Neuropharmacology Flashcards

1
Q

What is the main side effect of clozapine?

A

Agranulocytosis

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2
Q

Tricyclic antidepressants have many side effects. Give some side effects and the receptors responsible for these side effects.

A

TCAs antagonise…

M1 - dry mouth, blurred vision, constipation, urinary retention
H1 - sedation, weight gain
a1 - postural hypotension

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3
Q

For which group of people are TCAs contraindicated?

Which patients do get TCAs?

A

Contraindications:
Young and old people
Cardiac patients - due to increasde risk of conduction abnormalities
Suicidal patients - due to risk of overdose
Drivers and workers - due to sedation

Uses:
Severe and treatment-resistant depression

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4
Q

Which SSRIs have the highest affinity?

A

Sertraline and paroxetine

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5
Q

Which type(s) of MAO do the newer forms of MAOIs inhibit? Give an example.

A

MAOa only - this is responsible for the breakdown of 5-HT and noradrenaline
Old-generation MAOIs break down dopamine too, causing EPSE.

Newer forms block MAOa only - an example is moclopemide.

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6
Q

Name a drug which inhibits 5-HT release? Why is it not used clinically?

A

Ecstasy. It is addictive and neurotoxic.

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7
Q

Why do antidepressants take a while to work?

A

Initially levels increase, causing more activation of 5-HT1a receptors found on the neuronal cell body. This receptor inhibits 5-HT secretion.

Eventually, the 5-HT1a receptor become desensitised and this is when the inhibition of 5-HT is stopped.

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8
Q

What are some side effects of antipsychotics due to their interaction with the nigrostriatal pathway?

A

loss of control of fine movement, EPSE, tardive dyskinesia

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9
Q

How are first generation antipsychotics categorised? Give examples.

A

Group 1 - sedation = chlorpromazine
Group 2 - anticholinergic = thioridazine
Group 3 - EPSE = fluphenazine

Another first generation antipsychotic is haloperidol.

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10
Q

Give examples of second generation (atypical) antipsychotics.

A
Clozapine
Olanzapine
Risperidone
Amisulpiride
Quetiapine
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11
Q

Give some negative and positive symptoms of schizophrenia…

A

Positive - disorders of thought, hallucinations, paranoia

Negative - blunted emotions/withdrawal, social withdrawal, apathy

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12
Q

Categorise these neurotransmitters into high and low in anxiety…

  1. Serotonin
  2. Noradrenaline
  3. GABA
A
  1. Serotonin is increased
  2. Noradrenaline is increased
  3. GABA is decreased
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13
Q

Give a very short half life benzodiazepine and suggest uses for it.

A

Midazolam

Conscious sedative + status epilepticus

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14
Q

Give a long half-life benzodiazepine and suggest a use for it.

A

Lorazepam
Chlordiazepoxide - acute alcohol withdrawal
Diazepam (Valium)

They are all anxiolytics used in GAD

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15
Q

Why does diazepam have a long half life?

A

It undergoes oxidative metabolism into active metabolites.

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16
Q

Why is there a risk of overdose associated with barbiturates?

A

They work on GABAa receptors.
But they do not require GABA to open the channel, hence risk of overdose as their use is not limited by GABA concentration.

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17
Q

How do Z-hypnotics work?

A

THey are allosteric modulators of GABAa receptors.

They are more selective to a1 receptors, leading to sedation.

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18
Q

Give examples of Z-hypnotics.

A

Zopiclone
Zolpidem
Zaleplon

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19
Q

Give a melatonin agonist which is licensed for use.

Which group of people is it licensed for?

A

Circadin.
Long-lasting melatonin agonist.

Licensed for use in 55+.

20
Q

Give an example of a SNRI.

A

Venlafaxine is the most common one.

21
Q

Give examples of TCAs.

A

Amytryptiline

Imipramine

22
Q

Give an example of a 5-HT1A agonist.

A

Buspirone.

23
Q

What are some desirable effects of opioids?

A
Analgesia
Euphoria
Constipation (if used as antidiarrhoeal)
Sedation (used as a hypnotic)
Cough suppression (antitussive)
24
Q

What are some undesirable affects of opioids?

A
Respiratory depression
Euphoria (can be abused)
Constipation
Histamine release
Immunosuppression
Sedation
Nausea and vomiting
Tolerance and dependence
25
Q

What effects does stimulating the mu opioid receptor have?

A

Analgesic effects in brain
Respiratory depression
Reward and physical dependence
Miosis

26
Q

What effects does stimulating the kappa opioid receptor have?

A

Analgesic effects in the spinal cord
No respiratory effects
No reward or dependence
Miosis

27
Q

What effects does stimulating the delta opioid receptor have?

A

Analgesia in CNS and elsewhere
Interacts with enkephalins
Physical dependence and reward
Respiratory stimulation

28
Q

Which opioid receptors does morphine work on?

A

Mu and delta

29
Q

What is the active metabolite of morphine and through which process does it become this metabolite?

A

GLucuronidation to morphine-6-glucuronide

30
Q

What is the half life of morphine

A

3h

31
Q

What are some indications for morphine

A

Moderate-severe pain

Acute heart failure (as dilates blood vessels)

32
Q

What is diamorphine? How does it work? How is it administered?

A

It is heroine.
Works like morphine after acetylation.
Administration is parenteral.

33
Q

What is methadone?

A

It works the same as morphine, but is used as substitution therapy for heroin addicts.

34
Q

What is the half life of methadone and why is this beneficial?

A

Half life is 24h which allows once daily dosing at the pharmacy.

35
Q

What is an opioid used in obstetrics?

A

Pethidine, it works like morphine but is less potent and less euphoric.

36
Q

What are some indications for codeine?

A

Mild pain, diarrhoea, anti-tussive properties

37
Q

What is dextropropoxyphene?

A

It is an opioid which works similar to codeine.

38
Q

Which opioid is mainly a mu agonist?

What other effects does it have other than its analgesic properties?

A

Tramadol

It also inhibits serotonin and noradrenaline reuptake.

39
Q

Name an opioid antagonist. Give an indication.

A

Naloxone. Used for opiate overdose.

40
Q

Which drug is given for post-withdrawal treatment?

A

Naltrexone.

Reduces high from heroine in relapses. Also reduces cravings.

41
Q

Give two drugs that can be used in substitution therapy. How often do they need to be dosed?

A

Methadone - once daily

Buprenorphine - three times a week.

42
Q

What is a seizure?

A

A period of synchronous discharge of neurones.

43
Q

What is a convulsion?

A

Muscular contractions which sometimes accompany a seizure.

44
Q

What is epilepsy?

A

Epilepsy is a disorder characterised by repeated seizures.

45
Q

What symptom might somebody with temporal lobe epilepsy get during a seizure?

A

Hallucinations

46
Q

What circuit is affected in absence seizures?

A

Thalamocortical circuits.

47
Q

What are the three phases of a grand mal seizure?

A

Tonic - high frequency neuronal activity
Clonic - lower frequency neuronal activity
Post-ictal - electrical depression due to neuronal fatigue.