Antipsychotics

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• Antipsychotics

• First Generation

• Second Generation

• General Information

• Also known as Typical: Mostly blocks Dopamine Receptors (D2)

• Also known as Atypicals

• Blocks Dopamine and Seretonin Receptors (D2 and 5HT2A)

• Reudce halucinations and delusions associated with Schizofrenia

• Neurological Side Effects

• Most 2nd Gen Meds can help with negative symtpoms (Ex. Clozapina)

• D2 Blockers are not seletive, therefore they generate side effects

• Mesocortical Pathway

• Nigrostriatal Pathway

• Tuberoinfundibular Pathway

• Achieved by blocking D2 in the Mesolimbic Pathway

• Negative Symptoms & Executive Functioning Deficits

• Extrapyrimidal side effects

• Increased Prolactin

• Metabolic Side Effects

• Major Adverse Effects of receptor blockades

• D2 dopamine: Extrapyramidal Symptoms; Prolactin Increase

• Alfa 1 norepinephrine: Postural Hypotension

• H1 histamine: Sedation/drowsiness; weight gain

• M1 muscarinic ACh: Memory deficits; 

• 5HT(1B;2C) serotonin: weight gain

• Similar Efficacy Difference in Potency

• Pharmacokinetics 

• Lipid soluble

• 20-40 hour half life

• Some metabolites can persist for months of stopping Rx

• High Potency

• Low Potency

• Low or High Potency: This refers to a Rx affinity for D2 receptors. Influences adverse efects

• Haloperidol-Haldol

• Thiordazine

• Chlopromazine

• Perphenazine-Trilafon

• Pimozide-ORAP

• Fluphenazine

• Loxapine

• Prochlorperazine-COMPRO/PROCOMP

• Will cause sedation More Anticolinergic, antiadrenergic and antihistaminic 

• Less extrapyramidal effects​​​​

• Less Anticolinergic, antiadrenergic and antihistaminic 

• Less affinity for D2

• More affinity for D2

• More extrapyramidal effects​​​​

• Antipsychotic Overdose: Neuroleptic Malignant Syndrome

• -High Fever (102 to 104 F) -Muscle stiffness -Sweating a lot -Anxiety or other changes in mental state -Fast or abnormal heartbeat -Quick breathing NMS can damage muscles and cause very high or low blood pressure. If you’re not treated, you can get serious problems, like: -Kidney failure -Heart and lung failure -Lack of oxygen in the body -Infection in the lungs caused by breathing in fluid (aspiration pneumonia) More acid in the body

• Pine

• Done

• Pip

• Clozapine

• Olanzapine-Zyprexa

• Quetiapine-Seroquell

• Palipiperidone-Invega

• Ziprasidone-Geodon

• Risperidone-Risperdal

• Lurasidone-Latuda

• Aripiprazole-Abilify

• Increases flow of DA in the nigrostriatal pathway

• Diabetes, Hypercholesterolemia, weight gain and cardiac effects

• Less likely extrapyramidal effects​​​​

• This is done by allowing more DA in the PFC

• Tx: Aggression and Violence

• Tx at different dosages using XR: (High), antidepressant (medium), hypnotic (low)

• D2, 5HT2C, Alpha-1, H1

• Sedation: High; Weight Gain: High; EPS: Low

• Warning: Can supress bone marrow, cause convulsions and orthostatic hypotension

• Tx: Psychosis from 13 y/o and up

• High Dosage XR: Antipsychotic H1, 5HT2A, D2

• Medium Dosage XR: Antidepressant Agonist: 5HT1A; Antagonist: 5HT7, Alpha-2, 5HT!B

• Sedaion: Very High; Weight Gain: High: EPS: Low

• Warning: orthostatic hypotension, increase in triglycerides and resistance to insuline

• D2, 5HT2A, 5HT2C, H1, M3

• Sedation: High; Weight Gain: Very High; EPS: High

• Warning: increase in triglycerides and resistance to insuline

• Tx: Irritability and agression in autism (5-16); psychosis

• D2, 5HT2A, Alpha-1

• High Dosage: Works like Tipical Antipsychotic; High EPS

• Medium Dosage: Psychosis, Maniac Bipolar and can be used in children and adolecents

• Sedation: medium; Weight Gain: High; EPS: Very High

• Tx: Psychosis and Mania (13+); Irritability in autism (6-17)

• Warning: Even in low dosages it can inhibit prolactin and make kids fat

• D2,5HT2A, 5HT7, 5HT1A

• Sedation: Very Low; Weight Gain: Very Low; EPS: Low

• Tx: Psychosis patients that gained weight are out on this Rx

• D2, 5HT2A, 5HT2C, 5HT1A, 5HT7, Alpha-2

• Has to be taken with food

• Can be used as tranquilizers for agitated and disruptive behavior

• Withdrawl of Antipsychotics

• -Vomiting -Nausea -Diarrhea -Insomnia -Restlessness -Anxiety -Agitation -Dizziness -Loss of motor control

• Will usually show up in the first few days after abstiaining or reducing dosage

• NOT ADDICTIVE!

• AVOID ANFETAMINES, COCAIN AND L-DOPA!