Lectuer 16: analgesics Flashcards

1
Q

What is pain?

A

-unpleasant sensory and emotional experience assoc with tissue damage or non tissue damage

  • subjective, difficult to quantify
  • similar harm can vary between patients
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2
Q

What must health professionals be aware of with regards to patient and pain?

A

accept patients response to pain

  • be observant
  • show empathy
  • consider if injury matches the level of pain reported
  • know the personality of the patient
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3
Q

How is pain management carried out?

A

-must be individualised to patient based on cause, severity of pain and chronicity

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4
Q

What is the Nociceptive pain pathway?

A
  • begins with tissue damage either due to mechanical, chemical or chemical hurt
  • pain signals are generated and are sent to the dorsal horn, then CNS
  • when the brain receives the signal, it responds by sending a descending inhibtion to relieve the pain message.
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5
Q

What does the nociceptive pathway tell us?

A
  • that there is more than one way to stop the pain.

- therefore local anaesthetis can block the nerve transmission at two sites

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6
Q

What are other possibilities for treating pain?

A
  • reduce signals at local site
  • reduce signals transffered to CNS
  • enhance descending inhibition pathway
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7
Q

What are non-pharmacological alternatives to treating pain?

A
  • transcutaneous electrical nerve stimulation
  • electrica stimulation to manage the pain
  • relaxation therapy (can reduce pain from scale 10 to scale 3)
  • nerve block
  • acupuncture: may induce activation of endogenous opiod system
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8
Q

What is TENS?

A

transcutaneousl electrical nerve stimulation

-electrodes are placed on skin to generate an electrical force that will help to relieve the pain

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9
Q

What are analgesis?

A
  • drugs that mediate pain relief

- we use different drugs to treat different types of pain e.g. for mild-mod pain we use mild drugs.

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10
Q

Why is it important to save the stronger drugs for more severe pain?

A

this increases the pain tolerance and will also help to manage the pain feelings

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11
Q

What are the two most common classes of analgesics?

A

Opioids and non-narotics

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12
Q

What are opioids?

A
  • substances (exogenous or endogenous) which bind to opiiod receptors
  • pharmacologically similar to opium or morphine
  • e.g. codeine, morphine, tramadol,
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13
Q

What are endogenous opioids?

A

-opioids which are naturally relied from the human body and can bind to receptors

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14
Q

What are exogenous opioids?

A

opioids which you have to take as either a drug or other material

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15
Q

What are primary analgesics used for?

A
  • cough suppressants and to control diarrhoea
  • hence elderly often use opioids to treat other medical conditions
  • provides analgesic without anti-pyretic effect
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16
Q

What is a common error with mild opioid use?

A

-the overestimation of the amount of drug used for pain killer purposes

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17
Q

What are are examples of endogenous opioids?

A
  • endorphins
  • dynophins
  • encephalins
  • nociceptins

these bind to your opioid receptors and help to explain the benefits/evidence of acupuncture.

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18
Q

What is the mechanism of action of opioids?

A
  • bind to opioid receptors which are widespread around the CNS
  • highest concentration of receptors is in the pons and pain modulation pathways
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19
Q

What are the 3 subtypes of opioid receptors?

A
  • mu
  • delta
  • kappa

these are distributed differently in different tissues and have different physiological effects in the body.

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20
Q

What is the mu opioid receptor?

A
  • mainly located in brain, spinal cord
  • causes analgesia, respiratory depression, euphoria, addiction
  • blocks all pain messages
21
Q

What is the kappa opioid receptor?

A
  • found in brain and spinal cord
  • causes analgesia, sedation,
  • blocks all non thermal pain messages
22
Q

What is the delta opioid receptor?

A
  • found in the brain

- causes analgesia, anti-depression, dependence

23
Q

Which opioid receptor should be activated/targeted in order to manage pain but reduce the risk of addiction?

A

kappa receptor

24
Q

Which opiod receptor should be used to avoid side effects like respiratory depression?

A

mu receptor

25
What does morphine bind to?
-binds strongly to mu, but in kappa receptors are still the safest for analgesia
26
What happens when opioid receptor mu is bound?
- potassium channels open - membrane hyperpolarises - action potential pain is not sent - reduces neurotransmitter release - signal
27
What happens when opioid receptor kappa is bound?
- closes calcium channels - decreases calcium entry - reduces neurotransmitter release - pain message is not sent
28
Why is kappa the preferred opioid receptor to target?
- has lowered risk of dependence/addiction - no respiratory depression - reduced effect on reduction of GI motility
29
What are pure opiates?
- drugs directly extracted from opium plant without modification - e.g. morphine, thebaine, phenanthrenes, - these have a 4 ring structure
30
What are semisynthetic opiods?
- codeine - modified phenanthrenes - etorphine - oxycodone - naloxone - buprenorphine
31
What are synthetic opiates?
- pentazocine - pethidine - fentanyl - alfentanil - refmifentanil - methadone
32
What are the reasons for synthetic opiods?
- can increase potency and decrease side effects | - easier to isolate
33
What is naloxone for?
it is an antagonist at opioid receptors and is used to treat opiate overdose
34
What are the main uses for opioid drugs?
- analgesia (acute and chronic pain) - induce general anaesthetic - co induction of general anaesthesia - palliative care - antitussive (cough suppressant)
35
What are the three common agonists of mu receptors?
morphine, alfentanil, remifentanil
36
How do the three agonists of mu receptors differ ?
- their onset of action is different. - morphine is the slowest and alfentanil is the fastest - their duration of action is also different. - morphine lasts the longest while remifentail lasts the shortest - they are used for different purposes - remifentanil can be used as a controlled release drug
37
What are the side effects of opioids?
- the different receptors on different organs will have different effects - some side effects include respiratory depression, constipation, nausea, sedation
38
What is causes tolerance of opioids?
- mechanism uncertain but involves uncoupling of receptors from the G protein system - could also be due to down regulation of receptors and the upregulation of adenylate cyclase
39
Why do some opioid drugs cause dependence?
- depdence occurs when the upregulation of adenylate cylase is suddenly opposed. - the excessive production of cAMP will cause withdrawal symptoms
40
What are the two main analogues of morphine?
codeine and heroin
41
What is codeine?
- use for moderate pain - in cough formulations as an antitussive - also used to treat diarrhoea - 30-60mg enough for painrelief - 15-30mg enough for cough suppressant
42
What is heroin?
- analogue of morphine with activity 2x that of morphine - has medicinal purposes (terminal patients) - polar groups in heroin are hidden so it crosses the bbb much more easily - side effects include euphoria, addiction,m tolerance
43
How does heroin cause euphoria?
- when it crosses the bbb, it activates and releases morphine - morphine binds to the delta receptor and inhibits the effect and production of GABA - Dopamine and its effects are no longer inhibited - there is more dopamine released causing euphoria
44
What are the withdrawal symptoms of heroin?
- different between patients - drug seeking behaviour - lacrimation - rhinorrhea - yawning - sweating - restlessness - mydriasis - tremors - nausea - tachycardia - cramps/spasms - general CNS hyper-excitability - potential CV collapse
45
What is tramadol?
- purely synthetic opioid drug - has multifunctions: 1. full mu receptor agonist effect similar to morphine 2. inhibits reuptake of serotonin and enhances its release in inhibitory descending pathways - pretty good pain management effects - available in oral and IV (70% bioavailabiltiy) - no significant CV or respiratory effects with low tolerance and abuse potential
46
What is paracetamol?
- most commonly used drug in NZ - actual mechanism not understood but several hypothesis: 1. inhibits COX, selective for cox 2 to reduce side effects. has antipyretic effect 2. increases serotonin in descending pathways 3. modulation of neurotransmission in pain pathways in dorsal horn - can be oral or IV (oral bioavailability is 80%) - peak plasma levels after oral dose usually achieved within 30-60minutes - oral dose is 20-25mg/kg - pretty safe in pregnancy - mainly metabolised in liver
47
What is significant about paracetamol toxicity?
- rare but still severe and fatal - can cause skin disorders like stevens johnson's syndrome - minimal toxic dose causes liver damage (7.5-10g of paracetamol - about 20 tablets) - for children this is 150-200mg/kg - often seen in suicide attempts
48
What are the 3 different stages of toxicity responses to paracetamol toxicity?
1. nausea/vomiting and malaise 2. upper right quadrant abdominal pain, nausea, vomiting, tachycardia, hypotension 3. hepatic necrosis and dysfunction, kidney dysfunction