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Pharmacology > Antipsychotics > Flashcards

Antipsychotics Flashcards

1
Q

Paranoid schizophrenia

A

one or more delusions or frequent auditory hallucinations, someone is trying to “get them” hurt them, steal from them

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2
Q

Disorganized schizophrenia

A

speech and behavior oriented

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3
Q

Catatonic schizophrenia

A

stupor, posturing, mutism, fetal position

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4
Q

Residual

A

absence of prominent sx but evidence of illness and functional impairment

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5
Q

Epidemiology of schizophrenia

A

prevalence remarkably similar among most cultures, most common in late adolescence or early adulthood, prevalence in males and females, lifetime prevalence of .6-1.9%

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6
Q

Etiology of schizophrenia

A

abnormalities in brain structure an dysfunction, changes not consistent among all individuals, multifactorial causes, neurodevelopmental model, utero disturbance, schizophrenic lesions, genetics

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7
Q

Positive symptoms

A

hallucinations, delusions, false beliefs, disorganized speech, cannot follow train of thought, psychomotor agitation, bizarre behavior

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8
Q

Negative symptoms

A

alogia-poverty of speech, brief responses, lack of thought; flattened affect, avolition- lack in self initiated goal-directed activity, socially isolated; anhedonia- lack of interest and motivation in other people/activities, attentional impairment- psychomotor slowing

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9
Q

Clinical course

A

onset (acute/gradual), acute stabilization, stabilization, maintenance

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10
Q

approaches to therapy

A

individual- supportive/ counseling, personal therapy, social skills therapies, rehab; group- interactive/ social, cognitive behavioral- cog behavior therapy, compliance therapy

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11
Q

MOA of treating schizo

A

blockade of DA receptors in mesolimbic area, D2 blockade- affinity for this receptor accounts for antipsychotic activity, D1 blockade- partially responsible for antipsychotic activity, responsible for EPS sx, 5HT blockade- improve neg sx and motor ADRs

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12
Q

Receptor activity

A

D1-D5: relief of psychosis, EPS; 5HT2: helps suppress DA activity, protect from EPS, wt gain; a1: orhto hypo, dizziness, M1: ACh ADRs, may protect against EPS, drowsiness, dry mouth, blurred vision, constipation, H1: wt gain, drowsiness

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13
Q

Popular atypical antipsychotics

A

Quetiapine (Seroquel), Risperidone (Risperdal), ziprasidone (Geodon), Olanzapine (Zyprexa), Aripiprazole (Abilify)

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14
Q

Nausea and vomiting typical antipsychotics

A

Prochlorperazine (Compazine), Chlopromazine (Thorazine), Droperidol (Inapsine)

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15
Q

Antipsychotics typical

A

Haloperidol (Haldol), Thioridazine (Mellaril), Thiothixene (Navane), Loxapine (Loxitane), Perphenazine (Trilafon), Fluphenazine (Prolixin), Trifluoperazine (Stelazine)

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16
Q

Typical antipsychotic pearls

A

all have equal efficacy, MOA- non-selective blockade of D2 receptors, effective at treating positive sx, major concern is EPS

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17
Q

Haloperidol (Haldol) dosing forms

A

Available IM or PO, IM-fast acting, also available as Depot shot, given once monthly, IVP is linked to increased risk of arrythmias

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18
Q

Haloperidol (Haldol) Pearls

A

drug of choice for ICU psychosis, used occasionally for CI for EtOH withdrawals, watch for QTc prolongation, higher potensity for EPS and anticholinergic ADRs, many DI

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19
Q

Chlorpromazine (Thorazine)

A

available PO or IM (IM used in peds for acute mania), off label- retractable hiccups (DOC), migraines, also used for N/V

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20
Q

Droperidol (Inapsine)

A

N/V migraines, major concern being proarrhythmic

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21
Q

ADRs or antipsychotics

A

sedation, ACh- dry mouth, constipation, blurry vision, antiadrenergic- orthstatic hypotension, wt gain, prolongation of QT interval, inc prolactin secretion (menstrual changes)

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22
Q

EPS

A

related to blockade of D1 receptor in substantia nigra, reversible if discovered early, associated w/ all typicals and some atypicals, includes- dystonia, pseudoparkinsonism, akathisia

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23
Q

Prolonged QT

A

typicals increase Qt interval, inc risk of torsades/ ventricular arrythmia, medications- typical antipsychotics, antibiotics, antifungals, low mag/K, CHF, renal/ hepatic d, CVA

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24
Q

Treatment of Acute dystonia

A

diphenhydramine (Benadryl), benztropine (Cogentin), must be given right away for quick reversal, usually IV, follow w/ PO agent x 1-2 wks to prevent recurrence, will worsen tardive dyskinsias

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25
Q

EPS- pseudoparkinsonism

A

20-40%, happens within several months, because of DA blockade causing relative imbalance of DA and ACh, increased risk w/ use of typicals and high risperidone high dose

26
Q

Treatment ppseuodparkinsonism

A

decrease dose, change med, anticholinergics, amantadine to block DA

27
Q

Tardive dyskinesia

A

occurs in 10-20% of pts, not EPS, associated w/ chronic use, often irreversible, high risk w/ typicals, elderly and women

28
Q

Tardive dyskinesia presentation

A

largely orofacial, involuntary movements of face, neck, back, trunk and extremities, blinking, lip smacking, starts as tongue protrusion w/ appearance of lip smacking and difficulty speaking, chewing and swollowing

29
Q

Tardive dyskinesia treatment

A

can be controlled if pt concentrates, limited to duration and dose of drug, often occurs when drug is decreased, no effective drug therapy, inc dose back to where it was, ACh make worse

30
Q

Neuroleptic malignant syndrome

A

due to blockade of DA receptors, typicals have highest risk, Medical Emergency, 5-20% fatality,, mean age 40, higher risk in pts w/ mood disorders, lithium use, 1/3 cases develop subsequent NMS if re-chanllenged

31
Q

NMS diagnosis

A

tx w/ AP w/in 7 days of onset, hyperthermia >100.4, muscle rigidity, 5 of following- changed in mental status, tachy myoglobinuria, inc WBC, tremor, tachypnea, incontinence, CPK inc, metabolic acidosis, labile BP

32
Q

NMS TX

A

dec risk factors, early recognition, stop offending agent, supportive care, Dantrolene (Dantrium), amantadine, bromocriptine, lorazepam, may have to sedate, intubate and paralyze

33
Q

Atypical antipsychotics

A

Clozapine, risperidone, olanzapine, quetiapine, ziprasidone, aripiprazole, paloperidone, asenapine, iloperidone, lurasidone

34
Q

Atypical antipsychiotics MOA

A

D2 and 5HT antagonists, 5HT is an inhibitory neurotransmitter, mesolimbic selectvely for D2 blockage, 5HT has minimal effects on prolactin, dec EPS, beneficial on neg sx

35
Q

Clozapine (Clozaril)

A

first atypical, no EPS, TD or effect on prolactin, slow dose titration due to dec BP, strict monitoring for WBS

36
Q

Clozapine (Clozaril) use

A

considered to be most efficacious, only for pts who have failed other agents, most potent for tx of pos and neg sx, good for pt w/ hx of suicide, substance abuse, last line, avoid in combo w/ benzos

37
Q

Clozapine agranulocytosis

A

occurs in 3%, requires monitoring once weekly for 6 months, biweekly for next 6 months and once a month after, do not initiate if WBC 600 mg/d

38
Q

Risperidone (Risperdal)

A

EPS dose related (>6mg/d) low dose good for geriatric agitation, not as effective for treating neg sx

39
Q

Clozapine ADRs

A

hypersalivation, wt gain, dec bp, sig sedation, seizures if >600 mg/d

40
Q

Risperidone dose and ADRs

A

.5 mg PO BID up to 3 mg PO BID, elevated LFTs, hyperprolactinemia, orthostasis, sexual dysfunction, sedation, wt gain,

41
Q

Risperdal CONsta

A

IM injection q 2 weeks, must be overlapped w/ oral therapy upon initiation

42
Q

Olanzapine (Zyprexa)

A

similar to Clozaril, no EPS, low TD, also used for acute agitation, bipolar maintenance, acute mania

43
Q

Olanzapine ADRs and dose

A

20-60 mg PO QHS, significant sedation, wt gain, diabetes risk, low BP, no agranulocytosis, IM injection- short term treatment of acute agitation, at least as effective as Haldol, w/ quicker onset and lower incidence of dystonia and EPS

44
Q

Quetiapine (Seroquel)

A

Low risk EPS, low TD, can see addiction

45
Q

Quetiapine ADRs and dose

A

Sedation, mild hypo, wt gain, HA, cataracts in animals, 50-300 mg PO qHS, low doses used for anxiety, insomnia, depression

46
Q

Ziprasidone (Geodon)

A

Oral IM, 20-40 mg PO BID, IM favored by many for acute mania, acute agitation IM q 2 hrs prn, ADRs-prolonged QT, mild sedatioin, minimal wt gain, EPS- low, TD low

47
Q

Aripiprazole (Abilify) MOA

A

da modulator, only works when needs to, partially blocks D2 receptor when DA is inc, activate D2 receptor when DA is dec, 5HT2 antagonists improves efficacy for neg sx; often used in peds

48
Q

Aropiprazole Adrs, dose

A

little wt gain, inc prolactin levels, possible diabetes, anxiety insomnia, HA, nausea, vomiting, low incidence EPS, no TD, no QT, least low BP; 5-15 mg PO Daily

49
Q

Paliperidone (Invega)

A

active metabolite of risperidone, once daily, PO, less risk EPS and prolactin inc, niche- pts w/ liver disease, ADR- sedation, low BP

50
Q

Iloperidone (Fanapt)

A

schizo only, Qt prolongation, avoid in arrhythmias

51
Q

Luprasidone (Latuda)

A

schizo only, no Qt prolongation, $$$, not 1st line

52
Q

Asenapine (Saphris)

A

D2 antagonist, 5 HT2A antagonist, SL only

53
Q

Meatabolic syndrome

A

consider when starting therapy, do baseline screenings and regular monitoring, get good fam hx

54
Q

Transitioning

A

taper over 1-2 weeks to prevent w/ drawal, Risperidone- overlap oral and IM by 3 weeks, haloperidol- overlap oral and IM by 1 month

55
Q

Augmentation therapy for schizo

A

Benzos- lorazepam for agitaton and aggression, BB (aggression), mood stabilizers- improves aggitation, lithium, anticonvulsants (carbamazepine, valproate, gabapentin, topiramate), SSRI w/ 1st generation OCD

56
Q

General principals for APs

A

therapeutic trial for 6 weeks, (Clozapine needs 12), duration of tx- initial diagnosis (1-2 years) then reassess if relapse treat 5yrs-life, polypharm- consider clozapine before combo, not recommended unless failed others

57
Q

Compliance

A

1 reason for relapse, cog fun may be lower, lack of understanding, stigma, cost is little concern

58
Q

Summary of APs

A

considered 1st line, effectively treats all psychotic sx, enhanced tolerability, improved cog effects, better outcome in long-term, reduced rate of relapse and hospitalization

59
Q

Summary of TPs

A

not usually 1st line, inc risk of EPS/ TD, not as effective in treating neg sx, not likely to improve cog func, no more effective in treating pos sx

60
Q

Summary of compiance and duration of Tx

A

chronic disorder requiring life-long tx, tx after 1st episode continued for at least one year, nonadherence to meds is a complicated and signif issue, up to 70% of pts relapse w/in 1st 12 months if not taking maintenance meds

Pharmacology (61 decks)

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