................................................................... 19

3. Individuele variatie in GM-response .................................................................................................................................... 20
Oorzaken van individuele variatie ................................................................................................................................................ 20

4. Chemische transmissie en autonoom zenuwstelsel ............................................................................................................. 22
Autonoom zenuwstelsel ............................................................................................................................................................... 22

5. Cholinerg systeem ............................................................................................................................................................... 23
Cholinerge neurotransmissie ........................................................................................................................................................ 23

6. Noradrenerge neurotransmissie .......................................................................................................................................... 28
Adrenerge synthese ...................................................................................................................................................................... 28
Adrenerge receptoren .................................................................................................................................................................. 28
Adrenerge effecten ....................................................................................................................................................................... 29
α - receptor medicatie .................................................................................................................................................................. 30
Beta receptor medicamenteus ..................................................................................................................................................... 30
Overzicht receptormedicatie ........................................................................................................................................................ 32
Levenscyclus NA/A........................................................................................................................................................................ 32
Indirecte sympathicomimetica ..................................................................................................................................................... 33

7. Andere mediatoren ............................................................................................................................................................. 34
5 hydroxytryptamine (5-HT, serotonine) ...................................................................................................................................... 34
Purines .......................................................................................................................................................................................... 35
Stikstofoxide (NO)......................................................................................................................................................................... 36

8. Lokale hormonen, ontsteking en allergie ............................................................................................................................. 38
Inflammatie .................................................................................................................................................................................. 38
Histamine ..................................................................................................................................................................................... 38

, Eicosanoïden ................................................................................................................................................................................ 40
Bradykinine (BK) ........................................................................................................................................................................... 41

9. Anti-inflammatoire en immunosuppressieve farmaca ......................................................................................................... 42
NSAID ........................................................................................................................................................................................... 42
Glucocorticoïden (nucleaire receptoren) ...................................................................................................................................... 44
DMARD’s ...................................................................................................................................................................................... 46
Immunosuppressiva ..................................................................................................................................................................... 47

10. Hemostase ........................................................................................................................................................................ 49
Trombotische aandoeningen ........................................................................................................................................................ 49
Bloedplaatjes ................................................................................................................................................................................ 50
Stollingscascade en farmaca ........................................................................................................................................................ 52
Het fibrinolytisch systeem ............................................................................................................................................................ 56

, Farmacologie: partim I

= geneesmiddelenleer
- Farmacodynamiek
o “Hoe werkt een geneesmiddel (GM) in organisme?”
- Farmacokinetiek:
o “Wat doet een organisme met een GM?”
o Hoe komt het op de plaats waar het moet werken?


1. Farmacodynamiek

PK & PD bepalen biologisch effect

- Farmacokinetiek bepaalt wat er met de concentratie gebeurt
- Farmacodynamie: concentratie vh geneesmiddel thvh doelwit,
receptor --> hoe meer concentratie hoe groter effect
o Sigmoidale S curve
ð Samen: We hebben een bepaald effect van een geneesmiddel in
functie van de tijd




Geneesmiddelen

Ontwikkeling
- Kostelijk proces dat enkele jaren duurt: 1 à 2 miljard euro
- Verschillende fases


Wat is een geneesmiddel?
- Conventionele geneesmiddelen
o Kleine chemische moleculen (400g/mol)
o Bv. aspirine of statine
o Vooral over dedeze lesgeven
- Biologicals
o Bv insuline, antilichamen
o Voor immunologische ziekte of kankertherapie
o Veel grotere moleculen --> parenteraal toedienen (= via injectie: SC of IV)
o Kunnen heel specifiek met doelwit interageren


Aangrijpingspunten van geneesmiddelen

Specifiek via
- Via receptoren
- Ion kanalen
- Opnamesystemen
- Enzymen
- (Gentherapie)

, Niet specifiek
- Klassiek grotere hoeveelheden nodig
- Fysisch - chemische werking
- Bv
o Antacida: geven bij verhoogde zuurproductie --
> neutraliseert zuur: zouten toevoegen
§ Andere geneesmiddelen bv alginat leggen
beschermende laag op maagwand
§ Rechtstreeks inwerken op pariëtale cel
mbv antihistaminica of pompinhibitie
o Bulklaxativa
o Osmotische diuretica
o Actieve koolstof
o Plasmavervangers


Chemische selectiviteit
- Moleculen nemen bepaalde ruimte in
- Kunnen mooi op receptor binden --> ‘sleutel die op zen slot past’
- Als je 1 AZ afsplitst van angiotensie II krijg je de inactieve vorm want past niet meer in het ‘sleutelgat’
o 8AZ => 7 AZ = inactief
o L-AZ => D-AZ = inactief
ð Selectiviteit hangt sterk af van de ruimtelijke conformatie


Biologische specificiteit
- Angiotensine II werkt in op angiotensine II receptoren die voorkomen op bloedvaten, maar niet op GI systeem
- AGII-antagonisten gaan geen ongewenste effecten op GI systeem --> dankzij de biologische selectiviteit


Inwerking op receptoren
- Voor receptor:
o Activeren = agonist (direct of indirect)
o Inverse agonist
o Blokkeren = antagonist
- Voor ionkanalen: blokkers ó modulatoren
- Voor enzymen: inhibitor ó prodrug ó valse substraten
- Voor transport: normaal ó inhibitor ó valse substraat
==> maar veel geneesmiddelen die foute naam gekregen hebben: bv beta blokkers maar is receptor


Receptoren

Meeste zitten in plasmamembraan: signalen
capteren buiten cel en omzetten naar signalen
binnen cel

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