Trifluoperazine Hydrochloride
Pronouncation: (try-flew-oh-PURR-uh-zeen HIGH-droe-KLOR-ide)Class: Phenothiazine derivative
Trade Names:
Trifluoperazine HCl
- Tablet 1 mg
- Tablet 2 mg
- Tablet 5 mg
- Tablet 10 mg
Pharmacology
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Effects apparently related to dopamine receptor blocking in CNS.
Pharmacokinetics
Absorption
Absorption is erratic and variable. T max occurs 2 to 4 h after oral use.
Distribution
Trifluoperazine is widely distributed in tissues. CNS concentrations exceed those in plasma. Approximately 91% to 99% of the drug is protein bound. Because trifluoperazine is highly lipophilic, parent drug and metabolites accumulate in brain, lungs, and other tissues with high blood supply. The drug may be found in urine for up to 6 mo after the last dose.
Metabolism
Extensive biotransformation occurs in the liver. Numerous active metabolites, which persist for prolonged periods, have important adverse reactions and contribute to the biological activity of the parent drug.
Elimination
50% of excretion occurs via kidneys; the other 50% is through enterohepatic circulation. The t ½ is approximately 20 to 40 h. Less than 1% is excreted as unchanged drug.
Special Populations
ElderlyThe elderly have diminished capacity to metabolize and eliminate trifluoperazine.
ChildrenFetuses and infants have diminished capacity to metabolize and eliminate trifluoperazine; children tend to metabolize more rapidly than adults.
Indications and Usage
Management of schizophrenia; short-term treatment (less than 12 wk) of nonpsychotic anxiety.
Contraindications
Sensitivity to phenothiazines; comatose or severely depressed states; presence of large amounts of other CNS depressants; bone marrow depression or blood dyscrasias; liver disease.
Dosage and Administration
Individualize dose.
SchizophreniaAdults
PO 2 to 5 mg twice daily initially. Maintenance: 15 to 20 mg/day in single or divided doses. Few patients may require 40 mg/day or more.
ChildrenIndividualize dosage based on weight of child and severity of symptoms.
Children 6 to 12 yr of agePO 1 mg once or twice daily initially. Maintenance: Rarely over 15ߙmg/day in single or divided doses.
Nonpsychotic AnxietyAdults
PO 1 to 2 mg twice daily (max, 6ߙmg/day).
Storage/Stability
Store tablets at controlled room temperature (59° to 86°F).
Drug Interactions
Alcohol and other CNS depressants (eg, narcotics, sedatives)May result in increased CNS depression and may precipitate dystonic reactions.
AnticholinergicsMay reduce therapeutic effects of trifluoperazine and worsen anticholinergic effects of trifluoperazine. May lead to tardive dyskinesia.
Barbiturate anestheticsMay increase frequency and severity of neuromuscular excitation and hypotension.
Beta-blockersMay result in increased plasma levels of beta-blocker and trifluoperazine.
Cisapride, sparfloxacinThe risk of life-threatening cardiac arrhythmias, including torsades de pointes, may be increased.
GuanethidineMay inhibit hypotensive action of guanethidine.
MetrizamidePossibility of seizure may be increased when subarachnoid metrizamide injection is used.
ParoxetinePlasma levels of trifluoperazine may be elevated, increasing the risk of adverse reactions.
Laboratory Test Interactions
Drug may discolor urine pink to red-brown. False-positive pregnancy tests may occur but are less likely to occur with serum test. Increases in protein-bound iodine reported. False-positive test for phenylketonuria may occur.
Adverse Reactions
Cardiovascular
Orthostatic hypotension; tachycardia; syncope; cardiac arrest; circulatory collapse; ECG changes.
CNS
Lightheadedness; faintness; headache; weakness; tremor; fatigue; slurring of speech; insomnia; sedation; vertigo; seizures; twitching; ataxia; tardive dyskinesia; drowsiness; lethargy; paradoxical excitement; pseudoparkinsonism; motor restlessness; oculogyric crises; opisthotonos; hyperreflexia; tardive dyskinesia; dizziness; dystonia.
Dermatologic
Photosensitivity; skin pigmentation; dry skin; exfoliative dermatitis; urticarial rash; maculopapular hypersensitivity reaction; seborrhea; contact dermatitis.
EENT
Pigmentary retinopathy; glaucoma; photophobia; blurred vision; miosis; mydriasis; increased IOP; dry mouth or throat; nasal congestion.
GI
Dyspepsia; constipation; adynamic ileus (may result in death); nausea; anorexia.
Genitourinary
Urinary hesitancy or retention; impotence; sexual dysfunction; menstrual irregularities; priapism; breast enlargement; galactorrhea.
Hepatic
Cholestatic jaundice.
Hematologic
Agranulocytosis; eosinophilia; leukopenia; hemolytic anemia; thrombocytopenic purpura; pancytopenia.
Metabolic
Decreased cholesterol.
Respiratory
Laryngospasm; bronchospasm; shortness of breath.
Miscellaneous
Increases in appetite and weight; polydipsia; heat-illness; neuroleptic malignant syndrome (NMS); elevated prolactin levels.
Precautions
Pregnancy
Undetermined.
Lactation
Excreted in breast milk.
Children
In general, not recommended for children younger than 12 yr of age. When drug is used in children with acute illnesses (eg, chickenpox, measles, gastroenteritis, dehydration), they are more susceptible to neuromuscular reactions than adults. Avoid use of drug in children and adolescents with signs and symptoms suggestive of Reye syndrome.
Renal Function
Use with caution. Lower dose may be necessary.
Hepatic Function
Use with caution.
Special Risk Patients
Use with caution in patients with CV disease or mitral insufficiency, history of glaucoma, EEG abnormalities, seizure disorders, prior brain damage, or in those exposed to extreme heat.
CNS effects
Drug may impair mental or physical abilities, especially during first few days of therapy.
Elderly, debilitated, or emaciated patients
More susceptible to hypotensive and neuromuscular effects. Require lower initial dosage and more gradual increase in dosage.
Hepatic effects
Jaundice usually occurs between second and fourth weeks of treatment and is considered a hypersensitivity reaction; usually reversible.
NMS
NMS occurred with agents in this class and is potentially fatal. Signs and symptoms are hyperpyrexia, muscle rigidity, altered mental status, irregular pulse, irregular BP, tachycardia, and diaphoresis.
Pulmonary effects
Cases of bronchopneumonia, some fatal, have occurred.
Sudden death
Sudden death reported. Predisposing factors may be seizures or previous brain damage. Flare-ups of psychotic behavior may precede death.
Tardive dyskinesia
Syndrome of potentially irreversible involuntary body and facial movements may develop. Prevalence highest in elderly, especially women. Use smallest effective doses for shortest possible time.
Overdosage
Symptoms
CNS depression (somnolence to coma), hypotension, extrapyramidal symptoms, agitation, restlessness, seizures, fever, hypothermia, hyperthermia, autonomic reactions, ECG changes, cardiac arrhythmias.
Patient Information
- Advise patient, family, or caregiver that dose will be adjusted periodically until max benefit has been obtained.
- Advise patient, family, or caregiver not to change the dose or stop taking unless advised by health care provider.
- Instruct patient not to stop taking trifluoperazine when feeling better.
- Instruct patient, family, or caregiver to immediately report fainting or loss of consciousness, palpitations, dizziness, high fever, muscle rigidity, altered mental status, irregular pulse, unusual bruising, yellowing of the skin or eyes, sore throat, or other signs of infection.
- Advise patient, family, or caregiver to notify health care provider of excessive drowsiness, increased agitation or anxiety, or involuntary body or facial movements.
- Advise patient to avoid strenuous activity during periods of high temperature or humidity.
- Instruct patient to avoid alcoholic beverages and other depressants while taking this medication.
- Instruct patient to get up slowly from lying or sitting position and to avoid sudden position changes to prevent postural hypotension. Advise patient to report dizziness with position changes to health care provider. Caution patient that hot tubs and hot showers or baths may worsen dizziness.
- Advise patient to take sips of water, suck on ice chips or sugarless hard candy, or chew sugarless gum if dry mouth occurs.
- Advise patient that drug may cause drowsiness or impaired judgment or thinking skills and to use caution while driving or performing other tasks requiring mental alertness until tolerance is determined.
- Caution patient that medication may cause sensitivity to sunlight and to avoid unnecessary exposure to UV light (eg, sunlight, tanning booths), and use sunscreen and wear protective clothing when exposed to UV light until tolerance is determined.
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