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Samenvatting "partim I" - Farmacologie
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  • Course
  • Farmacologie
  • Institution
  • Universiteit Antwerpen (UA)

Samenvatting van "partim I" als onderdeel van het vak 'Farmacologie' gegeven door prof. Guns PJ. in de 2e Bachelor Geneeskunde aan de UA. Samenvatting gebaseerd op slides, lesnotities én cursus.

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Document information

  • September 4, 2024
  • 101
  • 2023/2024
  • Summary

Subjects

  • farmacodynamiek
  • farmacokinetiek
  • geneesmiddelinteracties
  • cholinerge transmissie
  • adrenerge transmissie
  • purines
  • serotonine
  • leukotriënen
  • bradykinine
  • immunosuppressieva
  • dmard
  • hemostase
  • fibrinolyse

Written for

  • Universiteit Antwerpen (UA)
  • Geneeskunde
  • Farmacologie
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Inhoudstafel
Inleiding.......................................................................................................................................................... 5
Biologisch effect......................................................................................................................................... 5
Geneesmiddelontwikkeling ....................................................................................................................... 5
Wat is een geneesmiddel........................................................................................................................... 5

Farmacodynamiek..........................................................................................................................................6
Aangrijpingspunten van geneesmiddelen.................................................................................................. 6
Specifieke geneesmiddelen................................................................................................................. 6
Nomenclatuur....................................................................................................................................... 7
Overzicht.............................................................................................................................................. 7
Receptoren.................................................................................................................................................7
Ionotropic receptoren........................................................................................................................... 8
Metabotropic receptoren (GPCR).........................................................................................................8
Tyrosine kinase linked receptoren (“-nibs”).......................................................................................... 9
Nucleaire receptoren............................................................................................................................ 9
Samenvatting....................................................................................................................................... 9
Geneesmiddel – receptor interacties....................................................................................................... 10
Agonist............................................................................................................................................... 10
Antagonisten...................................................................................................................................... 13
Samenvatting..................................................................................................................................... 16
Adaptatie............................................................................................................................................ 16

Farmacokinetiek...........................................................................................................................................18
Inleiding....................................................................................................................................................18
1. Passage door membranen...................................................................................................................18
(Ultra)filtratie.......................................................................................................................................18
Diffusie............................................................................................................................................... 19
Carrier-gemedieerd transport............................................................................................................. 21
Samenvatting..................................................................................................................................... 21
2. Absorptie (opname)..............................................................................................................................21
Galenische formulering...................................................................................................................... 22
Orale absorptie...................................................................................................................................23
Parenterale absorptie......................................................................................................................... 24
Lokale absorptie................................................................................................................................. 24
3. Distributie (verdeling)........................................................................................................................... 25
Verdelingsvolume (VD).......................................................................................................................25
Eiwit-binding....................................................................................................................................... 25
Bloed-hersenbarrière (BHB)...............................................................................................................26
Redistributie....................................................................................................................................... 26
4. Metabolisme.........................................................................................................................................26
Biotransformatie................................................................................................................................. 27
Enterohepatische circulatie................................................................................................................ 27
Pro-drug............................................................................................................................................. 27
5. Eliminatie (excretie)..............................................................................................................................28
Klaring................................................................................................................................................ 28
ADME: samenvatting............................................................................................................................... 29

1

, Farmacokinetische analyse en modellen................................................................................................. 29
Eén-compartiment model................................................................................................................... 29
Twee-compartiment model................................................................................................................. 30
Herhaalde toediening (steady-state)........................................................................................................ 30
1e orde kinetiek.................................................................................................................................. 31
Verzadigingskinetiek (niet-lineair).......................................................................................................32

Individuele variatie in geneesmiddelen respons...................................................................................... 33
Inleiding....................................................................................................................................................33
Oorzaken van individuele variabiliteit.......................................................................................................33
Genetische factoren........................................................................................................................... 33
Leeftijd................................................................................................................................................34
Ziekte..................................................................................................................................................34
Geneesmiddelinteracties....................................................................................................................35

Chemische transmissie en het autonoom zenuwstelsel..........................................................................37
Autonoom zenuwstelsel........................................................................................................................... 37
Chemische transmissie............................................................................................................................ 37
Presynaptische modulatie.................................................................................................................. 38
Co-transmissie................................................................................................................................... 38
Denervatie en supersensitiviteit......................................................................................................... 38

Cholinerge transmissie............................................................................................................................... 39
Cholinerge neurotransmissie................................................................................................................... 39
Voorkomen......................................................................................................................................... 39
Muscarine ACh-receptoren (mAChR)...................................................................................................... 40
mAChR agonisten.............................................................................................................................. 40
mAChR antagonisten......................................................................................................................... 42
Nicotinerge ACh-receptoren (nAChR)......................................................................................................43
nAChR-spierverslappers.................................................................................................................... 44
Afbraak van acetylcholine (ACh)..............................................................................................................45
Cholinesterase-remmers.................................................................................................................... 45
Samenvatting: cholinerg systeem............................................................................................................ 47

Adrenerge transmissie................................................................................................................................ 49
Fysiologie van adrenerge neurotransmissie............................................................................................ 49
Adrenerge receptoren.............................................................................................................................. 50
Adrenerge effecten.............................................................................................................................50
Sympathicomimetica................................................................................................................................ 51
-receptor agonisten............................................................................................................................ 52
-receptor agonisten............................................................................................................................ 53
Sympathicolytica...................................................................................................................................... 54
-receptor antagonisten....................................................................................................................... 54
-receptor antagonisten = “-blokkers” (-olol)........................................................................................ 54
Farmaca die aangrijpen op de levenscyclus van NA/A............................................................................56
NET-inhibitie....................................................................................................................................... 56
Indirecte sympathicomimetica............................................................................................................ 57
Samenvatting: adrenerge receptoren.......................................................................................................57
2

,Andere perifere mediatoren: 5-HT, purines, NO........................................................................................ 58
5-hydroxytryptamine = serotonine............................................................................................................58
Classificatie van 5-HT-receptoren...................................................................................................... 58
Farmaca............................................................................................................................................. 59
Samenvatting: 5-HT........................................................................................................................... 61
Ergotalkaloïden........................................................................................................................................ 61
Belangrijkste actieve stoffen...............................................................................................................62
Purines..................................................................................................................................................... 62
Nucleotide receptoren (in cytosol)......................................................................................................63
Farmaca............................................................................................................................................. 63
Stikstofoxide (NO).................................................................................................................................... 64
Effecten van NO................................................................................................................................. 64
NO-donoren........................................................................................................................................65
PDE-V remmers................................................................................................................................. 65

Lokale hormonen, ontsteking en allergie.................................................................................................. 67
Inleiding....................................................................................................................................................67
Immuunsysteem................................................................................................................................. 67
Histamine................................................................................................................................................. 67
Antihistaminica................................................................................................................................... 68
Indirecte antihistaminica.....................................................................................................................69
EicosanoÏden........................................................................................................................................... 70
Prostaglandines....................................................................................................................................... 70
Fysiologische effecten........................................................................................................................70
Klinische toepassingen.......................................................................................................................71
Leukotriënen............................................................................................................................................ 72
Fysiologische effecten........................................................................................................................72
Leukotriene-receptor antagonisten.....................................................................................................72
Bradykinine (BK)...................................................................................................................................... 72
Fysiologische effecten........................................................................................................................73

Anti-inflammatoire en immunosuppressieve farmaca............................................................................. 74
NSAID...................................................................................................................................................... 74
Nevenwerkingen.................................................................................................................................74
Farmaca............................................................................................................................................. 75
Glucocorticoïden...................................................................................................................................... 77
Kinetiek...............................................................................................................................................78
Effecten.............................................................................................................................................. 79
Indicaties............................................................................................................................................ 79
DMARD.................................................................................................................................................... 80
Conventionele/synthetische DMARD’s...............................................................................................81
Biologische DMARD’s........................................................................................................................ 82
Tyrosine kinase (JAK) inhibitoren.......................................................................................................82
Immunosuppressiva................................................................................................................................. 83
Aangrijpingspunten.............................................................................................................................83
Farmaca............................................................................................................................................. 84
Anti-jicht middelen....................................................................................................................................85
Acute aanval.......................................................................................................................................86
3

, Chronisch........................................................................................................................................... 86
Samenvatting: anti-jicht medicatie......................................................................................................87

Hemostase = bloedstolling......................................................................................................................... 88
Hemostase............................................................................................................................................... 88
Rol van endotheelcellen bij de regulatie van hemostase................................................................... 88
Trombo-embolische aandoeningen.................................................................................................... 89
Rol van bloedplaatjes...............................................................................................................................89
Stimuli van bloedplaatjes....................................................................................................................90
Farmaca............................................................................................................................................. 91
Samenvatting: bloedplaatjesremmers................................................................................................ 94
Rol van bloedplaatjes...............................................................................................................................94
Protrombinase complex (F–Va complex)........................................................................................... 95
Anticoagulantia...................................................................................................................................95
Vitamine K.......................................................................................................................................... 96
Injecteerbare anticoagulantia............................................................................................................. 97
Directe orale anticoagulantia..............................................................................................................99
DOAC vs. vitamine K antagonisten.................................................................................................. 100
Fibrinolyse..............................................................................................................................................101
Fibrinolytica...................................................................................................................................... 101




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