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Principles of disease AM > Drugs > Flashcards

Drugs Flashcards

1
Q

What is absorption?

A

Process of movement of the unchanged drug from the site of administration to the systemic circulation

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2
Q

What is Cmax?

A

Drug concentration peak

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3
Q

What is Tmax?

A

The time at which Cmax us observed

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4
Q

What is bioavailability?

A

The amount of the drug available for action in the systemic circulation

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5
Q

What factors affect bioavailability?

A

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

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6
Q

What are some physiological barriers drugs encounter?

A

Lipid solubility
pH
Ionisation

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7
Q

How does ionisation affect drug diffusion?

A

An ionised drug will not cross the cell membrane

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8
Q

What is the Henderson-Hasselbalch equation used to show?

A

The relationship between local pH and the degree of ionisation

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9
Q

What is the Henderson-Hasselbalch equation?

A

pH=pKa+log10([A-]/[HA])

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10
Q

What is the lipid water partition coefficient?

A

The ratio of the amount of drug which dissolves in the lipid and water phase when they are in contact

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11
Q

How does lipid solubility affect diffusion across a membrane?

A

A drug must be lipid soluble to diffuse across a membrane

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12
Q

By what methods can drugs pass across the membrane?

A 
Passive diffusion
Filtration
Bulk flow
Active transport
Facilitated diffusion
Ion pair transport
Endocytosis
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13
Q

What drugs cross the membrane via facilitated diffusion?

A

Monosaccharides, amino acids, vitamins

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14
Q

What is the driving force for filtration, bulk flow and pore transport?

A

The difference in hydrostatic or osmotic pressure

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15
Q

What gastrointestinal factors affect drug absorption?

A

Motility
Food
Illness

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16
Q

What is first pass metabolism?

A

Metabolism of drug prior to it reaching the systemic circulation

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17
Q

What are the 4 primary systems that affect first pass metabolism?

A

GI lumen
Gut wall enzymes
Bacterial enzymes
Hepatic enzymes

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18
Q

What are the benefits of subcutaneous and IM administration?

A

Only a small volume required
Avoids first pass metabolism
Water soluble drugs absorbed well

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19
Q

What are the benefits of buccal and sublingual administration?

A

Avoids first pass metabolism

Enter circulation directly

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20
Q

What are the benefits and disadvantages of suppositories?

A

Avoids first pass metabolism
Can be used for drugs that irritate stomach
Absorption tends to be slow

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21
Q

What are the benefits of inhalation of drugs?

A

Can be used for volatile agents
Relatively rapid action
Can be used for topical or systemic effects

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22
Q

What are the advantages and disadvantages of transdermal administration?

A

Avoids first pass metabolism
Controlled release
Few substances well absorbed
Needs to be nonirritant

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23
Q

What is drug distribution?

A

Reversible transfer of a drug between the blood and extravascular fluids and tissues of the body

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24
Q

What factor affect tissue distribution?

A 
Plasma protein binding
Tissue perfusion
Membrane characteristics
Transport mechanisms
Diseases and other drugs
Elimination
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25
Q

What is the effect of plasma protein binding?

A

Only unbound drugs are biologically active

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26
Q

What factors affect the amount of a drug that binds to plasma proteins?

A 
Renal failure
Hypoalbuminaemia
Pregnancy
Other drugs
Saturability of binding
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27
Q

What is the apparent volume of distribution (Vd)?

A

Theoretical volume that would be necessary to contain the amount of the administered drug at the same concentration as it is in the plasma

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28
Q

What is the correlation between Vd and the ability of a drug to diffuse?

A

The higher the Vd, the better the drug is at diffusing

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29
Q

What is clearance?

A

The theoretical volume from which a set amount of a drug is completely removed over time

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30
Q

What is drug clearance dependent on?

A

Urine flow rate for renal clearance

Metabolism and biliary secretion for hepatic clearance

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31
Q

What is half life (t1/2)?

A

Time taken for the drug concentration in the blood to half

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32
Q

What is the half life dependent on?

A

Volume of distribution and rate of clearance

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33
Q

What does prolongation of the half life cause?

A

Toxicity

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34
Q

When is steady state reached in chronic administration?

A

Usually after approx 4 half lives

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35
Q

What is elimination?

A

Removal of the active drug and its metabolites from the body

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36
Q

What are the 3 stages of drug elimination?

A

Metabolism and excretion

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37
Q

Where does most of drug metabolism take place?

A

Liver

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38
Q

What is the primary organ of drug excretion?

A

Kidneys

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39
Q

What are the 3 principle mechanisms of drug excretion?

A

Glomerular filtration
Passive tubular reabsorption
Active tubular secretion

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40
Q

What drugs are filtered during glomerular filtration?

A

All unbound drugs, as long as they size, charge or shape are not excessively large

41
Q

What happens in active tubular secretion?

A

Acidic and basic compounds are actively secreted into the proximal tubule

42
Q

Why is active tubular secretion important?

A

Eliminating protein bound cationic and anionic drugs

43
Q

What is the process of passive tubular reabsorption?

A

As the filtrate moves down the renal tubule, any drug present is concentrated and passive diffusion allows some of the drug to diffuse across the membrane back into circulation

44
Q

Where does passive tubular reabsorption tale place?

A

Distal tubule and collecting duct

45
Q

What is biliary secretion?

A

Secretion of the drug into the bile where it can then be reabsorbed into the enter-hepatic circulation

46
Q

What does metabolism in the liver lead to and what does this cause?

A

Conjugation of the drug

Cannot be reabsorbed into the circulation

47
Q

What ways are drugs delivered to patients?

A 
Tablets or capsules
Solutions or suspensions
Ointments and creams
Inhalation
Injections
Suppositories
Pessaries
48
Q

Why are there different drug formulations?

A

To allow selective targeting, avoid pre or systemic metabolism, allow for fast or slow release

49
Q

Where are oral medications absorbed?

A

GI tract

50
Q

Who are solutions or suspensions used for?

A

Young, old, those with difficulty swallowing

51
Q

What is the rate limiting step in absorption of tablets?

A

Break down of the tablet

52
Q

What are the advantages of tablets and capsules?

A 
Convenient
Accurate dose
Reproducability
Drug stability
Ease of mass production
53
Q

What are enteric coated tablets?

A

A drug with a protective coating to protect the drug from the stomach and the stomach from the drug

54
Q

Why are prolonged or delayed release formulations useful?

A

Most conditions require prolonged therapy
Maintains drug levels within therapeutic range
Reduces need for frequent dosing
Improved compliance

55
Q

What are prodrugs?

A

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

56
Q

What are buccal and sublingual administration ideal for?

A

Drugs with extensive first pass metabolism

57
Q

Who is the rectal route useful for?

A

Young, old, patients unable to swallow

58
Q

What can the rectal route be used to treat?

A

Local conditions, or systemic absorption

59
Q

What are pessaries used for?

A

To treat local conditions

60
Q

What are the 3 forms of injection based administration?

A

IV
IM
Subcutaneous

61
Q

When is IV used?

A

When rapid onset of action id required
Careful control of plasma levels required
Drug has short half life

62
Q

How can IV be given?

A

Rapidly
Slowly- to prevent toxic effects
Continuoisly- ensure accurate controls of plasma levels

63
Q

What does IM allow for?

A

More sustained duration of action

64
Q

What are subcutaneous injections used to administer?

A

Insulin
Heparin
Narcotic analgesics

65
Q

What are 2 types of subcutaneous administration?

A

Dermojet

Pellet implantation

66
Q

Why is subcutaneous injection uses?

A

Bypasses need for venous access

Slow absorption

67
Q

What is transdermal drug delivery?

A

Adhesive patched containing the drug are applied to the skin, drug crosses the surface by diffusion and goes into systemic circulation

68
Q

What is the benefit of transdermal drug delivery?

A

Bypasses first hepatic inactivation

69
Q

What can percutaneous drugs be used for?

A

Local or systemic

70
Q

Give an example of a systemic percutaneous drug?

A

Transderm-SCOP

71
Q

Give an example of a local percutaneous drug?

A

Hydrogel transdermal patch

72
Q

How can inhalation drugs be administered?

A

Pressurised aerosol, breath activated aerosol, nebuliser, dry powder device

73
Q

What are the advantages of inhalation?

A 
Delivered directly to site of action
Rapid effect
Small doses uses
Little systemic absorption
Reduced adverse effects
74
Q

What are the 3 types of carrier based drug delivery?

A

Monoclonal antibodies
Liposomal drug delivery
Nanoparticle based drug delivery

75
Q

How do monoclonal antibodies work as a carrier based drug delivery system?

A

Modified antibodies with attached toxins cytokines etc act directly when binding to a cancer specific antigen and induce immunological response

76
Q

How does a liposomal drug delivery system work?

A

Allows for drug accumulation at disease sites and avoidance of sensitive sites

77
Q

How do nanoparticles work as a carrier based drug delivery system?

A

Drug can be targeted to precise location, making the drug more effective and reduce side effects

78
Q

What are the 3 types of nano carriers?

A

Nanoparticle
Nanotubule
Nanoshell

79
Q

What are carbon nanotubes used to treat?

A

Bronchial asthma

80
Q

What are gold nano tubules used to treat?

A

Chemo

81
Q

What are nanoerythrosomes and what are they used for?

A

Resealed erythrocytes that carry proteins, enzymes and macromolecules
Used in treatment of liver tumour and enzyme and pancreatic diseases

82
Q

What is an adverse drug reaction?

A

Any response to a drug which is harmful, unintended and occurs in doses used for prophylaxis, diagnosis or treatment

83
Q

What are the classifications of onset of adverse drug reactions?

A

Acute- within 60 minutes
Sub-acute- 1-24 hours
Latent- >2days

84
Q

What are the classifications of severity of adverse drug reactions?

A 
Mild= bothersome but requires no change in treatment
Moderate= Requires change in therapy, additional treatment, hospitalisation
Severe= Disabling, life threatening
85
Q

What are the classifications of adverse drug reactions?

A 
Augmented
Bizarre
Chronic
Delayed
End of treatment
Failure of treatment
86
Q

What is a type A drug reaction?

A

Augmented
Dose related and predictable
Resolve when drug is reduced or stopped

87
Q

What causes a type A drug reaction?

A

Too high a dose
Pharmaceutical variation
Pharmacokinetic variation
Pharmacodynamic variation

88
Q

What is a type B drug reaction?

A

Bizarre
Rare and unrelated to dose
Can cause serious illness

89
Q

What causes a type B drug reaction?

A

Immunological or genetic response

90
Q

When are type B drug reactions more common?

A

With macromolecules
Patients with history of asthma or eczema
Presence of leukocyte antigen
Sex linked G6P deficiency

91
Q

What is a type C drug reaction?

A

Chronic
Does not occur with single dose
Semi predictable

92
Q

What is a type D drug reaction?

A

Delayed

Occur in children of patients or patients years after end of treatment

93
Q

What are some examples of type D drug reactions?

A

Second cancers in those treated with alkylating agent or immunosuppressants
Graniofacial malformations in children of those treated with isotrtinoin

94
Q

What is a type E drug reaction?

A

End of treatment

Adverse reaction when treatment is stopped, particularly when it was stopped suddenly

95
Q

What are some examples of type E drug reactions?

A

Unstable angina or MI when taken off beta blockers

Withdrawal seizures when taken off anti-epileptics

96
Q

What are type F drug reactions?

A

Failure of treatment
Common and dose related
Frequently caused by drug interactions

97
Q

What are the 4 steps in diagnosis a type F drug reaction?

A

Differential diagnosis
Medication history
Assess time of onset and dose relationship
Lap investigations

98
Q

What are the risk factors of adverse drug reactions?

A 
Age
Multiple medications
Inappropriate medication prescribing, use or monitoring
End organ dysfunction
Altered physiology
History of adverse drug reactions
Dose and duration of exposure
Genetic predisposition

Principles of disease AM (16 decks)

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