Pharmacokinetics and Pharmacodynamics Flashcards

(43 cards)

1
Q

what is the therapeutic window

A

range of concentrations of the drug in the plasma to allow it to have its desired effect

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2
Q

what is the bioavaliabilty of a drug

A

the fraction of the drug administered which reaches circulation

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3
Q

what factors affect the bioavaliabilty of a drug

A

first pass metabolism, age, food, vomiting, malabsorption

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4
Q

what is first pass metabolism

A

where a drug can be metabolised before it reaches systemic circulation

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5
Q

where does first pass metabolism occur

A

gut lumen, gut wall and liver

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6
Q

what is the bioavaliabilty for a drug given by IV

A

100% as it reaches the blood immediately

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7
Q

how does protein binding affect the distribution of a drug

A

if drugs bind to plasma proteins then they are not active so cant have therapeutic effects

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8
Q

what is the volume of distribution

A

how far through the body compartments a drug will dissolve

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9
Q

how does the Vd change with weight

A

in patients with larger weights the Vd increases as the drug can travel through the fat better - this means he drug has less of an effect as theres a lower drug plasma concentration

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10
Q

what is the equation for Vd

A

Vd = Dose/immediate plasma concentration

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11
Q

what is the equation for bioavalibilty

A

AUCoral/AUCiv

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12
Q

which group of enzymes carry out the first stage of metabolism

A

CYP4500 enzymes

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13
Q

what do CYP4500 enzymes do

A

cause oxidation, reduction, hydrolysis in order to change the ionic charge of the drug

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14
Q

what does Phase II enzymes do

A

conjugate the drug e.g. with sulphate or glutathione to increase its solubility

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15
Q

what are pro-drugs

A

drugs which must be metabolised in order to become activated

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16
Q

what factors affect metabolism

A

hepatic disease, age, alcohol, smoking

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17
Q

what are the routes for drug elimination

A

kidney elimination, salvia, breast milk, sweat, bile

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18
Q

what 3 processes in the kidney affect elimination

A

glomerular filtration, passive tubular reabsorption and active tubular secretion

19
Q

what happens to clearance if the GFR is decreased

A

clearance decreases

20
Q

what happens to the half life if the GFR Is decreased

A

half life increases because less of the drug is cleared

21
Q

what are first order kinetics

A

where the rate of clearance is proportional to the drug level

22
Q

what are zero order kinetics

A

where the rate of elimination is constant

23
Q

what is the hat life of a drug

A

amount of the it take for the concentration of a drug to half

24
Q

what is the equation for half life

A

t1/2 = 0.7 x Vd/Cl

25
how does hepatic disease affect clearance
less metabolism can occur
26
how does cardiac disease affect clearance
less perfusion to kidneys and liver
27
what is a loading dose
where a higher concentration of a drug is given first in a repeated prescription in order to reach a steady state quicker
28
true or false - a loading dose is used in drugs with a low half life
false - its for drugs with a high half life
29
what is the equation for loading dose
loading dose = Vd x target drug concentration
30
what is tornado de pointes
where interactions between drugs leads to a slower conduction of the heart giving a prolonged QT internal
31
what is digoxin used to treat
AF with heart failure
32
why is a loading dose needed with digoxin
the drug has a long half life, however patient with AF need immediate treatment so you cant wait days to reach the steady state of the drug
33
what are the different types of antagonist
competitive (reversible and irreversible) and non-competitive
34
what is the therapeutic index
the relationship between the concentration of the drug causing adverse and desirable effects
35
what is the equation for the therapeutic index
toxic dose/effective dose
36
what is the affinity of a drug
how well a drug binds to a receptor
37
what does a low Kd say about the affinity of a drug
high affinity
38
what is the efficacy of a drug
the ability of a drug to produce a response
39
what is the potency of a drug
the dose required to give 50% response. same as EC50. the more potent a drug the better a response it can give at lower concentrations
40
what is intrinsic efficacy
the ability to bind to a receptor and cause a response.
41
what does the potency of a drug depend on
affinity and efficacy
42
what is Bmax
drug concentration when all receptors are bound
43
what is Emax
drug concentration giving 100% response