CNS Drug Mechanisms of Action Flashcards
Ethosuximide
blocks thalamic T-type Ca2+ channels
Benzodiazepines
Facilitate GABA(A) action by increased frequency of Cl- channel opening
Barbiturates
Facilitate GABA(a) action by increasing duration of Cl- channel opening, thus decreasing neuronal firing
Non-benzodiazepine hypnotics
Act via BZ1 subtype of the GABA receptor- reversed by flumazenil
Suvorexant
Orexin (hypocretin) receptor antagonist
Ramelteon
Melatonin receptor agonist, binds MT1 and MT2 in suprachiasmatic nucleus
Triptans
5-HT(1B/1D) agonists; inhibit trigeminal nerve activation; prevent vasoactive peptide release; induce vasoconstriction
Bromocriptine
Dopamine agonist
Amantadine
Increases DA release and decreases DA reuptake
Carbidopa
Blocks peripheral conversion of L-DOPA to DA by inhibiting DOPA decarboxylase
Entacapone
COMT inhibitor
Tolcapone
COMT inhibitor
Selegiline
MAO-B inhibitor
Benztropine
Antimuscarinic adjunct to improve tremor and rigidity
Trihexyphenidyl
Antimuscarinic adjunct to improve tremor and rigidity
Rasagiline
MAO-B inhibitor
Tetrabenazine
Inhibit vesicular monoamine transporter (VMAT)–> decreases DA vesicular packaging and release
Reserpine
Inhibit vesicular monoamine transporter (VMAT)–> decreases DA vesicular packaging and release
Riluzole
Decreases glutamate excitotoxicity; ALS treatment
Memantine
NMDA receptor antagonist
Tacrine
AChE inhibitor
Baclofen
Activates GABA(A) receptors at level of spinal cord, inducing skeletal muscle relaxation
Cyclobenzaprine
Centrally acting skeletal muscle relaxant
Pentazocine
Kappa-opioid receptor agonist and mu-opioid receptor weak/ partial agonist; analgesia
Butorphanol
Kappa-opioid receptor agonist and mu-opioid receptor partial agonist; analgesic
Tramadol
Very weak opiod agonist; also inhibits 5-HT and NE reuptake
Methylphenidate/ Dextroamphetamine/ methamphetamine
Increases catecholamines in the synaptic cleft (esp NE and DA)
Typical antipsychotics
Block D2 receptors (increase cAMP)
Buspirone
Stimulates 5-HT1A receptors
TCAs
Inhibit NE and 5-HT reuptake
Bupropion
Inhibits reuptake of NE and DA
Mirtazapine
Alpha 2 antagonist (increases NE and 5-HT release), 5-HT 2&3 antagonist; H1 antagonist
Trazodone
Primarily blocks 5-HT2, alpha 1, and H1 receptors; weakly inhibits 5-HT reuptake
Varenicline
Nicotinic ACh receptor partial agonist
Vilazodone
Inhibits 5-HT reuptake; 5-HT1A receptor partial agonist
Vortioxetine
Inhibits 5-HT reuptake; 5-HT1A receptor agonist and 5-HT3 receptor antagonist