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2 - BB/HD > BB drugs > Flashcards

BB drugs Flashcards

1
Q

TCAs

A

Imipramine

Amitriptyline

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2
Q

TCA MoAs, AEs

A

Inhibit reuptake of amines
Also affinity for H1, M3, a1 and a2 receptors
AEs = anticholinergic effects (dry mouth, constipation, urinary retention), weight gain, arrhythmia, dizziness

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3
Q

MAOIs

A

Phenelzine

Iproniazid

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4
Q

MAOI MoAs, AEs

A

Irreversible inhibition of MAO enzymes (non-selective)
Treatment of atypical depression
AEs = cheese reaction (with tyramine containing foods), hepatotoxicity

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5
Q

SSRIs

A

Citaopram
Fluoxetine
Sertraline
Paroxetine

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6
Q

SSRI MoA, AEs

A 
Inhibition of serotonin reuptake 
No anticholinergic activity 
No cardiotoxic effects 
Safe in overdose 
AEs = nausea, headache, GI upset, anxiety, loss of libodi
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7
Q

Moclobemide

A

Reversible MAOa inhibitor
Safer than MAOIs but similar efficacy
AEs = nausea, agitation, confusion

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8
Q

Venlafaxine

A

SNRI

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9
Q

Reboxetine

A

NRI

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10
Q

Mirtazepine

A

NaSSA

Noradrenergic and specific serotonergic antidepressant

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11
Q

Trazodone

A

SARI

Serotonin antagonist and reuptake inhibitor

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12
Q

Lithium

A

Used for bipolar disorder as a mood stabiliser
Narrow therapeutic margin
Must check renal and thyroid function
AEs = thirst, nausea, fine tremor, polyuria, weight gain, oedema, acne

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13
Q

Drugs for short term insomnia

A

Lorazepam
Temazpam
= BZs with short half life

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14
Q

Drugs for long term insomnia

A

Z drugs

E.g. zolpidem, eszopiclone

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15
Q

Suvorexant

A

Dual orexin receptor antagonist

Can be used to treat insomnia

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16
Q

BZs used for anxiety

A

Clonazepam

Alprazolam

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17
Q

BZ MoA

A

Increase opening frequency of Cl- channels with GABA binding

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18
Q

Barbiturates MoA

A

Increase opening duration of Cl- channels with GABA binding

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19
Q

5-HT1a agonists

A

Buspirone
Ipsapirone
= partial agonists
Used in anxiety

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20
Q

Drug used in BZ overdose

A

Flumazenil
Antagonises BZ binding site
Short half-life so repeated dosing needed

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21
Q

Typical antipsychotics examples

A

Chlorpromazine
Fluphenazine
Haloperidol
Flupenthixol

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22
Q

Atypical antipsychotics examples

A

Risperidone
Olazanpine
Clozapine
Paliperidone

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23
Q

Targets of antipsychotics

A 
Typical = D2 receptors 
Atypical = D2 + 5HT2, a1, H1, M so have more effect on negative and cognitive symptoms
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24
Q

Clozapine

A

Atypical antipsychotic
Highest affinity for D4 receptors
Drug of choice in treatment resistance
Risk of agranulocytosis

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25
Q

Side effects of antipsychotics

A

General

  • allergic and toxic reactions
  • postural hypotension

Anticholinergic effects

  • haloperidol
  • clozapine

Typicals

  • extrapyramidal effects (acute dystopias, parkinsonism, tarditive dyskinesia)
  • hyperprolactinaemia
  • cardiotoxicity

Atypicals

  • weight gain
  • dyslipidaemia
  • insulin resistance –> type 2 diabetes
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26
Q

Antipsychotics in depot injection

A

Fluphenazine
Haloperidol
Can be used for low compliance

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27
Q

Disulfiram

A

Aldehyde dehydrogenase inhibitor

Makes alcohol hangover worse by allowing acetaldehyde build up

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28
Q

Naltrexone

A

Opioid antagoist

Can be used in alcohol and opiate addiction to help prevent relapse

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29
Q

Bupropion

A

Monoamine reuptake inhibitor

Useful in smoking cessation

30
Q

Methadone

A

Opioid agonist

Maintenance therapy for heroin addicts

31
Q

Clonidine

A

Alpha 2 agonist

Reduces opiate withdrawal symptoms

32
Q

Levodopa

A

= synthetic L-Dopa

Side effects

  • nausea and vomiting (increased peripheral levels stimulating area postrema)
  • postural hypotension
  • psychosis (from over-activation of mesolimbic pathway)

Motor complications

  • on-off effect
  • wearing off effect
  • dyskinesia
  • dystonia

Effects can be optimised by COMT inhibitors (tolcapone, entacapone)

33
Q

Carbidopa, bensarazide

A

Peripherally acting DOPA decarboxylase inhibitors

34
Q

Dopamine agonists

A 
Rotigotine (transdermal patch) 
Bromocriptine 
Pergolide 
Ropinirole 
Apomorphine (IV infusion)
35
Q

MAOb inhibitors

A

Selegiline
Rasagiline
Protect residual dopamine from oxidation

36
Q

COMT inhibitors

A

Entacapone
Tolcapone
Enhance the effect of L-Dopa

37
Q

Amantadine

A

Anti-viral used in Parkinson’s
Inhibits dopamine reuptake
Increases dopamine release

38
Q

Anticholinergics for Parkinson’s disease

A 
Benzatropine
Orphenadrine 
Procyclidine 
Trihexyphenidyl 
Benzhexol 
Used as dopamine loss leads to hyperactivity of cholinergic neurones
39
Q

Tetrabenazine

A

Drug used for treatment of Huntingdon’s disease
Synaptic vesicular amine transport inhibitor (VMAT-1)
Inhibits vesicular storage of dopamine

40
Q

Other drugs used in Huntingdon’s disease

A

Antipsychotics (antidopaminergic) = haloperidol, olanzapine

Antidepressants = imipramine, amitriptyline

41
Q

Opiate antagonist –> used in overdose

A

Naloxone

Short half-life so repeated dosing needed

42
Q

MoA of opiates

A

Increase potassium conductance
Decrease calcium conductance
Reduced excitability and NT release

43
Q

Practical aspects of opioid use

A

Morphine –> M6G active metabolite
Heroin –> high solubility, used in cachexia
Dextromoramide –> active sublingually
Methadone –> half life decreases –> accumulation
Metptazinol –> less respiratory depression
Pethidine –> poor oral availability

44
Q

Side effects of opioids

A 
Respiratory depression 
Drowsiness and sedation 
Nausea and vomiting 
Hypotension 
Delayed gastric emptying
45
Q

Paracetamol

A

COX2 inhibitor and modulator of endocannabinoid system
Analgesic and antipyretic
Little anti-inflammatory activity

46
Q

Aspirin

A

NSAID
COX1 and COX2 inhibitor
Analgesic, antipyretic, anti-inflammatory, anti-platelet

47
Q

Ibuprofen, diclofenac, ketoprofen

A

NSAIDs
COX1 and COX2 inhibitors
Analgesic, anti-inflammatory

48
Q

Non-opioids for pain management

A

Anti-convulsants –> carbamazepine, sodium valproate, pregabalin
TCAs –> amitriptyline

49
Q

Local anaesthetics

A

Lignocaine, bupivacine, prilocaine
MoA = blockage of sodium channels
Risk of systemic toxicity –> hypotension, respiratory depression, bradycardia

50
Q

General anaesthetics

A

Activate inhibitory receptors or inhibit excitatory receptors
Induce CV depression
Inhaled –> halothane, enflurane, NO, xenon
IV –> propofol, thiopental, ketamine

51
Q

Antiepileptics that act on sodium channels

A

Phenytoin (zero order kinetics)
Carbamazepine (enzyme induction)
Sodium valproate (all types of seizures)
Lamotrigine (also works on calcium channels)
Topiramate (also works on GABAa channels)

52
Q

Why drugs cannot be used in absence seizures?

A

Phenytoin

Carbamazepine

53
Q

Which drugs are used in absence seizures?

A

Ethosuxamide (T type calcium channels)

Sodium valproate

54
Q

Antiepileptics that act on calcium channels

A

Ethosuximide (T type calcium channels)

Gabapentin/pregabalin (alpha 2 delta subunit of N type calcium channels)

55
Q

Antiepileptics that act on GABAa channels

A

BZs –> clonazepam (sedation)

Barbiturates –> phenobarbitone (microsomal enzyme induction)

56
Q

Levetiracetam

A

Binds to SV2A synaptic protein

Modulates NT release

57
Q

Tiagabine

A

Targets GAT1 transporter

Modulates NT uptake

58
Q

Viagabatrin

A

Inhibits GABA transaminase

Inhibits GABA metabolism

59
Q

Antiepileptics used in myoclonic seizures

A

Sodium valproate, clonazepam, levetiracetam

60
Q

Treatment of status epilepticus

A

IV diazepam

61
Q

Beta interferons

A

SQ or IM injections
Reduce immune cell proliferation
AEs = flu-like symptoms, injection site reactions

62
Q

Glatiramer acetate

A

Also called copaxone
SQ daily injections
Blocks T cells from attacking myelin
AEs = injection site reactions, lipoatrophy, flu-like symptoms

63
Q

Dimethyl fumarate

A

Oral twice daily pill
Immune cell proliferation inhibitor
AEs = hot flushes, GI problems, infections

64
Q

Alemtuzumab

A

Anti-CD52
Reduces inflammation
AEs = infection, idiopathic thrombocytopaenia purpura, autoimmune thyroid disease

65
Q

Fingolimod

A

Oral drug
Sphingosine-1-phosphate receptor modulator
AEs = arrhythmias, infection

66
Q

Natalizumab

A

Antibody against A4 integrin
Prevents leukocyte attachment and entry to CNS
AE = progressive multifocal leukoencephalopathy (PML)

67
Q

Sumatriptan

A

Used for migraines and cluster headache
5-HT1b/d agonist
Promotes cerebral vasoconstriction

68
Q

Cholinesterase inhibitors

A

Used in AD

Donepezil, rivastigmine, galantamine

69
Q

Memantine

A

NMDA receptor antagonist
Reduces excitotoxicity
Used in AD

70
Q

Domperidone

A

Anti-emetic

Peripherally acting D2 receptor antagonist

71
Q

Ondansetron

A

Anti-emetic

5-HT3 receptor antagonist

72
Q

Flumazenil

A

BZ antagonist

Used in BZ overdose

2 - BB/HD (8 decks)

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