Pharmacokinetics and Clinical trials - Pharmacokinetics and related topics
26 important questions on Pharmacokinetics and Clinical trials - Pharmacokinetics and related topics
What is one characteristic that makes a good drug?
What additional characteristics are important for a good drug besides activity/selectivity?
What is the role of blood in drug administration?
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What barriers do drugs have to cross to reach their target?
What does oral bioavailability refer to?
What does membrane permeation depend on?
What is the penetration rate formula for membrane permeation?
P = partition into membrane
A = effective surfice area of membrane
C1-C2 = concentration gradient
What happens to drugs that are too polar (hydrofiel)?
What is the issue with drugs that are too fatty (hydrofoob)?
Geneesmiddelen die te vettig (hydrofoob) zijn, zijn onoplosbaar in water in het lumen van de darm en hebben daarom geen oppervlaktecontact met de darmwand.
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How do hydrogen bonds affect absorption?
How is the partition coefficient (P) calculated in the octanol/water model?
What is the partition coefficient?
De partition coefficient is de verhouding van de concentraties van de niet-geïoniseerde verbinding tussen twee oplossingen. De partition coefficient wordt gebruikt als maatstaf voor het hydrofobe karakter van een geneesmiddel. (kijken hoe goed het zich verdeeld over een hydrofiele en hydrofobe omgeving)
According to Lipinski's Rule of five, when is absorption more likely?
Mol. Weight < 500
ClogP < 5
Nr. of H-bond donors < 5
Nr. of H-bond acceptors < 10
What happens if Lipinski's rules are not obeyed by a drug?
The drug is poorly absorbed. (Exception: some polar drugs use a carrier protein)
What is shown as a general solution for the absorption problem of polar drugs?
How does distribution affect drugs in the body?
What does lipid solubility affect in terms of drug distribution?
Are there any openings between the cells in capillaries, and if so, what do they allow?
How does very high lipid solubility affect a drug's distribution?
What are plasma proteins involved in?
What happens when drugs bind to plasma proteins in the blood?
Where does the first phase of drug metabolism occur?
How do enzymatic reactions affect drug substances in Phase I metabolism?
What does Phase II of drug metabolism relate to?
What type of enzymes are involved in Phase II drug metabolism?
Betrokken enzymen zijn een groep transferasen die de cofactoroverdracht naar het substraat verzorgen. Het resultaat is een grote toename van het uitscheidingspotentieel.
Excretion![]()
What will not be re-absorbed into the blood?
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