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Mechanism of Drug Action (Drugs) > Neuropharmacology (Drugs - Specific) > Flashcards

Neuropharmacology (Drugs - Specific) Flashcards

1
Q

What are examples of clot busting drugs used in treating stroke?

A

Recombinant tissue plasminogen activators (rt-PA):

  1. Alteplase
  2. Duteplase
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2
Q

What are drugs used to prevent stroke (prophylaxis)?

A
  1. Statins: Reduces atherosclerosis
  2. Aspirin: Reduced blood clotting
  3. ACE inhibitors: Reduces blood pressure
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3
Q

How can phobias be treated?

A

Benzodiazepines

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4
Q

How can panic disorders be treated?

A
  1. Benzodiazepines
  2. Antidepressants
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5
Q

How can post-traumatic stress disorder be treated?

A
  1. Antidepressants
  2. β-blockers
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6
Q

How can general anxiety disorders be treated?

A
  1. Benzodiazepines
  2. Buspirone
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7
Q

What is the mechanism of action of buspirone?

A

5-HT1A agonist

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8
Q

How can obsessive compulsive disorders be treated?

A

Antidepressants

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9
Q

What are the drugs that induce sleep?

A
  1. Temazepam
  2. Zolpidem
  3. Trazodone
  4. Promethazine
  5. Ramelteon
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10
Q

What is the mechanism of action of temazepam in sleep induction?

A
  • Benzodiazepine
  • Enhances action of GABA on GABAA receptor
  • Promotes sleep-inducing effects of GABAinergic neurones
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11
Q

What is the mechanism of action of zolpidem in sleep induction?

A
  • Z-drug
  • Enhances effects of GABA on GABAA
  • Promotes sleep-inducing effects of GABAinergic neurones
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12
Q

What is the mechanism of action of trazodone in sleep induction?

A
  • Antidepressant
  • Inhibition of 5-HT2 receptors
  • Inhibits wakefulness-promoting effects of 5-HT neurones
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13
Q

What is the mechanism of action of promethazone in sleep induction?

A
  • Antihistamine
  • Inhibition of histamine H1 receptors
  • Inhibits wakefulness-promoting effects of histaminergic neurones
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14
Q

What is the mechanism of action of ramelteon in sleep induction?

A
  • Melatonin MT1 anf MT2 receptor agonists
  • Promotes sleep-inducing effects of melatonin
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15
Q

What are the drugs that induce wakefulness?

A
  1. Amphetamine
  2. Caffeine
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16
Q

What is the mechanism of action of amphetamine in wakefulness induction?

A
  • Inhibitor of NET, reducing synaptic uptake of NA
  • Inhibitor of VMAT, causing leakage of NA into synpatic clefts from pre-synpatic terminal
  • Promotes wakefulness-inducing effects of NA
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17
Q

What is the mechanism of action of caffeine in wakefulness induction?

A
  • Antagonist of adenosine receptors
  • Inhibits sleep-inducing effects of adenosine
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18
Q

What are the types of drugs used to treat epilepsy?

A
  1. Nav inhibitors
  2. Cav channel inhibitors
  3. Enhancers of GABA transmission
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19
Q

What is the mechanism of action of Nav inhibitors in treating epilepsy?

A
  • They show use-dependent block and stabilied the inactivated conformation of Navs, reducing CNS activity during seizures.
  • Due to their use-dependence, they don’t inhibit normal CNS activity but do inhibit when there is over-activity during seizures.
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20
Q

What are examples of Nav inhibitors used to treat epilepsy?

A
  1. Phenytoin
  2. Valproate
  3. Lamotrigine
  4. Carbamazepine
  5. Oxcarbazapine
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21
Q

What are examples of Cav inhibitors used to treat epilepsy?

A
  1. Ethosuximide/trimethadione
  2. Gabapentin
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22
Q

What is the mechanism of ethosuximide/trimethadione in treating epilepsy?

A
  • T-type Cav inhibitor
  • T-type Cavs are important in maintaining absence seizures
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23
Q

What is the mechanism of gabapentin in treating epilepsy?

A
  • L-type Cav inhibitor
24
Q

What are examples of drugs that enhance GABA transmission in treating epilepsy?

A
  1. Vigabatran
  2. Valproate
  3. Taigabine
  4. Barbiturates
  5. Benzodiazepines
25
Q

What is the mechanism of vigabatrin in treating epilepsy?

A
  • Inhibitor of GABA transaminase
  • Inhibits breakdown of GABA to succinic semialdehyde
26
Q

What is the mechanism of valproate in treating epilepsy?

A
  • SSADH inhibition
  • Prevents breakdown of succinic semialdehyde to succinic acid
27
Q

What is the mechanism of tiagabine in treating epilepsy?

A
  • Inhibitor of GAT-1
  • Prevents inactivation of GABA transmission by reuptake
28
Q

What is the mechanism of barbiturates in treating epilepsy?

A

Enhancement of GABAA receptor activity prevents spread of seizure from initial focus.

29
Q

What is the mechanism of benzodiazepines in treating epilepsy?

A

Enhancement of GABAA receptor activity prevents spread of seizure from initial focus.

30
Q

Which GABAA enhancers are better anticonvulsants?

A

Barbiturates

31
Q

What types of drugs are used to treat absence seizures?

A
  1. T-type Cav inhibitors
  2. Nav inhibitors
  3. GABAB antagonists
32
Q

What are the types of drugs used to treat depression?

A
  • Inhibitors of monoamine reuptake:
    1. Tricyclic antidepressants
    2. Selective serotonin re-uptake inhibitors (SSRIs)
    3. Serotonin & noradrenaline reuptake inhibitors (SNRIs)
  • MAO inhibitors
  • Atpical antidepressants
33
Q

What is the mechanism of action of tricyclic antidepressants?

A
  • Selective inhibitors of NET and SERT
  • Prevents re-uptake of monoamines, including 5-HT and NA
  • NET inhibition may alleviate biological symptoms of depression while SERT inhibition may alleviate emotional symptoms
34
Q

What are examples of tricyclic antidepressants?

A
  • Non-selective: Amitriptyline, imipramine, clomipramine
  • NA-selective: Protriptyline
35
Q

What are the side effects of tricyclic antidepressants?

A
  1. Sedation
  2. Postural hypotension
  3. Dry mouth
  4. Ventricular dysrhythmias
36
Q

What is the mechanism of SSRIs?

A

Selective inhibition of 5-HT reuptake over NA

37
Q

What are examples of SSRIs?

A
  1. Fluoxitine
  2. Paroxetine
  3. Citalopram
38
Q

What are the side effects of SSRIs?

A
  1. Nausea
  2. Insomnia
  3. Sexual dysfunction
  4. Aggression
  5. Suicidal thoughts?
39
Q

What is the mechanism of action of serotonin and noradrenaline reuptake inhibitors (SNRIs)?

A

Selective inhibition of 5-HT over NA reuptake, but still inhibits NA reuptake (between tricyclics and SSRIs)

40
Q

What are examples of SNRIs?

A
  1. Venlafaxine
  2. Duloxetine
41
Q

What is the mechanism of action MAO inhibitors in treating depression?

A
  • Irreversible, non-competitive inhibition of MAO-A and MAO-B
  • Since MAO-A mediates 5-HT breakdown, its inhibition is more important in treating depression
42
Q

What are examples of MAO inhibitors?

A
  1. Phenelzine
  2. Tranylcypromine
  3. Iproniazid
43
Q

What is the mechanism of action of reversible inhibitors of MAO-A (RIMA) in treating depression?

A

Selective, reversible inhibition of MAO-A

44
Q

What are examples of RIMAs?

A

Moclobemide

45
Q

What are the side effects of MAOIs?

A
  1. Excitement/tremors
  2. Parasympathomimetic effect
  3. Hepatotoxicity
  4. ‘Cheese effect’
46
Q

What are the atypical antidepressants?

A
  1. Mirtazapine
  2. Agomelatine
  3. Vortioxetine
47
Q

What is the mechanism of action of mirtazapine in treating depression?

A

Antagonism of large number of monoamine receptors (incl. α2-adrenoreceptors, histamine H1 and 5-HT2 receptors)

48
Q

What is the mechanism of action of agomelatine in treating depression?

A

Melatonin receptor MT1 and MT2 agonists

49
Q

What is the mechanism of action of vortioxetine in treating depression?

A

Inhibition of 5-HT reuptake and 5-HT1 agonist

50
Q

What types of drugs can be used to treat bipolar disorder?

A
  1. Antidepressants - Depression
  2. Antipsychotics - Mania
  3. Lithium - Mood stabilisation
51
Q

What is the mechanism of action of lithium in mood stabilisation in bipolar disorder?

A
  • Substitutes for Na+ to enter cell through Na+-K+-ATPase
  • Accumulation inside cell causes:
    1. Inhibition of insitol phosphotase, inositol recycling and IP3 synthesis
    2. Inhibition of glycogen synthase kinase (GSK)
    3. Upregulation of ERK-MAP kinase
52
Q

What are mood stabilising drugs that can be used as alternative to lithium?

A
  1. Antiepileptics (valproate/lamotrogine)
    - Ca2+ channel inhibitors (gabapentin)
    - Na+ channel inhibitors (valproate, lamotrogine)
  2. Antipsychotics (olanzapine)
53
Q

What is the mechanism of action of methylphenitide (ritalin)?

A

Inhibitor of DAT and dopamine reuptake

54
Q

What are the clinical uses of methylphenidate (ritalin)?

A

ADHD

55
Q

What and example of GABAA inverse agonist?

A

Flumazenil

56
Q

What are the clinical uses of flumazenil?

A

Treatment of benzodiazepine overdose

Mechanism of Drug Action (Drugs) (26 decks)

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