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Antipsychotics. Antipsychotics are drugs used to treat psychoses, which is a disorder associate with loosely organized thoughts, bizarre and illogical behaviors, hallucinations (usually auditory) and delusions. Schizophrenia is associated with these characteristics (positive symptoms).

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slide1

Antipsychotics

Antipsychotics are drugs used to treat psychoses, which is a disorder

associate with loosely organized thoughts, bizarre and illogical behaviors,

hallucinations (usually auditory) and delusions. Schizophrenia is associated

with these characteristics (positive symptoms).

Psychoses can be organic and related to drugs such as central anticholinergic

agents, NMDA antagonist (PCP, phenyclidine) and dementia. Idiopathic

psychoses possibly caused by stress.

Drugs are used in psychotic patients to produce a calming effect thus some are

classified as major tranquilizers. The ones the lessen response to emotional stimuli

without altering consciousness are called neuroleptics.

Typical antipsychotic blocks the dopamine at mesolimbic D2 and D3 receptors.

Atypical antipsychotic blocks the dopamine at mesolimbic D2 and D3 receptors in

addition 5-HT2A

slide2

Drugs that cause schizophrenia

Amphetamine and lysergic acid diethylamide (LSD) used in animal

models to produce schizophrenia.

Central anticholinergic produce schizophrenia by blocking M1 or M3.

Phenyclidine (PCP) induce psychosis a CNS stimulation

(Dissociative Agents)

slide3

Treatment for psychosis

Phenothiazine

SAR

Substitution at the 2-position with electron withdrawing groupsincrease activity alone with unshared electron pair.

Substitution at the 3-position can increase activity in comparison with unsubstituted but lesser of effect than substitution at 2-position.

Three-carbon atom chain is essential for activity. Shortening or lengthening will decrease activity (pseudo ring formation).

Branching -position by methyl activity varies. Dextro isomers are more activity of chiral isomers. Alkyl groups larger than methyl cause a decrease activity.

slide4

SAR continued

Dimethyl amino require for optimal activity. The monomethyl amino has less activity.

Activity can be enhanced by fusion the dimethyl groups to form a piperidine

piperazines groups

The substitutes are believed to for a pseudo ring with the protonated amino group

(X-ray crystal structure). Align the p-hydroxyl of Dopamine with sulfur and aliphatic

amine portions. Substitution at 1-position is believe interfere with the pseudo ring

formation thus a decrease in activity.

slide5

Important Notes for Antipsychotics

Side effects associated with antipsychotics

Extrapyramidal Side Effects (EPS): dystonia, motor restlessness Parkinson-like (rigidity and tremor), tardive dyskinesia (irreversible);

alone with tachycardia, hypotension, hyperprolactinemia,

gynecomastia.

Atypical antipsychotics have less risk of producing EPS

Atypical antipsychotics are effective in treating negative symptoms

(social withdraw, apathy, speech deficit)

Both cause increase risk of weight gain and diabetes but more so with

atypical psychotics

slide6

Metabolism:

Major metabolism is hydroxylation aromatic ring para to 10-nitrogen

(not ring bearing EW) follow by conjugation with glucuronic acid.

Dialkylamino

Thorazine (Chlorpromazine)

It was the first phenothiazine used as antipsychotic.

Uses include nausea and vomiting and hiccough

alone psychoses. It has significant sedative and

hypotensive properties. Contraindication with

antidepressant and anesthetics as with

other antipsychotics.

Sparine (Promazine)

It was introduce after 2-chloro

substituted Thorazine. It is less

activity than Thorazine.

slide7

Vesprin (Triflupromazine hydrochloride)

Greater activity per mg in comparison

with Thorazine. Lower sedative and

hypotensive side effects than Thorazine

slide8

Piperidine subgroup

Mellaril (Thioridazine hydrochloride)

High anticholinergic activity.

Sedation and hypotension are its

side effects.

Pigmentary retinopathy

Serentil (Mesoridazine Besylate)

Metabolite of Mellaril

Does not cause pigmentary

retinopathy.

slide9

Piperazine

Trilafon (Perphenazine)

Use as antipsychotic and

antiemetic. Ester (decanoate)

IM Depot

Compazine (Prochlorperazine maleate)

More activity per mg in comparison

with Thorazine. Mainly use as antiemetic.

slide10

Stelazine (Trifluperazine)

Tindal (Acetophenazine)

Ester (IM Depot)

Torecan (Triethylperazine)

slide11

Thioxanthene

Prolixin (Fluphenazine HCl)

Most potent on the mg basis

Ester (IM Depot)

Navane (Thiothixene)

Replacement of the nitrogen with a

double bonded carbon.

Z isomers is the most active.

Modified Ethyl alcohol ester

(Decanoate) (Flupenthixol)

slide12

Fluorobutyrophenones

SAR

AR1 is a aromatic system (p-fluoro increase activity)

X is carbonyl (highest activity)

CHOH and CH aryl (good activity)

When n=3 (highest activity)

longer or shorter chain decrease activity

Piperidine ring (highest activity) AR2 is required attached at 4-position.

Y group as hydroxyl can improve activity.

Neurotoxic metabolite (pyridine quaternary salt form)

Student tried to make meperidine

meperidine

slide14

Inapsine (Droperidol)

Antipsychotic with antiemetic properities

Used in combination Fentanyl preanesthetic

(Innovar)

Haldol (Haloperidol)

Use as antipsychotic in the treatment

schizophrenia, psychoses caused

by brain damage and Tourette’s syndrome.

slide15

Risperdal (Risperidone)

Atypical antipsychotic

Hydroxyl active metabolite (*)

Antipsychotic/antidepressant (Trazodone)

Structure like

Combination with Haldol for Parkinson

5HT2A and D2 antagonist

Invega (Paliperidone)

Approved Dec. 2006

Atypical antipsychotic

slide16

**Atypical psychotics**

Daxopin (Loxapine succinate)

Dibenzoxazepine

Side effects similar to phenothiazines.

Clozaril (Clozapine)

Dibenzodiazepine

Not potent antipsychotic on mg basis

Agranulocytosis (clinical monitoring

Weekly for 6 months)

slide17

Zyprexa (Olanzapine)

Atypical antipsychotic

Thienobenzodiazepine

D2 and strongly 5HT2

receptor antagonist

Loxitane (Loxapine)

Typical antipsychotic

Undergoes N-dealkylation

to an active metabolite

Use often as anti-depressant

slide18

Asendin (Amoxapine)

Use often as anti-depressant

Seroquel (Quetiapine)

Dibenzothiazepine

Binds to H1 and a1 and a2; 5-HT2A

Receptors and low affinity D2 receptors

slide19

Benzamide

Roxiam(S-Remoxipride)

Benzamide

Less EPS than Haldol

Reglan (Metoclopramide)

D2 receptor antagonist

Antiemetic (chemoreceptor

trigger in brain stem)

Prokinetic (GI emptying)