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samenvatting farmacodynamiek

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Samenvatting van 12 pagina's voor het vak Farmacologie aan de UGent (gebaseerd op les)

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  • December 19, 2024
  • 12
  • 2023/2024
  • Summary
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FARMACODYNAMIEK
TARGET SITES OF PHARMACEURICALS




Target site: plaats waar GM effect moet uitoefenen

• Enkel ONGEBONDEN fractie kan reageren met target
• Normaal moet GM in organisme worden opgenomen en interactie aangaan met endogene
celbestanddelen om effect teweeg te brengen
o Meestal via eiwitten




IONKANALEN




• Voltage-afhankelijk
o Stimulus leidt tot depolarisatie met Na-influx en repolarisatie met K-efflux
• Mediatoren:
o Blokkers: permanente blok
o Modulatoren: ↑ of ↓ open-probabiliteit




ENZYMEN

• Mediatoren:
o Inhibitor: normale reactie geinhibeerd
o Vals substraat: abnormale metabolische productie
o Pro-drug: actieve GM produceren


• Voorbeeld: COX-enzymes
o COX 1 = consitutioneel
§ Cytoprotectief
• Beschermen maagmucosa
• Plaatjesaggregatie
§ Inhibitie door NSAIDs

, o COX 2 = induceerbaar
§ Inhibiteit ledit tot
• Minder inflammatie
• Minder pijn
• Minder koorts




TRANSPORTERS (CARRIERS)




• Mediatoren:
o Inhibitor: transport geblokkeerd
o Vals substraat: abnormale accumulatie
• Voorbeeld:
o GM die interfereert met reuptake neurotransmitter zorgt voor langer behoud
neurotransmitter in synaptische spleet




RECEPTOREN

Receptoren: endogene eiwitten waarmee endogene mediatoren een signaal overbrengen

• Agonist → receptor → transductie → cellulaire respons → orgaan respons
• Structuur complementair voor endogene en exogene stoffen
• Meestal in celmembraan gelokaliseerd
o Soms intracellulair




KWANTITATIEVE ASPECTEN VAN FARMACON-RECEPTOR INTERACTIES


AFFINITEIT

Affiniteit: mate van “gemakkelijkheid” waarmee GM bindt op receptor

• In evenwicht:
o KA: dissociatie-evenwichtsconstante in mol/l
§ Concentratie waarop 50% van de receptoren bezet is
o 1/KA: affiniteits-evenwichtsconstante
§ Hoe lager KA , hoe hoger de receptoraffiniteit

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