Drugs Flashcards

1
Q

Benzodiazepines

A

Benzodiazepines enhance the effect of the INHIBITORY neurotransmitter gamma-aminobutyric acid (GABA) by increasing the frequency of chloride channels. They therefore are used for a variety of purposes:

  • sedation
  • hypnotic
  • anxiolytic
  • anticonvulsant
  • muscle relaxant

Patients commonly develop a tolerance and dependence to benzodiazepines and care should therefore be exercised on prescribing these drugs. The Committee on Safety of Medicines advises that benzodiazepines are only prescribed for a short period of time (2-4 weeks).

The BNF gives advice on how to withdraw a benzodiazepine. The dose should be withdrawn in steps of about 1/8 (range 1/10 to 1/4) of the daily dose every fortnight. A suggested protocol for patients experiencing difficulty is given:
switch patients to the equivalent dose of diazepam
reduce dose of diazepam every 2-3 weeks in steps of 2 or 2.5 mg
time needed for withdrawal can vary from 4 weeks to a year or more

If patients withdraw too quickly from benzodiazepines they may experience benzodiazepine withdrawal syndrome, a condition very similar to alcohol withdrawal syndrome. This may occur up to 3 weeks after stopping a long-acting drug. Features include:
insomnia
irritability
anxiety
tremor
loss of appetite
tinnitus
perspiration
perceptual disturbances
seizures
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2
Q

Antipsychotics - mechanism

A

Act as D2 receptor antagonists, blocking dopaminergic transmission in the MESOLIMBIC pathways.

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3
Q

Antipsychotics - side effects

A

Typical antipsychotics are associated with Extrapyramidal side -effects (EPSEs):

  • Parkinsonism
  • acute dystonia: sustained muscle contraction (e.g.torticollis. oculogyric crisis),
  • akathisia
  • tardive dyskinsea (late onset of choreoathetoid movements, abnormal, involuntary, may occur in 40% of patients, may be irreversible, most common is chewing and pouting of jaw)
    - EPSEs may be managed with PROCYCLINE

Specific warnings when antipsychotics are used in elderly patients:
- increased risk of STROKE
increased risk of venous thromboembolism -VTE

Other side-effects:

  • antimuscarinic: dry mouth, blurred vision, urinary retention, constipation
  • sedation, weight gain
  • raised prolactin
    • may result in galactorrhoea
    • due to inhibition of the dopaminergic tuberoinfundibular pathway
  • impaired glucose tolerance
  • neuroleptic malignant syndrome: pyrexia, muscle stiffness
  • reduced seizure threshold (greater with atypicals)
  • prolonged QT interval (particularly haloperidol)
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4
Q

Zopiclone and the risk to elderly

A

Increases the risk of FALLS

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5
Q

Depression: switching antidepressants

A

Switching from citalopram, escitalopram, sertraline, or paroxetine to another SSRI:
- the first SSRI should be withdrawn (this means gradually reduce the dose then stop) before the alternative SSRI is started

Switching from fluoxetine to another SSRI:
- withdraw then leave a gap of 4-7 days (as it has a long half-life) before starting a low-dose of the alternative SSRI

Switching from a SSRI to a tricyclic antidepressant (TCA):

  • cross-tapering is recommend (the current drug dose is reduced slowly, whilst the dose of the new drug is increased slowly)
  • an exceptions is fluoxetine which should be withdrawn prior to TCAs being started

Switching from citalopram, escitalopram, sertraline, or paroxetine TO VENLAFAXINE
- cross-taper cautiously. Start venlafaxine 37.5 mg daily and increase very slowly

Switching from fluoxetine to venlafaxine
- withdraw and then start venlafaxine at 37.5 mg each day and increase very slowly

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6
Q

Side effects of Mirtazapine

A
  • large increase in APPETITE (and subsequent weight gain)

- DROWNISNESS.

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7
Q

SSRIs and pregnancy?

A
  • BNF says to weigh up benefits and risk when deciding whether to use in pregnancy.
  • Use during the first trimester gives a small increased risk of congenital heart defects
  • Use during the third trimester can result in persistent pulmonary hypertension of the newborn

Paroxetine has an increased risk of congenital malformations, particularly in the first trimester

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8
Q

What is Venlafaxine?

A

An antidepressant

Used in the treatment of major depression, anxiety and panic disorder

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9
Q

Mechanism of action of Venlafaxine

A

Serotonin and noradrenaline reuptake inhibitor (SNRI)

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10
Q

SNRI mode of action, examples and uses

A

Serotonin and noradrenaline reuptake inhibitor (SNRI’s) are a class of relatively new antidepressants. Inhibiting the reuptake increases the concentrations of serotonin and noradrenaline in the synaptic cleft leading to the effects.

Examples include venlafaxine and duloxetine.

They are used to treat major depressive disorders, generalised anxiety disorder, social anxiety disorder and panic disorder and menopausal symptoms.

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11
Q

What is clomipramine?

A

TCA

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12
Q

Common side effect of clozapine

A

Constipation/intestinal obstruction

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13
Q

Adverse effects of atypical antipsychotics?

A
  • Weight gain
  • Clozapine is associated with agranulocytosis
  • hyperprolactinaemia
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14
Q

Examples of atypical antipsychotics

A
  • clozapine
  • olanzapine: higher risk of dyslipidemia and obesity
  • risperidone
  • quetiapine
  • amisulpride
  • aripiprazole: generally good side-effect profile, particularly for prolactin elevation
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15
Q

Adverse effects of clozapine

A
  • agranulocytosis (1%), neutropaenia (3%)
  • REDUCED SEIZURE THRESHOLD - can induce seizures in up to 3% of patients
  • constipation
  • myocarditis: a baseline ECG should be taken before starting treatment
  • hypersalivation
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16
Q

SSRI adverse effects?

A
  • GI symptoms - increased risk of GI bleeding. therefore PPI should be prescribed
  • HYPOnatraemia
  • patients should be counselled to be vigilant for increased anxiety and agitation after starting a SSRI
  • Fluoxetine and paroxetine have a tiger propensity for drug interactions
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17
Q

SSRIs and interactions?

A
  • NSAIDs: NICE guidelines advise ‘do not normally offer SSRIs’, but if given co-prescribe a proton pump inhibitor
  • warfarin / heparin: NICE guidelines recommend avoiding SSRIs and considering mirtazapine
  • aspirin
  • triptans: avoid SSRIs as increased risk of serotonin syndrome
  • monoamine oxidase inhibitors (MAOIs) - increased risk of serotonin syndrome
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18
Q

What is agranulocytosis a side effect of?

A

Clozapine

Agranulocytosis is the lowering of the white blood cell count, primarily neutrophils, as a consequence the abnormality found in the blood test results will be decreased leukocytes.

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19
Q

What is clozapine used in the treatment of?

A

Resistant schizophrenia

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20
Q

ECT therapy?

A
Short-term side-effects: 
- headache
- nausea
- short term memory impairment
memory loss of events prior to ECT
- cardiac arrhythmia

Long-term side-effects:
- some patients report impaired memory

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21
Q

Guidance on using hypnotics

A
  • The hypnotics recommended for treating insomnia are short-acting BENZODIAZEPINES or NON-BENZODIAZEPINES (zopiclone, zolpidem and zaleplon).
  • Diazepam is not recommended but can be useful if the insomnia is linked to daytime anxiety.
  • Use the lowest effective dose for the shortest period possible.
  • If there has been no response to the first hypnotic, doNOT prescribe another. You should make the patient aware that repeat prescriptions are not usually given.
  • It is important to review after 2 weeks and consider referral for cognitive behavioural therapy (CBT).
22
Q

What drugs can cause hyperprolactinaemia?

A

Risperidone

Amisulpride

23
Q

What are the effects of hyperprolactinaemia?

A

Can involve:

  • breast tenderness
  • breast enlargement
  • lactation
24
Q

If risperidone is causing side effects - what could you change to?

A

Aripiprazole

its known for its having fewer side effects especially with respect to prolactin elevation

25
Q

Which drug can be affected by smoking?

A

Clozapine - the dose may need to be changed if starting or stopping smoking

26
Q

Mechanism of antipsychotics?

A

Dopamine antagonists

- so would cause hyPERprolacrinaemia as dopamine is a prolactin agonist

27
Q

What is more likely to cause weight gain?

Atypical or typical antipsychotics?

A

Atypical

28
Q

TCAs common side effects

A
  • drowsiness
  • dry mouth
  • blurred vision
  • constipation
  • urinary retention
  • lengthening of QT interval
29
Q

Choice of tricyclic

A
  • low-dose amitriptyline is commonly used in the management of neuropathic pain and the prophylaxis of headache (both tension and migraine)
  • lofepramine has a lower incidence of toxicity in overdose
  • amitriptyline and dosulepin (dothiepin) are considered the most dangerous in overdose
30
Q

What are the more sedative TCAs

A

Amitriptyline
Clomipramine
Dosulepin
Trazodone*

31
Q

What are the less sedative TCAs

A

Imipramine
Lofepramine
Nortriptyline

32
Q

What can be used to treat moderate/severe tar dive dyskinesia?

A

Tetrabenazine

33
Q

What class of drugs does amitriptyline fall into?

A

TCAs

34
Q

What type of incontinence occurs in TCAs?

A

OVERFLOW incontinence

- TCAs have anticholinergic effects which may lead to urinary retention, leading to frequent leaking.

35
Q

Serious side effects of clozapine

A
  • Weight gain
  • excessive salivation
  • agranulocytosis
  • neutropenia
  • myocarditis
  • arrhythmias
36
Q

What do you do if clozapine doses are missed for 48 hours?

And why?

A
  • RE-TITRATE the clozapine doses again slowly (will need to be restarted again slowly) - like when they first started on it
  • you do this because when you start Clozapine after a break of >48 hours, it can make side effects worse, such as BP changes, drowsiness and dizziness.

If there is a gap in treatment of 3 days (72 hours) then you may also rewire more frequent blood tests for a short period

37
Q

What is the choice of SSRI post MI?

A

Sertraline

38
Q

What is the SSRI of choice in children and adolescents?

A

Fluoxetine

39
Q

What is the mechanism of action of lithium

A

Its not fully understood
2 theories:
- interferes with inositol triphosphate formation
- interferes with cAMP formation

40
Q

What are the adverse effects of lithium?

A
  • nausea/vomiting, diarrhoea
  • fine tremor
  • nephrotoxicity: polyuria, secondary to nephrogenic diabetes insipidus
  • thyroid enlargement, may lead to hypOthyroidism
  • ECG: T wave flattening/inversion
  • weight gain
  • idiopathic intracranial hypertension
  • leucocytosis
    hyperparathyroidism and resultant hypercalcaemia
41
Q

Monitoring of patients on lithium therapy

A
  • inadequate monitoring of patients taking lithium is common - NICE and the National Patient Safety Agency (NPSA) have issued guidance to try and address this.
  • after starting lithium levels should be performed WEEKLY and after each dose change until concentrations are STABLE
  • once established, lithium blood level should ‘normally’ be checked every 3 months
  • after a change in dose, lithium levels should be taken a week later and 12 hours after the last dose
  • thyroid and renal function should be checked every 6 months
  • patients should be issued with an information booklet, alert card and record book
42
Q

Why would someone prescribe Mirtazapine? and what is this drug?
How does it work?

A

Antidepressant

  • preserved due to its useful side effects
  • its known to stimulate APPETITE

works by blocking alpa 2 adrenergic receptors

Mirtazapine has FEWER SIDE EFFECTS and interactions than many other antidepressants and so is useful in OLDER PEOPLE who may be affected more or be taking other medications. Two side effects of mirtazapine, SEDATION and an INCREASED APPETITE, can be beneficial in older people that are suffering from insomnia and poor appetite.

It is generally taken in the evening as it can be sedative.

43
Q

Monoamine oxidase inhibitors - overview, examples of non -selective monoamine oxidase inhibitors, adverse effects

A

Overview
- serotonin and noradrenaline are metabolised by monoamine oxidase in the presynaptic cell

Non-selective monoamine oxidase inhibitors

  • e.g. tranylcypromine, phenelzine
  • used in the treatment of atypical depression (e.g. hyperphagia) and other psychiatric disorder
  • not used frequently due to side-effects

Adverse effects of non-selective monoamine oxidase inhibitors

  • hypertensive reactions with tyramine containing foods e.g. cheese, pickled herring, Bovril, Oxo, Marmite, broad beans
  • anticholinergic effects (DRY)
44
Q

What class of drugs is Amitriptyline? And effects from it ?

A

Tricyclic antidepressants

anticholinergic effects
- therefore associated with tachycardia, dry mouth, mydriasis and urinary retention.

45
Q

What are the effect of SSRI on GI?

A

Increased incidence of GI bleeding

therefore give a PPI

46
Q

How long do you have to gradually withdraw SSRI? And which one is not the same and why?

A

over a 4 week period

This not necessary with fluoxetine due to its longer half-life.

47
Q

What is the risk of using SSRIs in the first trimester and third?

A

small increased chance of congenital heart defects

Use during the third trimester can result in persistent pulmonary hypertension of the newborn

Paroxetine has an increased risk of congenital malformations, particularly in the first trimester

48
Q

What is the use of SSRIs in the third trimester?

A

Risk of PULMONARY HYPERTENSION of the newborn

49
Q

What is the first line treatment for delirium tremens?

A

Oral chlordiazepoxide

50
Q

What class of drugs is Mirtazapine? How does it work?

A
  • a noradrenergic and specific serotonergic antidepressant

- blocks alspha2 adrenergic receptors