Antipsychotic Drugs

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What are the functions impaired in Psychosis?

Mental capacity Affective response Capacity to recognize reality Communication Relating to others

What is Schizophrenia?
What are POSITIVE Symptoms of Schizophrenia?
A dimunition or loss of normal functions in Schizophrenia is termed?

Breakdown of integration between Emotions Thought Actions

Positive symptoms -An EXCESS of normal functions Delusion Thought disorder Perceptual disturbances Incongruous mood Increased motor function

NEGATIVE Symptoms Poverty of Speech Loss of emotional responsiveness Reduced motor function Social withdrawal

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What is the biological basis of the Positive symptoms in Schizophrenia? What evidence supports this Dopaminergic activity in Schiz?

Overactivity of DOPAMINE neurons in - MESO-LIMBIC Dopamine Pathway

Drugs that Increase Dopaminergic Activity - Increase or Produce Positive psychotic symptoms Drugs that Decrease Dopaminergic Activity - Decrease or Stop Positive symptoms

Which 2 drugs can cause a Paranoid psychosis indistinguishable from Schiz?

Amphetamines and Cocaine If given repeatedly

Which receptor does Antipsychotics block?

D2 recptors

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Name the 4 well defined Dopamine pathways in the brain

Mesolimbic NIgrostriatal Mesocortical Tuberoinfundibular

It projects from the Brainstem to the Limbic area Controls BEHAVIOUR

The Mesolimbic Pathway involves ..?

Overactivity of the Mesolimbic pathway produces..?

Delusions Hallucinations These symptoms are decreased when the Mesolimbic pathway is shut down by blocking Post synaptic dopamine receptors (hypothesized)

The Nigrostriatal Pathway projects from...?

the Substantia Nigra to the Corpus Striatum Controls MOVEMENT

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Blocking the dopamine receptors in the Nigrostriatal Pathway causes?

How are the side effects of blocking post synaptic dopamine receptors in the Nigrostriatal Pathway caused?

Disorders of movement like those in Parkinson's disease

The Nigrostriatal Pathway projects to the Basal Ganglia which forms part of the Extrapyramidal nueronal system of the CNS Side effects are called EXTRA PYRAMIDAL symptoms - a set of movement disorders

It may be involved in How is the mediating.. Mesocortical Pathway Positive and perharps involved in Schiz? Negative symptoms
How does Classical or Typical antipsychotics affect the Mesocortical Pathway?
Blockade of dopamine receptors in the pathway They produce Blunting of emotions and various Cognitive side effects They are not useful for negative symptoms

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How does blockade of dopamine receptors affect the Tuberoinfundibular pathway?

When dopamine receptors are blocked... They cause Prolactin levels to rise Galactorrhea Dopamine released f rom neurons in this pathway INHIBITS Prolactin secretion

What are the other names for antipsychotic drugs?

NEUROLEPTIC drugs MAJOR TRANQUILIZERS

Chlopromazine Fluphenazine Haloperidol Thioridazine Thiothixene Two famous drugs are Chlopromazine and Haloperidol

List the Classical or Typical antipsychotics.

List the Atypical antipsychotics

Clozapine Risperidone Olanzapine Quetiopine Ziprasidone Aripiprazole Paliperidone

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What is the efficacy of Classical antiphych. drugs related to? How are the Atypical antiphych. drugs different to Classical ? Clozapine an atypical antiphych. drugs has a high affinity for which receptors? Risperidone blocks which recptor to a greater extent than D2?

The efficacy is closely related to their ability to block D2 receptors in Mesolimbic pathway

They have Higher affinities for other receptors particularly 5-HT than D2 They appear to exert part of their action by blocking 5-HT receptors They are MUCH less likely to cause Extrapyramidal symptoms

D1, D4, 5HT2, M, Alpha adrenergic But it also blocks D2

5HT2 Unlike Clozipine it can cause EPS but this is rare at normal therapeutic doses

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Most of the Atypicals have High affinity for which 5-HT receptors? List the differences of Clozapine from Typical antipsychotic agents. What is the minimal definition for an Atypical antipsychotic?

'5-HT2A'
*Minimal. if any, Extrapyramidal Symptoms (EPS) *Essentially, NO Tardive dyskinesia *Minimal Increases in Prolactin *Negative symptom efficacy *Efficacy in treatment of refractory populations

*Dual antagonism of Serotonin 5-HT2A and Dopamine D2 receptors *Reduced propensity for EPS

What effect does Classical antipsych. have on the Mesolimbic and Nigrostriatal system?

D2 blockade of the Mesolimbic Relieves the Positive symptoms of Schizophrenia but.... D2 blockade of the Nigrostriatal system causes Extrapyramidal side effects

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How does SDAs (serotonin-dopamine antagonists) affect the Mesolimbic and Nigrostriatal system?

D2 blockade of the Mesolimbic -Relieves the Positive symptoms of Schizophrenia (same as classical) however..... They are Competitive Antagonists at Pre synaptic 5HT2 receptors in the Nigrostriatal pathway

How does the Competitive Antagonism at Pre synaptic 5HT2 receptors in the Nigrostriatal pathway assist in reducing the EPS effects by SDAs?

5-HT2 re ce pto rs functio n like alpha 2 re ce pto s o n pre syaptic ne uro ns The y inhibit the re le ase o f Do pamine whe n acte d o n by Se ro to nin but SDAs blo ck this inhibitio n and so Do pamine is re le ase d This de cre ase s the Do pamine blo ckade and pre ve nts the EPS

What are the 2 major actions of antipsychotics?

What are the Extra pyramidal effects associated with?

*Antips ychotics (as the name s ugges ts ) - they reduce halucination and agitation they have a calming effect *Antiemetics - mediated by blockade of D2 at the chemoreceptor trigger z one (mos t older antps ychotics hve this effect) Many als o block Mus carinic, alpha 1 adrenergic, and H1 receptors this caus es a variety of s ide effects

High potency of the drug for D2 receptors The more potent the drug for D2, the more EPS

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What r the 2 drugs that have a high affinity for D2 receptors? Which classical antipsych. is low potency at D2 receptors?

Haloperidol Fluphenazine both are Classical antipsychotics with High Potency

Thiorizadine EPS are less likely to occur

Thiorizadine Chlopromazine EPS are less likely to occur because of this

Which 2 classical antipsych. are Stong anticholinergics?

Which 2 antipsych. has no Antiemetic effects?

Aripiprazole Thioridazine Clopromazine is useful as pharmacological antiemetic

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How are antipsych. different from barbituates?

Antipsych. that have Low Potency at D2 also have what effect on EPS?

Antipsych. DO NOT depress intellectual function Motor incoordination is minimal

They have low Extrapyramidal symptoms Remember this is the same for High potency at 5HT2

Which drug causes the worse EPS? The Best antipsych. drug?

Haloperidol High potency at D2 -High EPS Low potency at M or 5HT2 No sedation

Clozapine Medium potency D2 Medium potency M High potency at 5HT2 - NO EPS

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Which 2 antipsych. drugs cause Hypotension?

Which receptor acted on by antipsych. drugs causes sedation? Rispiridone has High potency at D2 and at 5HT2. It thus has what effect on EPS? What is the Most important unwanted AE of antipsych. drugs?

Chlopromazine Thioridazine They block alpha 1 receptors

5HT1 Low EPS

Tardive dyskinesia late occuring syndrome of abnormal choreoathetoid movements

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May be due to UPWhat is the possible regulation of Dopamine cause of Tardive receptors - due to dyskinesia ? longterm blockade

Which antipsych. causes Agronulocytosis in 12% of patients?

Clozapine This makes it a 2nd line drug NOT the DOC

Blockade of D2 in Pituitary Increase Prolactin secretion In women- amenorrheagalactorrhea syndrome and infertility

What causes Galactorrhea from use of antipsych.?

What are the endocrine effects of antipsych. in men?

Impotence Loss of Libido Infertility

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Atypicals Which group of antipsych. is less likely They cause more Weight to produce elevations gain and incr. in Lipids in Prolactin? than some Typical agents

Which 2 Atypicals cause the worse Weight gain?

Which Atypical drug causes the LEAST Weight gain?

Clozapine Olanzipine Consequence of Wt gain: HTN, DM type 2, Hyperlipidemia

ZIPRASID ONE
Anticholinergic effects but... This antimuscarinic effect may be beneficial in relation to EPS

Blockade of Muscarinic receptors can cause..?

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Beside orthostatic Hypotension, blockade of alpha 1 can cause........in men?

Impaired Ejaculation
Thioridazine cause Retinal deposits Chlopromazine causes Cornea and Lens deposits

What effect does Thioridazine have on the eye?

Which drug causes reversible abnormalities in T waves?

Thiorazidine at High doses

Which Atypical has the Greatest risk of QT prolongation?

Ziprasidone

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What is the Rare but life-threatning disorder of antipsych.? What are the symptoms of Neuroleptic Malignant Syndrome? Apart from Schizophrenia what are the other clinical uses of antipsych.?

Neuroleptic Malignant Syndrome Occurs in patients who are extremely sensitive to the EPS of antipsych.

Muscle rigidity Fever altered mental status Stupor Unstable BP Myoglobinemia

Bipolar disorder Tourette's syndrome Huntington's disease -paranoid behaviour Alzheimer's Dementia-Control of disturbed behaviour

What are Nonpyschyatric uses of antipsych.?

Nausea, vomiting Droperidol is used in combo with Fentanyl in Neuroleptic -anesthesia

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Prochloperazin 2 antipsych e promoted solely as antiemetics? Benzquinamide

Which antipsych is Category B in pregnancy?
Why are Atypicals prefered as DOC?
Only Clopazine all others are Category C
*Benefit for Negative symptoms and cognition *Diminished risk of Tardive Dyskinesia, EPS *Lesser incr. of prolactin levels

Clozapine is reserved for refractory patients, why?

Potential for Agranulocytosi s

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Antipsych may be used to control Agitation or psychosis in ....?

Depressed patients Chloproma zine

Conventional antiParkinson's drugs of the Muscarinic type Never Levadopa

Jaundice is caused by which drug?

AE of Parkinsonism can be treated with?

What are some EPS?

Parkinsonism Akathisia -uncontrollable restlessness acute Dystonic Reactions spastic retrocollis or torticollis

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Whose reality is 'The real reality" ??

Us or them