Central Nervous System + Anaesthesia Flashcards
Dopaminergics
Basal Ganglia Disorders
Levodopa (precursor); Pramipexole, Ropinirole, Rotigotine (synthetic agonists)
MoA:
Increased dopamine synthesis and dopaminergic function
Indication:
Parkinson’s Disease
Adverse Effects/Interactions:
Confusion, agitation (MAOI)
Dopa-decarboxylase inhibitor
Basal Ganglia Disorders
Carbidopa, Benserazide
MoA:
Stops breakdown of Levodopa in the periphery by inhibiting dopa-decarboxylase
Indication:
Parkinson’s Disease
Adverse Effects/Interactions:
Confusion, agitation
Inhibitors of Monoamine Oxidase B (MAOI)
Basal Ganglia Disorders
Selegiline, Rasagaline
MoA:
Inhibition of dopamine breakdown
Indication:
Parkinson’s Disease
Adverse Effects/Interactions:
Inhibitor of COMT (catechol-O-methyl transferase)
Basal Ganglia Disorders
Entacapone, Tolcapone
MoA:
Blockade of dopamine precursor breakdown by inhibition of COMT
Indication:
Parkinson’s Disease
Adverse Effects/Interactions:
Nausea, vomiting
Anticholinergics
Basal Ganglia Disorders
Orphenadrine, Procyclidine, Trihexphenidyl
MoA:
Muscarinic cholinergic receptor antagonist
Indication:
Parkinson’s Disease, muscle rigidity, side effects of anti-psychotics
Adverse Effects/Interactions:
Dry mouth, constipation
Dopamine-depleting drugs
Basal Ganglia Disorders
Tetrabenazine
MoA:
Blocks VMAT, preventing uptake of DA into vesicles
Indication:
Huntington’s Chorea
Adverse Effects/Interactions:
Selective serotonin reuptake inhibitors (SSRIs)
Drugs for mental health treatment including dementia
Sertraline, Citalopram, Fluoxetine
MoA:
Inhibition of serotonin (5HT) reuptake pump in synaptic cleft
Indication:
Depression, generalised anxiety disorder
Adverse Effects/Interactions:
Insomnia, nausea
NSAIDs, lithium
Reversible Inhibitor of Monoamine Oxidase type A (RIMA)
Drugs for mental health treatment including dementia
Moclobemide
MoA:
Inhibits monoamine oxidise A, preferentially decreases breakdown of serotonin and noradrenaline
Indication:
Depression
Adverse Effects/Interactions:
Tachycardia
Tricyclic antidepressants (TCAs)
Drugs for mental health treatment including dementia
Amitriptyline, Nortriptyline, Dosulepin
MoA:
Inhibition of noradrenaline and serotonin reuptake in synaptic cleft, H1 antagonist, M1 antagonist, Adrenergic antagonist
Indication:
Depression
Adverse Effects/Interactions:
Anticholinergic syndrome
Atypical antidepressants
Drugs for mental health treatment including dementia
Roboxetine, Venlafaxine, Bupropion, Agomelatine, Mirtazapine
MoA:
Noradrenaline reuptake inhibitor (Reboxetine); Noradrenaline/serotonin reuptake inhibitor (Venlafaxine); Noradrenaline /Dopamine reuptake inhibitor (Buproprion); Melatonin agonist (Agomelatine); Alpha-2 antagonist (Mirtazepine)
Indication:
Depression
Adverse Effects/Interactions:
Antipsychotics - Classical (First Generation)
Drugs for mental health treatment including dementia
Chlorpromazine, Haloperidol
MoA:
Selective D2 dopamine receptor blockade
Indication:
Schizophrenia
Adverse Effects/Interactions:
Blurred vision, tremor,
Extrapyramidal symptoms, hypotension
Antipsychotics - Atypical (Second Generation)
Drugs for mental health treatment including dementia
Olanzapine, Risperidone, Quetiapine, Clozapine, Amisulpride
MoA:
Selective D2 dopamine and 5-HT receptor blockade
Indication:
Schizophrenia
Adverse Effects/Interactions: Extrapyramidal symptoms (less than classical antipsychotics), hypotension
Mood stabiliser
Drugs for mental health treatment including dementia
Lithium carbonate
MoA:
Unclear – possible neuronal calcium channel blockade
Indication:
Bipolar disorder
Adverse Effects/Interactions:
Tremor, hypothyroidism
NSAIDs, ACE inhibitors
Cholinesterase inhibitors
Drugs for mental health treatment including dementia
Donepezil, Galantamine, Rivastigmine
MoA:
Inhibition of acetylcholinesterase (reversible)
Indication:
Alzheimer’s Disease, mild to moderate dementia
Adverse Effects/Interactions:
Nausea, vomiting
NMDA receptor antagonist
Drugs for mental health treatment including dementia
Memantine
MoA:
VD blocker of NMDA receptors
Indication:
Alzheimer’s Disease, moderate to severe dementia
Adverse Effects/Interactions:
Constipation, hypertension
Anxiolytics
Drugs for mental health treatment including dementia
Benzodiazepines (see below), Buspirone
MoA: GABA PAM (γ-subunit); 5-HT1A partial agonist (Buspirone)
Indication:
Anxiety and related disorders
Adverse Effects/Interactions:
Non-benzodiazepine Hypnotic
Drugs for mental health treatment including dementia
Zopiclone
MoA:
GABA PAM (γ-subunit)
Enhanced effects of GABA
Indication:
Insomnia
Adverse Effects/Interactions:
Anti-Epilepsy Drugs (AEDs)
Drugs used to treat epilepsy
Sodium Valproate, Lamotrigine, Carbemezapine, Ethosuximide
MoA:
Na+ channel blockers;
(Ethosuximide – Ca2+ channel blocker)
Indication:
Epilepsy
Adverse Effects/Interactions:
Nausea, blurred vision
Macrolide antibiotics
Benzodiazepines (BDZs)
Drugs used to treat epilepsy
Lorazepam, Midazolam, Diazepam, Zolpidem (BDZ-like)
MoA:
GABA PAM (γ-subunit)
Enhanced effects of GABA
Indication:
Epilepsy, Acute seizures
Adverse Effects/Interactions:
Drowsiness, dependence
Sedatives
BDZ Antagonist
Drugs used to treat epilepsy
Flumazenil
MoA:
Antagonises GABA signalling
Indication:
Reversal of BDZ sedation
Adverse Effects/Interactions:
Barbiturates
Drugs used to treat epilepsy
Phenobarbitone, Pentobarbitone, Primidone
MoA:
GABA PAM (β-subunit)
Enhanced effects of GABA
Indication:
Epilepsy, Acute seizures
Adverse Effects/Interactions:
Drowsiness, fainting
Sedatives, anti-coagulants
Weak analgesic/antipyretic
Analgesics
Paracetamol
MoA:
Unclear – possible COX inhibitor in CNS
Indication:
Mild-moderate pain, pyrexia
Adverse Effects/Interactions:
Constipation
Warfarin
Non-steroidal anti-inflammatory drugs (NSAIDs)
Analgesics
Ibuprofen, Diclofenac, Naproxen
MoA:
Non-selective COX inhibitors, blockade of prostaglandin synthesis
Indication:
Mild-moderate pain, inflammation
Adverse Effects/Interactions:
GI disturbance, hypertension, Aspirin not suitable for under 16s
Diuretics, ACE inhibitors,
COX2-selective NSAIDs
Analgesics
Etoricoxib, Celecoxib
MoA:
COX-2 inhibition, localised prostaglandin blockade
Indication:
Pain, inflammation
Adverse Effects/Interactions:
Indigestion
ACE inhibitors, SSRIs
Weak opioid analgesics
Analgesics
Codeine, Dihydrocodeine
MoA:
Stimulation of analgesic opioid receptors
Indication:
Mild-moderate pain
Adverse Effects/Interactions:
Constipation, nausea
Sedatives
Strong opioid analgesics
Analgesics
Morphine, Diamorphine, Pethidine, Fentanyl
MoA:
Stimulation of analgesic opioid receptors
Indication:
Severe pain
Adverse Effects/Interactions:
Constipation, nausea
Sedatives
Partial/mixed agonist opioid analgesics
Analgesics
Buprenorphine, pentazocine
MoA:
Modulation of analgesic opioid receptors (µ and k)
Indication:
Moderate to severe pain
Adverse Effects/Interactions:
Constipation, nausea
Sedatives
Opioid antagonist
Analgesics
Naloxone, Naltrexone
MoA:
Opioid receptor antagonist
Indication:
Opiate overdose, respiratory depression
Adverse Effects/Interactions:
Nausea, tachycardia
Opioid addiction management
Analgesics
Methadone, Buprenorphine
MoA:
Narcotic opioid replacement; opioid receptor agonist/modulator
Indication:
Opiate addiction
Adverse Effects/Interactions:
Constipation
Sedatives
Drugs for neuropathic pain
Analgesics
Gabapentin, Pregabalin, Amitriptyline,
MoA: VDCC antagonist (gabapentin, pregabalin)/ TCA (amitriptyline)
Indication:
Neuropathic pain
Adverse Effects/Interactions:
Dizziness, fatigue
Antidepressants
Inhaled analgesics
Analgesics
Nitrous oxide + oxygen mixture (“Gas & Air”)
Entonox
MoA:
Unclear
Indication:
Analgesia during childbirth
Adverse Effects/Interactions:
Decreased vitamin B12 synthesis
General anaesthetic
Anaesthesia
Propofol, isoflurane, sevoflurane; Ketamine
MoA:
Unclear - possible enhancement of GABA function (Propofol, isoflurane, sevoflurane)
NMDA receptor blockade (ketamine)
Indication:
Induction of anaesthesia throughout major surgery
Adverse Effects/Interaction:
Hypotension
Local anaesthetic
Anaesthesia
Lidocaine, Bupivacaine, Levobupivacaine
MoA:
Voltage-gated sodium channel blockade
Indication:
Local anaesthesia
Adverse Effects/Interaction:
Rash
Neuromuscular blockers
Anaesthesia
Atracurium besilate, Vecuronium (non-depolarising)
Suxamethonium (depolarising)
MoA:
Competitive antagonist at AChR
Initially depolarisation and desensitisation of AChR
Indication:
Tracheal intubation and mechanical ventilation during surgery
Adverse Effects/Interaction:
Hypotension, skin flushing
Drugs for reversing neuromuscular block
Anaesthesia
Sugammadex; Neostigmine
MoA:
Oligosaccharide that forms a complex with NMBs removing them from NMJ (Sugammadex)
Peripheral acetylcholinesterase inhibitor
Indication:
Immediate reversal of NMB to reduce post-operative pulmonary complications (sugammadex)
(Neostigmine also used for myasthenia gravis)
Adverse Effects/Interaction:
Muscle relaxants & sedatives
Anaesthesia
Temazepam (BDZ), Zolpidem,
Dexmedetomidine (alpha-2 agonist)
Alfentanil, Fentanil, Remifentanil (opioids)
MoA:
See BDZs
Alpha-2 agonists inhibit sympathetic activity
See Opioids
Indication:
Maintain sedation and relaxed muscle tone
Adverse Effects/Interaction:
Bradycardia (alpha-2 agonist)
H1-receptor antagonist
Anti-emetics
Cyclizine
MoA:
Histamine H1 receptor blockade
Indication:
Nausea, vomiting
Adverse Effects/Interactions:
Dry mouth, sedation
Sedatives
D2-receptor antagonist
Anti-emetics
Domperidone
MoA:
Dopamine D2 receptor blockade in the Chemoreceptor Trigger Zone
Indication:
Nausea, vomiting
Adverse Effects/Interactions:
Cardiac disease
