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28 Cards in this Set

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Chlorpromazine
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
Neuroleptic Malignant Syndrome
Life-threatening muscle rigidity catatonia

treated with dantroline
Thioridazine
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
Fluphenazine
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
Trifluoperazine
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
Haloperidol
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
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
Gabapentin
Neurontin: GABA analogue

anticonvulsant & neurological pain

drowsiness and weight gain (ataxia, blurred vision, hypertension, back pain)

not recommended in pregnancy
Neurontin
Gabapentin: GABA analogue

anticonvulsant & neurological pain

drowsiness and weight gain (ataxia, blurred vision, hypertension, back pain)

not recommended in pregnancy
Topiramate
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)
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
Most likely antipsychotic to cause weight gain.
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
First line drug for treating psychosis
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
Risperidone
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
Ziprasidone
Atypical antipsychotic: used in mania, tourettes

Inhibits D2 and 5HT2A
some antidepressant activity,

oral or IM, CYP3A4

prolongs QT interval, seizures possible, sedation, hyperprolactinemia
Quetiapine
very similar to clozapine
no agranulocytosis, no prolactin elevation

does cause wegith gain, drowsiness, xeorstomia
Pimozide
similar to haloperidol

used for Tourette’s syndrome

causes extrapyramidal symptoms

prolongs QT interval
Aripiprazole
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
Dopamine Hypothesis of Psychosis
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?)
Low Potency Phenothiazines
Chlorpromazine, Thioridazine "Classical Antipsychotics"

D2 blockade
alpha adrenergic blockade
Histamine blockade
Anticholinurgic activity
High Potency Phenothiazides
Fluphenazine

D2 blockade
alpha adrenergic blockade
Histamine blockade
Less Anticholinergic Activity than LPP's
D2 Blockade
reduces + schizo sx

neuroleptic sedation

antiemetic

Side effects: unpleasant, sleepiniess, restlessnes, ANS
EPS
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)
Dopamine Hypothesis of Psychosis
Too much dopamine in mesolimbic pathway produces positive sx

not enough dopamine in mesocortical pathway produces negative sx
Low Potency Phenothiazines
Chlorpromazine, Thioridazine "Classical Antipsychotics"

D2 blockade
alpha adrenergic blockade
Histamine blockade
Anticholinurgic activity
High Potency Phenothiazides
Fluphenazine

D2 blockade
alpha adrenergic blockade
Histamine blockade
Less Anticholinergic Activity than LPP's
D2 Blockade
reduces + schizo sx

neuroleptic sedation

antiemetic

Side effects: unpleasant, sleepiniess, restlessnes, ANS
extrapyramidal sx
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