Antipsychotics

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!