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pharmacology > CNS > Flashcards

CNS Flashcards

1
Q

What class of medications are diazepam, lorazepam?

A

Anxiolytics

Benzodiazepines

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2
Q

What class of medications are diazepam, lorazepam, temazepam, midazolam?

A

Benzodiazepines

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3
Q

What are the indications for prescribing benzodiazepines such as diazepam, lorazepam

A

First line for management of seizures and status epilepticus
First line management of alcohol withdrawal reaction
Sedation for interventional procedures when general anaesthetic is unsuitable
Short term treatment of severe anxiety
Short term treatment of severe insomnia

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4
Q

What is the mechanism of action of benzodiazepines?

A

Enhance binding of GABA to its receptor, allowing chloride to flow into cell and making cell more resistant to depolarisation. This has a depressant effect upon synaptic transmission, causing reduced anxiety, sleepiness, and anticonvulsant effects. Alcohol also acts on GABAa receptor.

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5
Q

What class of medication are haloperidol, chlorpromazine and prochlorperazine?

A

Antipsychotics, first generation, typical

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6
Q

What are the indications for prescribing first generation antipsychotics such as haloperidol or chlorpromazine?

A

Urgent treatment of psychomotor agitation causing dangerous or violent behaviour
Schizophrenia
Bipolar disorder, particularly acute episodes
Nausea and vomiting, in a palliative care setting

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7
Q

What is the mechanism of action of antipsychotics such as haloperidol or chlorpromazine?

A

Block post synaptic dopamine D2 receptors of the mesolimbic/mesocortical pathway and chemoreceptors trigger zone (anti nausea and vomiting effects)

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8
Q

What class of medications are olanzapine, quetiapine, risperidone, clozapine?

A

Antipsychotics, second generation, atypical

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9
Q

What are the indications for prescribing atypical antipsychotics such as olanzapine, quetiapine, risperidone, clozapine?

A

Urgent treatment of psychomotor agitation leading to dangerous or violent behaviour, and permit assessment
Schizophrenia, especially when extrapyramidal side effects of typical antipsychotics are pertinent or when negative effects are prominent
Bipolar disorder, particularly in acute episodes of mania or hypomania

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10
Q

What is the mechanism of action of second generation antipsychotics such as olanzapine, quetiapine, risperidone, clozapine?

A

Block post synaptic dopamine D2 receptors particularly in the mesolimbic/mesocortical pathway. Fewer side effects than first generation and less treatment resistance in schizophrenia patients.

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11
Q

What are the contraindications for antipsychotics?

A

Heart disease, they can prolong the QT interval causing arrhythmias

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12
Q

What are the indications for valproate?

A

Epilepsy, first line medication for generalised or absent seizures. Option for focal seizures
Bipolar disorder, for treatment of manic episodes or prophylaxis of recurrance

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13
Q

What is the mechanism of action of valproate?

A

Inhibitor of neuronal sodium channels, stabilising resting membrane potentials and reducing neuronal excitability. Also increases brain GABA content, principal inhibitory neurotransmitter and regulates neuronal excitability. Full mechanism poorly understood.

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14
Q

What are the side effects of valproate?

A

Incompatible with pregnancy, foetal abnormalities
Thrombocytopenia
GI upset
Hypersensitivity resulting in hair loss and liver injury

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15
Q

What are the indications for lithium?

A

Bipolar disorder

Major depressive disorder, schizophrenia when alternative treatment is not effective

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16
Q

What are the complications of using lithium?

A

Needs regular serum level tests and monitoring of thyroid and kidney function, as it interferes with regulation sodium and water levels in the body. Inhibits ADH.
Adverse effects include confusion, constipation, thirst, polyuria, twitching, vomiting, hypothyroidism, kidney damage
Incompatible with pregnancy

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17
Q

What is the mechanism of action of lithium?

A

Widely dispersed within the CNS and interacts with many neurotransmitters and receptors. Decreases norepinephrine and increases serotonin, inhibits ADH. Specific mechanism unknown

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18
Q

What class of drugs are amitriptyline and lofepramine?

A

Antidepressants, tricyclics and related

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19
Q

What are the indications for prescribing tricyclics antidepressants such as amitriptyline and lofepramine?

A

Second line treatment for moderate to severe depression, behind SSRIs
Treatment for neuropathic pain and ADHD

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20
Q

What is the mechanism of action of tricyclics antidepressants such as amitriptyline, imipramine and lofepramine?

A

Inhibit neuronal reuptake of serotonin (5HT) and noradrenaline from synaptic cleft, increasing their availability for neurotransmission.
Also block a wide array of receptors including muscarinic, histamine, alpha adrenergic, and dopamine, which causes adverse effects and limits their clinical utility.

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21
Q

What are the contraindications for tricyclics antidepressants such as amitriptyline, imipramine and lofepramine?

A

Elderly, cardiovascular disease (can cause arrhythmias and ECG changes), epilepsy, constipation, prostatic hypertrophy, raised intraoccular pressure ect
Should not be given with monoamine oxidase inhibitors which also increases serotonin levels

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22
Q

What class of medication are citalopram, fluoxetine, sertraline?

A

Antidepressants, selective serotonin reuptake inhibitors SSRIs

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23
Q

What are the indications for prescribing SSRIs?

A

First line treatment for moderate to severe depression, and mild depression if psychological treatments fail.
Panic disorder
Obsessive compulsive disorder

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24
Q

What is the mechanism of action of SSRIs?

A

Selectively inhibit neuronal reuptake of serotonin (5HT) from the synaptic cleft, thereby increasing its availability for neurotransmission.
Less diverse effects than tricyclics as do not cause blockade of other receptors, although efficacy is similar

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25
Q

What are the contraindications of SSRIs?

A

Epilepsy, peptic ulcer disease, hepatic impairment.
Poor efficacy in young people.
Should not be given alongside monoamine oxidase inhibitors as these also increase synaptic serotonin levels.
Should not be withdrawn suddenly

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26
Q

What tyoe of medication are venlafaxine and mirtazapine?

A

Antidepressants

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27
Q

What are the indications for prescribing venlafaxine or mirtazapine?

A

Treatment of major depression where first line SSRIs are ineffective.
Generalised anxiety disorder (venlafaxine)

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28
Q

What is the mechanism of action of venlafaxine?

A

Serotonin and noradrenaline reuptake inhibitor SNRI, interfering with uptake of hers neurotransmitters into the synaptic cleft.
Increase availability of monoamines for neurotransmission.
Weaker antagonist of muscarinic and histamine receptors than tricyclic antidepressants

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29
Q

What is the mechanism of action of mirtazapine?

A

Antagonist of inhibitory presynaptic alpha2 adrenoreceptors.

Increase availability of monoamines for neurotransmission

30
Q

What are the indications for orlistat?

A

Treatment of obesity

31
Q

What is the mechanism of action of orlistat?

A

Inhibits gastric and pancreatic lipase, preventing the break down of triglycerides in the intestine, thus preventing their absorption.
Beware that is inpedes absorption of fat soluble vitamins as well, so A, D K, E supplements should be taken alongside medication

32
Q

What class of medications are cyclizine, cinnarizine, promethazine?

A

Antiemetic, histamine H1receptor antagonists

33
Q

What are the indications for histamine H1receptor antagonists such as cyclizine?

A

Prophylaxis and treatment of nausea and vomiting, particularly in the context of motion sickness and vertigo.

34
Q

What is the mechanism of action of histamine H1receptor antagonists such as cyclizine?

A

Block the ‘vomiting centre’ in the medulla which predominantly has histamine H1 and acetylcholine (muscarinic) receptors. Blocks communication with vestibular system.

35
Q

What class of medication are metoclopramide, domperidone?

A

Antiemetic, dopamine D2receptor antagonists

36
Q

What are the indications for prescribing dopamine D2 receptor antagonists such as metoclopramide, domperidone?

A

Prophylaxis and treatment of nausea and vomiting, particularly in the context of reduced gut motility.
Most effective in nausea and vomiting due to CTZ (chemoreceptors trigger zone) stimulation and due to reduced gut motility

37
Q

What is the mechanism of action of dopamine D2receptor antagonists such as metoclopramide, domperidone?

A

Nausea and vomiting are caused by a number of factors which converge on the ‘vomiting centre’ of the medulla, which receives input from chemoreceptor trigger zone, in which D2 receptor is main receptor.
Dopamine is also an important neurotransmitter in he gut, where it promotes relaxation of stomach and lower oesophageal sphincter, and inhibits gastroduodenal coordination. Prokinetic effect, promoting gastric emptying.
Risk of extrapyramidal side effects

38
Q

What class of medication do ondansetron and granisetron belong to?

A

Antiemetics, Serotonin 5 HT 3 receptor antagonists

39
Q

What are the indications for serotonin 5 HT 3 receptor antagonists such as ondansetron?

A

Prophylaxis and treatment of nausea and vomiting, particularly in the context of general anaesthesia and chemotherapy

40
Q

What is the mechanism of action of serotonin 5 HT 3 receptor antagonists such as ondansetron?

A

Nausea and vomiting are caused by a number of factors which converge on the ‘vomiting centre’ of the medulla, which receives input from chemoreceptor trigger zone, in which there is a high density of 5 HT 3 receptors. These are responsible for detecting emetogenic substances in the blood, e.g. drugs. Serotonin is the key neurotransmitter released by the gut in response to emetogenic stimuli, and acts on 5 HT3 receptors which activates the vagus nerve and in turn vomiting centre.
Therefore effective for nausea and vomiting due to CTZ activation, but not motion sickness

41
Q

What are the indications for prescribing paracetamol?

A

First line analgesic for acute and chronic pain.

Antipyretic that can reduce fever and it’s associated symptoms.

42
Q

What is the mechanism of action of paracetamol?

A

Weak selective COX 2 inhibitor. Increases pain threshold and reduces prostaglandin PG2 concentrations in thermoregulatory region of hypothalamus.
Only a weak anti inflammatory as actions inhibited by presence of peroxides
Full mechanism poorly understood.

43
Q

What class of drugs are morphine, diamorphine, oxycodone?

A

Strong opioids

44
Q

What are the indications for prescribing morphine?

A

Rapid relief of acute severe pain
For relief of severe chronic pain, when paracetamol, NSAIDs and weak opioids are ineffective
For relief of breathlessness in end of life care
To relieve breathlessness in acute pulmonary oedema alongside oxygen, furosemide and nitrates

45
Q

What is the mechanism of action of strong opioids?

A

Activate opioid mu receptors in the CNS (GPCRs). This, overall, reduces neuronal excitability and pain transmission. In medulla, they blunt response to hypoxia and hypercapnia, reducing respiratory drive. Reduce sympathetic nervous system activity, reducing myocardial oxygen demand in MI.
Beware tolerance and dependency with chronic use.

46
Q

To which class of drugs do tramadol, codeine, dihydrocodeine belong to?

A

Weak opioids

47
Q

What are the indications for prescribing weak opioids?

A

Mild to moderate pain, including post operative pain, as second line agents when simple analgesics are ineffective

48
Q

What is the mechanism of action of weak opioids?

A

Agonists of opioid mu receptors. Metabolised in liver to produce very small amounts morphine or dihydromorphine.

49
Q

What are the indications for prescribing carbamazepine?

A

Epilepsy, first line treatment for focal seizures and for primary generalised seizures
Trigeminal neuralgia, first line to control pain and reduce frequency and severity of attacks
Bipolar disorder, an option for prophylaxis of patients resistant to other medication

50
Q

What is the mechanism of action of carbamazepine?

A

Inhibits neuronal sodium channels, stabilising resting membrane potentials and reducing neuronal excitability.
Incompletely understood mechanism.
Metabolised by CYP450

51
Q

What are the indications for phenytoin?

A

To control seizures in status epilepticus, where benzodiazepines are ineffective
To reduce frequency of generalised or focal seizures in epilepsy, although other drugs with fewer side effects generally preferred

52
Q

What is the mechanism of action of phenytoin?

A

Reduces neuronal excitability and electrical conductance among brain cells, inhibiting spread of seizure activity. Binds to neuronal sodium channels in their inactive state, prolonging inactivity.
May have similar effect on cardiac purkinje fibres, causing arrhythmias.

53
Q

What is the mechanism of action of lamotrigine?

A

Sodium channel blocker, but has broad spectrum and also acts suppressing glutamate and aspartate, two dominant excitatory neurotransmitters in the CNS.

54
Q

What are the indications for lamotrigine use?

A

Epilepsy

Bipolar disorder

55
Q

What class of drugs are levodopa, ropinirole, pramipexol?

A

Dopaminergic drugs for Parkinson’s disease

56
Q

What are the indications for dopaminergic drugs in Parkinson’s disease such as ropinirole, pramipexol?

A

Early Parkinson’s disease

Secondary Parkinsonism

57
Q

What are the indications for dopaminergic drugs in Parkinson’s disease such as levodopa?

A

Later Parkinson’s disease, as dopamine agonist add on therapy
Secondary Parkinsonism

58
Q

What is the mechanism of action of dopaminergic drugs such as ropinirole and pramipexol for Parkinson’s disease?

A

Selective agonists for the D2 receptor, which predominates in the striatum, acting to increase dopaminergic stimulation.

There is a deficiency of dopamine in the nigrostriatal pathway, linking the substantia nigra (in the midbrain) to the corpus striatum (basal ganglia). This causes greater inhibition of thalamus, reducing excitatory input to motor cortex. Cannot give dopamine itself as does not cross BBB

59
Q

What is the mechanism of action of dopaminergic drugs such as levodopa for Parkinson’s disease?

A

Precursor of dopamine that can enter brain via membrane transporter.
There is a deficiency of dopamine in the nigrostriatal pathway, linking the substantia nigra (in the midbrain) to the corpus striatum (basal ganglia). This causes greater inhibition of thalamus, reducing excitatory input to motor cortex. Cannot give dopamine itself as does not cross BBB

60
Q

What is memantine used for?

A

Dementia, Alzheimer’s disease
Particularly when acetylcholinesterase inhibitors are unsuitable, or alongside such in worsening disease.
Used for moderate to severe disease.

61
Q

What is the mechanism of action of memantine?

A

Acts on the glutamatergic system by blocking the NMDA receptors, regulating its activity, and improving prognosis of Alzheimer’s. Helps improve mental function and ability to carry out ADLs.

62
Q

What class of medications do donepezil, rivastigmine and galantamine belong to?

A

Cholinesterase inhibitors

63
Q

What would be indications for broad spectrum penicillins such as amoxicillin and co-amoxiclav?

A

Empirical treatment of pneumonia
Empirical treatment of urinary tract infections
Part of combination of treatment for hospital acquired infections or intra abdominal sepis
Part of combination of treatment for H pylori associated peptic ulcers

64
Q

What is the mechanism of Cholinesterase inhibitors in Alzheimer’s disease?

A

Prevent the breakdown of acetylcholine, maintaining its levels high and slowing the worsening of symptoms.
Used for mild to moderate disease.

65
Q

What is lorazepam often used for?

A

To treat anxiety disorders, active seizures, alcohol withdrawal, trouble sleeping
Short term use only advised

66
Q

What is midazolam often used for?

A

Anaesthesia, procedural sedation, trouble sleeping, severe agitation

67
Q

What are SNRIs (serotonin noradrenaline reuptake inhibitors) used for?

A

Depression, anxiety disorders, OCD, ADHD,

68
Q

What is the mechanism of action of SNRIs (serotonin noradrenaline reuptake inhibitors)? E.g. duloxetine, venlafaxine

A

Monoamine reuptake inhibitors. Inhibit reuptake of serotonin and noradrenaline.

69
Q

What is the mechanism of action of monoamine oxidase inhibitors?

A

Inhibit the activity of one of both monoamine oxidase enzymes (A and B), thereby increasing the availability of the neurotransmitters.
A prevents breakdown of serotonin, melatonin, adrenaline, and noradrenaline
B prevents breakdown of phenethylamine and other trace amines
Both effect dopamine equally

70
Q

What are monoamine oxidase inhibitors used for?

A

Antidepressants. Also panic, agoraphobia, PTSD and social disorder.

pharmacology (9 decks)

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