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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
Q

Give examples of Diphenylheptanes

A

propoxyphene and methadone

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26
Q

Name the one opioid drug that is unique

A

Tramadol

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27
Q

Why is Tramadol unique

A

It doesn’t fit into the standard opioid classification system

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28
Q

Describe Tramadol

A

it is an atypical opioid as it is a partial mu agonist as well as having central GABAergic, catecholaminergic and serotonergic activities

29
Q

How can we further classify opioids after chemical class

A
  1. Agonists
  2. Partial agonist
  3. Antagonist
30
Q

What are agonists

A

They have affinity and efficacy

31
Q

Give examples of agonist opioid drugs

A

morphine,
fentanyl,
methadone

32
Q

What are partial agonists

A

They have affinity but only partial efficacy

33
Q

Give examples of partial agonist opioid drugs

A

buprenorphine

34
Q

What are antagonist

A

Have affinity but no efficacy

35
Q

Give examples of antagonist opioid drugs

A

naloxone and naltrexone

36
Q

What do we mean by affinity

A

Strength of the drugs bond to the receptor

37
Q

What do we mean by efficacy

A

The strength of action is affected by the binding at this receptor

38
Q

Where does opioid metabolism occur

A

In the liver

39
Q

Which enzyme is in charge of opioid metabolism

A

glucuronidation or P450

40
Q

What can effect the degree of opioid metabolism

A
  1. Genetic makeup
  2. Gender
  3. Age
  4. Diet
  5. Disease status
  6. Concurrent use of medications
41
Q

What does the kidney do in terms of opioids

A

Excretes opioids but does not metabolise them

42
Q

What can degree of sensitivity of opioids be controlled by

A

Polymorphic gene expression for Mu receptors

43
Q

How do polymorphic gene expression of mu receptors affect degree of sensitivity of opioids

A

They will influence analgesic effects dependence and tolerance

44
Q

What do the metabolites of opioids control

A

The undesirable effects seen

45
Q

What does morphine treat

A

Moderatley severe to severe pain

46
Q

How much of the morphine crosses the blood brain barrier

A

Less than half due to poor lipid solubility, rapid glucuronidation and ionisation of the drug at physiological pH

47
Q

What is morphine metabolise by

A

demethylation AND glucuronidation

48
Q

What are morphine side effect due to

A

Histamine release causing bronchospasm and hypotension and direct respiratory drive inhibition

49
Q

What can morphine reduce

A

Peripheral sympathetic tone leading to venous pooling and orthostatic hypotension

50
Q

What can morphine cause

A
  1. Spasms of digestive tract leading to decreased motility and resultant constipation as well as bladder spams
  2. Nausea and vomiting
51
Q

What is Codeine

A

A weak opioid analgesic has partial agonist activity at Mu receptors

52
Q

What is the half life of codeine

A

2.5 - 3 hours

53
Q

Codeine is a ______ drug

A

Pro drug

54
Q

What do we mean by pro drug

A

They just undergo some metabolism to be effective

55
Q

What is codeine metabolised into

A

Morphine

56
Q

Why is codeine a weak opioid analgesics

A

It is metabolised into morphine

57
Q

Is codeine Susceptible to drug drug interaction

A

Yes due to its metabolism but the CYP450 chain

58
Q

What is methadone

A

A synthetic Mu receptor agonist and NMDA antagonist

59
Q

What is methadone used to treat

A

Heroin addicts but can we useful to treat neuropathic pain

60
Q

What can methadone cause

A

Potentially serious cardiac arrhythmia and hypokalaemia and hypomagnesiumaemia

61
Q

What can methadone interact with

A

SSRIs and TCAs as well as with venlafaxine (antidepressant/ antipsychotic drugs)

62
Q

What do we mean by tolerance

A

having to take progressively higher doses of a drug in order to maintain the same effects as the initial dose

63
Q

What do we mean by dependence

A

Having to continue taking the drug in order to prevent intolerable side effect produced but sudden cessation of ingestion

64
Q

What do we mean by addiction

A

Is the compulsion to continue taking a substance and despite negative consequence, they are unable to stop doing so

65
Q

What is the problem with opioid drugs and analgesia

A

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
Q

What is the problem with tolerance in opioid drugs

A

Increasingly higher and higher doses of opioid will need to be taken
This increases the risk of adverse side effects

67
Q

What are the side effects of opioid withdrawal

A
  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
Q

What are the clinical signs of opioids withdrawal

A
  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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