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Pharmacology > Mental Health, Agitation, Alcohol > Flashcards

Mental Health, Agitation, Alcohol Flashcards

1
Q

Give 2 examples of 1st generation (typical) anti-psychotics:

A
  • Haloperidol
  • Chlorpromazine
  • Prochlorperazine
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2
Q

Give 3 indications for the use of 1st generation (typical) anti-psychotics:

A
  • urgent rx of severe psychomotor agitation
  • schizophrenia (esp. if metabolic SEs of 2nd gen are problematic)
  • bipolar disorder (esp. during acute episodes)
  • rx of N&V (esp. in palliation)
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3
Q

MOA of 1st generation (typical) anti-psychotics:

  • block post-synaptic __ receptors
  • the most effect comes from the blockade of the ___-___ pathway that runs between the ___ and the ___ cortex
  • the adverse effects can be explained by the blockade on the:
  • the anti-emetic properties can be explained by the blockade in the:
A
  • block post-synaptic D2 receptors
  • meso-limbic pathway (mid brain to frontal cortex)
  • nigrostriatal and tuberohypophyseal pathway
  • CTZ
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4
Q

Name 3 extrapyramidal/movement abnormalities that arise as adverse effects of 1st generation (typical) anti-psychotic therapy (due to D2 blockade in nigrostriatal pathway)…. one is a late SE that may not resolve on stopping medication

A
  • acute dystonic reactions (involuntary Parkinsonian movements/muscle spasms)
  • akathisia (state of inner restlessness)
  • neuroleptic malignant syndrome (rare-rigidity, confusion, autonomic dysregulation and pyrexia)
  • tardive dyskinesia (late SE.. pointless/involuntary/repetitive e.g. lip smacking)
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5
Q

Name 3 non-movement related SEs of 1st generation (typical) anti-psychotics:

A
  • drowsiness
  • hypotension
  • prolonged QT interval (&consequent arrhythmias)
  • erectile dysfunction
  • hypoprolactinaemia causing menstrual disturbance, galactorrhoea, breast pain…
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6
Q

1st generation (typical) anti-psychotics should be prescribed with caution/if possible avoided in:

A
  • the elderly (start lower doses)
  • avoid in dementia (increased risk of death and stroke)
  • avoid in Parkinson’s (due to extrapyramidal effects)
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7
Q

Name a class of drug that also prolongs the QT interval so can interact with 1st generation (typical) anti-psychotics..

A
  • amiodarone
  • macrolides
  • quinine
  • SSRIs
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8
Q

Name 2 examples of 2nd generation (atypical) anti-psychotics:

A
  • quetiapine
  • olanzapine
  • risperidone
  • clozapine
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9
Q

Give 3 indications for the use of 2nd generation (atypical) anti-psychotics:

A
  • urgent rx of severe psychomotor agitation
  • schizophrenia (esp. if extra-pyramidal SEs of 1st gen are problematic, or negative sx are prominent)
  • bipolar disorder (esp. during acute episodes)
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10
Q

2nd generation (atypical) anti-psychotics MOA:

A
  • block post-synaptic D2 receptors (“looser” binding to these)
  • higher affinity for other receptors esp. 5-HT2A –> better efficacy in rx-resistant schizophrenia, and vs. negative sx and lower risk of extra-pyramidal SEs
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11
Q

Name 3 SEs of 2nd generation (atypical) anti-psychotics:

A
  • sedation
  • (extra-pyramidal movement abnormalities but not as common as with 1st gen)
  • metabolic disturbance: weight gain, DM, lipid changes
  • prolong QT interval (–> arrythmias)
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12
Q

Risperidone specifically affects ____ pathway more, so due to effect on ___ secretion: SEs include (in both sexes)

Clozapine specific rare SEs

A

Risperidone: tuberophypophyseal pathway, prolactin secretion affected –> breast symptoms, sexual dysfuntion
Clozapine: severe def of neutrophils “agranulocytosis” and myocarditis

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13
Q

2 CIs for use of of 2nd generation (atypical) anti-psychotics:
1 caution?

A

CI: -SEVERE HEART DISEASE
CI: -NEUTROPAENIA
Caution: -cardiovascular disease, use with other dopamine-blocking anti-emetics, drugs that prolong QT interval

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14
Q

Name 3 Benzodiazepines and 3 indications for their use:

A
  • temazepam, lorazepam, chordiazepoxide, midazolam, diazepam
  • seizures/status epilepticus rx
  • alcohol withdrawal reactions
  • sedation for an interventional procedure if not candidate for GA
  • short term rx of severe/disabling anxiety or insomnia
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15
Q

Benzodiazepines MOA:

  • facilitate and enhance the binding of ___ to the ____ receptor, has a widespread ___ effect on synaptic transmission
  • what is the receptor and its function?
A
  • GABA to GABA-A receptor, depressant effect
  • GABA-A is a chloride channel that opens in response to binding by GABA (main inhibitory NT in brain)
  • opening the channel allows chloride to flow into cell, making it more resistant to depolarisation
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16
Q

Name 2 SEs of use of benzodiazepines:

What complication can lead to death if an overdose is taken?

A
  • dose-dependent drowsiness, sedation and coma
  • dependence if used for >weeks, and withdrawal reaction upon abrupt cessation
  • loss of airway reflexes in OD can –> airway obstruction and death
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17
Q

Give 3 situations in which you should exercise caution in the prescription of benzodiazepines:

A
  • elderly (more susceptible to effects, so lower dose)
  • avoid if signif respiratory impairment
  • avoid if signif neuromuscular disease (e.g. myasthenia gravis)
  • avoid in liver failure (can precipitate hepatic encephalopathy) - lorazepam choice if necessary
  • be careful of prescribing alongside CYP inhibitors (relied on for elimination so will lead to toxic levels)
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18
Q

Benzodiazepines should be avoided in liver failure (can precipitate hepatic encephalopathy) and liver and its CYP enzymes are needed for elimination of the drug.
If benzos are needed e.g. for alcohol withdrawal in a pt with liver failure, which is best choice and why?

A
  • Lorazepam

- depends less on liver for its elimination

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19
Q

Give 3 e.gs of SSRIs

Give 2 indications for their use

A
  • citalopram, sertraline, fluoxetine, escitalopram
  • moderate-severe depression, or mild depression if psychological rx are insufficient alone
  • panic disorder rx
  • obsessive compulsive disorder rx
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20
Q

SSRIs MOA

A
  • inhibit neuronal reuptake of serotonin from the synaptic cleft so increase it’s availability for neurotransmission
  • SSRIs have fewer adverse effects and less dangerous in OD than tricyclic ADs which also affect other NTs
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21
Q

SSRIs have many SEs, name 4

which SE is important esp in the elderly-can present with confusion and reduced consciousness…

A
  • GI upset
  • appetite changes
  • weight gain/loss
  • hypersensitivity reactions e.g. skin rash
  • increased suicidal thoughts/behaviour
  • prolonged QT interval (w citalopram)
  • increased bleeding risk
  • serotonin syndrome (!)
  • in elderly: hyponatraemia
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22
Q

Describe serotonin syndrome which can occur with SSRIs in high doses, in OD or in combo other serotonergic drugs e.g. antidepressants, tramadol

A

-autonomic hyperactivity
-altered mental state
-neuromuscular excitation
(responds to treatment withdrawal and supportive therapy)

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23
Q

Sudden withdrawal of SSRIs can cause…

A
  • GI upset
  • neurological sx
  • influenza-like sx
  • sleep disturbance
24
Q

In who should you exercise caution when wanting to prescribe SSRIs? (3)

A
  • caution: epilepsy, peptic ulcer disease, young people (poor efficacy and higher risk of self-harm)
  • hepatic impairment (as metabolised by liver)
25
Q

SSRIs should NOT BE USED WITH ___ INHIBITORS and other _____ drugs (e.g. tramadol) as together they may precipitate ______ ______

A
  • MAO INHIBITORS
  • OTHER SERATONERGIC DRUGS
  • SERATONERGIC DRUGS
26
Q

Antidepressants e.g. venlafaxine, mirtazapine

-these are used for rx of what? (2)

A
  • major depression when SSRIs are not effective/tolerated

- generalised anxiety disorder

27
Q

The antidepressant venlafaxine is a __and __ that interferes with uptake of these NTs from synaptic cleft
Mirtazapine is an antagonist of inhibitory pre-synaptic __ _____ and blocks ___ & ___ receptors.
Both drugs increase availability of m______ for neurotransmission

A
  • Venlafaxine is a serotonin and noradrenaline reuptake inhibitor (SNRI)
  • Mirtazapine is antagonist of a2 adrenoceptors and 5HT2 % 5HT3
  • Both drugs increase availability of monoamines
28
Q

name 3 adverse effects of the antidepressants e.g. venlafaxine, mirtazapine

A
  • GI upset (dry mouth, nausea, weight change, diarrhoea/constipation)
  • neurological SEs (headache, abnormal dreams, insomnia, confusion, convulsions)
  • hyponatraemia
  • serotonin syndrome
  • suicidal thoughts/behaviour increase
  • vanlafaxine prolongs the QT interval
  • abrupt withdrawal can -> GI, neuro, flu-like sx and sleep disturbance
29
Q

Gabapentin and pregabalin are indicated for what? Name 2 examples

A
  • add-on rx for focal epilepsies if other drugs give inadequate control
  • neuropathic pain 1st line rx e.g. diabetic neuropathy
  • pregabalin can be used for generalised anxiety disorder
30
Q

Gabapentin and pregabalin MOA relates to GABA

  • Their action occurs by binding with pre-synaptic ___
  • This inhibits the release of _____ NTs (interfering with NT release)
  • the resulting reduction of neuronal excitability in the brain explains the drugs ______ effect
  • similar effects in peripheral nerves –> reducing neuropathic pain
A
  • pre-synaptic VGCa2+Cs (voltage gates Ca2+ channels)
  • inhibits release of excitatory NTs
  • explains drugs anti-convulsant effects
31
Q

Name 1 SE of gabapentin/pregabalin?

A
  • drowsiness
  • dizziness
  • ataxia
32
Q

Lamotrigine is used for ____ prophylaxis in ____ and is an option for 1st line monotherapy or add-on therapy in ___ ___. generalised ___-____ ____ and ____ _____.
It is also used for ____ _____ (but not mania/hypomania).

A
  • seizure prophylaxis in epilepsy
  • focal seizures, generalised tonic-clonic seizures and absence seizures
  • bipolar depression treatment
33
Q

Like carbamazapine and phenytoin, lamotrigine binds to voltage sensitive neuronal ___ channels, interferring with __ influx into the neurone, this impedes repetitive firing. Also inhibits the post-synaptic glutamate ____ receptor

A
  • Na+ channels, Na+ influx

- AMPA receptor

34
Q

3 SEs of lamotrigine used for anti-epilepsy and bipolar depression treatment:
what mild SE requires urgent review of the drug?-

A
  • headache
  • drowsiness
  • irritability
  • blurred vision
  • diziness
  • GI SEs
  • skin rash (!) may be sign of hypersensitivity so discontinue immediately
35
Q

Lamotrigine is an anti-epileptic and bipolar depression rx, it is safe for use in pregnancy. In what 2 cases should it be used with caution?

A
  • pts with prior hypersensitivity to other anti-epileptic drugs
  • hepatic impairment as is metabolised by hepatic glucoronidation
36
Q

Lamotrigine is an anti-epileptic and bipolar depression rx.
Its use is cautioned in hepatic impairment as is metabolised by hepatic glucoronidation, therefore medications that induce hepatic glucoronidation can causes lamotrigine conc to fall –> rx failure vs. those that inhibit can -> toxicity.
Give 2 e.g.s of hepatic glucoronidation inducers, and one inhibitor

A

Inducers: carbamazepine, phenytoin, oestrogens, rifampicin, PIs
Inhibitors: valporate (co-administration with valporate also increases hypersensitivity risk)

37
Q

Valporate (valproic acid) e.g. sodium valporate, give 2 indications

A
  • seizure prophylaxis in epilepsy (broad-spec activity so useful vs. most seizure types, 1st line for: tonic-clonic, absence, focal and myoclonic seizures)
  • established convulsive status epilepticus not responsive to benzos
  • bipolar disorder for acute mania rx and prophylaxis vs. recurrence
38
Q

Valporate MOA relates to what 2 aspects?

A
  • weak inhibitor of neuronal Na+ channels (stabilising RMPs and reducing excitability)
  • increases brain content of GABA (inhibitory NT)
39
Q

name 4 Adverse effects of Valproate:

A
  • GI upset: nausea, gastric irritation, diarrhoea
  • neuro and psych effects: tremor, ataxia and behavioural disturbances
  • thrombocytopenia
  • transient increase in liver enzymes
  • hypersensitivity reactions: hair loss, rare, life-threatening effects of liver injury, pancreatitis, BM failure
40
Q

Give 1 CI and 2 cautions for the use of valproate either for seizure or bipolar treatment

A
  • CI: WOMEN OF CHILD-BEARING AGE (if poss)
  • CI: AROUND TIME OF CONCEPTION
  • CI: IN FIRST TRIMESTER OF PREGNANCY
  • Caution: hepatic impairment and severe renal impairment
41
Q

Valproate inhibits hepatic enzymes so it increases the concentration (&risk of toxicity) of drugs metabolised by ___ enzymes e.g. warfarin.
Valproate is itself metabolised by ___ enzymes so inducers e.g. _____, ____ reduce it’s effectiveness and inhibitors e.g. ____, ___ can increase risk of adverse effects and toxicity.

A
  • CYP
  • CYP
  • inducers e.g. phenytoin, carbamazepine –> less effective
  • inhibitors e.g. macrolides, protease inhibitors –> allow toxic concs to build up
42
Q

The following are examples of what class of medication? What are each used to treat mild-mod forms of what disease (2)?

  • Donepezil:
  • Rivastigmine:
A

Acetylcholinesterase Inhibitors

  • Donepezil: Alzheimer’s disease
  • Rivastigmine: Dementia in Parkinson’s disease
43
Q

What are the most common SEs of Acetylcholinesterase Inhibitors due to their increasing _____ activity in the peripheral NS.

A
  • increasing cholinergic activity

- nausea, diarrhoea, vomiting

44
Q

Pts with what chronic conditions may experience worsening of symptoms upon commencing an Acetylcholinesterase Inhibitor?

A

-Asthma or COPD

45
Q

Acetylcholinesterase Inhibitors rarely can cause peptic ulcers, bleeding, and what cardiac effects? Central effects include what unnerving sxs?

A
  • bradycardia, heart block

- central effects: hallucinations, altered/aggressive behaviour

46
Q

Suggest 3 groups to caution the use of Acetylcholinesterase Inhibitors in and one CI:

A
  • caution: asthma, COPD, those at risk of peptic ulcers

- CI: HEART BLOCK or SICK SINUS SYNDROME

47
Q

Based on the following info for Acetylcholinesterase Inhibitors, suggest some interactions:

  • risk: small risk of extrapyramidal SEs and neuroleptic malignant syndrome
  • caution: asthma, COPD, those at risk of peptic ulcers
  • CI: HEART BLOCK or SICK SINUS SYNDROME
A
  • concomitant therapy with NSAIDs and steroids will increase peptic ulcer risk
  • use with antipsychotics increase risk of neuroleptic malignant syndrome
  • concomitant therapy with rate-limiting meds e.g. B-blocker increased brady/heart block risk
48
Q

N-acetylcysteine is used for 3 indications:

  • an antidote vs what?
  • to prevent renal injury in the context of what?
  • and to reduce viscosity of what?
A
  • antidote vs paracetamol OD
  • prevent injury due to radiographic contrast nephropathy
  • reduce viscosity of respiratory secretions (a mucolytic)
49
Q

In paracetamol OD, some is converted to the hepatotoxic imine NAPQI. This should be detoxified by conjugation with ______ but in OD levels the supply is overwhelmed so liver damage accumulates. How does acetylcysteine work in this context?

A
  • glutathione

- replenishes body’s supply of glutathione

50
Q

IV N-acetylcysteine administered IV in paracetamol OD carries risk of anaphylactoid reaction, how does this differ from anaphylaxis (think pathophys and in terms of future rx)

A
  • anaphylactoid involves histamine release independent of IgE
  • so once reaction has settled (stopped infusion, given anti-histamine)
  • its safe to restart N-AC at a lower rate
51
Q

NB: if using N-acetylcysteine as a mucolytic (like carbocysteine), a bronchodilator is usually given just before hand. Why?

A

-to decrease risk of bronchospasm which can occur when nebulised N-acetylcysteine is administered

52
Q

Someone given N-acetylcysteine for paracetamol OD, should have which blood tests measured at presentation and on completion of the rx to track the liver injury trajectory? name 2

A
  • INR
  • serum ALT
  • creatinine concentration
53
Q

Lofepramine and amitriptyline are 2nd line for treatment of what? and are commonly prescribed (unlicensed) for what?

A
  • mod-severe depression if SSRIs ineffective

- for neuropathic pain

54
Q

Tricyclic antidepressants work by inhibiting neuronal uptake of which 2 NTs from the synaptic cleft.

A
  • seratonin

- noradrenaline

55
Q

Suggest 3 sx of tricyclic antidepressant overdose:

A
  • severe hypotension
  • arrhythmias
  • convulsions
  • coma
  • respiratory failure
56
Q

Due to tricyclic antidepressant’s anti-muscarinic effects, suggest 3 groups in which their use should be treated with caution?

A
  • elderly
  • epileptic pts
  • cardiovascular disease (arrythmia and long QT risk)
  • prostatic hypertrophy (urinary retention risk)
  • glaucoma (blurred vision risk)
  • those prone to constipation
57
Q

Name a withdrawal sx if TCAs are stopped suddenly:

A
  • flu like symptoms

- insomnia

Pharmacology (14 decks)

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