PHA4107: Psychopharmacology

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5-Hydroxytryptamine

Also known as serotonin - Receptors can be found in CNS, GI tract, smooth muscle, blood vessels, platelets

Phenelzine

Classical (non-selective) MAOi - irreversible inhibitor that has severe interaction with food and drugs (tyramine, meperidine, TCA) - inhibits degradation of monamines like 5HT and NA

Meperidine

Opioid that should not be used with phenelzine or other MAOi (headache, seizures, coma, death)

Moclobemide

MAO A inhibitor (MAO A only degrades MA linked to depression) - reversible, competitive inhibitor that has better side effect profile than classical MAOi

Imipramine

Tricyclic antidepressant - block reuptake of many MA (NA, 5HT, DA) - side effects have alpha-1 adrenergic antagonism (drowsiness, limp dick), histamine-1 antagonism (drowsiness), muscarinic antagonism (anti-SLUDGE+)

Amitriptyline

Tricyclic antidepressant - block reuptake of many MA (NA, 5HT, DA) - side effects have alpha-1 adrenergic antagonism (drowsiness, limp dick), histamine-1 antagonism (drowsiness), muscarinic antagonism (anti-SLUDGE+)

Paroxetine

SSRI - accumulation of 5HT and downregulation of post-synaptic and dendritic (5HT 1A, neg feedback) receptors - side effects nausea, insomnia, anorexia, suicide

Citalopram

SSRI - accumulation of 5HT and downregulation of post-synaptic and dendritic (5HT 1A, neg feedback) receptors - side effects nausea, insomnia, anorexia, suicide, sex dysfunction

Sertraline

SSRI - accumulation of 5HT and downregulation of post-synaptic and dendritic (5HT 1A, neg feedback) receptors - side effects nausea, insomnia, anorexia, suicide

Buproprion

NA/DA reuptake inhibitor - cessation of smoking

Venlafaxine

SNRI (serotonin-noradrenaline reuptake inhibitor) - effects on reuptake dependent on dose (5HT > NA > DA) - rapid effect (1 week instead of 2) - nausea, anorexia, sex dysfunction

Trazodone

SARI (Serotonin-2 antagonist/reuptake inhibitor) - increase 5HT and block 5HT-2 receptors for side effects

Mirtazapine

SNDI (serotonin and norepinephrine disinhibitor) - block alpha-2 negative feedback to increase release of 5HT and NA - block 5HT-2 receptor to decrease side effects (anxiety, nausea, insomnia, sex dysfunction)

Lithium

Mood stabilizer to treat mania - enters via Na+ channels to block phosphatidylinositol signaling cascade in the brain - affects central adrenergic, muscarinic, serotonergic neurotransmission - side effects nausea, polyuria and thirst, tremor

Chlorpromazine

Typical neuroleptic - treat schizophrenia - antagonistic D2 (relief of symptoms), H1 (weight gain/drowsiness), M1 (xerostomia, constipation), alpha-1 (hypotension) activity - better anticholinergic activity than haloperidol (block ACh in nigrostriatal means less extrapyramidal effects)

Haloperidol

Typical neuroleptic - treat schizophrenia - antagonistic D2 (relief of symptoms), H1 (weight gain/drowsiness), M1 (xerostomia, constipation), alpha-1 (hypotension) activity - worse anticholinergic activity than chlorpromazine (more EPR)

Clozapine

Atypical antipsychotic - treat schizophrenia - improve positive and negative symptoms - side effects agranulocytosis

Olanzapine

Atypical antipsychotic - treat schizophrenia - improve positive and negative symptoms - no agranulocytosis side effects

Risperidone

Atypical antipsychotic - treat schizophrenia - 5HT-2 (remove negative feedback in nigrostriatal) and D2 (block overactive mesolimbic pathway) antagonist

Sertindole

...

Quetiapine

Atypical antipsychotic - treat schizophrenia - acts on multiple receptors

Busipirone

Serotonergic anxiolytic - 5HT-1A partial agonist (interacts with somatodendritic negative feedback receptors) - decreases level of serotonin - side effects vertigo (no interaction with alcohol)

Diazepam

Benzodiazepine - GABAergic anxiolytic - increase effect of endogenous GABA (in CNS) to inhibit neurons - treat anxiety, sedate, epilepsy, induce amnesia - side effects drowsiness, amnesia, danger with alcohol, ataxia

Lorazepam

Benzodiazepine - GABAergic anxiolytic - increase effect of endogenous GABA (in CNS) to inhibit neurons - treat anxiety, sedate, epilepsy, induce amnesia - side effects drowsiness, amnesia, danger with alcohol, ataxia

Zopiclone

Non-benzodiazepine anxiolytic - treat insomnia with better side effect profile and short duration of action

GABA

Most abundant inhibitory NT in CNS - increasing affect has anxiolytic affect

GHB

Naturally in mammal brain - act on GABA receptors - treat anxiety - side effects amnesia, bradycardia/hypotension, depression, decreased muscular tone

Flunitrazepam

Benzodiazepine - treat insomnia, preanaesthetic - can be used for date rape - like diazepam but 10x more potent

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