, 2024-
2025
ALGEMENE
FARMACOLOGIE
MORGANE DE SAMBLANC
UGENT
1
,Inhoudsopgave
DEFINITIES..............................................................................................................................................4
Farmacologie :....................................................................................................................................4
Farmacokinetiek :...............................................................................................................................5
Farmacodynamiek :............................................................................................................................5
Farmacognosie :.................................................................................................................................5
Farmacotherapie :..............................................................................................................................5
Farmacotoxicologie :..........................................................................................................................5
Farmacogenomics :.............................................................................................................................5
ADME :................................................................................................................................................5
Basisbegrippen :.................................................................................................................................5
1. ALGEMEEN :................................................................................................................................5
2. FARMACEUTISCHE FASE :............................................................................................................5
3. FARMACOKINETISCHE FASE :......................................................................................................6
4. FARMACODYNAMISCHE FASE :...................................................................................................6
PASSAGE DOORHEEN CELMEMBRANEN.................................................................................................7
Algemeen :..........................................................................................................................................7
Manieren van passage :......................................................................................................................7
FARMACOKINETISCHE PROCESSEN.......................................................................................................11
Algemeen :........................................................................................................................................11
Absorptie of resorptie :.....................................................................................................................12
1. Toedieningswegen :..................................................................................................................12
2. Resorptie na orale toediening :.................................................................................................12
3. Resorptie na buccale en sublinguale toediening.......................................................................16
4. Resorptie na rectale toediening................................................................................................17
5. Intravasculaire toediening........................................................................................................17
6. Intramusculaire en subcutane toediening................................................................................17
7. Bijzondere geneesmiddelen voor IM/SC gebruik : depotpreparaten........................................18
8. Resorptie na toediening op de huid..........................................................................................18
9. Resorptie na inhalatie (bronchiale en pulmonaire toediening).................................................18
10. Intramammaire toediening.....................................................................................................19
11. Intrathecale toediening..........................................................................................................19
Distributie of verdeling.....................................................................................................................19
1. Bepalende factoren :................................................................................................................19
2. Verdelingsvolume of distributievolume....................................................................................22
2
, 3. Specifieke verdelingen..............................................................................................................23
Eliminatie..........................................................................................................................................23
1. Renale excretie :.......................................................................................................................23
2. Speekselexcretie.......................................................................................................................25
3. Melkklierexcretie......................................................................................................................25
4. Biliaire excretie.........................................................................................................................25
5. Hepatische klaring....................................................................................................................26
6. Biotransformatie.......................................................................................................................27
FARMACOKINETIEK...............................................................................................................................34
Inleiding............................................................................................................................................34
Eerste orde versus nulde orde processen.........................................................................................35
Compartimentele modellen..............................................................................................................35
Eerste orde kinetiek; één compartimenteel model..........................................................................35
Intraveneuze toediening = bolus (= éénmalige toediening)..........................................................36
Extravasculaire toediening – bolus...............................................................................................38
Biologische beschikbaarheid (biodisponibiliteit = F).....................................................................39
Kinetiek van de metabolieten :.....................................................................................................41
Invloed van verandering in Cli, Q en f(u) op de PK........................................................................41
Multiple dosering :........................................................................................................................43
Intraveneus infuus :......................................................................................................................44
Eerste orde kinetiek, 2-compartimenteel model..............................................................................44
Inleiding :......................................................................................................................................44
0e orde of niet-lineaire kinetiek :......................................................................................................45
Algemeen :....................................................................................................................................45
Niet lineair door absorptie :..........................................................................................................46
Niet lineair door distributie :........................................................................................................46
Niet lineair door renale excretie :.................................................................................................46
Niet lineair door metabolisme :....................................................................................................47
Tijdsafhankelijke farmacokinetiek :..............................................................................................48
Therapeutische drug monitoring of TDM :...................................................................................48
FARMACODYNAMIEK............................................................................................................................49
Inleiding :..........................................................................................................................................49
Doelwitten van geneesmiddelen :....................................................................................................49
1) Receptoren...............................................................................................................................49
2) Ion-kanalen...............................................................................................................................49
3) Enzymen...................................................................................................................................49
3
2025
ALGEMENE
FARMACOLOGIE
MORGANE DE SAMBLANC
UGENT
1
,Inhoudsopgave
DEFINITIES..............................................................................................................................................4
Farmacologie :....................................................................................................................................4
Farmacokinetiek :...............................................................................................................................5
Farmacodynamiek :............................................................................................................................5
Farmacognosie :.................................................................................................................................5
Farmacotherapie :..............................................................................................................................5
Farmacotoxicologie :..........................................................................................................................5
Farmacogenomics :.............................................................................................................................5
ADME :................................................................................................................................................5
Basisbegrippen :.................................................................................................................................5
1. ALGEMEEN :................................................................................................................................5
2. FARMACEUTISCHE FASE :............................................................................................................5
3. FARMACOKINETISCHE FASE :......................................................................................................6
4. FARMACODYNAMISCHE FASE :...................................................................................................6
PASSAGE DOORHEEN CELMEMBRANEN.................................................................................................7
Algemeen :..........................................................................................................................................7
Manieren van passage :......................................................................................................................7
FARMACOKINETISCHE PROCESSEN.......................................................................................................11
Algemeen :........................................................................................................................................11
Absorptie of resorptie :.....................................................................................................................12
1. Toedieningswegen :..................................................................................................................12
2. Resorptie na orale toediening :.................................................................................................12
3. Resorptie na buccale en sublinguale toediening.......................................................................16
4. Resorptie na rectale toediening................................................................................................17
5. Intravasculaire toediening........................................................................................................17
6. Intramusculaire en subcutane toediening................................................................................17
7. Bijzondere geneesmiddelen voor IM/SC gebruik : depotpreparaten........................................18
8. Resorptie na toediening op de huid..........................................................................................18
9. Resorptie na inhalatie (bronchiale en pulmonaire toediening).................................................18
10. Intramammaire toediening.....................................................................................................19
11. Intrathecale toediening..........................................................................................................19
Distributie of verdeling.....................................................................................................................19
1. Bepalende factoren :................................................................................................................19
2. Verdelingsvolume of distributievolume....................................................................................22
2
, 3. Specifieke verdelingen..............................................................................................................23
Eliminatie..........................................................................................................................................23
1. Renale excretie :.......................................................................................................................23
2. Speekselexcretie.......................................................................................................................25
3. Melkklierexcretie......................................................................................................................25
4. Biliaire excretie.........................................................................................................................25
5. Hepatische klaring....................................................................................................................26
6. Biotransformatie.......................................................................................................................27
FARMACOKINETIEK...............................................................................................................................34
Inleiding............................................................................................................................................34
Eerste orde versus nulde orde processen.........................................................................................35
Compartimentele modellen..............................................................................................................35
Eerste orde kinetiek; één compartimenteel model..........................................................................35
Intraveneuze toediening = bolus (= éénmalige toediening)..........................................................36
Extravasculaire toediening – bolus...............................................................................................38
Biologische beschikbaarheid (biodisponibiliteit = F).....................................................................39
Kinetiek van de metabolieten :.....................................................................................................41
Invloed van verandering in Cli, Q en f(u) op de PK........................................................................41
Multiple dosering :........................................................................................................................43
Intraveneus infuus :......................................................................................................................44
Eerste orde kinetiek, 2-compartimenteel model..............................................................................44
Inleiding :......................................................................................................................................44
0e orde of niet-lineaire kinetiek :......................................................................................................45
Algemeen :....................................................................................................................................45
Niet lineair door absorptie :..........................................................................................................46
Niet lineair door distributie :........................................................................................................46
Niet lineair door renale excretie :.................................................................................................46
Niet lineair door metabolisme :....................................................................................................47
Tijdsafhankelijke farmacokinetiek :..............................................................................................48
Therapeutische drug monitoring of TDM :...................................................................................48
FARMACODYNAMIEK............................................................................................................................49
Inleiding :..........................................................................................................................................49
Doelwitten van geneesmiddelen :....................................................................................................49
1) Receptoren...............................................................................................................................49
2) Ion-kanalen...............................................................................................................................49
3) Enzymen...................................................................................................................................49
3