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Samenvatting farmacologie: anti-emetica
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Samenvatting farmacologie: anti-emetica
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Gastro-intestinaal stelsel: anti-emetica
• braken = emesis
• GM tegen braken = anti-emetica
• gestuurd door braakcentrum (hersenstam)
• Braakcentrum krijgt info van allerlei gebieden uit het lichaam:
- hersenschors (emotionele toestanden: braken)
- evenwichtsorgaan (reisziekte)
- maag- en darmen (via nervus vagus)
- “Chemoreceptor Trigger Zone” (bv. chemotherapeutica, metabole problemen)
Braakreflex
• Verschillende signaalstoffen (neurotransmitters) spelen
een rol bij het activeren van de braakreflex:
- dopamine
- serotonine (5-HT)
- histamine
- ‘substance P’
- Deze signaalstoffen binden op hun
overeenkomstige receptor (‘sleutel in slot’
systeem):
- dopamine receptor (D2)
- serotonine receptor (5-HT3)
- histamine receptor (H1)
- Neurokinine receptor (NK1)
, Anti-emetica
• Om braken te verminderen willen activatie van het braakcentrum voorkomen
receptoren die leiden tot activatie van het braakcentrum blokkeren
Geneesmiddelen die receptoren blokkeren zijn antagonisten
1. dopamine receptor (D2) antagonisten
2. serotonine receptor (5-HT3) antagonisten
3. histamine receptor (H1) antagonisten
4. Neurokinine receptor (NK1) antagonisten
D2 antagonisten
blokkeren van de perifere dopamine receptoren
Domperidone (Motilium®)
= D2 antagonist: blokkeren dopamine receptoren
- in chemoreceptor-trigger zone
- in spijsverteringstelsel
dopamine = rem op beweging spijsverteringstelsel
door blokkeren dopamine-receptoren valt rem weg en de beweging
van de maag neemt toe
gaat niet doorheen bloedhersen-barrière: dit is belangrijk in verband
met bijwerkingen
Metoclopramide (Primperan®)
= D2 antagonist: blokkeren dopamine receptoren in spijsverteringsstelsel en chemoreceptor –trigger
zone
gaat WEL doorheen bloedhersen-barrière: kan bewegingsstoornissen geven
In hoge dosis is metoclopramide ook een 5-HT3 antagonist: blokkeren serotonine receptoren
in chemoreceptor-trigger zone
• Domperidone en metoclopramide doen de beweeglijkheid van de maag toenemen
Gastroprokinetica
Droperidol
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