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Pharmacology > Opioids > Flashcards

Opioids Flashcards

1
Q

What type of receptors are all opioid receptors

A

G protein coupled that. Inhibit adenylyl cyclase Gi

  • reducing Ca2+ influx
  • reducing k+ efflux
  • reducing neuronal firing and transmitter release
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2
Q

What doses are needed to control pain

A

High doses

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3
Q

What are the symptoms of acute opioid toxicity

A 
Respiratory depression 
Pinpoint pupils 
Coma 
Cyanosis
Apnea
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4
Q

Opioid toxicity treatment

A

Ventilation and opioid antagonist -naloxone i.v

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5
Q

What is morphine contraindicated in

A

In asthma and severe brain injury

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6
Q

Adverse effects of morphine

A
  • MIOSIS (pinpoint eyes) - little tolerance - patho genomic for morphine in coma
  • out of it (sedation)
  • respiratory depression - tolerance develops
  • pneumonia (antitussive) - cough suppression
  • hypotension
  • infrequency (constipation and urinary retention)
  • nausea
  • emesis
  • causes release of histamine and euphoria. Analgesic.
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7
Q

Most common cause of death with morphine

A

Respiratory depression

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8
Q

Morphine therapeutic uses

A

Analgesic, treatment of diarrhea, relief of cough (antitussive), to treat acute pulmonary edema and anaesthesia.

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9
Q

Effect of morphine on pregnant women

A

It can cross through the placenta and can cause addiction in infants and withdrawal symptoms

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10
Q

Can morphine cross BBB

A

No it can’t

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11
Q

Metabolites of morphine

A

M6G ( very potent analgesic)

M3G (Neurotoxic)

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12
Q

Which side effects is it impossible to develop tolerance against

A

MIOSIS and Constipation

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13
Q

What’s an opiate black box warning

A

Don’t give with benzodiazepines

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14
Q

What’s a naturally occurring opiate

A

Codeine

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15
Q

What is codeine used for

A

Used in mild to moderate pain

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16
Q

What is codeine converted to and why

A

Morphine to show analgesic action

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17
Q

What is codeine combined with for pain

A

Acetaminophen

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18
Q

What’s a better alternative than codeine for antitussive effects and why

A

Dectromethorphan synthetic cough depressant with much lower abuse potential

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19
Q

What is oxycodone

A

A semisynthetic analog

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20
Q

What can oxycodone be used with

A

APAP, aspirin or ibuprofen - it can be used on its own too!

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21
Q

When is hydromorphine preferred over morphine

A

In patients with renal dysfunction due to less active metabolite accumulation

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22
Q

Hydrocodone uses and what can it be combined with

A

A good antitussive also combined with NSAIDs and APAP for pain

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23
Q

What is Fentanyl related to

A

Chemically related to meperidine and is 100x more potent than morphine

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24
Q

What is fentanyl used for

A

Used in anaesthesia and pain

- can be given as a transdermal patch used in reliefing cancer pain

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25
Q

Fentanyl duration of action and uses

A

Rapid onset and short duration

  • Can be used with local anaesthetic
  • to provide analgesia for labour and post operative pain
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26
Q

When is fentanyl used as patches

A

For chronic pain (like cancer) with late offset and long duration

27
Q

Meperidine structure in comparison with morphine

A

Is it structurally unrelated to morphine

28
Q

Meperidine contraindications

A

Patients with impaired renal function

29
Q

Meperidine special unique effect

A

AntiMuscarinic effect so have increased chance of delirium and mydriasis

30
Q

What is meperidine metabolite

A

Normeperidine which is an active metabolite and is neurotoxic -> it is renally eliminated hence it is contraindicated in kidney failure

31
Q

Meperidine clinical uses

A

Used in labour

Used in acute pain for a short time

32
Q

Methadone receptors

A

Mu agonist as well as NMDA receptor antagonist

33
Q

Effect of methadone on serotonin and norepinephrine

A

Uptake inhibitor

34
Q

Methadone clinical uses

A

Used in the control of withdrawal effects of addicts and maintenance therapy because withdrawal symptoms with methadone are milder and prolonged

35
Q

Methadone mode of elimination

A

Excreted in feces

36
Q

Methadone adverse effects

A

It can cause QT prolongation and torsades des pointes

37
Q

What are partial agonists and mixed agonist antagonist used for

A

Partial agonists given to opioid

38
Q

What are partial agonists and mixed agonist antagonist used for

A

Partial agonists given to opioid naive can show agonistic response but when given to opioid addicts can show withdrawal symptoms

39
Q

What are diphenoxylate and loperamide used for

A

Management of diarrhea

40
Q

Petazocin receptors

A

Kappa agonist and weak atagonist or partial agonist of mu

41
Q

Petazocin a mixed agonist and antagonist- effect

A

Can produce withdrawal symptoms in morphine abusers

42
Q

Petazocin adverse effects

A

Increase in concentration can cause respiratory depression, tachycardia and hallucinations so it is rarely used

43
Q

When is Petazocin used with caution

A

With angina and CAD

44
Q

Buprenorphine receptors

A

Agonist at mu receptor and antagonist at Kappa receptor

45
Q

Buprenorphine clinical uses

A

Used in the treatment of addiction—> used in opiate detoxification because it has a less severe and shorter duration of withdrawal than methadone

46
Q

Buprenorphine mode of administration

A

Sublingual and subdermal formulation approved in treatment of opioid addiction due to providing prolonged suppression of opioid withdrawal

47
Q

Why is Buprenorphine better than methadone at detoxification

A

Shorter and less severe

48
Q

Buprenorphine adverse effects

A

Respiratory depression not easily reversed by naloxone also QT prolongation

49
Q

Tramadol receptors

A

Centrally acting mu agonist which undergoes extensive metabolism to an active metabolite more affinity to mu receptors than parent compound

50
Q

When is tramadol used

A

Used in moderate to severe pain

51
Q

Tramadol adverse effects

A

Anaphylactoid reaction

52
Q

Tapentadol receptors

A

Centrally acting analgesic and antagonist of mu receptors and NET inhibitor

53
Q

Tapentadol clinical uses

A

Manage moderate to severe acute to chronic pain

Including neuropathic pain associated with diabetic peripheral neuropathy

54
Q

Tapentadol should be avoided in which patients

A

Patients taking MAOIs within the last 2 weeks

55
Q

Tapentadol metabolism

A

Metabolised by glucuronidstion —> low drug interactions

56
Q

Tramadol drug drug interactions

A

SSRI MAOIs AND TCAs leading to CNS toxicity

57
Q

Tramadol should be used with caution in people with

A

Seizures

58
Q

Opioid antagonist

A

Naloxone and naltrexone

59
Q

Naloxone mode of administration

A

IV

60
Q

Naloxone receptors

A

Competitive antagonist at mu kappa and deltts receptors

10 time fold at mu> kappa

61
Q

Naloxone clinical use

A
  • Quick onset of action
  • Reverses respiratory depression and coma by opioid over dose 1-2 mins after IV administration
  • Could be used for withdrawal symptoms
62
Q

Naltrexone difference than naloxone

A

Longer duration of action and slower onset of actions and can be given orally

63
Q

Naltrexone mode of administration

A

Can be given as a sustained release IM/month

64
Q

Naltrexone clinical use

A

Opioid dependence and alcohol addiction

Pharmacology (33 decks)

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