Less sedation than the others and minimal muscarinic receptor effects D2 Schizo, Bipolar, Huntington's Chorea, Tourette's Toxicity = Extrapyramidal and hyperprolactinemia

Antipsychotic Drugs Flashcards by Fq Unknown

Psychosis

Inability to distinguish reality from delusion. Schizophrenia is the most common psychotic disorder and is the most hospitalized

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Delusions

False beliefs not held by people of the same cultural background

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Disordered Thinking

Confused thoughts that do not link up

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Hallucinations

Sensing things to feel real but do not exist

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Serotonin Hypothesis

LSD and other hallucinogens are agonists of 5-HT receptors. Serotonin is the endogenous agonist of these receptors. Modulate the release of dopamine, NE, glutamate, GABA and Ach in the cortex, limbic and striatum. Second gen antipsychotics are antagonists of this receptor keeping it in an inactivated state.

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Dopamine Hypothesis

Old and incomplete hypothesis. D2 receptor is targeted by 1st gen antipsychotics. Can cause psychosis with exogenous dopamine.

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Nigrastriatal pathway

Loss of these neurons contributes to Parkinson’s symptoms. 1st gen drugs block this pathway causing parkinsons symptoms.
Chlorpromazine / haloperidol

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Mesocortical pathway

Prefrontal cortex suppression causing flat mood, poor cognition and motivation + emotion

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Mesolimbic

When enhanced causes positive symptoms like hallucinations

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Tuberohypophyseal

Suppresion of this pathway by 1st gen antipsychotics can cause abnormal breast development in males.

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Extrapyramidal symptoms

Caused by blocking D2 receptors in the nigrostrital tract
-Parkinsonism (pill rolling tremor + rigidity) 5-30 days. Elderly
-Dystonia (grimacing and muscle spasms of the face and neck) 1-5 days. Generally in young individuals
- Akathisia (restlessness of the lower extremities) 5-60 days
-Tardive Dyskinesia (protrusion and rolling the tongue with a chewing motion) months to years. Elderly.

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Emergency Drug for Parkinsonism

Diphenhydramine

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Glutamate Hypothesis

PCP and MK-801 noncompetitive NMDA inhibitors causing cognitive impairment and psychosis

Serotonin antagonists better than D2 at blocking effects

Hypofuntion of NMDA receptors leads to decreased inhibition of neuronal function

Diminished GABAergic activity disinhibits leading to hyperstimulation

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Positive Symptoms

Hallucinations
Delusions
Disorganized thoughts

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Negative Symptoms

Alogia
Flattened Affect
Asocial

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Cognitive Sympotms

Memory issues
Attention Deficits
Planning
Decision Making

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Potency of First Gen

Low Potency
- Chlorpromazine
- Thioridazine
Most Potent
- Trifluoperazine
- Perphenzine
- Fluphenazine
Most Commonly Used
- Haloperidol

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Chlorpromazine

Stronger blocking D2 than serotonin

a receptor blockade (Hypotension)
Muscarinic receptor blockade (Dry mouth, nausea, constipation)
H1 receptor blockade (Drowsiness)
CNS Depression
Decreased Seizure Threshold
QT Prolongation (SCD)

Used un Schizo and Bipolar

Long Half Life

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Haloperidol (4)

Less sedation than the others and minimal muscarinic receptor effects

Schizo, Bipolar, Huntington’s Chorea, Tourette’s

Toxicity = Extrapyramidal and hyperprolactinemia

Second Gen Mechanism

Action is greater at the serotonin receptors than D2

Second Gen Effects

a receptor blockade 5ht

Muscarinic receptor blockade

Variable H1 receptor blockade

Second Gen Applications

Schizo, improves both positive and negative symptoms

Bipolar, adjuctive with valproate or lithium

Agitation in Alzheimers and Parkinson’s (Risperidone, Clozapine)

Major Depression, Tourette’s, ASD (Aripiprazole)

ASD(risperidone)

Parkinson’s dementia(Pimavanserin) - Also shortens lifespan for some reason

Why does aripiprazole not cause more severe side effects

Dual agonist/antagonist effects preventing dopamine response from going too low

Drugs with Strong Effects at Muscarinic (COC)

Clozapine, Olanzapine, Chlorpromazine

Constipation, bowel obstruction, urinary retention.

Monitor Bowel

Drugs with strong adrenergic blocking (CCT)

Clozapine, Chlorpromazine, Thioridazine Orthostatic Hypotension Titrate slowly

Drugs with strong histamine receptor blocking

Clozapine, Chlorpromazine, Olanzapine Sedation and Weight gain Cessation causes insomnia and sleep disturbances

Adverse Cardiac Effects

QRS Widening Ventricular Arrhythmia QT prolongation - SCD

Weight Gain from antipsychotics

Dyslipidemia and impairment in glycemic control Hyperleptinemia

Neuroleptic Malignant Syndrome

Decreased Activity at D2 from antipsychotics Parkinson's symptoms Hypothalamus effects ie, hyperthermia and increased BP + HR leading to CV and Resp complications Muscle Rigidity -> Rhabdo -> Renal failure

Management of Neuroleptic Malignant Syndrome

Mild : Rigidity + Tremor Benzos Moderate: Catatonia, confusion, and elevated temo Bromocriptine Severe Temp > 40 Dantrolene and cooling blankets

Serotonin Syndrome vs. NMS

Serotonin Syndrome Develops in 24 hours Neuromuscular hyperactivity Resolves Quickly Treat with Benzos and Serotonin blockers NMS Days to weeks Neuromuscular sluggishness Resolves slower Dantrolene and Bromocriptine

Schizophrenia(A)

Hallucinations and/or delusions and/or disorganized speech for 6 months Treat with second gen except clozapine b/c side effects Aripiprazole** Benzos for Catatonic schizo

Schizoaffective

Schizophrenia with mania+depression Treat with antipsychs and lithium/valproic

Drugs of choice for Bipolar

mood stabilizers rather than antidepressants because cause enhanced cycling Lithium/valproate + Aripiprazole/Olanzapine

Classification of Depression

Bipolar 1: high highs and low lows Bipolar 2: slight highs and still low lows Unipolar is just depression Cyclothymia: Moderate highs and lows Dysthymia: Mild depression

Unipolar Depression Drugs (AAL)

Antidepressants + Aripiprazole + Lithium

Carbamazepine

Mech: Unclear for bipolar. Sodium channel blocker Used in acute mania and for prophylaxis of depression SJS**

Lamotrigine

Not effective at treating acute mania SJS**

Valproic Acid

Increasingly used as first choice for acute maniaL

Lithium

Mech Unclear No significant antagonism on autonomic receptors or specific CNS No sedation Don't give to pregnant patients**

Lithium Toxicity

Intoxication, Ataxia, GI effects, CV, Hyperpyrexia Silent syndrome: Cerebellar and brainstem dysfunction, Extrapyramidal, Dementia

Tourette's

Looks like OCD early on Aripiprazole only approved therapy Haloperidol is used off label

Autism

Risperidone and aripiprazole used to treat irritability in autism patients

Psychosis in Parkinson's (ROC)

Loss of serotonin neurons and up-regulation of serotonin 2A receptors Risperidone, Olanzapine, Clozapine used Pimavanzserin is most effective parkinsons dementia but increased mortality

Huntington's(THC)

Overactivity in dopaminergic nigrostriatal pathways Tetrabenazine drug of choice Halperidol for chorea or clozapine for rigid HD

Alzheimer's (HRC)

Avoid use of medications with anticholinergic properties Tx Haloperidol, reperidone, or clozapine Nuerochemical disturbance deficiency Ach