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IMS > Topic 10 - Pharmacology > Flashcards

Topic 10 - Pharmacology Flashcards

1
Q

What is pharmacology?

A

The branch of medicine concerned with the uses, effects, and modes of action of drugs.

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2
Q

What are pharmacodynamics?

A

Specific to drug or drug class:

  • interaction with cellular component
  • concentration-effect relationship
  • modification of disease progression
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3
Q

What are pharmacokinetics?

A

Non-specific, general processes:

  • absorption from the site of administration
  • time to onset of effect
  • elimination from the body
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4
Q

What is the generic drug name?

A

Approved or official name

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5
Q

What is the trade/brand name of a drug?

A

‘Proprietary’ name is given to a drug by its

pharmaceutical producer

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6
Q

What is the chemical name of a drug?

A

Each drug has its own chemical structure

and given an appropriate chemical name

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7
Q

What is the use name of a drug?

A

Commonly drugs are categorised according
to the use for which they are prescribed
e.g. anti-hypertensives, contraceptives,
anti-inflammatories

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8
Q

What is the effect name of a drug?

A

For some drugs, the categorisation relates
to the physiological or biological response
in the body

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9
Q

What are the advantages of the oral route of administration?

A

Convenient, safe, economical

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10
Q

What are the disadvantages of the oral route of administration?

A

Cannot be used for drugs
inactivated by 1st pass metabolism
or that irritate the gut

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11
Q

What are the advantages of the intramuscular route of administration?

A

-Suitable for suspensions and oily vehicle
-Rapid absorption from solutions
-Slow and sustained absorption from
suspensions

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12
Q

What are the disadvantages of the intramuscular route of administration?

A
  • May be painful

- May cause bleeding at site of injection

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13
Q

What are the advantages of the subcutaneous route of administration?

A

Suitable for suspensions and pellets

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14
Q

What are the disadvantages of the subcutaneous route of administration?

A
  • Cannot be used to deliver large volumes of fluid

- Cannot be used for drugs that irritate cutaneous tissue

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15
Q

What are the advantages of the intravenous route of administration?

A
  • Bypasses absorption yielding immediate effect

- 100% immediate bioavailability

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16
Q

What are the disadvantages of the intravenous route of administration?

A

Poses more risk for toxicity

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17
Q

What are the advantages of the buccal route of administration?

A
  • Rapidly absorbed

- Avoids 1st pass metabolism

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18
Q

What are the disadvantages of the buccal route of administration?

A
  • Effective only for low doses

- Drugs must be water and lipid soluble

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19
Q

What are the advantages of the transdermal route of administration?

A

Avoids 1st pass metabolism

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20
Q

What are the disadvantages of the transdermal route of administration?

A

Effective only for low doses of drug that

are highly lipid soluble

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21
Q

What are the advantages of the inhalational route of administration?

A

Produce a localised effect

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22
Q

What are the disadvantages of the inhalational route of administration?

A
  • Drug particles must be correct size

- Dependent on patient technique

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23
Q

What are the advantages of the intrathecal route of administration?

A

Local and rapid effects

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24
Q

What are the disadvantages of the intrathecal route of administration?

A
  • Requires expert administration

- May introduce infection/toxicity

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25
Q

What are the advantages of the epidural route of administration?

A

Provides a targeted effect

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26
Q

What are the disadvantages of the epidural route of administration?

A
  • Risk of failure

- Risk of infection

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27
Q

What are the advantages of the topical route of administration?

A

Non-invasive and easy to

administer

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28
Q

What are the disadvantages of the topical route of administration?

A

-Poorly lipid soluble not absorbed via skin
or mucous membranes
-Very slow absorption

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29
Q

What are the advantages of using modified dose forms?

A

✓ Improved patient adherence
✓ Reduction in incidence and severity of GIT effects
✓ Improved control over
therapeutic plasma concentrations
✓ Improved treatment of chronic conditions in which steady plasma concentration required
✓ Maintenance of therapeutic action overnight
✓ Minimise adverse effects
associated with high plasma
concentrations

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30
Q

What are the disadvantages of using modified dose forms?

A

-Cost more per unit dose than conventional forms
-Possibility of unsafe over
dosage if used incorrectly or in failure of MR tablet
-Rate of transit through GIT
limits the maximum period
for which a therapeutic
response can be maintained
-Variability in physiological
factors e.g. GIT pH, enzymes,
food etc influence drug
bioavailability

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31
Q

What can an incorrect route of administration result in?

A

Adverse patient outcomes including death

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32
Q

What is ADME?

A

Absorption
Distribution
Metabolism
Excretion

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33
Q

What is absorption of a drug?

A

Transfer of the drug from the site of administration into

the general or systemic circulation

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34
Q

How much of an orally administered drug is absorbed in 1/3 hours?

A

75%

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35
Q

What are the factors affecting oral absorption?

A
  • Particle size and formulation
  • GIT Enzymes/Acid
  • GIT motility
  • Physicochemical factors
  • Food
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36
Q

What is drug distribution?

A

The process by which the drug is transferred reversibly

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37
Q

How does drug distribution generally occur?

A

Passive diffusion of un-ionised form across the cell membrane.

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38
Q

What is the volume of drug distribution?

A

The size of a compartment which will account for the total amount
of drug in the body based on the amount in the plasma at time zero.

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39
Q

What is the volume of distribution used for?

A
  • To determine the loading dose necessary for a desired blood concentration of a drug.
  • Estimating a blood concentration in the treatment of an overdose
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40
Q

What are the factors affecting drug distribution?

A
  • Plasma protein binding
  • Specific drug receptor sites in tissues
  • Regional blood flow
  • Lipid solubility
  • Disease
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41
Q

What is perfusion?

A

The passage of fluid through the circulatory system or lymphatic system to an organ or a tissue

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42
Q

What are some examples of albumin bound drugs?

A
  • Furosemide
  • Ibuprofen
  • Phenytoin
  • Thiazides
  • Warfarin
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43
Q

What are some examples of glycoprotein bound drugs?

A
  • Chlorpromazine
  • Propranolol
  • Tricyclic antidepressants
  • Lidocaine
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44
Q

When are changes in protein binding significant for drugs?

A

When the drug is more than 90% bound to plasma proteins

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45
Q

When a drug is 20% bound to plasma proteins?

A

Reduction of 5% in bound drug

• Unbound plasma concentration increases from 80% to 85% (negligible)

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46
Q

When a drug is 95% bound to plasma proteins?

A
  • Reduction of 5% in bound drug

* Unbound plasma concentration increases from 5% to 10% (significant)

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47
Q

What are the factors which can increase the fraction rate of unbound drug?

A

-Renal impairment due to rise in blood urea
-Low plasma albumin levels
-Late pregnancy
-Displacement from binding site by other drugs
-Saturability of plasma protein binding within
therapeutic range

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48
Q

How thick is the phospholipid bilayer?

A

About 10nm

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49
Q

What are the four aspects of metabolism?

A
  1. Activation of inactive drug
  2. Production of active drug with increased activity from active drug
  3. Inactivation of active drugs
  4. Change in the nature of the activity
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50
Q

What are the factors which affect drug metabolism?

A
  • First pass effect
  • Hepatic blood flow
  • Liver disease
  • Genetic factors
  • Other drugs
  • Age
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51
Q

What is first pass metabolism?

A

A phenomenon of drug metabolism whereby the concentration of a drug is greatly reduced before it reaches the systemic circulation. Occurs prior to and during absorption.

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52
Q

What are the 4 major metabolic barriers drugs have to pass before they reach general circulation?

A
  • Intestinal lumen
  • Intestinal wall
  • Liver
  • Lung
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53
Q

How does the intestinal lumen act as a metabolic barrier to drugs?

A
  • Digestive enzyme secreted by the mucosal cells and pancreas
  • Certain enzymes break down proteins and stop them from being absorbed
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54
Q

How does the intestinal wall act as a metabolic barrier to drugs?

A

Rich in enzymes that further metabolise drugs

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55
Q

How does the liver act as a metabolic barrier to drugs?

A

Major site of drug metabolism

56
Q

How does the lung act as a metabolic barrier to drugs?

A

Cells of the lung have high affinity for many drugs and are the Lung site of metabolism for many local hormones

57
Q

What are the phases of metabolism?

A
  • Lipophilic drug reacts (oxidation, reduction, hydrolysis).
  • Forms more reactive drug, which then reacts again
  • Forms hydrophilic drug
  • Excreted by kidneys
58
Q

What are isoenzymes?

A

Each of two or more enzymes with identical function but different structure.

59
Q

What are enzyme inducers?

A
  • Enhance production of liver enzymes which breakdown drugs

- Faster rate of drug breakdown

60
Q

What are enzyme inhibitors?

A
  • Inhibit production of enzymes which breakdown drugs

- Reduced rate of drug breakdown

61
Q

What is the metabolism of paracetamol?

A

Paracetamol, conjugation -> paracetamol glucuronide, paracetamol sulphate
Paracetamol, oxidation -> N-acetyl-p-benzoquinoneimine (NAPQI)
NAPQI + glutathione -> cysteine/mercapturate derivatives

62
Q

What is a possible toxic metabolite of paracetamol?

A

N-acetyl-p-benzoquine imine

63
Q

What is bioavailability?

A

The proportion of a dose which actually gets into the systemic circulation

64
Q

What is bioequivalence?

A

It means that two or more chemically or pharmaceutically equivalent products produce comparable
bioavailability characterises

65
Q

What is clearance?

A

The measure of the removal of drug from the body
or the volume of plasma completely emptied of drug per unit time. Clearance does not indicate the amount being removed
but the volume of plasma (or blood) from which the drug
is completely removed or cleared in a given time period.

66
Q

What is drug half life?

A

Time taken for the concentration to reduce by half

67
Q

What is the half-life of a drug increased by?

A
  • Diminished renal plasma flow e.g. heart failure
  • Addition of a second drug that displaces the first from albumin thereby increasing the volume of distribution of the drug
  • Decreased extraction ratio as seen in renal disease
  • Decreased metabolism as seen in liver disease
68
Q

What does drug elimination via the liver depend on?

A
  • blood flow to the liver
  • activity of the enzymes in the liver
  • liver enzymes will alter the drug to form metabolites which are inactive, active or more potent than the drug
69
Q

What are the steps of elimination via the kidney?

A
  1. Filtration
  2. Reabsorption
  3. Secretion
  4. Excretion
70
Q

How is renal function evaluated?

A

Estimation of creatinine clearance, estimates clearance of drugs filtered at the glomerulus.
(Creatinine is produced in skeletal muscle excreted by the kidneys. Neither passively reabsorbed or actively excreted)

71
Q

What is the cockroft gault equation?

A

-Estimated creatinine clearance

Serum Creatinine

72
Q

How is absorption affected in children?

A

Unreliable in neonates and greater transcutaneous absorption

73
Q

How is absorption affected in the elderly?

A

In general unchanged

74
Q

How is distribution affected in children and the elderly?

A

Fat components of body mass tends to be proportionately greater,
acting as a reservoir

75
Q

How is metabolism of drugs affected in children?

A

Reduced capacity due to

immature liver in infants – drug effects prolonged or excessive

76
Q

How is metabolism of drugs affected in the elderly?

A 
Slight reduction due to
impaired liver function, so
drug effects more
pronounced and longer
lasting
77
Q

How is excretion of drugs affected in children?

A

Reduce capacity due to immature kidneys in infants

78
Q

How is excretion of drugs affected in the elderly?

A

Reduction due to impaired

glomerular filtration rate

79
Q

What are the general mechanisms of drug action?

A
  • Action on receptors
  • Action on synapses
  • Enzyme action
  • Inhibit cell transport
80
Q

What is an agonist?

A

Drug that binds to receptors and initiates a cellular
response.
-high affinity and efficacy

81
Q

What are partial agonists?

A

Act on the same receptor but do not produce the same maximal response

82
Q

What are inverse agonists?

A

Acts on the same receptor but produces an opposite effect

83
Q

What is an antagonist?

A

Drug that binds to receptors but does not initiate a cellular response.
-affinity but no efficacy

84
Q

What is a competitive antagonist?

A

Binds to the same site as the agonist but does not activate it

85
Q

What is a non-competitive antagonist?

A

Binds to an allosteric site

to prevent activation of the receptor

86
Q

What is affinity?

A

The degree to which a substance tends to combine with another

87
Q

What is efficacy?

A

The ability to produce a desired or intended result

88
Q

What are receptors?

A

Macromolecules involved in the chemical signalling between and within cells.
Cell activity changes once stimulated.

89
Q

What is potency?

A

Dose of drug needed to produce a biological effect

90
Q

What are the 4 receptor families?

A
  • Ligand-gated ion channels
  • G-protein coupled receptors
  • Enzume-linked receptors
  • Intracellular receptors
91
Q

What are ligand-gated ion channels?

A 
A group of transmembrane
ion channel proteins which
open to allow ions to pass
through the membrane in
response to the binding of
a ligand such as a
neurotransmitter.
92
Q

What are some examples of ligand-gated ion channels?

A
  • Glutamate
  • Serotonin
  • Dopmaine
  • Acetylcholine
93
Q

What are G-protein-coupled receptors?

A

These receptors are linked to their responses by regulatory Guanosine Triphosphate (GTP)-binding proteins or G proteins. This complex induces conformational change in the G-protein.

94
Q

What is the use of second messengers?

A

To allow signals in conduction to be amplifies

95
Q

What are two examples of enzymes that produce second messengers?

A
  • Adenyl cylase (involved in activation of protein kinase)

- Phospholipase C (involved in production of inositol truphosphate (IPS3)and diacyglycerol (DAG))

96
Q

How is gastric acid secretion stimulated?

A
  • Histamine
  • Acetylcholine
  • Gastrin
97
Q

What does the activation of H2 receptors potentiate?

A

Gastrin induced acid secretion

Enhances cAMP

98
Q

What are receptor kinases?

A

-Activate cascades of intracellular signals
-Most are receptor tyrosine-kinases and are activated by
growth factors

99
Q

What are nuclear receptors?

A
  • The receptor is entirely intracellular
  • Ligand must be lipid soluble
  • Primary targets are transcription factors
100
Q

What is the function of acetylcholine?

A

Enables muscle action,

learning and memory

101
Q

What problems are caused by imbalance of acetylcholine?

A

Low levels – Alzheimer’s disease

102
Q

What is the function of noradrenaline?

A

Helps control alertness,

mood. Increases heart rate

103
Q

What problems are caused by imbalance of noradrenaline?

A

Low level – depression

High levels - insomnia

104
Q

What is the function of dopamine?

A

Influences movement,

attention and emotion

105
Q

What problems are caused by imbalance of dopamine?

A

Low levels – Parkinson’s disease

High levels – Schizophrenia

106
Q

What is the function of GABA?

A

Major inhibitory neurotransmitter

107
Q

What problems are caused by imbalance of GABA?

A

Low levels - anxiety

108
Q

What is GABA?

A

Gamma Amino Butyric Acid

109
Q

What is the function of GABA?

A

Affects sleep, mood,

hunger and arousal

110
Q

What problems are caused by imbalance of GABA?

A

Low levels – depression

111
Q

How so SSRIs work?

A

Block the reuptake of serotonin

112
Q

How do TCAs work?

A

Block the reuptake of both serotonin and noradrenaline

113
Q

What is the lock and key concept?

A

Enzyme and substrate bind temporarily to form enzyme-substrate complex

114
Q

What are NSAIDs?

A

Non-Steroidal Anti-Inflammatory Drugs

eg. Ibuprofen, Aspirin

115
Q

What does Cox1 (constitutional) result in?

A

-Cytoprotective prostaglandins
(Protect gastric mucosa, Protect renal perfusion)
-Thromboxanes
(Aid platelet aggregation)

116
Q

What does Cox2 (inducible) result in?

A

-Inflammatory prostaglandins

Recruit inflammatory cells (inflammation, vasodilation), Sensitise skin pain receptors (pain)

117
Q

What are ACE inhibitors?

A

Angiotensin Converting Enzymes

inhibit enzymes

118
Q

What are some examples of Calcium Channel Blockers?

A
  • Amlodipine
  • Diltiazem
  • Verapamil
119
Q

How do calcium channel blockers work?

A

Bind to calcium channels on smooth muscles, blocking the influx of calcium causes smooth muscle relaxation and decreased heart rate

120
Q

What are the 3 classes of CCBs?

A
  • Dihydropyridines
  • Phenylalkylamine
  • Benzothiazepine
121
Q

What are Dihydropyridines selective against?

A

Most smooth muscle selective

122
Q

What are selective Phenylalkylamines against?

A

Selective to myocardium and less effective as

a vasodilator

123
Q

What are selective Benzothiazepines against?

A

Has both cardiac depressant and vasodilator

actions

124
Q

What is the general structure of local anaesthetics?

A

-A lipid-soluble
hydrophobic aromatic group and a charged, hydrophilic
amine group.
-The bond between these two groups determines the class of the drug, and may be amide or ester.

125
Q

What are some examples of amide local anaesthetics?

A
  • Lignocaine
  • Bupivacaine
  • Prilocaine
126
Q

What are some examples of ester local anaesthetics?

A
  • Cocaine

- Amethocaine

127
Q

How are amides as local anaesthetics?

A

Relatively stable and hypersensitivity reactions

are rare

128
Q

How are esters as local anaesthetics?

A

Rapidly hydrolysed and the breakdown product
PABA (para amino benzoic acid) is associated
with allergic and hypersensitive reactions

129
Q

Which is more easily broken: ester linkage or amide bond?

A 
Ester linkage
(meaning ester drugs cannot be stored for as long as amides)
130
Q

How do local anaesthetics work?

A

Disrupt ion channel function within the neurone cell

membrane preventing the transmission of the neuronal action potential.

131
Q

What are adverse effects associated with local anaesthetics?

A

-Block sodium channels in the conduction system of the heart. This can cause
myocardial depression and vasodilatation.
-Affect the CNS. Stimulation
causes restlessness and at high doses, convulsions.
-Addition of adrenaline causes constriction of peripheral
blood vessels, lessening the distribution, prolonging
action and producing a relatively bloodless field.

132
Q

How are esters (except cocaine) broken down?

A

Rapidly by plasma
esterases to inactive compounds and consequently have a
short half life.

133
Q

How are amides broken down?

A

Metabolised hepatically by amidases. This is a

slower process, hence their half-life is longer and they can accumulate if given in repeated doses or by infusion.

134
Q

How is prilocaine metabolised?

A

Extra-hepatically

135
Q

What is the ceiling in drug concentration?

A

Lowest dose that

produces maximal effect

136
Q

What is the threshold in drug concentration?

A

Dose that produces a

just-noticeable effect

137
Q

What is the ED50 in drug concentration?

A

Dose that produces

50% of maximum response

IMS (13 decks)

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