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E-lfh FRCA Primary: Pharmacology - Pharmacodynamics > Primary FRCA Course Paper 10 Pharmacodynamics > Flashcards

Primary FRCA Course Paper 10 Pharmacodynamics Flashcards

1
Q

Partial agonists

Can never produce a maximal response at a receptor

A

True. By definition, they mediate a response which is less than maximal

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2
Q

Partial agonists

Cause a parallel shift in the semilogarithmic dose response curve

A

False. They shift the curve down and to the right

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3
Q

Partial agonists

Bind irreversibly to receptor sites

A

False. They bind reversibly

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4
Q

Partial agonists

Generally have a lower affinity for the receptor than the agonist

A

True. It can have the same affinity as the agonist, though in general it is lower

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5
Q

Partial agonists

If a partial agonist has the same affinity for a receptor as the agonist, it’s equilibrium constant will be the same

A

True

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6
Q

The following are examples of hepatic enzyme inducers

Ranitidine

A

False. Hepatic microsomal enzyme inducers inc: Rifampicin, Chronic alcohol abuse, Enflurane, Halothane, Phenobarbitol, Thiopental, Phenytoin, Cabemazepine, Glucocorticoids, Cigarette smoking

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7
Q

The following are examples of hepatic enzyme inducers

Erythromycin

A

False. Hepatic microsomal enzyme inducers inc: Rifampicin, Chronic alcohol abuse, Enflurane, Halothane, Phenobarbitol, Thiopental, Phenytoin, Carbamazepine, Glucocorticoids, Cigarette smoking

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8
Q

The following are examples of hepatic enzyme inducers

Phenytoin

A

True. Hepatic microsomal enzyme inducers inc: Rifampicin, Chronic alcohol abuse, Enflurane, Halothane, Phenobarbitol, Thiopental, Phenytoin, Cabemazepine, Glucocorticoids, Cigarette smoking

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9
Q

The following are examples of hepatic enzyme inducers

Amiodarone

A

False. Hepatic microsomal enzyme inducers inc: Rifampicin, Chronic alcohol abuse, Enflurane, Halothane, Phenobarbitol, Thiopental, Phenytoin, Cabemazepine, Glucocorticoids, Cigarette smoking

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10
Q

The following are examples of hepatic enzyme inducers

Cigarette smoking

A

True. Hepatic microsomal enzyme inducers inc: Rifampicin, Chronic alcohol abuse, Enflurane, Halothane, Phenobarbitol, Thiopental, Phenytoin, Cabemazepine, Glucocorticoids, Cigarette smoking

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11
Q

The following are examples of hepatic enzyme inhibitors

Amiodarone

A

True. Hepatic microsomal enzyme inhibitors inc: Metroniadazole, Isoniazid, Chloramphenical, Phenelzine, Tranylcypromine, Cimetidine and Grapefruit Juice

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12
Q

The following are examples of hepatic enzyme inhibitors

Carbamazepine

A

False. Hepatic microsomal enzyme inhibitors inc: Metroniadazole, Isoniazid, Chloramphenical, Phenelzine, Tranylcypromine, Cimetidine and Grapefruit Juice

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13
Q

The following are examples of hepatic enzyme inhibitors

Metronidazole

A

True. Hepatic microsomal enzyme inhibitors inc: Metronidazole, Isoniazid, Chloramphenical, Phenelzine, Tranylcypromine, Cimetidine and Grapefruit Juice

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14
Q

The following are examples of hepatic enzyme inhibitors

Fludrocortisone

A

False. Hepatic microsomal enzyme inhibitors inc: Metroniadazole, Isoniazid, Chloramphenical, Phenelzine, Tranylcypromine, Cimetidine and Grapefruit Juice

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15
Q

The following are examples of hepatic enzyme inhibitors

Ceftriaxone

A

False. Hepatic microsomal enzyme inhibitors inc: Metroniadazole, Isoniazid, Chloramphenical, Phenelzine, Tranylcypromine, Cimetidine and Grapefruit Juice

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16
Q

Concerning drug dose and response

A plot of % response against drug concentration gives a sigmoid shape

A

False. Dose response curves are normally plotted as % response against LOG drug concentration. The resultant graph is sigmoid shaped

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17
Q

Concerning drug dose and response

Antagonists must have a higher receptor affinity than agonists

A

False. A drug with high affinity and high intrinsic activity is an agonist. A drug with high affinity but no intrinsic activity will act as an antagonist, however displacement of an agonist also depends on the relative concentrations of the two drugs at the receptor sites

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18
Q

Concerning drug dose and response

Intrinsic activity determines maximal response

A

True.

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19
Q

Concerning drug dose and response

Maximal response occurs only when all receptor sites are occupied

A

False. A maximal response may be achieved by activation of a small proportion of receptor sites (eg the NMJ)

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20
Q

Concerning drug dose and response

Partial agonism implies low receptor affinity

A

False. Partial agonism may be displayed by a drug with low intrinsic activity, but it may well have high receptor affinity making it difficult to antagonize

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21
Q

The efficacy (or intrinsic activity)of a drug

Is greater for drug A if A is effective in a dose of 100 micrograms than for drug B if B is effective in a dose of 100 milligrams

A

False. The dose of a drug required to produce a given effect decribes its potency, not its efficacy. In the example described, drug A is more potent than drug B

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22
Q

The efficacy (or intrinsic activity)of a drug

Is a measure of its therapeutic index

A

False. The therapeutic index of a drug is a measure of its safety (ED50/LD50)

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23
Q

The efficacy (or intrinsic activity)of a drug

Is a measure of the amount of a drug required to produce a given effect

A

False. This describes potency. Efficacy is a measure of the maximal effect of an agonist.

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24
Q

The efficacy (or intrinsic activity)of a drug

Describes the ability of a drug to produce its therapeutic effect

A

True

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25
Q

The efficacy (or intrinsic activity)of a drug

Is a measure of the bioavailability of a drug

A

False.

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26
Q

Genetic polymorphisms of drug metabolism

Exhibit inter-ethnic differences

A

True. Some drugs are metabolised by enzymes susceptible to polymorphisms which affect their activity. This is the basis of fast and slow acetylation (e.g. hydralazine) and slow and poor metabolism (e.g. debrisoquine). The prevalence of these polymorphisms shows considerable variation between racial groups

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27
Q

Genetic polymorphisms of drug metabolism

Are not associated with adverse effects

A

False. The consequences of poor metabolism of a particular drug are clearly dependent on its pharmacological actions: drugs with a steep dose-response curve or a low therapeutic index may well produce toxic effects in poor metabolisers

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28
Q

Genetic polymorphisms of drug metabolism

Are dependent on the pharmacological actions of the drug

A

False.

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29
Q

Genetic polymorphisms of drug metabolism

Are due to altered gene expression

A

True. Genetic polymorphisms are determined by abnormalities of gene expression and are not dependent on the pharmacological actions of the drug

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30
Q

Genetic polymorphisms of drug metabolism

Are not clinically important for drugs that are eliminated by the kidney

A

True.

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31
Q

Metabolism of the following drugs are affected by the acetylator status of the individual

Digoxin

A

False.

Rapid acetylator status occurs in approximately 40% of the UK population and is inherited in an autosomal dominant pattern. Slow acetylator status occurs in approximately 60% of the UK population and is inherited in an autosomal recessive pattern. Metabolism of the following drugs are affected by the acetylator status of the individual, Hydralazine, Isoniazid, Sulphonamides, Phenelzine, Dapsone, Procainamide.

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32
Q

Metabolism of the following drugs are affected by the acetylator status of the individual

Hydralazine

A

True.

Rapid acetylator status occurs in approximately 40% of the UK population and is inherited in an autosomal dominant pattern. Slow acetylator status occurs in approximately 60% of the UK population and is inherited in an autosomal recessive pattern. Metabolism of the following drugs are affected by the acetylator status of the individual, Hydralazine, Isoniazid, Sulphonamides, Phenelzine, Dapsone, Procainamide.

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33
Q

Metabolism of the following drugs are affected by the acetylator status of the individual

Isoniazid

A

True.

Rapid acetylator status occurs in approximately 40% of the UK population and is inherited in an autosomal dominant pattern. Slow acetylator status occurs in approximately 60% of the UK population and is inherited in an autosomal recessive pattern. Metabolism of the following drugs are affected by the acetylator status of the individual, Hydralazine, Isoniazid, Sulphonamides, Phenelzine, Dapsone, Procainamide.

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34
Q

Metabolism of the following drugs are affected by the acetylator status of the individual

Propranolol

A

False.

Rapid acetylator status occurs in approximately 40% of the UK population and is inherited in an autosomal dominant pattern. Slow acetylator status occurs in approximately 60% of the UK population and is inherited in an autosomal recessive pattern. Metabolism of the following drugs are affected by the acetylator status of the individual, Hydralazine, Isoniazid, Sulphonamides, Phenelzine, Dapsone, Procainamide.

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35
Q

Metabolism of the following drugs are affected by the acetylator status of the individual

Amiodarone

A

False.

Rapid acetylator status occurs in approximately 40% of the UK population and is inherited in an autosomal dominant pattern. Slow acetylator status occurs in approximately 60% of the UK population and is inherited in an autosomal recessive pattern. Metabolism of the following drugs are affected by the acetylator status of the individual, Hydralazine, Isoniazid, Sulphonamides, Phenelzine, Dapsone, Procainamide.

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36
Q

Regarding log dose-response curves

Potency is the ability of a drug to produce maximal response

A

False. Potency is the dose (mg/kg) required to produce a given effect. Morphine and fentanyl have similar efficacy, but fentanyl is approximately 100 times more potent than morphine (10 mg of morphine is equivalent to 0.1 mg of fentanyl). Efficacy or intrinsic activity is the ability of a drug to produce maximal response.

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37
Q

Regarding log dose-response curves

A partial agonist binds to the receptor with a lower affinity than an agonist

A

False. Agonists are drugs that produce the maximal response. Partial agonists cannot produce a maximal response, though they may bind to the receptor with the same affinity as full agonists

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38
Q

Regarding log dose-response curves

In the presence of a competitive antagonist the log dose-response curve for an agonist shows a parallel shift to the right

A

True. In the presence of a competitive antagonist the log dose-response curve shows a parallel shift to the right so that a higher concentration of agonist is required to achieve the same response

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39
Q

Regarding log dose-response curves

In the presence of a non-competitive antagonist, the log dose-response curve for an agonist is shifted to the left

A

False. In the presence of a non-competitive antagonist the log dose-response curve is shifted to the right and the maximal response is reduced

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40
Q

Regarding log dose-response curves

A partial agonist can act as a competitive antagonist to a full agonist

A

True. A partial agonist, by binding to receptors but failing to produce a maximal response, can act as a competitive antagonist to a full agonist

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41
Q

The following interactions are antagonistic

Naloxone and dextropropoxyphe

A

True.

Antagonistic interactions may be classified into the following four categories: Competitive: The drugs bind reversibly and interaction is overcome by increasing the concentration of the agonist. Irreversible (non-competitive): The drugs bind irreversibly (usually covalent bonding) and this cannot be overcome by increasing the concentration of the agonist. Physiological: The interaction of two drugs whose opposing actions tend to cancel each other. e.g. noradrenaline increasing blood pressure and histamine decreasing blood pressure Chemical: Direct interaction of two drugs which either removes or prevents the drug from reaching the target. e.g. chelation of lead by penicillamine.u

42
Q

The following interactions are antagonistic

Acetylcysteine and paracetamol

A

False.

Antagonistic interactions may be classified into the following four categories: Competitive: The drugs bind reversibly and interaction is overcome by increasing the concentration of the agonist. Irreversible (non-competitive): The drugs bind irreversibly (usually covalent bonding) and this cannot be overcome by increasing the concentration of the agonist. Physiological: The interaction of two drugs whose opposing actions tend to cancel each other. e.g. noradrenaline increasing blood pressure and histamine decreasing blood pressure Chemical: Direct interaction of two drugs which either removes or prevents the drug from reaching the target. e.g. chelation of lead by penicillamine

43
Q

The following interactions are antagonistic

Atenolol and salbutamol

A

True.

Antagonistic interactions may be classified into the following four categories: Competitive: The drugs bind reversibly and interaction is overcome by increasing the concentration of the agonist. Irreversible (non-competitive): The drugs bind irreversibly (usually covalent bonding) and this cannot be overcome by increasing the concentration of the agonist. Physiological: The interaction of two drugs whose opposing actions tend to cancel each other. e.g. noradrenaline increasing blood pressure and histamine decreasing blood pressure Chemical: Direct interaction of two drugs which either removes or prevents the drug from reaching the target. e.g. chelation of lead by penicillamine

44
Q

The following interactions are antagonistic

Protamine and warfarin

A

False. Protamine is used to counteract the effect of heparin.

Antagonistic interactions may be classified into the following four categories: Competitive: The drugs bind reversibly and interaction is overcome by increasing the concentration of the agonist. Irreversible (non-competitive): The drugs bind irreversibly (usually covalent bonding) and this cannot be overcome by increasing the concentration of the agonist. Physiological: The interaction of two drugs whose opposing actions tend to cancel each other. e.g. noradrenaline increasing blood pressure and histamine decreasing blood pressure Chemical: Direct interaction of two drugs which either removes or prevents the drug from reaching the target. e.g. chelation of lead by penicillamine

45
Q

The following interactions are antagonistic

Tranexamic acid and streptokinase

A

True.

Antagonistic interactions may be classified into the following four categories: Competitive: The drugs bind reversibly and interaction is overcome by increasing the concentration of the agonist. Irreversible (non-competitive): The drugs bind irreversibly (usually covalent bonding) and this cannot be overcome by increasing the concentration of the agonist. Physiological: The interaction of two drugs whose opposing actions tend to cancel each other. e.g. noradrenaline increasing blood pressure and histamine decreasing blood pressure Chemical: Direct interaction of two drugs which either removes or prevents the drug from reaching the target. e.g. chelation of lead by penicillamine

46
Q

Non-competitive antagonists

Move the log dose-response curve for a drug to the right in a non-parallel manner

A

True.

47
Q

Non-competitive antagonists

Reduce the gradient of the log dose-response curve

A

True. Non-competitive antagonists reduce both the slope and the peak of the agonist log dose-response curve and can cause some degree of rightwards shift (non-parallel).

48
Q

Non-competitive antagonists

Have an effect unrelated to the agonist plasma concentration

A

False. Increasing the agonist dose will increase the response, however the maximum response will never be achieved in the presence of a non-competetive antagonist

49
Q

Non-competitive antagonists

Prevent a maximum agonist response

A

True.

50
Q

Non-competitive antagonists

Display surmountability

A

False. They are non-surmountable as no matter how high an agonist concentration exists, the peak response will not be reached

51
Q

The following drugs act via enzyme inhibition

Allopurinol

A

True. Allopurinol inhibits xanthine oxidase

52
Q

The following drugs act via enzyme inhibition

Physostigmine

A

True. Physostigmine is a naturally occurring anticholinesterase drug

53
Q

The following drugs act via enzyme inhibition

Indomethacin

A

True. Indomethacin reduces prostaglandin production by inhibiting cyclo-oxygenase

54
Q

The following drugs act via enzyme inhibition

Meptazinol

A

False. Meptazinol is an opioid agonist.

55
Q

The following drugs act via enzyme inhibition

Enoximone

A

True. Enoxomone is a selective phosphodiesterase inhibitor.

56
Q

An hereditary enzyme abnormality may lead to altered metabolism of

Propofol

A

False.

57
Q

An hereditary enzyme abnormality may lead to altered metabolism of

Isoniazid

A

True. Acetylation of drugs in the liver (e.g. isoniazid and hydralazine) within a population shows a bimodal distribution of plasma drug concentration following a fixed dose of that drug (fast acetylators and slow acetylators).

58
Q

An hereditary enzyme abnormality may lead to altered metabolism of

Thiopentone

A

False.

59
Q

An hereditary enzyme abnormality may lead to altered metabolism of

Suxamethonium

A

True. The activity of plasma cholinesterase is affected by genetric variation which can lead to an increase in the duration of action of suxamethonium

60
Q

An hereditary enzyme abnormality may lead to altered metabolism of

Atracurium

A

False.

61
Q

Competitive antagonists

Shift the log dose-response curve right

A

True. i.e. a higher agonist dose will be required for the same effect

62
Q

Competitive antagonists

Can bind to a different recepetor site than the agonist

A

False. This is true of non-competitive antagonists

63
Q

Competitive antagonists

At the neuromuscular junction, weak antagonists tend to have a faster onset

A

True. In general this is true, as they are given in higher dose so initially there are more molecules to occupy the receptors.

64
Q

Competitive antagonists

Shift the log dose-response curve down

A

False. The same maximal response will be possible, just at higher doses. It is shifted down by a non-competitive antagonist.

65
Q

Competitive antagonists

Are compared with one another by the degree of reduction in maximal response

A

False. They do not reduce maximal response. They are compared using the Dose Ratio of 2, which indicates the degree of right shift of the log dose-response curve

66
Q

Regarding partial agonists

If an agonist has an Intrinsic Activity of < 1, it is termed a partial agonist

A

True. Meaning it’s maximal response/effect is less than that of a full agonist.

67
Q

Regarding partial agonists

If given in very large doses partial agonists may achieve a full response

A

False. By definition, they cannot achieve a full response

68
Q

Regarding partial agonists

If given in combination with a full agonist, they can act as an antagonist

A

True.

69
Q

Regarding partial agonists

If given in combination with a full agonist, they can act as an agonist

A

True. If the full agonist is given at a low dose, the partial agonists effects are additive. As the full agonist dose increases, the partial agonist begins to act as a competitive antagonist

70
Q

Regarding partial agonists

If given alone, partial agonists can act as agonists or antagonists

A

False. Alone they act as agonists, with a reduced maximal response. When given with a full agonist can act as agonists or antagonists

71
Q

Regarding drug-receptor interactions

Affinity, refers to how well a drug binds to it’s receptor

A

True.

72
Q

Regarding drug-receptor interactions

Intrinsic activity refers to the magnitude of effect once a drug has bound to a receptor

A

True. Sometimes referred to as efficacy. It has a value of 0 - 1

73
Q

Regarding drug-receptor interactions

A drug with high affinity will produce a large response

A

False. A drug may have high affinity with low or no activity, ie be a partial agonist or an antagonist

74
Q

Regarding drug-receptor interactions

Partial agonists have a low receptor affinity

A

False.

75
Q

Regarding drug-receptor interactions

Antagonists will have a high receptor affinity

A

True. But with no intrinsic activity

76
Q

A drug that is 98% protein bound

Will double its free drug concentration if protein binding is decreased to 96%

A

True. If a drug is 50% protein bound, and this is decreased to 48%, the free drug concentration will increase by 4%. On the other hand, if the drug is 98% bound and this decreases to 96%, the free drug concentration doubles from 2% to 4% of total.

Drugs which are extensively bound and which are poorly extracted by the liver will display an increased clinical effect if displaced as free drug

77
Q

A drug that is 98% protein bound

Will show a 2% increase in free drug concentration if protein binding falls 2%

A

False. This is a 100% not 2% increase in free drug concentration

Drugs which are extensively bound and which are poorly extracted by the liver will display an increased clinical effect if displaced as free drug

78
Q

A drug that is 98% protein bound

Must have a pKa > 7.4

A

False. Drug pKa is in this case irrelevant

79
Q

A drug that is 98% protein bound

Might be diazepam

A

True

80
Q

A drug that is 98% protein bound

Might be midazolam

A

True

81
Q

The following are examples of pharmacokinetic drug interactions

Lithium and thiazide diuretics

A

True. Increased lithium levels are produced owing to an increase in lithium reabsorbtion

82
Q

The following are examples of pharmacokinetic drug interactions

Digoxin and amiodarone

A

True. Amiodarone reduces the renal clearance of digoxin

83
Q

The following are examples of pharmacokinetic drug interactions

Phenytoin and cimetidine

A

True. Cimetidine inhibits cyt P450 leading to phenytoin toxicity

84
Q

The following are examples of pharmacokinetic drug interactions

Beta blockers and verapamil

A

False. The interaction between beta blockers and verapamil is pharmacodynamic.

85
Q

The following are examples of pharmacokinetic drug interactions

Ethanol and diazepam

A

False. The interaction between ethanol and diazepam is pharmacodynamic.

86
Q

The following drugs exhibit tachyphylaxis

Glyceryl trinitrate

A

True.

87
Q

The following drugs exhibit tachyphylaxis

Ephedrine

A

True.

88
Q

The following drugs exhibit tachyphylaxis

Succinylcholine

A

False.

89
Q

The following drugs exhibit tachyphylaxis

Trimetaphan

A

True.

90
Q

The following drugs exhibit tachyphylaxis

Hydralazine

A

False.

91
Q

The rate of diffusion of a drug across a membrane is dependent upon

The drug concentration gradient across the membrane

A

True. Drug diffusion only occurs if a concentration gradient exists. It proceeds until the concentrations are equal

92
Q

The rate of diffusion of a drug across a membrane is dependent upon

Fick’s Law

A

True. Rate of transfer obeys Fick’s Law of diffusion

93
Q

The rate of diffusion of a drug across a membrane is dependent upon

Dalton’s Law

A

False. Dalton’s Law of partial pressures states that the pressure exerted by a mixture of gases or vapours enclosed in a given space, is equal to the sum of the pressures which each gas would exert if it alone were present

94
Q

The rate of diffusion of a drug across a membrane is dependent upon

The surface area of the membrane

A

True. Part of Fick’s Law

95
Q

The rate of diffusion of a drug across a membrane is dependent upon

The degree of ionization of the drug

A

True. Unionised molecules cross membranes more readily

96
Q

The following are examples of physiological antagonism

Morphine and naloxone

A

False. Morphine and naloxone are acting at the same receptor, thus this is a pharmacological antagonism.

Physiological antagonism is the interaction of two drugs whose opposing actions tend to cancel each other. e.g. noradrenaline increasing blood pressure and histamine.

97
Q

The following are examples of physiological antagonism

Fentanyl and doxapram

A

True.

Physiological antagonism is the interaction of two drugs whose opposing actions tend to cancel each other. e.g. noradrenaline increasing blood pressure and histamine.

98
Q

The following are examples of physiological antagonism

Morphine and pentazocine

A

False. Morphine and pentazocine are not acting on opposing physiological mechanisms. They are both analgesics.

Physiological antagonism is the interaction of two drugs whose opposing actions tend to cancel each other. e.g. noradrenaline increasing blood pressure and histamine.

99
Q

The following are examples of physiological antagonism

Ritodrine and syntocinon

A

True.

Physiological antagonism is the interaction of two drugs whose opposing actions tend to cancel each other. e.g. noradrenaline increasing blood pressure and histamine.

100
Q

The following are examples of physiological antagonism

Frusemide and amiloride

A

True - only in the context of sparing potassium. They are both diuretics.

Physiological antagonism is the interaction of two drugs whose opposing actions tend to cancel each other. e.g. noradrenaline increasing blood pressure and histamine.

E-lfh FRCA Primary: Pharmacology - Pharmacodynamics (3 decks)

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