Perphenazine: Difference between revisions

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{{drugbox |
{{DrugProjectFormSinglePage
| IUPAC_name = 2-[4-[3-(2-chloro-10H-phenothiazin-10-yl) propyl]piperazin-1-yl]ethanol
|authorTag=
| image = Perphenazine2d.png
 
| CAS_number = 58-39-9
 
| ATC_prefix = N05
<!--Overview-->
| ATC_suffix = AB03
 
| PubChem = 4748
|genericName=
| DrugBank = APRD00429
 
| C=21 | H=26 | Cl=1 | N=3 | O=1 | S=1
 
| molecular_weight = 403.97
 
| bioavailability = 40%
|aOrAn=
| metabolism = hepatic
 
| elimination_half-life = 8-12 (up to 20) hours
a
| excretion = biliar
 
| pregnancy_category = Only, if clearly needed (hyperemesis gravidarum)
|drugClass=
| legal_status = RX-medication-only
 
| routes_of_administration = oral and i.m.
 
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<!--FDA-Labeled Indications and Dosage (Pediatric)-->
 
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=====Endocrine=====
 
 
 
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===Acute Overdose===
 
====Signs and Symptoms====
 
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: [[File:{{PAGENAME}}01.png|thumb|none|600px|This image is provided by the National Library of Medicine.]]
 
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There is limited information regarding <i>Pharmacokinetics</i> of {{PAGENAME}} in the drug label.
 
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<!--How Supplied-->


'''Perphenazine''' is a [[typical antipsychotic]] [[psychoactive drug|drug]].  Chemically, it is classified as a piperazinyl [[phenothiazine]]. It has been in clinical use for decades.
|howSupplied=


Perphenazine is 10 to 15 times as potent as [[chlorpromazine]]; 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-effect]]s compared to [[haloperidol]].
*


==Pharmacokinetics==
<!--Patient Counseling Information-->
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]] and [[hypotension]] without loss of therapeutic activity. It has a high incidence of early and late [[extrapyramidal side-effect]]s ([[tardive dyskinesia]]).


==Uses==
|fdaPatientInfo=
Perphenazine is a highly potent typical neuroleptic for the treatment of psychotic patients (e.g. patients with [[schizophrenia]]) and for patients presenting with [[manic]] phases of [[bipolar disorder]].


In low doses it may be used to treat [[clinical depression|agitated depressive]] patients (together with an [[antidepressant]]). Fixed combinations of perphenazine and the [[tricyclic antidepressant]] [[amitriptyline]] 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]] (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]] action of perphenazine attenuates the fluoxetine-induced [[nausea]]/[[emesis]], as well as the initial agitation caused by Fluoxetine. Both actions can be helpful for many patients.  
There is limited information regarding <i>Patient Counseling Information</i> of {{PAGENAME}} in the drug label.


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]]). The short-time therapy of nausea/emesis and [[Vertigo (medical)|vertigo]] due to different reasons is another short-time-indication (days to weeks).
<!--Precautions with Alcohol-->


Perphenazine also has sedating and [[anxiolytic]] 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]], 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]] and correction of [[electrolyte]]s/fluids in the body.
|alcohol=


A valuable off-label indication is the short-time treatment of [[hyperemesis gravidarum]]; 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.
* Alcohol-{{PAGENAME}} interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.


==Side effects==
<!--Brand Names-->
As a member of the [[phenothiazine]] type of neuroleptics, perphenazine shares in general all allergic and toxic side-effects of [[chlorpromazine]]. It seems to have a lower incidence of allergic skin reactions, [[cholestatic]] [[liver]] damage and [[leukopenia]] compared to chlorpromazine. Likewise, the propensity for weight gain is lower and the risk of [[insulin resistance]] is smaller. Ocular and retinal damage to eyes has so far not been reported, but precipitation of [[glaucoma|closed angle glaucoma]] is possible.


As with other highly potent typical drugs, the suppression of [[schizophrenia|positive symptom]]s (agitation, [[Paranoia|paranoid]] ideation, [[hallucination]]s and [[delusion]]s) is far more pronounced than the improvement of [[schizophrenia|negative symptom]]s (emotional and social withdrawal etc.)
|brandNames=


When used for its strong [[antiemetic]] or [[antivertignosic]] effects in cases with associated brain injuries, it may obscure the clinical course and interferes with the diagnosis.
* ®<ref>{{Cite web | title =  | url =  }}</ref>


==Formulations==
<!--Look-Alike Drug Names-->
It sold under the brand names Trilafon® and Etrafon® (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.   
|lookAlike=


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]] 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.
* A® — B®<ref name="www.ismp.org">{{Cite web  | last =  | first =  | title = http://www.ismp.org | url = http://www.ismp.org | publisher =  | date =  }}</ref>


==Interactions==
<!--Drug Shortage Status-->
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.
|drugShortage=
}}


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.
<!--Pill Image-->


In general, all [[neuroleptic]]s may lead to seizures in combination with the opioid tramadol (Ultram®).
{{PillImage
|fileName=No image.jpg|This image is provided by the National Library of Medicine.
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Perphenazine may increase the [[insulin]] needs of [[diabetic]] patients. Monitor [[blood glucose level]]s of insulin-dependent patients regularly during long-term treatment.
<!--Label Display Image-->


{{Antipsychotics}}
{{LabelImage
|fileName={{PAGENAME}}11.png|This image is provided by the National Library of Medicine.
}}
 
{{LabelImage
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[[Category:Phenothiazines]]
<!--Category-->
[[Category:Typical antipsychotics]]
[[Category:Piperazines]]


[[pl:Perfenazyna]]
[[Category:Drug]]
[[ru:Перфеназин]]
[[sv:Perfenazin]]

Revision as of 15:27, 21 January 2015

Perphenazine
Black Box Warning
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1];

Disclaimer

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Black Box Warning

Title
See full prescribing information for complete Boxed Warning.
ConditionName:
  • Content

Overview

Perphenazine is a that is FDA approved for the {{{indicationType}}} of . There is a Black Box Warning for this drug as shown here. Common adverse reactions include .

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Condition1
  • Dosing Information
  • Dosage
Condition2
  • Dosing Information
  • Dosage
Condition3
  • Dosing Information
  • Dosage
Condition4
  • Dosing Information
  • Dosage

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

Condition1
  • Developed by:
  • Class of Recommendation:
  • Strength of Evidence:
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Guideline-Supported Use of Perphenazine in adult patients.

Non–Guideline-Supported Use

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Non–Guideline-Supported Use of Perphenazine in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding FDA-Labeled Use of Perphenazine in pediatric patients.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

Condition1
  • Developed by:
  • Class of Recommendation:
  • Strength of Evidence:
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Guideline-Supported Use of Perphenazine in pediatric patients.

Non–Guideline-Supported Use

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Non–Guideline-Supported Use of Perphenazine in pediatric patients.

Contraindications

  • Condition1

Warnings

Title
See full prescribing information for complete Boxed Warning.
ConditionName:
  • Content
  • Description

Precautions

  • Description

Adverse Reactions

Clinical Trials Experience

There is limited information regarding Clinical Trial Experience of Perphenazine in the drug label.

Body as a Whole
Cardiovascular
Digestive
Endocrine
Hematologic and Lymphatic
Metabolic and Nutritional
Musculoskeletal
Neurologic
Respiratory
Skin and Hypersensitivy Reactions
Special Senses
Urogenital
Miscellaneous

Postmarketing Experience

There is limited information regarding Postmarketing Experience of Perphenazine in the drug label.

Body as a Whole
Cardiovascular
Digestive
Endocrine
Hematologic and Lymphatic
Metabolic and Nutritional
Musculoskeletal
Neurologic
Respiratory
Skin and Hypersensitivy Reactions
Special Senses
Urogenital
Miscellaneous

Drug Interactions

  • Drug
  • Description

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA):

  • Pregnancy Category


Pregnancy Category (AUS):

  • Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Perphenazine in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Perphenazine during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Perphenazine with respect to nursing mothers.

Pediatric Use

There is no FDA guidance on the use of Perphenazine with respect to pediatric patients.

Geriatic Use

There is no FDA guidance on the use of Perphenazine with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Perphenazine with respect to specific gender populations.

Race

There is no FDA guidance on the use of Perphenazine with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Perphenazine in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Perphenazine in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Perphenazine in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Perphenazine in patients who are immunocompromised.

Administration and Monitoring

Administration

  • Oral
  • Intravenous

Monitoring

There is limited information regarding Monitoring of Perphenazine in the drug label.

  • Description

IV Compatibility

There is limited information regarding IV Compatibility of Perphenazine in the drug label.

Overdosage

Acute Overdose

Signs and Symptoms

  • Description

Management

  • Description

Chronic Overdose

There is limited information regarding Chronic Overdose of Perphenazine in the drug label.

Pharmacology

There is limited information regarding Perphenazine Pharmacology in the drug label.

Mechanism of Action

Structure

This image is provided by the National Library of Medicine.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Perphenazine in the drug label.

Pharmacokinetics

There is limited information regarding Pharmacokinetics of Perphenazine in the drug label.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of Perphenazine in the drug label.

Clinical Studies

There is limited information regarding Clinical Studies of Perphenazine in the drug label.

How Supplied

Storage

There is limited information regarding Perphenazine Storage in the drug label.

Images

Drug Images

{{#ask: Page Name::Perphenazine |?Pill Name |?Drug Name |?Pill Ingred |?Pill Imprint |?Pill Dosage |?Pill Color |?Pill Shape |?Pill Size (mm) |?Pill Scoring |?NDC |?Drug Author |format=template |template=DrugPageImages |mainlabel=- |sort=Pill Name }}

Package and Label Display Panel

{{#ask: Label Page::Perphenazine |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}

Patient Counseling Information

There is limited information regarding Patient Counseling Information of Perphenazine in the drug label.

Precautions with Alcohol

  • Alcohol-Perphenazine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

Look-Alike Drug Names

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

  1. Empty citation (help)
  2. "http://www.ismp.org". External link in |title= (help)


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