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Pharmacology 1 > LA > Flashcards

LA Flashcards

1
Q

The most common type of nociceptor is the?

A

Polymodal nociceptor.

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2
Q

Stimulation of the substantial gelatinosa produces what?

A

Inhibition of pain conduction to the Thalamus.

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3
Q

Dysphoria and hallucinations are mediated by which opioid receptor?

A

Kappa

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4
Q

A∂ nociceptors terminate in what lamina of the dorsal horn?

A

I and V

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5
Q

Which are more easily blocked by local anaesthetics?

(a) Large, myelinated axons.
(b) Small, myelinated axons.
(c) Non-myelinated axons.

A
  1. (b)
  2. (c)
  3. (a)
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6
Q

What is meant by “narcosis”?

A

A stupour and mental clouding produced by high doses of opioid receptor agonists.

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7
Q

Why is pethidine (a strong opioid receptor agonist) safe to use during labour, but other strong agonists aren’t?

A

Because pethidine doesn’t reduce uterine contractions.

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8
Q

C-fibres terminate in what lamina of the dorsal horn?

A

I and II

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9
Q

Respiratory depression is mediated by which opioid receptor?

A

µ

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10
Q

A∂ mechanoreceptors terminate in what lamina of the dorsal horn?

A

II and III

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11
Q

When a local anaesthetic is applied, what are the nerve functions lost first and in what order?

A
  1. Autonomic
  2. Pain
  3. Temperature detection
  4. Touch
  5. Proprioception
  6. Deep pressure
  7. Motor
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12
Q

What is the most common cause of death in an opiate overdose?

A

Respiratory cessation.

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13
Q

Dextropropoxyphene and tramadol belong to which group of opioids?

A

Mild to moderate agonists, the same classification as codeine.

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14
Q

Which opioid receptor has the least amount of effects?

A

∂ receptor

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15
Q

Which symptom tends to disappear with repetitive dosing and which symptom tends to remain even in opioid-dependent users?

A

Nausea and vomitting tends to disappear.

Pupillary constriction is found even in dependents.

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16
Q

Where or what is the substantial gelatinosa?

A

The second lamina of the dorsal horn.

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17
Q

The descending inhibitory pathways have what kind of effect on the substantial gelatinosa?

A

Excitatory.

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18
Q

What receptor mediates histamine release in opioid use?

A

Gotcha! None of them. It’s a direct effect on mast cells.

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19
Q

Lignocaine is used for something other than local anaesthesia, what is it?

A

To treat arrythmias.

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20
Q

Which are more stable, amide or ester local anaesthetics?

A

Amide.

Ester local anaesthetics are rapidly inactivated in the plasma and tissues.

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21
Q

Within what time frame does opioid tolerance develop?

A

12-24 hours

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22
Q

What are some strong opioid agonists?

A

Fentanyl, heroin, morphine and oxycodone.

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23
Q

What long-acting LA has cardiotoxicity? What does it do to the heart?

A

Bupivicaine.

AV block.
Vent. arrythmias.
Decreased cardiac contractility.
Smooth muscle relaxation => Hypotension

24
Q

How is opioid tolerance developed (celullarly)?

A

µ-receptor desensitisation.

25
Q

If a local anaesthetic is systemically circulated, what effects does it have?

A

CNS toxicity

Cardiotoxicity

26
Q

Which has more pharmacologically active metabolites, amide or ester LAs?

A

Amide LAs.

27
Q

Which is a more important factor for opioid dependence, physiological effects or psychological ones.

A

Psychological ones.

28
Q

What are the antagonists of the opioid receptors?

A

Naltrexone and naloxone.

29
Q

What is a moderate opioid receptor agonist?

A

Codeine

30
Q

What’s the average half-life of an opioid drug?

A

3-6hrs.

31
Q

A ‘bier block’ is also known as? How does it work?

A

An IV block. You torniquet the patient’s arm, then IV inject the LA. Anaesthetises the whole arm.

32
Q

Epidurals usually contain what two types of drug?

A

Local anaesthetic and an opioid.

33
Q

Diamorphine is also known as?

A

Heroin

34
Q

Nociceptive neurons are what kind of fibre?

A

C-fibres.

35
Q

Why do local anaesthetics promote themselves being systemically circulated?

A

Because they promote vasodilation.

36
Q

Why is buprenorphine so good for treating opioid addiction?

A

Has high binding to µ receptors.
Antagonises the kappa receptors (responsible for hallucination and dysphoria).
Has a long half-life (24-37hrs).
Has a ceiling on its dose-response effect.
Less sedation and less euphoria.

37
Q

What are the two chemical types of local anaesthetics?

A

Amide and ester anaesthetics.

38
Q

Nalbuphine and pentazocine are what kind of opioid/opiate?

A

Mixed agonist and antagonists.

39
Q

Why don’t local anaesthetics work very well in inflamed tissues?

A

Because inflamed tissues have a low pH (acidic) and hence tend to ionise a large proportion of the local anaesthetic weak base – reducing its effectiveness.

40
Q

What is a partial/mixed agonist of the opioid receptor?

A

Buprenorphine

41
Q

Naltrexone, although used for opioid overdose is also useful for:

A

Treating the craving for alcohol in alcoholics.

42
Q

Opioid receptor binding leads to what neuronal effect?

A

Decreaed neuronal excitability.

43
Q

What are the effects on the CNS from LA drugs?

A

Depressant effect at low doses

Excitation effect at high doses

Profound respiratory depression at high doses

44
Q

Why is methadone used to treat opioid dependence?

A

Weaker, long-acting, blocks the euphoric effect of other opioids, allows for tapering and diminishes abstinence symptoms.

45
Q

In the resting state, what are the statuses of the two gates?

A 
v = closed
t = open
46
Q

Why is adrenaline co-administered with local anaesthetics?

A

It produces vasoconstriction, counteracting the vasodilation of the local anaesthetic.

It also produces a relatively bloodless surgical field.

47
Q

If a local anaesthetic has an increased affinity to plasma proteins, what does that mean for its duration of action?

A

It will have a longer duration of action.

48
Q

Local anaesthetics bind the receptor in what states?

A

The active state or the inactive state, but not the open state.

49
Q

What are the two gates in the sodium voltage-gated channel?

A

‘v’ and ‘t’.

50
Q

If a local anaesthetic is ionised, is it more or less clinically effective?

A

Less clinically effective. Needs to be lipid soluble in order to diffuse through membranes and act.

51
Q

In the inactive state of the sodium voltage-gated channel, what are the statuses of the gates?

A 
v = open 
t = closed
52
Q

Which lamina of the dorsal horn conduct signals to the thalamus via the spinothalamic pathway?

A

I and V

53
Q

Euphoria is mediated by which opioid receptor?

A

µ

54
Q

What kind of pain are opioids useful for and not useful for?

A

Useful: Visceral, deep pain.

Not useful: Neuropathic pain.

55
Q

Respiratory depression is mediated by which opioid receptor?

A

µ

Pharmacology 1 (22 decks)

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