Farmacologie samenvatting + lesnotities

FARMACOLOGIE
3e Bachelor Farmacie




ACADEMIEJAAR 2024-2025

,INHOUDSOPGAVE

Hoofdstuk I: Autonomic nervous system................................................................................................................ 8
1. Presynaptische regulatie van transmitter-release van noradrenerge en cholinerge zenuwuiteinden .......... 8
2. Neurochemische transmissie .......................................................................................................................... 8
3. Cholinerge transmissie ................................................................................................................................... 9
3.1 Stimulatie van het parasympatisch zenuwstelstel.................................................................................. 10
4. Noradrenerge transmissie ............................................................................................................................ 13
4.1 Adrenoreceptor agonisten...................................................................................................................... 13
4.2 Adrenoreceptor antagonisten ................................................................................................................ 15
4.3 Drugs met invloed op noradrenaline-synthese ...................................................................................... 17
4.4 Drugs met invloed op noradrenaline vrijstelling, neuronale (re)uptake of degradatie .......................... 17
Hoofdstuk II: Cardiovasculair systeem.................................................................................................................. 18
1. Antihypertensieve drugs ............................................................................................................................... 18
1.1 Antihypertensieve drugs met centrale werking ..................................................................................... 18
1.2 Vasodilatoren .......................................................................................................................................... 18
2. Anti-anginale drugs ....................................................................................................................................... 19
2.1 Nitrovasodilatoren (nitraten en molsidomine) ....................................................................................... 19
3. Drugs gebruikt voor hartfalen ...................................................................................................................... 19
3.1 Digitalis glycosides .................................................................................................................................. 19
3.2 Fosfodiësterase-3 inhibitoren ................................................................................................................. 20
3.3 Sabcubitril/valsartan ............................................................................................................................... 20
3.4 Calcium antagonisten ............................................................................................................................. 20
3.5 Het renine-angiotensine systeem ........................................................................................................... 21
3.6 Diuretica ................................................................................................................................................. 22
4. Anti-arytmische drugs ................................................................................................................................... 24
4.1 Klasse 1: snelle natriumkanaalblokkers .................................................................................................. 25
4.2 Klasse 2: beta-blokkers ........................................................................................................................... 25
4.3 Klasse 3: kaliumkanaalblokkers .............................................................................................................. 26
4.4 Klasse 4: Calciumkanaalblokker .............................................................................................................. 26
5. Adenosine: IV ................................................................................................................................................ 26
6. Hypolipidemie drugs - lipide verlaagdende drugs ........................................................................................ 26
6.1 Statines ................................................................................................................................................... 27
6.2. Fibraten.................................................................................................................................................. 27
6.3 Drugs die cholesterol-absorptie inhiberen ............................................................................................. 27
6.4 Nicotinezuur (niacine) ............................................................................................................................. 28
6.5 Omega-3-vetten ...................................................................................................................................... 28


1

, 6.6 PCSK9-inhibitoren ................................................................................................................................... 28
6.7 Inclisiran .................................................................................................................................................. 28
6.8 Bempedoic acid ...................................................................................................................................... 28
6.9 Combinaties ............................................................................................................................................ 28
7. Antithrombotische drugs .............................................................................................................................. 29
7.1 Anti-aggregantia en antiplaatjes drugs ................................................................................................... 29
7.2 Anticoagulantia ....................................................................................................................................... 30
7.3 Thrombolytica, fibrinolytische drugs ...................................................................................................... 32
Hoofdstuk III: centraal zenuwstelsel..................................................................................................................... 33
1. Sedativa, hypnotica en anxiolytische drugs .................................................................................................. 33
1.1 Benzodiazepines ..................................................................................................................................... 33
1.2 Z-producten: zolpidem en zopiclon ........................................................................................................ 34
1.3 Barbituraten............................................................................................................................................ 34
1.4 Melatonine ............................................................................................................................................. 34
1.5 Plant-gebaseerde producten .................................................................................................................. 34
2. Antidepressiva .............................................................................................................................................. 35
2.1 reuptake inhibitoren, monoamine uptake inhibitoren ........................................................................... 35
2.2 Sint-janskruid .......................................................................................................................................... 36
2.3 Monoamine oxidase inhibitors, MAO i ................................................................................................... 36
2.4 Antidepressiva met actie op neuroreceptoren ....................................................................................... 36
2.5 Vortioxetine ............................................................................................................................................ 36
2.6 Esketamine ............................................................................................................................................. 37
2.7 Lithium .................................................................................................................................................... 37
3. Antipsychotische stoffen (vroeger: neuroleptica) ........................................................................................ 37
4. Centrale stimulantia ..................................................................................................................................... 39
4.1 Amfetamines en gerelateerde drugs ...................................................................................................... 39
4.2 Atomoxetine ........................................................................................................................................... 39
4.3 Cocaïne ................................................................................................................................................... 40
5. Drugs gebruikt indien sprake van afhankelijkheid ........................................................................................ 40
5.1 Drugs gebruikt bij alcoholgebruik ........................................................................................................... 40
5.2 Drugs gebruikt bij tabakmisbruik ............................................................................................................ 40
6. Drugs bij de behandeling van Parkinson ....................................................................................................... 41
6.1 L-DOPA + DDC inhibitor .......................................................................................................................... 41
6.2 Catechol-o-methyl-transferase (COMT) inhibitoren ............................................................................... 41
6.3 Mono-amino-oxidase b (MAO b) inhibitoren ......................................................................................... 41
6.4 Dopamine agonisten ............................................................................................................................... 42
6.5 Muscarinerge antagonisten .................................................................................................................... 42

2

, 7. Anti-epileptica .............................................................................................................................................. 42
7.1 Klassieke anti-epileptische drugs ............................................................................................................ 43
7.2 Nieuwe generatie anti-epileptische drugs .............................................................................................. 44
7.3 Teratogeniciteit van klassieke anti-epileptische drugs ........................................................................... 45
8. Drugs gebruikt bij spasmen .......................................................................................................................... 45
8.1 Centraal werkende spierrelaxantia ......................................................................................................... 45
8.2 Perifeer werkende spierrelaxantia ......................................................................................................... 45
9. Drugs gebruikt bij migraine .......................................................................................................................... 45
9.1 Drugs gebruikt bij acute migraine aanvallen .......................................................................................... 46
9.2 Profylactische antimigraine drugs .......................................................................................................... 46
Hoofdstuk IV: Gastro-intestinaal stelsel ............................................................................................................... 47
1. Drugs gebruikt voor gastrische en duodenale pathologie ............................................................................ 47
1.1 Inhibitoren van maagzuursecretie .......................................................................................................... 47
1.2 ANtacida ................................................................................................................................................. 49
2. Drugs gebruikt voor de lever-gal duct en pancreatische aandoeningen ...................................................... 49
2.1 Pancreatische enzymen .......................................................................................................................... 49
2.2 Ursodeoxycholic acid .............................................................................................................................. 49
3. Inflammatoire darmziekten .......................................................................................................................... 50
3.1 5-aminosalicylaten .................................................................................................................................. 51
3.2 Glucocorticoïden ..................................................................................................................................... 51
3.3 Immunosuppressiva................................................................................................................................ 51
3.4 Biologicals ............................................................................................................................................... 51
3.5 Proteïnekinase inhibitoren | 3.6 S1P (sfingosine-1-fosfaat) receptor modulator .................................. 51
4. Spasmolytica ................................................................................................................................................. 51
4.1 Anticholinergica (muscarine antagonisten) ............................................................................................ 51
4.2 Musculotrope spasmolytische stoffen .................................................................................................... 52
4.3 Peppermint en combinaties ................................................................................................................... 52
5. Anti-emetische drugs .................................................................................................................................... 52
5.1 Fasen van braken .................................................................................................................................... 52
5.2 regulatie van braken ............................................................................................................................... 52
6. Laxativa ......................................................................................................................................................... 55
6.1 Bulk-vormende laxativa .......................................................................................................................... 55
6.2 Lubricante laxativa .................................................................................................................................. 55
6.3 Osmotische laxativa ................................................................................................................................ 55
7. Antidiarree stoffen........................................................................................................................................ 56
7.1 Oral rehydration solutions ...................................................................................................................... 56
7.2 Adsobenten............................................................................................................................................. 57

3

, 7.3 Transit inhibitoren .................................................................................................................................. 57
7.4 Inhibitie van secreties ............................................................................................................................. 57
7.5 papaver somniferum .............................................................................................................................. 57
7.6 Probiotica ................................................................................................................................................ 57
Hoofdstuk V : Urogenitaal stelsel ......................................................................................................................... 58
1. Blaas dysfunctie ............................................................................................................................................ 58
1.1 Overactieve blaas ................................................................................................................................... 58
1.2 Stress incontinentie ................................................................................................................................ 58
1.3 Blaasatonie ............................................................................................................................................. 58
2. Benigne prostaathypertrofie ........................................................................................................................ 58
2.1 1 adrenoreceptor antagonist ............................................................................................................... 58
2.2 5-alfa-reductase inhibitoren ................................................................................................................... 58
3. Impotentie .................................................................................................................................................... 58
Hoofdstuk VI: Ademhalingsstelsel ........................................................................................................................ 59
1. Drugs voor respiratoire ziekten .................................................................................................................... 59
1.1 2 adrenoreceptor agonisten (1e lijnskeuze).......................................................................................... 59
1.2 Anticholinergica = muscarine receptor antagonsten .............................................................................. 60
1.3 Inhalatie glucocorticoïden ...................................................................................................................... 60
1.4 Cysteïnyl leukotriene receptor antagonist ............................................................................................. 61
1.5 Theophyline (xanthine drug) .................................................................................................................. 61
1.6 Natrium chromoglicaat ........................................................................................................................... 61
1.7 Monoklonaal antilichaam ....................................................................................................................... 62
2. Drugs gebruikt voor hoest ............................................................................................................................ 62
3. Mucolytica .................................................................................................................................................... 62
4. Expectorantia ................................................................................................................................................ 63
5. Rhinitis en sinusitis ....................................................................................................................................... 63
5.1 Systemische preparaat ........................................................................................................................... 63
5.2 Nasale preparaat .................................................................................................................................... 63
Hoofdstuk VII: pijn, koorts en inflammatie ........................................................................................................... 63
1. Cyclo-oxygenase inhibitoren......................................................................................................................... 63
1.1 NSAIDS .................................................................................................................................................... 64
1.4 COX2 selectieve NSAIDS ......................................................................................................................... 65
1.5 Bijwerkingen ........................................................................................................................................... 65
1.5 Paracetamol (acetaminophen) ............................................................................................................... 65
1.6 Acetylsalicylzuur ..................................................................................................................................... 65
2. Narcotische analgetische stoffen.................................................................................................................. 66



4

, 2.1 Pure agonist ............................................................................................................................................ 67
2.2 Partiële agonisten of gemengde agonist/antagonist .............................................................................. 67
2.3 Antagonisten........................................................................................................................................... 67
Hoofdstuk IX: Lokale anesthetica ......................................................................................................................... 68
Hoofdstuk X: Immunosuppressiva ........................................................................................................................ 68
1. Transplantatie ............................................................................................................................................... 68
2. Allergie .......................................................................................................................................................... 68
Hoofdstuk XI: Endocrien systeem ......................................................................................................................... 69
1. Antidiabetische drugs ................................................................................................................................... 69
1.1 Diabetes mellitus .................................................................................................................................... 69
2. Obesitas ........................................................................................................................................................ 73
2.1 GLP-1 agonisten ...................................................................................................................................... 73
2.2 GLP-1 / GIP dual incretine mimetica ....................................................................................................... 73
2.3 GLP-1 / glucagon dual receptor agonisten ............................................................................................. 73
2.4 Opkomende gewichtsverlies drugs ......................................................................................................... 73
3. Thyroïd .......................................................................................................................................................... 74
3.1 Thyroïde hormonen ................................................................................................................................ 74
3.2 Thyrostatische drugs............................................................................................................................... 74
3.3 Jodide ...................................................................................................................................................... 75
3.4 Radioactief jodide ................................................................................................................................... 75
4. Corticosteroïden ........................................................................................................................................... 75
5. Hypothalamus-hypofyse hormonen ............................................................................................................. 77
5.1 analogen van vasopressine ..................................................................................................................... 77
5.2 Groeihormoon, somatostatine en analogen .......................................................................................... 77
6. Geslachtshormonen en gerelateerde hormonen ......................................................................................... 78
6.1 Oestrogenen ........................................................................................................................................... 78
6.2 Selectieve oestrogeen receptor modulators (SERM) en anti-oestrogenen ............................................ 79
6.3 Aromatase inhibitoren ............................................................................................................................ 79
6.4 progesterons ........................................................................................................................................... 79
6.5 Homonale contraceptiva ........................................................................................................................ 80
6.6 ANdrogenen en anabolische steroïden .................................................................................................. 81
6.7 ANti-androgenen .................................................................................................................................... 82
6.8 Drugs die lactatie en hyperprolactinemie inhiberen .............................................................................. 83
6.9 Drugs met effect op uterus motiliteit ..................................................................................................... 83
Hoofdstuk XII: Osteo-articulaire aandoeningen ................................................................................................... 84
1. Antireumatische drugs.................................................................................................................................. 84
1.1 DMARD ................................................................................................................................................... 84

5

, 1.2 Biologicals (zie figuur) ............................................................................................................................. 85
2. Jicht ............................................................................................................................................................... 86
2.1 Acute therapie ........................................................................................................................................ 86
2.2 Onderhoudstherapie .............................................................................................................................. 86
3. Osteoporose en paget’s disease ................................................................................................................... 87
3.1 Calcium en vitamine D ............................................................................................................................ 87
3.2 Bisfosfonaten .......................................................................................................................................... 87
3.3 Selectieve oestrogeen receptor modulatoren (SERMs) (Raloxifen) ....................................................... 88
3.4 Denosumab ............................................................................................................................................. 88
3.5 Recombinant bijschildklierhormoon (Teriparatide) ............................................................................... 88
3.6 Calcitocine .............................................................................................................................................. 88
Hoofdstuk XIII: Kanker .......................................................................................................................................... 88
1. Evolutie van gerichte therapie ...................................................................................................................... 88
2. Cancer hallmarks: “new dimensions” ........................................................................................................... 89
2.1 Ongecontroleerde groei en overleving ................................................................................................... 89
2.2 Vermijden van celdood ........................................................................................................................... 90
2.3 ‘The next generation’ – verhinderen van immuunsysteem destructie .................................................. 92
Hoofdstuk XIV: Infecties ....................................................................................................................................... 94
1. Antimalaria drugs.......................................................................................................................................... 94
1.1 Chloroquine ............................................................................................................................................ 95
1.2 Quinine ................................................................................................................................................... 95
1.3 Mefloquine ............................................................................................................................................. 95
1.4 Folaat inhibitoren ................................................................................................................................... 96
1.5 Artemisinine ........................................................................................................................................... 96
1.6 Atovaquone ............................................................................................................................................ 96
1.7 Doxycycline ............................................................................................................................................. 96
1.8 Samenvatting .......................................................................................................................................... 96
2. Andere protozoale infecties ......................................................................................................................... 97
2.1 Giardiasis ................................................................................................................................................ 97
2.2 Amoebiasis .............................................................................................................................................. 97
2.3 Trichomoniasis ........................................................................................................................................ 97
2.4 Toxoplasmosis......................................................................................................................................... 98
3. Antihelminthica ............................................................................................................................................ 98
3.1 Benzimidazoles ....................................................................................................................................... 98
3.2 praziquantel ............................................................................................................................................ 99
3.3 Niclosamide ............................................................................................................................................ 99
3.4 Conclusies bij parasietinfecties ............................................................................................................... 99

6

, 4. Hepatitis B..................................................................................................................................................... 99
4.1 Nucleoside/Nucleotide analogen (NA) ................................................................................................. 100
4.2 Interferon.............................................................................................................................................. 101
4.3 Zwangerschap en ziektepreventie bij pasgeborenen ........................................................................... 101
5. Hepatitis C................................................................................................................................................... 101
5.1 NS5B inhibitoren ................................................................................................................................... 102
5.2 NS5A-remmers...................................................................................................................................... 102
5.3 NS3/4A-remmers .................................................................................................................................. 102
6. CMV infectie ............................................................................................................................................... 102
6.1 Ganciclovir ............................................................................................................................................ 103
6.2 Valganciclovir ........................................................................................................................................ 103
6.3 Foscarnet .............................................................................................................................................. 103
Hoofdstuk XV: Antidepressiva ............................................................................................................................ 103
Hoofdstuk XVI: Anti-epileptica ........................................................................................................................... 105
1. Wat is epilepsie ........................................................................................................................................... 105
2. Definities ..................................................................................................................................................... 105
3. Types aanvallen .......................................................................................................................................... 105
4. Prevalentie .................................................................................................................................................. 106
5. Indeling naargelang de oorzaak .................................................................................................................. 106
6. Differentiaaldiagnose ................................................................................................................................. 106
7. Behandeling ................................................................................................................................................ 106
8. Refractaire (of drug resistente) epilepsie ................................................................................................... 108
9. Neurostimulatie: targets en open/closed loop ........................................................................................... 109




7

,FARMACOLOGIE
HOOFDSTUK I: AUTONOMIC NERVOUS SYSTEM

Autonoom ZS:

• Sympatisch ZS: fight or flight + oiv stress (tachycardie, BD ↑, bronchodilatatie, pupildilatatie en
perifere weerstand ↑)
➔ Cholinerge banen lopen mee met sympaticus -> activatie sympaticus = zweten
➔ Bloedvaten: sympatisch bezenuwd
• Parasympatisch ZS: rust en vertering
• Processen beïnvloed door autonoom ZS: contractie/relaxatie v
gladde spieren, secreties, hartslag en energiemetabolisme

Sympaticus geactiveerd = parasympaticus geïnactiveerd (en omgekeerd)

Enterisch ZS (in darmen): intrisieke nervus plexus + ook beïnvloed door
extrinsiek ZS ((para)sympaticus)

Belangrijkste NT: acetylcholine, nordrenaline, (dopamine) en
(nordrenaline)

1. PRESYNAPTISCHE REGULATIE VAN TRANSMITTER -RELEASE VAN NORADRENERGE EN
CHOLINERGE ZENUWUITEINDEN

Speekselsecretie: bezenuwd door sympaticus en
parasympaticus

Sympatisch: NT = noradrenaline

• Presynaptische autoregulerende 2 rec: inhibitie
v eigen vrijstelling v noradrenaline
= homotrope interactie
• Cross-inhibitie vd acetylcholine-vezels
= heterotrope interactie

Parasympatisch: NT = acetylcholine

• Presynaptische autoregulerende muscarine en nicotine rec: inhibitie v eigen vrijstelling v acetylcholine
• Cross-inhibitie vd noradrenerge vezels

2. NEUROCHEMISCHE TRANSMISSIE

Op diffusie kunnen GM niet inwerken

Diffusie v precursor in zenuwuiteinde (1) -> Aanmaak v NT uit precursor (2) ->
Opstapeling vd NT in vesikels (3) -> Overmaat dat niet in vesikels past weer
afbreken (4) -> Depolariserend signaal (5) -> Opening Ca2+ kanalen en influx v Ca2+
(6) -> Versmelting vd vesikel met het membraan (7) -> Vrijstelling vd NT in de
synaptische spleet (8) -> Binden op postsynaptische of niet-neuronale rec (9) ->
Afbraak NT tot precursor (10) -> Rechtstreekse opname v NT door presynaptisch
neuron (11)

➔ Vele stadia waar GMen kunnen interfereren

8

, 3. CHOLINERGE TRANSMISSIE

Cholinerge neuronen: (para)sympathisch ZS

• Sympathisch: Postsynaptische nicotine receptor (uitzondering =
muscarine rec op zweetklieren)
• Parasympatisch: Postsynaptische nicotine receptor + muscarine
receptor
• Neuromusculaire junction: Nicotine receptoren

Figuur:

1. AcetylCoA + choline (mbv acetyltransferase) -> acetylcholine

2. Acetylcholine (mbv acetylcholinesterase) -> acetaat + choline

3. Heropname (= recyclage) v choline door presynaptisch neuron

NICOTINE RECEPTOR:

• Bestaat uit 5 verschillende subeenheden (soort subeenheden: afh v plaats v receptor)
• Ion kanaal (Na) binnenin receptor -> binding acetylcholine = opening kanaal
• OPM: Somatische nic receptor ≠ ganglion nic receptor
Nic receptoren thv ganglia w niet getarget door GMen, enkel die op spieren (bv. anesthesie)

MUSCARINE RECEPTOR:

• M1, M3 en M5: stimuleren Ca2+ release
• M2 en M4: inhibitie adenylaatcyclase -> cAMP↓
• Tragere transmissie dan nicotine receptor

Amanita muscaria (= paddenstoel): activeert parasympatisch ZS -> muscarinerge effecten

➔ Contractie gladde spieren (behalve bloedvaten), misselijkheid, braken, zweten, speeksel, speekselsecretie,
urinatie, ontlasting, bronchospasmen, bradycardie en hypotensie
➔ Wrm hypotensie als bloedvaten sympatisch w bezenuwd? Door exogene stimulatie wel mogelijk
Bloedvatwand opgebouwd uit endotheem (bevat musc rec) en omringd door gladde spieren (sympatisch
bezenuwd
 Exogeen muscarine -> muscarine rec -> stikstofmonoxide (NO) productie -> relaxatie gladde
spiercellen
➔ Antidotum tegen zwam : muscarine antagonist (bv. atropine) -> inhibitie parasympatisch ZS

Overstimulatie door te hoge dosis muscarine agonist => zeer toxische/overdreven effecten




9