Anti-Psychotic & Anti-Manic Drugs Part 2 Flashcards
What are the available Typical Antipsychotic Drugs?
-
Phenothiazines
- Chlorpromazine, Triflupromazine
- Thioridazine, Mesoridazine
- Trifluoperazine, Fluphenazine, Perphenazine, Prochlorperazine
-
Thioxanthine derivatives
- Chlorprothixene, Thiothixene
- **Butyrophenone derivative **
- Haloperidol
- Pimozide
What are the 3 types of Phenothiazines?
- Aliphatic side chain
- Piperidine side chain
- Piperazine side chain
**Phenothiazines: Aliphatic side chain **
Examples
Potency
Actions
- **Chlorpromazine, Triflupromazine **
- Low to medium potency
- Sedative
- Pronounced anti-cholinergic actions
Phenothiazines: Piperidine side chain
Examples
Potency
Actions
- Thioridazine, Mesoridazine
- Low potency
- Sedative
- Less extrapyramidal actions, anti-cholinergic
**Phenothiazines: Piperazine side chain **
Examples
Potency
Actions
- **Trifluoperazine, Fluphenazine, Perphenazine, Prochlorperazine **
- High potency
- Less sedative
- More extrapyramidal actions, less anticholinergic
Thioxanthine Derivatives
Examples
Pharmacology
- Chlorprothixene, Thiothixene
- Non-nitrogen containing analogs of the phenothiazines
- Pharmacology is similar to their equivalent phenothiazines
**Butyrophenone Derivative **
Example
Pharmacology
- Haloperidol
- Not chemically related to phenothiazines
- Pharmacologically similar to high-potency piperazine derivatives
Pimozide
Mechanism of Action
Use
- **Potent neuroleptic **
- Many side effects
- Approved for treatment of Tourette’s
- Commonly used when haloperidol doesn’t
What are the Atypical Antipsychotic Agents? (10)
- Clozapine
- Olanzapine
- Risperidone
- Quetiapine
- Aripiprazole
- Ziprasidone
- Paliperidone
- Asenapine
- Iloperidone
- Lurasidone
Clozapine
Mechanism of Action
Side effects
- Blocks D4 & 5-HT2 receptors
- Little effect on D2
- Muscarinic antagonist
- Improves positive symptoms even in patients not helped by other drugs
- Improves negative symptoms
- Lowers seizure thresholds more than other antipsychotics (5-10%)
- Can cause fatal agranulocytosis (monitor)
Olanzapine
Mechanism of Action
Side Effects
- Related to clozapine
- **Potent 5-HT2 antagonist **
- D1 & D2 antagonist, some D4
- Side effects
- Few extrapyramidal symptoms (5-HT>D)
- Less seizure incidence than clozapine
- No agranulocytosis
- **Weight gain & diabetes related adverse events **
- Reports of olanzapine abuse
Risperidone
Mechanism of Action
Side Effects
Pharmacokinetics
- **Combined D2 & 5-HT2 antagonist **
- Greater reduction in negative symptoms & less extrapyramidal symptoms than traditional antipsychotics
- Less seizure activity & less antimuscarinic than clozapine
-
Paliperidone is the active metabolite of risperidone
- Both available as IM depot preparations
Quetiapine
Mechanism of Action
Pharmacokinetics
Use
Side Effects
- Mechanism of Action
- Structurally related to clozapine
- Similar to risperidone & olanzapine in effects on schizophrenia symptoms & side effects
- Pharmacokinetics: shorter t1/2
- Use
- Approved for augmentation in depression
- Side Effects
- Some reports of abuse
Ziprasidone
Mechanism of Action
Side effects
- **5-HT2 & D2 antagonist **
- May have 5-HT1a activity (anxiolytic?)
- No weight gain
Aripiprazole
Mechanism of Action
Use
- **Partial D2 agonist **
- 5-HT2 antagonist
- Approved as an adjunct in depression (augmentation)