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
Side effects of antipsychotics
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
26
Antipsychotics in depot injection
Fluphenazine Haloperidol Can be used for low compliance
27
Disulfiram
Aldehyde dehydrogenase inhibitor | Makes alcohol hangover worse by allowing acetaldehyde build up
28
Naltrexone
Opioid antagoist | Can be used in alcohol and opiate addiction to help prevent relapse
29
Bupropion
Monoamine reuptake inhibitor | Useful in smoking cessation
30
Methadone
Opioid agonist | Maintenance therapy for heroin addicts
31
Clonidine
Alpha 2 agonist | Reduces opiate withdrawal symptoms
32
Levodopa
= 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
Carbidopa, bensarazide
Peripherally acting DOPA decarboxylase inhibitors
34
Dopamine agonists
``` Rotigotine (transdermal patch) Bromocriptine Pergolide Ropinirole Apomorphine (IV infusion) ```
35
MAOb inhibitors
Selegiline Rasagiline Protect residual dopamine from oxidation
36
COMT inhibitors
Entacapone Tolcapone Enhance the effect of L-Dopa
37
Amantadine
Anti-viral used in Parkinson's Inhibits dopamine reuptake Increases dopamine release
38
Anticholinergics for Parkinson's disease
``` Benzatropine Orphenadrine Procyclidine Trihexyphenidyl Benzhexol Used as dopamine loss leads to hyperactivity of cholinergic neurones ```
39
Tetrabenazine
Drug used for treatment of Huntingdon's disease Synaptic vesicular amine transport inhibitor (VMAT-1) Inhibits vesicular storage of dopamine
40
Other drugs used in Huntingdon's disease
Antipsychotics (antidopaminergic) = haloperidol, olanzapine | Antidepressants = imipramine, amitriptyline
41
Opiate antagonist --> used in overdose
Naloxone | Short half-life so repeated dosing needed
42
MoA of opiates
Increase potassium conductance Decrease calcium conductance Reduced excitability and NT release
43
Practical aspects of opioid use
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
Side effects of opioids
``` Respiratory depression Drowsiness and sedation Nausea and vomiting Hypotension Delayed gastric emptying ```
45
Paracetamol
COX2 inhibitor and modulator of endocannabinoid system Analgesic and antipyretic Little anti-inflammatory activity
46
Aspirin
NSAID COX1 and COX2 inhibitor Analgesic, antipyretic, anti-inflammatory, anti-platelet
47
Ibuprofen, diclofenac, ketoprofen
NSAIDs COX1 and COX2 inhibitors Analgesic, anti-inflammatory
48
Non-opioids for pain management
Anti-convulsants --> carbamazepine, sodium valproate, pregabalin TCAs --> amitriptyline
49
Local anaesthetics
Lignocaine, bupivacine, prilocaine MoA = blockage of sodium channels Risk of systemic toxicity --> hypotension, respiratory depression, bradycardia
50
General anaesthetics
Activate inhibitory receptors or inhibit excitatory receptors Induce CV depression Inhaled --> halothane, enflurane, NO, xenon IV --> propofol, thiopental, ketamine
51
Antiepileptics that act on sodium channels
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
Why drugs cannot be used in absence seizures?
Phenytoin | Carbamazepine
53
Which drugs are used in absence seizures?
Ethosuxamide (T type calcium channels) | Sodium valproate
54
Antiepileptics that act on calcium channels
Ethosuximide (T type calcium channels) | Gabapentin/pregabalin (alpha 2 delta subunit of N type calcium channels)
55
Antiepileptics that act on GABAa channels
BZs --> clonazepam (sedation) | Barbiturates --> phenobarbitone (microsomal enzyme induction)
56
Levetiracetam
Binds to SV2A synaptic protein | Modulates NT release
57
Tiagabine
Targets GAT1 transporter | Modulates NT uptake
58
Viagabatrin
Inhibits GABA transaminase | Inhibits GABA metabolism
59
Antiepileptics used in myoclonic seizures
Sodium valproate, clonazepam, levetiracetam
60
Treatment of status epilepticus
IV diazepam
61
Beta interferons
SQ or IM injections Reduce immune cell proliferation AEs = flu-like symptoms, injection site reactions
62
Glatiramer acetate
Also called copaxone SQ daily injections Blocks T cells from attacking myelin AEs = injection site reactions, lipoatrophy, flu-like symptoms
63
Dimethyl fumarate
Oral twice daily pill Immune cell proliferation inhibitor AEs = hot flushes, GI problems, infections
64
Alemtuzumab
Anti-CD52 Reduces inflammation AEs = infection, idiopathic thrombocytopaenia purpura, autoimmune thyroid disease
65
Fingolimod
Oral drug Sphingosine-1-phosphate receptor modulator AEs = arrhythmias, infection
66
Natalizumab
Antibody against A4 integrin Prevents leukocyte attachment and entry to CNS AE = progressive multifocal leukoencephalopathy (PML)
67
Sumatriptan
Used for migraines and cluster headache 5-HT1b/d agonist Promotes cerebral vasoconstriction
68
Cholinesterase inhibitors
Used in AD | Donepezil, rivastigmine, galantamine
69
Memantine
NMDA receptor antagonist Reduces excitotoxicity Used in AD
70
Domperidone
Anti-emetic | Peripherally acting D2 receptor antagonist
71
Ondansetron
Anti-emetic | 5-HT3 receptor antagonist
72
Flumazenil
BZ antagonist | Used in BZ overdose