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Neurology SB > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

what is the WHO analgesic ladder rungs

A

1 - NSAID (aspirin, diclofenac, naproxen, ibuprofen) or paracetamol
2 - Weak Opioid (codeine, tramadol)
3 - Strong Opioid (morphine, hydromorphone)

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2
Q

how is opioid action mediated

A

G protein coupled opioid receptors

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3
Q

what happens when a opioid binds with its receptor

A

Inhibition of opening of voltage-activated Ca2+ channels

Opening of K+ channels

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4
Q

what effect does Inhibition of opening of voltage-activated Ca2+ channels in opioids have

A

presynaptic effect – suppresses excitatory neurotransmitter release from nociceptor terminals

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5
Q

what effect does opening of potassium channel have in opioids

A

postsynaptic effect- suppresses excitation of projection neurones

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6
Q

what type of opioid receptor does agonist opioids work on

A

mainly through prolonged activation of μ-opioid receptors

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7
Q

features of morphine

A
  • used in acute severe and chronic pain
  • can be given IV, IM or SC
  • oral for chronic pain
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8
Q

features of diamorphine

A
  • more lipophilic than morphine
  • rapid onset of action when administered IV
  • used for post-operative pain
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9
Q

features of fentanyl

A
  • given IV to provide analgesia in maintenance anaesthesia

- suitable for transdermal delivery in chronic pain states, but not in acute pain

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10
Q

features of buprenophine

A
  • useful in chronic pain with patient-controlled injection systems
  • partial agonist
  • slow onset, but long duration of action
  • can be given by injection, or sublingually
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11
Q

features of pethidine

A
  • used in acute pain, particularly labour
  • rapid onset of action when given IV, IM, or SC,
  • short duration of action (no good for control of chronic pain)
  • should not be used in conjunction with MAO inhibitors (excitement, convulsions, hyperthermia)
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12
Q

features of codeine and dihydrocodeine

A
  • weaker opioids used in mild/moderate pain

- given orally, not IV

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13
Q

what opioid should not be used in epilepsy

A

tramadol

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14
Q

features of methadone

A
  • given orally, long duration of action

- main use is to assist in withdrawal from ‘strong opioids’, such as heroin

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15
Q

what opioid is used in animals not humans

A

etorphine

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16
Q

what are the agonist opioid drugs

A
  • morphine
  • diamorphine
  • fentanyl
  • buprenophine
  • pethidine
  • codeine and dihydrocodeine
  • tramadol
  • methadone
17
Q

what are the antagonists opioid drugs

A

naloxone

naltrexone

18
Q

what are features of naloxone

A
  • competitive antagonist at μ-receptors
  • given IV (can give IM and SC if cannot give IV)
  • short half life
19
Q

what is naloxone used for

A

to reverse opioid toxicity (i.e. respiratory and/or neurological depression) associated with ‘strong opioid’ overdosage

20
Q

what can naloxone cause in addicts

A

acute withdrawal response

21
Q

how does naltrexone differ from naloxone

A
  • longer half-life
22
Q

how do NSAIDs work

A

inhibiting the synthesis and accumulation of prostaglandins by enzymes COX-1 and COX-2

23
Q

in selective NSAIDs, what enzyme is blocked

A

just COX-2

24
Q

why is paracetamol not classed as an NSAID

A

it lacks anti-inflammatory activity

25
Q

what are conditions of neuropathic pain

A

trigeminal neuralgia
diabetic neuropathy
post-herpetic neuralgia
phantom limb pain

26
Q

neuropathic pain responses to NSAIDs - true or false

A

false

- also rather insensitive to opioids

27
Q

drugs (and their class) used for neuropathic pain

A

Gabapentin and Pregabalin
- anti-epileptics

Amitriptyline, nortryptiline and desipramine
- TCAs

Carbamazepine

28
Q

what specific neuropathic conditions are gabapentin and pregabalin used for

A

gabapentin - migraine prophylaxis

pregabalin - painful diabetic neuropathy

29
Q

how do TCAs work

A

decrease reuptake of noradrenaline

30
Q

how does carbamazepine work

A

blocks subtypes of voltage-activated Na+ channel that are upregulated in damaged nerve cells

31
Q

what is carbamazepine first line treatment for

A

Trigeminal neuralgia

Neurology SB (23 decks)

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