Basics of Drug Pharmacology Flashcards

1
Q

What is a drug?

A

Any substance intended for use in diagnosis, cure, mitigation, treatment or prevention of disease

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2
Q

What is a drug substance?

A

Material exerting pharmacological action with excipients used to formulate medicinal product

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3
Q

What is a drug product?

A

One or more drug substances that contains excipients

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4
Q

What are the general properties of drugs?

A

Therapeutic effect
Side effects
Drug interaction with other drugs

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5
Q

What is therapeutic effect?

A

Desirable drug action

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6
Q

What are side effects?

A

Undesirable or harmful drug actions

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7
Q

What can drug interactions with other drugs produce?

A

Unpredictable effects

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8
Q

What is the sequence of drug discovery?

A
Target selection
Lead discovery 
Medicinal chemistry
In vitro studies
In vivo studies
Clinical trials
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9
Q

What is hit identification?

A

Once you have a target, you need to synthesise compound

Molecules identified have affinity for target

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10
Q

What test systems are required for hit identification?

A

Recombinant protein expressed artificially in cells grown in lab
Isolated enzyme assay
Biochemical assay

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11
Q

How to identify suitable bioassay?

A

Test should be simple, quick + relevant

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12
Q

Describe in vitro identification of suitable bioassay

A

Cheap
Easier
Less controversial

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13
Q

Describe in vivo identification of suitable bioassay

A

Needed to check drug interaction with target

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14
Q

What are in vitro pharmacology assays?

A

Isolated tissues, cells or enzymes

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15
Q

What are enzyme inhibitors tested on?

In vitro pharmacology assays

A

Pure enzyme in solution

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16
Q

What are receptor agonist/antagonists tested on?

In vitro pharmacology assays

A

Isolated tissue/cells

17
Q

How are antibacterial drugs tested?

A

By measuring how effectively they kill in culture

18
Q

What is affinity?

A

Strength of chemical interactions responsible for drug-target interaction

19
Q

What is potency?

A

Degree of functional change imported to receptor upon binding of drug

20
Q

What if efficacy?

A

Extent of biological effect as result of drug-induced modulation of receptor activity

21
Q

Describe lead identification

A
Validated hits would be tested to determine factors such as:
Selectivity vs panel of other receptors
Physiochemical characteristics
Drug-like properties
Metabolic properties (half life)
22
Q

Describe optimisation

A

Molecules fulfilling lead identification criteria can go on to molecular finishing school

23
Q

What happens in optimisation?

A

Extensive SARs to improve potency + selectivity

24
Q

What is optimisation an opportunity for?

A

To improve physiochemical + drug-like properties

25
Q

What happens in preclinical studies?

A
Identify pharmacological properties
PD (mode of action)
PK (metabolism)
Toxicology
Safe initial dose
26
Q

What are the 3 R’s strategy?

A

Reduce no. of animals to min
Refine way experiment carried out = animals suffer as little as possible
Replace animal experiments with non-animal techniques

27
Q

How long does regulatory affairs take?

A

8-15 years

28
Q

What do regulatory affairs look at?

A

Attention to early development = reduce no. of development failures

29
Q

What happens if there is compliance to regulatory affairs?

A

Development success

30
Q

What is a hazard?

A

Potential for damaging effect

31
Q

What is a risk?

A

Includes likelihood that hazard would occur

32
Q

How can risks be reduced?

A

Patient evaluation prior to use for “once a day”
Restrict patient population to those with greatest need
Lower dose
Develop safer analogues

33
Q

When is a drug considered safe?

A

Expected therapeutic gain justifies risk

34
Q

What is pharmacovigilance?

A

Science + activities relating to detection assessment, understand + prevention of adverse effects

35
Q

What is an adverse event?

A

Any untoward medical occurrence in a patient or clinical trial subject administered a medicinal product, which does not necessarily have casual link with treatment

36
Q

What is an adverse reaction?

A

Any untoward + unintended response to an investigational medicinal product related to any drug administered

37
Q

What is an unexpected adverse reaction?

A

An adverse reaction, the nature or severity of which is not consistent with the product info

38
Q

What is a serious adverse event/reaction?

A
Any AE/AR/UAR that results in:
Death
Life threatening
Hospitalisation 
Persistent disability 
Birth defect