Introduction to pharmacology 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 (bioactive)

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3
Q

When did pharmacology emerge as a scientific discipline and what was it called?

A

1850s as materia medica (things of medicine)

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4
Q

What is dogma?

A

Belief that is passed down and expected to just be accepted without questioning. e.g. people thought walnuts improved intelligence because they look like the brain.

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5
Q

Famous quote from Paracelsus in 1700s (16th century)

A

“All drugs are poisons…it is only the dose which makes a thing poison”

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6
Q

What is pharmacogenomics?

A

field of medicine investigating how an individual’s genetic makeup influences the effect of a drug - leads to personalised medicine.

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7
Q

Example of a chemical compound used in anasthetics

A

ether

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8
Q

What is nitrous oxide?

A

Chemical compound used 50% with oxygen as a analgesic (painkiller) discovered in 1799

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9
Q

Example of drug used to relieve angina

A

amyl nitrate - dilates coronary arteries

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10
Q

What is angina?

A

Chest pain due reduced blood flow to cardiac muscle

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11
Q

Which drugs were first used as antibiotics in 1935?

A

sulphonamides

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12
Q

Fields that have contributed to the development of pharmacology

A

Therapeutics (magical potions, herbal remedies), Commerce, Chemistry, Biomedical sciences

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13
Q

How can drugs be developed?

A

From natural products (plants, animals), serendipity, altering the structure of an existing molecule, repurposing of an existing drug to treat a different disease, computer-aided design, studying disease processes.

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14
Q

Examples of drugs from plants

A

aspirin |(painkiller) from willow trees, cocaine (LA for eye surface) from cocoa plant, morphine (painkiller) from poppy, quinine (anti-malarial) from cinchona tree, digoxin (heart failure) from foxglove, statins (lower cholesterol) from guggul tree.

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15
Q

Examples of drugs from animals

A

insulin isolated from dog pancreases was injected into diabetics, hirudin (anticoagulant) from leeches, ziconotide (painkiller) from cone snail, peptide which lowers BP (forerunner of ACE inhibitors) from bothrops jararaca.

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16
Q

What is serendipity?

A

accidental drug discovery

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17
Q

Example of how computer-aided design can lead to drug discovery

A

high throughput screening can analyse possible effects of drugs, 3D modelling to design a molecule to bind to a receptor ect.

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18
Q

Example of serendipity

A

discovery of antibacterial properties of Penicillium mould by Fleming in 1928

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19
Q

Example of drug re-purposing

A

Sildenafil was invented as a drug to lower blood pressure (antihypertensive). During clinical trials the side effect of treating erectile dysfunction lead to the re-purposing of sildenafil and it was sold as Viagra (proprietary name)

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20
Q

What is pharmacoeconomics?

A

Branch of health economics that evaluates the cost of a drug with its outcomes and whether it will be successful in a market (e.g. in NHS?)

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21
Q

3 types of names drugs can have

A

chemical (describes chemical structure), generic (international non-proprietary name of molecule e.g. Sildenafil), proprietary (trade/brand name)

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22
Q

Ways of measuring the effect of a drug in the laboratory

A

second messenger responses (e.g. how much cAMP accumulates), membrane responses (e.g. membrane potential with LA), reflex responses to noxious stimuli (e.g. place dog on a heated plate to see if they lift their paws), behavioural responses to noxious environment (e.g. place animal in maze)

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23
Q

What is pharmacokinetics?

A

Describes the fate of a drug molecule following administration and how a drug is affected by exposure to cells (what the body does to the drug)

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24
Q

What is pharmacodynamics?

A

The mechanism of drug action and what happens to cells, organs, systems when exposed to the drug (what the drug does to the body)

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25
Q

Elements involved in pharmacokinetics

A

Absorption, distribution, metabolism and excretion of the drug

26
Q

Examples of proteins affecting pharmacokinetics

A

drug transporters, metabolising enzymes, plasma proteins e.g. drug-albumin binding.

27
Q

Examples of cells that affect pharmacokinetics

A

epithelial cells (oral administration), endothelial cells (IV administration), hepatocytes

28
Q

What are the possible routes of drug penetration into cells?

A

Diffusion through lipid membrane (lipophilic drugs) or aqueous channels (small drugs), carrier-mediated transport (hydrophilic drugs), pinocytosis (uptake of ECF and molecules)

29
Q

How do lipophilic drugs generally enter cells?

A

Diffusion through lipid membrane

30
Q

How may small, hydrophilic drugs enter cells?

A

diffusion through aqueous channels

31
Q

How may larger, hydrophilic drugs enter cells?

A

Carrier-mediated transport (uses ATP as drug moves against conc gradient)

32
Q

How is insulin transported into the brain?

A

By pinocytosis

33
Q

Where do drugs ultimately need to reach to be transported to their target?

A

Blood plasma

34
Q

Methods of administration

A

oral, rectal, percutaneous, intravenous, intramuscular (very vascular), intrathecal (injection into spinal canal - CSF), inhalation

35
Q

Which mode of administration delivers the drug directly into the blood plasma?

A

Intravenous

36
Q

Methods of drug elimination/excretion

A

urine, faeces, breast milk, sweat, expired air (used in breathalysers)

37
Q

Which structure must orally absorbed drugs be permeable through?

A

Epithelial cell membrane

38
Q

What features of a drug determines whether it can be orally absorbed?

A

Physicochemical properties - described by Lipinski’s rule of 5

39
Q

What set of rules determine whether a drug can be orally absorbed?

A

Lipinski’s rule of 5 - mw < 500 Daltons, H-bond donors < 6, H bond acceptors < 11, log P < 6.

40
Q

What are the stages of drug metabolism?

A

Phase I and II

41
Q

Why does the body metabolise drugs?

A

To prepare the drug for excretion

42
Q

Which phase of drug metabolism has a greater effect on reducing the drug effectiveness?

A

Phase II

43
Q

What possible reactions may occur during phase I of drug metabolism?

A

Oxidation, reduction, hydrolysis

44
Q

What are pharmacokinetic parameters?

A

monitoring drug behaviour in the body by measuring drug concentration in the plasma / urine.

45
Q

Pharmacokinetic parameters that can be labelled on a plasma concentration-time graph

A

Cmax, Tmax, AUC

46
Q

What is Cmax on a plasma concentration-time graph?

A

The maximum concentration of the drug in the plasma reached after administration

47
Q

What is Tmax in a plasma concentration-time graph?

A

The time at which the maximum drug concentration (Cmax) is reached.

48
Q

What is AUP on a plasma concentration-time graph?

A

Area under the graph which measures the total exposure of the patient to the drug.

49
Q

At what point on a plasma-concentration time graph does the rate of absorption equal elimination? (net conc change is 0)

A

Cmax (absorption phase -> elimination phase)

50
Q

What may lead to the accumulation of drug in the plasms?

A

Frequent doses

51
Q

Possible effects of drugs at a cellular level

A

effect on receptors, ion channels, enzymes, transporters, DNA

52
Q

Possible effects of drugs at an organ/system level

A

effects on heart, kidney, cardiovascular system, CNS

53
Q

Possible effects of drugs on the whole organism

A

therapeutic effect on disease state, side effects (tested on healthy individuals before patients)

54
Q

Possible effects of drugs on a societal level

A

cost (health economics), misuse, drug resistance

55
Q

How are tissues controlled?

A

By innervation, ECF, blood supply, exocrine and endocrine secretions

56
Q

Examples of specific sites drugs can target

A

receptors, ion channels, enzymes, transporters (all are proteins)

57
Q

How many cells in the human body?

A

100 trillion cells

58
Q

How many cell types in the human body?

A

200

59
Q

What are endogenous molecules?

A

Molecules that originate internally (e.g. neurotransmitters, hormones). Their action can be mimicked by drugs

60
Q

What are agonists?

A

Chemicals that stimulate a receptor to produce a response

61
Q

What are antagonists?

A

Binds to receptors, blocking them, which opposes their action.