Anxiolytics 1 GABA inhibitory neurotransmitter 2 GABA receptors GABAA and GABAB 3 4 A major binding site for GABA in CNS GABA receptor complex GABA binding site BZD binding site CL ion channel Picrotoxin binding site GABA Receptor Modulation Agonist Antagonist GABA potentiators 5 5HT1A receptor 5HT1A partial agonist buspirone 6 BZD pharmacokinetic Lipid solubility determines rate of onset Dosage adjustments Antidepressants 1 Neurotransmitters Involved NE 5HT DA 2 Major Mechanism of actions Monoamine oxidase inhibition phenelzine 5HT and NE reuptake inhibitors venlafaxine tricyclics and heterocyclic antidepressants Selective 5HT reuptake inhibitors SSRIs fluoxetine paroxetine sertraline fluvoxamine citalopram 5HT2 antagonist and 5HT reuptake inhibitor nefazodone NE and DA reuptake inhibitor bupropion 1 3 4 Noradrenergic and specific serotonergic mirtazepine Receptor Profile and Side effects 5HT2 5HT3 DA NE Antidepressant kinetics Protein binding Metabolism Antipsychotics 1 traditional DA blockade high vs low potency 2 Atypical DA blockade selectivity 5HT2 blockade 3 What make an antipsychotic an atypical 4 Receptor profile and side effects DA 5 5HT Histamine Alpha1 adrenergic Side effects of Atypical Clozapine seizures agranulocytosis weight gain orthostasis sialorrhea anticholinergic Risperidone dose related EPS low weight gain hyperprolactinemia anticholinergic Olanzapine weight gain akathisia sedation Quetiapine weight gain sedation cataracts Ziprasidone QTc prolongation no weight gain activating 2 6 Antipsychotic Pharmacokinetics Metabolized by CYP 450 Dose adjustments Mood Stabilizers 1 2 3 4 Lithium MOA unknown Valproate MOA GABA facilitation Carbamazepine neurotransmitter turnover second messenger systems Various others 5 Pharmacokinetics Serum levels correlated with efficacy 6 Metabolism 1 Lithium not metabolize excreted in urine 2 Carbamazepine hepatic induces hepatic isoenzymes autoinduction 3 Valproate inhibits some hepatic isoenzymes and glucoronidation Lithium Factor affecting clearance Stimulants 1 Mechanism of Action Inhibition of reuptake of DA NE Presynaptic release of DA NE 5HT Inhibition of Monoamine oxidase 2 Pharmacokinetics Drug interactions 1 2 Pharmacodynamic Additive effects Neurotoxicity Serotonin syndrome Cytochrome P450 isoenzymes Inhibitors 3 Pharmacokinetic interactions Protein binding saturation 4 Inducers Protein binding displacement Indication for Serum concentration monitoring 3
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