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Pharmacology Flashcards

1
Q

What type of drugs most effectively diffuse across the blood brain barrier?

A. Hydrophilic/ Lipophobic

B. Hydrophobic/ Lipophillic

C. Neither is better than the other

D. None of them do

A

B

To get into the brain drugs must be lipophillic

E.g. Atenolol is ineffective as anti-anxiety medication as it doesn’t actually enter the brain, but propranolol does and so therefore is effective

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2
Q

What class of antidepressants may be used to treat neuropathic pain?

A

tricyclics

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3
Q

What are some antidepressant drug classes?

A
  • Monoamine oxidase inhibitors
  • Monoamine reuptake inhibitors
    • Tricyclics
    • SSRIs
    • Noradrenaline reuptake inhibitors
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4
Q

What of the following neurotransmitters is not a monoamine?

A. Dopamine

B. Glutamate

C. Noradrenaline

D. 5-HT (Seratonin)

A

B

Glutamate is not a monoamine

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5
Q

In which nuclei is seratonin producted?

A

The raphe nuclei of the rostral group

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6
Q

What are some examples of monoamine oxidase inhibitors?

A

Phenelzine and Moclobemide

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7
Q

What is the mode of action of monoamine oxidase inhibitors?

A

Irreversable (Phenelzine) or reversable (Moclobemide) inhibitors of MAO- A and B

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8
Q

What are some side effects of monoamine oxidase inhibitors?

A
  • Cheese reaction/hypertensive crisis- caused by MAO-A inhibition in gut and liver by irreversable drugs which prevents breakdown of dietary tyramine
  • Potentiates effects of other drugs by decreasing their metabolism
  • Insomnia
  • Postural hypotension
  • Peripheral oedema
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9
Q

Which of the following side effects are more likley to be caused by an SSRI than a tricyclic?

A. Blurred vision

B. Constipation

C. Dry mouth

D. Nausea

E. Urinary retention

A

D

Tricyclics are anticholinergic and so A, B, C, and E are all classic side effects

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10
Q

Which of the following antidepressants should be avoided in a 57 year old man with ischaemic heart disease who became depressed following an MI 2 months ago?

A. Citalopram

B. Fluoxetine

C. Imipramine

D. Mirtazapine

E. Sertraline

A

C

Avoid using imipramine in ischameic heart disease

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11
Q

What class do the following antidepressants belong to?

Imipramine, Dosulepin, Amitriptyline, Lofepramine

A

Tricyclic antidepressants

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12
Q

How do tricyclic antidepressants work?

A

Block the reuptake of monoamines (mainly noradrenaline and 5-HT) into presynaptic terminals. This means more is avaliable in the cleft

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13
Q

What are some side effects of tricyclic antidepressants?

A
  • Anticholinergic= blurred vision, dry mouth, constipation, urinary retention
  • Sedation
  • Weight gain
  • CV= postural hypotension, tachycardia, arrythmias
  • Carditoxic in overdose
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14
Q

How do SSRIs work?

A

Selectively inhibit the reuptake of seratonin in the synaptic cleft leading to increased seratonin activity

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15
Q

What class of drugs do the following antidepressants belong to?

Fluoxetine, Citalopram, Sertraline

A

SSRIs

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16
Q

What are some common side effects of SSRIs?

A
  • Nausea
  • Headache
  • Worsened anxiety
  • Transient increase in self harm/ suicidal ideation <25
  • Sweating and vivid dreams
  • Sexual dysfunction
  • Hyponatreamia (elderly)
  • Discontinuation effects
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17
Q

How do SNRIs work and what are some examples?

A

Block the reuptake of monoamines (noradrenaline and 5-HT) into presynsaptic terminals.

Venlaxafine and Duloxetine

Similar side effects to SSRIs

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18
Q

What are the short and long term goals in treatment of Bipolar Disorder?

A

Acute treatment of symptoms- to reduce mood in episodes of mania and raise mood in episodes of depression

Long term treatment- to stabilise mood and prevent recurrence of both mania and depression (prophylaxis)

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19
Q

What of the following side effects would suggest lithium levels in the toxic range?

A. Ataxia

B. Hypothyroidism

C. Nausea

D. Polyuria

E. Tremor

A

A

Ataxia suggests toxic levels

The rest of the list are normal side effects

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20
Q

True or False?

Lithium is subject to extensive hepatic metabolism

A

False- not metabolised at all. Undergoes renal excretion

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21
Q

Lithium ions and sodium ions are indistinguishable to the renal tubules. What will the effect of dehydration be on lithium levels?

A. Decrease in lithium levels

B. Increase in lithium levels

C. No change in lithium levels

A

B

An increase in lithium levels. If dehydrated the tubules will absorb more Na to pull the water in and so will also absorb more lithium

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22
Q

What are the side effects of lithium?

A
  • Dry mouth/ strange taste
  • Polydipsia and polyuria
  • Tremor
  • Hypothyroidism
  • Long term reduced renal function
  • Nephropgenic diabetes insipidis
  • Weight gain
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23
Q

What are some of the toxic effects of Lithium?

A
  • Vommiting
  • Diarrhoea
  • Ataxia/ coarse termor
  • Drowsiness / altered concious level
  • Convuslions
  • Coma
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24
Q

A 27 year old women is diagnosed with bipolar disorder. She hopes to get pregnant some time in the future. Which mood stabiliser is to be avoided?

A. Aripiprazole

B. Lamotrigine

C. Lithium

D. Quetiapine

E. Valproic Acid

A

E is contraindicated

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25
What anticonvulsants are used as mood stabilisers in the treatment of BPD?
Valproic acid, Lamotrigine and Carbamazepine
26
What are the side effects of the anti-convulsants used as mood stabilisers?
* Valproate and carbamazepine - drowsiness, ataxia, CV effects, induces liver enzymes * Valproate- teratogenicity (neural tube defects) * Lamotrigine- very small risk of Stevens-Johnson syndrome
27
How do antipsychotics work?
Dopamine antagonism and 5-HT antagonism
28
What class do these mood stabilisers belong to? Quetiapine, Aripiprazole, Olanzapine, Lurasidone
Antipsychotics
29
What are some side effects of anti-psychotics?
* Sedation, weight gain and metabolic syndrome * extra-pyramidal side effects (Aripiprazole)
30
What are the 2 core symptoms of anxiety?
Fear- panic and phobia (amygdala-centered circuit) Worry- anxiety, apprehensions, obsessions (cortico-striatal-thalamic-cortical tract)
31
What does the neurotransmitter GABA do?
It is the main inhibitory neurotransmitter in the brain Reduces the activity of neurons in the amygdala and the CSTC
32
What are the main GABA receptors?
GABA-A, GABA-B and GABA-C
33
What GABA receptor is the target of benzodiazepines, barbituates and alcohol
GABA-A
34
What class of drugs do the following belong to? Lorazepam, Diazepam, Chlordiazepoxide
Benzodiazepines
35
What are the pharmacological effects of benzodiazepines? (5)
* Reduce anxiety and aggression * Hypnosis/ sedation * Muscle relaxation * Anticonvulsant effect * Anterograde amnesia
36
What are the problems associated with benzodiazepines?
* Paradoxical aggression * Anterograde amnesia and impaired coordination * Tolerance and dependence
37
What is given in benzodiazepine overdose?
Flumazenil
38
How should benzodiazepines be withdrawn?
1. Transfer patient to an equivelent daily dose of diazepam or chlordiazepoxide, preferably taken at night 2. Reduce dose every 2-3 weeks, in steps of 2 or 2.5mg. If withdrawal symptoms occur, maintain this dose till they improve 3. Reduce dose further- better to reduce too slowly than too quickly 4. Stop completely- time needed for withdrawal can vary from around 4 weeks to a year
39
How do SSRIs work?
Inhibit the reuptake of serotonin which leads to increased levels of it within the synaptic cleft
40
Roughly how long do SSRIs take to have an anxiolytic effect?
Around 12 weeks
41
What classes of antidepressants can be used to treat anxiety?
* SSRIs- panic disorder, OCD, PTSD, phobias, GAD * Tricyclics- second line for panic disorder * Venlafaxine (SNRI)- GAD * Moclobemide (MAOI)- social anxiety disorder
42
Other than antidepressants, what other classes of drugs can be used to treat anxirty?
* Pregabalin - Ca+ channel blocker, GABA enhancer * Only considered if not responsive to other treatments * Beta blockers- e.g. Propranolol * Best for somatic symptoms such as palpitation, tremor
43
What are the steps of treatment in the management of GAD?
1. Pyschoeducation 2. Self help/ psychoeducation groups 3. CBT **or** start drug treatment- SSRI 4. SNRI 5. Pregabalin 6. Combination of CBT and drug treatment
44
In GAD, how long should a patient be treated with antidepressants?
Takes around 12 weeks for full effect If works, continue the drug for 18 months When stopping, reduce the drug gradually to avoid discontinuation
45
What is the steps in the treatment of panic disorder?
1. Self help 2. CBT **or** SSRI, if long standing or no benefit from CBT 3. Tricyclics Continue treatment for 6 months
46
What is the management steps of OCD?
1. Low intensity psychological intervention- CBT or ERP 2. More intensive psychological intervention or SSRI * If effective continue for a year 3. Consider an increase in dose after 4-6 weeks 4. SSRI + ERP and CBT 5. Clomipramine 6. Augmentation with antipsychotic or clomipramine + citalopram
47
What are the steps in the management of PTSD?
1. Mild and less than 4 weeks since trauma= watchful waiting 2. Within 3 months of trauma: * Trauma focussed CBT * Hypnotic medication for sleep disturbance 3. More than 3 months after trauma * Trauma focussed CBT or EMDR 4. Limited evidence for drug treatment * Paroxetine or Mirtazepine * Amitryptiline or phenelzine
48
What are the steps in the management for social anxiety?
1. Individual CBT 2. SSRI (escitalopram or sertraline)- review at 12 weeks 3. SSRI + CBT 4. Alternative SSRI (e.g. fluoxetine) or SNRI (venlafaxine) 5. MAOI (moclobemide)
49
Describe the mesolimbic pathway
Begins at the VTA Projects dopaminergic action potentials into the nucleus accumbens Involved in pleasure and reward
50
Describe the mesocortical pathway
Starts in the VTA and then action potentials travel to the prefrontal cortex Involved in cognition, working memory and decision making
51
Describe the nigrostriatal pathway
Involved in motor planning and purpousful movement Dopamine projections start in the substantia nigra and go to the caudate and putamen of the basal ganglia
52
What side effects result from D2 antagonists in the nigrostriatal pathway?
Extra-pyramidal side effects e.g. parkinsonism, tardive dyskinesia
53
Describe the tuberoinfundibular pathway
Dopamine neurones from the hypothalamus project into the infundibular region Dopamine is released into the portal circulation that connects this region to the pituitary gland, where dopamine functions to inhibit prolactin release
54
What happens when dopamines inhibition of prolactin relase is blocked by antipsychotics?
Levels of prolactin increases which can lead to- menstrual cycle effects, decreased libido, fertility issues, bone problems, gynacomastia and galactorrhoea
55
What would the ideal antipsychotic inhibit?
D2 receptors in the mesolimbic pathway
56
What are the groups of antipsychotics?
1st generation (typicals) 2nd generation (atypicals)
57
What group of antipsychotics do the following belong to? Chlorpromazine, Haloperidol, Fluphenazine
1st generation antipsychotics
58
What class of antipsychotics do the following drugs belong to? Aripiprazole, Lurasidone, Olanzapine, Quetiapine, Risperadone, Ziprasidone and Clozapine
2nd generation antipsychotics
59
What group of antipsychotics are more likely to cause extra-pyramidal side effects?
1st generation 2nd gen are more likely to cause symptoms such as weight gain and sedation
60
2nd generation antipsychotics only block D2 receptos True or False?
False Also block serotonin receptors such as 5-HT2A
61
What antipsychotic can cause agranulocytosis and so patients on this require regular blood checks?
Clozapine
62
What are the extra-pyramidal side effects?
* Acute dystonic reaction (onset in minutes) * Parkinsonism * Tardice Dyskinesia (long-term and often permanent)
63
What are the dopaminergic side effects caused by antipsychotics?
* Extra pyramidal side effects * Neuroleptic malignant syndrome * Hyperprolactinaemia * Akathisia/ restless leg syndrome
64
What is neuroleptic malignant syndrome?
Life threatnening condition that can occur in response to antipyschotics Symptoms are high fever, confusion, rigid muscles, variable BP, sweating and fast HR
65
What is the treatment of neuroleptic malignant syndrome?
1. Stop the antipsychotic 2. Rapid cooling and renal support 3. Skeletal muscle relaxants e.g. Dantrolene 4. Dopamine agonists e.g. bromocriptine
66
What is the treatment of Akathisia?
1st line is propranolol 2nd line is a long acting benzodiazepine like clonazepam
67
In what order are antipsychotics selected?
1. Start on 2nd generation and titrate up for 6-8 weeks. Assess the effects. If it works, keep going. 2. If step 1 doesnt work, choose either a 1st or 2nd generation. Titrate up for 6-8 weeks. 3. If doesnt work- check diagnosis, consider psychological input, optimise social supports, check complience (depot?) 4. Consider Clozapine

Psychiatry (4 decks)

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