Perphenazine

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Perphenazine

Perphenazine is a typical antipsychotic

Typical antipsychotic

Typical antipsychotics are a class of antipsychotic drugs first developed in the 1950s and used to treat psychosis , and are generally being replaced by atypical antipsychotic drugs....
drug

Psychoactive drug

A psychoactive drug or psychotropic substance is a chemical substance that acts primarily upon the central nervous system where it alters brain function, resulting in temporary changes in perception, mood , consciousness and behaviour....
. Chemically, it is classified as a piperazinyl phenothiazine

Phenothiazine

Phenothiazine is the organic compound with the formula S2NH. This yellow tricyclic compound is soluble in acetic acid, benzene, and ether....
. It has been in clinical use for decades.

Perphenazine is 10 to 15 times as potent as chlorpromazine

Chlorpromazine

Chlorpromazine is a phenothiazine antipsychotic, and the oldest in the antipsychotic family of drugs. It is a typical antipsychotic. It is principally used in the treatment of schizophrenia, though it has also been used to treat severe manic episodes in people with bipolar disorder....
; thus perphenazine is considered a highly potent antipsychotic. In equivalent doses it has approximately the same frequency and severity of early and late extrapyramidal side-effects

Extrapyramidal system

In human anatomy, the extrapyramidal system is a neural network located in the human brain that is part of the motor system involved in the coordination of movement....
as haloperidol

Haloperidol

Haloperidol is a typical antipsychotic. It is in the butyrophenone class of antipsychotic medications and has pharmacology similar to the phenothiazines....
.

as an oral bioavailability of approximately 40% and a half-life of 8 to 12 hours (up to 20 hours), and is usually given in 2 or 3 divided doses each day.

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Encyclopedia

Perphenazine is a typical antipsychotic

Typical antipsychotic

Typical antipsychotics are a class of antipsychotic drugs first developed in the 1950s and used to treat psychosis , and are generally being replaced by atypical antipsychotic drugs....
drug

Psychoactive drug

Phenothiazine

Chlorpromazine

Extrapyramidal system

In human anatomy, the extrapyramidal system is a neural network located in the human brain that is part of the motor system involved in the coordination of movement....
as haloperidol

Haloperidol

Haloperidol is a typical antipsychotic. It is in the butyrophenone class of antipsychotic medications and has pharmacology similar to the phenothiazines....
.

Pharmacokinetics

It has an oral bioavailability of approximately 40% and a half-life of 8 to 12 hours (up to 20 hours), and is usually given in 2 or 3 divided doses each day. It is possible to give two-thirds of the daily dose at bedtime and one-third during breakfast to maximize hypnotic activity during the night and to minimize daytime sedation

Sedation

Sedation is a medical procedure involving the administration of sedative drugs, generally to facilitate a medical procedure with local anaesthesia....
and hypotension

Hypotension

In physiology and medicine, hypotension refers to an abnormally low blood pressure. This is best understood as a physiologic state, rather than a disease....
without loss of therapeutic activity. It has a high incidence of early and late extrapyramidal side-effects and tardive dyskinesia

Tardive dyskinesia

Tardive dyskinesia is a variety of Dyskinesia manifesting as a side effect of long-term or high-dose use of dopamine antagonists, usually antipsychotics....
.

Uses

Perphenazine is a highly potent typical neuroleptic for the treatment of psychotic patients (e.g. patients with schizophrenia

Schizophrenia

Schizophrenia , from the Ancient Greek Root schizein and phren, phren- is a psychiatry diagnosis that describes a mental disorder characterized by abnormalities in the perception or expression of reality....
) and for patients presenting with manic

Manic

Manic is a List of Belgrade neighborhoods of Belgrade, the capital of Serbia. It is located in the municipality of Barajevo.Manic developed on the eastern slopes of the Kosmaj mountain....
phases of bipolar disorder

Bipolar disorder

Bipolar disorder is a Classification of mental disorders that describes a category of mood disorders, or mood swings, defined by the presence of one or more episodes of abnormally elevated mood clinically referred to as mania or, if milder, hypomania....
.

In low doses it may be used to treat agitated depressive

Clinical depression

Major depressive disorder is a mental disorder characterized by a pervasive depression , low self-esteem, and anhedonia in normally enjoyable activities....
patients (together with an antidepressant

Antidepressant

An antidepressant is a psychiatric medication used for alleviating major depressive disorder or dysthymia. Drug groups known as MAOIs, tricyclics, and second-generation antidepressants such as SSRIs, and serotonin-norepinephrine reuptake inhibitors are particularly associated with the term....
). Fixed combinations of perphenazine and the tricyclic antidepressant

Tricyclic antidepressant

Tricyclic antidepressants are a class of antidepressant Medications first used in the 1950s. They are named after the drugs' molecular structure, which contains three rings of atoms ....
amitriptyline

Amitriptyline

Amitriptyline hydrochloride is a tricyclic antidepressant Medication. It is a white, odorless, crystalline compound which is freely soluble in water; it is usually dispensed in tablet form....
in different proportions of weight exist (see Etrafon below). Such combinations should never be used indiscriminately. When treating depression, perphenazine should be discontinued as fast as the clinical situation allows. Perphenazine has no intrinsic antidepressive activity. There are studies that the use of perphenazine together with fluoxetine

Fluoxetine

Fluoxetine hydrochloride is an antidepressant of the selective serotonin reuptake inhibitor class. Fluoxetine is approved for the treatment of major depressive disorder , obsessive-compulsive disorder , bulimia nervosa, anorexia nervosa, panic disorder and premenstrual dysphoric disorder....
(Prozac) in patients with psychotic depression is most promising, although fluoxetine interferes with the metabolism of perphenazine, causing higher plasma levels of perphenazine and a longer half life. In this combination the strong antiemetic

Antiemetic

An antiemetic is a medication that is effective against vomiting and nausea. Anti-emetics are typically used to treat motion sickness and the Adverse effect of opioid analgesics, general anaesthetics and chemotherapy directed against cancer....
action of perphenazine attenuates the fluoxetine-induced nausea

Nausea

Nausea is the sensation of unease and discomfort in the stomach with an urge to vomit....
/emesis, as well as the initial agitation caused by Fluoxetine. Both actions can be helpful for many patients.

Perphenazine has been used in low doses as a 'normal' or 'minor' tranquilizer in patients with a known history of addiction to drugs or alcohol, a practice which is now strongly discouraged (preferably an antidepressive drug such as doxepin

Doxepin

Doxepin is a psychoactive drug with tricyclic antidepressant and anxiolytic properties, known under many brand-names such as Aponal, the original preparation by Boehringer-Mannheim, now part of the Hoffmann-La Roche group; Adapine, Deptran, Sinquan and Sinequan ....
). The short-time therapy of nausea/emesis and vertigo

Vertigo (medical)

Vertigo is a specific type of dizziness, a major symptom of a balance disorder. It is the sensation of spinning or swaying while the body is actually stationary with respect to the surroundings....
due to different reasons is another short-time-indication (days to weeks).

Perphenazine also has sedating and anxiolytic

Anxiolytic

An anxiolytic is a Medication prescribed for the treatment of symptoms of anxiety. Some anxiolytics have been shown to be useful in the treatment of anxiety disorders as have antidepressants such as the class of selective serotonin reuptake inhibitors ....
properties making the drug particularly useful for the treatment of agitated psychotic patients and, in high doses (up to 100 mg per day), for patients with life-threatening (febrile) catatonia

Catatonia

Catatonia is a syndrome of psychic and motoric disturbances. Karl Ludwig Kahlbaum first described it in 1874: Die Katatonie oder das Spannungirresein ....
, a state in which the patient is extremely agitated, but is not able to express him-/herself. In this situation perphenazine may be used together with electroconvulsive therapy

Electroconvulsive therapy

Electroconvulsive therapy , also known as electroshock, is a well established, albeit controversial psychiatry treatment in which seizures are electrically induced in anesthetized patients for therapeutic effect....
and correction of electrolyte

Electrolyte

An electrolyte is any substance containing free ions that behaves as an electrical conductor medium. Because they generally consist of ions in solution, electrolytes are also known as ionic solutions, but molten electrolytes and solid electrolytes are also possible....
s/fluids in the body.

A valuable off-label indication is the short-time treatment of hyperemesis gravidarum

Hyperemesis gravidarum

Hyperemesis gravidarum is a severe form of morning sickness, with unrelenting, excessive pregnancy-related nausea and/or vomiting that prevents adequate intake of food and fluids. Hyperemesis is considered a rare complication of pregnancy but, because nausea and vomiting during pregnancy exist on a continuum, there is often not a good d...
; a state in which pregnant women experience violent nausea and emesis. This problem can become severe enough to endanger the life of the unborn. As perphenazine has not been shown to be teratogenic and works very well, it is sometimes given orally in the least possible dose.

Side effects

As a member of the phenothiazine

Phenothiazine

Phenothiazine is the organic compound with the formula S2NH. This yellow tricyclic compound is soluble in acetic acid, benzene, and ether....
type of neuroleptics, perphenazine shares in general all allergic and toxic side-effects of chlorpromazine

Chlorpromazine

Chlorpromazine is a phenothiazine antipsychotic, and the oldest in the antipsychotic family of drugs. It is a typical antipsychotic. It is principally used in the treatment of schizophrenia, though it has also been used to treat severe manic episodes in people with bipolar disorder....
. It seems to have a lower incidence of allergic skin reactions, cholestatic liver

Liver

The liver is a vital organ present in vertebrates and some other animals; it has a wide range of functions, a few of which are detoxification, protein synthesis, and production of biochemicals necessary for digestion....
damage and leukopenia

Leukopenia

Leukopenia is a decrease in the number of circulating white blood cells in the blood. As the principal function of white cells is to combat infection, a decrease in the number of these cells can place patients at increased risk for infection....
compared to chlorpromazine. Likewise, the propensity for weight gain is lower and the risk of insulin resistance

Insulin resistance

Insulin resistance is the condition in which normal amounts of insulin are inadequate to produce a normal Insulin#Physiological_effects from fat, muscle and liver cell ....
is smaller. Ocular and retinal damage to eyes has so far not been reported, but precipitation of closed angle glaucoma

Glaucoma

Glaucoma is a group of diseases of the optic nerve involving loss of ganglion cell in a characteristic pattern of optic atrophy. Raised intraocular pressure is a significant risk factor for developing glaucoma ....
is possible.

As with other highly potent typical drugs, the suppression of positive symptom

Schizophrenia

Paranoia

Paranoia is a thought process characterized by excessive anxiety or fear, often to the point of irrationality and delusion. Paranoid thinking typically includes persecutory beliefs concerning a perceived threat towards oneself....
ideation, hallucination

Hallucination

A hallucination, in the broadest sense, is a perception in the absence of a stimulus . In a stricter sense, hallucinations are defined as perceptions in a conscious and awake state in the absence of external stimuli which have qualities of real perception, in that they are vivid, substantial, and located in external objective space....
s and delusion

Delusion

A delusion is commonly defined as a fixed false belief and is used in everyday language to describe a belief that is either false, fanciful or derived from deception....
s) is far more pronounced than the improvement of negative symptom

Schizophrenia

Antiemetic

An antiemetic is a medication that is effective against vomiting and nausea. Anti-emetics are typically used to treat motion sickness and the Adverse effect of opioid analgesics, general anaesthetics and chemotherapy directed against cancer....
or antivertignosic effects in cases with associated brain injuries, it may obscure the clinical course and interferes with the diagnosis.

Formulations

It is sold under the brand names Trilafon (single drug) and Etrafon/Triavail (contains fixed dosages of amitriptyline). A brand name in Europe is Decentan pointing to the fact that perphenazine is approximately 10-times more potent than chlorpromazine. Usual oral forms are tablets (2, 4, 8, 16 mg) and liquid concentrate (4 mg/ml).

The 'Perphenazine injectable USP' solution is intended for deep intramuscular (i.m.) injection, for patients who are not willing to take oral medication or if the patient is unable to swallow. Due to a better bioavailability of the injection, two-thirds of the original oral dose is sufficient. The incidence of hypotension, sedation and extrapyramidal side-effects may be higher compared to oral treatment. The i.m.-injections are appropriate for a few days, but oral treatment should start as soon as possible.

In many countries, depot forms of perphenazine exist (as perphenazine enanthate). One injection works for 1 to 4 weeks depending on the dose of the depot-injection. Depot-forms of perphenazine should not be used during the initial phase of treatment as the rare neuroleptic malignant syndrome

Neuroleptic malignant syndrome

Neuroleptic malignant syndrome is a life-threatening neurological disorder most often caused by an adverse reaction to antipsychotic. It generally presents with muscle rigidity, fever, autonomic instability and cognitive changes such as delirium, and is associated with elevated creatine phosphokinase ....
may become more severe and uncontrollable with this form. Extrapyramidal side-effects may be somewhat reduced due to constant plasma-levels during depot-therapy. Also, patient compliance is sure, as many patients do not take their oral mediaction, particularly if feeling better once improvement in psychosis is achieved.

Interactions

Fluoxetine causes higher plasma-levels and a longer half-life of perphenazine, therefore a dose reduction of perphenazine might be necessary.

Perphenazine intensifies the central depressive action of drugs with such activity (tranquilizers, barbiturates, narcotics, antihistaminics, OTC-antiemetics etc.). A dose reduction of perphenazine or the other drug may be necessary.

The antihelmintic drug piperazine may intensify extrapyramidal side-effects. Avoid the concomitant use. Also, neurotoxic side-effects of the antibiotic streptomycin as well as of other aminoglycosids on the VIII. Brain nerve my be masked due to the strong antivertignosic effect of perphenazine. Avoid the concomitant use, too.

In general, all neuroleptics may lead to seizures in combination with the opioid tramadol (Ultram).

Perphenazine may increase the insulin

Insulin

Insulin is a hormone with extensive effects on both metabolism and several other body systems . Insulin causes most of the body's cells to take up glucose from the blood , storing it as glycogen in the liver and muscle, and stops use of fat as an energy source....
needs of diabetic patients. Monitor blood glucose levels of insulin-dependent patients regularly during long-term treatment.