Analgesics and Sedative Drugs Flashcards

1
Q

What is pain?

A

an unpleasant sensory and emotional experience associated with actual or potential tissue damage or described in terms of such damage

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2
Q

Anagesia

A

relieve pain by directly manipulating its physiological mechanisms

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3
Q

Pain cam be assessed using

A

unidimensional tools like scales/faces

multi-dimensional tools (more history)

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4
Q

What is an adjuvent?

A

Enhancing effect of a drug

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5
Q

WHO Analgesic Ladder:

A
  • needs to be bidirectional
  • step 4 = minimally invasive procedures
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6
Q

Principles of WHO Analgesic Ladder:

A
  • by the mouth = oral administration
  • by the clock = regular and at regular
    intervals
  • by the ladder = according with the pain
    intensity characterised by the patient
  • individualised therapy = dosing
  • medication adherence
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7
Q

Analgesia can be complicated:

A

insert slide

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8
Q

NSAIDs:

A
  • non-steroidal anti-inflammatory drug
  • ibuprofen
  • effects can be peripheral and central
  • competitive inhibitors of COX

Three Effects:
- analgesics
- anti-inflammatory
- antipyretic

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9
Q

Core Drug: Ibuprofen: Mechanism of Action:

A

Competitive inhibitors of COX

(reversible action)

hence:
- reduce production of prostaglandins
- prostaglandins increase Na+/Ca2+
influx into nociceptors, hence
decreasing pain signalling

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10
Q

Core Drug: Aspirin: Mechanism of Action:

A

irreversible inhibitor of COX

lowers amount of time needs to be taken

COX1 in platelets, platelets have no nucleus so can not synthetise new COX1

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11
Q

Arachidonic Acid

A

insert flowchart

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12
Q

Effects of NSAIDs:

A

insert flowchart (17)

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13
Q

Side Effects of Ibuprofen:

A
  • perforation
  • peptic ulcers
  • renal failure
  • fluid retention
  • constipation
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14
Q

How to avoid gastric pain from taking NSAIDs?

A

Proton Pump Inhibitors PPIs

omneprazole

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15
Q

Is paracetamol an NSAID?

A

No only an analgesic and antipyretic not an anti-inflammatory

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16
Q

Core Drug: Paracetamol: Drug Class:

A

Analgesic

17
Q

Core Drug: Paracetamol: Mechanism of Action:

A
  • inhibition of COX
18
Q

Core Drug: Paracetamol: Effects:

A

mainly central
benefit from regular full dosing

19
Q

Core Drug: Paracetamol: Metabolised:

A

Liver

20
Q

Core Drug: Paracetamol: Side Effects:

A
  • patients with liver failure
  • liver impairment
  • adverse effects are rare

NO INJURY TO GASTRIC MUCOSA

21
Q

What is the primary drug class for acute management of moderate to severe pain?

A

Opiods (agonist of opiod receptors)

22
Q

What type of receptors are responsible for most analgesic effects of opiods?

A

mu opiod receptors
coupled to G alpha i

23
Q

Opiod Receptors: Mechanism of Action:

A
  • bind to opiod receptors
  • activate G-alpha-i pathway
  • inhibition of adenylate cyclase, decrease
    in cyclic AMP, decreased
    phosphorylation
  • inhibits Ca2+ voltage gated channels,
    leading to decreased release of
    neurotransmitters
  • activates K+ channels, which
    hyperpolarise cell membranes, less APs
    fired
24
Q

An example of a weak opiod?

A

Core Drug: Codeine

25
Q

Codeine: Ceiling Dose:

A
  • pain relief will stop after a certain dose
  • continuing will simply increase risk or
    intensity of the adverse reactions
26
Q

Does morphine have a ceiling dose?

A

No

27
Q

Core Drugs:

How potent is codeine compared to morphine?

A

1/10th as potent as morphine

28
Q

Core Drug: Codeine: Metabolism:

A

metabolised to morphine by the liver

29
Q

Core Drug: Morphine: Metabolism:

A
  • metabolised to active metabolites
  • renally excreted

can cause renal impairment

30
Q

Core Drug: Codeine: Side Effects:

A
  • constipation = faecal softener +
    stimulant laxative (no)
  • nausea and vomiting = antiemetics (yes)
  • sedation
  • confusion = reduce dose + monitor renal
    function
  • respiratory depression = naloxone
31
Q

Opiod Toxicity: Management:

A
  • initial management:
    - reduce dose
    - hydrate
    - relieve agitation with low dose of
    haloperidol
  • if intolerant side effects with inadequate
    pain relief switch to an alternative
    analgesic
  • naloxone (with caution)
32
Q

Naloxone

A
  • opiod antagonist
  • all opiod receptors (many side effects)
33
Q

Sedation: Pharmacological Management:

A
  • opiods
  • propofol
  • dexmedetomidine
  • benzodiazepine: diazapam
  • Z-drugs; Zopiclone
34
Q

Core Drug: Diazepam: Mechanism of Action:

A
  • GABA receptor modulator (ionotropic)
  • bind in different site to GABA
  • GABA still needed for effect
  • simply facilitating the opening of
    channel
  • Cl- channel
  • hyperpolarise cell, stable and resting
  • depressive effect on the nervous system
35
Q

Core Drug: Diazepam: Side Effects:

A
  • oversedation
  • drowsiness
  • light-headedness
  • amnesia
  • muscle weakness
  • tolerance
  • dependance (need withdrawal
    management)
36
Q

Core Drug: Zopiclone: Mechanism of Action:

A
  • GABA receptor modulator (ionotropic)
  • bind in different site to GABA
  • GABA still needed for effect
  • simply facilitating the opening of
    channel
  • Cl- channel
  • hyperpolarise cell, stable and resting
  • depressive effect on the nervous system
37
Q

Core Drug: Zopiclone: Side Effects:

A
  • dry mouth***
  • metallic taste in mouth***
  • oversedation
  • drowsiness
  • light-headedness
  • confusion
  • amnesia
  • muscle weakness
  • tolerance
  • dependence