PHARMACOLOGY - Respiratory Pharmacology and General Anaesthetics Flashcards

1
Q

How can the lungs be used as a route of drug administration?

A

The lungs can be used as a route of drug administration through the inhalation of gaseous or vaporised drugs

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2
Q

Which pharmacokinetic properties of an inhaled drug would achieve systemic distribution?

A

An inhaled drug that is uncharged (highly lipid soluble) will be able to diffuse through lipid membranes into the bloodstream

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3
Q

What pharmacokinetic properties of an inhaled drug would achieve localised distribution?

A

An inhaled drug that is charged (limited lipid solubility) will not be able to diffuse though lipid membranes and thus remain in the lungs

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4
Q

Which type of drug, administered through inhalation, undergos systemic distribution?

A

General anaesthetics

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5
Q

Which types of drug, administered through inhalation, require localised distribution?

A

Bronchodilators
Corticosteroids

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6
Q

What is a premedicant (pre-med)?

A

A premedicant is a drug that is given prior to general anaesthetics

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7
Q

What is an induction drug?

A

An induction drug is a drug that achieves the transition from consciousness to unconsciousness

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8
Q

What is a maintenance drug?

A

A maintenance drug is a drug that maintains the anaesthetic state

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9
Q

(T/F) General anaesthetics have a large therapeutic index

A

FALSE. General anaesthetics have a narrow therapeutic index

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10
Q

What is the oil:gas partition coefficient?

A

The oil:gas partition coefficient is a measure of the distribution of a general anaesthetic between lipid and gas

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11
Q

What is indicated by a high oil:gas partition coefficient (explain why)?

A

A high oil:gas partition coefficient indicates that a general anaesthetic has a higher lipid solubility and thus a higher potency (lower quantity of drug is required to achieve the desired effect)

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12
Q

What is the blood:gas partition coefficient?

A

The blood:gas partition coefficient is a measure of the distribution of a general anaesthetic between blood and gas

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13
Q

What is indicated by a low blood:gas partition coefficient?

A

A low blood:gas partition coefficient indicates that a general anaesthetic has a more rapid induction and recovery

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14
Q

Which organ metabolises inhalational general anaesthetics?

A

Liver

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15
Q

How are inhalational general anaesthetics eliminated?

A

Expiration

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16
Q

What is the risk of more highly metabolised general anaesthetics?

A

General anaesthetics can be metabolised into toxic metabolites which can be eliminated through expiration and thus pose a risk to the staff in the operating theatre

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17
Q

What is the minimum alveolar concentration (MAC)?

A

The concentration of the drug required so 50% of patients will not respond to a particular stimulus

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18
Q

What is indicated by a low minimum alveolar concentration (MAC)?

A

A low minimum alveolar concentration (MAC) indicates that the general anaesthetic has a higher potency as a lower concentration is required to produce the desired effect

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19
Q

Which five factors can affect the minimum alveolar concentration (MAC)?

A

Species
Age
Pregnancy
Hypothermia
Other drugs (such as opioids)

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20
Q

What are inhalational general anaesthetics usually used for?

A

Inhalational general anaesthetics are typically used as maintenance drugs

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21
Q

What is the main advantage of using inhalational general anaesthetics as maintenance drugs?

A

Allows for rapid adjustment of anaesthetic depth

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22
Q

What are the two disadvantages of using inhalational general anaesthetics as maintenance drugs?

A

There is a lot of equipment required
Environmental pollution

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23
Q

(T/F) Halogenated drugs are gaseous general anaesthetics

A

FALSE. Halogenated drugs are vaporised anaesthetics

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24
Q

List four halogenated general anaesthetics

A

Halothane
Isofluorane
Sevofluorane
Desfluorane

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25
Q

Why is isofluorane not an appropriate induction drug?

A

Isofluorane has an unpleasant odour which will cause animals to resist the mask induction

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26
Q

Which halogenated general anaesthetic does not produce toxic metabolites?

A

Sevofluorane

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27
Q

Why is sevofluorane an appropriate induction drug?

A

Sevofluorane has a pleasant odour and causes minimal airway irritation

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28
Q

What is vapour pressure (mmHg)?

A

Vapour pressure is a measure of the ease of vaporisation. The higher the vapour pressure (mmHg) value, the more easily the drug is vaporised

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29
Q

Name a gaseous general anaesthetic

A

Nitrous oxide

30
Q

Why are you unable to use nitrous oxide as a general anaesthetic on its own?

A

Nitrous oxide has a very high minimum alveolar concentration (MAC) due to its very low oil:gas partition coefficient (i.e. very low lipid solubility)

31
Q

What are intravenous general anaesthetics usually used for?

A

Intravenous general anaesthetics are generally used as induction drugs

32
Q

What are the three advantages of using intravenous general anaesthetics as induction drugs?

A

Rapid induction
Rapid protection of the airway
No environmental pollution

33
Q

What is the main disadvantage of using intravenous general anaesthetics as induction drugs?

A

Required intravenous access

34
Q

Why are intravenous general anaesthetics mainly used as induction drugs and not maintenance drugs?

A

Intravenous general anaesthetics are used as induction drugs as they act quickly due to their high lipid solubility, however are not used as maintenance drugs as they are relatively slowly metabolised and eliminated from the body and their short duration of action would require constant infusion to maintain anesthesia

35
Q

Why do intravenous general anaesthetics have such a quick onset but a short duration of action?

A

Intravenous general anaesthetics are highly lipid soluble and thus quickly travel through the bloodstream to the brain to carry out the desired effects, however, these drugs will redistribute to other blood rich organs and even lipid (fat) stores where the drug will accumulate, resulting in a short duration of action

36
Q

Which organ metabolises intravenous general anaesthetics?

A

Liver

37
Q

Which organ eliminates intravenous general anaesthetics?

A

Kidneys

38
Q

What is total intravenous anaesthesia (TIVA)?

A

Total intravenous anaesthesia (TIVA) is the use of intravenous anaesthetic agents for both induction and maintenance of anaesthesia

39
Q

Which intravenous anaesthetic drugs are appropriate for total intravenous anaesthesia (TIVA)? Why?

A

Propofol and Alfaxolone are appropriate for total intravenous anaesthesia (TIVA) as they are rapidly metabolised and can thus be continuously infused for maintenance of general anaesthesia without accumulating in lipid (fat) stores

40
Q

Why would hypoproteinaemic patients alter the pharmacological effects of propofol?

A

Propofol is highly plasma protein bound and thus a hypovolaemic patient will have fewer plasma proteins so there will be more free drug within the bloodstream which will result in an enhanced pharmacological effect

41
Q

Describe how bronchidilation is stimulated

A

Stimulation of the sympathetic nervous system triggers the release of adrenaline which circulates and binds to β2 adrenergic receptors on bronchial smooth muscle, which stimulates adenylate cyclase and thus increases cAMP which inhibits the smooth muscle contrctile pathway, stimulating bronchodilation

42
Q

Which three drug classifications can be used as bronchodilators?

A

β-adrenergic agonists
Anticholinergic drugs
Methylxanthines

43
Q

How do β-adrenergic agonist drugs act as bronchodilators?

A

The drug will bind to β2 adrenergic receptors on bronchial smooth muscle, stimulating adenylate cyclase which will increase the production of cAMP which will inhibit the smooth muscle contractile pathway and stimulate bronchodilation

44
Q

List two β-adrenergic agonist drugs that can be used as bronchodilators?

A

Adrenaline
β2 specific adrenergic agonists

45
Q

When should you use adrenaline as a bronchodilator?

A

If there is emergency, life-threatening bronchoconstriction

46
Q

What are two side effects of β2 specific adrenergic agonists?

A

Tachycardia
Tremors

47
Q

Why should β2 specific adrenergic agonists be used intermittently?

A

β2 specific adrenergic agonists should be used intermittently to avoid tolerance through internalisation of the β2 receptors in response to excessive stimulation

48
Q

List two anticholinergic drugs you could use as bronchodilators

A

Atropine
Ipratroprium bromide

49
Q

What are two side affects of atropine?

A

Central nervous system (CNS) stimulation
Gastrointestinal inhibition

50
Q

What is the main advantage of ipratropium bromide?

A

Ipratropium bromide is a quaternary derivative of atropine which is permanently charged and thus cannot diffuse out of the lungs and cause any side affects

51
Q

What is the mechanism of action of methylxanthines?

A

Methylxanthines are phosphodiesterase (PDE) inhibitors. Phosphodiesterases (PDE) are enzymes which catalyse the hydrolysis of cAMP and thus inhibiting this action, there will be increased and prolonged cAMP, stimulating bronchodilation

52
Q

Name an example of a methylxanthine

A

Theobromine

53
Q

What are the two main functions of corticosteroids?

A

Immune suppressive
Anti-inflammatory

54
Q

What are the two classifications of corticosteroids?

A

Mineralocorticoids
Glucocorticoids

55
Q

Which region of the adrenal cortex produces mineralocorticoids?

A

Zona glomerulosa

56
Q

Which region of the adrenal cortex produces glucocorticoids?

A

Zona fasciculata

57
Q

Name the endogenous corticoid essential for normal physiological function

A

Cortisol

58
Q

Name three examples of synthetic glucocorticoids

A

Prednisolone
Hydrocortisone
Dexamethasone

59
Q

What is the mechanism of action of corticosteroids?

A

Glucocorticoids bind to glucocorticoid receptors to form a steroid-receptor complex which is translocated to the nucleus where this complex will alter gene expression of specific proteins

60
Q

Name three proteins which are upregulated by corticosteroids

A

Angiotensin converting enzyme
β2-adrenoreceptors
Lipocortin 1

61
Q

Name two proteins which are inhibited by corticosteroids

A

Cytokines
Cyclooxygenase (COX)

62
Q

What are water-soluble salt formations of corticosteroids useful for?

A

Water-soluble salt formations of corticosteroids are useful for intravenous (IV) administration, allowing for rapid and systemic delivery throughout the body - useful for immediate treatment

63
Q

What are insoluble ester formations of corticosteroids useful for?

A

Insoluble ester formations are useful for localised administration with a longer duration of action

64
Q

Why is minimal mineralocorticoid activity preferred when administering corticosteroids?

A

To minimise the side effects associated with fluid and electrolyte balance

65
Q

Why should you withdraw corticosteroid treatment gradually?

A

To minimise the risk of an ‘addisonian’ crisis

66
Q

What is Addisons disease?

A

Addisons disease is a deficiency in cortisol secretion

67
Q

What should be administered if an animal is suffering from an ‘addisonian’ crisis?

A

Intravenous (IV) hydrocortisone sodium succinate

68
Q

What is Cushing’s disease?

A

Cushing’s disease is a hypersecretion of cortisol

69
Q

What are the three main tests used to test for Cushing’s disease?

A

ACTH test
Low dose dexamethasone test
High dose dexamethasone test

70
Q

Which Cushing’s disease test is best to use to differentiate between a pituitary and adrenal abnormality?

A

High dose dexamethasone test