PSYCHOPHARMACOLOGY

PSYCHOPHARMACOLOGY:
ANTIPSYCHOTICS &
ANXIOLYTICS
General Psychopharmacology
 PRINCIPLES:
1. Is drug needed?
 If the illness is severe
 Not a personality or behavioral disorder
 Not a reaction to stress
2. Are the benefits more than the risks?
a) Special patient population:
 Elderly patients
 Pregnant and nursing mothers
 Patients with medical disorders
b) Interaction with:
 Alcohol
 Other drugs
c) Tolerance / dependence
e.g. benzodiazepine
d) Lethality in overdose
 Patients with suicidal tendencies
e) Financial cost
3. Has the drug worked before?
4. Would the patient adhere to treatment?
 Single drug
 Once daily
 Depot preparations
5. What dose and for how long?
 Severity of symptoms
 Body weight
 Pharmacokinetics
 Individual charcteristics
GENERAL RULES FOR DOSAGE:
1. Dosage should be determined empirically
for each patient
2. Optimal dosage should be approached
gradually based on:
1. Day to day clinical status
2. Blood level measurement
* A common error with antidepressants is
the use of sub-therapeutic doses!
Stages of Drug Treatment
1. Initiation of medication and escalation of
dosage
 Lasts from several days to weeks
 Aims:- reduce acute danger
- Protect from side-effects
 Stop escalation when:
1. There is good therapeutic progress
2. Moderate side-effects are observed
2. Stabilization stage
 Lasts for several weeks
 Aim:- resolution and normalization of target
symptoms
 There could be minor adjustment of dose
 Explain to the patient and relatives that it
takes sometime. E.g. symptoms of
schizophrenia take 4-6 weeks to respond
3. Short-term maintenance
 Begins after all target symptoms have
disappeared
 There may be increase in intensity of side-effects
 Psychosis and mood disorders need 4 -12 months
of effective treatment
 Medications should be stopped by tapering the
dose
 Close follow up and frequent visits when
medications are being tapered.
4. Long-term maintenance
– Aimed at preventing relapse
– When patients have multiple or serious
relapses
– Dosage is about 60% of that required to
resolve symptoms
– Patients can have drug holidays
 Drug holidays
– For selected patients
– At times of low psychosocial stressors
 Benefits of Drug holidays
1. Reduced cost
2. Reduce side-effects
3. Reduce superfluous tissue stores
Route of Administration
 Oral medication is the usual
 Liquids
– Easier for some patients to swallow
– Harder to hide in the mouth
– Better and faster absorption
 Parenteral (intramuscular)
– Relief from dangerous symptoms
– Excellent absorption
– Those who are unable to take orally
– Uncooperative patient
Route of Administration
 Disadvantages of parenteral route
– Danger of severe side-effect
– Uncooperative patient may interpret injection
as an assault
– Pain, irritation and sometimes abscess
formation
PATIENT EDUCATION
1. The need for medication
2. Why a particular compound is chosen
3. Anticipated benefits
4. Instructions of how to take
5. Possible side-effects
6. Increased vulnerability e.g. accidents
7. Anticipated duration
8. Reasons for changes
ANTIPSYCHOTICS
ANTIPSYCHOTICS
HISTORICAL BACKGROUND
 Era of psychopharmacology began with the
discovery of chlorpromazine
 The first effective antipsychotic in 1950 by
Paul Charpentier
 It was first used to decrease preoperative
anxiety and to make surgical shock less likely
 In 1952, it was used to treat mania and
schizophrenia
ANTIPSYCHOTICS
 Discovery of antipsychotic drugs resulted
in high discharge rates from mental
institutions
 However, medications do not substitute
psychological treatment or social care
 They cannot:
– Change poor life situations
– Resolve intrapsychic conflicts
– Alter adverse environment
ANTIPSYCHOTICS
 Medications can:
– Change the impact of psychosocial factors on the
patients’ functioning
– Alleviate overt and covert symptoms
– Bring severely disturbed patients within the reach
of psychotherapy
– Enable some persons to be treated less
expensively and more rapidly
 Best results are achieved by combination of
drugs and psychological treatment
ANTIPSYCHOTICS
I. DOPAMINE RECEPTOR ANTAGONISTS
 Phenothiazines:
 Mainly act by blocking D2 receptors
 Chlorpromazine is the prototype
 They have additional effects at muscarinic,
adrenergic and histaminergic receptors
 CHLORPROMAZINE (low potent)
 Oral or intramuscular administration
 Starting dose: 100mg bid
DOPAMINE PATHWAYS
Basal
Nucleus Ganglia
accumbens
a
Substantia
b c
nigra
hypothalamus
Tegmentum
10-7 Stahl S M, Essential

Psychopharmacology (2000
ANTIPSYCHOTICS
…CHLORPROMAZINE
 Usual daily dose: 300 – 800mg
 Intramuscular: 100mg q4-6hs (monitor BP!)
THIORIDAZINE (melleril) (low potent)
 Starting dose: 100mg bid
TRIFLUPERAZINE (Stelazine, mederate
potent)
 Starting dose: 2 - 5mg bid
ANTPSYCHOTICS
 FLUPHENAZINE (high potent)
 Only depot preparation available in Ethiopia
 Usual dose: 25 – 50mg i.m. every 2 – 3weeks
BUTYROPHENONES
 HALOPERIDOL (high potent)
 Starting dose: 2mg bid
 Short acting intramuscular: 5 – 10mg q2h
 Depot preparation: 25 – 100mg q4weekly
ANTPSYCHOTICS
 Indications:
1. Acute & maintenance treatment of schizophrenia and
schizoaffective disorders
2. Mania
3. Major depression with psychotic features
4. Delusional disorder
5. Borderline personality disorder
6. Delirium and dementia
7. Substance induced psychotic disorder
8. Psychotic disorder due to GMC
9. Behavioral problems in MR and Autistic disorder
10. Tourette’s disorder
11. Chorea (Huntington’s, Sydnham’s)
ANTIPSYCHOTICS
ADVERSE EFFECTS
 Cardiac: tachycardia, QT prolongation, T-wave
abnormalities (?sudden death)
 Orthostatic hypotension
 Peripheral anticholinergic: dry mouth and nose,
blurred vision, constipation, urinary retention
 Central anticholinergic: severe agitation,
disorientation, fever, stupor
 Extra-pyramidal reactions: e.g. parkinsonism
ANTIPSYCHOTICS
 Weight gain: may lead to non-compliance
 Endocrine: gynecomastia, galactorrhea
 Sexual: decreased libido; impotence in men;
anorgasmia in women
 In general high potent APs cause more
extrapyramidal syndromes
 Epileptogenic effects: low potent APs
 Allergic dermatitis; photosensitivity
 Retinitis pigmentosa – particularly thioridazine
ANTIPSYCHOTICS
II. SEROTONIN DOPAMINE ANTAGONISTS
 Second generation; atypical
antipsychotics
 They act by antagonism at the D2 and
5HT2A receptors
 They have less potential to cause
extrapyramidal adverse effects
 They treat both positive and negative
symptoms
ANTIPSYCHOTICS
A. RISPERIDONE
 First line (elsewhere the world)
 0.5 – 6mg daily
 Extrapyramidal effects when used >6mg/d
 Depot form available
 Adverse effects include: hypotension,
sedation, hyperprolactinemia, nausea,
weight gain
ANTIPSYCHOTICS
B. CLOZAPINE
 The most atypical with negligible
extrapyramidal side-effects
 The most effective against negative symptoms
 Can treat Tardive Dyskinesia
 Fatal agranulocytosis (1-2%) – second line
 Usual daily dose: 300 – 900mg/d
 S/E – sedation, weight gain, seizure,
sialorrhea, anticholinergic effects etc.
ANXIOLYTICS
BENZODIAZEPINES & NON-
BENZODIAZEPINES
BENZODIAZEPINES
 1957 - Chlordiazepoxide (librium)
 Safe and effective medical management of
anxiety
 Increase the affinity of GABAA receptor for GABA
– influx of Chloride ions
 Short acting – Midazolam, Triazolam
 Intermediate – Alprazolam, Bromazepam,
Lorazepam, Oxazepam, Temazepam
 Long acting – Chlordiazepoxide, Clonazepam,
Diazepam
BENZODIAZEPINES
INDICATIONS
 Generalized anxiety disorder (Diazepam)
 Status Epilepticus
 Panic disorder, Social Phobia (Alprazolam,
Clonazepam)
 Neuroleptic induced akathisia and acute dystonia
 Alcohol withdrawal
 Catatonia (Lorazepam, Diazepam, i.v.)
 Depression (Alprazolam)
 Acute mania as adjunct (Clonazepam)
 Short-term treatment of Insomnia
BENZODIAZEPINES
ADVERSE EFFECTS
 Drowsiness, dizziness, ataxia
 Serious CNS effects when combined with other
substances like alcohol
 Tiredness; cognitive effects (poor concentration,
anterograde amnesia)
 Tolerance and dependence – withdrawal effects
 Withdrawal – anxiety, irritability, insomnia,
fatigue, headache, muscle aches, tremor, etc.
BETA-ADRENERGIC BLOCKERS
PROPRANOLOL can be used in cases of:
 Social phobia (to reduce performance anxiety)
 Tremors (Familial, Medication induced)
 Neuroleptic induced akathisia
 Prophylaxis against Migraine headache
 Aggression associated with brain injuries
 Adverse effects:- Bradycardia, hypotension,
insomnia, fatigue, nausea, impotence
BUSPIRONE
 Not related to Benzodiazepines
 Acts at 5HT1A receptors
 No sedative, hypnotic, anticonvulsant or muscle
relaxant effects
 No abuse potential or cross tolerance
 Its effect starts after 2-3 weeks
 Indications: GAD, adjunct with SSRIs in the
treatment of Depression or OCD
 Adverse effects: headache, dizziness, insomnia,
nausea, diarrhea

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PSYCHOPHARMACOLOGY:

10-7 Stahl S M, Essential

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