BB drugs Flashcards
TCAs
Imipramine
Amitriptyline
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
MAOIs
Phenelzine
Iproniazid
MAOI MoAs, AEs
Irreversible inhibition of MAO enzymes (non-selective)
Treatment of atypical depression
AEs = cheese reaction (with tyramine containing foods), hepatotoxicity
SSRIs
Citaopram
Fluoxetine
Sertraline
Paroxetine
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
Moclobemide
Reversible MAOa inhibitor
Safer than MAOIs but similar efficacy
AEs = nausea, agitation, confusion
Venlafaxine
SNRI
Reboxetine
NRI
Mirtazepine
NaSSA
Noradrenergic and specific serotonergic antidepressant
Trazodone
SARI
Serotonin antagonist and reuptake inhibitor
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
Drugs for short term insomnia
Lorazepam
Temazpam
= BZs with short half life
Drugs for long term insomnia
Z drugs
E.g. zolpidem, eszopiclone
Suvorexant
Dual orexin receptor antagonist
Can be used to treat insomnia
BZs used for anxiety
Clonazepam
Alprazolam
BZ MoA
Increase opening frequency of Cl- channels with GABA binding
Barbiturates MoA
Increase opening duration of Cl- channels with GABA binding
5-HT1a agonists
Buspirone
Ipsapirone
= partial agonists
Used in anxiety
Drug used in BZ overdose
Flumazenil
Antagonises BZ binding site
Short half-life so repeated dosing needed
Typical antipsychotics examples
Chlorpromazine
Fluphenazine
Haloperidol
Flupenthixol
Atypical antipsychotics examples
Risperidone
Olazanpine
Clozapine
Paliperidone
Targets of antipsychotics
Typical = D2 receptors Atypical = D2 + 5HT2, a1, H1, M so have more effect on negative and cognitive symptoms
Clozapine
Atypical antipsychotic
Highest affinity for D4 receptors
Drug of choice in treatment resistance
Risk of agranulocytosis
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
Antipsychotics in depot injection
Fluphenazine
Haloperidol
Can be used for low compliance
Disulfiram
Aldehyde dehydrogenase inhibitor
Makes alcohol hangover worse by allowing acetaldehyde build up
Naltrexone
Opioid antagoist
Can be used in alcohol and opiate addiction to help prevent relapse
Bupropion
Monoamine reuptake inhibitor
Useful in smoking cessation
Methadone
Opioid agonist
Maintenance therapy for heroin addicts
Clonidine
Alpha 2 agonist
Reduces opiate withdrawal symptoms
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)
Carbidopa, bensarazide
Peripherally acting DOPA decarboxylase inhibitors
Dopamine agonists
Rotigotine (transdermal patch) Bromocriptine Pergolide Ropinirole Apomorphine (IV infusion)
MAOb inhibitors
Selegiline
Rasagiline
Protect residual dopamine from oxidation
COMT inhibitors
Entacapone
Tolcapone
Enhance the effect of L-Dopa
Amantadine
Anti-viral used in Parkinson’s
Inhibits dopamine reuptake
Increases dopamine release
Anticholinergics for Parkinson’s disease
Benzatropine Orphenadrine Procyclidine Trihexyphenidyl Benzhexol Used as dopamine loss leads to hyperactivity of cholinergic neurones
Tetrabenazine
Drug used for treatment of Huntingdon’s disease
Synaptic vesicular amine transport inhibitor (VMAT-1)
Inhibits vesicular storage of dopamine
Other drugs used in Huntingdon’s disease
Antipsychotics (antidopaminergic) = haloperidol, olanzapine
Antidepressants = imipramine, amitriptyline
Opiate antagonist –> used in overdose
Naloxone
Short half-life so repeated dosing needed
MoA of opiates
Increase potassium conductance
Decrease calcium conductance
Reduced excitability and NT release
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
Side effects of opioids
Respiratory depression Drowsiness and sedation Nausea and vomiting Hypotension Delayed gastric emptying
Paracetamol
COX2 inhibitor and modulator of endocannabinoid system
Analgesic and antipyretic
Little anti-inflammatory activity
Aspirin
NSAID
COX1 and COX2 inhibitor
Analgesic, antipyretic, anti-inflammatory, anti-platelet
Ibuprofen, diclofenac, ketoprofen
NSAIDs
COX1 and COX2 inhibitors
Analgesic, anti-inflammatory
Non-opioids for pain management
Anti-convulsants –> carbamazepine, sodium valproate, pregabalin
TCAs –> amitriptyline
Local anaesthetics
Lignocaine, bupivacine, prilocaine
MoA = blockage of sodium channels
Risk of systemic toxicity –> hypotension, respiratory depression, bradycardia
General anaesthetics
Activate inhibitory receptors or inhibit excitatory receptors
Induce CV depression
Inhaled –> halothane, enflurane, NO, xenon
IV –> propofol, thiopental, ketamine
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)
Why drugs cannot be used in absence seizures?
Phenytoin
Carbamazepine
Which drugs are used in absence seizures?
Ethosuxamide (T type calcium channels)
Sodium valproate
Antiepileptics that act on calcium channels
Ethosuximide (T type calcium channels)
Gabapentin/pregabalin (alpha 2 delta subunit of N type calcium channels)
Antiepileptics that act on GABAa channels
BZs –> clonazepam (sedation)
Barbiturates –> phenobarbitone (microsomal enzyme induction)
Levetiracetam
Binds to SV2A synaptic protein
Modulates NT release
Tiagabine
Targets GAT1 transporter
Modulates NT uptake
Viagabatrin
Inhibits GABA transaminase
Inhibits GABA metabolism
Antiepileptics used in myoclonic seizures
Sodium valproate, clonazepam, levetiracetam
Treatment of status epilepticus
IV diazepam
Beta interferons
SQ or IM injections
Reduce immune cell proliferation
AEs = flu-like symptoms, injection site reactions
Glatiramer acetate
Also called copaxone
SQ daily injections
Blocks T cells from attacking myelin
AEs = injection site reactions, lipoatrophy, flu-like symptoms
Dimethyl fumarate
Oral twice daily pill
Immune cell proliferation inhibitor
AEs = hot flushes, GI problems, infections
Alemtuzumab
Anti-CD52
Reduces inflammation
AEs = infection, idiopathic thrombocytopaenia purpura, autoimmune thyroid disease
Fingolimod
Oral drug
Sphingosine-1-phosphate receptor modulator
AEs = arrhythmias, infection
Natalizumab
Antibody against A4 integrin
Prevents leukocyte attachment and entry to CNS
AE = progressive multifocal leukoencephalopathy (PML)
Sumatriptan
Used for migraines and cluster headache
5-HT1b/d agonist
Promotes cerebral vasoconstriction
Cholinesterase inhibitors
Used in AD
Donepezil, rivastigmine, galantamine
Memantine
NMDA receptor antagonist
Reduces excitotoxicity
Used in AD
Domperidone
Anti-emetic
Peripherally acting D2 receptor antagonist
Ondansetron
Anti-emetic
5-HT3 receptor antagonist
Flumazenil
BZ antagonist
Used in BZ overdose
