pharmacokinetics and pharmacodynamics Flashcards

1
Q

what is pharmacokinetics and pharmacodynamics

A

how drugs affect the body’s physiology

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2
Q

what are the 4 phases of how a drug effects the body

A
  • absorption
  • clinical effect
  • metabolism
  • excretion
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3
Q

what are the 5 routes of administration of a drug

A
  • oral
  • intravenous injections
  • intramuscular injections
  • subcutaneous injections
  • inhalation
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4
Q

what is a misconception of asthma inhalers way of absorption

A

not Inhalation as inhalers have powder in them which do not make it far enough into the alveoli to be absorbed the way - instead absorbed like a cream

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5
Q

what are the advantages and disadvantages of oral administration

A
advantages
- people don't mind taking pills 
disadvantages 
- slow onset
- variable absorption (may lose some in stomach, gut mucosa not good at absorption)
- gastric acid may destroy drug 
- needs to get through liver
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6
Q

what are the other factors that affect oral drugs absorption

A
  • lipid solubility and ionisation
  • drug formulation
  • gastrointestinal motility
  • interactions with other substances in the gut
  • GIT diseases
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7
Q

how does lipid solubility and ionisation affect absorption of oral drugs

A

will only be absorbed if lipid soluble

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8
Q

how does drug formulation affect absorption of oral drugs

A
  • may have coating which lets different parts of a drug be absorbed at different times
  • coating would need to dissolve first (could take hours or be immediate)
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9
Q

how can GIT diseases affect absorption of oral drugs

A

Crohn’s disease - bowel would be removed so can’t absorb as well/much

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10
Q

what is first pass metabolism

A

all blood from GIT drains into the hepatic portal vein and into the liver which then metabolises drug
- al blood from GIT must pass through liver before entering systemic circulation

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11
Q

how does first pass metabolism work

A
  • drug needs to pass through the liver where it will meet hepatocytes and be metabolised before entering the circulation
  • can lose a lot of the drug through this
  • but knowing this can mean drugs are designed to allow some to be lost in liver but still having enough to work
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12
Q

how can first pass metabolism activate the drug

A
  • can make an active form of an inactive drug (pro-drug)
  • means less needed by oral route
  • e.g. valaciclovir turns into acyclovir
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13
Q

how can first pass metabolism inactivate the drug

A
  • all is lost in liver through metabolism
  • means more is needed by oral route to get the desired effect
  • glyceryl trinitrate
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14
Q

how is drug dosage effected by first pass metabolism

A
  • might need to increase/decrease dose to allows right amount into circulation
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15
Q

what are does based off of

A

a healthy individual

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16
Q

how are drugs from the mouth absorbed

A
  • anything from the mouth doesn’t go through first pass metabolism as doesn’t pass through hepatic portal vein
  • goes dow veins in neck once absorbed and then into systemic circulation
  • different dosage is then needed than oral tablet
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17
Q

what are the advantages of non-oral drugs (injections)

A
  • predictable metabolism
  • no first pass metabolism (goes straight to the circulation- amount given is amount received in blood)
  • works quickly
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18
Q

what are the disadvantages of non-oral drugs

A
  • allergic reaction are more severe as affects the whole body
  • access difficult (patients don’t like giving themselves injections)
  • cost higher (expensive to ensure purity is checked)
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19
Q

what is bioavailability

A

how much does the drug work

- proportion of an ingested drug that is available for clinical affect

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20
Q

what is intravenous bioavailability

A

100%

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21
Q

why is oral drugs bioavailability less than intravenous

A
  • due to first pass metabolism

- lots of variables affect it - can change daily in the same person

22
Q

how is bioavailability modified

A
  • dosage form
  • destruction in the gut
  • poor absorption
  • first pass metabolism
23
Q

what are clinical trials used for

A

guarantee does and what happens/effects

24
Q

why is amoxicillin used more instead of penicillin

A

because it is more predictable in its bioavailability

25
how are drugs distributed throughout the body
in the blood
26
what does the vascularisation have to do with drug distribution
the more vascularised a part of the body is, the more drug will go to that part of the body
27
what is "volume of distribution"
the more blood in the tissue, the more drug
28
what are the different 'compartments' of the body the drug will go through
vascular, tissues, CNS
29
how does lipid binding affect drug distribution
drugs are slowly released from accumulation
30
what role does plasma proteins have in drug distribution
- the bound drug is inactive (can act as a reservoir if too much in the body to handle) - drug interactions are possible by competitive binding which causes differences in how drugs work (warfarin and aspirin for example)
31
what is drug metabolism
preparing the drug for elimination from the body
32
what are phase 1 metabolism reactions
- carry out little reaction to the molecule - change molecule conformation - oxidation, reduction and hydrolysis
33
what are phase 2 metabolism reactions
- add drug to another molecule to be excreted | - conjugation (glucoronidation, sulphating, methylation, acetylation, glutathione - helps excretion)
34
what fruit can activate the P45O mono-oxygenate system
grapefruit
35
how can drug levels in the body be tested
by any bodily fluid excreted - why the police us a breathalyser (amount in breath is proportional to amount in the body) - renal = urine - liver = bile - lungs = exhaled gas - also get sweat and saliva
36
what disorders can affect drug excretion
renal disease or liver disease
37
how does renal disease affect drug excretion
- chronic renal failure | - need less dose as it takes longer to excrete
38
how does liver disease affect drug excretion
- liver failure | - doses must be reduced
39
how is planning drug use based
on 'body compartments'
40
what is the single compartment model
drug behaves as if it is evenly distributed throughout eh body
41
what is the 2 compartment model
drug behaves as if it is in equilibrium with different tissues in the body - goes to tissue with large blood flow first then distributes throughout the rest of the body
42
what is the plasma half life
the time it takes for half of the drug to leave the system
43
what is the 1st order kinetics for drug clearance
- drug elimination or absorption is by passive diffusion only - removed at rate proportional to concentration of drug - higher concentration = faster clearance - can predict from half life - logarithmic graph of elimination is a straight line
44
what order of kinetics do most drugs undergo
first order
45
what is 0 order kinetics
- only remove a certain amount an hour - drug elimination is an active process and can be saturated by a high drug concentration - can have too much for an enzyme system to remove at time (causes different system to kick in which can leaf to liver failure ) - have constant rate of drug elimination (predictable)
46
what kind of kinetics does alcohol undergo
0 order kinetics | - enzymes become over saturated which is why it takes so long to leave system
47
what order of kinetics is paracetamol
0 order
48
what is drug accumulation
plasma concentration will build up if repeated doses of a drug are given - drug administration should balance drug clearance (changes per person - doses differ)
49
how is dosing determined
by drugs 'therapeutic index'
50
what happens with too frequent dosing
cause raised plasma levels that may be toxic
51
what happens with infrequent dosing
results in sub-therapeutic plasma levels and no clinical effect