Central Nervous System- MoA Flashcards
Dopaminergics
Increased dopamine synthesis and dopaminergic function
Dopa-decarboxylase inhibitors
Stops breakdown of Levadopa in the periphery by inhibiting dopa-decarboxylase
Inhibitors of Monoamine Oxidase B (MAOI)
Inhibition of dopamine breakdown
Inhibitor of COMT (catechol-O-methyl transferase)
Blockade of dopamine precursor breakdown by inhibition of COMT
Anticholinergics
Blockade of acetylcholine function
Muscarinic cholinergic receptor antagonist
Dopamine-depleting drugs
Blocks VMAT, preventing uptake of DA into vesicles
Selective serotonin reuptake inhibitors (SSRIs)
Inhibition of serotonin (5HT) reuptake pump in synaptic cleft
Reversible Inhibitor of Monoamine Oxidase type A (RIMA)
Inhibits monoamine oxidase A, preferentially decreases breakdown of serotonin and noradrenaline
Tricyclic antidepressants (TCAs)
Inhibition of noradrenaline and serotonin reuptake in synaptic cleft, H1 antagonist, M1 antagonist, adrenergic antagonist
Atypical antidepressants
5-HT1A partial agonist (Busprione)
Noradrenaline reuptake inhibitor (Venlafaxine, Reboxetine)
Noradrenaline /Dopamine reuptake inhibitor (Buproprion)
Melatonin agonist (Agomelatine)
Alpha-2 antagonist (Mirtazepine)
Antipsychotics- Classical (also known as First Generation)
Selective D2 dopamine receptor blockade
Antipsychotics- Atypical (also known as Second Generation)
Selective D2 dopamine and 5-HT receptor blockade
Mood Stabiliser
Neuronal calcium channel blockade
Unclear – possible neuronal calcium channel blockade
Cholinesterase inhibitors
Inhibition of acetylcholinesterase (reversible)
NMDA receptor antagonist
VD blocker of NDMA receptors
Anxiolytics
GABA PAM (gamma-subunit) 5-HT1A partial agonist (Buspirone)
Non-benzodiazepine Hypnotic
Modulation of the GABA-A receptor GABA PAM (γ-subunit) Enhanced effects of GABA
Anti-epilepsy drugs (AEDs)
Anticonvulsant, decrease neuronal transmission
Na+ channel blockers; (Ethosuximide-Ca2+ channel blocker)
Benzodiazepines (BDZs)
Enhanced effects of GABA neurotransmission GABA PAM (γ-subunit) Enhanced effects of GABA
BDZ Antagonist
Antagonises GABA signalling
Barbiturates
Enhanced effects of GABA neurotransmission GABA PAM (β-subunit) Enhanced effects of GABA
Weak analgesic/antipyretic
Non-opioid analgesic (precise MoA unknown)
Unclear – possible COX inhibitor in CNS
NSAIDs
Non-selective COX inhibitors, blockade of prostaglandin synthesis
COX2-selective NSAIDs
COX-2 inhibition, localised prostaglandin blockade
Weak opioid analgesics
Stimulation of analgesic opioid receptors
Strong opioid analgesics
Stimulation of analgesic opioid receptors
Partial/mixed agonist opioid analgesics
Stimulation of analgesic opioid receptors
Modulation of analgesic opioid receptors (μ and )
Opioid antagonist
Opioid receptor antagonist
Opioid addiction management
Narcotic opioid replacement; opioid receptor agonist/modulator
Drugs for neuropathic pain
VDCC antagonist (gabapentin, pregabalin)/ TCA (amitriptyline)
Inhaled analgesics
Unclear
Drugs used to treat migraine
Stimulation of 5-HT receptors (Sumatriptan); blockade of voltage-gated sodium & calcium channels (Topiramate)
5-HT3-receptor antagonist (anti-emetic)
Serotonin type 3 (5-HT3) receptor blockade
Busprione
5-HT1A partial agonist
Sumatriptan
Stimulation of 5-HT receptors
Topiramate
blockade of voltage-gated sodium & calcium channels
D2-receptor antagonist
Dopamine D2 receptor blockade in the Chemoreceptor Trigger Zone
Cyclizine
Histamine H1 receptor blockade
Ondansetron
Serotonin type 3 (5-HT3) receptor blockade
