Trifluoperazine

Trifluoperazine is an oral antipsychotic medication used for the management of schizophrenia. Trifluoperazine is one of the older, first-generation antipsychotic medications. Examples of other first-generation antipsychotics include:

• prochlorperazine (Compazine, Compro, Procomp)
• chlorpromazine (Promapar, Thorazine)
• perphenazine (Trilafon)
• thioridazine (Mellaril)

Although the exact mechanism of antipsychotics is unknown, scientists believe that they may work by blocking the action of dopamine in the brain. Dopamine is a neurotransmitter (chemical) that nerves use to communicate with one another. Trifluoperazine is used when patients do not respond to other antipsychotics.

Combining trifluoperazine with medications such as procainamide (Pronestyl), sotalol (Betapace), amiodarone (Cordarone), and dofetilide (Tikosyn) that affect heart rate and rhythm can cause abnormal heart beats.

Antidepressants such as fluoxetine (Prozac), sertraline (Zoloft), and and tricyclic antidepressants may reduce the break down of trifluoperazine, leading to increased blood levels and more side effects of trifluoperazine.

Trifluoperazine should be used with caution with medications that depress the central nervous system and cause sedation or drowsiness. Examples include alprazolam (Xanax), lonazepam (Klonopin), zolpidem (Ambien), codeine, morphine, and alcohol. Such combinations can cause excessive sedation, drowsiness, weakness, confusion, speech impairment, and in severe cases coma or death. Combining alcohol with trifluoperazine also increases the risk of low blood pressure.

Use of trifluoperazine during pregnancy has not been adequately studied. Neonates exposed to antipsychotics during the third trimester of pregnancy are at risk for extrapyramidal and withdrawal symptoms after birth. Symptoms reported included agitation, hypertonia, hypotonia, tremor, somnolence, depressed breathing, and feeding disorder.

Safe use of trifluoperazine by nursing mothers has not been established.

Tablets: Each round, blue, film-coated tablet contains trifluoperazine hydrochloride equivalent to trifluoperazine as follows: 1 mg imprinted SKF and S03; 2 mg imprinted SKF and S04; 5 mg imprinted SKF and S06; 10 mg imprinted SKF and S07. Inactive ingredients consist of cellulose, croscarmellose sodium, FD&C Blue No. 2, FD&C Yellow No. 6, FD&C Red No. 40, gelatin, iron oxide, lactose, magnesium stearate, talc, titanium dioxide and trace amounts of other inactive ingredients.

Multi-Dose Vials, 10 mL (2 mg/mL)—Each mL contains, in aqueous solution, trifluoperazine, 2 mg, as the hydrochloride; sodium tartrate, 4.75 mg; sodium biphosphate, 11.6 mg; sodium saccharin, 0.3 mg; benzyl alcohol, 0.75%, as preservative.

Concentrate—Each mL of clear, yellow, banana-vanilla-flavored liquid contains 10 mg of trifluoperazine as the hydrochloride. Inactive ingredients consist of D&C Yellow No. 10, FD&C Yellow No. 6, flavor, sodium benzoate, sodium bisulfite, sucrose and water.

N.B.: The Concentrate is for use in schizophrenia when oral medication is preferred and other oral forms are considered impractical.

For the management of schizophrenia.

Stelazine (trifluoperazine HCl) is effective for the short-term treatment of generalized non-psychotic anxiety. However, Stelazine (trifluoperazine) is not the first drug to be used in therapy for most patients with non-psychotic anxiety because certain risks associated with its use are not shared by common alternative treatments (i.e., benzodiazepines).

When used in the treatment of non-psychotic anxiety, Stelazine (trifluoperazine) should not be administered at doses of more than 6 mg per day or for longer than 12 weeks because the use of Stelazine (trifluoperazine) at higher doses or for longer intervals may cause persistent tardive dyskinesia that may prove irreversible (see WARNINGS).

The effectiveness of Stelazine (trifluoperazine) as a treatment for non-psychotic anxiety was established in a 4-week clinical multicenter study of outpatients with generalized anxiety disorder (DSM-III). This evidence does not predict that Stelazine (trifluoperazine) will be useful in patients with other non-psychotic conditions in which anxiety, or signs that mimic anxiety, are found (i.e., physical illness, organic mental conditions, agitated depression, character pathologies, etc.).

Stelazine (trifluoperazine HC1) has not been shown effective in the management of behavioral complications in patients with mental retardation.

Trifluoperazine is a prescription medication used to treat schizophrenia or anxiety. Trifluoperazine belongs to a group of drugs called typical antipsychotics, which work by altering the level of certain natural substances in the brain to restore mental balance.

This medication comes in tablet form and is typically taken 2 times a day, with or without food.

Common side effects of trifluoperazine include drowsiness, dizziness, skin reactions, rash, and dry mouth. Do not drive or operate heavy machinery until you know how trifluoperazine affects you.

Trifluoperazine is not approved for use in psychotic conditions related to dementia. Trifluoperazine may increase the risk of death in older adults with dementia-related conditions.

You should not use trifluoperazine if you have bone marrow suppression, liver disease, a blood cell disorder, or if you have drowsiness, slow breathing, weak pulse, or decreased alertness (such as after drinking alcohol or taking medicines that make you sleepy).

Follow all directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results. Do not take this medicine in larger or smaller amounts or for longer than recommended.

Call your doctor if your symptoms do not improve, or if they get worse while using trifluoperazine.

Do not stop using trifluoperazine suddenly, or you could have unpleasant withdrawal symptoms. Ask your doctor how to safely stop using trifluoperazine.

Store at room temperature away from moisture, heat, and light.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Overdose symptoms may include dry mouth, constipation, extreme drowsiness or feeling restless and agitated, changes in heart rate, fainting, and seizure (convulsions).

Use trifluoperazine as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• Drink lots of noncaffeine liquids unless told to drink less liquid by your doctor.
• Keep taking this medicine as you have been told by your doctor or other health care provider, even if you feel well.

What do I do if I miss a dose?

• Take a missed dose as soon as you think about it.
• If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
• Do not take 2 doses at the same time or extra doses.

• Store at room temperature.
• Store in a dry place. Do not store in a bathroom.
• Protect from light.
• Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
• Check with your pharmacist about how to throw out unused drugs.

Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Analyses of 17 placebo-controlled trials (modal duration of 10 weeks), largely in patients taking atypical antipsychotic drugs, revealed a risk of death in drug-treated patients between 1.6 and 1.7 times the risk of death in placebo-treated patients. Over the course of a typical 10-week controlled trial, the rate of death in drug-treated patients was approximately 4.5%, compared to a rate of approximately 2.6% in the placebo group. Although the causes of death were varied, most of the deaths appeared to be either cardiovascular (eg, heart failure, sudden death) or infectious (eg, pneumonia) in nature. Observational studies suggest that, similar to atypical antipsychotic drugs, treatment with conventional antipsychotic drugs may increase mortality. The extent to which the findings of increased mortality in observational studies may be attributed to the antipsychotic drug as opposed to some characteristic(s) of the patients is not clear. Trifluoperazine is not approved for the treatment of patients with dementia-related psychosis.

Consult your pharmacist.

Applies to trifluoperazine: oral tablets

Side effects include:

Extrapyramidal reactions (e.g., Parkinson-like symptoms, dystonia, akathisia), drowsiness, fatigue, muscular weakness, insomnia, blurred vision, skin reactions or rash, anorexia, dry mouth, hypotension, amenorrhea, galactorrhea.

Applies to trifluoperazine: compounding powder, intramuscular solution, oral concentrate, oral tablet

Nervous system

Frequency not reported: Drowsiness, dizziness, tremulousness, extrapyramidal symptoms, parkinsonism, acute dystonia/dyskinesia, facial grimacing, opisthotonos, hyperreflexia, tardive dyskinesia/tardive dyskinesia of the facial muscles, involuntary movement of the extremities, neuroleptic malignant syndrome, altered consciousness, autonomic instability, grand/petite mal convulsions, altered cerebrospinal fluid proteins, cerebral edema, headache, akathisia (with motor restlessness and difficulty sitting still)[Ref]

Extrapyramidal symptoms were more common in doses of over 6 mg/day. Symptoms included parkinsonism, torticollis, facial grimacing, trismus, tongue protrusion, abnormal eye movements, akathisia with motor restlessness and difficulty sitting still.

Acute dystonia/dyskinesia typically occurred early in treatment and was likely to be severe in children; this side effect included torticollis, facial grimacing, trismus, tongue protrusion, and abnormal eye movements.

Neuroleptic malignant syndrome was characterized by hyperpyrexia, muscle rigidity, altered consciousness and autonomic instability.

Grand/petite mal convulsions occurred in patients with/a history of EEG abnormalities.[Ref]

Cardiovascular

Severe hypotension occurred in patients with specific medical problems (e.g., mitral insufficiency, pheochromocytoma).

ECG changes, including QT prolongation and T-wave distortions, were typically reversible and occurred in patients taking phenothiazine antipsychotics.[Ref]

Frequency not reported: Mild postural hypotension/hypotension, edema/peripheral edema, tachycardia, ECG changes, QT prolongation, T-wave changes, ventricular arrhythmias/fibrillation/tachycardia, atrioventricular block, paroxysmal tachycardia, serious arrhythmias, cardiac arrest, Torsade de pointes, venous thromboembolism, deep vein thrombosis, severe hypotension/fatal hypotension[Ref]

Dermatologic

Skin pigmentation and epithelial keratopathy occurred in patients receiving substantial doses for a prolonged duration.

Contact dermatitis occurred in patients who handled phenothiazines.[Ref]

Frequency not reported: Skin reactions/disorders, photosensitivity reactions, skin pigmentation, epithelial keratopathy, itching/pruritus, erythema, urticaria, angioneurotic edema, erythema multiforme, contact dermatitis, eczema (up to exfoliative dermatitis)[Ref]

Psychiatric

Frequency not reported: Transient restlessness, stimulation, insomnia, confusion/toxic confusional states, feelings dulled, agitation, increased aggressiveness, withdrawal reactions, reactivation of the psychotic processes, catatonic-like states[Ref]

Dulled feelings and/or agitation have occurred at low doses, especially in non-psychotic patients.[Ref]

Other

Sudden death from cardiac arrest or asphyxia (cough reflex failure) has been reported in patients receiving phenothiazines.[Ref]

Frequency not reported: Lassitude, fatigue, hyperpyrexia, sudden, unexplained death, signs of persistent infection, neonatal drug withdrawal syndrome, autonomic reactions, reversed epinephrine effect, intensification/prolongation of the action of atropine/heat/organophosphorous insecticides/central nervous system depressants (e.g., opiates, analgesics, antihistamines, barbiturates, alcohol)[Ref]

Hematologic

Frequency not reported: Blood dyscrasias, agranulocytosis, pancytopenia, leukopenia, thrombocytopenia, thrombocytopenic purpura, eosinophilia, hemolytic anemia, aplastic anemia[Ref]

Ocular

Lenticular and corneal deposits occurred in patients receiving substantial doses for a prolonged duration.[Ref]

Frequency not reported: Blurred vision, abnormal eye movements, oculogyric crisis, lenticular opacities, pigmentary retinopathy, lacrimation, keratoconjunctivitis, miosis and mydriasis, lenticular and corneal deposits[Ref]

Gastrointestinal

Frequency not reported: Dry mouth, constipation, tongue protrusion, nausea, vomiting, obstipation, ileus/adynamic ileus, atonic colon[Ref]

Genitourinary

Frequency not reported: Urinary hesitancy/retention, lactation, galactorrhea, menstrual irregularities, false-positive pregnancy tests, amenorrhea, ejaculation disorders/impotence, priapism[Ref]

Musculoskeletal

Frequency not reported: Muscular weakness, torticollis, trismus, muscle rigidity, systemic lupus erythematosus-like syndrome[Ref]

Metabolic

Frequency not reported: Anorexia, weight gain/change, hyperglycemia, hypoglycemia, increased appetite[Ref]

Respiratory

Frequency not reported: Pulmonary embolism, nasal congestion, asthma, bronchospasm, laryngeal edema[Ref]

Hepatic

Frequency not reported: Mild cholestatic jaundice, liver damage, jaundice, biliary stasis[Ref]

Endocrine

Hyperprolactinemia occurred in patients given higher doses, and was associated with the development of galactorrhea, amenorrhea, and/or gynecomastia.[Ref]

Frequency not reported: Gynecomastia, hyperprolactinemia/elevated prolactin levels, endocrine disturbances[Ref]

Hypersensitivity

Frequency not reported: Other allergic reactions, anaphylaxis/anaphylactoid reactions[Ref]

Oncologic

Frequency not reported: Hormone-dependent breast neoplasms[Ref]

Renal

Frequency not reported: Glycosuria[Ref]

Some side effects of trifluoperazine may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA.