Psychiatric Drugs
Training Lecture #1
Grace E. Jackson, MD
(last revised: 7/18/10)

Outline of Lecture
Major Classes of Psychiatric Drugs
America’s Drug Problem
III. Killing the Mentally Ill
IV. Psychiatric Drug Toxicity

"I"
I.    Types of Psychiatric Drugs

5 Major Classes of Psych Drugs
Antidepressants
Antipsychotics
Mood Stabilizers
Sedative Hypnotics / Anxiolytics
Stimulants

"II"
II.   America’s Drug Problem

Question #1

Question #1
Most Common Disease (point prevalence)
asthma
Alzheimer’s
diabetes
arthritis

Question #1
Most Common Disease
d) arthritis                                   þ

Somatic vs. Psychiatric
Lifetime Prevalence - USA
depression            16%
specific phobia       9%
ADHD                     5%
PTSD                    3.5%
bipolar                    3%
panic                   3%
OCD                1%
schizophrenia       1%
cancer           30-50%
arthritis     ~ 20%
asthma        12%
diabetes            9%
MI/angina          7%
stroke                3%
epilepsy             3%
dementia       2%

Question #2

Question #2
Top Selling Drug Class in the U.S.A.
cancer medicines
insulin
asthma inhalers
antipsychotics

Question #2
Top Selling Drug Class in the U.S.A.
d) antipsychotics     þ

U.S. Drug Sales 2009
[IMS Health]
Total Drug Sales 300.3 billion
APs #1 14.6 billion
   lipid #2 14.3 billion
   PPI #3 13.6 billion
   ADs #4   9.9 billion
   insulin #9   6.3 billion
   stimulants #11   5.8 billion
   seizure  #13   5.3 billion
APs = antipsychotics
ADs = antidepressants

# of U.S. Prescriptions - 2009
[IMS Health]
Total Prescriptions          3.9 billion
lipid #1 210.5 million
   codeine #2 200.2 million
  ADs #3 168.7 million
   ACEi #4 162.8 million
   AEDs #7 104.5 million
   benzos #11        87.9 million
   arthritis #13       77.9 million

U.S. = 4.5 % of world population
90% of stimulant sales
63% of AP sales
51% of AD sales
41% of AED sales

U.S.A.:  Psychiatric Drugs 2009
[Source: Express Scripts 2009 Drug Trend Report]
antidepressants 9.9%         31,000,000
anticonvulsants 4.0%         12,300,000
stimulants 2.2% 6,754,000
*antipsychotics 1.8% 5,526,000
*part of Express Scripts’ “mental/neurological” class:
 includes lithium, dementia drugs, sub. abuse

Question #3

Question #3
Leading Cause of Death in the U.S.A.
heart disease
HIV/AIDS
stroke
cancer

"1"
  1) cardiac disease
2) cancer
3) stroke
           4) chronic lower respiratory
5) accidents (unintentional injuries)
6)        Alzheimer’s disease
7)        diabetes mellitus
8)        influenza and pneumonia
9)        kidney disease
         10)        septicemia

Question #3
Leading Cause of Death in the U.S.A.
heart disease                          þ
but . . . this is only part of the story…

Institute of Medicine (1999)
44,000 to 98,000 dead from errors

             JAMA (2000)
N ADVERSE EFFECTS N
106,000 inpatient deaths
199,000 outpatient deaths
----------------------------------
305,000 deaths from Rx

Reality Check:  # of deaths (2006)
 1. cardiac disease 629,191
 2. cancer 560.102
 3. adverse drug reactions 305,000
 4. stroke 137,265
 5. accidents 124,614
 6. medical errors   98,000
 7. Alzheimer’s disease   73,177
 8. diabetes mellitus   72,507
 9. flu & pneumonia   56,247
10. septicemia   44,791

"III"
III.       What’s Killing the Mentally Ill


Morbidity and Mortality in Public MH Patients
 [Sources:  2006 - Colton & Manderscheid & NASMHPD 13th Technical Report]
     annual death rates
     SMI        1 - 3.5%
     non-SMI   0.5 - 0.8%

Slide 26

Causes of death 1997-2000…
non-SMI % of deaths
cardiac     21-30%
cancer     18-22%
stroke         5%
chronic respiratory    2-4%
diabetes         2%
suicide      0.3-1%
dementia
SMI % of deaths
cardiac               17-31%
cancer       5-10%
suicide        5-9%
chronic respiratory    4-5%
stroke        2-5%
diabetes        1-3%
Missing from the discussion:

Slide 28

Swedish SMR Trends

Public MH patients = 5.9 million per year
Compared to non-SMI, those with SMI:
 die in greater numbers each year
 die earlier than expected
 experience more illnesses than non-SMI

High Rate of Health Disorders
 SMI Compared to Non-SMI Groups 
Maine Medicaid – 2004

Burden of Medical Illness:
Maine Medicaid 2004

"IV"
IV. Psychiatric Drug Toxicity

Psychiatric Drugs á the Odds of Disease
AD   AP
á 1.4-2x      á 2-3x
       unclear     á 1.2-7x
  á 1.6x       á 1.9x
  á 2-15x         unclear
á 1.3-1.6x   á 1.4-6x
á 2-5x       á 2-14x
Risk of heart disease
Risk of diabetes
Risk of pneumonia
Risk of suicidality
Risk of stroke
Risk of dementia

Dementia defined:
From Latin de mens / de mentis
out of  (away from) one’s mind

Features of Dementia
 Memory impairment
 Aphasia (impaired language)
 Apraxia (impaired ability to carry out motor activities)
 Agnosia (failure to recognize objects)
 Executive functioning deficits
planning, organizing, sequencing, abstracting

"≥ 65 with dementia"
≥ 65 with dementia
             2.3% in 2000       è       4.5% in 2040
                7.6 million           18.3  million

Slide 38

≥ 65 years of age
12% to 18% to 21%

Drug-Induced Dementia
DSM-IV, Text Revision (2000)
Substance-Induced Persisting Dementia
“Features are those associated with
dementias generally…can occur in
association with…alcohol, sedatives,
hypnotics and anxiolytics, or other or
unknown substances…”

A perfect crime…

Antipsychotic Timeline
*timeline  = year that the drug was invented or first used
1st generation drugs 1950 to 1960s
Thorazine, Haldol, *Clozaril
2nd generation drugs 1970 to 1990s
Risperdal, Zyprexa, Seroquel, Geodon
3rd generation drugs 2000 to 2010
Abilify
*Invented in 1958, clozapine was introduced in Europe in the early
1960s.  It did not gain FDA approval in the U.S.A. until 1989.  Partly for this
reason, American physicians refer to it as a “second generation” drug.

U.S. Drug Sales – 2009 ($ billions)
9.9

Dept. of Veterans Affairs
Kales et al (2007)
23,436 patients (national database)
≥ 65 years of age
diagnosis of dementia in 2002 or 2003
12-month mortality risk after starting a
psychiatric drug

"12,821 avoided psychiatric drugs"
12,821 avoided psychiatric drugs
18% died within one year
10,615 started psychiatric drugs
23% using newer APs died
25% using old (“conventional”) APs died
   29% using both kinds of APs died

"Other folks started to notice..."
Other folks started to notice the same
trend in different patients…

Black Box Warnings
“not for dementia-related psychosis”

"In England"
In England, some physicians began to
wonder ---
what would happen to dementia patients
if they stopped taking antipsychotic drugs ?

U.K. - DART-AD
Dementia AP Reduction Trial
Enrolled residents of nursing or residential homes in four
areas (2001-2004); followed patients to April 2006
All patients had been diagnosed with possible or
probable Alzheimer’s and all had taken APs for
≥ 3 months (APs = risperidone, thioridazine, haloperidol,
trifluoperazine, or chlorpromazine)
Mean duration of drug use: 25 months

DART-AD
Ballard et al (2009)
 165 patients were randomly assigned to
antipsychotic (83) or placebo (82)
 Assessed patients according to treatment
fidelity (compliance) and outcome…
 Primary outcome: 12-month mortality

Outcomes Based Upon Continuing
Use of Drugs vs. Placebo
APs PBO
% surviving
1 year 75% 79%
2 year 46% 71%
3 year 30% 59%
3 ½ years 26% 53%
APs = antipsychotic drugs
PBO = placebo

Antipsychotic drugs are deadly for
dementia patients…
what about giving them to the non-demented ?

Slide 53

Slide 54

Slide 55

Slide 56

How Do Doctors Diagnose Alzheimer’s Disease?
No way to know for sure while a patient is
still living…
look at symptoms and how they evolve
“biomarkers” are in development
3)  gold standard  = autopsy pathology

Postmortem Pathology

Do Antipsychotic Drugs Cause Alzheimer’s Disease ?
If they do, we should expect to see evidence
of Alzheimer’s pathology (abnormal
anatomy) among patients who have
received antipsychotic drugs…

Postmortem Studies of Humans
1988 Buhl and Bojsen-Moller – 100 patients (consecutive autopsies)
schizophrenia 35% Alz. pathology
non-psych controls 0%   Alz. pathology
 Soustek – 225 pts with chronic schizophrenia (dying in 1975-85)
41% showed Alz. pathology
6x higher rate than general population
1994 Wisniewski – 102 patients with history of schizophrenia
41 died prior to antipsychotic era 46% had tangles
62 died after antipsychotic era 74% had tangles

"2002 Bozikas – 18 schizophrenia..."
2002 Bozikas – 18 schizophrenia patients vs. 14 age-matched controls
patients had 400% á tangle density in cortex (layer II of EC)
patients had á plaque density (throughout the brain)
2005 Ballard et al – studied 40 patients with Lewy body dementia
23 patients avoided antipsychotic drugs
17 patients received antipsychotics
when compared to the other patients, the 17 drug-consumers exhibited:
30%        higher density of cortical plaques
65-367%     higher density of tangles

apoD is marker of neuropathology
      University of Pittsburgh (Desai et al, 2005)
      apoD is key a feature of Alzheimer’s disease
 63% of the beta-amyloid plaques contained apoD

Thomas et al (2001)
autopsy study of brain levels of apoD (ug/mg)
schiz bipolar controls
n=20    n=8   n=19
% using APs                 90%  (18) 75% (6)                        0
DLPFC 0.244 0.233 0.115
caudate 0.132 0.112 0.059
       apoD levels were 2X higher in users of APs
APs = antipsychotic drugs (1st generation and clozapine)

apoD in Animals
mice and rats (multiple investigations) >>
14 to 45 days of OLZ, RISP, or CLZ
all three drugs resulted in higher mRNA and
higher protein levels of apoD in cortical and
subcortical regions of brain
mRNA = messenger RNA (a molecular precursor for protein synthesis)

Other Postmortem Studies
rabbits, rats, monkeys, guinea pigs
1958 – 1975
all showed damage to
cortex, subcortex, and
brainstem following
brief (2 wks) or chronic
exposure (up to 1 yr)

University of Pittsburgh
(2005, 2007, 2008)
Do lab techniques
(specimen processing)
affect the structure of
the brain?
As an aside:
What about drugs?

Experiment
18 adult male macaques (4.5 to 5.3 yrs old)
oral doses of haloperidol or placebo (27 months)
oral doses of olanzapine                   (17 months)
relevant doses of drugs vis-à-vis human therapy
1-1.5 ng/mL for HAL
10-25 ng/mL for OLZ

Changes in Behavior and Brain
4 of 6 monkeys on OLZ  >>    aggressive
2 of 6 monkeys on HAL  >>    aggressive
      atrophy of cortex/cerebellum/brainstem
HAL 9% lower volume of brain
9% decreased brain weight
OLZ 10.5% lower volume of brain
11%  decreased brain weight

f/u Studies of Parietal Lobe

Parietal Lobe Cell Loss
   Reductions in Cell Number After Drug Treatment
      haloperidol    olanzapine
total cells   10.6%     7.4%
neurons     6.3%                    5.5%
oligodendrocytes   13.9%                   11.8%
astrocytes    20.4%                  20.5%

  Biomarkers in Humans

Old and new antipsychotics
all increase Alzheimer’s proteins…
Protein changes in antipsychotic recipients,
relative to drug-free controls:
      source      biomarker      change
Austria 2005    (CSF)   tTG         ↑ 200-400%
Italy      2005    (CSF) tau   ↑ 24%
USA     2002    (blood) apoD    ↑ 58%
CSF = cerebrospinal fluid

Neuroimaging
(brain scans)

Numerous studies…
Without exception, “before and after”
brain scans have revealed shrinkage
(atrophy) of the brain under the influence of
old or new antipsychotic drugs
In some cases, patients have experienced
a 4-9% reduction in volume in < 3 years


What about children ?

NIMH / UCLA study
child onset schizophrenia
Using sophisticated neuroimaging methods (3D “cortical mapping”), longitudinal studies were performed on three groups of adolescents
Goal: check changes in brain anatomy
            over time (baseline, 2.3 years, 4.6 years)

Multiple brain scans > age 13.5 to 18
Study Design:
12 children with Childhood Onset Schizophrenia
(onset of symptoms before age 12)
all had histories of poor response to / intolerance
of at least two typical antipsychotic
10 children with transient psychosis
mood and behavioral problems
12 age & gender matched  “normal” controls
Psychiatric patients received treatment with the following antipsychotic
drugs:  risperidone, olanzapine, or clozapine.

Slide 78


Gray Matter Loss Due to “Disease”
Thompson et al (2001) – multiple scans of teens (aged 13.9 to 18.6)
UCLA & NIMH

Reduced Exposure to APs
no gray matter deficit in temporal lobe

Recap of Lecture
Major Classes of Psychiatric Drugs
America’s Drug Problem
III. Killing the Mentally Ill
IV. Psychiatric Drug Toxicity