Iloperidone

Iloperidone is a prescription medication used to treat schizophrenia. Iloperidone belongs to a group of drugs called antipsychotics. These work by altering the activity of certain natural substances in the brain.

This medication comes in tablet form and is taken twice a day, with or without food.

Common side effects include dry mouth, fatigue, and dizziness. Do not drive or operate heavy machinery until you know how iloperidone affects you.
 

CYP2D6 is a protein in your body that is involved in the elimination of iloperidone and other drugs from your body. Some patients have less of this protein in their bodies, affecting how much of the drug gets eliminated. Levels of CYP2D6 can vary greatly between individuals, and those having less of this protein are known as "poor metabolizers." 

CYP2D6 testing is done to determine whether you are a poor metabolizer. If you are a poor metabolizer, the levels of iloperidone in your blood can become too high. As a result you may be at an increased risk of having more side effects from iloperidone. 

Your doctor may adjust your dose of iloperidone if you are a poor metabolizer.

Iloperidone is a prescription medication used to treat schizophrenia.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.
 

Iloperidone may be found in some form under the following brand names:

• Fanapt

Common side effects include:

• dizziness
• dry mouth
• fatigue
• nasal congestion
• fatigue
• a fast heart beat
• low blood pressure
• weight increase

This is not a complete list of iloperidone side effects. Ask your doctor or pharmacist for more information.

Tell your doctor if you have any side effect that bothers you or that does not go away.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take:

• medications that block a protein in the body (CYP2D6) such as quinidine (Qualaquin), fluoxetine (Prozac, Sarafem), amitriptyline (Elavil, Amitril), and paroxetine (Paxil)
• medications that block a protein in the body (CYPA4) such as some macrolide antibiotics (clarithromycin, telithromycin), some HIV protease inhibitors (indinavir, nelfinavir, ritonavir, saquinavir), some HCV protease inhibitors (boceprevir, telaprevir), some azole antifungals (ketoconazole, itraconazole, posaconazole, voriconazole), conivaptan (Vaprisol), delavirdine (Rescriptor), and nefazodone
• dextromethorphan
• medications that can prolong the QT Interval such as quinidine (Nuedexta), procainamide, amiodarone (Nexterone, Pacerone, Cordarone), sotalol (Betapace), chlorpromazine, thioridazine, gatifloxacin (Zymar), moxifloxacin (Avelox)

This is not a complete list of iloperidone drug interactions. Ask your doctor or pharmacist for more information.

Serious side effects have been reported with iloperidone including the following:

• QT Prolongation. This is a condition when changes in the electrical activity of your heart occur, causing irregular heartbeats that can be life threatening. Talk to your healthcare provider about other medicines you are taking before you start taking iloperidone. Tell your healthcare provider right away if you have any signs or symptoms of QT prolongation:
  • feeling faint
  • lightheadedness
  • dizziness
  • feeling like your heart is beating irregularly or quickly
• Neuroleptic Malignant Syndrome (NMS). Neuroleptic Malignant Syndrome (NMS) is a rare and potentially fatal side effect reported with iloperidone and similar medicines. Call your doctor immediately if the person being treated develops symptoms such as high fever; stiff muscles; shaking; confusion; sweating; changes in pulse, heart rate, or blood pressure; or muscle pain and weakness. Treatment should be stopped if the person being treated has NMS.
• Tardive Dyskinesia (TD). Tardive Dyskinesia (TD) is a serious, sometimes permanent side effect reported with iloperidone and similar medications. TD includes uncontrollable movements of the face, tongue, and other parts of the body. The risk of developing TD and the chance that it will become permanent is thought to increase with the length of therapy and the overall dose taken by the patient. This condition can develop after a brief period of therapy at low doses, although this is much less common. There is no known treatment for TD, but it may go away partially or completely if therapy is stopped.
• High blood sugar and diabetes. High blood sugar and diabetes have been reported with iloperidone and similar medications. If the person being treated has diabetes or risk factors such as being overweight or a family history of diabetes, blood sugar testing should be performed at the beginning and throughout treatment with iloperidone. Complications of diabetes can be serious and even life-threatening. If signs of high blood sugar or diabetes develop, such as being thirsty all the time, going to the bathroom a lot, or feeling weak or hungry, contact your doctor.
• Weight gain.
• Seizures. Iloperidone should be used cautiously in people with a seizure disorder, who have had seizures in the past, or who have conditions that increase their risk for seizures.
• Orthostatic Hypotension and Syncope. Some people taking iloperidone may feel faint or lightheaded when they stand up or sit up too quickly. This is more common when you first start taking iloperidone or when your dose is increased. To avoid this problem, get out of bed slowly, resting your feet on the floor for a few minutes before standing up. By standing up or sitting up slowly and following your healthcare professional’s dosing instructions, this side effect can be reduced or it may go away over time.
• Low blood counts. Blood problems such as low numbers of white blood cells have been reported in patients taking iloperidone and similar medications. In some cases it has been serious and life-threatening. Depending upon your medical condition, your doctor may choose to test your blood as you start therapy with iloperidone.
• Hyperprolactinemia. Iloperidone and similar medications can raise the blood levels of a hormone known as prolactin, causing a condition known as hyperprolactinemia. Blood levels of prolactin remain elevated with continued use. Some side effects seen with these medications include the absence of a menstrual period; breasts producing milk; the development of breasts by males; and the inability to achieve an erection.
• Body Temperature Regulation. Iloperidone may make you more sensitive to heat. You may have trouble cooling off, or be more likely to become dehydrated, so take care when exercising or when doing things that make you warm. Tell your doctor if you plan to do vigorous exercise or be exposed to extreme heat.
• Dysphagia. Tell your doctor if you have trouble swallowing.
• Suicide. Call your doctor right away if you have any of the following symptoms, or call 911 if an emergency, especially if they are new, worse, or worry you:
  • attempts to commit suicide
  • acting on dangerous impulses
  • acting aggressive or violent
  • thoughts about suicide or dying
  • new or worse depression
  • new or worse anxiety or panic attacks
  • feeling agitated, restless, angry or irritable
  • trouble sleeping
  • an increase in activity or talking more than what is normal for you
  • other unusual changes in behavior or mood
• Painful, long-lasting erections. Painful, long-lasting erections have been reported with the use of iloperidone. Call your doctor immediately if you think you are having this problem.
• Cognitive and Motor Impairment. Iloperidone may affect your thinking, judgment, and ability to move. Do not drive a car or operate machinery until you know how this medication affects you.

Ask your doctor about the safe use of alcoholic beverages while you are taking iloperidone. Alcohol can make the side effects from iloperidone worse.

Iloperidone can cause dizziness. Do not drive or operate heavy machinery until you know how iloperidone affects you.

Iloperidone is not approved by the Food and Drug Administration (FDA) for the treatment of behavior problems in older adults with dementia. Talk to the doctor who prescribed this medication if you, a family member, or someone you care for has dementia and is taking iloperidone.

Do not take iloperidone if you are allergic to iloperidone or to any of its ingredients.

Grapefruit and grapefruit juice may interact with iloperidone and lead to potentially dangerous effects. Discuss the use of grapefruit products with your doctor.

Before taking iloperidone, tell your doctor about all of your medical conditions. Especially tell your doctor if you:

• are allergic to iloperidone or to any of its ingredients
• use or have ever used street drugs or have overused prescription medications
• if you have difficulty swallowing
• or anyone in your family has or has ever had diabetes 
• have or have ever had prolonged QT interval (a rare heart problem that may cause irregular heartbeat, fainting, or sudden death), a slow or irregular heartbeat, a recent heart attack, a low level of potassium or magnesium in your blood, seizures, breast cancer, or heart or liver disease
• have a low level of white blood cells or if you have ever developed a low level of blood cells as a side effect of a medication that you took
• have severe vomiting or diarrhea or become dehydrated at any time during your treatment
• tell your doctor if you are pregnant, especially if you are in the last few months of your pregnancy, or if you plan to become pregnant or are breast-feeding. If you become pregnant while taking iloperidone, call your doctor. Iloperidone may cause problems in newborns following delivery if it is taken during the last months of pregnancy.

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements.

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

Iloperidone falls into category C. In animal studies, pregnant animals were given this medication and had some babies born with problems. No well-controlled studies have been done in humans. Therefore, this medication may be used if the potential benefits to the mother outweigh the potential risks to the unborn child.

Tell your doctor if you are breastfeeding or plan to breastfeed.

It is not known if iloperidone crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication. Your doctor and you will decide if the benefits outweigh the risk of using iloperidone.

It is recommended that women receiving iloperidone should not breast feed.

Take iloperidone exactly as prescribed.

Iloperidone comes in tablet form and is taken twice a day, with or without food.

If you miss a dose, take the missed dose as soon as you remember. If it is almost time for the next dose, skip the missed dose and take your next dose at the regular time. Do not take two doses of iloperidone at the same time.

Take this medication exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.

The dose your doctor recommends may be based on the following:

• the condition being treated
• other medical conditions you have
• other medications you are taking
• how you respond to this medication
• if you are a poor metabolism of CYP2D6

The recommended dose range of iloperidone (Fanapt) is 12 to 24 mg/day administered twice daily.

This target dosage range is achieved by daily dosage adjustments, starting at a dose of 1 mg twice daily, then moving to 2 mg, 4 mg, 6 mg, 8 mg, 10 mg, and 12 mg twice daily on days 2, 3, 4, 5, 6, and 7 respectively.

If you take too much iloperidone, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

• Store iloperidone at room temperature 25°C (77°F).
• Protect iloperidone tablets from exposure to light and moisture.
• Keep this and all medicines out of the reach of children.

Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Iloperidone is not approved for use in patients with dementia-related psychosis.