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Chapter 180: Antipsychotics

Michael Levine; Frank LoVecchio

ANTIPSYCHOTICS

INTRODUCTION

The first-generation (typical) antipsychotics, introduced in the 1950s, were effective against the positive features of psychosis (e.g., delusions, hallucinations, disorganized thought) but provided no treatment for the negative features (e.g., avolition, alogia, social withdrawal). In addition, numerous adverse side effects associated with these agents led to poor patient compliance. The second-generation (atypical) antipsychotics were introduced in the 1990s, and the third generation followed in the 2000s. These second- and third-generation drugs work on both the positive and negative symptoms and, when taken at therapeutic doses, are associated with fewer extrapyramidal effects than the first-generation antipsychotics (Table 180-1).

TABLE 180-1Common Antipsychotics
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TABLE 180-1 Common Antipsychotics
Generic Name Brand Name in the United States Typical Adult Maintenance Dose (milligrams) Maximum Adult Daily Dose for Psychosis (milligrams) Elimination Half-Life (oral dosing)
First-generation or typical antipsychotics
Chlorpromazine Thorazine®* 50–100 orally 3 or 4 times day 1000

23–37 h (parent drug)

10–40 h (active metabolite)
Fluphenazine Prolixin®* 1–2.5 orally 3 or 4 times a day 40 15 h
Haloperidol Haldol®* 0.5–2 orally 2 to 3 times a day 100 21–24 h
Loxapine Loxitane® 15–25 orally 2 to 4 times a day 250 3–4 h
Perphenazine Trilafon®* 8–16 orally 2 to 4 times a day 64 9–12 h
Pimozide Orap® 2–10 orally once or twice a day 10 55 h
Prochlorperazine# Compazine®* 5–10 orally 3 or 4 times a day 150 3–5 h
Promethazine# Phenergan® 6.25–25 orally 3 to 4 times a day 100 7–14 h
Thioridazine Mellaril®* 50–100 orally 3 to 4 times a day 800 24 h
Thiothixene Navane®* 2–5 orally 2 to 3 times a day 60 34 h
Trifluoperazine Stelazine®* 2–5 orally twice a day 40 18 h
Second-generation or atypical antipsychotics
Amisulpride† Solian® 200 orally twice a day 1200 12 h
Asenapine Saphris® 5–10 SL twice a day 20 24 h
Brexpiprazole Rexulti® 2–4 orally once a day 4 91 h
Cariprazine Vraylar® 1.5–6 orally once a day 6

2–4 d (parent drug)

1–3 wk (active metabolite)
Clozapine Clozaril® 150–300 orally twice a day 900

8 h (single dose)

12 h (steady state)
Iloperidone Fanapt® 6–12 orally twice a day 24

18 h (extensive metabolizers)

33 h (poor metabolizers)
Lurasidone Latuda® 4–160 orally once a day 160 18 h
Olanzapine Zyprexa® 10 orally once a day 20 21–54 h
Paliperidone Invega® 6 orally once a day in the morning 12 23 h
Pimavanserin Nuplazid® 34 orally once a day 34

57 h (parent drug)

200 h (active metabolite)
Quetiapine Seroquel® 50–100 orally 2 or 3 times a day 800 6–7 h
Risperidone Resperidal® 1–2 orally once or twice a day 16 20 h
Sulpiride† Dogmatil® 200–400 orally twice a day 1200 11 h
Ziprasidone Geodone® 20 orally twice a day 160 7 h
Third-generation antipsychotics
Aripiprazole Abilify® 10–15 orally once a day 30

75 h (extensive metabolizers)

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