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Concepts In Pharmacology > Module 3 - Pharmacokinetics and Pharmacodynamics > Flashcards

Module 3 - Pharmacokinetics and Pharmacodynamics Flashcards

1
Q

What is pharmacodynamics?

A

What a drug does to the body

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2
Q

What is involved in pharmacodynamics?

A

The effect of the drug, mechanism and their action

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3
Q

What is drug selectivity?

A

The number of molecular targets the drug interacts with

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4
Q

What is drug specificity?

A

The number of effects the drug produces

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5
Q

What is drug affinity

A

Affinity = affection
Tendency of a drug to combine with receptor site

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6
Q

What is an adverse reaction?

A

A biological effect that is not intended

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7
Q

What are the four main types of molecular drug targets?

A

Transporter
Enzyme
Ion channel
Receptor

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8
Q

What is meant by receptor agonist?

A

A drug/substance that binds to a receptor and causes the SAME effect

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9
Q

What is a partial agonist?

A

Unable to produce an active response even when all receptors are occupied?

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10
Q

What is an orthosteric site?

A

An active site

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11
Q

What is an allosteric site?

A

Binds to a different site and causes a reaction

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12
Q

What is a receptor antagonist?

A

Binds to a receptor target but DOES NOT elicit a response

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13
Q

What effect does a receptor agonist produce?

A

Prevents binding of agonist to receptor thus preventing activation of receptor

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14
Q

What are the three (3) types of receptor antagonists?

A

Reversible, irreversible and non-competitive

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15
Q

What does a reversible receptor antagonist do?

A

Interferes with binding of endogenous agonist to orthosteric (active) site

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16
Q

What does a irreversible receptor antagonist do?

A

Causes target receptor to become permanently unavailable for binding of agonist

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17
Q

What does a non-competitive receptor antagonist do?

A

Blocks response to agonist

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18
Q

What do allosteric modulators do?

A

Indirectly alters function of a receptor in positive or negative way

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19
Q

How do allosteric modulators produce a pharmacological response?

A

Activating receptor to cause different biological response
Alter binding affinity
Changing the efficacy of receptor

20
Q

What is potency?

A

How much drug is required to produce an effect

21
Q

What is EC50?

A

The drug concentration as which a drug produces 50% of the maximal response

22
Q

What is efficacy?

A

Measure of how big an effect the drug will have when all targets are occupied

23
Q

What are the two types of transporters?

A

Facilitated and active

24
Q

When must transporters be utilised?

A

When a drug is not soluble and cannot passively diffuse across a membrane

25
Q

What are ion channels?

A

Transmembrane proteins that control ion flow across a cell membrane

26
Q

What are the main ion channels?

A

Voltage gated ion channels and intracellular ligand gated ion channels

27
Q

What are enzymes?

A

Catalysts that speed up rate of all chemical reactions that take place with cells

28
Q

What are receptors?

A

Signalling proteins that recognise and response to chemical messengers to change a function within a cell

29
Q

What are the four (4) families of receptors?

A
  1. Ligand gated ion channels
  2. G-coupled protein receptors
  3. Kinase receptors
  4. Nuclear receptors
30
Q

How do ligand gated channels work?

A

A drug binds to a particular site on the transmembrane protein to open up the gate and allow ions to flow through

31
Q

How do G-coupled protein receptors work?

A

A ligand will bind to outside of a G-coupled protein receptor. Receptor undergoes conformational change that allows it to interact with G-protein that will pass signal on to other intermediates in signalling pathway

32
Q

What is pharmacokinetics?

A

What the BODY does to the drug

33
Q

What is involved in pharmacokinetics

A
  1. Concentration of a drug increases as it is absorbed in the body
  2. Hits peak concentration
  3. Process of elimination occurs (drug concentration in the plasma reduces)
34
Q

What is the importance of understanding a drugs pharmacokinetic profile?

A

Allows use to decide appropriate dosages, determine dosing regimes, interpret drug reactions and adjust doses according to response

35
Q

What are the two main categories of drug administration?

A

Systemic administration and target administration

36
Q

What occurs during systemic administration?

A

Drug enters circulation and is carried to site of action (needs to be able to cross biological membranes)

37
Q

What occurs during target administration?

A

Drug is delivered to the site of action (proximity delivered to tissue/organ where desired effect is intended)

38
Q

What is the difference between lipid soluble drugs and ionised/charged drugs?

A

Lipid soluble drugs readily pass through lipid membrane, ionised/charged drugs have difficulty crossing cell membranes

39
Q

What are the four (4) main ways a drug can cross cell membranes?

A

Passive diffusion
Facilitated transport
Active transport
Aquaporin

40
Q

What is lipophilicity?

A

Passes through cell membrane more easily (easier absorption)

41
Q

What is hydrophilicity?

A

Difficulty crossing lipid bilayer

42
Q

What is the impact of ionisation on drug absorption?

A

Un-ionised drugs (lipid soluble) easily diffuse across lipid membrane compared to ionised drugs

43
Q

What are the main physiological barriers of drug absorption?

A

Nature of the tissue
Channel and transporter
Surface area (large surface area increases absorption)
Blood flow (increased blood supply results in increased absorption)

44
Q

What factors mainly impact distribution?

A

Physiochemical properties of a drug (e.g. size/molecular weight, lipophilicity/hydrophilicity, ionisation and tissue binding)
Physiology of the person (e.g. circulation, permeability of membranes, tissue mass and channel/transporter)

45
Q

What is the impact of a hydrophilic drug on distribution?

A

A large portion will remain in the extracellular fluid compartment as it cannot cross cell membranes

46
Q

What is the impact of a Lipophilic drug on distribution?

A

Can move between intracellular and intravascular compartments

Concepts In Pharmacology (8 decks)

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