Summary
Samenvatting "partim I" - Farmacologie
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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Uploaded on
September 4, 2024
Number of pages
101
Written in
2023/2024
Type
Summary
farmacodynamiek
farmacokinetiek
geneesmiddelinteracties
cholinerge transmissie
adrenerge transmissie
purines
serotonine
leukotriënen
bradykinine
immunosuppressieva
dmard
hemostase
fibrinolyse
Institution
Universiteit Antwerpen (UA)
Education
Geneeskunde
Course
Farmacologie
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Samenvatting + flashcards - Farmacologie
1. Summary - Samenvatting "partim i" - farmacologie
2. Summary - Samenvatting "partim ii" - farmacologie
3. Summary - Flashcards geneesmiddelen - 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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