brands

Class

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

Prolinate commonly prescribed for

(Bold for FDA approved)

How Prolinate works

• Blocks dopamine 2 receptors, reducing positive symptoms of psychosis

How long until Prolinate works

• Psychotic symptoms can improve within 1 week, but it may take several weeks for full effect on behavior

Notable Side Effects

• Neuroleptic-induced deficit syndrome

• Akathisia

• Priapism

• Drug-induced parkinsonism

• Tardive dyskinesia, tardive dystonia

• Risk of potentially irreversible involuntary dyskinetic movements may increase with cumulative dose and treatment duration

• Galactorrhea, amenorrhea

• Dizziness, sedation

• Dry mouth, constipation, urinary retention, blurred vision

• Decreased sweating, depression

• Sexual dysfunction

• Hypotension, tachycardia, syncope

• Weight gain

Life Threatening Side Effects

• Rare neuroleptic malignant syndrome may cause hyperpyrexia, muscle rigidity, delirium, and autonomic instability with elevated creatine phosphokinase, myoglobinuria (rhabdomyolysis), and acute renal failure

• Rare jaundice, agranulocytosis

• Rare seizures

• As a class, antipsychotics are associated with an increased risk of death and cerebrovascular events in elderly patients with dementia; not approved for treatment of dementia-related psychosis

weight gain

not usual

sedation

not usual

What to do about Prolinate side effects

• Wait

• Wait

• Wait

• For drug-induced parkinsonism, add an anticholinergic agent

• Beta blockers, benzodiazepines, or serotonin 2A antagonists (e.g., mirtazapine, cyproheptadine) may reduce akathisia

• Reduce the dose

• For sedation, take at night

• Switch to an atypical antipsychotic

• Weight loss, exercise programs, and medical management for high BMIs, diabetes, dyslipidemia

• Metformin may help prevent or reverse antipsychotic-induced weight gaiN

usual dosage range

• Oral: 1–20 mg/day maintenance

• Intramuscular: generally 1/3 to 1/2 the oral dose

• Decanoate for intramuscular or subcutaneous administration: 12.5– 100 mg/2 weeks maintenance (see Fluphenazine Decanoate section after Pearls for dosing and use)

Dosage Forms

• Tablet 1 mg, 2.5 mg scored, 5 mg scored, 10 mg scored

• Decanoate for long-acting intramuscular or subcutaneous administration 25 mg/mL

• Injection for acute intramuscular administration 2.5 mg/mL

• Elixir 2.5 mg/5 mL

• Concentrate 5 mg/mL

long term use

• Should periodically reevaluate long-term usefulness in individual patients, but treatment may need to continue for many years

habit forming

• No

Renal Impairment

• Use with caution; titration should be slower

Hepatic Impairment

• Use with caution; titration should be slower

Cardiac Impairment

• Cardiovascular toxicity can occur, especially orthostatic hypotension

Elderly

• Titration should be slower; lower initial dose (1–2.5 mg/day)

• Elderly patients may be more susceptible to adverse effects

• Although conventional antipsychotics are commonly used for behavioral disturbances in dementia, no agent has been approved for treatment of elderly patients with behavioral symptoms of dementia such as agitation

• Elderly patients with dementia-related psychosis treated with antipsychotics are at an increased risk of death compared to placebo, and also have an increased risk of cerebrovascular events

Children and Adolescents

• Safety and efficacy not established

• Decanoate and enanthate injectable formulations are contraindicated in children under age 12

• Generally consider second-line after atypical antipsychotics

Pregnancy

• Effective June 30, 2015, the FDA requires changes to the content and format of pregnancy and lactation information in prescription drug labels, including the elimination of the pregnancy letter categories; the Pregnancy and Lactation Labeling Rule (PLLR or final rule) applies only to prescription drugs and will be phased in gradually for drugs approved on or after June 30, 2001

• There is a risk of abnormal muscle movements and withdrawal symptoms in newborns whose mothers took an antipsychotic during the third trimester; symptoms may include agitation, abnormally increased or decreased muscle tone, tremor, sleepiness, severe difficulty breathing, and difficulty feeding

• Reports of drug-induced parkinsonism, jaundice, hyperreflexia, hyporeflexia in infants whose mothers took a phenothiazine during pregnancy

• Fluphenazine should only be used during pregnancy if clearly indicated

• Psychotic symptoms may worsen during pregnancy and some form of treatment may be necessary

• Atypical antipsychotics may be preferable to conventional antipsychotics or anticonvulsant mood stabilizers if treatment is required during pregnancy

Breast Feeding

• Some drug is found in mother’s breast milk

• Effects on infant have been observed (dystonia, tardive dyskinesia, sedation)

• Recommended either to discontinue drug or bottle feed