Pharmakokinetics Flashcards
With regard to exponential processes:
T/F
When considering a volatile anaesthetic ash-in curve, the rate of increase of the function decreases with time
True
With a volatile anaesthetic wash-in curve the FA/FI ratio (ratio of alveolar concentration/inspired concentration) is plotted against time. As time passes, the graph flattens as the alveolar and inspired concentrations equilibrate. Therefore the gradient of the graph reduces with time and consequently the rate of increase of the function decreases.
With regard to exponential processes:
T/F
Nitrogen washout during pre-oxygenation mist closely fits a linear process
False
With regard to exponential processes:
T/F
Bacterial growth is an example of an exponential tear-away function
True
Bacterial growth starts slowly and rapidly ‘takes off’ in an increasing exponential way - it is a ‘tear away’ function.
With regard to exponential processes:
T/F
When charging a capacitor, the graph of current versus time is similar to a volatile anaesthetic wash-in curve
False
When a capacitor charges, the charge versus time and the voltage versus time graphs resemble the wash-in curves. But, with respect to current, as charging proceeds less electrons are required to attempt to complete the charge and the current therefore falls. The current versus time graph therefore resembles a drug elimination curve.
In mathematics, with regard to exponential functions:
T/F
The term natural is used when the scaling uses base 2
False
The number e is the natural exponential because it arises naturally in mathematics and physical sciences, i.e. ‘real life’ situations. When the term natural is used, the base is e or 2.718.
In mathematics, with regard to exponential functions:
T/F
A natural exponential function can be transformed to give a straight line by usung any logarithmic transform
False
Natural exponential processes need natural logarithmic transforms to produce straight line graphs.
In mathematics, with regard to exponential functions:
T/F
Eulers number is 7.218
False
Euler’s number is 2.718
In mathematics, with regard to exponential functions:
T/F
They describe processes where a variable changes at a rate proportional to how long the process has been in operation
False
Natural exponential functions describe processes where the variable changes at a rate proportional to its own magnitude, not to time.
In mathematics, with regard to exponential functions:
T/F
A rectangular hyperbola is a special type of exponential function
False
Rectangular hyperbolae are conic sections and exponential functions model natural processes; look again at the graphs in the session and compare their features.
With regard to exponential processes:
T/F
They are useful when considering the mechanisms of physiological action potentials
True. Many of the processes surrounding the action potential relate to the difference in charges across the membrane and the capacitance of the cell; they are exponential.
Regarding the time constant, the rate constant and half-life:
T/F
The time constant, tau, is the time taken for the initial value to fall by e
False. The time constant is the time to fall to 1/e or 1/eth of the original value.
Regarding the time constant, the rate constant and half-life:
T/F
The half-life is never longer than the time constant
True. Since the half-life is the time to fall to 50% of the original value and time constant is the time to fall to 37% of the original value , the time constant must be greater.
Regarding the time constant, the rate constant and half-life:
T/F
The rate constant never has any units
False. The clue is in the phrase ‘rate constant’, the units must therefore be the units of rate i.e. per second (S-1).
Regarding the time constant, the rate constant and half-life:
T/F
The half-life is half the time constant
False. The half-life is 0.693 Tau i.e. roughly 2/3 of the time constant
Regarding the time constant, the rate constant and half-life:
T/F
It is necessary to know both the rate constant and the time constant to be able to plot an accurate graph of the function
False. You only need one of the constants to describe the graph, they are all mathematically related.
Regarding τ, k and t1/2:
T/F
τ is the time taken for the initial value to fall by e
False. τ is the time to fall to 1/e or 1/eth of the original value. Go back to page 20 for the three definitions.
Regarding τ, k and t1/2:
T/F
t1/2 is never longer than the time constant
True. Since t1/2 is the time taken to fall to 50% of the original value and τ is the time taken to fall to 37% of the original value, τ must be greater
Regarding τ, k and t1/2:
T/F
k never has any units
False. The clue is in the phrase ‘rate constant’, the units must be the units of rate i.e. per second (S-1).
Regarding τ, k and t1/2:
T/F
t1/2 is half of τ
False. The t1/2 is 0.693 τ i.e. roughly 2/3 of τ.
Regarding τ, k and t1/2:
T/F
It is necessary to know both k and τ to be able to plot an accurate graph of the function
False. You only need one of the constants to describe the graph, they are all mathematically related.
With regard to exponential drug elimination:
T/F
37% of the process is complete in one τ
False. The process is 63% complete in one τ
With regard to exponential drug elimination:
T/F
A bigger k describes a steeper fall in concentration
True. A bigger k describes a bigger slope/height ratio for the graph i.e. a steeper fall
With regard to exponential drug elimination:
τ is equal to t1/2 x 0.693
T/F
False. It is the other way round. t1/2 = 0.693 x τ.
With regard to exponential drug elimination:
T/F
t1/2 is directly proportional to k
False. t1/2 is inversely proportional k.
With regard to exponential drug elimination:
T/F
After three x τ the process is 95% complete
True. After one τ a process is 63% complete.
After two τ 63% + 63% of the 37% which remains = 86.3% complete.
After three τ 86.3% + 63% of the 13.7% which remains = 94.9% complete.
With regard to exponential drug elimination:
T/F
Taking logarithms of the time axis transforms the graph into a straight line
False. To achieve a straight line, you take natural logarithms of the concentration axis, not the time axis.
With regard to exponential drug elimination:
T/F
τ is the reciprocal of the elimination k
True. τ and elimination k are inversely related; if you plot τ against k you get a rectangular hyperbola.
With regard to exponential drug elimination:
T/F
τ is the time taken for the variable to reach 1/e of its initial value
True. This is one of the three definitions given; the other two are to reach 37% of original value or the initial concentration’s tangential intersection with the time axis.
With regard to exponential drug elimination:
T/F
Three t1/2 is the time required for the variable to fall to 12.5% of its original value
True. In one t1/2 the variable falls to half. In two t1/2 the variable falls by 50% + 50% of 50% = 75%. In three t1/2 the variable falls by 75% + 50% of 25% = 87.5% which leaves only 12.5% of the original concentration.
With regard to exponential drug elimination:
T/F
The graph shows asymptotes on both axes
False. There is only a single asymptote which is to the Time axis.
Regarding drug clearance
T/F
It is the volume of plasma that is cleared of a drug per unit time
True. This is the definition.
Regarding drug clearance
T/F
Correct units include ml/kg/min and litre/min
True. The units of clearance are ‘volume per time’ or, if looking at clearance per kg body weight, then ‘volume per time per kg’.
Regarding drug clearance
T/F
It cannot be greater than liver blood flow
False. For drugs that have some extra-hepatic metabolism such as propofol, this can occur
Regarding drug clearance
T/F
It is closely related to t1/2
False. Cl is determined by both Vd and the shape of the elimination curve for the drug
Regarding drug clearance
T/F
It is the volume of distribution divided by the τ
True. This is one of definitions.
Regarding the volume of distribution
T/F
The initial Vd for propofol is large
True. The initial Vd of propofol is variously described by the different models, Schnider 4.27 L and Marsh 15.9 L.
Regarding the volume of distribution
T/F
The Vd of a drug can be greater than the volume of the body
True. Vd is a virtual concept, it can be much larger than body volume - see diagram on Marsh model.
Regarding the volume of distribution
T/F
Vd = Cl/elimination k
False. This is a way of showing how clearance links Vd and the exponential wash out curve
Regarding the volume of distribution
T/F
Correct units include kg/litre and litres
False. Units must be units of volume or in scientific papers, units of volume/kg of body mass - the first of these units is the ‘wrong way round’.
Regarding the volume of distribution
T/F
It can be calculated by using a drug infusion if the half-life and steady state drug concentration is known
True. You do not need to know t1/2 for this method and do need to know Cl.
The rate of drug absorption from the stomach is:
lower for fentanyl than diclofenac
True
The rate of drug absorption from the stomach is:
greater for weak acids than weak bases for drugs with a pKa of 6
True
The rate of drug absorption from the stomach is:
increased in the presence of metoclopromide
False
The rate of drug absorption from the stomach is:
always increased by omeprazole
False
The rate of drug absorption from the stomach is:
less important than absorption from the small intestine for most oral medication
True
When considering absorption of drugs from the GI tract:
fentanyl is better absorbed from the small intestine than the stomach
True
When considering absorption of drugs from the GI tract:
thiopental cannot be given through the GI tract route
False
When considering absorption of drugs from the GI tract:
atracurium cannot be given orally
True
When considering absorption of drugs from the GI tract:
neostigmine is better absorbed than physostigmine
False
When considering absorption of drugs from the GI tract:
ketoconazole absorption is increased in patients taking omeprazole
False
Which of the following drugs bind more to alpha-1 acid glycoprotein than to albumin?
diazepam
False
Which of the following drugs bind more to alpha-1 acid glycoprotein than to albumin?
fentanyl
True
Which of the following drugs bind more to alpha-1 acid glycoprotein than to albumin?
phenytoin
True
Which of the following drugs bind more to alpha-1 acid glycoprotein than to albumin?
ibuprofen
False
Which of the following drugs bind more to alpha-1 acid glycoprotein than to albumin?
lidocaine
True
Which of the following are true of plasma protein binding of therapeutic drugs?
Displacement of protein-bound drug by a second drug will necessarily cause toxic effects
False
Which of the following are true of plasma protein binding of therapeutic drugs?
Drugs with a low hepatic extraction ratio and high degree of protein binding are most affected by changes in protein binding
True
Which of the following are true of plasma protein binding of therapeutic drugs?
Drugs that show flow-dependent hepatic extraction are unaffected by changes in protein binding
True
Which of the following are true of plasma protein binding of therapeutic drugs?
The interaction between amiodarone and wafarin is entirely due to competition for plasma protein binding sites
False
Which of the following are true of plasma protein binding of therapeutic drugs?
The renal filtration of a drug is increased when plasma protein binding is decreased
True
Regarding the distribution of the drugs through the body:
the volume of dstribution at steady state for a drug is dependent only on its lipid solubility
False
Regarding the distribution of the drugs through the body:
in a one-compartment model, volume of distribution is directly proportional to drug clearance
True
Regarding the distribution of the drugs through the body:
drugs with greater than 95% protein binding have a realtively small volume of distribution
False
Regarding the distribution of the drugs through the body:
volume of distribution at a steady state is approximately equal to total body water for most drugs
False
Regarding the distribution of the drugs through the body:
Non-depolarising muscle relaxants have smaller volume of distribution than induction agents
True
Which of the following describe the distribution of propofol?
It has a volume of distribution of approximately 1.4L/Kg
False
Which of the following describe the distribution of propofol?
It is an acidic drug so binds albumin in plasma
True
Which of the following describe the distribution of propofol?
The volume of distribution is very large as it is essentially unionized at plasma pH
True
Which of the following describe the distribution of propofol?
the initial volume of distribution in adults is age-dependant
False
Which of the following describe the distribution of propofol?
The volume of distribution is high because propofol is highly protein bound
False
Which of the following are metabolites of atracurium?
cisatracurium
False
Which of the following are metabolites of atracurium?
desmethylatracurium
False
Which of the following are metabolites of atracurium?
laudanosine
True
Which of the following are metabolites of atracurium?
3,17-dihydroxy atracurium
False
Which of the following are metabolites of atracurium?
a monoquarternary alcohol derivative
True
Which of the following enzymes demonstrate important pharmacogenetic variation?
CYP2E1
False