PSYCHOACTIVE AGENTS AND

LITHIUM

BY: DR. EMILIANO Z. SISON JR.

PSYCHOACTIVE
AGENTS
 ANTIPSYCHOTIC AGENTS
• The terms antipsychotic and
neuroleptic are used
interchangeably to denote a group of
drugs that have been used mainly for
treating schizophrenia but are also
effective in some other psychoses and
agitated states.
 NATURE OF
PSYCHOSIS AND SCHIZOPHRENIA
• The term "psychosis" denotes a variety of mental
disorders.
• Schizophrenia is a particular kind of psychosis
characterized mainly by a clear sensorium but a
marked thinking disturbance.
• The pathogenesis of schizophrenia is unknown.
 LITHIUM
AND
OTHER MOOD-STABILIZING
DRUGS
 Lithium & Other Mood-Stabilizing Drugs

• Lithium carbonate is often referred to as an

"antimanic" drug, but in many parts of the world it
is considered a "mood-stabilizing" agent because of
its primary action of preventing mood swings in
patients with bipolar affective (manic-depressive)
disorder.
• Discovery of its benefits was based on an incorrect
hypothesis and extremely good fortune in choosing
the correct dosage.
 Lithium & Other Mood-Stabilizing Drugs
• Carbamazepine has also been recognized as
effective in some groups of manic-depressive
patients despite not being formally approved for
such use.
• Valproate has recently been approved for the
treatment of mania and is being evaluated as a
mood stabilizer.
• Atypical antipsychotics, beginning with olanzapine,
are being investigated and approved as antimanic
agents and potential mood stabilizers.
Nature of Bipolar Affective Disorder
• Bipolar affective (manic-depressive) disorder is
a frequently diagnosed and very serious
psychiatric disorder.
• Patients with cyclic attacks of mania have many
symptoms of paranoid schizophrenia
(grandiosity, bellicosity, paranoid thoughts, and
overactivity).
• The gratifying response to lithium therapy of
patients with bipolar disorder has made such
diagnostic distinctions important.
Summary of Antipsychotic Drugs and
Lithium

Phenothiazines

Thioxanthene

Butyrophenone

Atypical Psychotics

Lithium
Newer Agents for Bipolar Disorder
PHENOTHIAZINES & THIOXANTHENE
1. CHLORPROMAZINE
2. FLUPHENAZINE 1. THIOTHIXENE
3. THIORIDAZINE

MECHANISM OF ACTION
Blockade of D2 receptors >>
5HT2A receptors
 CLINICAL APPLICATIONS
• 1. PSYCHIATRIC:
• •Schizophrenia (alleviate positive symptoms)
• •Bipolar Disorder (manic phase)
• 2. NONPSYCHIATRIC:
• •Anti-emesis
• •Preoperative sedation
• 3. Pruritus
BUTYROPHENONE
1. HALOPERIDOL

MECHANISM OF ACTION
Blockade of D2 receptors >>
5HT2A receptors
 CLINICAL APPLICATIONS
• 1. SCHIZOPRENIA (alleviates positive
symptoms)
• 2. BIPOLAR DISORDER (manic phase)
• 3. HUNTINGTON’S CHOREA
• 4.TOURETTE’S SYNDROME
ATYPICAL ANTIPSYCHOTICS
1. ARIPIRAZOLE
2. CLOZAPINE
3. OLANZAPINE
4. QUETIAPINE
5. RISPERIDONE
6. ZIPRASIDONE

MECHANISM OF ACTION
Blockade of D2 receptors >>
5HT2A receptors
 CLINICAL APPLICATIONS
• 1. SCHIZOPRENIA (improve both positive and
negative symptoms)
• 2. BIPOLAR DISORDER (olanzapine or
risperidone adjunctive with lithium)
• 3. Agitation in ALZHEIMER’S & PARKINSON’S
(low doses)
• 4. MAJOR DEPRESSION (aripiprazole)
LITHIUM

MECHANISM OF ACTION

Mechanism of action is uncertain.

Suppresses inositol signaling and inhibits

glycogen synthase kinase-3 (GSK-3), a
multifunctional protein kinase
 17

CLINICAL APPLICATIONS
• 1. BIPOLAR AFFECTIVE DISORDER
• 2. PROPHYLACTIC USE can prevent mood
swings between mania and depression
NEWER AGENTS FOR BIPOLAR
DISORDER
1. CARBAMAZEPINE
2. LAMOTRIGINE
3. VALPROIC ACID

MECHANISM OF ACTION

Mechanism of action is unclear.

 CLINICAL APPLICATIONS
• 1. Valproic acid is increasingly used as first
choice in acute illness.

• 2. Carbamazepine and Lamotrigine are also used

both in acute mania and for the prophylaxis in
• depressive phase.
END OF DISCUSSION ABOUT
PSYCHOACTIVE AGENTS AND
LITHIUM...