Fluphenazine hydrochloride

Name: Fluphenazine hydrochloride

Introduction

Propylpiperazine-derivative phenothiazine; conventional (prototypical, first-generation) antipsychotic agent.a b c d f g i k

Uses for fluphenazine hydrochloride

Psychotic Disorders

Symptomatic management of psychotic disorders (i.e., schizophrenia).a b c f g i

The long-acting decanoate ester is used mainly for maintenance therapy in patients with chronic schizophrenic disorder who cannot be relied on to take oral antipsychotic drugs; do not use for acute management of severely agitated patients.a b

Mental Retardation

Efficacy not established for management of behavioral complications in mental retardation.a b c f g i

Interactions for fluphenazine hydrochloride

Specific Drugs and Laboratory Tests

Drug or Test

Interaction

Comments

Anticonvulsants

Phenothiazines may lower seizure threshold, but CNS depressant effects do not potentiate anticonvulsant activity of anticonvulsantsd

Dosage adjustment of anticonvulsant may be necessary to maintain seizure control during concomitant used

Atropine

Possible potentiated effects of atropine in some patients receiving fluphenazine because of added anticholinergic effectsb c f g i

CNS depressants (e.g., alcohol, analgesics, antihistamines, barbiturates, general anesthetics, opiates)

Possible additive effects or potentiated action of other CNS depressantsb c d f g i

Use concomitantly with caution to avoid excessive sedation or CNS depression (see Contraindications)b c d

During surgery in patients receiving high fluphenazine dosages, may need to reduce dosages of anesthetics or other CNS depressantsb c f g i

Epinephrine

Reversal of epinephrine actionb c f g i

Do not use epinephrine for phenothiazine-induced hypotension; further lowering of BP may resultb c f g i

Lithium

An acute encephalopathic syndrome reported occasionally, especially when high serum lithium concentrations presentd

Observe patients receiving combined therapy for evidence of adverse neurologic effects; promptly discontinue if such signs or symptoms appeard

Test for phenylketonuria (PKU)

False-positive test results may occur during phenothiazine used

Tests for pregnancy

False-positive results reported in some patients receiving phenothiazinesb c d f g i

Tests for urobilinogen, amylase, uroporphyrins, porphobilinogens, 5-hydroxyindolacetic acid

Urinary metabolites of phenothiazines may cause urine to darken and result in false-positive test resultsd

fluphenazine hydrochloride Pharmacokinetics

Absorption

Bioavailability

Rapidly absorbed from GI tract and from parenteral sites.a Peak serum concentrations were attained within 1.5–2 or 0.5 hours after IM or oral administration, respectively, of fluphenazine hydrochloride.a

Onset

Fluphenazine hydrochloride: Usually occurs within 1 hour following oral or IM administration.a

Fluphenazine decanoate: Within 24–72 hours.a b

Duration

Fluphenazine hydrochloride: 6–8 hours following oral or IM administration.a

Fluphenazine decanoate: Usually 1–6 weeks (average: 2 weeks).a

Distribution

Extent

Not fully elucidated; reportedly crosses blood-brain barrier.a

Phenothiazines cross the placenta and are distributed into milk.e o

Elimination

Metabolism

Metabolic fate not fully elucidated.a

Elimination Route

Excreted in feces and urine as unchanged drug, fluphenazine sulfoxide, and 7-hydroxyfluphenazine following IM administration of fluphenazine decanoate in 1 patient studied; also excreted in urine as metabolite conjugates.a

Half-life

Fluphenazine hydrochloride: 14.7–15.3 hours following IM or oral administration.a

Fluphenazine decanoate: 6.8–9.6 days following IM administration.a

Advice to Patients

  • Importance of advising patients and caregivers that geriatric patients with dementia-related psychosis treated with antipsychotic agents are at an increased risk of death.100 101 102 103 c f g i Importance of informing patients and caregivers that fluphenazine is not approved for treating geriatric patients with dementia-related psychosis.100 101 c f g i

  • Importance of informing patients and caregivers about the risk of NMS, which can cause high fever, stiff muscles, sweating, fast or irregular heart beat, change in BP, confusion, and kidney damage.b c f g i

  • Risk of drowsiness and impairment of mental and physical abilities required for driving a car or operating heavy machinery.a b c f g i

  • Importance of avoiding alcohol during fluphenazine therapy.a b c f g i

  • Importance of informing patients in whom chronic fluphenazine use is contemplated of risk of tardive dyskinesia, taking into account clinical circumstances and competency of patient to understand information provided.b c f g i

  • Importance of clinicians informing patients of risk of extrapyramidal reactions and providing reassurance that these reactions usually can be controlled by administration of antiparkinsonian drugs (e.g., benztropine) and by subsequent dosage reduction.b c f g i

  • Risk of leukopenia/neutropenia.b c f g i Importance of advising patients with a preexisting low WBC count or history of drug-induced leukopenia/neutropenia that their CBC count should be monitored during fluphenazine therapy.b c f g i

  • Importance of informing clinician if sore throat or other signs of infection occur.b c f g i

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses (e.g., cardiovascular disease, seizures).a b c f g i

  • Importance of avoiding exposure to temperature extremes.b c d f g i

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.a b c f g i o Importance of clinicians informing patients about the benefits and risks of taking antipsychotics during pregnancy (see Pregnancy under Cautions).b c f g i o Importance of advising patients not to stop taking fluphenazine if they become pregnant without consulting their clinician; abruptly stopping antipsychotic agents may cause complications.o

  • Importance of informing patients of other important precautionary information.b c f g i (See Cautions.)

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