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22 Cards in this Set
- Front
- Back
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What is a neuroleptic drug?
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refers to the production of extrapyramidal SE and often used to describe 1st generation antipsychotics.
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What is Chlorpromazine?
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1st generation antipsychotic
Structure: Phenothiazine |
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What are the properties of Chlorpromazine?
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lipid soluble, 90% plasma bound, long half-life ~30hrs
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Where does Chlorpromazine act?
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1. D2R antag-potent (def. propr)
2. a1 antag-fairly potent 3. weahe cholinergic antag 4. weak H1 antag 5. noncompetitvive channel blocker (ca and na) |
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What are the rapidly developing effects of Chlorpromazine?
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sedation, disinterest in environment, psychomotore slowing, emotional quieting.
"chemical straightjacket" |
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What is Chlorpromazine used for?
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treat acute psychotic symptoms, includes schizo and mania
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What are the delayed effects of Chlorpromazine?
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Anti-Schizo effects 92-3wks later)
*alleviates: tension, hyperactivity, combativenes, hostilility, hallucinations, acute delusions, anorexia, negativism and smts withdrawal. Less improved cognitive functions |
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What are the early onset SE of Chlorpromazine?
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Extrapyramidal SE
*Parkinson like sx *Akathisia *Acute dystonic reactions ***more common kids and young soon after start |
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What are the late onset SE of Chlorpromazine?
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Extrapyramidal:not reversible
*Tardive dyskinesia--prob. due to Receptor regulation |
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What is the mechanism of Chlorpromazine?
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Therapeutic and neuroleptic SE due to D@-R blocking by inc. conductance of K and reducing cAMP.
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Where does Chlorpromazine work in the CNS?
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Targets the frontal cortex and limbic system. i.e. Cortex, hippocampus, Nucleus accumbens, VTA...principlly the VTA that stretches to the other spots
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Why are their extrapyramidal SE?Chlorpromazine
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D2-R block in the striatum.
1. inc. anticholin. activity of striatum. 2. (late) change is genetic in receptors |
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Other SE of Chlorpromazine?
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Oversedation, OD in kids, Seizure with hx, CVS: a1blcok-ortho Hypotension, quinidine-like;dec. contract, reflex tachy; drymouth, inhibit ejeact, galactorrhea, amenorrhea
***neuroleptic malignant syndrome |
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What is Neuroleptic malignant syndrome?
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hyperthermia, diffuse muscle rigidity, autonomic sx-HTN,incontinence.
TX-dantrolene IV (muscle relax) then bromocriptine (d2 agonist) |
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How do you manage the early EP SE of Chlorpromazine?
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1.anticholinergic antipark drugs: diphenhydramine, trihexiphenidyl, benztropine
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What are the other 1st generation antipsychotic drugs?
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Depot form: fluphenazine decanoate
Low potency: Chlorpromazine, Thioridazine Intermed: Trifluoperazine, Perphenazine, Thiothixene High Pot: Haloperidol, Fluphenazine |
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What are the uses of 1st generation antipsychotics?
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1. Schizo
2. Gilles de la Tourette Syndrome 3. Huntington's Chorea 4. Acute manic episodes while on Li being built up 5. Schizo-affective disorders 6. Emesis |
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What is Clozapine?
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2nd generation antipsychotic/Atypical antipsych.
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What is different about 2nd generation anti-psychotics?
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*relatively little EPS, and more effective at negative sx
*antagonize 5-HT2R, D2, D2,(and/or)D4 |
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What are the properties of Clozapine?
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more anticholinergic than most antipsy, low affinity for D2R
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What are the SE of Clozapine?
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MAJOR: 1-2% Agranulocytosis, fatal if unchecked
minor:can cause weight gain and induce/exacerbate DM2, HTN, sleep apnea |
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What are the other 2nd generation Antipsy, that are diff. from Clozapine?
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olanzapine (zyprexa)
risperidone (Risperidal) quetiapine (Seroquel) sertindole (ziprasidone) |
