Quiz
MD30 Systemic availability
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Fragen in diesem Quiz (12)
1Bioavailability — historic term: “A measure of the [blank_start]rate and extent[blank_end] of drug absorption, that quantifies the [blank_start]amount[blank_end] of drug that reaches the [blank_start]systemic[blank_end] circulation”. By referring to drug absorption, it implies that we can ignore [blank_start]first pass metabolism[blank_end], which we can't.
Systemic availability "F" — "The [blank_start]fraction[blank_end] of a dose that reaches the systemic circulation." Applicable to [blank_start]any[blank_end] administration route but ignores [blank_start]rate[blank_end].- Arate and extent
- Bamount
- Csystemic
- Dfirst pass metabolism
- Efraction
- Fany
- Grate
2Parameters for the [blank_start]extent[blank_end] of drug absorption:
[blank_start]Cmax[blank_end] - Maximum observed concentration
[blank_start]AUC[blank_end] - Area under the concentration-time curve
Parameters for the [blank_start]rate[blank_end] of drug absorption:
[blank_start]Tmax[blank_end] - Time that the maximum concentration (Cmax) is observed
[blank_start]Ka[blank_end] - Absorption rate constant- Aextent
- BCmax
- CAUC
- Drate
- ETmax
- FKa
3Absolute bioavailability (F) is the ratio of the AUC in the [blank_start]systemic circulation[blank_end] after oral ingestion, and the AUC from [blank_start]intravenous dosing[blank_end]. Oral bioavailability is [blank_start]less[blank_end] due to first pass metabolism.
To calculate the dose that reaches the systemic circulation from an oral dose we multiply the [blank_start]oral dose[blank_end] by [blank_start]F[blank_end].
In theory, you might need to give a [blank_start]bigger[blank_end] oral dose to achieve the same drug exposure (AUC) as [blank_start]intravenous[blank_end] dosing.- Asystemic circulation
- Bintravenous dosing
- Cless
- Doral dose
- EF
- Fbigger
- Gintravenous
4Relative bioavailability refers to a case where the intravenous dose is [blank_start]not the comparator[blank_end].
Requirements for a comparison of AUC’s:
1. Same [blank_start]drug and dose[blank_end]
2. [blank_start]Clearance[blank_end] must not change between the comparators
3. Linear pharmacokinetics (AUC is [blank_start]proportional[blank_end] to dose)
4. No other factors alter drug [blank_start]bioavailability[blank_end] (food, drug interactions)- Anot the comparator
- Bdrug and dose
- CClearance
- Dproportional
- Ebioavailability
5There are three primary determinants of bioavailability;
1. [blank_start]Disintegration and dissolution[blank_end] of the drug
2. [blank_start]Absorption[blank_end] across the membranes in the gut wall
3. Pre-systemic [blank_start]metabolism[blank_end] (or ‘first-pass’) and [blank_start]elimination[blank_end]- ADisintegration and dissolution
- BAbsorption
- Cmetabolism
- Delimination
6Choose the correct equation.
- AF = fa / fh
- BF = fa x fh
- CF = fh / fa
7Mechanisms for first pass elimination:
1. Metabolism in the [blank_start]gut wall[blank_end] (e.g. oestrogens, atorvastatin)
2. [blank_start]Efflux[blank_end] from the gut wall (e.g. dabigatran)
3. [blank_start]Esterase[blank_end] metabolism in the plasma of the [blank_start]portal circulation[blank_end] (e.g. aspirin)
4. Metabolism in the [blank_start]liver[blank_end] (most common)- Agut wall
- BEfflux
- CEsterase
- Dportal circulation
- Eliver
8Pre-systemic drug interactions impact peak plasma concentration (Cmax) not clearance.
- ARichtig
- BFalsch
9P-gps are responsible for gut wall efflux.
- ARichtig
- BFalsch
10High E by the liver means low fh.
- ARichtig
- BFalsch
11If E by an organ is high, [blank_start]clearance[blank_end] is equivalent to rate of [blank_start]perfusion[blank_end], and clearance of drug is [blank_start]high[blank_end].
- Aclearance
- Bperfusion
- Chigh
12The higher the E and clearance of a drug, the less variability in pharmacokinetics between people.
- ARichtig
- BFalsch
Informationen
- Beschreibung
- PHCY211 (Medicines) Quiz am MD30 Systemic availability, erstellt von Mer Scott am 27/05/2018.
- Autor
- Mer Scott
- Sprache
- English
- Aufrufe
- 7
- Schlagwörter
- Bewertung
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