ANTIPSYCHOTIC MEDICATIONS
Including Interventions to Manage Their Side Effects
I “Typical” or First Generation Antipsychotics - the “old” ones that primarily block
dopamine from the (D2) receptors and have serious side effects. They only affect
the “positive symptoms” of schizophrenia.
A.
High Potency - 1 to 20 mg-High EPS, low anticholinergic side effects
1. haloperidol (Haldol)
2. fluphenazine (Prolixin)
Both these meds come in PO, IM, and Depo IM (long-acting form)
B.
In-betweens - 4-20 mg
1. trifluoperazine (Stelazine)
2. perphenazine (Trilafon)-comes in slow release form
3. thiothixene Navane
4. loxapin (Loxitane)
5. molindone (Moban)
C.
Low Potency - 50 to 1000 mg
1. chlorpromazine (Thorazine)
2. thioridazine (Mellaril, Novoridazine)
II “Atypical” or Second Generation Antipsychotics: “Newer” medications that block
both dopamine D receptors and serotonin receptors. Have a somewhat better side effect
profile and decrease the “positive” and “negative” symptoms. They are very expensive.
Depending on drug, may be available in PO form ( including sublingual, disintegrating
lozenge, liquid), IM, or depot IM form.
A. clozapine (Clozaril) - 300 mg This medication is prescribed infrequently due to
high incidence of agranulocytosis.
B. risperidone (Risperdal) - 6-12 mg – Available in prolonged-action form (IM) every
2 wk. dosing. Note: On April 16, 2003, Janssen Pharmaceutica Products, Inc.,
published the following warning: Cerebrovascular adverse events (e.g., stroke,
transient ischemic attack), including fatalities, were reported in patients (mean age
85 years; range 73-97) in trials of risperidone in elderly patients with dementiarelated psychosis. In placebo-controlled trials, there was a significantly higher
incidence of cerebrovascular adverse events in patients treated with risperidone
compared to patients treated with placebo.Risperdal has not been shown to be
safe or effective in the treatment of patients with dementia-related psychosis.
C. olanzepine (Zyprexa) - 10 mg ; available in disintegrating tablet
D. quetiapine (Seroquel) - 150-300 mg Lowest side effect profile
E. ziprasidone (Geodon) - 20- 80 mg BID
F. paliperidone (Invega)- 6-12 mg. /day- Available in prolonged-action form (IM)
every 4 week dosing
Atypical Agent sometimes called “Novel” agent
G. aripiprazole (Abilify) –Different activity: blocks dopamine and serotonin in some
brain areas while acting as a partial dopamine agonist in others 10-30 mg/day
Newest Atypical Agents
H. asenapine (Saphris)-5-10 mg BID taken sublingually
I. lurasidone (Latuda)-40-160 mg/day –less likely to cause weight gain
III. Side Effects of Antipsychotics
A. Sedation: common during the first few days of treatment; usually disappears in one
to two weeks. Patients should avoid alcohol and medications such as
antihistamines and sleeping aids.
B. Extrapyramidal Side Effects (EPSEs): Predominate where a drug causes D2
receptor blockade
1. Dystonias/Dystonic reactions-impairment of muscle tone
Usually occur during the first 5 days of treatment, almost never after the first 3
months of treatment. They can occur after each injection of IM medication. Risk
factors include high potency agents, large doses, and parental (IM or IV) route
of administration. Acute effects are readily reversible with intramuscular
injections of antiparkinsonian drugs. Oral antiparkinson agents may need to be
continued for a few weeks to prevent recurrence of the reaction. (see below)
Patients will often times refer to these reactions as drug allergies or seizures.
These however are not allergic or epileptogenic in nature, and do not preclude
continued use of the agent. These reactions are most often spasms of the head,
neck and tongue:
eye-oculogyric crisis-eyes roll back
neck-torticollis
tongue-glossopasm
laryngospasm
other muscles: back-retrocollis/opisthotonus
2. Pseudoparkinsonism or Drug-Induced Parkinsonism: Occurs as a result of
the imbalance of acetylcholine and dopamine in the basal ganglia, similar to
idiopathic Parkinson’s disease, except this effect is reversible. Treatment
consists of reducing the dose, changing to a different agent, or using oral
antiparkinson agents (see below) Symptoms include: decreased movements
(bradykinesia, akinesia), muscle rigidity (cogwheel and lead pipe), resting hand
tremor, drooling, mask-like face, and shuffling gait.
3. Akathisia: can’t remain still, constantly pacing. Patients may describe this effect
as a feeling of inner restlessness. This effect can easily be confused with
anxiety and agitation. Differences between akathisia and anxiety/agitation
improve with increases in antipsychotic doses, and vice-versa; and the patient
can usually control anxiety/agitation for a period of time whereas the patient
cannot typically control akathisia. Treated by changing to a different agent,
reducing the dose if possible, or by the use of an antiparkinson agent or
benzodiazepine.
4. Bradykinesia and Akinesia: Slowed or difficulty with movements and absence
of movement. See above for interventions
5. Tardive Dyskinesia: Abnormal, repetitious movements. These appear a month
or more after starting on the antipsychotic. Symptoms consist of involuntary lip
and tongue movements, and writhing movements (choreoathetoid) of the arms
and legs. Movements disappear during sleep. Risk factors include increased
age, long duration of therapy, use of high potency agents, and large doses.
There is no effective treatment for tardive dyskinesia. Reducing the dose of the
antipsychotic agent and addition of an antiparkinson agent result in worsening
of the symptoms. May improve somewhat with use of cholinergic drugs (e.g.
physostigmine). Early detection is vital to improved outcomes.
C. Anticholinergic Side Effects: tolerance usually develops to these side effects over
1-2 months.
- dry mouth - use of ice chips, sugarless gum, or sugarless sour candy may be
helpful
- blurred vision - reading in well lighted areas and varying the distance of the
material being read may be helpful
- constipation - exercise, drinking plenty of fluids daily, and increasing the
amount of bulk food (bran, salads) intake may relieve this effect. Chronic
problems may require short term use of topical nasal decongestant.
- increase in heart rate
- ejaculation inhibition - most common with thioridazine (Mellaril)
D. Cardiovascular Side Effects:
- postural/orthostatic hypotension (dizziness or fainting) - commonly occurs with
sudden changes in position e.g. laying or sitting to standing position, or in hot
temperatures such as hot showers, saunas, and summer heat. Patients
should be told to change positions slowly, and use good judgment in extreme
heat.
- arrhythmias/palpitations (changes in heart rhythm)—Increase in QT interval
may cause fatal arrhythmia
E. Metabolic Side Effects
- weight gain-This is a real problem esp. with the Atypical agents, likely due to
serotonin blockade. Leads to metabolic syndrome, insulin resistence/glucose
dysregulation and Diabetes Type II. Careful attention to diet, weight and exercise is
part of pt. teaching. Checking blood glucose levels.
F. Endocrine ( from elevated prolactin levels )
-menstrual irregularities
-gynecomastia (breast enlargement)
-galactorrhea
G. Autonomic NS Effects
- Body temperature regulation problems –impaired sweating, hyperthermia. Teach
pt. to take care when engaging in sports and in outside activities in hot weather.
- Neuroleptic Malignant Syndrome (NMS) - ANS instability causes fever, altered
consciousness, fluctuation in other VS, muscle rigidity. Emergency: May be fatal
H. “Miscellaneous” Side Effects:
- skin rash: usually 2 to 8 weeks after initiation of treatment
- photosensitivity: severe sunburn, most common with chlorpromazine
(Thorazine). Patients should be instructed to wear hats, and long sleeve
clothing, sunscreen, until the effects from the sun are determined .
-sexual performance problems and lower libido
I.
Rare side effects
- agranulocytosis-check CBC and differential, especially if on clozapine.
- jaundice-check liver enzymes
- lowered seizure threshold-check history and other medications
- pigmentary retinopathy-eye exams
IV. Antiparkinsonian Agents AKA Anticholingerigc Agents: Treat extrapyramidal side
effects (EPSE) caused by dopamine (D2) blockade. Action: Block ACh receptors; lower
the level of acetylcholine to restore the brain’s normal dopamine:acetylcholine ratio
A. benztropine (Cogentin) 1-2 mg IM form available
B. diphenhydramine (Benadryl) 25-50 mg TID-QID IM form available
C. trihexyphenidyl (Artane) 1-2 mg
D. biperiden (Akineton) 2 mg; 1-4X day
E. amantadine (Symmetrel) 100 mg
A. Side Effects of Antiparkinsonian/anticholinergic Agents:
-Exacerbation of anticholinergic effects (30-50% of patients): dry mouth, constipation,
urinary retention, nausea, blurred vision
-CNS Effects: drowsiness, dizziness, cognitive alterations, confusion, agitation
ABNORMAL INVOLUNTARY MOVEMENT SCALE
(AIMS)
Instructions:
Complete examination procedure before making ratings. Movement ratings: rate
highest severity observed, rate movements that occur upon activation one less
than those observed spontaneously.
CODE
0 = NONE
1 = MINIMAL, MAY BE EXTREME NORMAL
2 = MILD
3 = MODERATE
4 = SEVERE
EXAMINATION PROCEDURE
Either before or after completing the examination procedure observe the patient unobtrusively at rest (e.g., in waiting
room). The chair to be used in this examination should be a hard, firm one without arms.
1. Ask patient whether there is anything in his/her mouth
(i.e., gum, candy, etc.) And if there is, to remove it.
2. Ask patient about the current condition of his/her
6. Ask patient to open mouth. (observe tongue at rest
teeth. Ask patient if he/she wears dentures. Do
within mouth,) do this twice.
teeth/dentures bother patient now?
7. Ask patient to protrude tongue. Observe abnormalities of
tongue movement.) Do this twice.
*8. Ask patient to tap thumb. With each finger, as rapidly
possible for 10-15 seconds; separately with right hand,
Then with left hand. (observe facial and leg movements.)
9. Flex and extend patient’s left and right arms (one at
time). (note any rigidity and rate on dotes.)
10. Ask patient to stand up. (observe in profile. Observe
body areas again. Hips included.)
*11. Ask patient to extend both arms outstretched in front
with palms down. (observe trunk, legs. And mouth.)
*12. Have patient walk a few paces, turn, and walk back to
chair. (observe hands and gait) do this twice.
* Activated movements
3. Ask patient whether he/she notices any movements in
mouth, face. Hands, or feet. If yes, ask to describe and to
what extent they currently bother patient or interfere with
his/her activities.
4. Have patient sit in chair with hands on knees legs
slightly apart and feet flat on floor. (look at entire
body for movements while in this position
5. Ask patient to sit with hands hanging unsupported. If
male, between legs; if female and wearing a dress,
hanging over knees (observe hands and other body
areas.)
FACIAL AND
ORAL
MOVEMENTS
EXTREMITY
MOVEMENTS
1. Muscles of facial expression e.g., movements of forehead, eyebrows, periorbital area, cheeks; include frowning, blinking, smiling, grimacing
2. Lips and perioral area e.g., puckering pouting, smacking
0
1
2
3
4
0
1
2
3
4
3. Jaw e.g., biting clenching, chewing, mouth opening, lateral movement
0
1
2
3
4
4. Tongue rate only increase in movement both in and out of mouth. Not
inability to sustain movement
0
1
2
3
4
5. Upper (arms, wrists hands fingers include choreic movements (i.e.,
rapid, objectively purposeless, irregular spontaneous). Athetoid
movements (i.e., slow irregular, complex serpentine). Do not include
tremor (i.e., repetitive, regular, rhythmic)
0
1
2
3
4
6. Lower (legs, knees, ankles, toes) e.g., lateral knee movement, foot
tapping, heel dropping, foot squirming, inversion and eversion of foot
0
1
2
3
4
TRUNK
MOVEMENTS
7. Neck, shoulders, hips e.g., rocking. Twisting, squirming pelvic
gyrations
0
1
2
3
4
GLOBAL
JUDGMENTS
8.
9.
10.
11.
12.
0
0
0
0
0
1
1
1
1
1
2
2
2
2
2
3
3
3
3
3
4
4
4
4
4
DENTAL
STATUS
Severity of abnormal action
Incapacitation due to abnormal movements
Patient's awareness of abnormal movements
Current problems
Does patient usually wear dentures?
NOT APPLICABLE: PATIENT HAS NO HISTORY OF TREATMENT WITH NEUROLEPTICS FOR ONE MONTH
OR MORE.
EXAMINATION COMPLETED
SIGNATURE _________________________________________
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DATE OF EXAMINATION