THERAPEUTICS

Brands

• Tercian
• see index for additional brand names

Generic?

• Not in the U.S.

Class

• Conventional antipsychotic (neuroleptic, phenothiazine, dopamine 2 antagonist, serotonin dopamine antagonist)

Commonly Prescribed For

• (bold for FDA approved)
• Schizophrenia
• Anxiety associated with psychosis (short-term)
• Anxiety associated with nonpsychotic disorders, including mood disorders and personality disorders (short-term)
• Severe depression
• Bipolar disorder
• Other psychotic disorders
• Acute agitation/aggression (injection)
• Benzodiazepine withdrawal

How The Drug Works

• Blocks dopamine 2 receptors, reducing positive symptoms of psychosis
• Although classified as a conventional antipsychotic, cyamemazine is a potent serotonin 2A antagonist
• Affinity at a myriad of other neurotransmitter receptors may contribute to cyamemazine’s efficacy
• Specifically, antagonist actions at 5HT2C receptors may contribute to notable anxiolytic effects in many patients
• 5HT2C antagonist actions may also contribute to antidepressant actions in severe depression and to improvement of cognitive and negative symptoms of schizophrenia in some patients

How Long Until It Works

• Psychotic symptoms can improve with high doses within 1 week, but it may take several weeks for full effect on behavior
• Anxiolytic actions can improve with low doses within 1 week, but it may take several days to weeks for full effect on behavior

If It Works

• High doses most often reduce positive symptoms in schizophrenia but do not eliminate them
• Low doses most often reduce anxiety symptoms in psychotic and nonpsychotic disorders
• Most schizophrenia patients do not have a total remission of symptoms but rather a reduction of symptoms by about a third
• Continue treatment in schizophrenia until reaching a plateau of improvement
• After reaching a satisfactory plateau, continue treatment for at least a year, after first episode of psychosis in schizophrenia
• For second and subsequent episodes of psychosis in schizophrenia, treatment may need to be indefinite
• For symptomatic treatment of anxiety in psychotic and nonpsychotic disorders, treatment may also need to be indefinite while monitoring the risks versus the benefits of long term treatment
• Reduces symptoms of acute psychotic mania but not proven as a mood stabilizer or as an effective maintenance treatment in bipolar disorder
• After reducing acute psychotic symptoms in mania, consider switching to a mood stabilizer and/or an atypical antipsychotic for long term mood stabilization and maintenance

If It Doesn’t Work

• For treatment of psychotic symptoms, consider trying one of the first line atypical antipsychotics (risperidone, olanzapine, quetiapine, ziprasidone, aripiprazole, paliperidone, amisulpiride)
• Consider trying another conventional antipsychotic
• If 2 or more antipsychotic monotherapies do not work, consider clozapine
• For treatment of anxiety symptoms, consider adding a benzodiazepine or switching to a benzodiazepine

Best Augmenting Combos for Partial Response or Treatment-Resistance

• Generally, best to switch to another agent
• Augmentation of conventional antipsychotics has not been systematically studied
• Addition of a mood stabilizing anticonvulsant such as valproate, carbamazepine, or lamotrigine may be helpful in both schizophrenia and bipolar mania
• Augmentation with lithium in bipolar mania may be helpful
• Addition of a benzodiazepine, especially for short term agitation
• Addition of antidepressants for severe depression

Tests

• Since conventional antipsychotics are frequently associated with weight gain, before starting treatment, weigh all patients and determine if the patient is already overweight (BMI 25.0–29.9) or obese BMI ≥30)
• Before giving a drug that can cause weight gain to an overweight or obese patient, consider determining whether the patient already has pre-diabetes (fasting glucose 100–125 mg/dL), diabetes (fasting plasma glucose >125 mg/dL) or dyslipidemia (increased total cholesterol, LDL cholesterol and triglycerides; decreased HDL cholesterol), and treat or refer such patients for treatment, including nutrition and weight management, physical activity counseling, smoking cessation and medical management
• Monitor weight, and BMI during treatment
• Consider monitoring fasting triglycerides monthly for several months in patients at high risk for metabolic complications and when initiating or switching antipsychotics
• While giving a drug to a patient who has gained >5% of initial weight, consider evaluating for the presence of pre-diabetes, diabetes or dyslipidemia, or consider switching to a different antipsychotic
• Should check blood pressure in the elderly before starting and for the first few weeks of treatment
• Monitoring elevated prolactin levels of dubious clinical benefit