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fluphenazine (Prolixin, Anatensol, Triflumethazine, Calmansial, Modecate)
Tradenames: Permitil, Prolixin. (hydrochlorides) (fluphenazine hydrochloride, enanthate, decanoate)
Indications:
1) symptomatic management of psychiatric disorders
2) generally used in combination with anticholinergic agent, i.e. Cogentin
Contraindications:
1) narrow-angle glaucoma
2) bone marrow depression
3) severe liver or cardiac disease
4) cross-sensitivity to other phenothiazines may exist
Dosage:
1) 1.25 mg IM every 6-8 hours (observe for hypotension)
2) 1-2 mg PO every 6-8 hours
Tabs: 1, 2.5, 5, 10 mg.
Elixir: 2.5 mg/5 mL.
Prolixin decanoate 12.5-25 mg IM every 2-4 weeks.
Injection: (decanoate) 25 mg/mL (5 mL)
Avoid contact of oral solution or injection with skin.
Risk of contact dermatitis
Pharmacokinetics:
1) rapidly absorbed from the GI tract & from parenteral sites
2) onset of action for decanoate is within 24-72 hours
3) duration of action is 1-6 weeks
Adverse effects:
1) common (> 10%)
- extrapyramidal symptoms (very common)
- pseudoparkinsonism
- akathisia
- dystonias
- tardive dyskinesia
- 10-20% of patients on long term therapy
- generally irreversible
- hypotension & orthostatic hypotension
- pigmentary retinopathy
- constipation
- decreased sweating
- dizziness
- nasal congestion
2) less common (1-10%)
- difficulty urinating, photosensitivity, rash, changes in menstrual cycle, impotence, breast tenderness, weight gain, nausea/vomiting, stomach pain, trembling of fingers
3) uncommon (< 1%)
- agranulocytosis, leukopenia, priapism, neuroleptic malignant syndrome (rare), blue-gray discoloration of skin, galactorrhea impairment of temperature regulation, hepatotoxicity, cholestatic jaundice, lowering of seizure threshold, cornea & lens changes, pigmentary retinopathy
4) other
- low sedation, low anticholinergic, low orthostatic hypotension effects
- QT prolongation
- direct myocardial depression
Drug interactions:
1) see chlorpromazine
2) risk of QT prolongation & torsades de pointes with astemizole, terfenadine & cisapride
3) fluphenazine may inhibit metabolism of some beta-blockers
4) tricyclic antidepressants may inhibit metabolism of fluphenazine
Laboratory:
1) specimen:
a) plasma (heparin)
b) stable for at least 3 weeks at -20 degrees C
2) methods: GC, GC-MS, HPLC, RIA
3) interferences:
a) RIA: prochlorperazine, perphenazine, trifluoperazine, fluphenazine metabolites
b) fluphenazine may be displaced from protein-binding sites by plasticizers in collecting devices
4) labs with Loincs
- fluphenazine in specimen
- fluphenazine in blood/urine
- fluphenazine in gastric fluid
- fluphenazine in serum/plasma
- fluphenazine in urine
Mechanism of action:
- high potency dopamine D2 receptor antagonist.
Interactions
drug interactions
drug adverse effects (more general classes)
Related
benztropine (Cogentin)
chlorpromazine (Thorazine, Ormazine, Propaphenin, Sonazine, Chloractil)
General
antipsychotic agent
dopaminergic receptor antagonist
phenothiazine
Properties
MISC-INFO: elimination route LIVER
KIDNEY
1/2life 13-58 HOURS
therapeutic-range 0.2-4.0 NG/ML
protein-binding >99%
pregnancy-category ?
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Saunders Manual of Medical Practice, Rakel (ed),
WB Saunders, Philadelphia, 1996, pg 1147
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed.,
W.B. Saunders, 1995