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MODULE 14 - Patient Support > PHARMACOLOGY - Analgesic Drugs > Flashcards

PHARMACOLOGY - Analgesic Drugs Flashcards

1
Q

What is the mechanism of action of opioids?

A

Opioids activate μ (mu) κ (kappa) and δ (delta) receptors to decrease neuronal excitability

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2
Q

What are the two desired effects that opioids have on the central nervous system (CNS)?

A

Analgesia
Sedation

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3
Q

What are the seven side affects of opioids?

A

Euphoria
Nausea/vomiting
Respiratory depression
Antitussive (suppresses cough reflex)
Miosis (pupil constriction) Mydriasis in cats
Constipation
Histamine release

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4
Q

Why is oral administration of opioids unreliable?

A

Oral administration of opioids is unreliable due to first pass metabolism

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5
Q

What are the five indications to administer opioid drugs?

A

To reduce moderate to severe pain
To provide sedation
To reduce the dose of general anaesthetic required
To treat diarrhoea
To control excessive coughing

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6
Q

Why are opioids contraindicated in patients with existing hypoventilation?

A

Administering opioids to a patient with existing hypoventilation will make the patient more at risk to respiratory depression

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7
Q

Why are opioids contraindicated in patients with increased intracranial pressure (ICP)?

A

Opioids cause respiratory depression through decreasing the sensitivity of the respiratory centre in the brainstem to changes in partial pressure of CO2 which can result in hypercapnia. Hypercapnia triggers cerebral vasodilation to increase blood flow to flush out the excess CO2, however this can further increase intracranial pressure (ICP)

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8
Q

(T/F) Opioids which act on the κ (kappa) receptor have the most profound analgesic effect

A

FALSE. Opioids which act on the μ (mu) receptor have the most profound analgesic effect

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9
Q

What are the three classifications of opioids?

A

Agonists
Partial agonists
Antagonists

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10
Q

Which classification of opioids has the most efficacious effect?

A

Agonists

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11
Q

What are partial agonists?

A

Partial agonists are drugs which induce a submaximal response (i.e. lower efficacy)

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12
Q

Why is it ineffective to use an agonist opioid following the administration of a partial agonist opioid?

A

Partial agonist opioid have a very high affinity for opioid receptors, reducing the number of receptors that the full agonist opioid would have to bind to, reducing its desired effect

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13
Q

Give six examples of opioid drugs

A

Methadone
Pethidine
Bupremorphine
Butorphanol
Fentanyl
Tramadol

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14
Q

Give three examples of full μ (mu) agonists

A

Methodone
Pethidine
Fentanyl

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15
Q

(T/F) Pethidine has a long duration of action

A

FALSE. Pethidine has a short duration of action

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16
Q

(T/F) Fentanyl has a short duration of action

A

TRUE.

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17
Q

Give an example of a partial μ (mu) agonist

A

Buprenorphine
Tramadol

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18
Q

Give an example of a partial κ (kappa) agonist

A

Butorphanol

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19
Q

What is the mechanism of action for NSAIDS?

A

NSAIDS inhibit the production of proinflammatory mediators prostaglandin and thromboxane A through reversible inhibition of the cyclooxygenase (COX) enzyme

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20
Q

What are the two main isoforms of cyclooxygenase (COX)?

A

Cyclooxygenase-1 (COX-1)
Cyclooxygenase-2 (COX-2)

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21
Q

Which cyclooxygenase isoform is mainly involved in physiological function?

A

Cyclooxygenase-1 (COX-1)

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22
Q

Which cyclooxygenase isoform is up-regulated in response to inflammatory stimuli?

A

Cyclooxygenase-2 (COX-2)

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23
Q

What are the five useful effects of NSAIDS?

A

Analgesic
Anti-pyretic
Anti-inflammatory
Anti-thrombotic
Anti-tumour effects

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24
Q

What are the four indicators to administer NSAIDS?

A

Pain management
Management of inflammatory disorders
Management of pro-thrombotic states
Management of specific tumours

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25
Q

What are the seven contraindicators to the administration of NSAIDS?

A

Patients with gastrointestinal tract disease
Patients with acute or chronic renal disease
Patients with impaired hepatic funtion
Patients with haemostatic disorders
Patients being concurrently treated with steroids
Breeding, pregnant or lactating animals
Patients with unstable asthma

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26
Q

What are the physiological roles of prostaglandins within the gastrointestinal tract?

A

Within the gastrointestinal tract, prostaglandins inhibit gastric secretion and cause vasodilation to increase blood flow to the stomach and increase mucus production to protect the gastric mucosa

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27
Q

Why are NSAIDS contraindicated in patients with gastrointestinal disease?

A

NSAIDS inhibit cyclooxygenase-1 (COX-1) and thus reduce prostaglandin synthesis which will cause a reduction in blood flow to the gastric mucosa, mucosal ischaemia followed by impairment of the protective mucosal barrier which will expose the gastric mucosa to the gastric acid causing ulceration

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28
Q

Why should NSAIDS always be given with food?

A

NSAIDS should always be given with food to protect the gastrointestinal mucosa as the contact area of the tablet will receive a high localised concentration of the drug which will increase the risk of ulceration in that area

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29
Q

Which cyclooxgenase (COX) isoform is primary involved in physiological renal function?

A

Cyclooxygenase 2 (COX-2)

Important to note that COX-2 specific NSAIDS will not have any less adverse affects on the kidneys

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30
Q

What are the physiological roles of prostaglandins in the kidneys?

A

Renal prostaglandins have a vasodilatory effect and thus increase renal blood flow, improving renal function and excretion. Prostaglandins also provide compensatory vasodilation i.e. maintain blood flow in the presence of vasoconstrictors

31
Q

Why are NSAIDS contraindicated in patients with acute or chronic renal disease?

A

NSAIDS inhibit cyclooxygenase and thus reduce prostaglandin production which will impair renal blood flow putting these patients at a higher risk of dehydration and acute renal failure

32
Q

Why are NSAIDS contraindicated in patients with impaired hepatic function?

A

NSAIDS are metabolised by the liver and thus in patients with impaired hepatic function there is an increased risk of drug accumulation and therefore an increased risk of side effects

33
Q

Why are NSAIDS contraindicated in breeding, pregnant or lactating animals?

A

NSAIDS are teratogenic. Furthermore, NSAIDS inhibit prostaglandin production and since prostaglandins have a role in ovulation, embryo implantation and parturition, this can have adverse effects

34
Q

Why are NSAIDS contraindicated in patients with unstable asthma?

A

NSAIDs inhibit the cyclooxygenase pathway which can result in a shift to increase arachidonic acid metabolite production via the lipoxygenase pathyway which results in the production of lipoxins and leukotriens. Leukotriens trigger bronchoconstriction which exacerbates asthma

35
Q

Which species is more prone to asthma?

A

Cats

36
Q

What are the three classifications of NSAIDS?

A

Non-selective COX inhibitors
Preferential COX-2 inhibitors
Specific COX-2 inhibitors

37
Q

Which classification of NSAIDS has reduced side effects?

A

Specific COX-2 inhibitors

38
Q

Give two examples of non-selective COX inhibitors

A

Flunixin
Ketoprofen

39
Q

Give two examples of preferential COX-2 inhibitors

A

Meloxicam
Carprofen

40
Q

Give two examples of specific COX-2 inhibitors

A

Fibrocoxib
Robenacoxib

41
Q

Give an example of a non-COX inhibiting NSAID

A

Grapiprant

42
Q

What is the mechanism of action for Grapiprant?

A

Grapiprant is an EP4 prostaglandin receptor antagonist. EP4 receptors mediate pain caused by inflammation, thus inhibition of this receptor prevents the binding of prostaglandin resulting in an analgesic effect

43
Q

Why does grapiprant have fewer adverse effects than other NSAIDS?

A

Grapiprant does not inhibit the physiological production of prostaglandins resulting in fewer adverse effects

44
Q

What is the mechanism of action for local anaesthetics?

A

Local anaesthetics prevent the initiation and conduction of action potentials through blocking the voltage-gated sodium channels of nociceptive afferent (sensory) nerve fibres

45
Q

What are the two desirable effects of local anaesthetics?

A

Analgesia
Antiarrhythmic

46
Q

Which local anaesthetic is antiarrhythmic?

A

Lidocaine

47
Q

Are local anaesthetics weak acids or weak bases?

A

Local anaesthetics are weak bases

48
Q

Why are inflamed tissues resistant to local anaesthetics?

A

Inflammatory tissue has an acidic environment, which means the equilibrium will shift to the left and more of the local anaesthetic will exist in its charged form, reducing the quantity of uncharged drug available to cross the cell membrane

49
Q

How does protein binding influence the duration of action of local anaesthetics?

A

Local anaesthetics have the ability to bind to local structural proteins. The higher degree of protein binding increases the duration of action as there will be a larger reservoir of drug available

50
Q

Why is bicarbonate sometimes added to local anaesthetics?

A

Bicarbonate increases the pH causing the equilibrium to shift to the right to increase the quantity of local anaesthetic in its unionised form (uncharged) to increase the quantity of drug that can cross the cell membranes and carry out it’s effect - increasing speed of onset

51
Q

Why is adrenaline sometimes added to local anaesthetics?

A

Adrenaline acts on α1 adrenoreceptors on vascular smooth muscle which causes a local vasoconstriction which will limit the blood flow to the area which will decrease the volume of blood that can wash the drug away. This will increase the length of time the local anaesthetic can enter surrounding cells, prolonging it’s effect

52
Q

When are harmful side affects to local anaesthetics most likely to occur?

A

Harmful affects are most likely to occur following an overdose of local anaesthetics or accidental intravenous administration

53
Q

What are the harmful affects that local anaesthetics can have on the central nervous system?

A

Convulsions
Depression
Coma
Death

54
Q

What are the harmful affects that local anaesthetics can have on the cardiovascular system?

A

Bradycardia
Hypotension

55
Q

When would you use topical anaesthesia?

A

To desensitise intact skin or mucous membranes

56
Q

When would you use local infiltration of local anaesthesia?

A

To desensitise dermal and subcutaneous tissues for minor surgery

57
Q

When would you use cavity instillation of local anaesthetics?

A

Cavity instillation of local anaesthetics can often be used for diagnostics

58
Q

When would you use a peripheral nerve block?

A

Peripheral nerve blocks can be used both diagnostically and therapeutically

59
Q

What is epidural administration of a local anaesthetic?

A

Epidural administration is the administration of a local anaesthetic into the epidural space

60
Q

When is epidural administration of local anaesthetics contraindicated?

A

Patients with haemostatic disorders
Patients with pyoderma

61
Q

Why is epidural administration of local anaesthetics contraindicated in patients with haemostatic disorders?

A

If you cause bleeding when introducing the needle into the epidural space, a patient with a haemostatic disorder won’t be able to clot which can result in blood accumulating and haematoma formation in the epidural space causing spinal cord compression

62
Q

Why is epidural administration of local anaesthetics contraindicated in patients with pyoderma?

A

In patients with pyoderma you can introduce bacteria into the epidural space when injecting the local anaesthetic

63
Q

Which local anaesthetic drug can you use for intravenous regional anaesthesia?

A

Adrenaline free preparation of lidocaine

64
Q

Which local anaesthetic drug should you NEVER use for intravenous regional anaesthesia?

A

Bupivicaine

65
Q

What is emla cream?

A

Emla cream is a local anaesthetic cream made by a mix of lidocaine and prilocaine. This is especially useful for patients with very sensitive skin such as rabbits

66
Q

What is oral transmucosal administration?

A

Oral transmucosal administration is the absorption of a drug through the buccal mucosa into the systemic circulation

67
Q

What is the main benefit of oral transmucosal administration compared to oral administration?

A

Oral transmucosal administration reduces the impact of first pass metabolism so the bioavailability is greater than it would be following ingestion

68
Q

What is transdermal administration?

A

Transdermal administration is when lipid soluble, potent drugs are absorbed through the skin into the systemic circulation

69
Q

Give an example of an opioid drug that can be administered transdermally

A

Fentanyl patch

70
Q

What are the two main advantages of a fentanyl patch?

A

Allows for opioid treatment at home
Long duration of action (three days)

71
Q

What are the four disadvantages of a fentanyl patch?

A

Takes time to reach peak effect
Variable uptake
Problems with adhesion of the patch
Risk of recreational abuse by owners

72
Q

How long does it take a fentanyl patch to reach it’s peak effect in dogs?

A

24 hours

73
Q

How long does it take a fentanyl patch to reach it’s peak effect in cats?

A

12 hours

74
Q

Which factors should you consider when choosing analgesic drugs?

A
  1. Patient pain severity, health status and temperament
  2. Procedure invasiveness and possible complications
  3. Environment in which the drug is being given (i.e. at home? at the practice?)
  4. Convenience/practicality and affordability for the client
  5. Controlled drug legislation and veterinary medicine register

MODULE 14 - Patient Support (25 decks)

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