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Z YEAR 2 Pharm > Introduction to Pharma > Flashcards

Introduction to Pharma Flashcards

1
Q

What does pharmacodynamics deal with?

A

What the drug does to the body

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2
Q

What does pharmacokinetics deal with?

A

what the body does to the drug

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3
Q

What questions do you need to know to. see how drugs exert their effects on the body?

A

Where is this effect produced?
What is the target for the drug?
What is the response that is produced after interaction with this target?

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4
Q

What is the effect and where for cocaine?

A
  • euphoric high (+local anaesthetic)

- dopaminergic neurons nucelus accumbens

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5
Q

What are the target for cocaine?

A

dopaminergic neurone, (dopamine reuptake protein on pre-synaptic terminal)

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6
Q

What is the response of cocaine?

A

Cocaine blocks dopamine re-uptake protein so dopamine not removed from synapse quickly - so more available to bind to the dopamine (D1) receptor - activation of this receptor causes euphoria

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7
Q

What are the the drug target proteins?

A
  1. Receptors
  2. Enzymes
  3. Ion channels
  4. Transport proteins
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8
Q

What is the drug target protein for aspirin?

A

Enzyme

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9
Q

What is the drug target protein for local anaesthetic?

A

Ion channel

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10
Q

What is the drug target protein for prozac?

A

Transport protein

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11
Q

What is the drug target protein for nicotine?

A

receptor

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12
Q

What is the action of aspirin?

A
  • binds to the ‘enzyme’ cyclooxygenase

- blocks the production of prostaglandins

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13
Q

What is the action of local anaesthetic?

A
  • block sodium ‘ion channels’

- prevent nerve conduction

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14
Q

What is the action of prozac?

A
  • block serotonin ‘carrier proteins’

- prevent serotonin being removed from the synapse.

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15
Q

What is the action of nicotine?

A

binds to and activates the nicotinic acetylcholine ‘receptor’

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16
Q

How do drugs act on targets?

A
  1. enhance activation of the target (stimulate an effect)

2. prevent activation of the target (block an effect from being produced)

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17
Q

What do drugs need?

A

High degree of selectivity for a particular drug target

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18
Q

Can drugs bind to different receptors then needed?

A
  • Dopamine, seretonin, noradrenaline similar structure
  • some degree of specificity for other receptor e.g. the dopamine receptor is the most specific receptor for dopamine, but serotonin receptors and adrenergic receptors have some degree of specificity for dopamine
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19
Q

When do you get side effects?

A
  1. If want to use a drug that produces its useful therapeutic effect via an action at dopamine receptors
  2. also a chance that the drug will also interact with serotonin and adrenergic receptors and produce other effects that you don’t want (side-effects)
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20
Q

What does drug dose relate to?

A

selectivity of drug effect

21
Q

Give an example of how drugs dose relates to selectivity do drug effect

A
  1. Drug is fifty times more selective for drug target A compared to drug target B
  2. Start very low dose of drug and increase the dose until we first start seeing an effect at target A
  3. Know that we will need to increase the dose 50-fold before we start seeing effects at target B
22
Q

Why do parkinson’s drugs have side effect?

A

Pergolide most selective for dopamine receptors but can also bind to serotonin receptors and adrenergic receptors

23
Q

What happens at a high and low dose for pergolide?

A
  1. Low dose effect is more specific as Pergolide only interact with one target
  2. As dose increase effect becomes less specific Peroglide starts to interact with other drugs targets producing other unwanted effects
24
Q

What are the 4 different drug receptor interactions?

A
  1. Electrostatic interactions
  2. Hydrophobic interactions
  3. Covalent bonds
  4. Stereospecific interactions
25
Q

What are electrostatic interactions?

A
  • most common mechanism

- includes hydrogen bonds and Van der Waals forces

26
Q

What are hydrophobic interactions important for?

A

lipid soluble drugs

27
Q

What are covalent bond interactions?

A
  • least common

- as the interactions tend to be irreversible

28
Q

What are stereospecific interactions?

A

-Lots of drugs exist as stereoisomers and interact stereospecifically with receptors

29
Q

If there a limit to how many receptors can be occupied?

A
  1. certain number of receptors for adrenaline
  2. if add a certain concentration of adrenaline to this tissue
  3. Then a certain number of receptors will become ‘occupied’ by adrenaline:
30
Q

What happens to the equilibrium if the concentration of the drug increases?

A

Equilibrium strongly shifted to right. (more drug receptors complex produced), because more drug available to bind to free receptors

31
Q

What happens if you decrease the amount of drug available?

A

More receptors available again due to the lower drugs concentration so equilibrium shifts to the left

32
Q

What can agonists do that antagonists can’t ?

A

only agonists can bind and activate receptors

33
Q

What does an agonist do?

A

fit into the receptors and activate the receptors

34
Q

What does an antagonist do?

A

fit in receptors but jam mechanisms and prevent the ‘lock’ from being activated

35
Q

What does the affinity of the drug determine?

A

strength of binding of the drug to the receptor

36
Q

What is affinity linked to?

A
  • receptor occupancy
  • drug with the higher affinity will form stronger drug receptor complexes and thus at any given moment, it is more likely that more of this drug will be bound to receptors
37
Q

What is each individual drug receptor interaction?

A
  • transient

- with many interactions only lasting milliseconds

38
Q

What does efficacy mean?

A

ability of an individual drug molecule to produce an effect once bound to a receptor

39
Q

What sort of response is produced when a drug occupies a receptor?

A
  • complete response
  • no response
  • some partial response
40
Q

What type of drug binds to the receptor and produces no response?

A
  • Affinity for receptro
  • No efficacy (stops agonist binding)
  • Antagonist
41
Q

What type of drug binds to the receptors and can produce a partial response, but is not capable of inducing the maximal response?

A
  • Affinity for the receptor
  • Sub-maximal efficacy
  • Partial Agonist
42
Q

Why type of drug binds to the receptor and produces the maximal response?

A
  • affinity for the receptor
  • maximal efficacy
  • Full agonist
43
Q

What is potency?

A

the concentration or dose of a drug required to produce a defined effect
The standard measure of potency is to determine the concentration or dose of a drug required to produce a 50% tissue response

44
Q

What is EC50?

A
  • Add specific ‘concentrations’ of the drug to your in vitro preparation to test effectiveness
  • The concentration that produced a 50% response would be the EC50
45
Q

What is ED50?

A

dose of drug that produced the desired effect in 50% or the individuals tested

46
Q

When is a drug more potent?

A

less drug you require to produce a particular effect, the more potent the drug is
(ED50 smaller)

47
Q

Is potency and efficacy related to dose?

A
  • A highly potent drug produces a large response at relatively low concentrations.
  • A highly efficacious drug can produce a maximal response and this effect is not particularly related to drug concentration
48
Q

What is more important clinical efficacy or potency?

A
  1. Efficacy is more important
  2. Want to know if the drug you are giving can induce a maximal response
  3. The potency simply determines the dose that you will need to administer to produce a response. If you have two drugs that have equal efficacy, then it doesn’t really matter if one is more potent than the other, since you can still produce the maximal response with the less potent drug – you just need to administer a slightly higher concentration.

Z YEAR 2 Pharm (9 decks)

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