Fluphenazine, a first-generation antipsychotic drug, was introduced in 1959 to treat symptomatic psychosis in schizophrenia patients. Fluphenazine is not approved for enhancing mood stabilization or treating concomitant psychotic symptoms in bipolar disorder patients. These drugs are frequently prescribed off-label for psychosis or psychotic symptoms associated with a major neurocognitive disorder; however, all antipsychotics and related dementia medications are not FDA-approved. The use of this fluphenazine, like that of many other first-generation drugs, has decreased as a result of improved side effect profiles and increased efficacy of second-generation drugs.
BRAND NAMES:
Prolixin – It consists of fluphenazine hydrochloride as the major active ingredient with strengths 5 and 10mg and is available in the form of tablets.
Modecate – These are available as injections, such as modecate injection 25mg /ml and modecate injection 100mg/ml which contain the active ingredient fluphenazine decanoate.
MECHANISM OF ACTION :
Fluphenazine primarily inhibits postsynaptic dopamine-2 - 2 receptors in mesolimbic, tuberoinfundibular, and nigrostriatal neutral pathways. Positive symptoms in schizophrenia, such as hallucinations, delusions, and disorganized speech, are targeted by blocking postsynaptic dopamine-2 receptors in the mesolimbic pathway. It also has a strong antagonistic effect on both muscarinic -1 and histamine-1 receptors. It belongs to the class of phenothiazine-derived neuroleptic antipsychotics, which also includes thioridazine and chlorpromazine.
PHARMACODYNAMICS:
Fluphenazine was ineffective in treating behavioral complications in patients with mental retardation. It is a trifluoromethyl phenothiazine derivative used to treat schizophrenia and other psychotic disorders.
DOSAGE AND ADMINISTRATION:
It is available as oral tablets, intramuscular injections, and long-acting or subcutaneous injections. Different types of dosage forms are available in the market, depending upon the patient's conditions and the dose that will be prescribed. Oral dosing ranges from 1 to 40mg and 1mg,2.5mg, 5mg, and 10mg tablets are available.
• In elder patients the oral dose starts from 1 to 2.5mg per day divided every 6 to 8 hours. 2.5 to 10mg per day is also recommended based on the patient's condition.
• Intramuscular formulation for acute administration starts from a 1.25mg s initial dose and ranges from 2.5mg to 10mg once a day. It is generally administered in patients with acute agitation with psychosis.
• Intramuscular or subcutaneous formulation is Initially, the dose starts from 12.5mg to 25mg.
• Fluphenazine dose should range more than 40mg per day.
CONTRAINDICATIONS:
Fluphenazine is contraindicated in patients with hepatobiliary disease or hepatic insufficiency, as it can precipitate or worsen cholestatic jaundice. It also should be avoided during pregnancy, lactation, and breastfeeding.
DRUG INTERACTIONS:
Some drugs used along with fluphenazine may cause serious side effects. When fluphenazine interacts with other medications, the actual mechanism of the fluphenazine may decrease. So before using fluphenazine, it is necessary to discuss with the doctor the drugs that are already used for other treatments. Based on the patient's conditions, they might decrease the dosage of fluphenazine to decrease the side effects when interacting with other drugs.
The drugs mentioned below should be avoided using with fluphenazine.
• Medications used for blood pressure
• Depression medications like fluoxetine, sertraline, and amitriptyline.
• Antihistamines
• Narcotic medicines
• Seizure-related drugs like primidone, phenobarbital, phenytoin
• Muscle relaxant medications for surgery
• Levodopa for Parkinson's disease
• Atripoin
• Bladder problem-related drugs like tolterodine, oxybutynin
• Medicines for anxiety
• Epinephrine
• Pimozide
• Cisapride
• Thioridazine
• Saquinavir
• Metoclopramide
• Dronedarone
• Lithium
• Stomach problem medications like dicyclomine, hyoscyamine
• General anesthetic medications like halothane, propofol, isoflurane, and methoxyflurane
FOOD INTERACTIONS:
Avoid consuming alcohol and take with food can reduce irritation.
ADVERSE EFFECTS:
• Blurred vision
• Dizziness
• Frequent urination
• Constipation
• Excessive sweating
• Dry mouth
• Insomnia
• Nightmares
• Skin sensitivity when exposed to sunlight than usual
• Weakness
• Stomach upset
• Trouble in keeping balance
• Sudden changes in weight and appetite
• Jaundice
• Seizures
• Gynecomastia in men
• Amenorrhea
TOXICITY:
If the person has taken the overdose then prescribed it leads to some toxic effects
• Collapsed
• Seizures
• Trouble in breathing
• Trouble to wake
STORAGE:
Store the medication at room temperature, away from direct sunlight and moisture. Store medication in a firmly closed container.
