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Typical Antipsychotics - low potency
Low potency - low affinity for DA receptors -> higher dose is required
- Chlorpromazine (Thorazine)
- Thioridazine (Mellaril)
lower incidence of EPS and NMS, higher incidence of anticholinergic and anti histaminic SEs, more likely to cause seizures
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Typical Antipsychotics - high potency
High potency for DA receptors -> lower dose
- Haloperidol (Haldol)
- Fluphenazine (Prolixin)
- Trifluoperazine (Trilafon)
- Perphenazine (orap)
higher incidence of EPS and NMS, lower incidence of anticholinergic and anti histaminic SEs
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Typical Antipsychotics - usage
treat positive psych sxs - hallucinations, delusions
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Typical Antipsychotics - SEs
AntiDA (EPS), AntiHAM, Weight gain, increased liver enzymes, jaundice, ophthalmologic probs, dermatologic problems, seizures, tardive dyskinesia
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Typical Antipsychotics - AntiDA
- EPS:
- 1. Parkinsonism: mask-like face, cogwheel rigidity, pill-rolling tremor
- 2. akathisia: subjective anxiety/restlessness, objective fidgetiness
- 3. Dystonia: sustained contraction of muscles of neck, tongue, eyes (PAIN)
- 4. Hyperprolactinemia -> decreased libido, galactorrhea, gynecomastia, impotence, amenorrhea, osteoporosis
TX EPS - STOP meds, give antiparkinsonisn/anticholengeric/antihistamines ie: amantadine (Symmetrel), Benadryl, benztropine (Cogentin)
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Typical Antipsychotics - anti-HAM
- 1. AntiHistaminic - sedation
- 2. AntiAlpha Adrenergic - orthostatic hypotn, cardiac abnormalities, sexual dysfunction
- 3. AntiMuscarinic - anticholengeric: dry mouth, tachycardia, urinary retention, blurry vision, constipation
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Typical Antipsychotics - opthalmologic/dermatologic problems
Mellaril -> irreversible retinal pigmentation
Chlorpromazine -> deposits in lens/cornea, blue/gray skin discoloration
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Typical Antipsychotics - Tardive Dyskinesia
choreoathetoid movements of mouth and tongue that may occur in pts on neuroleptics for >6 mts
esp in older women
50% remit, 50% PERMANENT
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Typical Antipsychotics - Neuroleptic Malignant Syndrome sxs
MED EMERGENCY - 20% mortality rate, preceded by catatonic state
- SXS: FALTER
- Fever, Autonomic instability (tachy, labile htn, diaphoresis), Leukocytosis, Tremor, Elevated creatine phosphokinase, Rigidity (lead pipe)
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Typical Antipsychotics - Neuroleptic Malignant Syndrome tx
stop meds, supportive care (cooling/hydration)
sodium dantrolene, bromocriptine, amantadine
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Atypical Antipsychotics - Action
block DA & 5HT receptors, associated with fewer SEs (rarely EPS, tradive, NMS)
More important for treating negative sxs -> first line for sz
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Atypical Antipsychotics - Examples
- Clozapine (Clozaril)
- Risperidone (risperdal)
- Quetiapine (seroquel)
- Olanzapine (Zyprexa) - also for mania
- Ziprasidone (Geodon) - also for mania
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CLOZAPINE
1% -> agranulocytosis and 2/5% -> seizures
need weekly blood draws to check WBCs
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Olanzapine
hyperlipidemia, glucose intolerance, weight gain, liver toxicity
need to monitor LFTs
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Quetiapine
less weight gain
cataracts in dogs -> slit lamp studies
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Mood stabilizers
"anti-manic"= used to treat acute mania and prevent relapses (ie Lithium, carbamazepine, valproic acid)
also used for: dual therapy in refractory depression, with antipsychotics in SZ, tx alcoholism, treat aggression and impulsivity.
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Lithuim - use/mech
Tx acute mania and prophylaxis for manic/depressive episodes of bipolar
mech - alter neuronal Na transport
secreted by kidneys and takes action in 3-5 days
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Lithium - therapeutic index
- narrow therapeutic range = effective 0.7-1.2 (can still be toxic)
- toxic > 0.5 (causes altered mental status, coarse tremors, convulsions, death)
- Lethal > 2
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lithium - SE
tremor, sedation, ataxia, thirst, metallic taste, polyuria, edema, weight gain, GI problems, benign leukocytosis, thyroid enlargement, HYPOTHYROID, NEPHROGENIC DI
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Carbamazepine (Tegretol) - use/action
tx mixed episodes and rapid cycling bipolar, manage trigeminal neuralgia
Blocks Na channels and stops APs
onset of action in 5-7 days
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Carbamazepine (Tegretol) - SEs
skin rash, drowsiness, ataxia, slurred speech, leukopenia, hyponatremia, aplastic anemia, agranulocytosis,
Elevates LFTs -> need pretx blood LFTs and CBC
NOT in preg -> neural tube defects
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Valproic Acid (Depakene) - use/mech
tx - mixed manic episodes and rapidly cycling bipolar d/o
mech - increase GABA in CNS
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Valproic Acid (Depakene) - SE
sedation, weight gain, alopecia, hemorrhagic pancreatitis, hepatotoxicity, thrombocytopenia
NOT in preg -> neural tube defects
monitor LFTs and CBC
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Anxiolytics/Hypnotics
- (ie benzos, barbs, buspirone)
- Depress CNS -> sedation
- USES = anxiety d/o, muscle spasm, seizures, sleep d/o, alcohol w/d, anesthesia induction
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Benzodiazepines
- 1st line
- safe at high doses (unlike barbs)
- SEs = drowsiness, impair intellectual functioning, decreased motor coordination
- TOXIC = resp depression in OD (esp with Alcohol)
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Chlordiazepoxide (Librium)
- Long Acting (1-3 days)
- alcohol detox, presurgery anxiety
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Diazepam (Valium)
- Long Acting - 1-3 days
- rapid onset, tx anxiety and seizure control
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Alprazolam (Xanax)
- Intermediate acting (10-20 hrs)
- tx panic attack
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Clonazepam (Klonopin)
- Intermediate acting (10-20 hrs)
- tx panic attack, anxiety
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Lorazepam (Ativan)
- Intermediate acting (10-20 hrs)
- tx panic attack, alcohol w/d
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Temazepam (Restoril)
- Intermediate acting (10-20 hrs)
- tx insomnia
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Triazolam (Halcion)
- Rapid onset (3-8 hrs)
- tx insomnia
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Zolpidem (Ambien)/ Zaleplon (Sonata)
- Shrt term tx insomnia
- selectively bind benzo binding site on GABA receptor
- NO anticovulsant/muscle relaxor properties, no w/d, minimal rebound insomnia, little/no tolerance
- NOT bnzo, but acts like one
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Buspirone (BuSpar)
- use = alternative to BDZ/venlafaxine for treating GAD
- Slower onset of action than BZD (1-2 wks)
- Mech = 5HT partial agonist
- does NOT increase CNS depression of alcohol
- low potential for abuse/addiction
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Propranolol
Tx= autonomic effects of panic attacks or performance anxiety (palpitations, tachy, sweating), akathisia
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