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
The amount of bound drug can be changed by what
``` Renal failure Hypoalbuminaemia Pregnancy Other drugs Saturability of binding ```
26
What is the volume of distribution
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
27
Define clearance
The theoretical volume from which a drug is completely removed over a period of time. Is a measure of elimination
28
Define half life
The time taken for the drug concentration in the blood to decline to half of the correct value
29
What does half life depend on
Volume of distribution and rate of clearance
30
What increases as half life is prolonged
Toxicity of a drug
31
What is drug elimination
The removal of active drug and metabolites from the body and determines the length of action of the drug
32
What are the 2 parts of drug elimination
Drug metabolism - usually in liver | Drug excretion - usually in kidney
33
What is the primary organ for drug excretion
Kidneys
34
What are the three principal mechanisms used in excretion
Glomerular filtration Passive tubular reabsorption Active tubular reabsorption
35
Modes of drug delivery
``` Tablets or capsules Solutions or suspensions Ointments and creams Inhalation Injections Suppositories Pessaries ```
36
What three factors determine the drug delivery system we use
The dose to be given The frequency of administration The timing of administration
37
When is a solution or suspension useful
For elderly or young with swallowing difficulties
38
What is the most commonly used formulation for drug delivery
Tablets and Capsules
39
What are the advantages of tablets and capsules
``` Convenience Accuracy of dose Reproducibility Drug stability Ease of mass production ```
40
What is the purpose of enteric coating
Delay disintegration of the tablet until it reaches the small intestine Protect drug from stomach acid and protect stomach from the drug
41
What are prodrugs
Synthesised inactive derivatives of an active drug which requires to be metabolically activated after administration
42
What are the advantages of using pro drugs
Prolongation of duration of action | Avoidance of degradation of drug in the gut
43
What type of drug would be used in the sublingual or buccal routes
Ones with extensive first pass metabolism
44
Why would the rectal route be used
If patient is unable to swallow | To bypass pre systemic metabolism
45
Properties of injection based drug delivery
Fast systemic effects Bypassing first pass metabolism Can be administered to unconscious/comatose patients Can be infused continuously
46
Why would you use intravenous administration
Rapid onset of action is required Careful control of plasma levels is requires Drug has a short half life
47
Properties of intramuscular injection
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
Features of subcutaneous injection
Easy Bypasses need for venous access Used for insulin, heparin and narcotic analgesics
49
What would percutaneous drugs be used for
Local effect by administration to skin
50
Advantages of drug delivery via inhalation
``` Delivered directly to site of action Rapid Small doses Little systemic absorption Reduced adverse affects ```
51
Big disadvantage of drug delivery via inhalation
Patient education is essential
52
Definition of adverse drug reaction
Any response to a drug which in noxious, unintended and harmful/unpleasant
53
What is acute onset of ADR
Within an hour | Bronchoconstriction
54
What is sub acute onset of ADR
1-24hours | Rash, serum sickness
55
What is latent onset of ADR
Over 2 days | Eczematous eruptions
56
Define mild severity of ADR
Bothersome but no change in therapy | Metallic taste
57
Define moderate severity of ADR
Requires change in therapy and additional treatments, possibly hospitalisation Amphotericin induced hypokalemia
58
Define severe ADR
Disabling or life threatening | Renal failure
59
Predisposing factors to ADRs
``` Multiple drug therapy Inter current disease Race and genetic polymorphisms Age Sex ```
60
Define drug interaction
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
Types of drug interactions
``` Drug-drug Drug-herbal Drug-food Drug-drink Pharmacogenetic ```
62
What name is given to the drug whose activity is effected by an interaction
Object drug
63
What is the name given to the drug which precipitates a drug interaction
Precipitant
64
Which chronic conditions make patients susceptible to severe drug interactions
``` Liver disease Renal impairment Diabetes Epilepsy Asthma ```
65
Effects of absorption due to drug interaction in GI tract
Most result in change to absorption rate rather than extent
66
Effects on GI tract after drug interactions
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
How can drug distribution be altered by drug interactions
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