Pharm:psychiatric Drugs

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Phenobarbital, pentobarbital, thiopental, secobarbital

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Barbiturates
Names

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barbiturates:
used for
MOA

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Sedatives for anxiety, seizures, insomnia, induction of anesthesia (thiopental)

MOA: facilitate GABA action by increasing duration of Cl channel openingthus decreasing neuron firing

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barbiturates: SE/Tox--

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Dependence,
additive CNS depression effects with alcohol
Resp, CV depression that can result in death
drug interaction dt inductoin of liver microsomal enzymes

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Diazepam, Lorazepam, triazolam, temazepam, axazepam, midazolam, chlordiazepoxide

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Benzodiazepines:
names

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Benzodiazepines:
MOA

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facilitate GABA action by increasing frequency of Cl channel opening. Most have long half-lives and active metabolites.

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Benzodiazepines: Clinical use

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Anxiety, spasticity, status epilepticus (diazepam), detox (esp ETOH wdrawl)

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Benzodiazepines: SE

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dependence
additive CNS depresion with ETOH
less risk of Resp depression and coma w/ barbiturates
Treat overdose with flumazenil--competitive antagonist at GABA receptor

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Thioridazine, haloperidol, fluphenazine, chlorpromazine

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Antipsychotics:
name

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Antipsychotics:
MOA

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block Dopamine (D2) receptors

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Antipsychotics: Clinical use

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schizophrenia, psychosis

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Antipsychotics: SE

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1)Extrapyramidal system (EPS)PAGE 304!!!!!
sedation
endocrine SE
SE dt blocking muscarinic, Alpha, and histamine receptors

2)Neuroleptic malignant Syn--rigidity, autonomic instability, hyperpyrexia(trt with dantrolene and dopamine agonist)

3) Tardive dyskinesia--stereotypic oral-facal movements probably dt dopamine receptor sensitization; results from long term antipsychotic use

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Clozapine, olanzapine, risperidone

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atypical anti-psychotics

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Clozapine, olanzapine, risperidone
MOA

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block 5 HT2 and dopamine receptors

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Clozapine, olanzapine, risperidone:
clinical use

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Schizophrenia, for both positive and negative Sx.

Olanzapine--also for OCD, anxiety disorders, depression

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Clozapine, olanzapine, risperidone: SE

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fewer extrapyramidal SE than other antipsychotics

Clazapine--may cause agranulocytosis so requires weekly WBC monitoring

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Lithium
family
MOA

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atypical antipsychotic
Not establiched..possibly related to inhibition of phosphoinositol cascade

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Lithium: Clinical use

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Mood stabilizer for bipolar affective disorders, blocks relapse, and acute maniac events

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Lithium: tox/se

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tremor, hypothyroidism, polyuria (ADH antagosist causing nephrogenic diabetes insipidus), teratogenesis

narrow therapeutic window requires close monitoring of serum levels.

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Fluoxetine, sertaline, paroxetine, citalopram

Family

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SSRIs

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SSRIs

MOA

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Seretonin specific reuptake inhibitors

Usually takes about two to three weeks for an effect

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SSRIs
Clinical use

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Endogenous depression

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SSRIs TOX

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Fewer than TCA
CNS stimulation---anxiety, insomnia, tremor, anorexia, nausea, vomiting

Seretonin syndrome w/ MAO inhibitor--hyperthermia, muscle rigidity, CV collapse

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Imipramine
Amitriptyline
desipramine
nortriptyline
clomipramine
doxepin

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Tricyclic antidepressants

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Tricyclic antidepressants--MOA

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Block reuptake of NE and serotonin

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Tricyclic antidepressants--clinical use

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Endogenous depression
bedwetting (imipramine)
OCD (clomipramine)

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Tricyclic antidepressants SE

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Sedation
alpha blocking effects
atropoine like side effefct (anticholinergic incl tachycardia, urinary retention)

3rd TCAs (amitriptyline) have more anticholinergic effects do 2rd TCAs (nortriptyline)

Desipramine is least sedating

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Tricyclic antidepressants Tox

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Tri-Cs--convulsions, Coma, cardiotoxicity (arrythmias)

resp depression
hyperpyrexia

Confusion and hallucinations in elderly dt anticholinergic side effects

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Trazodone
Buproprion
Venlafaxine
Mirtazapine
Maprotiline

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heterocyclics---2nd and 3rd generation antidepressants with varied and mixed mechanisms of action.

Used in major depressive disorders

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trazodone

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primarily inhibit serotonin reuptake

Toxicity--sedation, nausea, priapism, postural hypotension

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buproprion

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Smoking cessation
MOA not well known

Tox: stimulant effect -(tachycardia, agitation)
dry mouth
aggravation of psychosis

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venlafaxine

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Also used in general anxiety disorders

MOA--inhibits serotonin, NE, and dopamine reuptake

Tox--stimulant effects (anxiety, agitation, HA, insomnia)

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Mirtapine

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Alpha 2 agonist (increases release of NE, seretonin)
Potent 5-HT2 receptor antagonist

Tox--sedation, increase serum cholesterol, increases appetite

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Maprotiline--

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Blocks NE reuptake

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Phenezine
Tranylcypromine

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MOA inhibitors

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Phenezine
Tranylcypromine--MOA

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nonselective MOA inhibition

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Phenezine
Tranylcypromine--clinical use

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Atypical depression (ie with psychotic or phobic features)
Anxiety, hypochondriasis

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Phenezine
Tranylcypromine---Tox

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Hypertensive crisis with tyramine ingestion (from foods) and meperidine

CNS stimulation

Contraindication with SSRI or B agonist