Antipsychotic Agents& Lithium (Pharmacology)
Antipsychotics
Bipolar drugs
2.Thioxanthene
3.Butyrophenone
1.Phenothiazines
4.Atypicals
Effects
Clinical uses
Mechanism of Action
Pharmacokinetics
Drugs
Toxicities
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Chlorpromazine
Fluphenazine
Thioridazine
Block of D2,receptors >>5-HT2 receptors
Block α, M, and H1 receptors
Schizophrenia, Bipolar disorder(Manic phase)
Oral and parenteral forms, hepatic metabolism , long half-life
Extensions of α- and M receptor-blocking actions ,Extrapyramidal dysfunction, tardive dyskinesias,
hyperprolactinemia
Drug
Thiothixene
Effects
Clinical uses
Mechanism of Action
Pharmacokinetics
Drug
Toxicities
Haloperidol
Block of D2 receptors >>5-HT2 receptors
Some α block
Schizophrenia ; bipolar disorder (manic phase), Huntington’s chorea, Tourette’s syndrome
Oral and parenteral form, Hepatic Metabolism
Extrapyramidal dysfunction(major)
Mechanism of Action
Effects
Clinical uses*
Pharmacokinetics
Drugs
Toxicities
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Aripiprazole
Clozapine
Olanzapine
Quetiapine
Risperidone
Ziprasidone
Block of 5-HT2 Block of 5-HT2
receptors >> D2
receptors
Some α block (clozapine, risperidone, ziprasidone) and M block (clozapine, olanzapine), variable H1 block
Schizophrenia (positive and negative): Bipolar disorder,Major Depressive,agitation in Alzheimer’s and Parkinson’s.
Oral and parenteral form, Hepatic Metabolism
Agranulocytosis s (clozapine);DM,Weight gain (clozapine, olanzapine), hyperprolactinemia (Risperidone),QT Prolong (ziprasidone)
1.Lithium
2.Alternative drugs for bipolar affective disorder
Clinical uses
Pharmacokinetics
Effects
Toxicities
Mechanism of Action
Uncertain, suppresses IP3 and DAG signaling
No specific actions on ANS receptors or specific CNS Receptors:No sedation
Bipolar affective disorder: Prevenrt Mood swings (Prophylaxis)
Renal elimination half life 20 hr : Narrow Therapeutic window Monitor Blood levels
Tremor, edema, hypothyroidism, renal dysfunction Pregnancy Category D
Effects
Mechanism of Action
Clinical uses
Pharmacokinetics
Drugs
Toxicities
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Carbamazepine
Lamotrigine
Valproic acid
Unclear actions in bipolar disorder
Ataxia and diplopia(carbamazepine),Nausea,Dizeness,and headache (Lamotrigine)Gastrointestinal Distress, Weight Grain,Alopesia(Valproic acid)
Valproic acid competes with lithium as
first choice in bipolar disorder, acute phase
Carbamazepine forms active metabolite (phase I); lamotrigine and valproic acid form conjugates (phase II)
Hematotoxicity and
induction of drug metabolism,Rash, Hepatic dysfunction,Weight gain,Inhibition drug metabolism