Glossary of Antipsychotic Drugs-CNS Pharm
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- What is a neuroleptic drug?
- refers to the production of extrapyramidal SE and often used to describe 1st generation antipsychotics.
- What is Chlorpromazine?
- 1st generation antipsychotic
Structure: Phenothiazine
- What are the properties of Chlorpromazine?
- lipid soluble, 90% plasma bound, long half-life ~30hrs
- Where does Chlorpromazine act?
- 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)
- What are the rapidly developing effects of Chlorpromazine?
- sedation, disinterest in environment, psychomotore slowing, emotional quieting.
"chemical straightjacket"
- What is Chlorpromazine used for?
- treat acute psychotic symptoms, includes schizo and mania
- What are the delayed effects of Chlorpromazine?
- Anti-Schizo effects 92-3wks later)
*alleviates: tension, hyperactivity, combativenes, hostilility, hallucinations, acute delusions, anorexia, negativism and smts withdrawal. Less improved cognitive functions
- What are the early onset SE of Chlorpromazine?
- Extrapyramidal SE
*Parkinson like sx
*Akathisia
*Acute dystonic reactions
***more common kids and young soon after start
- What are the late onset SE of Chlorpromazine?
- Extrapyramidal:not reversible
*Tardive dyskinesia--prob. due to Receptor regulation
- What is the mechanism of Chlorpromazine?
- Therapeutic and neuroleptic SE due to D@-R blocking by inc. conductance of K and reducing cAMP.
- Where does Chlorpromazine work in the CNS?
- Targets the frontal cortex and limbic system. i.e. Cortex, hippocampus, Nucleus accumbens, VTA...principlly the VTA that stretches to the other spots
- Why are their extrapyramidal SE?Chlorpromazine
- D2-R block in the striatum.
1. inc. anticholin. activity of striatum.
2. (late) change is genetic in receptors
- Other SE of Chlorpromazine?
- 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
- What is Neuroleptic malignant syndrome?
- hyperthermia, diffuse muscle rigidity, autonomic sx-HTN,incontinence.
TX-dantrolene IV (muscle relax) then bromocriptine (d2 agonist)
- How do you manage the early EP SE of Chlorpromazine?
- 1.anticholinergic antipark drugs: diphenhydramine, trihexiphenidyl, benztropine
- What are the other 1st generation antipsychotic drugs?
- Depot form: fluphenazine decanoate
Low potency: Chlorpromazine, Thioridazine
Intermed: Trifluoperazine, Perphenazine, Thiothixene
High Pot: Haloperidol, Fluphenazine
- What are the uses of 1st generation antipsychotics?
- 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
- What is Clozapine?
- 2nd generation antipsychotic/Atypical antipsych.
- What is different about 2nd generation anti-psychotics?
- *relatively little EPS, and more effective at negative sx
*antagonize 5-HT2R, D2, D2,(and/or)D4
- What are the properties of Clozapine?
- more anticholinergic than most antipsy, low affinity for D2R
- What are the SE of Clozapine?
- MAJOR: 1-2% Agranulocytosis, fatal if unchecked
minor:can cause weight gain and induce/exacerbate DM2, HTN, sleep apnea
- What are the other 2nd generation Antipsy, that are diff. from Clozapine?
- olanzapine (zyprexa)
risperidone (Risperidal)
quetiapine (Seroquel)
sertindole (ziprasidone)