Pharmacological Management Of Anxiety Disorders and Depression Flashcards

1
Q

What is the function of the 5HT2-a receptor?

A

Located in the limbic system, involved in anxiety and panic attacks.

In the sleep centre, involved in insomnia and disruption of slow wave sleep.

In the basal ganglia, involved in muscle restlessness.

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2
Q

What is the function of the 5-HT1a receptor?

A

Autoreceptor responsible for the delayed effect of anxiolytics, which eventually become desensitised over time.

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3
Q

What is the function of the 5HT3 receptor?

A

Present in the hypothalamus and gut to cause vomiting, diarrhoea and muscle cramps.

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4
Q

What is the function of the 5HT2-C receptor?

A

Located in the spinal cord and activation causes sexual dysfunction.

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5
Q

What is the action of SSRIs?

A

Reduce the reuptake of serotonin in the synaptic cleft by SER/serotonin transporters on the presynaptic neurons to increase availability and reduce psychological symptoms.

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6
Q

How is serotonin synthesised?

A

Dietary protein, in the form of the amino acid tryptophan -> serotonin

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7
Q

Where is serotonin stored/found in the body?

A

-> Platelets

-> Neurons in the CNS

-> Enterochromaffin cells in the gut

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8
Q

What are the general side effects of SSRIs?

A

They increase bleeding time, with possible risk in pregnant women for post-partum haemorrhage.

Prolonging of the QT interval

Vomiting, diarrhoea and muscle cramps

Arthralgia (joint pain)

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9
Q

What is the first line SSRI commonly used in anxiety and depression?

A

Citalopram or Fluoxetine
Followed by Escitalopram, Paroxetine and Sertraline.

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10
Q

What are the contraindications for SSRIs?

A

Poorly controlled epilepsy and QT interval prolongation.

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11
Q

How are the catecholeamines synthesised?

A

Dietary protein in the form of phenylalanine -> tyrosine -> levadopa -> dopamine -> noradrenaline - > adrenaline

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12
Q

What is the action of SNRIs?

A

Block action of SER and NE transporters on the presynpatic neurons to increase availability of serotonin and noradrenaline.

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13
Q

Which SNRIs are first line treatment for anxiety and depression?

A

Venlafaxine and Duloxetine

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14
Q

What is the action of venlafaxine?

A

It has a wider use than duloxetine; major depression, GAD, social anxiety and panic disorder. It is an SNRI with a greater affinity for serotonin than noradrenaline.

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15
Q

What is the action of duloxetine?

A

Potent inhibitor of serotonin, noradrenaline and a lesser inhibitor of dopamine. It’s given for major depressive disorder and anxiety.

It decreases the transmission of painful stimuli; Increases vasoconstriction, hypertension and muscle contraction.

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16
Q

What is the action of TCAs?

A

Tricyclic antidepressants inhibit serotonin transporters, noradrenaline transporters, histamine, muscarinic, Na+ channels and alpha 1 receptors.

They are a second line treatment for depression due to the risk of overdose and more significant side effects compared to SSRIs.

17
Q

What are the side effects of tricyclic antidepressants?

A

Tricyclic antidepressants are likely to induce mania amnd are contraindicated for mania during bipolar.

-> Inhibition of histamine= sedation and weight gain.

-> Inhibition of muscarinic receptors= orthostatic hypotension and dizziness.

-> Inhibition of Na+ channels= cardiac channel abnormalities

-> Increase in serotonin= sexual dysfunction, diarrhoea and vomiting

-> Increase in noradrenaline= hypertension

18
Q

What are the contraindications of tricyclic antidepressants?

A

Cardiovascular disease/arrythmias
Conditions related to hypertension such as Glaucoma, Urinary retention and Prostate hypertrophy.

19
Q

What are the primary tricyclic antidepressants?

A

Amitryptilline

Lofepramine

Imipramine

20
Q

What is the action of amitryptilline?

A

Given for major depressive disorder and those with neuropathic pain. Inhibits SER and NER transporters and inhibits the action of histamine, a1 receptors and muscarinic receptors.

21
Q

What is the action of MAO inhibitors?

A

Prevent the action of monoamine oxidase within the presynaptic neuron via the packaging of dopamine, serotonin and noradrenaline. They were divided into non-selective MAO inhibitors, MAO-A inhibitors and MAO-B inhibitors.

22
Q

What are the non-selective MAO inhibitors?

A

Phenelzine
Tranylcycloprine

23
Q

What is the action of monoamine oxidase A?

A

Greatest affinity for packaging of serotonin than noradrenaline and dopamine.

24
Q

What are the MAO-A inhibitors?

A

Moclobemide which targets serotonin to increase its availability. It is a treatment for depression and social anxiety.

Moclobemide is contraindicated for phaeochormocytoma and acute confusional state like delirium.

25
Q

What is the action of monoamine oxidase B?

A

Greatest affinity for packaging of dopamine.

26
Q

What is an important contraindication with the use of MAO?

A

When taking MAO, the ingestion of fermented foods high in tyramine, a precursor to monoamine like noradrenaline will result in its accumulation and a hypertensive crisis.

-> Cardiovascular disease and cerebrovascular disease.

27
Q

What are the risks with the use of combination antidepressants such as SSRIs, SNRIs and mAO inhibitors?

A

Combination use of antidepressants results in accumulation of serotonin and serotonin syndrome, characterised by MAD:
->Mental state changes
->Autonomic dysregulation of hypertension and tachycardia
->Neuromuscular abnormalities such as clonus.

28
Q

What is the treatment of the somatic symptoms of anxiety?

A

Benzodiazepines which act on the modulators site on the GABA receptor, acting as a positive allosteric modulator. It causes a conformational change to occur on the receptor which enhances the effects of GABA for the influx of Cl-.

-> Benzodiazepines are used for rapid tranquilisation to avoid physical intervention and acute treatment of anxiety.

29
Q

What are the side effects of benzodiazepines?

A

Sedation
Respiratory depression
Sleep induction with high drug concentration
Anterograde amnesia (inability to form new memories following drug use)
Anticonvulsant activity via reduction in muscle tone.

30
Q

What is monitored in rapid tranquilisation?

A

Temperature, pulse, BP, hydration, consciousness and respiratory rate.

31
Q

What is agomelatine?

A

Melatonin agonist and selective serotonin antagonist of 5HT2-C. It is indicated for major depression and can cause abdominal pain and anxiety.y

32
Q

What is reboxetine?

A

Noradrenaline reuptake inhibitor used for a treatment of major depression that can cause hypertension, akithisia and constipation.

33
Q

What are z drugs?

A

Non benzodiazepine drugs which act on the alpha subunit of the GABA receptor to cause sedation. These include zopiclome and zolpidem and have a similar risk profile like benzodiazepines for increased fill risk in elederly and intracranial pressure.

34
Q

What is an atypical antidepressant?

A

Bupropion used in smoking cessation which is a Weak dopamine and noradrenaline reuptake inhibitor to prolong the action of the neurotransmitters at the synaptic cleft and antagonises nicotinic anticholinergic receptors, used during smoking cessation and continued for weeks with gradual decline.

35
Q

Which antidepressant is commonly prescribed for those with anorexia?

A

Mirtazapine, indicated for major depression which increases noradrenergic and serotonin activity and induces weight gains and increased appetite.

36
Q

Which SSRI is ideal for use with an antidepressant?

A

Fluoxetine

37
Q

Which drugs should be avoided for pres rising with SSRIs?

A

NSAIDs due to bleeding risk
Warfarin and heparin
Aspirin
Monoamine oxidase inhibitors due to risk of serotonin syndrome

38
Q

What is the risk of citalopram use?

A

Prolonged QT inerval