PIMOZIDE

COMMON BRAND NAME(S): Orap

GENERIC NAME(S): PIMOZIDE

 

Description: Pimozide is an antipsychotic that works by changing the the actions of chemicals in the brain.

Pharmacokinetics: 
Absorption: >50% absorbed (oral); peak plasma levels after 4-12 hr.
Metabolism: Extensively hepatic via N-dealkylation.
Excretion: Urine and faeces (as unchanged drug and metabolites).

This medication is used to reduce uncontrolled movements (motor tics) or outbursts of words/sounds (vocal tics) caused by Tourette syndrome. Pimozide is a medication that works by decreasing the activity of a natural substance (dopamine) in the brain.

 

Pimozide should not be used for mild symptoms. It should only be used if symptoms cause severe problems in everyday life and other medicines or treatments have not been effective.

 

OTHER USES:

In Canada, this medication has been used to treat a certain mental/mood disorder (chronic schizophrenia).

 

There may be a slightly increased risk of serious, possibly fatal side effects (such as heart failure, fast/irregular heartbeat, pneumonia) when this medication is used by older adults with dementia. This medication is not approved for the treatment of dementia-related behavior problems. Discuss the risks and benefits of this medication, as well as other effective and possibly safer treatments for dementia-related behavior problems, with the doctor.

 

How to use pimozide:

Take this medication by mouth with or without food, usually once a day at bedtime or as directed by your doctor.

 

Dosage is based on your medical condition and response to treatment. Your doctor may direct you to take a low dose at first, gradually increasing the dose to lower the chance of side effects such as shaking (tremors).

 

Do not take this drug more often or increase the dose. Your symptoms will not improve any faster, and the risk for heart rhythm problems will be increased. Follow your doctor’s directions carefully.

 

Your doctor may order an electrocardiogram (EKG) and laboratory tests before you start this medication. These tests are to find out whether you are at risk for heart rhythm problems from pimozide. Keep all medical/lab appointments.

 

Other drugs, such as stimulant medications (such as methylphenidate, dextroamphetamine), may occasionally worsen tics. Before deciding to start pimozide, your doctor may try to reduce your tics by lowering the stimulant dose. Consult your doctor for more details.

 

Avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor instructs you otherwise. Grapefruit can increase the amount of this medication in your bloodstream. Consult your doctor or pharmacist for more details.

 

Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.

 

Do not stop taking this medication without consulting your doctor. Your condition may become worse when the drug is suddenly stopped. Your dose may need to be gradually decreased.

 

Tell your doctor if your condition persists or worsens.

Pregnancy Risk: Category C (Risk cannot be ruled out)

If any of the following side effects occur while taking pimozide, check with your doctor immediately:

More common

  • Difficulty with speaking
  • dizziness or fainting
  • fast or irregular heartbeat
  • lack of facial expression
  • loss of balance control
  • mood or behavior changes
  • restlessness or need to keep moving
  • shuffling walk
  • slowed movements
  • stiffness of the arms and legs
  • swelling or soreness of the breasts (less common in males)
  • trembling and shaking of the fingers and hands
  • unusual secretion of milk (rare in males)

Less common or rare

  • Difficulty with swallowing
  • inability to move the eyes
  • increased blinking or spasms of the eyelid
  • lip smacking or puckering
  • menstrual changes
  • muscle spasms, especially of the face, neck, or back
  • puffing of the cheeks
  • rapid or worm-like movements of the tongue
  • skin rash and itching
  • sore throat and fever
  • swelling of the face
  • uncontrolled chewing movements
  • uncontrolled movements of the neck, trunk, arms, or legs, including twisting movements
  • unusual bleeding or bruising
  • unusual facial expressions or body positions
  • yellow eyes or skin

Rare

  • Convulsions (seizures)
  • difficult or unusually fast breathing
  • fast heartbeat or irregular pulse
  • fever (high)
  • high or low (irregular) blood pressure
  • increased sweating
  • loss of bladder control
  • muscle stiffness (severe)

If any of the following symptoms of overdose occur while taking pimozide, get emergency help immediately:

Symptoms of overdose

  • Coma
  • dizziness (severe)
  • muscle trembling, jerking, or stiffness (severe)
  • troubled breathing (severe)
  • uncontrolled movements (severe)

Some pimozide side effects may not need any medical attention.:

More common

  • Blurred vision or other vision problems
  • constipation
  • dizziness, lightheadedness, or fainting when getting up from a lying or sitting position
  • drowsiness
  • dryness of the mouth
  • skin discoloration

Less common

  • Decreased sexual ability
  • diarrhea
  • headache
  • loss of appetite and weight
  • mental depression
  • nausea and vomiting

tiredness or weakness

Precautions

 

Before taking this medication, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

 

Before using this medication, tell your doctor or pharmacist your medical history, especially of: blood problems (such as a low white blood cell count), a certain eye condition (glaucoma), dementia, depression, heart problems (such as slow/fast/irregular heartbeat, low blood pressure), slow movement of the gut/intestines (such as chronic constipation, blockage), kidney disease, liver disease, brain disorder/tumor/injury, drug/alcohol/substance abuse, breast cancer, Parkinson’s disease, seizure disorder, a certain severe reaction to other antipsychotic-type medications (neuroleptic malignant syndrome-NMS), difficulty urinating (such as due to prostate problems).

 

This drug may make you dizzy or drowsy or cause vision changes. Do not drive, use machinery, or do any activity that requires alertness or clear vision until you are sure you can perform such activities safely. Avoid alcoholic beverages.

 

Pimozide may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can infrequently result in serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.

 

The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may cause QT prolongation. Before using pimozide, tell your doctor or pharmacist of all the drugs you take and if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).

 

Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/”water pills”) or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using pimozide safely.

 

Before having surgery or imaging procedures (such as certain X-rays, CT scans) requiring the use of contrast dye (such as metrizamide), tell your doctor or dentist that you are using this medication and about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

 

Older adults may be more sensitive to the side effects of this drug, especially QT prolongation (see above).

 

During pregnancy, this medication should be used only when clearly needed. Babies born to mothers who have used this drug during the last 3 months of pregnancy may infrequently develop symptoms including muscle stiffness or shakiness, drowsiness, feeding/breathing difficulties, or constant crying. If you notice any of these symptoms in your newborn especially during their first month, tell the doctor right away.

 

Since untreated mental/mood problems (such as schizophrenia) can be a serious condition, do not stop taking this medication unless directed by your doctor. If you are planning pregnancy, become pregnant, or think you may be pregnant, immediately discuss with your doctor the benefits and risks of using this medication during pregnancy.

 

It is unknown if this drug passes into breast milk. Consult your doctor before breastfeeding.

 

Interactions

 

Some products that may interact with this drug include: anticholinergic/antispasmodic drugs (such as atropine, dicyclomine, scopolamine), drugs that increase the amount of dopamine in your body (such as bromocriptine, cabergoline, levodopa, pergolide, ropinirole).

 

Other medications can affect the removal of pimozide from your body, which may affect how pimozide works. Examples include aprepitant, azole antifungals (such as ketoconazole, itraconazole), delavirdine, HIV protease inhibitors (such as ritonavir, nelfinavir), hepatitis C virus protease inhibitors (such as boceprevir, telaprevir), macrolide antibiotics (such as azithromycin, erythromycin), nefazodone, SSRI antidepressants (such as fluvoxamine, paroxetine, sertraline), zileuton, among others.

 

Tell your doctor or pharmacist if you are taking other products that cause drowsiness including alcohol, antihistamines (such as cetirizine, diphenhydramine), drugs for sleep or anxiety (such as alprazolam, diazepam, zolpidem), muscle relaxants, and narcotic pain relievers (such as codeine).

 

Check the labels on all your medicines (such as allergy or cough-and-cold products) because they may contain ingredients that cause drowsiness. Ask your pharmacist about using those products safely.

 

Many drugs besides pimozide may affect the heart rhythm (QT prolongation). Examples include amiodarone, cisapride, citalopram/escitalopram, chlorpromazine, dofetilide, procainamide, quinidine, ranolazine, sotalol, macrolide antibiotics (such as clarithromycin, erythromycin), among others.

 

Also report the use of drugs that might increase seizure risk when combined with pimozide, such as bupropion, isoniazid (INH), phenothiazines (such as promethazine), lithium, theophylline, or tricyclic antidepressants (such as amitriptyline), among others. Consult your doctor or pharmacist for details.

Overdose

 

If overdose is suspected, contact a poison control center or emergency room immediately. Symptoms of overdose may include: slow/shallow breathing, inability to wake up (coma).

 

Notes

Do not share this medication with others.

 

Laboratory and medical tests (such as electrocardiogram-EKG, complete blood count) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

 

Missed Dose

If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

 

Storage

Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.

 

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

 

Brands

 

There are no brands containing this molecule.

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