FARMACOLOGIE DEEL 5
FARMACOTHERAPIE
JAN DE HOON EN MINNE CASTEELS
Inhoudsopgave
INLEIDING: AUTACOÏDEN BIJ INFLAMMATIE EN ALLERGIE..................................3
H1: NSAIDS.................................................................................................... 6
CHEMIE.............................................................................................................................. 6
WERKINGSMECHANISME......................................................................................................... 7
FARMACOKINETIEK................................................................................................................ 8
FAMRACODYNAMIEK.............................................................................................................. 8
INDICATIES.......................................................................................................................... 8
BIJWERKINGEN..................................................................................................................... 8
GI................................................................................................................................. 9
BP................................................................................................................................. 9
Renaal en CV................................................................................................................ 9
Overgevoeligheidsreacties.........................................................................................10
Hepatotoxiciteit en hematologische toxiciteit............................................................10
CONTRA-INDICATIES EN RISICOPOPULATIES...............................................................................10
INTERACTIE....................................................................................................................... 10
PRAKTIJK: KIEZEN VAN NSAID.............................................................................................. 11
VERSCHILLENDE GROEPEN VAN NSAIDS..................................................................................11
salicylaten.................................................................................................................. 11
para-aminofenol derivaten......................................................................................... 12
indool- en arylazijnzuurderivaten...............................................................................13
arylpropionzuurderivaten........................................................................................... 14
oxicams...................................................................................................................... 14
pyrazolonderivaten.................................................................................................... 14
selectieve COX-2 inhibitoren (coxibs).........................................................................15
H2: GLUCOCORTICOÏDEN...............................................................................16
CHEMIE............................................................................................................................ 16
WERKINGSMECHANISME....................................................................................................... 16
FARMACOKINETIEK.............................................................................................................. 17
FARMACODYNAMIEK............................................................................................................ 18
INDICATIES........................................................................................................................ 18
BIJWERKINGEN................................................................................................................... 19
RISICOPOPULATIES.............................................................................................................. 21
,H3: TWEEDELIJNS ANTI-REUMATISCHE GENEESMIDDELEN...............................22
DMARDS......................................................................................................................... 22
csDMARDs.................................................................................................................. 22
bDMARDs................................................................................................................... 23
tsDMARDs.................................................................................................................. 24
IMMUNOSUPPRESSIVA.......................................................................................................... 24
H4: MIGRAINE.............................................................................................. 27
BEHANDELING:................................................................................................................... 27
acute aanval............................................................................................................... 27
profylactische medicatie............................................................................................30
H5: JICHT..................................................................................................... 32
NSAID............................................................................................................................ 33
COLCHICINE...................................................................................................................... 33
GLUCOCORTICOÏDEN........................................................................................................... 33
URICOSTATICA................................................................................................................... 33
URICOSURICA.................................................................................................................... 34
RECOMBINANT URAAT OXIDASE............................................................................................. 35
CANAKINUMAB................................................................................................................... 35
H6: ANTIHISTAMINICA (TYPE I ALLERGIE).......................................................35
HISTAMINE........................................................................................................................ 36
H1-RECEPTORANTAGONISTEN............................................................................................... 38
H7: ASTMA................................................................................................... 42
ANTI-ASTMAGENEESMIDDELEN............................................................................................... 43
ß2-agonist.................................................................................................................. 44
Anticholinergica.......................................................................................................... 45
Corticosteroïden......................................................................................................... 45
Theofylline.................................................................................................................. 46
Leukotriënreceptor-antagonisten...............................................................................47
Andere........................................................................................................................ 47
Aandachtspuntsen...................................................................................................... 48
inhalatiesystemen...................................................................................................... 48
H8: ANAFYLACTISCHE REACTIES....................................................................49
H9: DIABETES MELLITUS...............................................................................50
NORMALE FYSIOLOGIE.......................................................................................................... 51
INSULINE EN ANALOGEN....................................................................................................... 53
ORALE ANTIDIABETICA......................................................................................................... 55
Biguaniden................................................................................................................. 55
Sulfamiden/sulfonylureumderivaten...........................................................................56
Gliniden...................................................................................................................... 57
Thiazolidinedionen of glitazonen................................................................................59
Alfa-gucosidase inhibitoren........................................................................................59
Gliptinen..................................................................................................................... 59
Gliflozinen.................................................................................................................. 60
INCRETINEMIMETICA............................................................................................................ 61
H10: OSTEOPOROSE.....................................................................................62
NIET-FARMACOLOGISCHE OPTIES............................................................................................ 63
, Calcium + vitamine D................................................................................................63
Vitamine D................................................................................................................. 64
FARMACOLOGISCHE OPTIES................................................................................................... 65
Bisfosfonaten............................................................................................................. 65
SERMs........................................................................................................................ 66
Teriparatide................................................................................................................ 67
Monoclonale AL: denosumab en romosozumab..........................................................67
H11: KANKER............................................................................................... 68
INLEIDING......................................................................................................................... 68
KANKERTHERAPIE............................................................................................................... 69
Principes..................................................................................................................... 69
Terminologie.............................................................................................................. 69
Nevenwerkingen........................................................................................................ 70
Stoffen....................................................................................................................... 70
H12: SUPPORTIEVE THERAPIE BIJ KANKERBEHANDELNG.................................76
RECOMBINANT ERYTHROEPOËTINE.......................................................................................... 76
MELOÏDE GROEIFACTOR, G-CSF............................................................................................ 77
PROFYLACTISCHE ANTI-EMETICA............................................................................................. 78
BOTMETASTASEN................................................................................................................ 78
H13: PALLIATIEVE EN TERMINALE ZORG.........................................................78
INLEIDING......................................................................................................................... 78
SYMPTOOMCONTROLE PALLIATIEVE ZORG.................................................................................79
MEDICATIETOEDIENINGSROUTES............................................................................................ 84
PALLIATIEVE SEDATIE........................................................................................................... 86
EUTHANASIE...................................................................................................................... 86
H14: GI STELSEL........................................................................................... 87
ACID-PEPTIC DISEASE........................................................................................................... 87
H2-receptorantagonisten...........................................................................................87
Protonpompinhibitoren (PPI).......................................................................................88
Misoprostol................................................................................................................. 89
Antacida..................................................................................................................... 89
antibiotica.................................................................................................................. 90
(GASTRO)-PROKINETICA....................................................................................................... 90
Dopamine-2-receptorantagonisten.............................................................................90
Cisapride.................................................................................................................... 91
ANTI-EMETICA.................................................................................................................... 91
PANCREASENZYM-SUBSTITUUT............................................................................................... 92
LAXANTIA......................................................................................................................... 92
ANTI-DIARRHEÏCA............................................................................................................... 93
INFLAMMATOIR DARMLIJDEN (IBD)......................................................................................... 93
BEHANDELING VAN INFESTATIE MET WORMEN...........................................................................94
INLEIDING: AUTACOÏDEN BIJ INFLAMMATIE EN ALLERGIE
Autacoïden = endogene stoffen die antwoorden op weefselbeschadiging (zelf-
remedie)
o Lokale hormonen
, o Kort halfleven
o Autocrien (op zelfde cel) of paracrien (op nabijgelegen cellen)
o Processen: ontsteking, allergie
o Stoffen
NT (vb serotonine, histamine)
Peptiden (vb bradykinine, angiotensine II, VIP)
Vetzuurderivaten (vb prostanoïden = autocoïden betrokken bij
inflammatie, PAF)
Anorganische moleculen (NO)
Eicosanoïden
o = autacoïden gevormd door oxidatie van membraangebonden poly-
onverzadigde vetzuren
o = prostanoïden en leukotriënen
Via COX: vorming prostanoïden (= prostaglandines en
tromboxanen) uit arachidonzuur
Via lipoxygenase: vorming leukotriënen
Prostanoïden
o = prostaglandines en tromboxanen
o Effecten (hieruit kan men bijwerkingen van NSAID’s raden)
Hersenen
Verhoging lichaamstemperatuur
Stimulatie PGE2 door IL-1
Luchtwegen
Bronchodilatatie door PGE2 en PGI2
Bronchoconstrictie door PGF2alfa en TXA2
Reproductie-orgaan
Vrouw
o Menstruatie: meer prostaglandins die contractie
veroorzaken pijn
o Abortus: prostaglandines gebruikt
o Bevalling: contracties en cervixrijping NSAID:
premature arbeid onderdrukken
Man
o Prostaglandines in semen rol conceptie en
infertiliteit
o Erectie: PGE2 via relaxatie van gladde spieren
Bloedvaten: BALANS
PGI2: remt BP aggregatie
TXA2: stimuleert BP aggregatie
Cave: rokers onevenwicht: minder PGI2 en meer TXA1
waardoor meer constrictie
Maag: BESCHERMEND
PGE2 en PGI2
o Inhibitie maagzuur
o Flow maagwand door vrijstelling NO
o Mucus maagwand
In utero
PGE2 en PGI2 zorgen voor normale circulatie tussen linker en
rechter bloedsomloop van ongeboren kind
Nier
PGE2 en PGI2: dilatatie afferente arteriolen
FARMACOTHERAPIE
JAN DE HOON EN MINNE CASTEELS
Inhoudsopgave
INLEIDING: AUTACOÏDEN BIJ INFLAMMATIE EN ALLERGIE..................................3
H1: NSAIDS.................................................................................................... 6
CHEMIE.............................................................................................................................. 6
WERKINGSMECHANISME......................................................................................................... 7
FARMACOKINETIEK................................................................................................................ 8
FAMRACODYNAMIEK.............................................................................................................. 8
INDICATIES.......................................................................................................................... 8
BIJWERKINGEN..................................................................................................................... 8
GI................................................................................................................................. 9
BP................................................................................................................................. 9
Renaal en CV................................................................................................................ 9
Overgevoeligheidsreacties.........................................................................................10
Hepatotoxiciteit en hematologische toxiciteit............................................................10
CONTRA-INDICATIES EN RISICOPOPULATIES...............................................................................10
INTERACTIE....................................................................................................................... 10
PRAKTIJK: KIEZEN VAN NSAID.............................................................................................. 11
VERSCHILLENDE GROEPEN VAN NSAIDS..................................................................................11
salicylaten.................................................................................................................. 11
para-aminofenol derivaten......................................................................................... 12
indool- en arylazijnzuurderivaten...............................................................................13
arylpropionzuurderivaten........................................................................................... 14
oxicams...................................................................................................................... 14
pyrazolonderivaten.................................................................................................... 14
selectieve COX-2 inhibitoren (coxibs).........................................................................15
H2: GLUCOCORTICOÏDEN...............................................................................16
CHEMIE............................................................................................................................ 16
WERKINGSMECHANISME....................................................................................................... 16
FARMACOKINETIEK.............................................................................................................. 17
FARMACODYNAMIEK............................................................................................................ 18
INDICATIES........................................................................................................................ 18
BIJWERKINGEN................................................................................................................... 19
RISICOPOPULATIES.............................................................................................................. 21
,H3: TWEEDELIJNS ANTI-REUMATISCHE GENEESMIDDELEN...............................22
DMARDS......................................................................................................................... 22
csDMARDs.................................................................................................................. 22
bDMARDs................................................................................................................... 23
tsDMARDs.................................................................................................................. 24
IMMUNOSUPPRESSIVA.......................................................................................................... 24
H4: MIGRAINE.............................................................................................. 27
BEHANDELING:................................................................................................................... 27
acute aanval............................................................................................................... 27
profylactische medicatie............................................................................................30
H5: JICHT..................................................................................................... 32
NSAID............................................................................................................................ 33
COLCHICINE...................................................................................................................... 33
GLUCOCORTICOÏDEN........................................................................................................... 33
URICOSTATICA................................................................................................................... 33
URICOSURICA.................................................................................................................... 34
RECOMBINANT URAAT OXIDASE............................................................................................. 35
CANAKINUMAB................................................................................................................... 35
H6: ANTIHISTAMINICA (TYPE I ALLERGIE).......................................................35
HISTAMINE........................................................................................................................ 36
H1-RECEPTORANTAGONISTEN............................................................................................... 38
H7: ASTMA................................................................................................... 42
ANTI-ASTMAGENEESMIDDELEN............................................................................................... 43
ß2-agonist.................................................................................................................. 44
Anticholinergica.......................................................................................................... 45
Corticosteroïden......................................................................................................... 45
Theofylline.................................................................................................................. 46
Leukotriënreceptor-antagonisten...............................................................................47
Andere........................................................................................................................ 47
Aandachtspuntsen...................................................................................................... 48
inhalatiesystemen...................................................................................................... 48
H8: ANAFYLACTISCHE REACTIES....................................................................49
H9: DIABETES MELLITUS...............................................................................50
NORMALE FYSIOLOGIE.......................................................................................................... 51
INSULINE EN ANALOGEN....................................................................................................... 53
ORALE ANTIDIABETICA......................................................................................................... 55
Biguaniden................................................................................................................. 55
Sulfamiden/sulfonylureumderivaten...........................................................................56
Gliniden...................................................................................................................... 57
Thiazolidinedionen of glitazonen................................................................................59
Alfa-gucosidase inhibitoren........................................................................................59
Gliptinen..................................................................................................................... 59
Gliflozinen.................................................................................................................. 60
INCRETINEMIMETICA............................................................................................................ 61
H10: OSTEOPOROSE.....................................................................................62
NIET-FARMACOLOGISCHE OPTIES............................................................................................ 63
, Calcium + vitamine D................................................................................................63
Vitamine D................................................................................................................. 64
FARMACOLOGISCHE OPTIES................................................................................................... 65
Bisfosfonaten............................................................................................................. 65
SERMs........................................................................................................................ 66
Teriparatide................................................................................................................ 67
Monoclonale AL: denosumab en romosozumab..........................................................67
H11: KANKER............................................................................................... 68
INLEIDING......................................................................................................................... 68
KANKERTHERAPIE............................................................................................................... 69
Principes..................................................................................................................... 69
Terminologie.............................................................................................................. 69
Nevenwerkingen........................................................................................................ 70
Stoffen....................................................................................................................... 70
H12: SUPPORTIEVE THERAPIE BIJ KANKERBEHANDELNG.................................76
RECOMBINANT ERYTHROEPOËTINE.......................................................................................... 76
MELOÏDE GROEIFACTOR, G-CSF............................................................................................ 77
PROFYLACTISCHE ANTI-EMETICA............................................................................................. 78
BOTMETASTASEN................................................................................................................ 78
H13: PALLIATIEVE EN TERMINALE ZORG.........................................................78
INLEIDING......................................................................................................................... 78
SYMPTOOMCONTROLE PALLIATIEVE ZORG.................................................................................79
MEDICATIETOEDIENINGSROUTES............................................................................................ 84
PALLIATIEVE SEDATIE........................................................................................................... 86
EUTHANASIE...................................................................................................................... 86
H14: GI STELSEL........................................................................................... 87
ACID-PEPTIC DISEASE........................................................................................................... 87
H2-receptorantagonisten...........................................................................................87
Protonpompinhibitoren (PPI).......................................................................................88
Misoprostol................................................................................................................. 89
Antacida..................................................................................................................... 89
antibiotica.................................................................................................................. 90
(GASTRO)-PROKINETICA....................................................................................................... 90
Dopamine-2-receptorantagonisten.............................................................................90
Cisapride.................................................................................................................... 91
ANTI-EMETICA.................................................................................................................... 91
PANCREASENZYM-SUBSTITUUT............................................................................................... 92
LAXANTIA......................................................................................................................... 92
ANTI-DIARRHEÏCA............................................................................................................... 93
INFLAMMATOIR DARMLIJDEN (IBD)......................................................................................... 93
BEHANDELING VAN INFESTATIE MET WORMEN...........................................................................94
INLEIDING: AUTACOÏDEN BIJ INFLAMMATIE EN ALLERGIE
Autacoïden = endogene stoffen die antwoorden op weefselbeschadiging (zelf-
remedie)
o Lokale hormonen
, o Kort halfleven
o Autocrien (op zelfde cel) of paracrien (op nabijgelegen cellen)
o Processen: ontsteking, allergie
o Stoffen
NT (vb serotonine, histamine)
Peptiden (vb bradykinine, angiotensine II, VIP)
Vetzuurderivaten (vb prostanoïden = autocoïden betrokken bij
inflammatie, PAF)
Anorganische moleculen (NO)
Eicosanoïden
o = autacoïden gevormd door oxidatie van membraangebonden poly-
onverzadigde vetzuren
o = prostanoïden en leukotriënen
Via COX: vorming prostanoïden (= prostaglandines en
tromboxanen) uit arachidonzuur
Via lipoxygenase: vorming leukotriënen
Prostanoïden
o = prostaglandines en tromboxanen
o Effecten (hieruit kan men bijwerkingen van NSAID’s raden)
Hersenen
Verhoging lichaamstemperatuur
Stimulatie PGE2 door IL-1
Luchtwegen
Bronchodilatatie door PGE2 en PGI2
Bronchoconstrictie door PGF2alfa en TXA2
Reproductie-orgaan
Vrouw
o Menstruatie: meer prostaglandins die contractie
veroorzaken pijn
o Abortus: prostaglandines gebruikt
o Bevalling: contracties en cervixrijping NSAID:
premature arbeid onderdrukken
Man
o Prostaglandines in semen rol conceptie en
infertiliteit
o Erectie: PGE2 via relaxatie van gladde spieren
Bloedvaten: BALANS
PGI2: remt BP aggregatie
TXA2: stimuleert BP aggregatie
Cave: rokers onevenwicht: minder PGI2 en meer TXA1
waardoor meer constrictie
Maag: BESCHERMEND
PGE2 en PGI2
o Inhibitie maagzuur
o Flow maagwand door vrijstelling NO
o Mucus maagwand
In utero
PGE2 en PGI2 zorgen voor normale circulatie tussen linker en
rechter bloedsomloop van ongeboren kind
Nier
PGE2 en PGI2: dilatatie afferente arteriolen
