Nervous System Flashcards

1
Q

What are 3 examples of anxiolytics?

A

Diazepam
Lorezepam
Midazolam

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2
Q

How do anxiolytics work?

A

Increase GABA activity - inhibit neurotransmission

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3
Q

When can anxiolytics be used?

A
  • Epilepsy

* Anxiety

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4
Q

What drug classes can be used for nausea and vomiting?

A
  • H1 antagonists
  • D2 antagonists
  • 5HT3 antagonists
  • Neurokinin-1 antagonists
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5
Q

Give an example of a H1 antagonist.

A

Cyclizine

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6
Q

Give an example of two D2 antagonists.

A

Domperidone

Metoclopramide

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7
Q

What is an example of a 5HT3 antagonist?

A

Ondansetron

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8
Q

What is the mechanism of action of ondansetron peripherally and centrally?

A

Peripherally - reduces GI motility and GI secretions

Centrally - inhibits the chemoreceptor trigger zone (CTZ)

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9
Q

Who is ondansetron good for?

A

Almost everyone - often 1st line treatment

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10
Q

What are some side effects of ondansetron?

A

Uncommon - constipation, headache, increased liver enzymes, prolonged QT interval, extra-pyramidal effects e.g. dystonia and parkinsonism

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11
Q

What is an example of a muscarinic antagonist used to treat nausea and vomiting?

A

Hyoscine hydrobromide

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12
Q

What is the mechanism of action of hyoscine hydrobromide?

A

Competitively block EACh receptors in the vestibular nuclei and at the CTZ

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13
Q

What are some side effects of the muscarinic antagonist hyoscine hydrobromide?

A
  • Sedation
  • Memory problems
  • Glaucoma
  • Dry mouth
  • Constipation

(ACh receptors all over body, part of parasympathetic nervous system)

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14
Q

What are the common indications for hyoscine hydrobromide?

A
  • Motion sickness
  • Bowel obstruction

Good for those who can’t take tablets - available as patches

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15
Q

What is an example of a neurokinin-1 antagonist?

A

Aprepitant

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16
Q

What is the mechanism of action of aprepitant?

A
  • Prevents substance P action at CTZ and in peripheral nerves
  • Boosts effects of 5HT3 receptors antagonists
  • Anxiolytic and antidepressant properties
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17
Q

What is aprepitant often used for?

A
  • Chemotherapy (especially delayed emesis)
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18
Q

What are some side effects of aprepitant?

A
  • Headache
  • Diarrhoea/constipation
  • Stevens-Johnson syndrome - rash
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19
Q

Give two examples of antipsychotic drugs.

A
  • Chlorpromazine

* Haloperidol

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20
Q

What can chlorpromazine and haloperidol be used for aside being antipsychotics?

A

Can be used as anti-emetics

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21
Q

What is the mechanism of action of chlorpromazine and haloperidol?

A

D2 receptor antagonists (post synaptic D2 receptors)

Act on CTZ

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22
Q

What circumstances is haloperidol good and not good for?

A

Chemo and palliation (esp due to sedative action)

Not good if someone has Parkinson’s (Parkinsonism side effects)

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23
Q

What is chlorpromazine good for?

A

Motion sickness and vertigo

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24
Q

Give 9 examples of analgesics.

A
  • Aspirin
  • Paracetamol
  • Buprenorphine
  • Codeine
  • Diamorphine
  • Fentanyl
  • Methadone
  • Morphine
  • Tramadol
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25
Q

What is the mechanism of aspirin as an analgesic?

A

Inhibits prostaglandin synthesis

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26
Q

What is the mechanism of action of paracetamol?

A

COX-2 inhibition in the spinal cord?

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27
Q

What do you give in paracetamol overdose?

A

N-acetylcysteine

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28
Q

What metabolite is it that builds up when you take paracetamol, that causes the overdose?

A

NAPQI - at normal doses, conjugates with glutathione, but hepatic glutathione is limited

29
Q

What dose of paracetamol is sufficient to cause irreversible damage?

A

150mg/kg

30
Q

What class of drugs are buprenorphine, codeine, diamorphine, fentanyl, methadone and tramadol?

A

Opioid receptor agonists

31
Q

By which two mechanisms can people develop tolerance to opioids?

A
  • Phosphorylation and uncoupling - phosphorylation modulates the neuroreceptors
  • cAMP production - if you remove the opioid, there’s a rebound effect, increased cAMP production, increased excitability so withdrawal symptoms
32
Q

Which three opioids are the strong agonists?

A
  • Methadone
  • Morphine
  • Fentanyl
33
Q

Which opioid is a moderate agonist?

A

Codeine

34
Q

Which opioid is a mixed agonist/antagonist or partial agonist?

A

Buprenorphine

35
Q

Which opioid is “other”?

A

Tramadol

36
Q

Does fentanyl have more or less side effects than morphine? Why?

A

Less, due to less histamine release and less sedation and constipation

37
Q

What should you prescribe alongside codeine?

A

A laxative

38
Q

How is buprenorphine eliminated?

A

Mostly in the biliary system (over renally)

39
Q

When is buprenorphine used?

A
  • Moderate to severe pain

* Opioid addiction treatment

40
Q

What are some of the side effects of buprenorphine?

A
  • Respiratory depression
  • Low BP
  • Nausea
  • Dizziness
41
Q

How does buprenorphine work?

A

It’s a partial agonist, so has a low Kd and a high affinity for mu receptors

Not easily displaced, so harder to reverse an overdose with buprenorphine, but this isn’t as likely

42
Q

How does N-aceytlcysteine work?

A

Glutathione donation (glutathione precursor), so glutathione can then bind to NAPQI

43
Q

What is used to treat opioid overdose?

A

Naloxone

44
Q

How does naloxone work?

A

It’s a opioid receptor antagonist (binds competitively)

Infusion rather than quick delivery, otherwise wears off quickly as has a short-half life

45
Q

Name 3 antiepileptic drugs that work by blocking sodium channels.

A
  • Carbamazepine
  • Lamotrigine
  • Phenytoin
46
Q

What is an AED that increases GABA synthesis?

A

Sodium valproate

47
Q

What is levetiracetam?

A

An AED, that possibly blocks presynaptic calcium activity

48
Q

When is phenytoin used?

A
  • Status epilepticus

* Adjunct in generalised seizures

49
Q

What’s unique about phenytoin?

A

Zero order kinetics

50
Q

What are specific side effects if phenytoin?

A
  • Myelosuppression
  • Hypotension
  • Arrhythmias if given by IV
51
Q

What drug is good for focal epilepsy?

A

Lamotrigine

52
Q

Which AED is most safe in pregnancy?

A

Levetiracetam

53
Q

Which 3 AEDs are CYP inducers?

A
  • Phenytoin
  • Carbamazepine
  • Barbituates
54
Q

Which AED is a CYP inhibitor?

A

Sodium valproate

55
Q

What is the initial management of a seizure?

A

ABCDE, get help, start a clock

56
Q

What is the pharmacological staging in status epilepticus?

A
  • 0-5 mins - benzodiazepine
  • 0-15 mins - second benzodiazepine dose
  • 15-45 mins - Phenytoin or levetiracetam
  • 45+ mins - Thiopentone/anaesthesia and support

(consider IV thiamine if with alcohol use)

57
Q

What classes of drugs are used to treat Parkinson’s disease?

A
  • Dopamine receptor agonists
  • Monoamine oxidase (MAO) type B inhibitors
  • Catechol-O-methyl transferase (COMT) inhibitors
  • Anticholinergics
58
Q

Give 6 examples dopamine receptor agonists.

A
  • Amantadine
  • Apomorphine
  • Ropinirole
  • Rotigotine
    Pre-cursors of dopamine
  • Levodopa (L-DOPA)
  • Co-careldopa
  • Co-beneldopa
59
Q

Give two examples of MAO type B inhibitors.

A
  • Rasagiline

* Selegiline

60
Q

Give an example of a COMT inhibitor.

A

Entacapone

61
Q

Give two examples of anticholinergics used to treat Parkinson’s.

A
  • Orphenadrine

* Procyclidine

62
Q

Only when is apomorphine used?

A

In patients with severe motor fluctuations

63
Q

What are the advantages and disadvantages of dopamine receptor agonists?

A
  • direct acting
  • less dyskinesia/motor complications
  • some neuroprotection
  • less efficient than L-DOPA
  • lead to impulse control disorders
  • more psychiatric side effects
  • expensive
64
Q

What are the ADRs of dopamine receptor agonists?

A
  • Sedation
  • Hallucinations
  • Confusion
  • Nausea
  • Hypotension
65
Q

What is the mechanism of action of MAO B inhibitors?

A

Prevent breakdown of dopamine

66
Q

Why don’t you give COMT inhibitors alone?

A

No therapeutic effect alone - only act to increase the amount of dopamine present, by reducing it’s peripheral breakdown

67
Q

Why can you use anticholinergics to treat Parkinson’s?

A

ACh may have antagonistic effects to dopamine

68
Q

What are the ADRs of anticholinergics?

A
  • Confusion
  • Drowsiness
  • Anticholinergic side effects - dry mouth, constipation, blurry visions, problems urinating (esp. an issue in the elderly)
69
Q

What are two advantages of using anticholinergics to treat Parkinson’s? What is a disadvantage?

A

Doesn’t act on dopamine systems and treats the tremor

No effect on the bradykinesia