Deepika vegiraju at 14:54, 23 January 2023

2023-01-23T14:54:39Z

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== '''What is Pimozide?''' ==

* Pimozide ('''Orap''') is '''an orally active antipsychotic agent of the diphenyl-butylpiperidine series''' used largely in the therapy of [[Tourette syndrome]].

[[File:Pimozide.svg|thumb|Pimozide]]

[[File:Pimozide molecule ball.png|thumb|Pimozide molecule ball]]

[[File:Pimozide molecule spacefill.png|thumb|Pimozide molecule spacefill]]

[[File:Pimozide2DACS.svg|thumb|Pimozide2DACS]]

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== '''What are the uses of this medicine?''' ==

* Pimozide ('''Orap''') is used for the suppression of motor and [[Phonic tic|phonic tics]] in patients with [[Tourette’s syndrome|Tourette’s Disorder]] who have failed to respond satisfactorily to standard treatment.

'''Limitations of use:'''
* Pimozide should only be used to treat people who cannot take other medications or who have taken other medications without good results.
* Pimozide Tablets,should be reserved for use in Tourette’s Disorder patients whose development and/or daily life function is severely compromised by the presence of motor and phonic tics.

== '''How does this medicine work?''' ==

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* Pimozide (pim' oh zide) is '''a diphenylbutylpiperidine derivative''' that differs structurally from the [[phenothiazines]] and appears to '''act by blocking dopamine type 2 (D2) receptors'''.
* '''Pimozide has other central and peripheral effects including anticholinergeric and alpha adrenergic blockade'''.
* Pimozide is indicated for the therapy of severe motor and verbal tics in patients with Tourette syndrome.
* It has also been used in therapy of [[schizophrenia]].

== '''Who Should Not Use this medicine ?''' ==

This medicine cannot be used:
* in the treatment of [[Simple tic|simple tics]] or tics other than those associated with Tourette’s Disorder.
* in patients taking drugs that may, themselves, cause motor and [[Phonic tic|phonic tics]] (e.g., [[pemoline]], [[methylphenidate]] and [[amphetamines]]).
* in patients with congenital [[long QT syndrome]], patients with a history of [[cardiac arrhythmias]], patients taking other drugs which prolong the QT interval.
* patients with known [[hypokalemia]] or [[hypomagnesemia]].
* in patients with severe toxic [[central nervous system depression]] or [[comatose]] states from any cause.
* in patients with [[hypersensitivity]] to it.
* in patients receiving the [[macrolide antibiotics]] clarithromycin, erythromycin, azithromycin,dirithromycin, and troleandomycin.
* in patients taking [[Celexa]] or [[Lexapro]].
* with paroxetine and other strong CYP 2D6 inhibitors.
* in patients taking [[sertraline]].
* in patients receiving the azole [[antifungal]] agents itraconazole and ketoconazole.
* in patients receiving [[Protease inhibitor|protease inhibitors]] such as ritonavir, saquinovir, indinavir, and nelfinavir.
* in patients receiving [[Nefazodone]].

== '''What drug interactions can this medicine cause?''' ==

* Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.
Be sure to mention any of the following:
* certain [[antibiotics]] including azithromycin (Zithromax, Z-Pak), clarithromycin (Biaxin), erythromycin (E.E.S., E-Mycin, Erythrocin), and moxifloxacin (Avelox)
* [[antifungals]] such as itraconazole (Sporanox) and ketoconazole (Nizoral)
* [[arsenic trioxide]] (Trisenox)
* [[dofetilide]] (Tikosyn)
* [[chlorpromazine]]
* [[dolasetron]] (Anzemet)
* [[droperidol]] (Inapsine)
* [[HIV-1 Protease Inhibitor ASC09|HIV protease inhibitors]] such as indinavir (Crixivan), nelfinavir (Viracept), saquinavir (Invirase), and ritonavir (Norvir, in Kaletra)
* medications for irregular heartbeat such as amiodarone (Cordarone), disopyramide (Norpace), procainamide, quinidine, and sotalol (Betapace) medications for mental illness and nausea
* [[mefloquine]] (Lariam)
* [[nefazadone]]
* [[pentamidine]] (Nebu-Pent)
* certain [[selective serotonin reuptake inhibitors]] (SSRIs) such as citalopram (Celexa), escitalopram (Lexapro), fluoxetine (Prozac, Sarafem), fluvoxamine (Luvox), paroxetine (Paxil, Pexeva), and sertraline (Zoloft)
* [[tacrolimus]] (Prograf)
* [[thioridazine]]
* [[zileuton]] (Zyflo)
* [[ziprasidone]] (Geodon)
* [[antidepressants]]
* [[cimetidine]] (Tagamet)
* [[diuretics]] ('water pills')
* medications for anxiety, pain, and seizures
* [[sedatives]]
* [[sleeping pill]]s
* [[ticlopidine]] (Ticlid)
* [[tranquilizers]]

Also, tell your doctor if you are taking medications that may cause tics,
* including [[amphetamines]] such as amphetamine (Adderall) and dextroamphetamine (Dexadrine, Dextrostat)
* [[pemoline]] (Cylert) (not available in the US)
* [[methylphenidate]] (Concerta, Ritalin)

== '''Is this medicine FDA approved?''' ==

* Pimozide was approved for use in the United States in 1984.
* As therapy of schizophrenia, pimozide has been replaced in large part by the [[atypical antipsychotics]], which have fewer extrapyramidal side effects.
* Pimozide continues to be used in patients with [[Tourette syndrome]].

== '''How should this medicine be used?''' ==

'''Recommended dosage:'''
'''In Children:'''
* Treatment should be initiated at a dose of '''0.05 mg/kg''' preferably taken once at bedtime.
* The dose may be increased every third day to a m'''aximum of 0.2 mg/kg not to exceed 10 mg/day'''.
* At doses above 0.05 mg/kg/day, CYP 2D6 genotyping should be performed.
* In poor CYP 2D6 metabolizers, Pimozide Tablets, USP doses should not exceed 0.05 mg/kg/day, and doses should not be increased earlier than 14 days.

'''In Adults:'''
* In general, treatment with Pimozide Tablets, should be initiated with a dose of '''1 to 2 mg a day''' in divided doses.
* The dose may be increased thereafter every other day.
* Most patients are '''maintained at less than 0.2 mg/kg/day, or 10 mg/day''', whichever is less.
*'''Doses greater than 0.2 mg/kg/day or 10 mg/day are not recommended'''.

'''Administration:'''
* Pimozide comes as a tablet to take by mouth.
* It is usually taken once a day at bedtime or two or more times a day.
* Take pimozide at around the same time every day.
* Your doctor will probably start you on a low dose of pimozide and gradually increase your dose, not more than once every 2 or 3 days.
* Your doctor may decrease your dose once your condition is controlled.
* Be sure to tell your doctor how you are feeling during your treatment with pimozide.
* Pimozide controls Tourette's disorder but does not cure it.
* It may take some time before you feel the full benefit of pimozide.
* Continue to take pimozide even if you feel well.
* Do not stop taking pimozide without talking to your doctor.
* If you suddenly stop taking pimozide, you may experience difficulty controlling your movements.
* Your doctor will probably decrease your dose gradually.

== '''What are the dosage forms and brand names of this medicine?''' ==

This medicine is available in fallowing doasage form:
* As Pimozide tablet contains either 1 mg or 2 mg of pimozide

This medicine is available in fallowing brand namesː
* '''Orap'''

=='''What side effects can this medication cause?'''==

The most common side effects of this medicine include:
* [[drowsiness]], [[dizziness]], headache, blurred vision, [[dry mouth]], and [[constipation]].

Additional side effects may include:
* [[Extrapyramidal symptoms|Extrapyramidal Reactions]]
* [[Withdrawal symptoms]]
* [[Tardive Dyskinesia]]
* [[QT prolongation|prolongation of the QT interval]]
* [[Neuroleptic Malignant Syndrome]]
* [[Hyperpyrexia]]

==''' What special precautions should I follow?''' ==

* A syndrome consisting of potentially irreversible, [[involuntary]], [[dyskinetic]] movements may develop in patients treated with antipsychotic drugs. If signs and symptoms of [[tardive dyskinesia]] appear in a patient on antipsychotics, drug discontinuation should be considered. However, some patients may require treatment despite the presence of the syndrome.
* A potentially fatal symptom complex sometimes referred to as [[Neuroleptic Malignant Syndrome]] (NMS) has been reported in association with antipsychotic drugs.
* The management of NMS should include 1) immediate discontinuation of antipsychotic drugs and other drugs not essential to concurrent therapy, 2) intensive symptomatic treatment and medical monitoring, and 3) treatment of any concomitant serious medical problems for which specific treatments are available. There is no general agreement about specific pharmacological treatment regimens for uncomplicated NMS.
* Sudden, unexpected deaths have occurred in experimental studies of conditions other than Tourette’s Disorder. These deaths occurred while patients were receiving dosages in the range of 1 mg per kg. One possible mechanism for such deaths is prolongation of the QT interval. An electrocardiogram should be performed before pimozide treatment is initiated and periodically thereafter, especially during the period of dose adjustment.
* Events of [[leukopenia]]/[[neutropenia]] and [[agranulocytosis]] have been reported temporally related to antipsychotic agents. Patients with clinically significant neutropenia should be carefully monitored for fever or other symptoms or signs of infection and treated promptly if such symptoms or signs occur. Patients with severe neutropenia (absolute neutrophil count <1000/mm3) should discontinue pimozide and have their WBC followed until recovery.
* Pimozide may impair the mental and/or physical abilities required for the performance of potentially hazardous tasks, such as driving a car or operating machinery, especially during the first few days of therapy.
* Pimozide produces [[anticholinergic]] side effects and should be used with caution in individuals whose conditions may be aggravated by anticholinergic activity.
* Pimozide should be administered cautiously to patients with impairment of liver or kidney function, because it is metabolized by the liver and excreted by the kidneys.
* Antipsychotics should be administered with caution to patients receiving [[anticonvulsant]] medication, with a history of [[seizures]], or with EEG abnormalities. If indicated, adequate anticonvulsant therapy should be maintained concomitantly.
* Pimozide tablets, USP is intended only for use in patients with Tourette’s Disorder whose symptoms are severe and who cannot tolerate, or who do not respond to HALDOL® (haloperidol).
* Because substances in [[grapefruit juice]] may inhibit the metabolism of pimozide by CYP 3A4, patients should be advised to avoid grapefruit juice.
* Pimozide therapy has not been associated with serum [[aminotransferase]] elevations nor with cases of clinically apparent [[acute liver injury]].
* It is not known whether pimozide is excreted in human milk.

== '''What to do in case of emergency/overdose?''' ==

Symptoms of overdose may include:
* [[electrocardiographic]] abnormalities
* severe [[extrapyramidal]] reactions
* [[hypotension]]
* a [[comatose]] state with respiratory depression

Management of overdosage:
* {{overdose}}
* In the event of overdosage, [[gastric lavage]], establishment of a patent airway and, if necessary, mechanically-assisted [[respiration]] are advised. [[Electrocardiographic]] monitoring should commence immediately and continue until the ECG parameters are within the normal range.
* [[Hypotension]] and [[circulatory collapse]] may be counteracted by use of intravenous fluids, plasma, or concentrated [[albumin]], and [[vasopressor]] agents such as metaraminol, phenylephrine and norepinephrine.
* [[Epinephrine]] should not be used.
* In case of severe [[Extrapyramidal symptoms|extrapyramidal reactions]], [[antiparkinson]] medication should be administered.
* Because of the long half-life of pimozide, patients who take an overdose should be observed for at least 4 days.
* As with all drugs, the physician should consider contacting a poison control center for additional information on the treatment of overdose.

== '''Can this medicine be used in pregnancy?''' ==

* Pregnancy Category C.
* Because animal reproduction studies are not always predictive of human response, pimozide should be given to a pregnant woman only if the potential benefits of treatment clearly outweigh the potential risks.

=='''Can this medicine be used in children?'''==

* There is limited information available on the use of pimozide tablets, USP in children under 12 years of age.

== '''What are the active and inactive ingredients in this medicine?''' ==

'''Active Ingredient:'''
* pimozide

'''Inactive Ingredients:'''
* calcium stearate, microcrystalline cellulose, lactose anhydrous and corn starch.

== '''Who manufactures and distributes this medicine?''' ==

'''Dist. by:'''
* [[Par Pharmaceuticals|Par Pharmaceutical]]
* Chestnut Ridge, NY U.S.A.

'''Mfg. by:'''
* [[Par Formulations Private Limited]],
* 9/215, Pudupakkam, Kelambakkam
* Made in India

== '''What should I know about storage and disposal of this medication?''' ==

* Store at 20°C to 25°C (68°F to 77°F).
* Dispense in a tight, light-resistant container as defined in the official compendium with a child-resistant closure as required.

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[[Category:1-(4,4-Bis(4-fluorophenyl)butyl)piperidines]]
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Pimozide - Revision history

Deepika vegiraju at 14:54, 23 January 2023