Analgesics Flashcards

1
Q

What is included in step 1-3 of the WHO Analgesic ladder?

A
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2
Q

What is the paracetamol method of action

A

Inhibits cyclo-oxygenase (COX) and therefore prostaglandin production

Acts only centrally as it cannot reach inflammation sites due to susceptibility to peroxides

Anti-pyrexial action

Inhibits take up of anandamine (endocannabinoid)

Inhibit CNS Na+ channels → analgesic

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3
Q

How is paracetamol metabolised?

A

Toxic phase 1 biproduct (N-acetyl-P-Benzoquinonelmine)

Conjugated with Glutathione

When body runs out, toxic product NAPQBI builds up → liver damage

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4
Q

What are the paracetamol OD symptoms and treatment?

A

After 24 hours:

  • N&V
  • Anorexia

After 3-5 days:

  • Abdominal Pain
  • Metabolic Problems etc. - Hyper/hypoglycaemia

Treatment: Activated charcoal; N-acetylcysteine; Methionine

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5
Q

What is perfalgan?

A

IV form of paracetamol

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6
Q

What is the mode of action of NSAIDs?

A

Competitively inhibit COX1 and/or COX2 Enzymes

COX converts Arachidonic Acid to Prostaglandins

COX2 - inflammatory prostaglandins

COX1 - protective prostaglandins - gastric repair, renal perfusion

Analgesic and Anti-inflammatory action

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7
Q

What are the safety concerns of using NSAIDs?

A

GI damage

Damage to kidneys

Sodium and Water retention

Worsening of asthma

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8
Q

What should be done for GI complications when using NSAIDs

A

PPIs used when ↑Risk of GI complications

Prostaglandin Analogues (Misoprostol) can also be added to mimic → ↑Healing and HCO3 production

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9
Q

What are some non-selective COX-inhibitors? and what are the side effects?

A

Ibrupofen, Naproxen, Diclofenac

S/E: GI irritation/Ulceration

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10
Q

Name some COX-2 inhibitors

A

Celecoxib, Etoricoxib

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11
Q

What are the first and second line NSAIDs and what should they be prescribed with in the case of GI problems?

A

Ibrupofen - 1st

Naproxen - 2nd (less thrombotic risk)

Add PPI

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12
Q

What is the mode of action of opioids?

A

Inhibit ascending pathways

Direct inhibition: Bind to 1st order nociceptors in periphery → Induces K+ influx into presynaptic membrane → hyperpolarisation

Indirect inhibition: Activation of descending pathways:

Bind to opioid Rs in Nucleus Raphe Magnus (medulla) → stimulation of serotinergic descending pathway → further release of opioids in dorsal horn → further inhibition

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13
Q

Name some weak opioids

A

Codeine

Dihydrocodeine

Tramadol

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14
Q

How does codeine work? and what is it normally used in combination with?

A

Analgesic properties comes from 〜10% of drug being metabolised in liver → morphine

Best used with paracetamol for analgesia: Co-codamol

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15
Q

What is the mode of action of Tramadol?

A

Has opioid and non-opioid properties

Opioid - weak affinity for μ-receptors

Non-opioid: Serotonin-Noradrenaline Reuptake Inhibitor (and stimulates serotonin release)

Naloxone only partially reverses analgesic properties

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16
Q

When should tramadol be taken with caution?

A

In those with risk of seizures (due to ↑S/N)

May induce CNS toxicity in those using anti-depressants

17
Q

Name some strong opioids

A

Morphine, Fentanyl, Diamorphine, Hydromorphone, Methadone, Oxycodone

18
Q

What is the most appropriate starting agent for strong opioids? and which is used with kidney impairment?

A

Morphine most apporpriate starting agent

Diamorphine quicker onset, and shorter duration of action

Fentanyl in kidney impairment

19
Q

What is the antidote for opioids OD?

A

Naloxone - competitive antagonist of all opioid Rs

Short half life, so OD patients may need top up

20
Q

Name and anti-spasmodic and what is it’s mode of action?

A

Baclofen - GABAB R Agonist - ↑inhibition of motoneurone signals

Relieve pain caused by muscle spasm by reducing spasm

21
Q

Name some anti-convulsants and what are they used for in pain management?

A

Gabapentin/Pregabalin, Carbamazepine

Gabapentin: GABA analogue, unknown mechanism - licensed for neuropathic pain

S/E: Drowsiness, confusion, dizziness

Pregabalin: also used as adjunct antiepileptic and anxiety disorders

22
Q

Name some antidepressants used for neuropathic pain

A

Amitryptiline - neuropathic analgesic

Tricyclic Antidepressant - works as SNRI

S/E: Drowsiness, Arrhythmias, dry mouth, blurred vision

23
Q

Name an NMDA-R Antagonist used for analgesia

A

Ketamine

NMDAR - Induction and maintenance of central sensitisation

Ketamine stops this action

24
Q

What anaesthetics are used in pain management?

A

Lidocaine Patch

Emla cream (Lidocaine + Prilocaine)

Nerve blocks

25
Q

What is Entonox?

A

50% Oxygen; 50% NO

Breathe in through mouth, 4+ breaths for full effect

Eliminated after 30 mins