Pharmacology: Test 2 Antipsychotics Lec 35

Front 1

Drugs to remember in this lecture?

Back 1

chlorpromazine, haloperidol, clozapine, risperidone, olanzapine, quetiapine, ziprasidone, aripiprazole, diphenhydramine, benztropine, trihexphenidyl.

Front 2

What's the dopamine hypothesis in Schizophrenia?

Back 2

All antipsychotics (neuroleptics) block the DA receptors. These pts were found to have higher D2 receptor density. The sx are exacerbated with DA agonists.

Front 3

What's neuroleptic syndrome?

Back 3

it is the sx following antipsychotic drugs: lack of initiative, disinterest in the environment, and limited range of affect.

Front 4

Side effects of antipsychotics?

Back 4

due to their blockade of cholinergic and alpha-adrenergic receptors, and DA-Rs. Side effects are common but not severe and are reversible excepto for 'tardive dyskinesia'.

both neurological and non-neurological side effects.

Front 5

What are the non-neurological side effects?

Back 5

orthostatic hypotension (alpha blockade), >> reflex tachycardia.// decrease sex drive, decrease ejaculation (alpha blockade).// increased PRL secretion (DA blockade).// Weight gain especially with never drugs.// sedation esp. w/ chlorpromazine, least with haloperidol.// anticholinergic effects, phototoxicity.// Bloody dyskriasis (leukopenia).//

Front 6

Neurological side effects of antipsychotic drugs?

Back 6

aka extrapyrimidal b/c involve involuntary motor activity, common with older 'typical' antipsychotics.//

Front 7

Neurological side effects of antipsychotic drugs: Parkinsonism Syndrome

Back 7

Parkinsonism syndrome: DA-r blockage in striatum incl. dyskinesia, tremor, mask-like face, shuffline gait//

control by: lowering dose, adding anticholinergic (benztropine, trihexphenidyl)

Front 8

Neurological side effects of antipsychotic drugs: Dystonias

Back 8

bizzare, jerking, spastic movement of neck, face, eyes, tongue, tosor, arms, or legs. //

Trt with anticholinergic (benztropine) or antihistamine (diphenhydramine).//

Front 9

Neurological side effects of antipsychotic drugs: akathisias

Back 9

aka Restless Leg Syndrome: feeling of restlessness or agitation, pt unable to sit still //

Tx by lowering dose or with benztropine.

Front 10

Tardive Dyskinesia

Back 10

No tx, not reversible, appears late after months or years of treatment. Involuntary, rhythmic movement of sucking, chewing, licking, and pursing of tongue and mouth.//

Due to upregulation of DA-Rs. supressed by increase antipsychotic dose. Antiparkinon drugs not useful.

Front 11

Newer Atypical antipsychotics

Back 11

These drugs have fewer extrapyramidal side effects than typical drugs. Incl. Risperidone, clozapine, olanzapine, quetiapine, ziprasidone.//

Problem: weight gain with atypical drugs.

Front 12

Newer Atypical antipsychotics vs. typical drugs

Back 12

compared to haloperidol, atypical drugs are as good in relieving pos. sx (paranoia, delusions, hallucinations) in schizopherenics. It is better than haloperidol in relieving neg. sx (apathy and withdrawal).

block DA D2-R, and 5HT-2a-Rs.//

Weight gain a huge problem leading to Type II diabetes.

Front 13

Risperidone

Back 13

some PRL elevation, at higher conc. causes extrapyramidal sd effects

Front 14

clozapine

Back 14

no Tardive dyskinesia. but AGRANULOCYTOSIS. Therefore, requires weekly WBC count tests.//

has great affinity for D4 DA-Rs.// D4 not found in striatum (caudate-putamen)

Front 15

Olanzapine

Back 15

structuraly similar to clozapine, and thus binds D4 and 5HT-2a-R, but also has moderate affinity for D2-R.//

Low extrapyramidal effects, less PRL elevatin. NO evidence of tardive dyskinesia or hematologic abnormalities.

Front 16

What's so special about clozapine and olanzapine?

Back 16

Only drugs that improve congnitive fxn.

Front 17

Quetiapine and ziprasidone

Back 17

higher affinity for 5HT-2a-r than D2 >> Antagonist to histamine receptor >> sedation.// alpha blockade causes some hypotension. //

Higer dose do not increase extrapyramidal sx or hyperprolactinemia as much as risperidone or olanzapine.//

Front 18

See page 5 of lect 35 for table on drugs covered

Back 18

End of CNS drugs.