Analgesics - Opioids Flashcards
Which 2 of the following drugs are part of stage 1 of the analgesic ladder for mild pain between 1-3?
1 - codeine
2 - tramadol
3 - paracetamol
4 - NSAIDs
3 - paracetamol
4 - NSAIDs
Which 2 of the following drugs are part of stage 2 of the analgesic ladder for moderate pain between 4-6?
1 - codeine
2 - tramadol
3 - paracetamol
4 - NSAIDs
1 - codeine
2 - tramadol
Which of the following is on stage 3 of the analgesic ladder for severe pain 7-10?
1 - codeine
2 - morphine
3 - paracetamol
4 - NSAIDs
2 - morphine
NSAIDS have 3 properties: analgesic (pain-killing), anti-inflammatory and antipyretic (fever-reducing) properties. Which of the following is NOT classed as a NSAIDs?
1 - aspirin
2 - paracetamol
3 - ibuprofen
4 - diclofenac
2 - paracetamol
- analgesic and antipyretic only
- NOT anti-inflammatory
A 22-year-old man presents with complaints of ankle pain and swelling from a sports injury oneday prior. X-rays are negative for a fracture and he is directed to rest the joint and allow it to heal. Which drug will provide LESS benefit in alleviating pain and inflammation of the swollen joint?
A. Celecoxib
B. Naproxen
C. Diclofenac
D. Acetaminophen
D. Acetaminophen
- more commonly known as paracetamol
- other 3 drugs are NSAIDS
A patient with which of the following conditions is the most appropriate candidate for use of acetaminophen to manage chronic pain associated with osteoarthritis?
A. Chronic malnutrition
B. Obesity
C. Alcoholism
D. Viral hepatitis
B. Obesity
- other conditions increase risk of acetaminophen (paracetamol) related hepatotoxicity.
- acetaminophen depletes glutathione concentrations in the liver and NAPQI builds up.
- low levels of glutathione are common in malnutrition, again increasing levels of NAPQI
- alcoholism depletes endogenous glutathione
- viral hepatitis damages the liver, and could reduce levels of glutathione
Among NSAIDs, aspirin is unique because it:
(A) Irreversibly inhibits its target enzyme
(B) Prevents episodes of gouty arthritis with long-term use
(C) Reduces fever
(D) Reduces the risk of colon cancer
(E) Selectively inhibits the COX-2 enzyme
(A) Irreversibly inhibits its target enzyme
- non-selective irreversibly inhibition of cyclooxygenase 1 and 2
Which of the following is an analgesic and antipyretic drug that lacks an anti-inflammatory action?
(A) Acetaminophen
(B) Celecoxib
(C) Colchicine
(D) Indomethacin
(E) Probenecid
(A) Acetaminophen
An 18-month-old boy dies from an accidental overdose of acetaminophen. Which of the following is the most likely cause of this patient’s death?
(A) Arrhythmia
(B) Haemorrhagic stroke
(C) Liver failure
(D) Noncardiogenic pulmonary edema
(E) Ventilatory failure
(C) Liver failure
- liver failure as a result of its conversion by hepatic cytochrome P450 enzymes to a highly reactive metabolite NAPQI
A 54-year-old woman presented with signs and symptoms consistent with an early stage of rheumatoid arthritis. The decision was made to initiate NSAID therapy. Which of the following patient characteristics is the most compelling reason for avoiding celecoxib (selective COX-2 inhibitor) in the treatment of her arthritis?
(A) History of alcohol abuse
(B) History of gout
(C) History of myocardial infarction
(D) History of osteoporosis
(E) History of peptic ulcer disease
(C) History of myocardial infarction
- COX-2-selective inhibitor
- does not inhibit Thromboxane A2
- increased risk of arterial thrombotic events.
- history of MI would be a compelling reason to avoid a COX-2 inhibitor
Which of the following statements is correct regarding morphine?
1 - Morphine is the most lipophilic opioid.
2 - Morphine is metabolised through CYP2D6 and CYP3A4 and has numerous drug interactions.
3 - Morphine has active metabolites that can accumulate in renal impairment, leading to clinically relevant effects.
4 - Morphine can cause opioid-induced constipation upon initiation of opioid therapy, but tolerance occurs after 1 to 2weeks of opioid exposure.
3 - Morphine has active metabolites that can accumulate in renal impairment, leading to clinically relevant effects.
- Morphine has two active metabolites M3G and M6G, which are renally eliminated.
Which of the following is NOT an core opioid that we need to be aware of?
1 - Morphine sulphate
2 - Oxycodone
3 - Diclofenac
4 - Codeine phosphate
5 - Tramadol
6 - Methadone
3 - Diclofenac
- this is an NSAID
The 5 core opioid that we need to be aware of are below. Which are strong and which are weak/moderate?
1 - Morphine sulphate
2 - Oxycodone
3 - Codeine phosphate
5 - Tramadol
6 - Methadone
- strong = morphine sulphate, oxycodone and methadone
- weak/moderate = codeine phosphate and tramadol
Of the 5 core opioid that we need to be aware of are below, which are prodrugs that need to be metabolised in the liver?
1 - Morphine sulphate
2 - Oxycodone
3 - Codeine phosphate
5 - Tramadol
6 - Methadone
3 - Codeine phosphate
5 - Tramadol
- metabolised to become morphine or dihydromorphine
Which of the following is NOT an opioid receptor?
1 - Mu
2 - Kappa
3 - Delta
4 - Alpha
4 - Alpha
Which endogenous opioid (made in the body) can bind with opioid receptors which then inhibits GABA release and allows neurotransmitters such as dopamine, serotonin and noradrenaline to be released?
1 - endorphins
2 - methadone
3 - heroin
4 - fentanyl
1 - endorphins
Once opioid receptors are activated this inhibits GABA in the brain at specific locations. Those locations are pain processing regions of the brain. Which 2 of the following neurotransmitters are released in the pain processing regions and thus reduce sensitivity to pain?
1 - dopamine
2 - serotonin
3 - noradrenaline
4 - GABA
2 - serotonin
3 - noradrenaline
Once opioid receptors are activated this inhibits GABA in the brain at specific locations. This location can be in the reward pathways creating a calming effect. Which neurotransmitters is released in the reward pathway regions of the brain?
1 - dopamine
2 - serotonin
3 - noradrenaline
4 - GABA
1 - dopamine
Opioids are indicted in acute pain, in all of the following EXCEPT which one?
1 - trauma
2 - surgery
3 - acute coronary syndrome
4 - acute pulmonary oedema
4 - acute pulmonary oedema
Opioids are indicted in chronic pain, but only when what has happened?
1 - patient is elderly
2 - patient has multiple comorbidities
3 - milder analgesics have failed to alleviate pain
4 - patient requests opioids
3 - milder analgesics have failed to alleviate pain
- if pain management fails we move up the ladder
Opioids are indicated for which of the following?
1 - pain following major surgery
2 - breathlessness in palliative care
3 - broken bone
4 - GIT obstruction
2 - breathlessness in palliative care
Opioids are indicated for acute pulmonary oedema alongside 3 other medications. Which one is NOT indicated here?
1 - oxygen
2 - furosemide
3 - tramadol
4 - nitrates
3 - tramadol
Specifically in pain processing regions, which opioid receptor do opioids bind with to reduce pain?
1 - alpha
2 - delta
3 - mu
4 - kappa
3 - mu
- these are GPCR
In addition to alleviating pain, opioids can have a significant affect on other factors. Which of the following actions do opioids perform?
1 - inhibit respiratory drive and breathlessness
2 - attenuate response to hypoxia and hypercapnia
3 - reduce pain and associated anxiety
4 - reduce sympathetic drive
5 - reduce cardiac workload and O2 demand (acute coronary syndrome)
6 - all of the above
6 - all of the above
Opioids can have which of the following adverse events in the brain or brain stem?
1 - respiratory depression
2 - neurological depression
3 - activate chemoreceptor trigger zone and vomiting centre, inducing nausea and vomiting
4 - pupillary constriction due to stimulation of the Edinger-Westphal nucleus
5 - all of the above
5 - all of the above
Opioids have a high risk of patients becoming dependent on them. Which medication can be given to reduce withdrawal symptoms?
1 - alprazolam
2 - methadone
3 - amphetamines
4 - methylphenidate
2 - methadone
- weak opioid with short half life
- good for withdrawal from morphine
- all other drugs here are also addictive
In addition to locations in the brain or brain stem, which of the following are adverse events from opioids in the peripheral tissues?
1 - constipation (u receptors)
2 - itching
3 - hyperalgesia (increased sensitivity to pain)
4 - all of the above
4 - all of the above
Which of the following conditions should the doses of opioids be reduced in?
1 - hepatic failure
2 - renal impairment
3 - older patients
4 - all of the above
4 - all of the above
- liver and renal are responsible for elimination, so if not cleared they can become toxic
- older patients livers and kidneys do not functional as well
Should opioids ever be given to patients with respiratory failure?
- generally no
- unless under direct supervision
Opioids should not be prescribed alongside the following medications: anti-psychotics, benzodiazepines and tricyclic antidepressants. Why is this?
1 - increase risk of dependence
2 - extrapyramidal effects
3 - increase risk of toxicity
4 - accentuate sedation of opioids
4 - accentuate sedation of opioids
- if used they must be under direct supervision
What other medication should be prescribed alongside opioids?
1 - laxatives
2 - anticholinergics
3 - Beta blockers
4 - PPIs
1 - laxatives
- senna is most commonly used
- due to risk of constipation
