Fluphenazine information from DrugsUpdate
P - Contraindicated in pregnancy
L - Contraindicated in lactation
Fluphenazine is a typical antipsychotic drug used for the treatment of psychoses such as schizophrenia and acute manic phases of bipolar disorder. It belongs to the piperazine class of phenothiazines and is extremely potent; more potent than haloperidol and around fifty to seventy times the potency of chlorpromazine. It is marketed under the brand name of Prolixin and Sydocate(Surge Laboratories.)
Its main use is as a long acting injection given once every two or three weeks to people with schizophrenia who have a poor compliance with medication and suffer frequent relapses of illness. In some countries this can be involuntary under Community Treatment Orders. Its side effect profile is similar to haloperidol, namely predominantly dopamine-blocking effects which give rise to akathisia, parkinsonism and tremor. Long term side effects include the potentially irreversible tardive dyskinesia and the potentially fatal neuroleptic malignant syndrome.
Pharmacodynamics
Pharmacokinetics
Fluphenazine blocks postsynaptic dopamine D1 and D2 receptors in the mesolimbic system and decreases the release of hypothalamic and hypophyseal hormones. It reduces aggressiveness with disappearance of hallucinations and delusions.
Onset
1-3 days.
Duration
2-4 days.
Absorption
Absorbed as HCl from the GI tract (oral); slowly absorbed as decanoate and enantate (SC/IM).
Distribution
Crosses the placenta; enters breast milk. Protein-binding: 91-99%.
Metabolism
Hepatic.
Excretion
Urine (as metabolites); 14.7 hours (elimination half-life).
Fluphenazine Indications / Fluphenazine Uses
Information Not Available
Fluphenazine Adverse Reactions / Fluphenazine Side Effects
Tardive dyskinesia, sedation, mental confusion; hypotension; hyperprolactinaemia leading to galactorrhoea and amenorrhoea in women; loss of libido, impotence and sterility in males. Allergic reactions, cholestatic jaundice, corneal and lens deposits, skin pigmentation.
Potentially Fatal: Agranulocytosis; neuroleptic malignant syndrome.
Precautions
Monitor
Frequently assess patient for response to treatment. Periodically review therapy to determine if it needs to be continued without change or if a dose change is indicated.
Special Precautions
Presence of convulsive disorders; hepatic, renal, cerebrovascular, resp and CV diseases; elderly or debilitated patients. May elevate prolactin levels which may persist after chronic admin. May exacerbate depression. Closed-angle glaucoma. History of jaundice, parkinsonism, DM, hypothyroidism, myasthenia gravis, paralytic ileus, prostatic hyperplasia or urinary retention. Regular eye examinations in patients receiving long term therapy. Avoid direct sunlight exposure.
Other Drug Interactions
Reduces antihypertensive effects of guanethidine, methyldopa and clonidine. Lithium toxicity. Reduced bioavailability with antacids. Increased risk of arrhythmia when used with drugs that prolong QT interval. May cause electrolyte disturbance when used with diuretics.
Potentially Fatal: Additive CNS depressant effects with alcohol, barbiturates, hypnotics, sedatives, opiates and antihistamines.
Other Interactions
Information Not Available
Dosage
Oral
Psychoses
Adult: Initially, 2.5-10 mg daily in 2-3 divided doses, increased according to reponse. Maintenance: 1-5 mg daily.
Max Dosage: Adult: 20 mg/day. Elderly: 10 mg/day.
Oral
Mania
Adult: Initially, 2.5-10 mg daily in 2-3 divided doses, increased according to reponse. Maintenance: 1-5 mg daily.
Max Dosage: Adult: 20 mg/day. Elderly: 10 mg/day.
Oral
Schizophrenia
Adult: Initially, 2.5-10 mg daily in 2-3 divided doses, increased according to reponse. Maintenance: 1-5 mg daily.
Max Dosage: Adult: 20 mg/day. Elderly: 10 mg/day.
Oral
Short-term adjunct in severe anxiety or behavioral disturbances
Adult: 1 mg bid increased to 2 mg bid if necessary.
Intramuscular
Psychoses
Adult: As decanoate: Initially, 12.5 mg adjusted according to response. Maintenance: 12.5-100 mg at intervals of 2-6 weeks. For doses >50 mg, increments should be made slowly in steps of 12.5 mg. The enantate ester can be given in similar doses at intervals of 1-3 weeks.
Elderly: 6.25 mg adjusted according to response.
Intramuscular
Mania
Adult: As decanoate: Initially, 12.5 mg adjusted according to response. Maintenance: 12.5-100 mg at intervals of 2-6 wk. For doses >50 mg, increments should be made slowly in steps of 12.5 mg. The enantate ester can be given in similar doses at intervals of 1-3 weeks.
Elderly: 6.25 mg adjusted according to response.
Intramuscular
Schizophrenia
Adult: As decanoate: Initially, 12.5 mg adjusted according to response. Maintenance: 12.5-100 mg at intervals of 2-6 wk. For doses >50 mg, increments should be made slowly in steps of 12.5 mg. The enantate ester can be given in similar doses at intervals of 1-3 weeks.
Elderly: 6.25 mg adjusted according to response.
Food(before/after)
May be taken with or without food.
List of Contraindications
Fluphenazine and Pregnancy
Contraindicated in pregnancy
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Fluphenazine and Lactation
Contraindicated in lactation
Fluphenazine and Children
Safety and efficacy not established.
Fluphenazine and Geriatic
More susceptible to effects; consider reduced dose.
Fluphenazine and Other Contraindications
Hypersensitivity; comatose or severely depressed states; blood dyscrasias; liver disease; bone marrow depression; phaeochromocytoma; suspected or established subcortical brain damage with or without hypothalamic damage; pregnancy (3rd trimester), lactation.
Storage
Intramuscular
Store at 15-30°C.
Oral
Store at 15-30°C.
Lab interference
Intramuscular
Store at 15-30°C.
Oral
Store at 15-30°C.
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