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NSB! > Analgesics and Sedative drugs > Flashcards

Analgesics and Sedative drugs Flashcards

1
Q

What does analgesia mean?

A
  • group of drugs that relieve pain
  • able to manipulate physiological mechanism of pain
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2
Q

Should all patients have the same pain management plan?

A
  • no
  • should be personalised
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3
Q

The WHO have created a analgesic ladder, what is this?

A
  • framework for pain management
  • not a rigid protocol but used to guide
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4
Q

The analgesic ladder has 3 main principles to remember:

1 - by the mouth
2 - by the clock
3 - by the ladder

What does the principle by the clock refer to?

A
  • purpose is to maintain freedom from pain
  • drugs administered around the clock
  • drugs administered on a scheduled basis
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5
Q

The analgesic ladder has 3 main principles to remember:

1 - by the mouth
2 - by the clock
3 - by the ladder

What does the principle by the mouth refer to?

A
  • oral administration is the preferred route
  • ease of access in clinical settings
  • administration of drug should be based on least invasive to most invasive
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6
Q

The analgesic ladder has 3 main principles to remember:

1 - by the mouth
2 - by the clock
3 - by the ladder

What does the principle by the ladder refer to?

A
  • if pain occurs drugs should be administered in the following order:

1 - non-opiods (NSAIDS and paracetamol)
2 - mild opiods (codeine or tramadol)
3 - strong opiods (morphine or hydromorphone)

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7
Q

Pain can be assessed using unidimensional or multidimensional tools. What are these?

A
  • unidimensional = measuring the quantity of one dimension of the pain experience
  • multidimensional = measuring a combination of dimensions
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8
Q

What does the acronym prn stand for?

1 - preferred route needs
2 - preferred route required
3 - prescribed as needed
4 - prescribed at a specific time

A

3 - prescribed as needed

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9
Q

What are non-anti-inflammatory drugs (NSAIDs)?

A
  • class of drugs that are non steroidal
  • used to treat pain peripherally and centrally
  • target COX-1 and COX-II
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10
Q

What are the 3 effect NSAIDs commonly used to treat?

A
  • pain
  • inflammation
  • fever
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11
Q

NSAIDs are commonly used to treat pain, inflammation and fever. What do all 3 of these things have in common? (as the cause)

A
  • all caused by an increase in prostaglandins
  • prostaglandins are created by COX-I and COX-II
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12
Q

What are prostaglandins?

A
  • active lipid compounds produced by most cells
  • involved in pain, inflammation and fever
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13
Q

Prostaglandins are not present automatically, but are created by the body in response to inflammation. Immune cells use an enzyme called phospholipase A2 to create arachidonic acid, which is a substrate for cyclooxygenase (COX). How is this achieved?

A
  • phospholipase A2 converts membrane phospholipids into a 20-carbon polyunsaturated fatty acid, called arachidonic acid.
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14
Q

Prostaglandins are not present automatically, but are created by the body in response to inflammation. Immune cells use an enzyme called phospholipase A2 to create arachidonic acid, which is a substrate for cyclooxygenase (COX). Phospholipase A2 converts membrane phospholipids into a 20-carbon polyunsaturated fatty acid, called arachidonic acid. What is arachidonic acid then able to do?

A
  • provide a substrate for COX-1 and COX-2
  • COX-1 = constitutive (always switched on)
  • COX-2 = inducible (needs to be turned on)
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15
Q

COX-1 and 2 are able to produce a compound that is involved in inflammation, what is this compound?

A
  • prostaglandin
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16
Q

COX-1 and 2 are able to produce prostaglandin, a compound that is involved in inflammation. What are the 4 mechanisms that prostaglandin is able to cause inflammation, pain and fever?

A

1 - induce vasodilation and increase vessel permeability
2 - attract immune cells
3 - sensitise nociceptors to pain (pain receptors)
4 - stimulate the hypothalamus to increase temperature

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17
Q

What is the main mechanism of action of NSAIDs?

A
  • competitively inhibit COX (both COX-1 and COX-2)
  • causes a reduction in prostaglandin
  • this is reversible
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18
Q

Prostaglandins are able to sensitise nociceptors to thermal, mechanical and chemical (all stimuli for nociceptors) stimuli, all relating to pain and increase pain sensation. How are they able to do this?

1 - allow K+ to leave the cell and Na+ influxes into the cell
2 - blocks K+ entering the cell
3 - blocks K+ leaving the cell and increases Na+ and Ca2+ entering the cell
4 - increases Na+ and Ca2+ entering the cell

A

3 - blocks K+ leaving the cell and increases Na+ and Ca2+ entering the cell
- essentially mean that depolarisation will continually occur

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19
Q

Which drug is a NSAIDs able to irreversibly inhibit COX?

1 - naproxen
2 - aspirin
3 - ibuprofen
4 - paracetamol

A

2 - aspirin
- has anti-platelet formation, so reduces blood coagulation
- reduces the risk of thrombosis (thins the blood)

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20
Q

NSAIDs are able to have 3 effects, what are they?

A
  • analgesis (pain relief)
  • anti-inflammatory
  • antipyretic (an-tee-pie-ret-ik) (reduce fever)
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21
Q

What does antipyretic mean?

A
  • anti = against
  • pyretic = feverish
  • so means to stop fevers
  • pronounced as an-tee-pie-ret-ik
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22
Q

Arachidonic acid is the precursor for what?

A
  • prostaglandins
  • COX-1 and COX-2 use arachidonic acid as a substrate for prostaglandins
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23
Q

COX-1 is considered to be constitutive, but what does that mean?

A
  • that it is always active
  • COX-1 has a number of physiological effects
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24
Q

COX-1 is considered to be constitutive, meaning that it is always active. It has positive physiological effects in the stomach. What does it do?

A
  • COX-1 derived prostaglandins are responsible for gastric mucosal protection
  • vasodilation, stimulation, and secretion of gastroduodenal mucus and bicarbonate
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25
Q

COX-1 is considered to be constitutive, meaning that it is always active. It has positive physiological effects in renal homeostasis. What does it do?

A
  • COX-1 derived prostaglandins are potent local vasodilators
  • important for maintaining renal blood flow by attenuating reducing vasoconstriction of the afferent arteriole
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26
Q

COX-2 is primarily considered to be inducible (does have some constitutive activity). What does this mean?

A
  • it needs to be activated
  • activated by immune cells (macrophages) and cytokines TNF-a which are common in inflammation and tissue injury
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27
Q

COX-2 is primarily considered to be inducible (does have some constitutive activity) meaning it needs to be activated. What are the negative effect of COX-2 derived prostaglandins?

A
  • pain, inflammation and fever
28
Q

COX-1 is considered to be constitutive, meaning that it is always active. COX-1 derived prostaglandins are responsible for gastric mucosal protection through vasodilation, stimulation, and secretion of gastroduodenal mucus and bicarbonate. Therefore, if someone takes a lot of NSAIDs on a regular basis, what could the side effects in the stomach be?

A
  • peptic ulcers
  • bleeding
  • perforations
29
Q

COX-1 is considered to be constitutive, meaning that it is always active. COX-1 derived prostaglandins are responsible for maintaining renal blood flow by attenuating vasoconstriction of the afferent arteriole. If someone takes a lot of NSAIDs, what could the adverse events on renal function be?

A
  • renal failure or chronic kidney disease
  • reduced estimated glomerulus filtration rate
  • fluid retention leading top heart failure
30
Q

NSAIDs inhibit all COX enzymes, but does inhibition of COX-1 or COX-2 cause more adverse events?

A
  • inhibitions of COX-1
31
Q

Is paracetamol an NSAID?

A
  • no
32
Q

Paracetamol is not an NSAID, why is this?

A
  • it is not anti-inflammatory
  • anti-pyretic and analgesic only
  • also acts predominantly on CNS
33
Q

Paracetamol is not an NSAID because it does not possess anti-inflammatory properties and works predominantly on the CNS. What 2 beneficial effects does paracetamol have on the body?

A

1 - analgesic (relieves pain)
2 - antipyretic (anti-fever)

34
Q

Paracetamol is metabolised by one organ in the body, which organ is this?

A
  • liver
35
Q

Paracetamol is metabolised by the liver, what can happen with a paracetamol overdose?

A
  • hepatic necrosis
  • liver failure
36
Q

Although the main mechanism of action of paracetamol is not known, what is the main suspected mechanism?

A
  • inhibition of COX in CNS
37
Q

Does paracetamol have adverse events on the stomach (mucosal lining) and platelets?

A
  • no
38
Q

What is the drug class that is used to treat moderate to severe pain?

1 - opioids
2 - NSAIDs
3 - paracetamol
4 - steroids

A

1 - opioids
- codeine would be first drug of choice
- steps 2 and 3 of the analgesic ladder

39
Q

Opioids are used for moderate to severe pain, so levels 2 and 3 on the analgesic ladder. How do these drugs have an effect on the body?

1 - moderate opioid receptors
2 - antagonist of opioid receptors
3 - agonist of opioid receptors

A

1 - moderate opioid receptors
- suspected to be combination of agonist and antagonist
- works through G protein coupled receptors (Gai)

40
Q

There are 3 types of opioid receptors, what are they?

1 = GPCR, d (delta), k (kappa)
2 = u (mu), GPCR, k (kappa)
3 = u (mu), d (delta), k (kappa)
4 = u (mu), d (delta), GPCR

A

3 = u (mu), d (delta), k (kappa)

41
Q

Opioid receptors are G protein coupled receptors. Specifically which G protein coupled receptor do they bind with?

1 - Gas
2 - Gaq
3 - Gai

A

3 - Gai

42
Q

What is the normal pathway for a Gai G protein coupled receptor?

A
  • inhibition
  • inhibit adenylate cyclase (reduces cAMP)
  • reduces overal phosphorylation (protein kinase A)
43
Q

The normal pathway for a Gai G protein coupled receptor is through inhibiting adenylate cyclase (reduces cAMP) and reducing overall phosphorylation. In addition to this once opioids bind to opioid receptors they are able to do 2 other key things that reduce the potential of depolarisation, what are they?

1 - increase Na+ and Ca2+ influx on pre-synapse reducing neurotransmitter release
2 - decrease Na+ and Ca2+ influx on pre-synapse reducing neurotransmitter release
3 - increase K+ efflux out of post-synapse cell and reduce Ca2+ influx on pre-synapse reducing neurotransmitter release
4 - increase K+ and Ca2+ influx on pre-synapse reducing neurotransmitter release

A

3 - increase K+ efflux out of post-synapse cell and reduce Ca2+ influx on pre-synapse reducing neurotransmitter release

44
Q

What is the weak opioid drug that we need to know as a core drug?

1 - Diazepam
2 - Zopiclone
3 - Codeine
4 - Morphine

A

3 - codeine

45
Q

What is the strong opioid drug that we need to know as a core drug?

1 - Diazepam
2 - Zopiclone
3 - Codeine
4 - Morphine

A

4 - morphine

46
Q

Codeine is a weak opioid drug and has a ceiling dose. What does a ceiling dose mean?

A
  • patients can continue to experience pain despite taking the maximum dosage of codeine
  • even an increase in dosage cannot reduce pain any further
  • patient has reached a ceiling effect of the effectiveness of codeine
47
Q

Codeine is metabolised where in the body, and what is it metabolised into?

1 - liver and into morphine
2 - kidney and into morphine
3 - not metabolised
4 - spleen and into morphine

A

1 - liver and into morphine

48
Q

Codeine is metabolised by the liver into morphine. Is codeine effective for everyone?

A
  • no
  • 10% caucasians lack active enzymes required
  • may be ultra-rapid metaboliser or poor metaboliser
49
Q

Are the effects of morphine the same for everyone?

A
  • no
  • consider age, genetics, etc..
  • can become tolerant where the medication no longer works as well as previously (may be due to receptor desensitisation)
50
Q

What is morphine metabolised into?

A
  • active metabolites
51
Q

Where is morphine excreted from?

A
  • kidneys
  • important to consider patients eGFR
52
Q

Does morphine have a ceiling effect?

A
  • no
53
Q

There are a number of adverse effects of opioids. What are the key 2 that we need to be aware of?

1 - anxiety and nausea/vomiting
2 - constipation and nausea/vomiting
3 - respiratory distress and nausea/vomiting
2 - constipation and anxiety

A

2 - constipation and nausea/vomiting
- constipation - MAIN ADVERSE EFFECT (however, can be used in patients with diarrhoea)
- nausea and vomiting

54
Q

Opioids have adverse events, so often need to be taken alongside other medication. Constipation is a side effect of opioids, so what is often prescribed alongside opioid use?

A
  • laxatives or faecal softeners
55
Q

Opioids have adverse events, so often need to be taken alongside other medication. Nausea and vomiting are side effects of opioids, so what is often prescribed alongside opioid use?

A
  • stool softners for constipation
  • antiemetics (anti sickness drugs)
  • emetic is greek for vomit
56
Q

What does tolerance refer to with drug administration?

1 - patient no longer responds to a drug in the way they did at first
2 - patient feels as though they cannot function normally without the medication
3 - patients dose can be lowered as no significant symptoms anymore
4 - drug has harmful effects patient is aware of but still takes the drug

A

1 - patient no longer responds to a drug in the way they did at first
- could be due to desensitisation

57
Q

What is the most common adverse event of opioids?

A
  • constipation
  • 50-90% of patients
58
Q

Constipation is an adverse event of opioid use. Why does this occur?

A
  • u (mew) receptors in GI tract
  • opioids inhibit peristaltic contractions
59
Q

What is the difference between addiction and dependance?

A
  • addiction = drug is harmful but patient unable to stop using a drug despite negative effects
  • dependance = the body has become use to a drug, but not the brain
60
Q

Opioids can become toxic to the body, and although the initial response is to stop the drug, reduce the dose or change the opioid, this does not always work. What is the core opioid antagonist that we need to be aware of?

1 - citalopram
2 - gabapentin
3 - naloxone
4 - codeine

A

3 - naloxone
- binds with opioid receptors

61
Q

Sedation is generally characterised as an adverse effect of opioids. However, is it always bad?

A
  • no in critically ill patients who cannot sleep, opioids may be beneficial
  • help sleep, calm and relax the patient
62
Q

Benzodiazepines are a group of drugs that are used for their anxiolytic (anti-anxiety). What is the core drug we need to be aware of?

1 - diazepam
2 - chlorpromazine
3 - haloperidol
4 - clozapine

A

1 - diazepam
- all this group of drugs end in pam

63
Q

Diazepam is one of the denzodiazepines drugs are a group of drugs that are used for their anxiolytic (anti-anxiety) effects. What receptor does diazepam bind with?

1 - NMDA
2 - AMPA
3 - dopamine receptors
4 - GABA A receptors

A

4 - GABA A receptors
- binds with subunit a on GABA A receptors
- allosteric effect as binds to different place than GABA
- increases effects of GABA (essentially no depolarisation)

64
Q

Diazepam is one of the denzodiazepines drugs are a group of drugs that are used for their anxiolytic (anti-anxiety). It is able to bind with subunit a on GABA-A receptors, which is different to the binding site of GABA (allosteric binding). What does binding with the a subunit of the GABA receptors cause the cell to then do?

1 - inhibits effects of GABA
2 - increases the effects of GABA
3 - reduces GABA breakdown
4 - increase GABA breakdown

A

2 - increases the effects of GABA
- causes an influx of Cl- and hyperpolarises
- reduces potential of depolarisation
- reduces activity of neurons causing anxiety
- essentially increases the effect of normal GABA

65
Q

Z-drugs or non-benzodiazepines have a similar affect as benzodiazepines, in as much as that they possess anti-anxiety effects. What is the mechanism of action of this drug?

A
  • binds with subunit a on GABA receptors (allosteric effect as binds to different place to GABA)
  • causes an influx of Cl- and hyperpolarises
  • reduces potential of depolarisation
  • reduces activity of neurons causing anxiety
66
Q

Benzodiazepines (diazepam) and Z-drugs (zopiclone) elicit anti-anxiety effects. Are these 2 groups of drugs agonists of GABA?

A
  • no
  • they are modulators, as they still require GABA to be effective
  • BUT can increase the effects of normal GABA
67
Q

Benzodiazepines (diazepam) and Z-drugs (zopiclone) elicit anti-anxiety effects. There are a wide range of side effects of these drugs, what is the most common side effect of Z-drugs?

1 - constipation
2 - nausea and vomitting
3 - dry mouth
4 - neutropenia

A

3 - dry mouth

NSB! (53 decks)

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