Analgesia Flashcards

1
Q

What you need to know when prescribing analgesia?

A
  • Choose a limited number drugs and know them well
  • Mechanism of action
  • Doses
  • Side effects
  • Interactions
  • Groups of patients to avoid
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2
Q

What is the Arachidonic Acid pathway?

A
  • Tissue injury
  • Leads to Injury to Phospholipid Cell membrane
  • Phospholipase A2 released and causes release of arachidonic acid from phospholipid membrane
  • Leads to two pathways

Pathway 1 - Cyclooxygenase Pathway (COX-1, COX-2)
- Lead to Prostaglandin G2 (PGG2)
- Lead to Prostaglandin H2 (PGH2)
- Lead to Prostacyclin/ Prostaglandin which causes pain, inflammation/ Thromboxane cause platelet aggregation

Pathway 2 - 5- Lipoxygenase Pathway
- Lead to Leukotrienes which cause bronchoconstriction, asthma attacks and smooth muscle contraction

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3
Q

How do Prostaglandins cause pain?

A
  • Do not cause pain directly but
  • Sensitise tissues to other inflammatory products such as leukotrienes
  • If prostaglandin production decreases, this will moderate pain
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4
Q

What is Aspirin?

A
  • NSAIDs drug
  • Effective for dental and TMJ pain
  • Superior anti-inflammatory properties to paracetamol
  • Less common in dentistry as Ibuprofen more common
  • Can be bought over counter
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5
Q

What are the Properties of Aspirin (Acetylsalicylic acid)?

A
  • Analgesic
  • Antipyretic
  • Anti-inflammatory
  • Metabolic
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6
Q

What is the mechanism of action for Aspirin?

A
  • Aspirin inhibits cyclo-oxygenases (COX-1 and 2)
  • Therefore reduces production of Prostaglandin
  • More effective at inhibiting COX-1
  • COX-1 inhibition reduces platelet aggregation (predisposes to damage of gastric mucosa)
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7
Q

What are Aspirins Analgesic Properties?

A
  • Analgesic action of NSAIDs exerted both peripherally and centrally
  • Peripheral actions predominate
  • Analgesic action results from inhibition of prostaglandin synthesis in inflamed tissues (Cyclo-oxygenase inhibition)
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8
Q

What are the Antipyretic properties of Aspirin?

A
  • Aspirin prevents temperature raising effects of interleukin-1 and rise in brain prostaglandin levels
  • So reduces elevated temperature in fever
  • Doesn’t reduce normal temp
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9
Q

What are the Anti-inflammatory properties of Aspirin?

A
  • Prostaglandins are vasodilators therefore affect capillary permeability
  • Aspirin good anti-inflammatory
  • Reduces redness and swelling as well as pain at site of injury
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10
Q

What are some problems with Aspirin?

A
  • Adverse/side effect
  • Groups to avoid
  • Caution when prescribing
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11
Q

What are some adverse effects of Aspirin?

A
  • GIT problems
  • Hypersensitivity
  • Overdose (tinnitus, metabolic acidosis)
  • Aspirin burns (mucosal)
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12
Q

What is metabolic acidosis?

A
  • Condition where excess acid in bodily fluids
  • Causes rapid breathing, confusion, tiredness, headache, jaundice and increased heart rate
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13
Q

What are the GIT problems associated with Aspirin?

A
  • Mostly on mucosal lining of stomach
  • Prostaglandins (PGE2 and PGI2)
  • Inhibit gastric acid secretion
  • Increase blood flow through gastric mucosa
  • Help production of mucin by cells in stomach lining (cytoprotective action)
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14
Q

Why do you need to take care with patients with GIT problems when prescribing aspirin?

A
  • Patients may have ulcers or Gastro-oesophageal reflux
  • Most pt taking aspirin will suffer some blood loss from GIT (not detectable macroscopically and asymptomatic)
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15
Q

What reactions can occur with hypersensitivity adverse effects of apsirin?

A
  • Acute bronchospasm/ asthma type attacks
  • Skin rashes / urticaria/ angiodema
  • Other allergies
  • Take care when prescribing to asthmatics
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16
Q

What can happen during overdose of aspirin?

A
  • Hyperventilation
  • Tinnitus, deafness
  • Vasodilatation & sweating
  • Metabolic acidosis (can be life threatening)
  • Coma (Uncommon)
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17
Q

What can happen during mucosal burn adverse effect of Aspirin?

A
  • Direct effect of salicylic acid
  • Aspirin applied locally to oral mucosa results in a chemical burns
  • Aspirin has no topical effect.
    *Ensure aspirin taken with water
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18
Q

What groups should you avoid/ caution when prescribing Aspirin?

A
  1. Peptic Ulceration
  2. Epigastric pain
  3. Bleeding abnormalities e.g. Haemophilia
  4. Anticoagulants
  5. Pregnancy/breast-feeding
  6. Patients on steroids
  7. Renal/Hepatic impairment
  8. Children & Adolescents under 16 years
  9. Asthma
  10. Hypersensitivity to other NSAIDs
  11. Taking other NSAIDs
  12. Elderly
  13. G6PD-deficiency
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19
Q

Why should you avoid groups with peptic ulceration when prescribing aspirin?

A
  • Gastric or duodenal ulcer could result in perforation in people with peptic ulcer disease
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20
Q

Why should you avoid groups with Epigastric pain when prescribing aspirin?

A

When History of epigastric pain / discomfort or gastro-oesophageal reflux but no ulcer diagnosed

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21
Q

Why avoid prescribing Aspirin when patients taking Anticoagulants?

A
  • Aspirin enhances warfarin and other coumarin anticoagulants
  • Displaces warfarin from binding sites on plasma proteins
  • Increases free warfarin
  • The majority of warfarin is bound (inactive). If more is released this will become active increasing bleeding tendency
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22
Q

Why avoid prescribing Aspirin in groups who are pregnant/lactation?

A
  • Especially 3rd trimester:
  • This is nearer delivery and may cause impairment of platelet function:
    • Increased risk of haemorrhage
    • Increased risk of jaundice in baby
    • Can prolong/delay labour (don’t know why)
      (contraindicated in breastfeeding – Reye’s syndrome)
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23
Q

Why avoid prescribing Aspirin for patients on steroids?

A
  • Approx. 25% of patients on long term systemic steroids will develop a peptic ulcer
  • If they have an undiagnosed ulcer, Aspirin may result in perforation
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24
Q

Why avoid prescribing Aspirin for patients with Renal/ Hepatic impairment?

A
  • Aspirin metabolised in liver and excreted mainly in the kidney
  • If renal impairment - excretion may be reduced/delayed
  • Not a complete contraindication but administer with care/reduce dose and avoid if renal or hepatic impairment severe
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25
Q

What is Nephrotoxicity?

A
  • Prostaglandins PGE2 and PGI2 are powerful vasodilators
  • PGE2 synthesised in renal medulla
  • PGI2 synthesised in glomeruli
  • Both involved in control of renal blood flow and excretion of salt and water
  • Inhibition of renal prostaglandin synthesis may result in;
  • sodium retention
  • reduced renal blood flow
  • renal failure,
  • NSAIDs may cause interstitial nephritis and hyperkalaemia.
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26
Q

Why should you avoid prescribing Aspirin to Children and Adolescents under 16years?

A
  • Can cause Reye’s syndrome which is very serious with up to 50% mortality
  • Avoid during fever or viral infections in adolescents
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27
Q

What is Reye’s Syndrome?

A
  • Very rare
  • Fatty degenerative process in liver
  • Profound swelling in brain
  • Can lead to liver damage and Encephalopathy
  • Mortality rate 50% related to brain damage due to encephalopathy
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28
Q

Why should you avoid/caution patients with Asthma when prescribing Aspirin?

A
  • NSAIDs not completely contraindicated as some asthmatics have no problem with them
  • Ask the patient if they have used them before and if any problems
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29
Q

Why should you avoid patients with hypersensivity to other NSAIDs?

A
  • Contraindicated in patients with history of hypersensitivity to Aspirin or any other NSAIDs
  • Using a combo of NSAIDs will increase the risk of side effects
30
Q

Why should elderly groups be avoided/cautioned when prescribing Aspirin?

A
  • Elderly more susceptible to drug induced side effects in general
  • They often smaller/ smaller circulating blood volume
  • On other medications
  • Have other medical problems
31
Q

What deficiency should be avoided/cautioned when prescribing Aspirin?

A
  • Glucose 6-phosphate dehydrogenase deficiency prevalent in individuals originating from parts of Africa/ Asia/ Oceana/ Southern Europe
  • More susceptible to developing acute haemolytic anaemia on taking number of common drugs
  • Aspirin carries poss risk of haemolysis in some deficient individuals
  • Acceptable up to dose of at least 1g daily in most deficient individuals
32
Q

What groups is Aspirin completely contraindicated in?

A
  1. Children & Adolescents under 16 years; breast feeding (Reye’s Syndrome)
  2. Previous or active peptic ulceration
  3. Haemophilia
  4. Hypersensitivity to Aspirin or any other NSAID
33
Q

How does Ibuprofen effect gastric mucosa?

A
  • Irritant to gastric mucosa but lower risk than aspirin
34
Q

Why should you take care when prescribing Ibuprofen for asthmatics?

A
  • May cause bronchospasm but not completely contraindicated
35
Q

What is the max adults does of Ibuprofen?

A
  • 2.4g
36
Q

What groups should you take caution with Ibuprofen?

A
  • Previous or active peptic ulceration
  • The Elderly
  • Pregnancy & lactation
  • Renal, cardiac or hepatic impairment
  • History of hypersensitivity to Aspirin & other NSAIDs
  • Asthma
  • Patient taking other NSAIDs
  • Patients on long term systemic steroids
37
Q

What are the side effects of Ibuprofen?

A
  • GIT discomfort, occasionally bleeding & ulceration
  • Hypersensitivity reactions e.g. rashes, angioedema & bronchospasm
  • Others: headache, dizziness, nervousness, depression, drowsiness, insomnia, vertigo, hearing disturbance/tinnitus, photosensitivity, haematuria, blood disorders, fluid retention, renal impairment, hepatic damage, pancreatitis, eye changes, Stevens-Johnson syndrome & others (see BNF)
38
Q

What are the potential drug interactions of Ibuprofen?

A
  • ACE Inhibitors
  • Other Analgesics
  • Antibiotics
  • Anticoagulants
  • Antidepressants
  • Antidiabetics
  • Corticosteroids
  • Cytotoxics
  • Diuretics
  • Beta-blockers
  • Calcium-channel blockers
  • Cardiac glycosides
  • Ciclosporin
  • Clonidine
  • Clopidogrel (an antiplatelet drug)
  • Lithium
  • Tacrolimus
  • Vasodilator Antihypertensives
    (CHECK BNF)
39
Q

What are the symptoms and treatment for Ibuprofen overdose?

A
  • Nausea
  • Vomiting
  • Tinnitus (more serious toxicity very uncommon)

Activated charcoal followed by symptomatic measures are indicated if more than 400mg/kg has been ingested within the preceding hour.

40
Q

What is paracetamol?

A
  • AKA Acetaminophen
  • Simple analgesic without anti-inflammatory activty
41
Q

What are the benefits of Paracetamol?

A
  • Analgesic
  • Antipyretic
  • Little or no anti-inflammatory action
  • No effects on bleeding time
  • Does not interact significantly with Warfarin
  • Less irritant to GIT
  • Suitable for children
42
Q

What is the mode of action of Paracetamol?

A
  • Hydroperoxides are generated from the metabolism of arachidonic acid by COX and exert a positive feedback to stimulate COX activity
  • This feedback is blocked by paracetamol, thus indirectly inhibiting COX – especially in the brain
43
Q

What does Paracetamol mode of action result in?

A
  • Analgesia
  • Antipyretic action
  • No reduction in peripheral inflammation
44
Q

Where is the main site of action of Paracetamol?

A
  • Reduction of prostaglandin in pain pathways of CNS, in thalamus
45
Q

What is the alternative central mechanism for mode of action of Paracetamol?

A
  • Reduced 5HT production
  • Interference with the excitatory amino acid NMDA (N-Methyl-D-Aspartate) in spinal cord pathways
    Exact mode of action still unclear
46
Q

What cautions should take when prescribing Paracetamol?

A
  • Hepatic impairment
  • Renal impairment
  • Alcohol dependence
47
Q

What are the side effects of Paracetamol?

A
  • Rare but can still occur
  • Rashes
  • Blood disorders
  • Hypotension reported on infusion
  • Liver damage (and less frequently kidney damage) following overdose
48
Q

What drugs interact with Paracetamol?

A
  • Anticoagulants (prolonged regular use of Paracetamol possibly enhances the anticoagulant effects of the coumarins)
  • Cytotoxics
  • Domperidone
  • Lipid-regulating drugs
  • Metoclopramide
49
Q

What is the dosage of Paracetamol?

A

500mg tablets

  • Adults: 1-2 tablets (0.5-1g) 4-6 hourly
    Max. Dose: 4g daily (8 tablets)
  • Children: Depends on weight/age – see BNF

Always warn patients of max dose and not to exceed this

50
Q

What can happen if a patient has an overdose of Paracetamol?

A
  • 10-15g (20-30 tablets) or 150mg/kg taken within 24hrs may cause severe hepatocellular necrosis, and less frequently, renal tubular necrosis
  • Liver damage maximal at 3-4 days after ingestion - lead to liver failure then death
  • Transfer to hospital immediately
51
Q

How do opioid analgesics work?

A
  • Act on spinal cord esp in dorsal horn pathways
  • Central regulation of pain
  • Produce their effects via specific receptors which are closely associated with the neuronal pathways that transmit pain to the CNS
    BNF -‘Opioid analgesics are relatively ineffective in dental pain’
52
Q

What are some examples of Opioids?

A
  • Fentanyl (extremely potent)
  • Morphine
  • Tramadol
  • Codeine (weak)
53
Q

What problems can arise from Opioid Problems?

A

Psychological and Physical Dependence - Withdrawal of the drug will lead to psychological cravings and the patient will also be physically ill

Tolerance - To achieve the same therapeutic effects the dose of the drug needs to be progressively increased

  • Constipation (can occur after just a few doses)
  • Urinary & bile retention
54
Q

How do Opioid Analgesics effect CNS?

A

Depresses;
- Pain centre (alters awareness/perception of pain)
- Higher centres
- Respiratory centre
- Cough centre

55
Q

What are the side effects of Opioids?

A
  • Nausea, vomiting & drowsiness
  • Larger doses produce respiratory depression & hypotension
  • Dry mouth
  • Hallucinations
  • Sweating
  • Dysphoria
  • Facial flushing
  • Mood changes
  • Headache
  • Dependence
  • Vertigo
  • Bradycardia
  • Tachycardia
  • Rashes/Urticaria/Pruritis
  • Palpitations
56
Q

What groups should you caution when prescribing Opioids?

A
  • Hypotension
  • Hypothyroidism
  • Asthma
  • Decreased respiratory reserve
  • Pregnancy/Breast-feeding
  • May precipitate coma in hepatic impairment (reduce dose or avoid)
  • Renal impairment (reduce dose or avoid)
  • Elderly & debilitated (reduce dose)
  • Convulsive disorders
  • Dependence
57
Q

What are some contraindications of Opioids?

A
  • Acute respiratory depression
  • Acute alcoholism
  • Raised intracranial pressure/head injury
    • Interferes with respiration
    • Affects pupillary responses vital for neurological assessment.
58
Q

What is Codeine?

A
  • A natural alkaloid found in opium poppy
  • 1/12th the potency of morphine
  • Effective orally
  • Low dependence
  • Usually in combination with NSAIDs or Paracetamol e.g. Co-codamol (8mg Codeine : 500mg Paracetamol)
  • Effective cough suppressant
  • Common side effect – constipation
  • Available over the counter
59
Q

What codeine combination is on the dental list?

A
  • Dihydrocodeine
  • Codeine phosphate is not
60
Q

What is Dihydrocodeine?

A
  • Potency similar to codeine
  • Routes: SC / IM / Oral
  • Only route on Dental List = Oral
  • Oral Dose: 30mg every 4-6 hours as necessary
    (40mg, 60mg, 120mg tablets not on the Dental List)
61
Q

What are the side effects of Dihydrocodeine?

A
  • Nausea/Vomiting
  • Constipation
  • Drowsiness
  • Larger Doses: Respiratory depression, Hypotension, and many more
62
Q

What are the two main drugs Dihydrocodeine interacts with?

A
  • Antidepressants MAOIs
  • Dopaminergics (Parkinsonism)
63
Q

What groups should you caution when prescribing Dihydrocodeine?

A
  • Hypotension
  • Asthma
  • Pregnancy/lactation
  • Renal/Hepatic disease
  • Elderly/Children
    Remember: Never prescribe in raised intracranial pressure/suspected head injury
64
Q

When should you use Dihydrocodeine?

A
  • Moderate to severe pain
  • However, BNF states that due to the side effects of nausea and vomiting it is of little value for dental pain
  • Patients look ill – very pale
  • BNF also states that it is not very effective for post-operative dental pain
65
Q

What can opioid overdose cause?

A
  • Coma
  • Respiratory depression
  • Pinpoint pupils
66
Q

What is the antidote for Opioid overdose?

A
  • Naloxone if there is coma or bradypnoea
  • Naloxone has a shorter duration of action than many opioids. Therefore, close monitoring and repeated injections/infusion may be necessary
67
Q

What is included in the BNF category related to neuropathic and functional pain?

A
  • Trigeminal neuralgia
  • Post-herpetic neuralgia
  • Functional – TMJ or Atypical facial pain
68
Q

What drug can be used to control trigeminal neuralgia?

A
  • Carbamazepine
  • Proprietary brand e.g. Tegretol
  • Anti-convulsant
  • Gabapentin and Phenytoin can also be used but they are not on Dental List
69
Q

What are the clinical features of Trigeminal Neuralgia?

A
  • Severe spasms of pain: ‘Electric shock’, lasts seconds
  • Usually unilateral
  • Older age-group
  • Trigger spot identified
  • Females more than males
  • Periods of remission
  • Recurrences often greater severity
70
Q

What is the dose of Carbamazepine for Trigeminal Neuralgia?

A
  • 100 or 200 mg tablets
  • Starting dose 100mg once or twice daily (but some patients may require higher initial dose)
  • Increase gradually according to response
  • Usual dose 200mg 3-4 times daily, up to 1.6g daily in some patients