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28 Cards in this Set
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Chlorpromazine
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low potency phenothiazine: Schizophrenia, N/V, pre-anesthetic sedation, manic psychotic episodes, EtOH hallucinations, Drugs induced psychosis
absorbed erratically if oral, IM effective in 30 min; metabolized slowly by liver 24h λ SdEfx: anticholinurgic: blurred vision, constip'n, urinary retnt'n GI stasis Alpha blockade: postural hypotension, inhibited ejaxn prolonged QT intervals, Reducsed Seizure Threshold, Extrapyramidal Effects, Tardive Dyskineasia, Neuroleptic Malignant Syndrome Jaundice w/in a month must change rx |
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Neuroleptic Malignant Syndrome
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Life-threatening muscle rigidity catatonia
treated with dantroline |
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Thioridazine
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More anti-ACh, less extrapyramidal sx than Chlorpromazine, more sedation and hypotension, may produce retinal deposits
low potency phenothiazine: Schizophrenia, N/V, pre-anesthetic sedation, manic psychotic episodes, EtOH hallucinations, Drugs induced psychosis absorbed erratically if oral, IM effective in 30 min; metabolized slowly by liver 24h λ SdEfx: anticholinurgic: blurred vision, constip'n, urinary retnt'n GI stasis Alpha blockade: postural hypotension, inhibited ejaxn prolonged QT intervals, Reducsed Seizure Threshold, Tardive Dyskineasia, Neuroleptic Malignant Syndrome Jaundice w/in a month must change rx |
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Fluphenazine
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high potency phenothiazine: Schizophrenia, N/V, pre-anesthetic sedation, manic psychotic episodes, EtOH hallucinations, Drugs induced psychosis
absorbed erratically if oral, IM effective in 30 min; metabolized slowly by liver 24h λ SdEfx: anticholinurgic: blurred vision, constip'n, urinary retnt'n GI stasis Alpha blockade: postural hypotension, inhibited ejaxn prolonged QT intervals, Reducsed Seizure Threshold, Tardive Dyskineasia, Neuroleptic Malignant Syndrome Jaundice w/in a month must change rx Low anti-ACh, more extrapyramidal sx than Chlorpromazine, less sedat'n and hypotens'n |
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Trifluoperazine
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high potency phenothiazine: Schizophrenia, N/V, pre-anesthetic sedation, manic psychotic episodes, EtOH hallucinations, Drugs induced psychosis
absorbed erratically if oral, IM effective in 30 min; metabolized slowly by liver 24h λ SdEfx: anticholinurgic: blurred vision, constip'n, urinary retnt'n GI stasis Alpha blockade: postural hypotension, inhibited ejaxn prolonged QT intervals, Reducsed Seizure Threshold, Tardive Dyskineasia, Neuroleptic Malignant Syndrome Jaundice w/in a month must change rx Low anti-ACh, more extrapyramidal sx than Chlorpromazine, less sedat'n and hypotens'n |
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Haloperidol
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Haldol: selective blockade of D2: sedation, indifference
most likely of all antipsychotics to cause extrapyramidal sx much like phenothiazines well abnorbed orally, often injected in acute psychotic situations, Rx abuse slow metabolism, elimination takes >1wk |
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Clozapine
(Clozaril) |
Atypical antipsychotic, used for negative Sx of schizophrenia, delusions in pts with parkinson's
Binds D4 and 5HT2A = mesocortical specificity (↓ EPS) Oral, large variation in bioavailability, liver metzm Agranulocytosis most serious potential side effect Mn: must monitor Clozapine Clozely (routine blood draws) Among top 3 seizure causing antipsychotics (with olanzapine & chlorpromazine) SE's: HαM blockade --> sedation, decreased seizure threshold, hypotension, fever, salivation, dizziness, weight gain |
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Gabapentin
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Neurontin: GABA analogue
anticonvulsant & neurological pain drowsiness and weight gain (ataxia, blurred vision, hypertension, back pain) not recommended in pregnancy |
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Neurontin
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Gabapentin: GABA analogue
anticonvulsant & neurological pain drowsiness and weight gain (ataxia, blurred vision, hypertension, back pain) not recommended in pregnancy |
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Topiramate
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For Bipolar
usually causes weight loss (used as an anticonvulsant, alcoholism tx, offset weight loss from SSRI's, reduce binge eating and for prevention of migraine and essential tremor) |
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Olanzapine
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Atypical Antipsychotic: effective for negative sx of schizo, useful for bipolar
Blocks D4 and 5HT2A: Tx negative sx Anticholinergic: no Extrapyramidal Sx Some affinity for D2, will improve both + and - sx, Oral, long halflife, Liver Most likely antipsychotic to cause weight gain. Hyperglycemia and T2DM risk Does not cause agranulocytosis |
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Most likely antipsychotic to cause weight gain.
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Olanzapine, Atypical Antipsychotic: effective for negative sx of schizo, useful for bipolar
Blocks D4 and 5HT2A: Tx negative sx Anticholinergic: no Extrapyramidal Sx Some affinity for D2, will improve both + and - sx, Oral, long halflife, Liver Most likely antipsychotic to cause weight gain. Hyperglycemia and T2DM risk Does not cause agranulocytosis |
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First line drug for treating psychosis
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Risperidone: postive and negative sx
oral, protein bound, active metabolite, ideosyncratic halflife 3-24 hours Inhibits D2 and esp 5HT2A, enhances DA transmission in basal ganglia (extremely low EPS) alphablockade: postural hypotension lengthens QT interval Other Side Effects May increase mortality w/ Alzheimers |
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Risperidone
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atyical antipsychotic: First line drug for treating psychosis; postive and negative sx
oral, protein bound, active metabolite, ideosyncratic halflife 3-24 hours Inhibits D2 and esp 5HT2A, enhances DA transmission in basal ganglia (extremely low EPS) alphablockade: postural hypotension lengthens QT interval Other Side Effects May increase mortality w/ Alzheimers |
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Ziprasidone
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Atypical antipsychotic: used in mania, tourettes
Inhibits D2 and 5HT2A some antidepressant activity, oral or IM, CYP3A4 prolongs QT interval, seizures possible, sedation, hyperprolactinemia |
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Quetiapine
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very similar to clozapine
no agranulocytosis, no prolactin elevation does cause wegith gain, drowsiness, xeorstomia |
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Pimozide
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similar to haloperidol
used for Tourette’s syndrome causes extrapyramidal symptoms prolongs QT interval |
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Aripiprazole
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First drug of "DA system stabalizers"
partial agonist at D2 and 5HT1A, antagonist at 5HT2A oral, CYP3A4, 2D6 Does ont affect prolactin, does not lengthen QT, does not cause weight gain alpha1 and histamine blockade orthostatic hyptotension, blood glucose elevation, siezures, sedation, decrreased esophageal motility Low Extrapyramidal effects |
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Dopamine Hypothesis of Psychosis
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Too much dopamine in mesolimbic pathway produces positive sx
Classical Antipsychotics: D2 Blockade --> decreased negative Sx not enough dopamine in mesocortical pathway produces negative sx Atypical Antipsychotics block 5HT2A, reduce negative Sx (? by restoring DA:5HT ratio?) |
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Low Potency Phenothiazines
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Chlorpromazine, Thioridazine "Classical Antipsychotics"
D2 blockade alpha adrenergic blockade Histamine blockade Anticholinurgic activity |
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High Potency Phenothiazides
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Fluphenazine
D2 blockade alpha adrenergic blockade Histamine blockade Less Anticholinergic Activity than LPP's |
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D2 Blockade
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reduces + schizo sx
neuroleptic sedation antiemetic Side effects: unpleasant, sleepiniess, restlessnes, ANS |
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EPS
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Extrapyramidal Sx: mbalance between DA and ACh in nigrostriatal system
More D2 blockade, Less Muscarinic Blockade: More Severe Haldol >> Pimozode, Fluphenazine 4h: dystonia (muscle spasms, rigidity, oculogyric crisis) 4d: akinesia (parkinsonianism) 4wk: akathisia (restlessness, rocking) 4mo: tardive dyskinesia Tx: anticholinergic Benzotropine (Cogentin) |
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Dopamine Hypothesis of Psychosis
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Too much dopamine in mesolimbic pathway produces positive sx
not enough dopamine in mesocortical pathway produces negative sx |
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Low Potency Phenothiazines
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Chlorpromazine, Thioridazine "Classical Antipsychotics"
D2 blockade alpha adrenergic blockade Histamine blockade Anticholinurgic activity |
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High Potency Phenothiazides
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Fluphenazine
D2 blockade alpha adrenergic blockade Histamine blockade Less Anticholinergic Activity than LPP's |
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D2 Blockade
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reduces + schizo sx
neuroleptic sedation antiemetic Side effects: unpleasant, sleepiniess, restlessnes, ANS |
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extrapyramidal sx
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in nigrostriatal system: akathisia (rocking), dystonia (sustained abnormal postures), parkinsonian sx;
tx with anticholinergic drugs Rx's with anticholinergic effects will have less extrapyramidal sx thiodazine will have few EPS fluphenazine and trifluoperazine will have more EPS |