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Phase 2a Medicine > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What is pharmacology?

A

The branch of medicine concerned with the uses, effects and modes of action of drugs.

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2
Q

What is draggability?

A

The likelihood of being able to modulate a target with a with a small-molecule drug.

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3
Q

What are most drug targets?

A

Proteins

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4
Q

What is a receptor?

A

A component that interacts with a specific ligand to initiate a change of biochemical events leading to the ligand observed effects.

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5
Q

What are the 3 main chemical stimuli and why are they important to receptors?

A

These chemicals can be neurotransmitters, autacoids or hormones. Receptors are the main way to chemical stimuli.

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6
Q

What are ligand-gated ion channels?

A

A group of transmembrane ion-channel proteins which open to allow ions to pass through the cell membrane.

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7
Q

How are ligand-gated ion channels mediated?

A

They are mediated by an influx of any kind of cation and an efflux of any kind of anion.

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8
Q

What are G protein coupled receptors?

A

The largest and most diverse group of membrane receptors in eukaryotes.

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9
Q

What percentage of drugs target GPCR?

A

They are the largest group of druggable receptors. Targeted by more than 30% of drugs.

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10
Q

What ligands stimulate GPCR?

A

Ligands include light, peptides, lipids, sugars and proteins.

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11
Q

What is the activity of G proteins regulated by?

A

Factors linked to GTP and GDP.

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12
Q

What are kinase linked receptors?

A

Enzyme-linked receptors localized at the plasma membrane.

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13
Q

What are kinases?

A

Enzymes that catalyse the transfer of phosphate groups between proteins (phosphorylation). Uses ATP for the phosphate group.

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14
Q

What are cytosolic/nuclear receptors and how do they work.

A

Normally intracellular molecules. Work by modifying gene transcription.

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15
Q

How does receptor characterisation work?

A

Identify the receptor involved in pathophysiological response. Develop drugs that act on that receptor and quantify drug action at that receptor.

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16
Q

Apart from receptors, what else might drugs target?

A

Enzymes, transporters and ion channels.

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17
Q

What is potency?

A

An expression of the activity of a drug in terms of the concentration or amount of the drug required to produce a defined effect.

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18
Q

What is EC50?

A

The concentration that gives half the maximal response.

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19
Q

What does intrinsic activity refer to?

A

The ability of a drug to produce a maximum receptor response?

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20
Q

What do agonists do?

A

Binds to a receptor and produces an effect within the cell.

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21
Q

What do antagonists do?

A

Antagonists also tend to bind to the receptor, but do not activate it. Block the receptor from being activated.

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22
Q

What is selective agonism?

A

Using agonists as a way of classifying receptors. Potency of a range of agonists.

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23
Q

What is selective antagonism?

A

Using antagonists as a way of classifying receptors. Competitive antagonist.

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24
Q

Affinity definition

A

How well the ligand binds to the receptor. Shown by both agonists and antagonists.

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25
Q

Efficacy definition

A

How well the ligand activates the receptor.

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26
Q

What are the 2 tissue related factors governing drug action?

A

Receptor number and signal amplification.

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27
Q

What is the receptor reserve?

A

Some agonists need to activate only a small fraction of the existing receptors to produce the maximal system response.

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28
Q

What is signal transduction?

A

The transmission of molecular signals from a cell’s exterior to its interior. Signal cascade/amplification means that the final reaction is much greater.

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29
Q

What are allosteric modulators?

A

A group of chemicals that bind to the receptor and make it produce a different response.

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30
Q

What is inverse agonism?

A

A drug binds to the same receptor as an agonists but induces a reverse pharmacological reaction.

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31
Q

What is tolerance in relation to pharmacology?

A

A reduction in the effect of an agonist over time.

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32
Q

What is desensitisation in relation to pharmacology?

A

A rapid reaction. Uncoupled, internalised and degraded.

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33
Q

Does the drug show specificity or selectivity?

A

No compound is ever truly specific. Selectivity is a better term to describe activity.

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34
Q

How does enzyme inhibition work?

A

Enzyme inhibitors bind to an enzyme. They prevent the substrate from entering the enzyme’s active site and prevent it from catalysing its reaction.

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35
Q

Is enzyme inhibition reversible?

A

Can be reversible or irreversible. When the inhibition is irreversible this is usually through covalent bonds.

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36
Q

How are statins enzyme inhibitors?

A

They block the rate limiting step in the cholesterol pathway.

37
Q

What is Parkinson’s disease?

A

Neurological disease that leads to degeneration of dopaminergic neurons in the nigrostriatal pathway leading to autonomic dysfunction and dementia.

38
Q

How is Parkinson’s disease pharmacologically treated?

A

Treated with multiple enzymatic inhibitor drugs.

39
Q

What ion channels require no energy to work (passive)

A

Symporter and channels.

40
Q

What are the 3 main types of protein ports?

A

Uniporters, symporters and antiporters.

41
Q

How do uniporters work?

A

Use energy from ATP to pull molecules in.

42
Q

How do symporters work?

A

Use the movement of one molecule to pull in another molecule against a concentration gradient.

43
Q

How do antiporters work?

A

One substance moves against its gradient, using energy from the second substance (mostly Na+, K+ or H+) moving down its gradient.

44
Q

What are some examples of channels and what goes wrong if they fail?

A

Epithelial channel (sodium)- heart failure. Voltage-gated (calcium, sodium)- nerve, arrhythmia. Metabolic (potassium)- diabetes. Receptor activated (chloride).

45
Q

Xenobiotics definition

A

Chemical substances that are foreign to animal life and therefore include drugs, pesticides, flavourings etc.

46
Q

What is pharmacokinetics?

A

The study of drug absorption, distribution, metabolism, and excretion.

47
Q

What is bioavailability?

A

The proportion of a drug or other substance which enters the circulation when introduced into the body and so is able to have an active effect.

48
Q

How do allergic reactions to drugs develop?

A

Interaction of drug/metabolite/non drug element with patient and diseases.
Subsequent re-exposure.

49
Q

What are the target organs of allergy?

A

Skin, respiratory tract, GI tract, blood and blood vessels.

50
Q

What are the 2 types of anaphylaxis?

A

Immunological or non-immunological (previously known as anaphylactoid).

51
Q

What is type 1 hypersensitivity reaction?

A

Mediated drug hypersensitivity.

52
Q

What is the process of type 1 sensitivity development?

A

Prior exposure to antigen/drug. IgE antibodies are formed. IgE becomes attached to mast cells or leukocytes. Re-exposure then causes mast cell granulation and release of pharmacologically active substances.

53
Q

How quickly does anaphylaxis start and how long does it tend to last?

A

Occurs within minutes and lasts 1-2 hours.

54
Q

What physiological changes occur during anaphylaxis?

A

Vasodilation, increased vascular permeability, bronchoconstriction, urticaria, angio-oedema.

55
Q

What is the most common cause of anaphylaxis?

A

Insect venom. Second most common is medications.

56
Q

What is type 2 hypersensitivity reaction?

A

IgG mediated cytotoxicity.

57
Q

What is the mechanism for type 2 hypersensitivity reactions?

A

Antibody dependent. Drug or metabolite combines with a protein. Body treats it as foreign and forms antibodies (IgG, IgM). Antibodies combine with the antigen and complement activation damages the cells.

58
Q

What is type 3 hypersensitivity reaction?

A

Immune complex deposition.

59
Q

What is the mechanism for type 3 hypersensitivity reactions?

A

Antigen and antibodies form large complexes and activate complement. Small blood vessels are damaged or blocked. Leucocytes attracted to the site of reaction release pharmacologically active substances leading to an inflammatory process.

60
Q

What is type 4 hypersensitivity reaction?

A

T cell mediated.

61
Q

What is the mechanism for type 4 hypersensitivity reactions?

A

Antigen specific receptors develop on T-lymphocytes. Subsequent admin, administration leads to local or tissue allergic reaction.

62
Q

What causes non-immune anaphylaxis?

A

Direct mast cell degranulation. No prior exposure required. Some drugs are recognised to cause this.

63
Q

How does non-immune anaphylaxis present differently to immune anaphylaxis?

A

It doesn’t. They are clinically identical.

64
Q

What are the main features of anaphylaxis?

A

Immediate rapid onset. Rash (absent in 10-20%)
Swelling of lips, face, oedema, central cyanosis
Wheeze / SOB
Hypotension (Anaphylactic shock).

65
Q

How do you managed anaphylaxis?

A

Commence basic life support (ABC). Stop the drug if via infusion. Adrenaline IM 500mcg (300mcg epi-pen).
High flow oxygen
IV fluids
IV antihistamine
IV hydrocortisone
If anaphylactic shock may need IV adrenaline.

66
Q

How does adrenaline cause vasoconstriction in anaphylaxis?

A

Increase in peripheral vascular resistance, increased BP and coronary perfusion via alpha1-adrenoreceptors.

67
Q

How does adrenaline have positive effects on the heart during anaphylaxis?

A

Stimulation of Beta1-adrenoceptors positive inotropic and chronotropic effects on the heart.

68
Q

How does adrenaline attenuates further release of mediators during anaphylaxis?

A

Attenuates further release of mediators from mast cells and basophils by increasing intracellular c-AMP and so reducing the release of inflammatory mediators.

69
Q

What medicinal factors increase the risk of a hypersensitivity reaction?

A

Protein or polysaccharide based macromolecules.

70
Q

What host factors increase the risk of a hypersensitivity reaction?

A

Females>males, EBV and HIV, having had previous drug reactions, uncontrolled asthma.

71
Q

What genetic factors increase the risk of a hypersensitivity reaction?

A

Certain HLA groups. Acetylator status.

72
Q

Polypharmacy definition

A

Regular use of at least five medications.

73
Q

What group of people are most likely to have polypharmacy?

A

Old age people.

74
Q

What is latrogenesis?

A

Any injury or illness that occurs as a result of medical care.

75
Q

What are the 3 types of drug interactions?

A

Synergy, antagonism or other.

76
Q

What are synergy drug interactions?

A

Multiple drugs combining together to have a different effect. Can be positive or negative.

77
Q

What are antagonism drug reactions?

A

One drug stops the other from working.

78
Q

What are other drug reactions?

A

Everything that isn’t either synergy or antagonism.

79
Q

What are the risk factors for drug reactions?

A

Polypharmacy, pharmacokinetic, pharmacodynamic, inhibition, induction, food, hepatic disease, renal disease, old age and genetics (including race)

80
Q

What is a narrow therapeutic index (NTI)?

A

Those drugs where small differences in dose or blood concentration may lead to dose and blood concentration dependent, serious therapeutic failures or adverse drug reactions.

81
Q

Pharmacodynamic definition

A

The study of a drug’s molecular biochemical and physiologic effects or actions.

82
Q

What does drug development consist of?

A

Lead compound identification,

pre-clinical research, filing for regulatory status, clinical trials on human, marketing the drug

83
Q

Why is developing drugs complicated?

A

It takes an enormous amount of time, effort and money

84
Q

What is tested in pre-clinical testing?

A

The test antigens and test adjuvants

85
Q

What is tested on during pre-clinical testing?

A

Animal models- can be mouse, ferret or rhesus macaque

86
Q

What happens during phase I of clinical testing?

A

Dose tested on a small number of volunteers from the at-risk population (about 40) to find out side effects

87
Q

What happens during phase II of clinical testing?

A

Tests both safety and effectiveness of the drug on a larger number of volunteers from the at-risk population

88
Q

What happens during phase III of clinical testing?

A

Tests on

Phase 2a Medicine (6 decks)

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