Quiz
Pharmacokinetics
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Questions in this quiz (10)
1To achieve its effect a drug must first be presented in a suitable formulation at an appropriate site of [blank_start]ADMINISTRATION[blank_end] and then (usually) [blank_start]ABSORBED[blank_end] and [blank_start]DISTRIBUTED[blank_end] through the body to its site of action. For the effect to wear off the drug must almost always be [blank_start]METABOLISED[blank_end] and/or [blank_start]EXCRETED[blank_end] with these residues being [blank_start]VOIDED[blank_end] (REMOVED) from the body.
- AADMINISTRATION
- BABSORBED
- CDISTRIBUTED
- DMETABOLISED
- EEXCRETED
- FVOIDED
2Administration:
[blank_start]SYSTEMIC[blank_end] - the entire organism
[blank_start]LOCAL[blank_end] – restricted to one area of the organism
[blank_start]ENTERAL[blank_end] - Gastro-intestinal admin + involvement
[blank_start]PARENTERAL[blank_end] – Outside GI tract admin- ASYSTEMIC
- BLOCAL
- CENTERAL
- DPARENTERAL
3Absorption:
Drug molecules move around the body in two ways:
[blank_start]Bulk flow[blank_end] transfer i.e. in the bloodstream
[blank_start]Diffusional[blank_end] Transfer i.e. molecule by molecule over short distances
Drugs have to traverse both aqueous and lipid environment
[blank_start]Compartments[blank_end] = Aqueous e.g. Blood, lymph, extra-cellular fluid, intra-cellular fluid
[blank_start]Barriers[blank_end] = Lipid i.e. cell membranes (epithelium/endothelium)- ABulk flow
- BDiffusional
- CCompartments
- DBarriers
4How do drugs cross barriers?
1) Diffusing through [blank_start]lipid[blank_end]
2) Diffusing through [blank_start]aqueous pores[blank_end] in the [blank_start]lipid[blank_end]
3) [blank_start]Carrier[blank_end] molecules
4) [blank_start]Pinocytosis[blank_end]
1 and 3 being main mechanisms- Alipid
- Baqueous pores
- Clipid
- DCarrier
- EPinocytosis
5Non-polar substances can freely dissolve in non-polar solvents i.e. can penetrate lipid membranes freely.
Passive diffusion - the [blank_start]pH partition[blank_end] hypothesis
Also gives rise to the mechanism of [blank_start]ion trapping[blank_end]
Very Important:
Most drugs are either [blank_start]weak[blank_end] acids or [blank_start]weak[blank_end] bases.
Therefore drugs exist in ionised (polar) and non-ionised (non-polar) forms – the ratio depends on the [blank_start]pH[blank_end]- ApH partition
- Bion trapping
- Cweak
- Dweak
- EpH
6Factors influencing drug distribution…
[blank_start]Regional blood flow[blank_end] – rate of tissue perfusion
[blank_start]Extracellular binding[blank_end] (Plasma-protein binding means only a certain amount is active to be absorbed)
[blank_start]Capillary permeability[blank_end] (tissue alterations – renal, hepatic, brain/CNS, placental)
[blank_start]Localisation[blank_end] in tissues, usually [blank_start]fatty[blank_end] tissues allow drugs to persist for a long time- ARegional blood flow
- BExtracellular binding
- CCapillary permeability
- DLocalisation
- Efatty
7Distribution:
If a drug is distributed through the bloodstream to tissues, the effect under strenuous exercise will be quite different
If body is stressed, blood flow changes
Localisation: Fat is [blank_start]15%[blank_end] body weight but [blank_start]2%[blank_end] blood supply
Very fat soluble drugs – [blank_start]75%[blank_end] partitioned in fat at
[blank_start]equilibrium[blank_end]- A15%
- B2%
- C75%
- Dequilibrium
8The two major routes of drug excretion:
Liver: Some drugs are concentrated in the [blank_start]bile[blank_end] (usually [blank_start]large[blank_end] molecular weight conjugates)
[blank_start]Biliary[blank_end] excretion (effective for [blank_start]large[blank_end] molecular weight molecules, as they can [blank_start]concentrate[blank_end])
Active transport systems – into [blank_start]bile[blank_end] (bile acids and glucuronides)
[blank_start]Kidney[blank_end]:ultimately responsible for the elimination of most drugs
1. [blank_start]Glomerulus[blank_end] – drug-protein complexes not filtered
2. Proximal tubule – active secretion of [blank_start]acids and bases[blank_end]
3. Proximal and distal tubules – lipid soluble drugs [blank_start]reabsorbed[blank_end]- Abile
- Blarge
- CBiliary
- Dlarge
- Econcentrate
- Fbile
- GKidney
- HGlomerulus
- Iacids and bases
- Jreabsorbed
9First-order kinetics describes the rate of elimination of a drug where the amount of a drug decreases at a rate that is [blank_start]proportional[blank_end] to the concentration of the drug remaining in the body.
[blank_start]First[blank_end]-order kinetics is dependent on the concentration of drug at any given time and applies to most drugs in clinical use.
Co: is concentration at time zero – cannot be measured since instantaneously [blank_start]clearance[blank_end] begins, therefore [blank_start]extrapolated[blank_end]
Vd: Volume of distribution
Cl: clearance
clearance is proportional to drug concentration in plasma/serum- Aproportional
- BFirst
- Cclearance
- Dextrapolated
10Zero-order kinetics
[blank_start]Half life[blank_end] doesn't apply.
Note: drug-concentration axis is [blank_start]linear[blank_end]
If it were on a log scale the first-order plot would be [blank_start]straight[blank_end] and the zero- order plot would be [blank_start]curved[blank_end]
Implies a [blank_start]saturable[blank_end] (usually enzymic) metabolic process
(applies to very few drugs) since drug is always metabolised at same ([blank_start]maximal[blank_end]) rate- AHalf life
- Blinear
- Cstraight
- Dcurved
- Esaturable
- Fmaximal
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- Description
- Medicine (Pharmacology) Quiz on Pharmacokinetics, created by april yao on 07/10/2016.
- Author
- april yao
- Language
- English
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- History
- Created on 7 Oct 2016 · updated on 8 Oct 2016
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