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Phase 2a Medicine - Riona > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Give 3 protein targets for drug action

A
  • ) Receptors
  • ) Ion channels
  • ) Enzymes
  • ) Transporters
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2
Q

What are ion channels?

A

Gateways in cell membranes that selectively allow ion passage

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3
Q

What are ligand gated ion channels?

A

Channels that open when an agonist molecule binds

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4
Q

What are voltage gated ion channels?

A

Open when transmembrane potential changes

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5
Q

How can drugs affect ion channel function?

A

By binding to the orthosteric (primary) site and blocking the allosteric (non-primary) site, and changing the configuration for that the ligand cannot bind

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6
Q

What are 2 types of inhibitors?

A

Competitive and non-competitive

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7
Q

What are G protein coupled receptors?

A

Receptors coupled to intracellular effector systems by G proteins

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8
Q

Give an example of a G protein coupled receptor (GPCR)

A

Beta adrenoreceptors

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9
Q

What are G proteins?

A

Membrane proteins which function to recognise activated GPCRs and pass on the message to intracellular effectors

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10
Q

Give an example of an intracellular effector

A

CAMP

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11
Q

What do kinase linked and related receptors mainly respond to?

A

Protein mediators

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12
Q

Give an example of a kinase linked receptor

A

Growth factor receptor

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13
Q

What do nuclear receptors do?

A

Regulate gene transcription and recognise foreign molecules

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14
Q

Give an example of a nuclear receptor

A

Steroid receptor

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15
Q

What is an agonist?

A

Binds to receptor and activates it

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16
Q

What is an antagonist?

A

Binds to receptor and reduces its effect by reversing its action

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17
Q

What is Emax?

A

Describes the maximum response for a given agonist - full agonists give maximal responses

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18
Q

What is affinity?

A

How well a ligand binds to a receptor - agonists and antagonists

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19
Q

What is efficacy?

A

How well a ligand activates a receptor - agonists only

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20
Q

What is potency?

A

How much of a drug needs to be given, binding affinity

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21
Q

What is the equation for intrinsic activity?

A

Emax of partial agonist/ Emax of full agonist

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22
Q

What is EC50?

A

The concentration of a drug that gives half of the maximal response

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23
Q

How can we find out the EC50?

A

From a potency (sigmoidal shaped) curve

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24
Q

What 2 things can we compare drugs by?

A

Potency (how much is needed for it to work)

Efficacy (maximal response)

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25
Q

What are the 2 main types of cholinergic receptors?

A

Nicotinic and muscarinic

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26
Q

Where are the 4 types of histamine receptors found?

A

H1 - allergic conditions
H2 - gastric acid secretion
H3 - mostly in CNS disorders
H4 - immune system and inflammatory conditions

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27
Q

Is histamine an agonist or antagonist?

A

Agonist

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28
Q

What does histamine do?

A

Causes contraction of the ileum and acid secretion from parietal cells (H2)

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29
Q

What causes reversed contraction of the ileum?

A

Mepyramine, antagonist

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30
Q

What is allosteric modulation?

A

A second ligand has the capacity to modify the response whilst not being in the agonist site

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31
Q

What is the difference between an antagonist and an inverse agonist?

A

Antagonist usually just neutralises the effects of an agonist, whereas an inverse agonist has the capacity to repress the response to the receptor - do the opposite

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32
Q

What is an enzyme inhibitor?

A

A molecule that binds to an enzyme and (normally) decreases its activity

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33
Q

How does an enzyme inhibitor work?

A

By preventing the substate from entering the enzyme’s active site and thus preventing it from catalysing its reaction

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34
Q

What are the 2 main type of enzyme inhibitors?

A

Irreversible and reversible

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35
Q

How do irreversible inhibitors usually work?

A

Bind via a covalent bond and change enzyme chemically

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36
Q

What ways can an inhibitor bind to the enzyme?

A

Enzyme or enzyme-substrate complex

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37
Q

How do statins work?

A

By blocking the rate limiting step in the cholesterol pathway

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38
Q

How does aspirin work?

A

Irreversible inactivation of cyclooxygenase (COX)

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39
Q

How does ibuprofen work?

A

Completely inhibiting arachidonic acid at the active site of COX

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40
Q

How does penicillin work?

A

Inhibits transpeptidases, preventing cross linking and inhibiting bacterial wall synthesis

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41
Q

How do PPIs work?

A

Inhibit gastric acid secretion from parietal cells by irreversibly inactivating proton pumps

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42
Q

How do (some) diuretics work?

A

Inhibit symporters in areas of the kidney nephron so that there is a reduced reabsorption of salt from the filtrate

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43
Q

What does xenobiotic mean?

A

Compounds foreign to an organism’s normal biochemistry

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44
Q

What are the 3 main types of protein port?

A
  • ) Uniporter
  • ) Symporter
  • ) Antipoter
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45
Q

How do uniporters work?

A

Uses energy from ATP

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46
Q

How do symporters work?

A

Use movement of one molecule to pull another molecular in against its concentration gradient

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47
Q

How do antiporters work?

A

One substance moves against its gradient using energy from the second substance moving down its gradient

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48
Q

What are the 4 phases of pharmacokinetics?

A
  • ) Absorption
  • ) Distribution
  • ) Metabolism
  • ) Elimination
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49
Q

What is absorption?

A

The process of transferring the drug from the site of administration into the general or systemic circulation

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50
Q

Give 3 methods of administration of a drug

A
  • ) Oral
  • ) IV
  • ) Intra-arterial
  • ) IM
  • ) SC
  • ) Inhaled
  • ) Topical
  • ) Sublingual
  • ) Rectal
  • ) Intrathecal
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51
Q

Give 3 ways in which drugs move around the body

A
  • ) Blood
  • ) Lymphatics
  • ) CSF
  • ) Diffusion
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52
Q

Give 3 methods of transport for molecules

A
  • ) Simple diffusion
  • ) Facilitated diffusion
  • ) Active transport
  • ) Through extracellular spaces
  • ) Via aquaporins
  • ) Pinocytosis
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53
Q

What sort of pH is aspirin?

A

Weak acid

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54
Q

What sort of pH is propranolol?

A

Weak base

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55
Q

How do drugs with ionisable groups exist?

A

In equilibrium between charged (ionised) and uncharged forms

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56
Q

What are the most water soluble types of drugs?

A

Ionised

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57
Q

Define pKa of a drug

A

Dissociation or ionisation constant

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58
Q

What does pKa of a drug mean?

A

The pH at which half of the substance is ionised and half is unionised

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59
Q

Where are weak acids best absorbed?

A

Stomach

60
Q

Where are weak bases best absorbed?

A

Intestine

61
Q

What does bioavailability mean?

A

The amount of drug taken up as a proportion of the amount administered

62
Q

What do drugs commonly bind to?

A

Albumin (plasma protein)

63
Q

What does binding of a drug to protein cause?

A

Lowers the free concentration of the drug, and can act as a source by releasing the drug

64
Q

What is irreversible binding of a drug to a protein equivalent to?

A

Elimination

65
Q

What is the volume of distribution? (Vd)

A

The volume the drug would occupy if it was distributed through all of the components

66
Q

What does a higher Vd mean?

A

The drug is more lipid soluble

67
Q

What Vd will a drug have if it has a low plasma concentration?

A

High Vd

68
Q

Where fo lipophilic drugs adhere to?

A

Hydrophobic areas of plasma proteins

69
Q

How do we calculate Vd?

A

The total amount of drug in the body (dose)/ plasma concentration

70
Q

What is the Vd if we give 50mg of a drug and find that the plasma concentration is 1mg/L?

A

50L

50mg/1mg/L = 50L

71
Q

What is metabolism?

A

Transformation of the drug molecule into a different molecule

72
Q

What do high hepatic/renal extraction ratio drugs have?

A

A high first pass metabolism

73
Q

What does a high first pass metabolism also mean?

A

The bioavailability is limited

74
Q

What is phase I metabolism?

A

Hepatic metabolism

75
Q

What does phase I hepatic metabolism include?

A

Non-specific reactions that remove functional groups of side chains and add -OH or =O to make the molecule soluble

76
Q

What catalyses phase I hepatic metabolism?

A

Cytochrome P450 catalyses oxidative hydroxylation

77
Q

What does enterohepatic circulation do?

A

Prolongs some drug actions by liberating phase I metabolites to rediffuse into the blood

78
Q

What is phase II metabolism?

A

Coagulation reactions

79
Q

What does phase II coagulation reactions metabolism include?

A

Conjugating drugs with an OH group and glucuronic acid to make a glucuronide

80
Q

How is a glucuronide made in a phase II reaction?

A

Formation of a covalent bond between the drug/phase I metabolite and an endogenous substance

81
Q

Give 2 examples of endogenous substances

A
  • ) Glucuronic acid
  • ) Sulfate
  • ) Acetyl group
  • ) Methyl group
82
Q

What are the resulting products of phase II reactions like?

A

Less active and readily excreted by kidneys

83
Q

What is clearance?

A

Removal of the drug from the plasma by the liver or kidneys

84
Q

How do we calculate clearance?

A

The volume of plasma that can be completely cleared of drug per unit time

85
Q

What can reduce clearance?

A

Kidney or liver damage

86
Q

What is the clearance if 10% od a drug carrier to the liver is cleared at a flow rate of 1000ml/min?

A

100ml/min

87
Q

Give 3 states of matter and an example of a different form of excretion for each

A

Liquid - urine, bile, sweat, tears, breast milk
Solid - faeces, hair
Gas - expired air

88
Q

How can we measure the fall in plasma concentration of a drug with time?

A

Taking repeat plasma samples

89
Q

What is first order kinetics?

A

A constant fraction of the drug is eliminated per unit of time, exponential decline in plasma concentration of drug

90
Q

What is zero order kinetics?

A

Rate of removal of drug is constant decline, unaffected by increase in concentration, enzyme system that removes drug is saturated

91
Q

What order of kinetics does ethanol follow once alcohol dehydrogenase has been saturated?

A

Zero order

92
Q

What does the graph look like for first order kinetics?

A

Exponential decline

93
Q

What does the graph look like for zero order kinetics?

A

Constant gradient decline

94
Q

What is half life?

A

The time taken for a concentration of a drug to reduce by a half

95
Q

How do we calculate bioavailability?

A

As the fraction of the administered drug that reaches the systemic circulation unaltered (F)

96
Q

What is the bioavailability of IV drugs?

A

F=1

97
Q

What is the bioavailability of oral drugs?

A

F<1

98
Q

How much larger will the dose need to be for a drug with an oral bioavailability of 0.1 compared to its IV dose?

A

10x

99
Q

How do we measure the bioavailability on a graph?

A

Measure the areas under the curve (AUC)

100
Q

How do we compare IV and oral plasma concentrations?

A

AUC oral/ AUC IV

101
Q

What is the rate of elimination inversely proportional to?

A

Vd

102
Q

What is the rate constant factor of elimination?

A

K

103
Q

What is the equation relating clearance, elimination and volume of distribution?

A

K = CL/Vd

104
Q

What is the calculation for clearance of an IV drug?

A

CL = dose/AUC

105
Q

What is the calculation for clearance of an oral drug with F<1?

A

CL = dose x F/AUC

106
Q

What is Css?

A

Steady state, balance between drug input and elimination

107
Q

How do we get to Css?

A

Repeat drug administration

108
Q

Give 2 things that will delay Css

A
  • ) Slow elimination of drug

- ) High Vd

109
Q

What is the calculation for when the rate of elimination equals the rate of infusion? (In IV infusions)

A

CL x Css

110
Q

What is the equation for Css for oral administration?

A

D x F/t = CL x Css

t is the time interval between doses

111
Q

Give 2 ways in which we can alter the plasma Css

A
  • ) Change dose

- ) Change interval

112
Q

What is the equation for the loading dose?

A

Css x Vd

113
Q

What is the loading dose?

A

A high initial dose which shortens the time to a steady state

114
Q

Define synergy

A

2 drugs working towards the same effect

115
Q

What does inhibition mean in the term of drug interactions?

A

Drug A blocks the metabolism of drug B thus leaving more free drug B in the plasma to have more of an effect

116
Q

What does induction mean in the term of drug interactions?

A

Drug C induces an enzyme, leading to increased drug D metabolism so there is less of an effect

117
Q

What does a narrow therapeutic index mean?

A

There is a small range between the drug not working and it being toxic

118
Q

Define adverse event

A

Any unintended outcome

119
Q

Define adverse drug reaction (ADR)

A

Unwanted or harmful reaction following administration of a drug/combination of drugs under normal conditions of use, and is suspected to be related to the drug

120
Q

What are the 5 classes of ADRs?

A 
Type A - augmented pharmacological
Type B - bizarre or idiosyncratic
Type C - chronic
Type D - delayed
Type E - end of treatment
121
Q

Describe a type A ADR

A

Predictable, dose dependent, common (constipation and morphine)

122
Q

Describe a type B ADR

A

Consider hypersensitivity types, not predictable, not dose dependent (anaphylaxis and penicillin)

123
Q

Give an example of a type C ADR

A

Osteoporosis and steroids

124
Q

Give an example of a type D ADR

A

Malignancies after immunosuppression

125
Q

Describe a type E ADR

A

Occurs after abrupt drug withdrawal

126
Q

Give 3 causes for an ADR

A
  • ) Pharmaceutical variation
  • ) Receptor abnormality
  • ) Abnormal biological system unmasked by drug
  • ) Abnormalities in drug metabolism
  • ) Immunological
  • ) Drug-drug interactions
  • ) Multifactorial
127
Q

Give 2 instances when we should suspect an ADR

A
  • ) Symptoms after starting a new drug
  • ) Symptoms after increased dose
  • ) Symptoms disappearing/reappearing when drug stopped/restarted
128
Q

What is the scheme for reporting ADRs?

A

Yellow card scheme

129
Q

What is substance use?

A

The ingestion of a substance that affects the CNS which then leads to behavioural and psychological changes

130
Q

What does dependence refer to?

A

The effects of withdrawal (cravings, euphoria)

131
Q

What does addiction refer to?

A

Physical and psychological dependence

132
Q

What does tolerance mean?

A

The body needs more of the drug for the same effect

133
Q

Give 3 factors that influence drug response

A
  • ) Food
  • ) Alcohol
  • ) Smoking
  • ) Complementary medicines
  • ) Medial herbalism
  • ) OTC medicines
134
Q

What is homeopathy?

A

Using small doses of natural substances that would produce symptoms of the illness in large amounts

135
Q

What is the placebo effect?

A

Beneficial effect produced by positive expectation of homeopathic therapy, not by the therapy itself

136
Q

What is allopathy?

A

The treatment leads to opposite effects of the symptoms (coughing to no coughing)

137
Q

Which opioid does not have the desired effect in everyone?

A

Codeine

138
Q

How do opioids work? (3)

A
  • ) Inhibit release of pain transmitters at the spinal cord and midbrain
  • ) Modulate pain perception in higher centres
  • ) Change emotional perception of pain
139
Q

What drug to we give to reverse an opioid overdose?

A

Naloxone

140
Q

What is a pro-drug?

A

A drug that doesn’t work until it is metabolised

141
Q

Give an example of a pro-drug

A

Codeine

142
Q

What do the names of corticosteroids usually end in?

A

Sone

Dexamethasone

143
Q

What do the names of monoclonal antibodies usually end in?

A

Mab

Reslizumab

144
Q

What do the names of bronchodilators usually end in?

A

Terol

Salmeterol

145
Q

What do the names of kinase inhibitors usually end in?

A

Nib

Nintendanib

Phase 2a Medicine - Riona (17 decks)

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