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Principles of Disease > Drug Lectures > Flashcards

Drug Lectures Flashcards

1
Q

What are the four basic factors that determine drug pharmacokinetics

A

Absorption
Distribution
Metabolism
Elimination

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2
Q

Modes of drug distribution

A 
Oral
Intravenous
Subcutaneous
Intramuscular
Sublingual
Rectal
Inhalation
Nasal
Transdermal
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3
Q

Define absorption

A

The process of movement of unchanged drug from the site of administration of the systemic circulation

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4
Q

What happens as rate of absorption increases

A

The earlier the drug concentration peak

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5
Q

What happens when dose is increased

A

The peak concentration is increased

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6
Q

What does the area under the drug time curve represent

A

The amount of drug which reaches the systemic circulation

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7
Q

What is the therapeutic range

A

The concentration range over which a drug is active

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8
Q

What occurs outwith therapeutic range

A

Above - toxicity

Before - insufficient/no pharmacological action

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9
Q

What does the AUC allow us to estimate

A

The amount of drug which reaches the circulation and which is available for action

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10
Q

Factors affecting bioavailability

A

Formulation
Ability of drug to pass physiological barriers
Gastrointestinal effects
First pass metabolism

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11
Q

What are some physiological barriers that affect bioavailability

A 
Passive diffusion
Filtration
Bulk flow
Active transport
Facilitated diffusion
Ion pair transport
Endocytosis
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12
Q

Can ionised or non ionised forms of a drug pass across a membrane

A

Non ionised

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13
Q

What two things must a drug be to pass a lipid layer

A

Lipid soluble

In solution

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14
Q

What is the lipid-water partition coefficient

A

The ratio of the amount of the drug which dissolves in the lipid and water phase when they are in contact
The ability of a drug to diffuse across a lipid barrier

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15
Q

Characteristics of passive diffusion

A 
Very common
Occurs along concentration gradient
Non selective
Not saturable
Requires no energy
No carrier
Depends on lipid solubility  and degree of ionisation
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16
Q

Characteristics of active absorption

A 
Occurs against concentration gradient 
Requires carrier and energy 
Specific and uncommon
Saturable
Drugs must resemble naturally occurring compounds
Reversibly bound to carrier system
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17
Q

Characteristics of facilitated diffusion

A

Occurs along the concentration gradient
Requires carriers
Saturable and specific
No energy required

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18
Q

How does motility affect drug absorption

A

Motility of gastric absorption will affect speed at which drug reaches site of absorption. Motility can be affected by other drugs, food/drink and illnesses

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19
Q

Gastrointestinal factors affecting drug absorption

A

Motility
Food
Illness

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20
Q

How does food affect drug absorption

A

Can enhance or impair rate of absorption

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21
Q

How does illness affect drug absorption

A

Malabsorption can increase or decrease rate of absorption

Migraine reduces rate of stomach emptying and therefore rate of absorption

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22
Q

Upon which route is first pass metabolism inhibiting

A

Oral

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23
Q

Why would you use the rectal route

A

For drugs which cause irritation of the somach

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24
Q

What is drug distribution

A

Drug distribution refers to the reversible transfer of a drug between the blood and he extra vascular fluids and tissues of the body

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25
Q

The amount of bound drug can be changed by what

A 
Renal failure
Hypoalbuminaemia
Pregnancy
Other drugs
Saturability of binding
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26
Q

What is the volume of distribution

A

The volume of plasma that is necessary to account for the total amount of drug in a patients body, if that drug were present throughout the body at the same concentration as found in the plasma

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27
Q

Define clearance

A

The theoretical volume from which a drug is completely removed over a period of time. Is a measure of elimination

28
Q

Define half life

A

The time taken for the drug concentration in the blood to decline to half of the correct value

29
Q

What does half life depend on

A

Volume of distribution and rate of clearance

30
Q

What increases as half life is prolonged

A

Toxicity of a drug

31
Q

What is drug elimination

A

The removal of active drug and metabolites from the body and determines the length of action of the drug

32
Q

What are the 2 parts of drug elimination

A

Drug metabolism - usually in liver

Drug excretion - usually in kidney

33
Q

What is the primary organ for drug excretion

A

Kidneys

34
Q

What are the three principal mechanisms used in excretion

A

Glomerular filtration
Passive tubular reabsorption
Active tubular reabsorption

35
Q

Modes of drug delivery

A 
Tablets or capsules
Solutions or suspensions
Ointments and creams
Inhalation
Injections
Suppositories
Pessaries
36
Q

What three factors determine the drug delivery system we use

A

The dose to be given
The frequency of administration
The timing of administration

37
Q

When is a solution or suspension useful

A

For elderly or young with swallowing difficulties

38
Q

What is the most commonly used formulation for drug delivery

A

Tablets and Capsules

39
Q

What are the advantages of tablets and capsules

A 
Convenience
Accuracy of dose
Reproducibility
Drug stability
Ease of mass production
40
Q

What is the purpose of enteric coating

A

Delay disintegration of the tablet until it reaches the small intestine
Protect drug from stomach acid and protect stomach from the drug

41
Q

What are prodrugs

A

Synthesised inactive derivatives of an active drug which requires to be metabolically activated after administration

42
Q

What are the advantages of using pro drugs

A

Prolongation of duration of action

Avoidance of degradation of drug in the gut

43
Q

What type of drug would be used in the sublingual or buccal routes

A

Ones with extensive first pass metabolism

44
Q

Why would the rectal route be used

A

If patient is unable to swallow

To bypass pre systemic metabolism

45
Q

Properties of injection based drug delivery

A

Fast systemic effects
Bypassing first pass metabolism
Can be administered to unconscious/comatose patients
Can be infused continuously

46
Q

Why would you use intravenous administration

A

Rapid onset of action is required
Careful control of plasma levels is requires
Drug has a short half life

47
Q

Properties of intramuscular injection

A

Injection into muscle mass
May be painful
Drug may be insoluble or formulated in an oil base
More sustained duration of action, up to months incase of contraceptive

48
Q

Features of subcutaneous injection

A

Easy
Bypasses need for venous access
Used for insulin, heparin and narcotic analgesics

49
Q

What would percutaneous drugs be used for

A

Local effect by administration to skin

50
Q

Advantages of drug delivery via inhalation

A 
Delivered directly to site of action
Rapid
Small doses
Little systemic absorption
Reduced adverse affects
51
Q

Big disadvantage of drug delivery via inhalation

A

Patient education is essential

52
Q

Definition of adverse drug reaction

A

Any response to a drug which in noxious, unintended and harmful/unpleasant

53
Q

What is acute onset of ADR

A

Within an hour

Bronchoconstriction

54
Q

What is sub acute onset of ADR

A

1-24hours

Rash, serum sickness

55
Q

What is latent onset of ADR

A

Over 2 days

Eczematous eruptions

56
Q

Define mild severity of ADR

A

Bothersome but no change in therapy

Metallic taste

57
Q

Define moderate severity of ADR

A

Requires change in therapy and additional treatments, possibly hospitalisation
Amphotericin induced hypokalemia

58
Q

Define severe ADR

A

Disabling or life threatening

Renal failure

59
Q

Predisposing factors to ADRs

A 
Multiple drug therapy
Inter current disease
Race and genetic polymorphisms
Age
Sex
60
Q

Define drug interaction

A

The modification of a drugs effect by prior or concomitant administration of another drug, herb foodstuff, drink etc
OR
When the pharmacological effect of two or more drugs given together is not just a direct function of their individual effects

61
Q

Types of drug interactions

A 
Drug-drug
Drug-herbal
Drug-food
Drug-drink
Pharmacogenetic
62
Q

What name is given to the drug whose activity is effected by an interaction

A

Object drug

63
Q

What is the name given to the drug which precipitates a drug interaction

A

Precipitant

64
Q

Which chronic conditions make patients susceptible to severe drug interactions

A 
Liver disease
Renal impairment
Diabetes
Epilepsy
Asthma
65
Q

Effects of absorption due to drug interaction in GI tract

A

Most result in change to absorption rate rather than extent

66
Q

Effects on GI tract after drug interactions

A

May lead to failure of oral contraceptive or digoxin toxicity
Gastric emptying is rate limiting step, some drugs increase and many delay this process

67
Q

How can drug distribution be altered by drug interactions

A

Protein binding displacement, occurs when there is a reduction in extent of plasma protein binding of a drug caused by presence of another
Results in increased bioavalibility

Principles of Disease (5 decks)

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