drug administration and absorption Flashcards

1
Q

what are the main types of targets for drugs

A

enzymes, transporters, ion channels and receptors
- most often than not they interact with proteins

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2
Q

what is the most common drug target

A

enzymes

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3
Q

what are receptors

A

proteins that respond to an endogenous messenger by initiating a signal

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4
Q

what do selective binding sites act as

A

molecular switches, switching the cell on and off

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5
Q

what are the two types of receptor drugs

A

agonists and antagonists

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6
Q

how does an agonist receptor drug work

A

it reproduces the effects of endogenous messengers

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7
Q

how do antagonists drug receptors work

A

they block the effects of the endogenous messenger

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8
Q

what does the extent to which a drug binds to its
target protein depend on

A

its local concentration

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9
Q

which 3 targets are predominantly targeted by inhibitors

A

enzymes, transporters and receptors

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10
Q

what type of drug target is effected by agonists and antagonists

A

receptors

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11
Q

what does ADME[Tox] stand for

A

Absorption
Distribution
Metabolism
Excretion
Toxicity

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12
Q

define PHARMACOKINETICS

A

How body controls drug
concentration at site of action

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13
Q

define PHARMACODYNAMICS

A

Effect of drug on target
cell / tissue

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14
Q

why is pK important

A
  • Analysis of the behaviour of drugs after administration
  • Essential for designing dosing regimen and understanding
    variation in responses between patients

-PK parameters can offer insight into the disposition of the
drug after administration

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15
Q

what are the 10 routes of administration

A

PO, NG, S/L, MR, PR, IV, TOPICAL, OPHTHALMIC, INHALATION , NASAL

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16
Q

that route of administration is PO

A

enteral (oral)

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17
Q

that route of administration is NG

A

nasogastric

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18
Q

that route of administration is S/L

A

sublingual

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19
Q

that route of administration is MR

A

controlled release

20
Q

that route of administration is PR

A

rectal

21
Q

that route of administration is IV

A

parenteral

22
Q

that route of administration is TROPICAL

A

skin

23
Q

that route of administration is OPHTHALMIC

A

eye

24
Q

that route of administration is INHALATION

A

lungs

25
Q

that route of administration is NASAL

A

nose

26
Q

concentration an be found by

A

measuring the drug concentration of the blood plasma as most drugs circulate via the circulatory system

27
Q

what is a therapeutic window

A

the therapeutic range where the drug is effective, too much and it becomes toxic too little and its ineffective within the body

28
Q

why are drugs with a narrow therapeutic range difficult to use

A

patients will need to be monitored more frequently

29
Q

what does MTC stand for

A

maximum tolerated concentration

30
Q

what does MEC stand for and what does it tell you

A

minimum efficacious concentration
- tells you the minimum amount of a drug that can be taken for it to still be effective

31
Q

why does absorption cause a delay

A

as the drug has the diffuse into the blood plasma before traveling to the target area

32
Q

what is the half life of a drug

A

the time taken for the concentration of the drug in the blood to decrease by half

33
Q

what is the half life of oxazepam

A

5-10 hours

34
Q

what is the half life of diazepam

A

20-80 hours

35
Q

what is considered when choosing a route of administration

A
  • ease e.g. complient patient
  • kinetics of the drug (duration of action)
  • local vs systemic effects
36
Q

define absorption in the administration of drugs

A

the transfer of a drug from its site of administration to its site of action (PK)

37
Q

define bioavailability in the administration of drugs

A

The extent to which a drug can overcome the
barriers to absorption (including first pass
metabolism) and enter the systemic circulation

38
Q

what 2 mechanisms can dugs travel by to enter the blood stream

A

passive diffusion and active transport

39
Q

how does passive diffusion work during drug absorption

A

diffuses through phospholipid bilayers
- the rate of diffusion depends upon
– the concentration across the membrane
–thickness of the membrane
– the surface area of the absorption surface

40
Q

A number of factors affect uptake in the GI tract such as….

A

-Formulation of drug ( Tablet vs. solution, variation in additives between brands)

-Gastrointestinal mobility ( Presence of food or pathology can delay transit time)

-Food constituents ( Ca2+binds tetracyclines making them unavailable for absorption)

-G secretions & gut wall enzymes (Can destroy / inactivate drugs)

41
Q

what are the advantages using the GI tract as the site of absorption

A

-Large surface area

  • Range of pH environments promote uptake of weak
    acids/bases

-Rich blood supply

-Long dwell time

-Some active transport (e.g. Levodopa taken up by
phenylalanine transporter)

-Small intestine is major site for absorption

42
Q

why are there differences in rates of absorption from different muscle groups

A

each muscle group will experience different flows of blood to them

43
Q

The efficiency of absorption can be quantified by what two variables

A
  • Bioavailability (F)
  • Time to peak (tmax)
44
Q

what is Time to peak (tmax)

A

a measure of the rate of absorption

45
Q

what is Bioavailability (F) a measure of

A

a measure of the proportion of dose absorbed (Compared to iv delivery of the same dose)

46
Q
A