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4th yr- CMS- drugs and medication > Opioid drugs > Flashcards

Opioid drugs Flashcards

1
Q

What are opioids

A

They are substances which act at opioid receptors in rtes central and peripheral nervous system

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2
Q

Name the 3 families of naturally occurring opioids

A
  1. Beta-endorphins
  2. Enkephalins
  3. Dynorphins
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3
Q

What are opioids also known as

A

neuropeptides” aka “endogenous endorphins”

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4
Q

When were opioids discovered

A

in the 1970s

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5
Q

What properties do endorphins have

A

They have morphine like properties

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6
Q

What are endorphins responsible for

A

Responsible fro the feelings of euphoria elicited from physical or emotional pleasure, pleasure or stress

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7
Q

What are endorphins described as

A

Natural painkillers that are very potent

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8
Q

What roles do opioids play

A

Selective roles in:

  1. Pain modulation
  2. Neurotransmission
  3. Stress responses
  4. Reward processing
  5. Autonomic function regulation
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9
Q

In which system do opioid act in

A

CNS and PNS at the pre and post synaptic membranes to trigger their responses

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10
Q

Name the 3 families of opioid receptors

A
  1. Mu
  2. Delta
  3. Kappa
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11
Q

Where are Mu receptor found

A

Found in the brainstem and media thalamus

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12
Q

What do Mu receptors control

A
  1. Super spinal analgesia,
  2. respiratory depression
  3. Euphoria
  4. Sedation
  5. Decreased GIT motility
  6. Physical dependence
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13
Q

Where are delta receptors found

A

In the brain

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14
Q

Where are kappa receptors found

A

In the limbic system, diencephalon, brainstem, spinal cord

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15
Q

What are Kappa receptors responsible for

A
  1. Spinal analgesia
  2. Sedation
  3. Dyspnoae
  4. Dependence
  5. Dysphoral
  6. Respiratory depression
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16
Q

Describe all opioid receptors

A

They are G protein couples

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17
Q

What do opioid receptors cause

A

cAMP inhibition at intracellular targets which then act as second messenger to activate protein kinases and affect gene transcription

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18
Q

How do opioid receptors act on presynaptic membranes of A delta and C fibres neurones

A

They will inhibit voltage gated calcium channels decreasing cAMP levels blocking the release of pain transmitters like glutamate, substance p and calcitonin with the end result being analgesia

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19
Q

Name the 4 chemical classes of opioids

A
  1. Phenanthrenes
  2. Benzomorphans
  3. Phenylpiperidines
  4. Diphenylheptanes
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20
Q

Give examples of Phenanthrenes

A
  1. Morphine
  2. Codeine
  3. hydromorphone
  4. Oxycodone
  5. buprenorphine
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21
Q

Describe morphine

A

Is a hydroxyl containing opioid which has a higher incidence of nausea and hallucinations

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22
Q

Descrive codeine

A

Is a hydroxyl containing opioid which has a higher incidence of nausea and hallucinations

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23
Q

Give examples of Benzomorphans

A

Pentazocine

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24
Q

Give examples of Phenylpiperidines

A
  1. fentanyl,
  2. alfentanil,
  3. sufentanil,
  4. meperidine
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25
Give examples of Diphenylheptanes
propoxyphene and methadone
26
Name the one opioid drug that is unique
Tramadol
27
Why is Tramadol unique
It doesn't fit into the standard opioid classification system
28
Describe Tramadol
it is an atypical opioid as it is a partial mu agonist as well as having central GABAergic, catecholaminergic and serotonergic activities
29
How can we further classify opioids after chemical class
1. Agonists 2. Partial agonist 3. Antagonist
30
What are agonists
They have affinity and efficacy
31
Give examples of agonist opioid drugs
morphine, fentanyl, methadone
32
What are partial agonists
They have affinity but only partial efficacy
33
Give examples of partial agonist opioid drugs
buprenorphine
34
What are antagonist
Have affinity but no efficacy
35
Give examples of antagonist opioid drugs
naloxone and naltrexone
36
What do we mean by affinity
Strength of the drugs bond to the receptor
37
What do we mean by efficacy
The strength of action is affected by the binding at this receptor
38
Where does opioid metabolism occur
In the liver
39
Which enzyme is in charge of opioid metabolism
glucuronidation or P450
40
What can effect the degree of opioid metabolism
1. Genetic makeup 2. Gender 3. Age 4. Diet 5. Disease status 6. Concurrent use of medications
41
What does the kidney do in terms of opioids
Excretes opioids but does not metabolise them
42
What can degree of sensitivity of opioids be controlled by
Polymorphic gene expression for Mu receptors
43
How do polymorphic gene expression of mu receptors affect degree of sensitivity of opioids
They will influence analgesic effects dependence and tolerance
44
What do the metabolites of opioids control
The undesirable effects seen
45
What does morphine treat
Moderatley severe to severe pain
46
How much of the morphine crosses the blood brain barrier
Less than half due to poor lipid solubility, rapid glucuronidation and ionisation of the drug at physiological pH
47
What is morphine metabolise by
demethylation AND glucuronidation
48
What are morphine side effect due to
Histamine release causing bronchospasm and hypotension and direct respiratory drive inhibition
49
What can morphine reduce
Peripheral sympathetic tone leading to venous pooling and orthostatic hypotension
50
What can morphine cause
1. Spasms of digestive tract leading to decreased motility and resultant constipation as well as bladder spams 2. Nausea and vomiting
51
What is Codeine
A weak opioid analgesic has partial agonist activity at Mu receptors
52
What is the half life of codeine
2.5 - 3 hours
53
Codeine is a ______ drug
Pro drug
54
What do we mean by pro drug
They just undergo some metabolism to be effective
55
What is codeine metabolised into
Morphine
56
Why is codeine a weak opioid analgesics
It is metabolised into morphine
57
Is codeine Susceptible to drug drug interaction
Yes due to its metabolism but the CYP450 chain
58
What is methadone
A synthetic Mu receptor agonist and NMDA antagonist
59
What is methadone used to treat
Heroin addicts but can we useful to treat neuropathic pain
60
What can methadone cause
Potentially serious cardiac arrhythmia and hypokalaemia and hypomagnesiumaemia
61
What can methadone interact with
SSRIs and TCAs as well as with venlafaxine (antidepressant/ antipsychotic drugs)
62
What do we mean by tolerance
having to take progressively higher doses of a drug in order to maintain the same effects as the initial dose
63
What do we mean by dependence
Having to continue taking the drug in order to prevent intolerable side effect produced but sudden cessation of ingestion
64
What do we mean by addiction
Is the compulsion to continue taking a substance and despite negative consequence, they are unable to stop doing so
65
What is the problem with opioid drugs and analgesia
Due to their pharmacology opioid drugs do not have an upper ceiling to how much analgesia they can achieve meaning a patient can build up tolerance
66
What is the problem with tolerance in opioid drugs
Increasingly higher and higher doses of opioid will need to be taken This increases the risk of adverse side effects
67
What are the side effects of opioid withdrawal
1. Cravings 2. Restlessness and irritability 3. Increased sensitivity to pain 4. nausea, 5. abdominal cramps, 6. myalgia, 7. dysphoria, 8. insomnia and anxiety.
68
What are the clinical signs of opioids withdrawal
1. Pupillary dilatation, 2. sweating, 3. piloerection, 4. tachycardia, 5. vomiting and diarrhoea, 6. hypertension, 7. yawning, 8. fever, 9. rhinorrhoea.

4th yr- CMS- drugs and medication (4 decks)

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