7.3: Antipsychology Drugs (Lithium) Flashcards by Margaux Amaro

Q

What are the two types of drugs for psychoses and bipolar disorders?

A

Antipsychotics
Bipolar drugs

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Q

The antipsychotic drugs have two types, what are those?

A

Classic drugs (D2 receptor affinity)
Newer agents (5HT2 receptor affinity)

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Q

What are the main class of first generation antipsychotic drugs (D2 receptor affinity)?

A

Chlorpromazine
Haloperidol
Fluphenazine
Thioridazine
Trifluoperazine

CHeaF TT

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Q

What are the main class of second generation antipsychotic drugs (5HT2 receptor affinity)?

A

Clozapine
Risperidone
Olanzapine
Quetiapine
Ziprasidone

CROQ Z

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Q

Identify this medication:

Used to treat schizophrenia, other psychoses and agitated states
Protracted therapy (years)
Severe toxicity

A

Neuroleptics

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Q

Enumerate the symptoms of schizophrenia:

A

Disorganized speech
Catatonic or disorganized behavior
Hallucinations
Delusions
Negative symptoms

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Q

True or False:

In schizophrenia, impairment in major areas of functioning at work or interpersonal relationship or self care, schizoaffective and bipolar disorder are ruled out, and the disturbance is not due to other substance abuse.

A

True

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Q

What are the other associated features in Schizophrenia?

A

Inappropriate laughing
Disturbed sleep pattern
Dysphoric mood (depression, anger, anxiety
Anxiety and phobia
Cognitive deficits impacting language processing, executive function or memory
Hostility and aggression

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Q

Identify if manic or hypomanic in Bipolar Disorder:

Distinct episode of abnormally and persistently elevated expansive or irritable mood for 1 week

A

Manic episode

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Q

Identify if manic or hypomanic in Bipolar Disorder:

During the period of mood disturbance, three (or more) of the following have persisted (4 if mood is only irritable)
- Inflated self esteem or grandiosity
- Decrease need for sleep (3 hrs still feels rested)
- More talkative than usual or pressure to keep talking
- Insomnia or hypersomnia everyday
- Psychomotor agitation or retardation
- Flight of ideas or subjective experience that thoughts are racing
- Increase in goal-directed activity or psychomotor agitation
- Excessive involvement in pleasurable activities that have high potential for painful consequences (e.g buying sprees, sexual indiscretions, foolish)

A

Manic episode

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Q

Identify if manic or hypomanic in Bipolar Disorder:

During the mood disturbance is sufficiently severe to cause impairment in occupational functioning or in usual social activities or relationships or necessitates hospitalizations
Not due to physical substance abuse

A

Manic episode

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Q

Identify if manic or hypomanic in Bipolar Disorder:

Low mood
Lack of interest or pleasure in activities once enjoyed
Slowed down behavior
Fatigue or loss of energy

A

Hypomanic episode

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Q

Identify if manic or hypomanic in Bipolar Disorder:

Thinking of death or suicide
Feeling guilty
Sleeping problems
Problems concentrating

A

Hypomanic episode

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Q

What are the four major chemical subgroups of antipsychotic drugs and lithium?

A

Phenothiazines
Thioxanthenes
Butyrophenones
Atypical Antipsychotics

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Q

Identify this major chemical subgroup:

Aliphatic (Chlorpromazine)
Advantage: Generic, inexpensive
Disadvantage: Many adverse effects, especially autonomic

A

Phenothiazines

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Q

Identify this major chemical subgroup:

Piperidine (Thioridazine)
Advantage: Slight extrapyramidal syndrome, generic
Disadvantage: 800 mg/d limit; no parenteral form; cardiotoxicity

A

Phenothiazines

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Q

Identify this major chemical subgroups:

Piperazine (Fluphenazine)
Advantage: Depot form also available (enanthate, decanoate)
Disadvantage: Possible increased tardive dyskinesia

A

Phenothiazines

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Q

Identify this major chemical subgroups:

Thiothixene
Advantage: Parenteral form also available; possible decreased tardive dyskinesia
Disadvantage: Uncertain

A

Thioxanthenes

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Q

Identify this major chemical subgroups:

Haloperidol
Advantage: Parenteral form also available; generic
Disadvantage: Severe extrapyramidal syndrome

A

Butyrophenones

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Q

Identify this major chemical subgroup:

Clozapine
Advantage: May benefit treatment-resistant patients; little extrapyramidal toxicity
Disadvantage: May cause agranulocytosis in up to 2% of patients

A

Atypical Antipsychotic

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Q

Identify this major chemical subgroups:

Loxapine
Advantage: Possible no weight gain
Disadvantage: Uncertain

A

Atypical Antipsychotic

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Q

Identify this major chemical subgroup:

More effective
Less toxic
More costly
Prescribed generically

A

Atypical Antipsychotic

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Q

What are the pharmacokinetics of antipsychotic drugs and lithium?

A

Well absorbed when given orally
Lipid soluble
Bound extensively to plasma proteins
Require metabolism by liver enzymes before elimination
Long plasma half-lives
IV forms

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Q

Whats the IV forms in pharmacokinetics of Antipsychotic Drugs and Lithium?

A

Rapid initiation
Depot treatment

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# Identify this mechanism of action: Relative excess of functional activity of dopamine

The Dopamine Hypothesis

# Identify this mechanism of action: - Not fully satisfactory - Antipsychotic drugs are only partly effective in most patients - Many effective drugs have a much higher affinity for other receptors than D2 receptors

The Dopamine Hypothesis

# Identify this mechanism of action: Many antipsychotic drugs **block brain dopamine receptors** (especially D2 receptors)

The Dopamine Hypothesis

What are the dopamine-agonist drugs that exacerbate schizophrenia?

- Amphetamine - Levodopa

# Identify this mechanism of action: Increased density of dopamine receptors has been detected in certain brain regions of **untreated schizophrenia.**

Dopamine hypothesis

# Identify this mechanism of action: - Has 5 different dopamine receptors - Therapeutic efficacy of most older antipsychotic drugs correlate with relative affinity to D2 receptors

Dopamine Receptors

# Identify this mechanism of action: Correlation between blocking of D2 receptors and extrapyramidal dysfunction

Dopamine Receptors

# Identify this mechanism of action: Newer atypical antipsychotic agents have higher affinities for other receptors than for the D2 receptor

Other receptors

# Identify this mechanism of action: Table on relative receptor blocking actions of neuroleptic drugs (Katzung)

Other receptors

# Identify this mechanism of action: Alpha adrenoceptor blockade- antipsychotic effect of most drugs

Other receptors

# Enumerate the receptor based on this mechanism of actions: - **Newer** atypical drugs - High affinity for **5-HT2A** - May also interact with D2 and other receptors

* Olanzapine * Quetiapine * Risperidone

# Enumerate the receptor based on this mechanism of actions: - Significant **D4** and **5-HT2** receptor blocking actions - **Low** affinity for **D2** receptors

Clozapine

# Identify this mechanism of action: Causes less extrapyramidal dysfunction than standard drugs

OTHER RECEPTORS

All antipsychotic drugs have H1 receptor blockade to some degree, except:

Haloperidol

# True or False: In **Dopaminergic receptor blockade**, it has major effect for **older** antipsychotics.

True

What are the Dopaminergic tracts in the brain?

- Mesocortical-mesolimbic - Nigrostriatal tract - Tuberoinfundibular pathways - Chemoreceptor trigger zone | Mintis (MNTC)

# Identify what Dopaminergic tracts: Menstruation and mood

Mesocortical-mesolimbic pathway

# Identify what Dopaminergic tracts: Extrapyramidal function

Nigrostriatal tract

# Identify what Dopaminergic tracts: Prolactin release

Tuberoinfundibular pathways

# Identify what Dopaminergic tracts: Emesis

Chemoreceptor trigger zone

# Identify what blockade: Blockade of Antipsychotic effect of the drug

Blockade #1

# Identify what blockade: Blockade of Antiemetic properties

Blockade of #4

# Identify what blockade: Blockade of Adverse effects like extrapyramidal dysfunction and hyperprolactinemia respectively

Blockade #2 and#3

Treatment of schizophrenia includes reducing some of the positive symptoms, what are these positive symptoms?

- Hyperactivity - Bizarre ideation - Hallucinations and delusions

Facilitate functioning in both out and inpatient environments

Treatment of schizophrenia

Negative symptoms of Treatment of schizophrenia

- Older drugs do not have much effect - Newer atypical drugs improve some 1. Emotional blunting 2. Social withdrawal

Other psychiatric and neurologic indications:

Mania | Used together with lithium.

Drug that is sole agent in the manic phase

Olanzapine

Drug that is mood stabilizer in bipolar disorders

Olanzapine

What is the drug treated for Tourette's syndrome?

Molindone

What is the treatment for Alzheimer’s and Parkinsonism?

Newer drugs

What are the effects of nonpsychiatric indications?

- Antiemetic action - Antipruritics

# Identify this nonpsychiatric indication: H1 receptor blockade basis for use.

Antipruritics

# Identify this nonpsychiatric indication: - Phenothiazines except thioridazine - Prochlorperazine

Antiemetic action

Parkinson-like syndrome

* Rigidity * Akinesia * Flat facies * Tremor

# Identify this toxicity: Dose dependent extrapyramidal effects

Reversible neurologic effects

# Identify this toxicity: Decrease in dose and antagonized with muscarinic blocking agents

Reversible neurologic effects

What are the drugs that occurs most frequently in reversible neurologic effects?

* Haloperidol * Fluphenazine * Trifluoperazine

# Identify this toxicity: Less frequent with clozapine Less common with the newer drug

Reversible neurologic effects

# Identify this toxicity: Other neurologic dysfunction in Reversible neurologic effects

* Akathisia * Dystonia * Respond to diphenhydramine and muscarinic blocking agents

# Identify this toxicity: Choreoathetoid movements of the muscle of the lips and buccal cavity

Tardive dyskinesia

# Identify this toxicity: - Tend to develop after years of therapy - May appear as early as 6 months - Maybe irreversible

Tardive dyskinesia

# Identify this toxicity: Antimuscarinic drugs that **improve extrapyramidal effects** increase the severity of symptoms.

Tardive dyskinesia

# Identify this disorder: - No effective drug for treatment - Switching to clozapine does not exacerbate the condition

Tardive dyskinesia

# Identify this toxicity: - Improved temporarily by increasing neuroleptic dosage - Maybe caused by dopamine receptor sensitization

Tardive dyskinesia

# Identify this toxicity: Result from blockade of peripheral muscarinic receptors and alpha adrenoceptors

Autonomic effects

# Drug: Strongest autonomic effects

Thioridazine

# Drug: Weakest autonomic effects

Haloperidol

# Toxicity: Intermediate autonomic effects

Clozapine and most atypical antipyschotics

# Toxicity: Atropine-like effects

* Dry mouth * Constipation * Urinary retention * Visual problems * Not with ziprasidone and aripiprazol

# Toxicity: Alpha receptor blockade

- Postural hypotension - All atypical drugs

# Drug: Failure to ejaculate

Phenothiazines

# Endocrine and metabolic effects: Dopamine D2 receptor blockade in the pituitary

* Hyperprolactinemia * Gynecomastia * Amenorrhea-galactorrhea syndrome * Infertility

Endocrine and metabolic effects

- Dopamine D2 receptor blockade in the pituitary - Weight gain and hyperglycemia

# Drug: Weight gain and hyperglycemia

* Clozapine * Olanzapine

# Toxicity: Neuroleptic malignant syndrome (NMS) signs and symptoms

* Muscle rigidity * Impairment of sweating * Hyperpyrexia * Autonomic instability

# Toxicity: * Patients who are sensitive to the extrapyramidal effects are prone to develop NMS * Life threatening

Neuroleptic malignant syndrome

What are the treatment used for Neuroleptic malignant syndrome (NMS)?

* Dantrolene * Dopamine agonist

# Sedation (toxicity): More marked sedation

Phenothiazines (chlorpromazine)

# Sedation (toxicity): Less sedating among the older drugs

Fluphenazine and haloperidol

# Sedation (toxicity): Least sedating among newer drugs

Aripiprazole

# Miscellaneous (toxicity): Visual impairment due to retinal deposits

Thioridazine

# Miscellaneous (toxicity): At high doses, fatal ventricular arrhythmias

Thioridazine

# Miscellaneous (toxicity): Arrhythmias

Ziprasidone

# Miscellaneous (toxicity): Agranulocytosis, seizure at high doses

Clozapine

Miscellaneous toxicities

* Arrhythmias * Agranulocytosis, seizure at high doses * At high doses, fatal ventricular arrhythmias * Visual impairment due to retinal deposits

# Overdosage toxicity: Drug for seizures:

* Diazepam * Phenytoin

This is absorbed rapidly and completely from the gut and distributed throughout the body water.

Lithium

Lithium is cleared by the kidney at a rate of __ of creatinine.

1/5

Half-life of Lithium:

20 hours

# What week of therapy for Lithium: * Plasma levels monitored * Effective and safe dosage regimen

1st week of therapy

Lithium may increase to toxic levels by:

* Dehydration * Treatment with thiazide diuretics

Drug that increases renal clearance in lithium:

Theophylline

MOA of lithium

* Recycling of neuronal membrane phosphoinosotides (IP3 & DAG - neurotransmission)

Alternative drugs for lithium:

* Olanzapine * Valproic acid * Carbamazepine * Clonazepam * Gabapentin * Lamotrigine

# Toxicity of Lithium: Increase congentical cardiac anomalies

Ebstein's anomaly

# T or F: The toxicity of Lithium has containdicated in nursing mothers.

True