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fluphenazine (Modecate, Modecate Concentrate, Moditen, Prolixin, RhoFluphenazine)

 

Classes: Antipsychotics, 1st Generation; Antipsychotics, Phenothiazine

Dosing and uses of Modecate, Modecate Concentrate (fluphenazine)

 

Adult dosage forms and strengths

tablet

  • 1mg
  • 2.5mg
  • 5mg
  • 10mg

elixir

  • 2.5mg/5mL

oral concentrate

  • 5mg/mL

injectable solution

  • 2.5mg/mL (fluphenazine hydrochloride)
  • 25mg/mL (fluphenazine decanoate)

 

Psychotic Disorders

Fluphenazine hydrochloride

  • 2.5-10 mg/day PO divided q6-8hr initially; maintenance: 1-5 mg PO/IM divided q6-8hr; not to exceed 40 mg/day

Fluphenazine decanoate

  • 12.5-25 mg (25 mg/mL) IM/SC every 2-4 weeks

Dosing considerations

  • Conversion from hydrochloride salt to decanoate: 10 mg/day PO HCl salt = ~12.5 mg IM/SC every 3 weeks of decanoate salt

 

Dosing Modifications

Renal impairment: Use with caution; monitor

Hepatic impairment: Use with caution; monitor

 

Pediatric dosage forms and strengths

Safety and efficacy not established

 

Geriatric dosage forms and strengths

1-2.5 mg/day PO; dosage titrated according to response

 

Modecate, Modecate Concentrate (fluphenazine) adverse (side) effects

Frequency not defined

Confusion

Decreased gag reflex

Extrapyramidal symptoms

  • Akathisia
  • Dystonia
  • Dyskinesia
  • Muscle stiffness
  • Neuroleptic malignant syndrome (NMS; infrequent but serious)
  • Parkinsonism
  • Tardive dyskinesia

Common

  • Anticholinergic effects
  • Sedation
  • Weight gain
  • Erectile dysfunction
  • Oligomenorrhea or amenorrhea

Less common

  • Orthostatic hypotension (after IM injection), tachycardia
  • Agitation, anxiety, cerebral edema, depression, dizziness, euphoria, headache, poikilothermia, restlessness, weakness
  • Anorexia, constipation, dyspepsia, ileus
  • Lens opacities (with prolonged use)

Uncommon

  • ECG changes
  • Photosensitivity
  • Pruritus
  • Diarrhea
  • Blood dyscrasia
  • Galactorrhea
  • Ejaculatory disorder

Rare

  • Seizure
  • Priapism
  • Cholestatic jaundice

 

Warnings

Black box warnings

Patients with dementia-related psychosis who are treated with antipsychotic drugs are at increased risk for death, as shown in short-term controlled trials; deaths in these trials appeared to be either cardiovascular (eg, heart failure, sudden death) or infectious (eg, pneumonia) in nature

This drug is not approved for treatment of patients with dementia-related psychosis

 

Contraindications

Documented hypersensitivity

Coma, severe hypotension, severe central nervous system (CNS) depression, concurrent use of large amounts of CNS depressants, subcortical brain damage, poorly controlled seizure disorder, blood dyscrasias, severe cardiovascular disease

Narrow-angle glaucoma

Lactation

 

Cautions

Glaucoma, prostatic hypertrophy, stenosing peptic ulcer disease (PUD), history of NMS, Parkinson disease, hypocalcemia, renal or hepatic impairment, history of severe reaction to insulin or electroconvulsive therapy (ECT), history of seizures, asthma, respiratory tract infections, cardiovascular disease

Mild leukocytosis, leukopenia, and eosinophilia occasionally occur

Dermatologic reactions are common

Watch for urinary retention, blurred vision, dry mouth, and constipation as result of anticholinergic effects

Risk of extrapyramidal symptoms (EPS), NMS, hypotension; hypotension may be particularly severe in patients with pheochromocytoma or mitral insufficiency 

May need anticholinergic antiparkinsonian agent to counter EPS; in case of severe hypotension, use norepinephrine or phenylepinephrine, and do not use epinephrine or dopamine

Depresses hypothalamic thermoregulatory mechanism; exposure to extreme temperatures may cause hypo- or hyperthermia

US Food and Drug Administration (FDA) warning regarding off-label use for dementia in elderly

 

Pregnancy and lactation

Pregnancy category: C

Lactation: Drug enters breast milk; not recommended

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Modecate, Modecate Concentrate (fluphenazine)

Mechanism of action

Phenothiazine; antagonizes dopaminergic D1 and D2 receptors; depresses release of hypothalamic and hypophyseal hormones

 

Absorption

Bioavailability: Rapidly absorbed

Onset: Hydrochloride salt, 1 hr; decanoate, 24-72 hr

Duration: Hydrochloride salt, 6-8 hr; decanoate, 4 weeks

Peak plasma time: Hydrochloride salt, 2 hr; decanoate, 8-10 hr

Peak effect: Decanoate, 48-96 hr

 

Elimination

Half-life: Hydrochloride salt, 14-16 hr; decanoate, 14 days

Excretion: Urine, feces