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Samenvatting algemene farmacologie
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Samenvatting algemene farmacologie, volledig beide onderdelen: Farmacokinetiek en farmacodynamiek. Voldoende voor 18/20 ;)
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Samenvatting Algemene FarmacologieInhoudsopgave
Algemene inleiding tot de farmacologie ........................................................................................................... 4
Farmacodynamiek ............................................................................................................................................ 4
Algemeen ............................................................................................................................................................ 4
Aangrijpingspunten geneesmiddelen ............................................................................................................. 4
Maag(zuur)klachten ............................................................................................................................................ 5
Inhibitie van zuursecretie ................................................................................................................................ 5
Ishemisch herseninfarct ...................................................................................................................................... 6
Thrombo-embolische aandoeningen .............................................................................................................. 6
Hemostase ...................................................................................................................................................... 6
Remmers van de plaatjesaggregatie (weefselschade) .................................................................................... 6
Remmers van de stollingscascade (stase) ....................................................................................................... 7
Adrenerg systeem................................................................................................................................................ 7
Selectiviteit ...................................................................................................................................................... 8
Cardiovasculaire geneesmiddelen .................................................................................................................. 9
Reumatoïde artritis (RA).................................................................................................................................... 10
Geneesmiddelen bij reumatoïde artritis ....................................................................................................... 10
Aangrijpingspunten van geneesmiddelen ......................................................................................................... 11
4 klasses. ....................................................................................................................................................... 11
Basisprincipes van receptorinteracties .............................................................................................................. 11
Receptoren: agonist binding ......................................................................................................................... 11
Receptoren: effecten meten ......................................................................................................................... 11
Dosis-antwoord curve (DAC) ......................................................................................................................... 11
Receptor binding: intrinsieke activiteit 𝜀 ...................................................................................................... 12
Allosterische modulatie ................................................................................................................................ 12
Receptoren: antagonisten ............................................................................................................................. 12
Adaptatie ....................................................................................................................................................... 13
Therapeutische index .................................................................................................................................... 14
Farmacokinetiek............................................................................................................................................. 15
Inleiding, dissolutie en permeabiliteit ............................................................................................................... 15
Therapeutische concentratie ........................................................................................................................ 15
Relatie tussen farmacodynamiek en farmacokinetiek .................................................................................. 15
Farmacokinetiek, farmacodynamiek en de pathofysiologie ......................................................................... 15
ADME ............................................................................................................................................................ 15
Farmacokinetiek parameters ........................................................................................................................ 15
Dissolutie en permeabiliteit: Fysicochemische eigenschappen en formuleringsaspecten ........................... 16
Absorptie en distributie ................................................................................................................................. 21
Absorptie ........................................................................................................................................................... 21
ADME ............................................................................................................................................................ 21
Verschillende barrières naar het target ........................................................................................................ 21
Parenterale toediening ................................................................................................................................. 21
Biologische beschikbaarheid ......................................................................................................................... 22
Factoren die de absorptie beïnvloeden ........................................................................................................ 23
, Distributie .......................................................................................................................................................... 24
Therapeutisch venster................................................................................................................................... 24
Factoren die distributie beïnvloeden ............................................................................................................ 24
Schijnbaar distributievolume ........................................................................................................................ 25
Eiwitbinding................................................................................................................................................... 26
Metabolisme en excretie................................................................................................................................ 28
Metabolisme ..................................................................................................................................................... 28
Geneesmiddel metabolisme ......................................................................................................................... 28
Farmacokinetische parameters gerelateerd aan het metabolisme .............................................................. 29
Factoren die metabolisme beïnvloeden........................................................................................................ 31
Excretie .............................................................................................................................................................. 31
Renaal............................................................................................................................................................ 31
Eliminatie: biliarie excretie ............................................................................................................................ 33
Farmacokinetische modellen ......................................................................................................................... 35
Plasmaconcentratie – tijdsverloop afhankeljk van ADME ............................................................................ 35
Farmacokinetische paramters ....................................................................................................................... 35
Niet-compartimentele analyse...................................................................................................................... 35
Type van modellen ............................................................................................................................................ 35
Empirische modellen ..................................................................................................................................... 35
Compartimentele modellen .......................................................................................................................... 35
Fysiologische modellen ................................................................................................................................. 35
Waarom een farmacokinetisch model gebruiken? ........................................................................................... 35
Xde orde processen ............................................................................................................................................. 35
Lineaire of eerste orde kinetiek .................................................................................................................... 36
Grafische voorstelling ................................................................................................................................... 36
Één-compartimenteel IV-model ........................................................................................................................ 36
Berekening van farmacokinetische parameters ........................................................................................... 36
2-Compartimenteel IV-model ............................................................................................................................ 38
Concentratie/compartiment ......................................................................................................................... 38
...................................................................................................................................................................... 38
Absorptiemodel ................................................................................................................................................. 39
Orale absorptie, farmacokinetisch model ..................................................................................................... 39
Absorptiekinetiek .......................................................................................................................................... 39
Lag-tijd........................................................................................................................................................... 39
0de orde kinetiek ................................................................................................................................................ 40
Michaelis-Menten kinetiek ................................................................................................................................ 40
Oorzaken van niet-lineaire kinetiek .............................................................................................................. 40
Interpsecies schaling ......................................................................................................................................... 40
Empirische benadering // allometrische schaling ......................................................................................... 40
Mechanische benadering .............................................................................................................................. 40
Interspecies allometrie.................................................................................................................................. 40
Fysiologische (PB/PK) modelling ................................................................................................................... 40
Meervoudige toediening en infuus .................................................................................................................... 41
Meervoudige toediening ............................................................................................................................... 41
Steady state................................................................................................................................................... 41
Effect van de dosis ........................................................................................................................................ 41
Effect van dosisinterval (𝝉 – tau) ................................................................................................................... 41
Keuze dosis en interval.................................................................................................................................. 41
Berekening ladingsdosis ................................................................................................................................ 42
, Belang van farmacokinetische parameters ................................................................................................... 42
Variabiliteit: Extensive and poor metabolizers ............................................................................................. 42
Meervoudige toediening – lineaire kinetiek ................................................................................................. 42
Enkelvoudige toediening, meervoudige toediening en niet-lineariteit ........................................................ 42
Infuus ............................................................................................................................................................ 42
Farmacokinetische/farmacodynamische modellen ........................................................................................ 43
Effect classificatie .............................................................................................................................................. 43
Direct zonder hysteresis, direct link models ................................................................................................. 43
Direct met hysteresis, direct link models ...................................................................................................... 44
Indirect link model ........................................................................................................................................ 45
Indirect respons models ................................................................................................................................ 45
Complexiteiten in farmacokinetiek/farmacodynamiek modelling .................................................................... 46
Tolerantie ...................................................................................................................................................... 47
Waarde van PK/PD ............................................................................................................................................ 48
Doseringsvoorspelling: interspecies extrapolatie ......................................................................................... 48
Doseringsvoorspelling PK/PD ........................................................................................................................ 48
Vergelijking farmacodynamiek verschillende geneesmiddelen .................................................................... 48
Samenvatting therapeutische dosis en PK variabiliteit en dosering ............................................................. 48
, Algemene inleiding tot de farmacologie
Studie van de werking en effect van een geneesmiddel
Er zijn twee aspecten die bekeken kunnen worden
- Farmacokinetiek: Geeft concentratie ten opzichte van de tijd weer; zegt iets over de
opname van het geneesmiddel
- Farmacodynamiek: Geeft het effect ten opzichte van de concentratie; zegt iets over
het effect bij bepaalde concentraties, sigmoïdale curve.
Farmacokinetisch-farmacodynamisch is de combinatie, dat is het effect ten opzichte van de
tijd.
Geneesmiddelenontwikkeling
Eerst wordt een stof ontdekt/ontwikkeld, daarbij wordt er in een basisonderzoek gekeken naar welk eiwit
opgereguleerd wordt en het target gaat zijn. In een preclinical fase kijken of het geneesmiddel efficiënt en
veilig is. In de klinische studies 3 fases, I: kleine groepen, langzaamaan hogere dosissen, inzicht in
farmacokinetiek en farmacodynamiek. II: optimaliseren, werkzaamheid en veiligheid aantonen. III: grotere
patiëntenpopulaties werkzaamheid en veiligheid documenteren. Laatste fase is het voorleggen aan de
commissie voor goedkeuring.
Farmacodynamiek
Algemeen
Meeste geneesmiddelen kleine chemische moleculen, de nieuwe geneesmiddelen soms antilichamen, die zijn
veel groter. Qua selectiviteit zijn kleine molecules vaak minder goed, grotere moleculen kunnen beter contact
maken met hun doelwit, zijn selectiever, minder ongewenste effecten.
Biologicals
Kleine chemische moleculen kunnen vaak oraal opgenomen worden, de biologicals moeten meestal subcutaan
of intraveneus toegediend worden.
Chemische selectiviteit
Juiste sleutel in het slot. Bepaalde 3D configuratie nodig zodat de sleutel in het slot zou passen.
Biologische specificiteit
Het doelwit van een geneesmiddel komt maar op bepaalde plaatsen voor.
Agonist: als je een receptor hebt, is de agonist de molecule die de receptor activeert
Antagonist: de molecule die de receptor blokkeert.
Aangrijpingspunten geneesmiddelen
Geneesmiddel kan specifiek of niet-specifiek werken.
Aangrijpingspunt kan receptor gemedieerd of niet-receptor
gemedieerd zijn.
- A: Bij receptoren spreken we van agonist en antagonist
- B: Bij ionkanalen spreken we van blokkers of modulatoren
- C: Bij enzymen spreken we van inhibitoren
- D: Bij transporters spreken we van inhibitoren
Geneesmiddelen als volgt kennen: Waarvoor het wordt gebruikt, wat is het werkingsmechanisme,
farmacokinetisch of farmacodynamisch principe eraan koppelen
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