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Applied Pharmacology bs > Analgesics and Anti-emetics > Flashcards

Analgesics and Anti-emetics Flashcards

1
Q

What is acute/ nociceptive pain ?

A
  • short term pain
  • easily identifiable cause
  • warning of present damage to tissue or disease which responds well to medication
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2
Q

What is chronic or neuropathic pain?

A
  • pain which persists
  • constant or intermittent
  • outlived its purpose since it no longer helps the body to prevent further injury
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3
Q

what is allodynia in reference to pain?

A

pain from a stimulus that does not normally cause pain

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4
Q

What is parasthesis?

A

painful feelings (eg pins and needles) with no apparent stimulus

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5
Q

Where do anti-inflammatorys normally act?

A

upon the relay station of the afferent pain impulse,
up the CNS.
- this intensifies the signalling process

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6
Q

opioids, serotonin (5HT) and norepinephrine/ noradrenaline act naturally to …

A

suppress inhibitory pathways

- drugs can enhance this pathway

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7
Q

What two ways can we reduce pain?

A
  • prevent transmission of information upwards towards CNS (opioids)
  • enhance inhibitory pathway
  • anti - inflammatory’s too
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8
Q

There are three broad types of pain relief (not including anti-inflammatory) they include:
- opioids
- anti-depressants & antiepileptic’s
- local anaesthetics
What are the key things of each of these?

A

OPIOIDS
- modify the transmission of pain signals and the subjective perception of pain
ANTIDEPRESSANTS & ANTI-EPILEPTICS
- trigeminal neuralgia (pain with nerve in shoulder and jaw)
- neuropathic pain which is resistant to opioids
LOCAL ANAESTHETICS
- particularly effect for severe intractable or crescendo neuropathic pain
- associated with trauma

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9
Q

What is the mechanism of action for opioids?

A
  • block pain pathway
  • within CNS, with spinal cord
  • decrease the transmitters that mediate pain pathway
  • activate inhibitory pathways / MIMIC OUR ENDOGENOUS LIGANDS (ENKEPHALINS)
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10
Q

What are the unwanted side effects of opioids?

A
  • will interact with medications and alcohol
  • nausea and vomiting
  • constipation
  • drowsiness
  • respiratory depression
  • hypotension
  • sedation
  • dependency
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11
Q

What are the targets for anti-emetics and where do they act?

A

Dopamine
Substance P/ neurokinin NK
Serotonin/ 5HT receptors
ALL ACT ON THE CHEMORECEPTOR TRIGGER ZONE

serotonin/ 5HT
ACT ON VAGAL PATHWAY

histamine
muscarinic
ACT ON VESTIBULAR PATHWAY

muscarinic 
histamine antagonist 
5HT3
substance P
ACT ON VOMITING CENTRE
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12
Q

What are histamine antagonist used for?

A

motion sickness
vestibular diseases (affects the body balance)
GI irritants

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13
Q

What are examples of histamine antagonist used to treat motion sickness, vestibular disease and GI disturbance ?

A

CYCLIZINE - for motion sickness
CINNARIZINE - motion sickness, vestibular disease (vertigo and menieres disease)
PROMETHAZINE - severe morning sickness

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14
Q

Histamine antagonist are of limited use against substances that act directly on chemotherapy triggering zone. What are there other side effects?

A

drowsiness

sedation

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15
Q

What do muscarinic receptor antagonist treat in sickness? examples of this drug is hyoscine or scopolaimine

A

general use in sickness

motion sickness

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16
Q

What are the side effects of acetylcholine/ muscarinic receptor such as hyoscine or scopolaimine used to treat sickness?

A

dry mouth
blurred vision
less sedative than antihistamines

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17
Q

Dopamine receptor have strong representation in the chemoreceptor triggering zone and will also act on muscarinic and histamine and so has a more powerful anti-emetic response. what are they used to treat?

A
  • uraemia
  • Opioid induced emesis
  • CINV
  • GI disorders
  • viral gastroenteritis
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18
Q

What are examples of dopamine receptors?

A
  • phenothiazines
  • perphenazine
  • prochloropromazine
  • metoclopramide
  • domperidone
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19
Q

What are the side effects of dopamine receptor antagonist such as

  • phenothiazines
  • perphenazine
  • prochloropromazine
  • metoclopramide
  • domperidone
A

sedative
hypotension
dystonia (muscle spasm and abnormal posture)
dyskinesia (abnormal or impairment of voluntary movement)

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20
Q

What dopamine mechanism of action?

A

receptors on chemoreceptor triggering zone

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21
Q

5HT/ serotonin antagonist are the choice of CINV (chemo sickness) and PONV (aesthetic sickness). What are the side effects?

A

GI disturbances

headaches

22
Q

What are 5HT / serotonin antagonist used for?

A

chemotherapy sickness
aesthetic sickness
radiation induced vomiting

23
Q

What is an example of 5HT/ serotonin antagonist?

A

ondansetron

24
Q

Aprepitant is a neurokinin antagonist/ substance P. What are its side effects?

A 
fatigue 
constipation/ diarrhoea
loss of appetite 
hiccups 
dizziness 
ringing in ears 
anorexia 
headache
25
Q

Aprepitant is a neurokinin antagonist/ substance P. What is it used to treat?

A

chemo sickness

aesthetic sickness

26
Q

Neurokinin antagonist / substance P active in the late stage emesis with what drug?

A

cytotoxic

27
Q

Cannabinoids are valuable in the treatment of CINV and thought to act via which receptors?

A

via opioid receptors in chemoreceptor triggering zone
agonist of the cannabinoid receptors
- also used for chronic pain management

28
Q

Corticosteroids such as dexamethasone can act as anti-emetics. what is it effective against?

A
  • vomiting caused by cytotoxins
29
Q

Corticosteroids such as dexamethasone can act as anti-emetics. What are they used in combination with ?

A

dopamine receptors
5HT/ serotonin
as this improves actions

30
Q

What drug would you give for morning sickness?

A

Promethazine (histamine receptor antagonist)

phenothiazine (dopamine receptor antagonist)

31
Q

What drug would you give for motion sickness?

A

hyoscine (muscarinic antagonist)
promethazine (histamine antagonist )
cyclizine (histamine antagonist)

32
Q

What drugs would you used to treat PONV?

A

phenothiazine (dopamine receptor antagonist)

metoclopramide (dopamine receptor antagonist)

33
Q

What drugs would you used to treat CINV?

A

ondansetron (serotonin receptor antagonist )

phenothiazines (dopamine receptors antagonist)

34
Q

What drugs would you use to treat sickness related to opioids?

A 
haloperidol 
metoclopramide (dopamine receptor antagonist )
35
Q

What drugs would you used to treat sickness related to gastroenteritis?

A

metoclopramide (dopamine receptor antagonist)

36
Q

What drugs would you for anticipatory emesis?

A

benzodiazepines

37
Q

Most opioids are U-receptor agonist. what do these act on?

A
  • CNS
  • spinal cord
  • GI tract
  • peripheral sensory neurones
38
Q

How do antidepressants work in stopping pain?

A

Serotonin and noradrenaline mediate descending inhibition of ascending pain pathways in the brain and spinal cord

39
Q

What types of pain are antidepressants that act on serotonin and noradrenalin are they effective against?

A
  • neuropathic pain

- appear to work well in the disease environment such as diabetes or HIV related neuropathy

40
Q

What are examples of antidepressants that work on inhibition of serotonin and noradrenalin ?

A
  • citalopram
  • paroxetine
    ^^^ serotonin
  • venlafaxine
  • duloxetine
    ^^noradrenalin
41
Q

how do SNRI/ SSRI work?

A

prevent the recycling of neurotransmitters & enhance the signal

42
Q

What are the side effects of the SNRI such as venlafaxine and duloxetine?

A

venlafaxine

  • prescribed for diabetic neuropathy
  • nausea, sedation, headache and dizziness

duloxetine

  • prescribed for peripheral neuropathy particularly in diabetic neuropathy
  • nausea, somnolence, insomnia, dizziness

*they both interact with a lot of drugs

43
Q

how do anti-epileptic drugs work in preventing pain?

A
  • inhibit of voltage gated sodium and calcium
  • inhibit glutamate and GABA
  • inhibit action potential firing
  • prevent impulse transmission
  • limit neuronal excitation
  • enhance neuronal inhibition
44
Q

What are examples of anti-epileptic drugs and what kind of pain do they help with?

A

CARBAMAZEPINE

  • glossopharyngeal neuralgia
  • post herpetic neuralgia
  • trigeminal neuralgia
  • diabetic neuropathy

GABAPENTIN
- various neuropathy states

45
Q

What are the side effects of carbamazepine?

A
  • dizziness
  • diplopia
  • drowsiness
  • fatigue
  • nausea
  • hepatotoxicity
  • renal impairment
  • tremor
    skin reaction
    caution with hepatic/renal impairment and cardiac disease
46
Q

What are the side effects of gabapentin?

A

*current drug of choice due to limited side effects
- anorexia
-dyspepsia
- tremor
caution with :
- elderly
- renal impairments
- diabetes
- pregnancy

47
Q

How do local anaesthetics work?

A
  • inhibit of voltage gated sodium
  • prevent nerve to nerve cell communication
  • inhibit firing
  • prevent impulse transmission
48
Q

What are examples of local anaesthetics and their specific actions?

A

Lidocaine (xylocaine)

  • blocks sodium channels
  • effective in non cancer patients

Ketamine (ketalar)
- blocker of glutamate receptors (NMSA subtype)

49
Q

How are lidocaine and ketamine administered ?

A
  • lidocaine = IV

- Ketamine - is injectable but not favoured due to side effects

50
Q

What are the side effects of lidocaine ?

A
  • CNS effects (confusion)
  • respiratory depression
  • convulsions
  • hypotension
  • bradycardia

caution with:epilepsy, hepatic and respiratory impairments, AF, heart failure

51
Q

What are the side effects of ketamine ?

A
  • hypertension
  • tachycardia
  • tremor
  • diplopia (double vision)
  • myocardial depression
    Caution with : hypertension, angina, heart failure, aneurysms, cerebral trauma and psychotic disorders

Applied Pharmacology bs (10 decks)

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