Intro to pharmacology Flashcards

1
Q

Pharmacology

A

Science of drug action

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2
Q

Drug

A

Anything w/ positive or desired effect

Substance used in diagnosis, treatment or prevention of disease or as a component of a medication

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3
Q

Poison

A

Anything w/ negative or undesired effect

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4
Q

Legal status of drugs

A

POM
PM
GSL

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5
Q

POM

A

Prescription only medication

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6
Q

PM

A

Pharmacy medication

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7
Q

GSL

A

General sales medication

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8
Q

Branches of pharmacology

A

Pharmacokinetics

Pharmacodynamics

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9
Q

Pharmacokinetics

A

How the body affects the drug

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10
Q

Pharmacodynamics

A

How the drug affects the body

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11
Q

Drugs can be …

A

Agonist

Antagonist

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12
Q

Agonist

A

Activate receptors and elicit a response e.g. drugs, hormones, neurotransmitters bitter, signalling molecules

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13
Q

Antagonist

A

Prevent (block) effect of agonist; can be competitive or non-competitive

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14
Q

Examples of agonist/antagonist interactions

A

Morphine is released at a synapse (agonist) and naloxone fits into the dips on the other neurone (antagonist) blocking the morphine

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15
Q

Receptors

A

Proteins located on cell membranes, respond to endogenous compounds (hormones)

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16
Q

Transport systems

A

Ion channels, either voltage gated (Ca2+, K+, Na+) or ligand gated

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17
Q

G coupled proteins

A

Located in cell membranes and bounds extracellular substances to an intracellular molecule

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18
Q

Affinity

A

How well does the drug bind to receptor

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19
Q

What does drug affinity depend on

A

Conc of drug [D]

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20
Q

What does removal of a drug depend on

A

How well it bound in 1st place

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21
Q

Receptor binding

A

How many receptors are occupied

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22
Q

How is rship between drug conc and receptor binding calculated

A

p = [D]/ [D] + Kd

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23
Q

Dose

A

How much drug is needed for therapeutic response

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24
Q

What should drug + receptor =

A

Chemical response but this depends on efficacy

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25
Efficacy
``` 2 drugs Same concept Same receptor binding ability (affinity) Different efficacy Diff chemical effects ```
26
Examples of drugs w/ diff efficacy
Benzodiazepines, lorazepam and temazepam have a 10-fold diff in dose
27
Key point about efficacy and dosage
``` Not all drugs in the same class and receptor site will have similar doses As a result, medication ha sits own currency ```
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Stages of pharmacokinetics
Absorption Distribution Metabolism (after body realises drug is exogenous) Excretion
29
Absorption in pharmacokinetics
Getting drug into body - so it can work Everything given via mouth will go through dissolution phase Pass through gut wall into bloodstream ---> even distribution around the body
30
What does absorption depend on
Drug solubility - lipophilic or hydrophilic
31
Why is drug solubility important
Allows us to decipher how to get the drug into the body
32
Lipid soluble drugs
Pass through the gut and enter the bloodstream a lot quicker e.g. hormones
33
What happens when drugs are distributed unto water compartments in the blood
Exposed to plasma proteins - where once bound can become ineffective (unable to traverse cell membranes)
34
Routes of administration
``` Oral (po) Inhaled (inh) Topical (top) Sub lingual (s/l) Rectal (pr) Parental ```
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Oral administration
po | Most common, ease of administration
36
Inhaled administration
Volatile anaesthetics/ local delivery in asthma
37
Topical administration
Skin/eyes/ears - local delivery
38
Sub lingual administration
Rapid onset action | Under tongue
39
Example of drug given sub lingually
GTN - Glyceryl trinitrate | Used to treat angina
40
Rectal administration
Bypass portal circulation
41
Parental administration
Bypassing GI system | Straight into blood stream
42
Types of parental administration
``` Subcutaneous Intramuscular Intravenous Transdermal Implantation ```
43
Subcutaneous parental administration
Drug infected into fat at 90 degrees, usually in stomach
44
Drugs given by subcutaneous parental adminstarion
Insulin | LMWH
45
LMWH
Low molecular weight heparin
46
Intramuscular parental administration
Less common mode of administration Usually done in big muscles e.g. thigh Not many licensed to do Used when we want to give drugs slowly i.e. give the drug in a neuroleptic preparation (depressing nerve functions)
47
Transdermal parental administration
Continual drug release
48
Examples of drugs given by transdermal parental administration
Morphine | NRT
49
NRT
Nicotine replacement therapy
50
Intravenous parental administration
100% bioavailability | Good for infusions, rapid access and drug delivery in large volumes
51
Bioavailability
% unchanged drug that reaches the systemic circulation
52
Implantation parental administration
Hormones/steroids | Targeted and continual drug release
53
What allows us to figure out the dose of a drug
Half life Vd Clearance
54
Half life
Time it takes drug conc to drop to half of orig
55
Vd
Volume of distribution | How much volume the drug has to distribute itself into
56
Clearance
Volume of plasma/ blood cleared of drug
57
Metabolism in pharmacokinetics
Occurs throughout body - usually in liver (lipophilic) | Important because determines therapeutic and toxic effects of drugs and allows you too optimise therapy, minimise harm
58
Metabolites
Products of metabolism | Commonly less potent than the drug but can be more potent - prodrugs
59
Prodrugs
The drug given to patient is partially active, once metabolised becomes a more potent agent that can provide local relief Offshoots are active drugs
60
Excretion in pharmacokinetics
Principally occurs in kidneys Kidney = hydrophilic agents Clearance via glomerular filtration
61
Why do we aim to make drugs more hydrophilic
More water soluble --> more easily excreted by the kidneys
62
Kinase linked receptors
Ligand binding activates an intracellular protein that triggers a cascade of phosphorylation reactions
63
Selectivity
Propensity for a drug to bind to one target rather than an other
64
Partial agonists
Activate the receptor but cannot produce a maximal signalling effect equivalent to that of a full agonist, even when all receptors are occupied
65
Potency
Amount of drug required for a given response
66
What do more potent drugs produce
Biological effects at lower doses
67
ED 50
Dose producing half the value of the maximum response
68
Therapeutic index
Ratio of the ED50 for therapeutic efficacy and for a major adverse effect Indicates how much margin prescribers have when choosing a dose that will provide beneficial effects w/ out causing adverse effects
69
Toxic effects
Adverse effects that occur at doses above the therapeutic range
70
Side effects
Adverse effects that occur within the therapeutic range
71
Hyper-susceptible effects
Adverse effects occurring below the therapeutic range
72
Why do we have to give drugs on a frequent basis
The body will wash it out
73
Factors to consider when choosing a drug
``` Absorption Distribution Metabolism Excretion Efficacy Avoiding adverse effects and drug interactions Features of the disease Severity of disease Coexisting disease Cost Patient adherence to therapy ```