BB drugs Flashcards Preview

2 - BB/HD > BB drugs > Flashcards

Flashcards in BB drugs Deck (72):
1

TCAs

Imipramine
Amitriptyline

2

TCA MoAs, AEs

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

3

MAOIs

Phenelzine
Iproniazid

4

MAOI MoAs, AEs

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

5

SSRIs

Citaopram
Fluoxetine
Sertraline
Paroxetine

6

SSRI MoA, AEs

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

7

Moclobemide

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

8

Venlafaxine

SNRI

9

Reboxetine

NRI

10

Mirtazepine

NaSSA
Noradrenergic and specific serotonergic antidepressant

11

Trazodone

SARI
Serotonin antagonist and reuptake inhibitor

12

Lithium

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

13

Drugs for short term insomnia

Lorazepam
Temazpam
= BZs with short half life

14

Drugs for long term insomnia

Z drugs
E.g. zolpidem, eszopiclone

15

Suvorexant

Dual orexin receptor antagonist
Can be used to treat insomnia

16

BZs used for anxiety

Clonazepam
Alprazolam

17

BZ MoA

Increase opening frequency of Cl- channels with GABA binding

18

Barbiturates MoA

Increase opening duration of Cl- channels with GABA binding

19

5-HT1a agonists

Buspirone
Ipsapirone
= partial agonists
Used in anxiety

20

Drug used in BZ overdose

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

21

Typical antipsychotics examples

Chlorpromazine
Fluphenazine
Haloperidol
Flupenthixol

22

Atypical antipsychotics examples

Risperidone
Olazanpine
Clozapine
Paliperidone

23

Targets of antipsychotics

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

24

Clozapine

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

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