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BDS1 BAMS molecules and cells > introduction to pharmacology > Flashcards

introduction to pharmacology Flashcards

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Organic Chemistry 101 flashcards
1
Q

what is pharmacology?

A

The study of the action of drugs on the function of living systems

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2
Q

what is a drug?

A

a chemical substance or natural product that affects the function of cells, organs, systems or the whole body (i.e. is bioactive)

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3
Q

where do drugs come from?

A

Natural products (i.e. plants, animals)
Serendipity (i.e. by accident)
Changing the structure of an existing molecule (i.e. structure-activity relationships)
Using an existing drug in a new disease (i.e. re-purposing)
Computer-aided design
Studying disease processes

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4
Q

what are the three types of names of drugs?

A

Chemical – IUPAC name that describes the chemical structure of the drug
Generic – international non-proprietary name given to a molecule
Proprietary – ‘trade’ name(s) given to an approved drug by the manufacturer

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5
Q

what is pharmacokinetics?

A

what the body does to the drug
- used as a generic term to describe the fate of a drug molecule following administration to a living organism or how a drug molecule is affected by exposure to living cells

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6
Q

what is pharmacodynamics?

A

what is drug does to the body
- used as a generic term to describe the mechanism of drug action or what happens to cells, organs, systems, etc., as a result of drug exposure

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7
Q

how are proteins involved with drugs?

A
  • drug transporters
  • metabolising enzymes
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8
Q

what cells are involved with drugs?

A
  • epithelial cells
  • endothelial cells
  • hepatocytes
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9
Q

drug administration paths…

A
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10
Q

what are the different routes of drug penetration into cells?

A

Diffusion through lipid membrane
- Major route for lipophilic drugs
Diffusion through aqueous channels
- Most drugs too large!
Carrier-mediated transport
- Major route for hydrophilic drugs
Pinocytosis
- Transport of insulin into brain

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11
Q

what does oral absorption of drugs require?

A

permeation of epithelial cell membrane

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12
Q

what is lipinski’s rule of 5?

A

an oral drug must have:
- molecular mass less than 500 Daltons
- no more than 5 H-bond donors (total number of N-H and O-H bonds)
- no more than 10 H-bond acceptors (all nitrogen or oxygen atoms)
- an octanol-water partition coefficient log P not greater than 5

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13
Q

basics of drug metabolism…

A
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14
Q

oral dosing…

A
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15
Q

what are the drug effects at the level of the cell?

A

Effects on receptors, ion channels, enzymes, transporters, DNA, etc.

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16
Q

what are the drug effects at the level of the organ/system?

A

Effects on heart, kidney, cardiovascular system, central nervous system, etc.

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17
Q

what are the drug effects at the level of the organism?

A

Therapeutic effect on disease state or process; adverse effects or side effects

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18
Q

what are the drug effects at the level of society?

A

cost , misuse, drug resistance

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19
Q

what are the sites of drug action?

A
  • Human body = 100 trillion cells, 200 different cell types
  • Primary tissues: muscle, nerves, epithelial, bone, connective, etc.
  • Tissues controlled by: innervation, extracellular fluids, blood supply, exocrine and endocrine secretions
  • Many drugs mimic (or block) the action of endogenous molecules (e.g. neurotransmitters, hormones)
  • Act at specific sites; receptors, ion channels, enzymes, transporters (all of which are proteins)
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20
Q

what are the particular constituents of cells which drug molecules must bind to to produce an effect?

A

drug targets

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21
Q

how to drugs act?

A
  • exert a chemical influence on constituents of cells to produce a pharmacological response
  • must get close enough to cellular constituents in order that they can interact chemically
  • leads to an alteration in molecular / cellular function
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22
Q

what are the protein targets for drug binding?

A
  • receptors
  • enzymes
  • ion channels
  • transporters
  • circulating proteins, DNA, bacterial cell wall etc.
23
Q

what is the main function of receptors?

A

cell to cell communication

24
Q

where is cell to cell communication important?

A
  • Neurotransmission (e.g. nerve to nerve; nerve to muscle)
  • Effects of chemical mediators in bloodstream (e.g. adrenaline on heart)
  • Hormone and growth factor signalling (e.g. action of insulin on muscle)
25
Q

what is a receptor?

A

A recognition molecule for a chemical mediator through which a response is transduced
- often a protein/ protein complex on cell surface
- many drugs act to mimic/block the effect of the endogenous molecules at their receptors

26
Q

describe the basic lock and key concept

A
  • Receptor is the lock, drug is the key
  • Some keys fit into the lock (i.e. Drug A) but others do not (i.e. Drug B)
  • Depends on chemical structure
  • Most locks (i.e. receptors) have a master key (an endogenous ligand)
27
Q

what are the three parts of the structure of a receptor?

A
  • extracellular domain
  • transmembrane domain
  • intracellular domain
28
Q

describe the extracellular domain of a receptor

A

Contains ligand binding sites
Comprised of hydrophilic amino acids

29
Q

describe the transmembrane domain of a receptor

A

Anchors protein in membrane
Comprised of hydrophobic amino acids
Typically has α-helical structure

30
Q

describe intracellular domain of a receptor

A

Interacts with effector mechanisms
Comprised of hydrophilic amino acids

31
Q

describe the steps of signal transduction

A
  • Signal: ligand arrives at receptor
  • Reception: ligand binds to receptor
  • Transduction: ligand-bound receptor changes conformation (i.e. shape change)
  • Response: change in conformation leads to some form of intracellular response
32
Q

what is an example of a very fast signal transduction?

A

nicotinic acetylcholine receptor

33
Q

what is an example of a fast signal transduction?

A

muscarinic acetylcholine receptor

34
Q

what is an example of a slow signal transduction?

A

cytokine receptor

35
Q

what is an example of a very slow signal transduction?

A

oestrogen receptor

36
Q

what is a ligand?

A

any chemical that binds to a receptor

37
Q

what is an agonist?

A

a drug that binds to a specific site on a receptor, mimics the effect of the endogenous ligand for that site
- affinity and efficacy

38
Q

what is an antagonist?

A

a drug that binds to a specific site on a receptor, blocks the effect of the endogenous ligand (same or different binding site as ligand)
- affinity NO efficacy

39
Q

what is affinity?

A

fits in

40
Q

what is efficacy?

A

fits and causes a response

41
Q

are responses to drugs always the same?

A

no drug response varies
- Age
- Genetics
- Disease state
- Drug interactions
- Environment

42
Q

what is the difference between general and local anaesthetics?

A

general sedates entire body (loss of consciousness) whereas local only sedates the localised area (consciousness remains)

43
Q

how does anaesthetic work?

A

blocks the transmission of the impulse

44
Q

what is the chemical structure of local anaesthetic?

A

aromatic linked by ester (shorter half-life= shorter effect) or amide bond (longer half-life=longer effect) to a basic side chain

45
Q

how does conduction of a nerve action potential come about?

A

opening of voltage gated Na+ channel and rapid influx of Na+ which depolarises the cell

46
Q

what are the three main states of the Na+ channel

A

resting (negative)
open
inactivated

47
Q

how does local anaesthetic act on the cell?

A
  • LA binds to taget site on INTRAcellular side of Na+ channel (blocks the channel and stabalises it in the inactivated form_
  • this prevents influx of Na+, preventing depolarisation, preventing an action potential, preventing pain perception
  • causes a REVERSIBLE blockage of nerve conduction
48
Q

what needs to happen for local anaesthetic to be effective?

A
  • it must diffuse from the site of administration, across the nerve cell membrane to the intracellular side
  • it must bind to the local anaesthetic target site
  • this being possible is linked to the chemical structures
49
Q

what does the aromatic group influence on local anaesthetic?

A

the hydrophobicity of the drug

50
Q

what does the amine group influence on local anaesthetic?

A

the charge on the drug

51
Q

are local anaesthetics acidic or basic?

A

weak bases

52
Q

why are local anaesthetics used along side vasoconstrictors?

A
  • less blood loss
  • prevents entry into systemic circulation
53
Q

what three things would you want to know about a drug?

A
  • what it does
  • its potency (measure of dose at which it is effective, potent drug= effective at low dosage)
  • its selectivity (selective= works on one receptor not on others)

BDS1 BAMS molecules and cells (20 decks)

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