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Samenvatting geneesmiddelen: farmacokinetiek
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Een samenvatting van de besproken geneesmiddelen tijdens de lessen
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GM Acetylcholine
Receptor= cholinerge receptor
Acyclovir
>< herpes virus infectie
Zeer hydrofiel
Adefovir
Sterke tubulaire secretie
Nucleotide analoog
Actieve secretie in urine (OAT1/MRP4)
>< HIV -> afgekeurd voor niertoxiciteit: hOAT1: accumulatie in niertubulus
>< Hepatitis B -> goedgekeurd
Enkel lage concentraties
Adrenaline
Endogene ligand
Receptor= andrenerge receptor
=epinerfine
Lichaam in staat van verhoogde alertheid
Antipyrine
P-gp substraat
Aspirine (acetylsalicylzuur)
Pijnstillend
Koortswerend
Ontstekingsremmend
pKa=3.5
Astemizole
QT verlenging
H1-receptor antagonisten
><allergische reacties
Atazanavir
HIV protease inhibitor
+omeprazole: lagere conc. in plasma
pKa=5.25
[ ] in CSF < [ ] in plasma
Atenolol
β-blokker
matig tubulaire secretie
Atorvastatine
+rifampicine: meer eliminatie
Bosentan
endotheline receptor antagonist
>< pulmonaire art. hypertensive
Veroorzaakt cholestase ([galzouten]↑)
, Cefolexin
β –lactam antibioticum
Cimetidine
Histamine receptor blokker
Ciprofloxacine
Antibioticum
Sterke tubulaire secretie
+probenicid: verhoogde [plasma] door inhibitie OATs -> Cl r↓ -> meer blootstelling
Cisapride
QT verlenging
5-HT4-receptor antagonist
Cisplatin
Nefrotoxiciteit
Cimetidine biedt hiertegen bescherming -> competitie met receptor hOCT2
Clenbuterol
β2-sympathomimeticum (bronchodilatatie)
Anabolische werking
Cyclosporine A
bij afstotingsverschijnselen
bij orgaantransplantatie
immunosuppressief GM
veroorzaakt cholestase
Danazol
BCS klasse 2
+voedsel: beter oplosbaar (meer gal secretie)
Erg lipofiel
Digoxine
P-gp substraat
+rifampicine: minder blootstelling
Domperidone
QT verlenging (massieve dosissen)
Dopamine antagonist
CYP3A4 substraat
Doxorubicin
Chemotherapeutica
Ethanol
Meest gebruikte drug in onze maatschappij
0de orde kinetiek
o Alcohol dehydrogenase(ADH), aldehyde dehydrogenase (disulfiram), CYP2E1
o Verzadiging ADH vanaf 100mg/L -> 0.1promille (1g/l =1promille =0.1%)
o Eliminatiesnelheid: 15mg/dl/h
o Langere blootstelling dan bij 1ste orde
CYP2E1 inducer
Farmacokinetiek alcohol
o Acute inname
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