Drugs Flashcards
What are the 4 basic factors that determine drug pharmacokinetics?
Absorption
Distribution
Metabolism
Elimination
What is absorption?
Absorption is defined as the process of movement of unchanged drug from the site of administration to the systemic circulation
To have a biological effect where does the drug have to enter?
The blood stream
What does taken orally mean?
In the mouth
What does administered intravenously mean?
Straight into the blood stream
What does subcutaneous mean?
Under the tongue
What does administered intramuscular mean?
Straight into the muscles
Give an example of a drug you inhale?
Asthma subutanol
Why is intravenous not absorbed?
As it just goes straight to the systemic circulation
What is Tmax?
The time for the drug to reach peak concentration
What is Cmax?
The peak concentration of the drug
Give a factor that can affect absorption of drugs?
How much food you have eaten
What is bioavailability?
The amount of drug that is available to achieve a certain effect
What is the therapeutic range?
The range of conc. at which a drug is active
If the drug is under the therapeutic range what happens?
There is no pharmalogical effect
If the drug is over the therapeutic range what happens?
Toxicity occurs
What is therapeutic index?
The range at which a drug is safe and active
How much bioavailability does a drug given intravenously have?
100%
What physical properties of a drug affect its absorption?
Particle size
Lipid solubility
pH and ionisation
What does the drug need to pass to get to the blood stream?
The cell membrane
Do ionised or un-ionised drugs cross the membrane?
Un-ionised
What can alter the ionisation of a drug?
Small pH changes
What happens to an ionised drug at the cell membrane?
Does not cross the membrane
May not be absorbed at all
What happens to an un-ionised drug at the cell membrane?
Should distribute across the membrane until equilibrium is reached - will rapidly diffuse across the membrane
Does food enhance or impair the rate of drug absorption?
Can do either
What is first pass metabolism?
Metabolism of the drug prior to reaching system circulation. There can be a limit on this on oral routes for some drugs
What is intramuscular administration most commonly used for now?
Vaccinations
How will sublingual be absorbed?
Under the tongue
Enters the circulation directly
Does sublingual bypass first past mechanism?
Yes - it is absorbed straight into the blood stream
What kind of agents is inhalation administration best for?
Better for volatile agents
Are substances well absorbed by transdermal route?
No - few substances are well absorbed this way
What does transdermal administration mean?
Absorbed through the skin
For a drug to be active where must it leave then enter?
Must leave the blood stream and enter the intercellular or intracellular spaces
What do many drugs bind to?
Plasma proteins
What drug is the active drug?
The drug that is not bound to plasma protein
Is the binding of a drug to a plasma protein reversible?
Yes
What is the clearance of a drug?
Defined as the theoretical volume of fluid from which a drug is completely removed over a period of time
What is clearance a measure of?
Elimination
What is the clearance of a drug dependent on?
How quickly the kidneys clear the drug
The rate of metabolism
What is the half life of a drug?
The half life is defined as the time taken for the drug concentration in the blood to decline to half of the current value
If it takes 4 hours for the conc. of a drug in the blood stream to drop from 10mg to 5mg then what is the half life?
4 hours
What does half life depend on?
The volume of distribution and the rate of clearance
If the half life is prolonged what is the effect?
There is a reduction in the drugs clearance
What does drug elimination mean?
This means the removal of the drug from the body
What is drug elimination dependent on?
Drug metabolism
Drug excretion
What is the primary organ for drug excretion?
The kidneys
What damage is important in causing drug toxicity?
Renal damage
Are most medicines taken once off or chronically?
Chronically
In theory what should the Vd be?
42L
What determines the drug delivery system we use?
The dose of drug to be given
The frequency of administration
The timing of administration
What do we refer to for finding out the recommended dose of a drug in adults?
BNF
What do we refer to for finding out the recommended dose of a drug in children?
BNFc
What two organs do we consider the function o in drug prescription?
Kidneys (renal function)
Liver (hepatic function)
What is the most common form or drug administration?
Orally
Oral medication
In what state are suspended drugs?
Liquid
Who are solutions and suspensions useful for?
The young and elderly with swallowing difficulties