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Samenvatting Farmacologie - deel 5
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Dit document bevat alle hoofdstukken van deel 5 Farmacologie. Dit vak werd gegeven door prof. de Hoon en prof. Casteels.
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INHOUDDEEL 5 ..................................................................................................................................................................... 9
Inleiding................................................................................................................................................................... 9
Fysiologische effecten van prostanoïden ............................................................................................................ 9
Prostaglandines en inflammatie ....................................................................................................................... 10
Hoofdstuk 1: niet-steroïdale anti-inflammatoire geneesmiddelen (NSAID) ......................................................... 11
Structuur ........................................................................................................................................................... 11
Werkingsmechanisme ....................................................................................................................................... 11
Farmacokinetiek ................................................................................................................................................ 11
Farmacodynamiek ............................................................................................................................................. 12
Indicaties ........................................................................................................................................................... 12
Bijwerkingen ..................................................................................................................................................... 12
Gastro-intestinaal.......................................................................................................................................... 12
Bloedplaatjes................................................................................................................................................. 12
Renaal en cardiovasculair.............................................................................................................................. 12
Overgevoeligheidsreacties ............................................................................................................................ 13
Hepatotoxiciteit en hematologische toxiciteit .............................................................................................. 13
Interacties ......................................................................................................................................................... 13
Praktijk: keuze NSAID ........................................................................................................................................ 13
Individuele groepen NSAID ............................................................................................................................... 13
Salicylaten ..................................................................................................................................................... 13
Typische effecten ...................................................................................................................................... 13
Contra-indicaties ....................................................................................................................................... 14
Klinisch gebruik ......................................................................................................................................... 14
Intoxicatie.................................................................................................................................................. 14
Aspirine bij electieve chirurgie .................................................................................................................. 14
Para-aminofenol derivaten ........................................................................................................................... 14
Klinisch gebruik ......................................................................................................................................... 14
Farmacokinetiek ........................................................................................................................................ 15
Toxiciteit .................................................................................................................................................... 15
Indool- en arylazijnzuurderivaten ................................................................................................................. 15
Arylpropionzuurderivaten ............................................................................................................................. 16
Oxicams ......................................................................................................................................................... 16
Pyrazolonderivaten ....................................................................................................................................... 16
Selectieve COX-2 inhibitoren ........................................................................................................................ 16
Hoofdstuk 2: glucocorticoïden .............................................................................................................................. 17
1
, Inleiding............................................................................................................................................................. 17
Producten .......................................................................................................................................................... 17
Werkingsmechanisme ....................................................................................................................................... 17
Farmacokinetiek ................................................................................................................................................ 18
Farmacodynamiek ............................................................................................................................................. 18
Effecten op witte bloedcellen ....................................................................................................................... 18
Effecten op ontstekingsmediatoren.............................................................................................................. 18
Indicaties ........................................................................................................................................................... 19
Richtlijnen behandeling met glucocorticoïden ................................................................................................. 19
Bijwerkingen/ongewenste effecten .................................................................................................................. 19
Metabole effecten ........................................................................................................................................ 19
Feedback effecten ......................................................................................................................................... 20
Effecten op mesenchymale cellen ................................................................................................................ 20
Anti-inflammatoir en immuunsuppressief effect .......................................................................................... 20
Effecten in centraal zenuwstelsel (CZS) ........................................................................................................ 20
Andere ........................................................................................................................................................... 20
Risicopopulaties ................................................................................................................................................ 21
Hoofdstuk 3: tweede lijns anti-reumatische geneesmiddelen ............................................................................. 22
Inleiding............................................................................................................................................................. 22
Disease Modifying Antirheumatic Drugs (DMARDs) ......................................................................................... 22
Conventionele synthetische small molecule DMARDs (csDMARDs) ............................................................. 22
Methotrexaat (MTX) ................................................................................................................................. 22
Sulfasalazine .............................................................................................................................................. 23
Hydroxychloroquine .................................................................................................................................. 23
Leflunomide .............................................................................................................................................. 23
Biological DMARDs (bDMARDs) .................................................................................................................... 23
Targeted synthetic DMARDs (tsDMARDs) ..................................................................................................... 24
Andere immunomodulatoren ........................................................................................................................... 24
Ciclosporine ................................................................................................................................................... 24
Tacrolimus, sirolimus en derivaten ............................................................................................................... 24
Azathioprine .................................................................................................................................................. 25
Mycofenolaatmofetil..................................................................................................................................... 25
Monoclonale antistoffen ............................................................................................................................... 25
Hoofdstuk 4: farmacotherapie van migraine ........................................................................................................ 26
Medicijnen om aanval te couperen .................................................................................................................. 26
Niet-specifieke anti-migraine geneesmiddelen ............................................................................................ 26
Specifieke anti-migraine geneesmiddelen .................................................................................................... 27
2
, Moederkoornalkaloïden............................................................................................................................ 27
Triptanen ................................................................................................................................................... 27
Richtlijnen bij behandeling van migraine .......................................................................................................... 28
Profylactische therapie ..................................................................................................................................... 28
Hoofdstuk 5: farmacotherapie van jicht ............................................................................................................... 29
Inleiding............................................................................................................................................................. 29
NSAID ................................................................................................................................................................ 29
Colchicine .......................................................................................................................................................... 29
Glucocorticoïden ............................................................................................................................................... 30
Urostatica: allopurinol, febuxostat ................................................................................................................... 30
Uricosurica: probenecid .................................................................................................................................... 30
Recombinant uraat oxidase .............................................................................................................................. 31
Canakinumab .................................................................................................................................................... 31
Hoofdstuk 6: farmacotherapie van hooikoorts, urticaria, angio-oedeem: antihistaminica (type I allergie)......... 32
Inleiding............................................................................................................................................................. 32
Histamine .......................................................................................................................................................... 32
Synthese, distributie, vrijstelling, metabolisme ............................................................................................ 32
Farmacologische effecten ............................................................................................................................. 32
H1-receptor antagonisten.................................................................................................................................. 33
Eigenschappen, structuur, werkingsmechanisme ......................................................................................... 33
Farmacokinetiek ............................................................................................................................................ 33
Farmacodynamiek ......................................................................................................................................... 34
Indicaties ....................................................................................................................................................... 34
Bijwerkingen/ongewenste effecten .............................................................................................................. 34
Interacties ..................................................................................................................................................... 34
Bijzonderheden in verband met behandeling van urticaria .......................................................................... 35
Bijzonderheden in verband met behandeling van seizoensgebonden allergische rhino-conjunctivitis ....... 35
H2-receptor antagonisten.................................................................................................................................. 35
Hoofdstuk 7: farmacotherapie van astma ............................................................................................................ 36
Inleiding............................................................................................................................................................. 36
Astma stadia .................................................................................................................................................. 36
Behandelingstappen ..................................................................................................................................... 36
Anti-astma geneesmiddelen ............................................................................................................................. 36
Kortwerkende β2-mimetica ........................................................................................................................... 37
Werkingsmechanisme ............................................................................................................................... 37
Gebruik ...................................................................................................................................................... 37
Bijwerkingen/ongewenste effecten .......................................................................................................... 37
3
, Langwerkende β2-mimetica .......................................................................................................................... 37
Werkingsmechanisme ............................................................................................................................... 37
Gebruik ...................................................................................................................................................... 37
Corticosteroïden ........................................................................................................................................... 38
Werkingsmechanisme ............................................................................................................................... 38
Gebruik ...................................................................................................................................................... 38
Bijwerkingen/ongewenste effecten .......................................................................................................... 38
Theofylline..................................................................................................................................................... 38
Werkingsmechanisme ............................................................................................................................... 38
Gebruik ...................................................................................................................................................... 38
Bijwerkingen/ongewenste effecten .......................................................................................................... 39
Anti-cholinergica ........................................................................................................................................... 39
Werkingsmechanisme ............................................................................................................................... 39
Gebruik ...................................................................................................................................................... 39
Bijwerkingen/ongewenste effecten .......................................................................................................... 39
Leukotrieenreceptor antagonisten ............................................................................................................... 39
Werkingsmechanisme ............................................................................................................................... 39
Gebruik ...................................................................................................................................................... 40
Bijwerkingen/ongewenste effecten .......................................................................................................... 40
Andere geneesmiddelen ............................................................................................................................... 40
Aandachtspunten .......................................................................................................................................... 40
Inhalatiesystemen ......................................................................................................................................... 40
Hoofdstuk 8: farmacotherapie van anafylactische reacties .................................................................................. 41
Inleiding............................................................................................................................................................. 41
Symptomen ....................................................................................................................................................... 41
Oorzaak ............................................................................................................................................................. 41
Behandeling ...................................................................................................................................................... 41
Hoofdstuk 9: farmacotherapie van diabetes mellitus ........................................................................................... 43
Inleiding............................................................................................................................................................. 43
Insuline en analogen ......................................................................................................................................... 43
Structuur, vrijstelling, werking, effecten ....................................................................................................... 43
Farmacokinetiek ............................................................................................................................................ 44
Indicaties ....................................................................................................................................................... 44
Bijwerkingen/ongewenste effecten .............................................................................................................. 45
Orale diabetica .................................................................................................................................................. 45
Biguaniden .................................................................................................................................................... 45
Structuur, werking..................................................................................................................................... 45
4
, Farmacokinetiek ........................................................................................................................................ 45
Farmacodynamiek ..................................................................................................................................... 45
Indicaties ................................................................................................................................................... 45
Bijwerkingen/ongewenste effecten .......................................................................................................... 45
Sulfonylureumderivaten (sulfamiden) .......................................................................................................... 45
Structuur, werking..................................................................................................................................... 45
Farmacokinetiek ........................................................................................................................................ 46
Farmacodynamiek ..................................................................................................................................... 46
Indicaties ................................................................................................................................................... 46
Bijwerkingen/ongewenste effecten .......................................................................................................... 46
Interacties ................................................................................................................................................. 46
Gliniden ......................................................................................................................................................... 46
Thiazolidinedionen (glitazonen) .................................................................................................................... 46
Alfa-glucosidase inhibitoren.......................................................................................................................... 47
Gliptinen ........................................................................................................................................................ 47
Gliflozinen (SGLT2-inhibitoren) ..................................................................................................................... 47
Incretinemimetica (GLP..................................................................................................................................... 48
Hoofdstuk 10: farmacotherapie en preventie van osteoporose ........................................................................... 49
Inleiding............................................................................................................................................................. 49
Calcium.............................................................................................................................................................. 50
Vitamine D......................................................................................................................................................... 50
Bisfosfonaten .................................................................................................................................................... 50
Werkingsmechanisme ................................................................................................................................... 50
Farmacokinetiek ............................................................................................................................................ 51
Indicaties ....................................................................................................................................................... 51
Bijwerkingen/ongewenste effecten .............................................................................................................. 51
Selectieve oestrogeenreceptor modulatoren (SERM) ...................................................................................... 51
Werkingsmechanisme ................................................................................................................................... 51
Indicaties ....................................................................................................................................................... 51
Bijwerkingen/ongewenste effecten .............................................................................................................. 51
Teriparatide ....................................................................................................................................................... 52
Monoclonale antilichamen: denosumab, romosozumab ................................................................................. 52
Hoofdstuk 11: farmacotherapie van kanker ......................................................................................................... 53
Inleiding............................................................................................................................................................. 53
Terminologie ................................................................................................................................................. 53
Kankertherapie.................................................................................................................................................. 54
Bijwerkingen/ongewenste effecten en toxiciteit .......................................................................................... 54
5
, Methotrexaat (MTX) ..................................................................................................................................... 54
Plantderivaten/antimitotica: taxanen ........................................................................................................... 55
Specifieke cytostatica .................................................................................................................................... 55
Hormonale stoffen ........................................................................................................................................ 55
Glucocorticoïden ....................................................................................................................................... 55
Gonadotropine-releasing hormoon (GnRH) .............................................................................................. 55
Somatostatine analogen ........................................................................................................................... 55
Anti-oestrogenen ...................................................................................................................................... 56
Immuuntherapie ............................................................................................................................................... 56
Monoklonale antilichamen ........................................................................................................................... 56
Checkpoint inhibitoren (CI) ........................................................................................................................... 57
Tyrosine kinase inhibitoren ........................................................................................................................... 57
Specifieke biologicals .................................................................................................................................... 57
Hoofdstuk 12: supportieve therapie bij kankerbehandeling ................................................................................ 58
Botmetastasen .................................................................................................................................................. 58
Epoëtine ............................................................................................................................................................ 58
Myeloïde groeifactor, G-CSF ............................................................................................................................. 58
Anti-emetica ...................................................................................................................................................... 59
Aprepitant – netupitant .................................................................................................................................... 59
Hoofdstuk 13: farmacologische aspecten in palliatieve en terminale zorg .......................................................... 60
Inleiding............................................................................................................................................................. 60
Symptoomcontrole ........................................................................................................................................... 61
Pijn ................................................................................................................................................................ 61
Inschatten pijn........................................................................................................................................... 61
Inschatten patiënt en omgeving ............................................................................................................... 61
Principes .................................................................................................................................................... 61
Gastro-intestinale problemen ....................................................................................................................... 62
Nausea en braken ..................................................................................................................................... 62
Diarree....................................................................................................................................................... 62
Obstructie.................................................................................................................................................. 62
Obstipatie (constipatie)............................................................................................................................. 63
Dehydratatie ............................................................................................................................................. 63
Respiratoire problemen ................................................................................................................................ 63
Dyspnee..................................................................................................................................................... 63
Stridor ....................................................................................................................................................... 64
Doodsreutel (death rattle) ........................................................................................................................ 64
Neurologische problemen............................................................................................................................. 64
6
, Delier (verwardheid) ................................................................................................................................. 64
Epilepsie .................................................................................................................................................... 64
Angst ......................................................................................................................................................... 64
Medicatie toedieningsroutes ............................................................................................................................ 64
Palliatieve sedatie ............................................................................................................................................. 65
Euthanasie ......................................................................................................................................................... 65
Hoofdstuk 14: farmacotherapie van gastro-intestinaal stelsel ............................................................................. 66
Farmacotherapie van peptische aandoeningen: ulcera en gastroesophagal reflux disease (GERD) ................ 66
H2-receptor antagonisten.............................................................................................................................. 66
Eigenschappen, structuur, werkingsmechanisme ..................................................................................... 66
Farmacokinetiek ........................................................................................................................................ 66
Farmacodynamiek ..................................................................................................................................... 66
Indicaties ................................................................................................................................................... 66
Interacties ................................................................................................................................................. 66
Protonpomp inhibitoren (PPI) ....................................................................................................................... 66
Eigenschappen, structuur, werkingsmechanisme ..................................................................................... 66
Farmacokinetiek en farmacodynamiek ..................................................................................................... 67
Indicaties ................................................................................................................................................... 67
Bijwerkingen/ongewenste effecten .......................................................................................................... 67
Interacties ................................................................................................................................................. 67
Misoprostol ................................................................................................................................................... 67
Antacida ........................................................................................................................................................ 67
Antibiotica ..................................................................................................................................................... 67
GAstro-prokinetica ............................................................................................................................................ 68
Dopamine-2 receptorantagonisten ............................................................................................................... 68
Cisapride........................................................................................................................................................ 68
Anti-emetica ...................................................................................................................................................... 68
5-HT3 antagonisten........................................................................................................................................ 68
Glucocorticoïden ........................................................................................................................................... 68
Fenothiazines, butyrofenonen ...................................................................................................................... 68
Prokinetica .................................................................................................................................................... 68
H1-antihistaminica ......................................................................................................................................... 69
Anticholinergica ............................................................................................................................................ 69
Neurokininereceptor antagonisten ............................................................................................................... 69
Pancreasenzym-substituut ............................................................................................................................ 69
Laxantia ............................................................................................................................................................. 69
Bulk-laxantia, osmotische laxantia ................................................................................................................ 69
7
, Lokaal-irriterende, stimulerende laxantia ..................................................................................................... 69
Prucalopride .................................................................................................................................................. 69
Anti-diarrheïca .................................................................................................................................................. 70
Farmaca inflammatoir darmlijden (IBD)............................................................................................................ 70
Farmaca infestatie wormen .............................................................................................................................. 70
Addendum 1: geneesmiddelen en QT-verlenging................................................................................................. 71
8
,FARMACOLOGIE
DEEL 5
INLEIDING
Aurtocaïden = endogene stoffen die een belangrijke rol spelen in normale celhomeostase en in
pathofysiologische processen als antwoord op weefselschade
- Ontstekingsprocessen
- Allergische reacties
- Stoffen: NT, peptiden, VZ-derivaten, anorganische moleculen
Autocriene effecten = effect uitoefenen op de cel, die zelf de hormonen afscheidt
Paracriene effecten = effect uitoefen op nabij gelegen cellen, dan deze die hormonen afscheiden
FYSIOLOGISCHE EFFECTEN VAN PROSTANOÏDEN
Cyclo-oxygenase (COX)
- COX-1: constitutief enzyme dat tot expressie komt in meeste organen en belangrijke functie in orgaan
homeostase
- COX-2: induceerbare enzyme dat tot expressie komt door tussenkomst van LPS en cytokines, in cellen
van immuunsysteem en inflammatoire cellen
Cardiovasculair
- PGE2 en PGI2
o Relaxatie gladde spiercellen → daling bp en stijging perfusie
o Openhouden ductus arteriosus (ductus van Botalli) in utero
- PGF2α en TXA2
o Vasoconstrictie → stijging bp
Bloedplaatjes
- PGI2: inhibitie BP, > endotheel → remmen aggregatie
- TXA2: stimulatie BP, > BP → versterken aggregatie
Gastro-intestinaal
- PGE2 en PGI2: cytoprotectief
o Inhibitie maagzuursecretie
o Stimulatie mucussecretie
o Stijging mucosa doorbloeding (via vrijzetting NO)
Renaal
- PGE2 en PGI2
o Dilatatie afferente arteriolen → stijging renale doorbloeding
o In situaties met minder renale doorbloeding: OZS tonus, Ang II, nierinsufficiëntie
o Controle van water- en zoutexcretie via veranderingen renale perfusie
-
9
, - TXA2
o Constrictie afferente arteriolen → daling renale doorbloeding
Reproductieve organen
- Mannen:
o PG: conceptie, fertiliteit
o PGE2: relaxatie gladde spieren → erectie
- Vrouwen:
o PG
▪ Uteruscontracties tijdens menstruatie → dysmenorree, koliekpijnen
▪ Inductie abortus
▪ Cervixrijping en onderhouden uteruscontracties bij bevalling
o Inhibitie COX → onderdrukken premature arbeid (niet gewenst indien voldragen
zwangerschap)
Luchtwegen
- PGE2 en PGI2: bronchodilatatie
- PGF2α en TXA2: bronchoconstrictie
Centraal zenuwstelsel (CZS)
- PGE2
o Stijging temperatuur
o Stimulatie door IL-1 (endogeen pyrogeen) → vrijstelling IL-1 bij inflammatie
PROSTAGLANDINES EN INFLAMMATIE
Verschillende stimuli kunnen een inflammatoire reactie veroorzaken: mechanisch, warmte, hormonaal,
bacterieel…)
- Symptomen:
o Rubor (roodheid): PGE2 en PGI2 → vasodilatatie
o Calor (warmte): PGE2 en PGI2 → vasodilatatie
o Dolor (pijn): PG stimuleren gevoeligheid van afferente zenuwen voor bradykinine (BK) en
histamine → hyperalgesie
o Tumor (oedeem): PGE2 en PGI2 → vasodilatatie
- Acute fase
o Verhoogde capillaire permeabiliteit en vasodilatatie
o Vrijstelling autacoïden tgv weefselschade: histamine, serotonine, bradykinine, PG,
leukotriënen (LT), neuropeptiden
- Subacute fase
o Infiltratie leukocyten en macrofagen → neutralisatie toxisch agens
o Leukotriënen, PAF, cytokines (IL-1, TNF)
▪ Koorts, anorexie, mobilisatie leukocyten, inductie COX en LOX, inductie expressie
adhesie-moleculen, activatie T- en B-cellen, productie cytokines
- Chronische fase
o Fibrose
o Leukotriënen, PAF, cytokines (IL-1, TNF)
▪ Koorts, anorexie, mobilisatie leukocyten, inductie COX en LOX, inductie expressie
adhesie-moleculen, activatie T- en B-cellen, productie cytokines
10
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