Pharm 1-Liners: Antipsychotics

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Extrapyramidal dysfunction is more common with these agents, which block this subtype of dopamine receptor

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Older antipsychotic agents, D2 receptors

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MOA of neuroleptics

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Dopamine blockade

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Side effects occuring in antipsychotics that block dopamine

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Hyperprolactinemia, menorrhea, galactorrhea, confusion, mood changes, decreased sexual interest, and weight gain

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Antipsychotics that reduce positive symptoms only

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Older antipsychotics

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Newer atypical antipsychotics that also improve some of the negative symptoms and help acute agitation

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Olanzapine, aripiprazole, and sertindole

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Antipsychotic used in the treatment of psychiatric symptoms in patients with dementia

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Risperidone

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Atypical antipsychotic causing high prolactin levels

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Risperidone

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Newer atypical antipsychotic used for bipolar disorder, known to cause weight gain, and adversely affect diabetes

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Olanzapine

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Agent more frequently associated with extrapyramidal side effects that can be treated with benzodiazepine, diphenhydramine or muscarinic blocker

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Haloperidol

Front 10

Drug used in neuroleptic malignant syndrome

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Dantrolene

Front 11

Agents may exacerbate tardive dyskinesias (may be irreversible and there is no treatment)

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Muscarinic blockers

Front 12

Antipsychotic having the strongest autonomic effects

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Thioridazine

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Antipsychotic having the weakest autonomic effects

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Haloperidol

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Only phenothiazine not exerting antiemetic effects, can cause visual impairment due to retinal deposits, and high doses have been associated with ventricular arrhythmias

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Thioridazine

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Agent having no effect on D2 receptors, blocks D4, reserved for resistant schizophrenia, and can cause fatal agranulocytosis

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Clozapine

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Anti-psychotic not shown to cause tardive dyskinesia

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Clozapine

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Anti-psychotics available in depot preparation

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Fluphenazine and haloperidol

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Reduced seizure threshold

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Low-potency typical antipsychotics and clozapine

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Orthostatic hypotension and QT prolongation

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Low potency phenothiazines and ziprasidone

Front 20

Increased risk of developing cataracts

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Quetiapine, Lithium

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Major route of elimination for Lithium

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Kidneys

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Patients being treated with lithium, who are dehydrated, or taking diuretics concurrently, could develop

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Lithium toxicity

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Drug increases the renal clearance hence decreases levels of lithium

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Theophylline

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Lithium is associated with this congenital defect

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Cardiac anomalies and is contraindicated in pregnancy or lactation

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DOC for bipolar affective disorder

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Lithium

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Concern using lithium

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Low therapeutic index

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SE of lithium

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Tremor, sedation, ataxia, aphasia, thyroid enlargement, and reversible diabetes insipidus

Front 28

Example of three antidepressants that are indicated for obsessive compulsive disorder

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Clomipramine, fluoxetine and fluvoxamine

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Neurotransmitters affected by the action of antidepressants

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Norepinephrine and serotonin

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Usual time needed for full effect of antidepressant therapy

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2 to 3 weeks

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Population group especially sensitive to side effects of antidepressants

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Elderly patients

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All antidepressants have roughly the same efficacy in treating depression, agents are chosen based on these criterion

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Side-effect profile and prior pt response

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Well-tolerated and are first-line antidepressants

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SSRI's, bupropion, and venlafaxine

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Most useful in patients with significant anxiety, phobic features, hypochondriasis, and resistant depression

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Monamine oxidase inhibitors

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Condition will result from in combination of MAOI with tyramine containing foods (ex. wine, cheese, and pickled meats)

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Hypertensive crisis

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MAOI should not be administered with SSRI's or potent TCA's due to development of this condition

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Serotonin syndrome

Front 37

Sedation is a common side effect of these drugs, they lower seizure threshold, uses include BAD, acute panic attacks, phobias, enuresis, and chronic pain and their overdose can be deadly

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Tricyclic antidepressants (TCA)

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Three C's associated with TCA toxicity

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Coma, Convulsions, Cardiac problems (arrhythmias and wide QRS)

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Agents having higher sedation and antimuscarinic effects than other TCA's

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Tertiary amines

Front 40

TCA used in chronic pain, a hypnotic, and has marked antimuscarinic effects

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Amitriptyline

Front 41

TCA used in chronic pain, enuresis, and ADD

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Imipramine

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TCA with greatest sedation of this group, and marked antimuscarinic effects, used for sleep

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Doxepin

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TCA used in obsessive compulsive disorder (OCD), most significant of TCA's for risk of seizure, weight gain, and neuropsychiatric signs and symptoms

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Clomipramine

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Secondary amines that have less sedation and more excitation effect

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Nortriptyline, Desipramine

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Side effects seen with tricyclic antidepressants

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Muscarinic blockade (dry mouth, constipation); weak alpha-1 block (orthostatic hypotension); weak hisamine block (sedation)

Front 46

Antidepressant associated with neuroleptic malignant syndrome

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Amoxapine

Front 47

Antidepressant associated with seizures and cardiotoxicity

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Maprotiline

Front 48

Antidepressant having stimulant effects similar to SSRI's and can increase blood pressure

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Venlafaxine

Front 49

Antidepressant inhibiting norepinephrine, serotonin, and dopamine reuptake

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Venlafaxine

Front 50

Antidepressant also used for sleep that causes priapism

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Trazodone

Front 51

Antidepressant which is inhibitor of CYP450 enzymes and may be associated with hepatic failure

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Nefazodone

Front 52

Heterocyclic antidepressants least likely to affect sexual performance, used for management of nicotine withdrawal, SE's include dizziness, dry mouth, aggravation of psychosis, and seizures

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Bupropion

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Antidepressant with MOA as alpha 2 antagonist, has effects on both 5-HT and NE, blocks histamine receptors, and is sedating

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Mirtazapine

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SE of mirtazapine

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Liver toxicity, increased serum cholesterol

Front 55

Except for these agents all SSRI have significant inhibition of CytP450 enzymes

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Citalopram and its metabolite escitalopram

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Side effects frequently seen with SSRIs

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CNS stimulation; GI upset

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Antidepressants with no effect on BP, no sedation

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SSRIs

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SSRI with long T1/2 and can be administered once weekly for maintenance, not acute tx

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Fluoxetine

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SSRI indicated for premenstrual dysphoric disorder

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Fluoxetine (Sarafem)

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Some of SSRIs' therapeutic effects besidedepression

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Panic attacks, social phobias, bulimia nervosa, and PMDD (premenstrual dysphoric disorder), OCD

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SSRI less likely to cause a withdrawal syndrome

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Fluoxetine