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CNS: antipsychotics
antipsychotics
29
Other
Professional
10/12/2010

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Term
PHENOTHIAZINES
Definition
chlorpromazine
fluphenazine
thioridazine
Term
CHLORPROMAZINE (THORAZINE)
Definition
ANTIPSYCHOTIC (PHENOTHIAZINE DERIVATIVE WITH aliphatic side chain)
Machanism by D2 receptor: antagonist of D2, inhibit adenylate cyclase, block PKA, inhibit NMDAR mediated glutamate transmission and LTP
Term
FLUPHENZAINE (PERMITIL)
Definition
ANTIPSYCHOTIC (PHENOTHIAZINE DERIVATIVE WITH piperazine side chains)
Machanism by D2 receptor: antagonist of D2, inhibit adenylate cyclase, block PKA, inhibit NMDAR mediated glutamate transmission and LTP
Term
THIORIDAZINE (MELLARIL)
Definition
ANTIPSYCHOTIC (PHENOTHIAZINE DERIVATIVE WITH piperidine side chains)
Machanism by D2 receptor: antagonist of D2, inhibit adenylate cyclase, block PKA, inhibit NMDAR mediated glutamate transmission and LTP
Term
THIOTHIXENE (NAVANE)
Definition
ANTIPSYCHOTIC (THIOXANTHENE DERIVATIVE)
Machanism by D2 receptor: antagonist of D2, inhibit adenylate cyclase, block PKA, inhibit NMDAR mediated glutamate transmission and LTP
Term
HALOPERIDOL (HALDOL)
Definition
ANTIPSYCHOTIC (BUTYROPHENONES)
Machanism by D2 receptor: antagonist of D2, inhibit adenylate cyclase, block PKA, inhibit NMDAR mediated glutamate transmission and LTP
Term
CLOZAPINE (CLOZARIL)
Definition
NEW GENERATION ANTIPSYCHOTIC
Mechanism by 5-HT receptors - antagonist of 5-Ht, activate PLC, activate PKC, CK1 and PP2B, interfere with glutamate transmission
Term
OLANZAPINE (ZYPREXA)
Definition
NEW GENERATION ANTIPSYCHOTIC'
Mechanism by 5-HT receptors - antagonist of 5-Ht, activate PLC, activate PKC, CK1 and PP2B, interfere with glutamate transmission
Term
RISPERIDONE (RISPERDAL)
Definition
NEW GENERATION ANTIPSYCHOTIC
Mechanism by 5-HT receptors - antagonist of 5-Ht, activate PLC, activate PKC, CK1 and PP2B, interfere with glutamate transmission
Term
PROMETHAZINE (PHENERGANL)
Definition
ANTIPSYCHOTIC
USE: antiemetic
Mechanism: blcosk H1 receptor blocker - antihistamine
- phenothiazine nucleaus
Term
PROCHLORPERAZINE (COMPAZINE)
Definition
ANTIPSYCHOTIC
USE: antiemetic
MechanismL D1 and D2 receptor blocker
-phenothiazine nucleus
Term
ANTIEMETICS (ANTIPSYCHOTICS)
Definition
promethazine
prochlorperazine
Term
psychosis
Definition
variety of metnal disorders
- disturbance of perception, impaired cognitive function
- schizo, dementias, bipolar
Term
schizophrenia
Definition
to split the mind
- affects 1% with early onset and a life long progressive disease
- brain abnormality and NT imbalance
10% with a genetic factor
- can develop due to prenatal viral infections and revealed due to stress and changes in lifestyle
Term
schizophrenia symptoms
Definition
Positive: chronic psychotic condition characteried by marked disorganized thinking with loosely connected thoughts or hallucinations, false ideas or delusions, paranoid delusions, mood disturbances, condusion and suicidal thoughts
Negative: loss of normal function, social withdrawal, reduced speech and though, loss of enegy and inability to experience mental or physical pleasure
Term
Etiolgoy of schizophrenia
Definition
1. biochemical abnormalities with increased dopamine receptors
2. structural abnormalities like enlarged ventricles, atrophy of cortical layers and decreased basal ganglia volume
3. functional abnormalities with reduced blood flow and decrease glucose used in prefrontal cortex
4. genetics
Term
DOPAMINE HYPOTHESIS FOR SCHIZOPHRENIA
Definition
symptoms are due in part to the increase in activity of Dopaminergic neurons
- correlation of therapuetic potency and binding affinity as antagonist for dopamine receptors (D2), drugs enhancing dopamine tranmission can cause schizophrenic symptoms (l-DOpa, chronic amphetamines, apomorphine)
- D2 receptors are increased in brain sof schizophrenics
Term
dorsal mesostriatial path (nigrostriatal)
Definition
controls motor path - dopamine path
Term
ventral mesostriatal (mesolimibic)
Definition
dopamine path - controls behavior and emotion and increased in schizophrenia
Term
mesolimbocortical
Definition
dopamine path - controls behavior and emotiona nd increase din schizophrenia
Term
tuberohypophyseal
Definition
dopamine path inhibiting prolactin secretion
Term
Antipsychotic cholinergic muscarinic block
Definition
chlorpromazine and thioridazine
- dry mouth, urinary retention, memory impairment, blurred vision, constipation and confusion, increased HR
Term
antipsychotic a-adrenoceptor block
Definition
chlorpromazine
- orthostatic hypotension, light headed, reflex tachy, sex dysfunction
Term
antipsychotic pituitary D2 receptor blcok
Definition
all but predominately haloperidol
- increase prolactin and lead to infertility and impotence
Term
H1 histamine receptor block by antipsychotics
Definition
chlorpromazine and clozapine
- sedation and weight gain
Term
Neuroleptic malignant syndrome
Definition
collapse of autonomics
- fever, daiphoresis, cardio instability
- 1-2% of patients and fatal in 10%
treat with BROMOCRIPTINE (D agonist)
Term
Other Antipsychotic side effects
Definition
1. cholinergice muscarine block
2. a-adrenoceptor block
3. H1 histamine block
4. pituitary D2 receptor block
5. nausea and vomiting
6. striatal dopamine receptor block - parkinsonia effects like tremor, bradykinesia, muscle rigidity and dystonias
7. dopamine receptor upregulation and supersensitivity after several month - tardive dyskinesia
8. increased drug metabolis, increase analgesia effect, anesthetics and CNS depressants, block efficacy of L-DOPA, decreased BP, seizure, coma, tachy
Term
typica antipsychotics
Definition
more selective for D2 receptors and high potential for extrapyramidal effects
Term
atypical antipsychotics
Definition
newer drugs
as/more pttent and selective for 5-HT receptors
some more effective at a lower dose and low incidence of extrapyramidal effects
no prolatcin elevation but high risk of agranulocytosis and weight gain
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