Aripiprazole

Name: Aripiprazole

How should this medicine be used?

Aripiprazole comes as a tablet, a solution (liquid), and an orally disintegrating tablet (tablet that dissolves quickly in the mouth) to take by mouth. It is usually taken once a day with or without food. Take aripiprazole at around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take aripiprazole exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Do not try to push the orally disintegrating tablet through the foil. Instead, use dry hands to peel back the foil packaging. Immediately take out the tablet and place the entire tablet on your tongue. Do not try to split the tablet. The tablet will quickly dissolve and can be swallowed without liquid. If necessary, liquid can be used to take the orally disintegrating tablet.

Your doctor may start you on a low dose of aripiprazole and gradually increase or decrease your dose depending on how well the medication works for you and the side effects you experience.

Aripiprazole may help control your symptoms but will not cure your condition. It may take 2 weeks or longer before you feel the full benefit of aripiprazole. Continue to take aripiprazole even if you feel well. Do not stop taking aripiprazole without talking to your doctor.

What special precautions should I follow?

Before taking aripiprazole,

  • tell your doctor and pharmacist if you are allergic to aripiprazole, any other medications, or any of the ingredients in aripiprazole tablets, orally disintegrating tablets, or oral solution. Ask your doctor or pharmacist for a list of the ingredients.
  • tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: antidepressants (mood elevators); antifungals such as itraconazole (Sporanox) and ketoconazole (Nizoral); antihistamines; bupropion (Wellbutrin); carbamazepine (Tegretol); clarithromycin (Biaxin); fluoxetine (Prozac, Sarafem); HIV protease inhibitors such as atazanavir (Reyataz), indinavir (Crixivan), nelfinavir (Viracept), ritonavir (Norvir), and saquinavir (Invirase); ipratropium (Atrovent); medications for anxiety, high blood pressure, irritable bowel syndrome, mental illness, motion sickness, Parkinson's disease, seizures, ulcers, or urinary problems; nefazodone; paroxetine (Paxil, Pexeva); quinidine; rifampin (Rifadin, Rimactane); sedatives; sleeping pills; telithromycin (Ketek); and tranquilizers. Your doctor may need to change the doses of your medications or monitor you carefully for side effects. Many other medications may also interact with aripiprazole, so be sure to tell your doctor about all the medications you are taking, even those that do not appear on this list.
  • tell your doctor if you have severe diarrhea or vomiting or you think you may be dehydrated. . Also tell your doctor if you have or have ever had heart disease, heart failure, a heart attack, an irregular heartbeat, high or low blood pressure, a stroke, a ministroke, seizures, a low number of white blood cells, dyslipidemia (high cholesterol levels), trouble keeping your balance, or any condition that makes it difficult for you to swallow. Tell your doctor if you or anyone in your family use or have ever used street drugs or have overused prescription medication or alcohol or has or has ever had diabetes, obsessive compulsive disorder, impulse-control disorder, bipolar disorder, or an impulsive personality. Also tell your doctor if you have ever had to stop taking a medication for mental illness because of severe side effects.
  • 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 breastfeeding. If you become pregnant while taking aripiprazole, call your doctor. Aripiprazole may cause problems in newborns following delivery if it is taken during the last months of pregnancy.
  • if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking aripiprazole.
  • you should know that aripiprazole may make you drowsy. Do not drive a car or operate machinery until you know how this medication affects you.
  • you should know that alcohol can add to the drowsiness caused by this medication. Do not drink alcohol while taking aripiprazole.
  • you should know that you may experience hyperglycemia (increases in your blood sugar) while you are taking this medication, even if you do not already have diabetes. If you have schizophrenia, you are more likely to develop diabetes than people who do not have schizophrenia, and taking aripiprazole or similar medications may increase this risk. Tell your doctor immediately if you have any of the following symptoms while you are taking aripiprazole: extreme thirst, frequent urination, extreme hunger, blurred vision, or weakness. It is very important to call your doctor as soon as you have any of these symptoms, because high blood sugar that is not treated can cause a serious condition called ketoacidosis. Ketoacidosis may become life-threatening if it is not treated at an early stage. Symptoms of ketoacidosis include dry mouth, nausea and vomiting, shortness of breath, breath that smells fruity, and decreased consciousness.
  • you should know that aripiprazole may cause dizziness, lightheadedness, and fainting when you get up too quickly from a lying position. This is more common when you first start taking aripiprazole. To avoid this problem, get out of bed slowly, resting your feet on the floor for a few minutes before standing up.
  • you should know that aripiprazole may make it harder for your body to cool down when it gets very hot. Tell your doctor if you plan to do vigorous exercise or be exposed to extreme heat.
  • if you have phenylketonuria (PKU, an inherited condition in which a special diet must be followed to prevent mental retardation), you should know that the orally disintegrating tablets contain phenylalanine. If you have diabetes, you should know that aripiprazole solution contains sugar.
  • you should know that some people who took medications such as aripiprazole developed gambling problems or other intense urges or behaviors that were compulsive or unusual for them, such as increased sexual urges or behaviors, excessive shopping, and binge eating. Call your doctor if you have intense urges to shop, eat, have sex, or gamble, or you are unable to control your behavior. Tell your family members about this risk so that they can call the doctor even if you do not realize that your gambling or any other intense urges or unusual behaviors such as have become a problem.
  • you should know that when aripiprazole is used to treat children, it should be used as part of a treatment program that may include counseling and special education. Be sure that your child follows all of his or her doctor's or therapist's instructions.

What other information should I know?

Keep all appointments with your doctor and the laboratory. Your doctor may order laboratory tests before and during your treatment with aripiprazole.

Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your prescription.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.

How to take aripiprazole

  • Before you start the treatment, read the manufacturer's printed information leaflet from inside the pack. It will give you more information about aripiprazole and it will also provide you with a full list of the side-effects which you may experience from taking it.
  • The recommended dose for adults is 15 mg once daily. Your dose, however, may be adjusted to suit your condition, so take aripiprazole exactly as your doctor tells you to. The directions for taking your doses will be printed on the label of the pack to remind you about what the doctor said to you.
  • You can take aripiprazole either before or after meals.
  • Try to get into the habit of taking your doses at the same time of day each day, as this will help you to remember to take it. If you do forget to take a dose, take it as soon as you remember. If you do not remember until the following day, skip the missed dose. Do not take two doses at the same time to make up for a forgotten dose.
  • Aripiprazole tablets should generally be taken swallowed whole with a drink of water. However, if you have been given Abilify® orodispersible tablets (these are tablets which dissolve in your mouth), peel open the packaging, remove the tablet from the blister and place it on your tongue to dissolve. Alternatively if you prefer, you can take the orodispersible tablet stirred into a small glassful of water.
  • If you have been given Abilify® oral solution liquid medicine, you must take this undiluted. Measure your dose out carefully using the cup or dropper supplied in the pack. If you are in any way unsure about measuring out your dose, you can ask your local pharmacist to show you what to do.

Aripiprazole Dosage

Take aripiprazole exactly as prescribed by your doctor. Follow the directions on your prescription label carefully. The recommended dose varies depending upon which condition is being treated as well as other factors.

Aripiprazole tablets and oral solution

  • The recommended dose range for aripiprazole (Abilify) is 5 mg -15 mg per day. The maximum dose per day is 30 mg.
  • The target dose for adolescents is 10 mg/day.
  • Your doctor will start you on a smaller dose and then increase the dose to a target dose.

Aripiprazole immediate-release injection

  • The recommended dose is 9.75 mg injected into the muscle (IM) once. If another dose is needed, the second dose can be administered 2 hours later. The maximum dose of aripiprazole (Abilify) per day is 30 mg.

Aripiprazole orally disintegrating tablet

  • The recommended dose for aripiprazole orally disintegrating tablet (Abilify Discmelt) is 10 mg or 15 mg by mouth daily. The target dose for adolescents is 10 mg/day.
  • The dose may be increased to a maximum of 30 mg daily after 2 weeks.

Aripiprazole extended-release injection

  • The recommended starting dose and maintenance dose is 400 mg administered monthly as a single injection. If you have side effects, your dose can be reduced to 300 mg.
  • In conjunction with first dose, take 14 consecutive days of concurrent oral aripiprazole (10 mg to 20 mg) or current oral antipsychotic.
  • Dosage adjustments are required for missed doses.
  • If you are a known CYP2D6 Poor metabolizers, the recommended starting dose and maintenance dose is 300 mg administered monthly as a single injection.

Proper Use of aripiprazole

Take aripiprazole exactly as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. To do so may increase the chance of side effects.

aripiprazole should come with a Medication Guide. Read and follow the instructions carefully. Ask your doctor if you have any questions.

If you are using the orally disintegrating tablet, make sure your hands are dry before you handle the tablet. Do not open the blister pack that contains the tablet until you are ready to take it. Remove the tablet from the blister pack by peeling back the foil, then taking the tablet out. Do not push the tablet through the foil. Do not break or split the tablet. Place the tablet in your mouth. It should melt quickly. After the tablet has melted, you may swallow or take a sip of water.

Swallow the tablets whole. Do not break, crush, or chew them.

Aripiprazole may be taken with or without food. If your doctor tells you to take it a certain way, follow your doctor's instructions.

Dosing

The dose of aripiprazole will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of aripiprazole. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For oral dosage forms (tablets and orally disintegrating tablets):
    • For bipolar mania:
      • Adults—At first, 15 milligrams (mg) once a day. When it is given with lithium or valproate, the starting dose is 10 to 15 mg once a day. Your doctor may adjust your dose as needed. However, the dose is usually not more than 30 mg per day.
      • Children 10 years of age and older—At first, 2 mg once a day. The dose will be gradually increased to 10 mg once a day. Your doctor may adjust your dose again as needed. However, the dose is usually not more than 30 mg per day.
      • Children younger than 10 years of age—Use and dose must be determined by your doctor.
    • For depression:
      • Adults—At first, 2 to 5 milligrams (mg) once a day. Your doctor may adjust your dose as needed. However, the dose is usually not more than 15 mg per day.
      • Children—Use and dose must be determined by your doctor.
    • For irritability in children with autistic disorder:
      • Children 6 to 17 years of age—At first, 2 milligrams (mg) once a day. Your doctor may adjust your dose as needed. However, the dose is usually not more than 15 mg per day.
      • Children younger than 6 years of age—Use and dose must be determined by your doctor.
    • For schizophrenia:
      • Adults—At first, 10 to 15 milligrams (mg) once a day. Your doctor may adjust your dose as needed. However, the dose is usually not more than 30 mg per day.
      • Children 13 to 17 years of age—At first, 2 mg once a day. The dose will be gradually increased to 10 mg once a day. Your doctor may adjust your dose again as needed. However, the dose is usually not more than 30 mg per day.
      • Children younger than 13 years of age—Use and dose must be determined by your doctor.
    • For Tourette's disorder:
      • Children 6 to 18 years of age—At first, 2 milligrams (mg) once a day. Your doctor may adjust your dose as needed. However, the dose is usually not more than 20 mg per day.
      • Children younger than 6 years of age—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of aripiprazole, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Index Terms

  • BMS 337039
  • OPC-14597

Pharmacology

Aripiprazole is a quinolinone antipsychotic which exhibits high affinity for D2, D3, 5-HT1A, and 5-HT2A receptors; moderate affinity for D4, 5-HT2C, 5-HT7, alpha1 adrenergic, and H1 receptors. It also possesses moderate affinity for the serotonin reuptake transporter; has no affinity for muscarinic (cholinergic) receptors. Aripiprazole functions as a partial agonist at the D2 and 5-HT1A receptors, and as an antagonist at the 5-HT2A receptor (de Bartolomeis 2015).

Absorption

IM: Extended-release: Slow, prolonged

Oral: Well absorbed

Distribution

Vd: 4.9 L/kg

Metabolism

Hepatic dehydrogenation, hydroxylation and N-dealkylation via CYP2D6, CYP3A4 (dehydro-aripiprazole metabolite has affinity for D2 receptors similar to the parent drug and represents 40% of the parent drug exposure in plasma) (Sheehan 2010)

Excretion

Feces (55%, ~18% of the total dose as unchanged drug; 37% of the total dose as changed drug); urine (25%, <1% of the total dose as unchanged drug; 25% of the total dose as changed drug) (Sheehan 2010)

Special Populations Renal Function Impairment

In severe renal impairment (CrCl <30 mL/minute), Cmax increased by 36% (aripiprazole) and 53% (dehydro-aripiprazole), but AUC was 15% lower for aripiprazole and 7% higher for dehydro-aripiprazole.

Use Labeled Indications

Oral:

Bipolar I disorder: Acute treatment of manic and mixed episodes associated with bipolar I disorder.

Irritability associated with autistic disorder: Treatment of irritability associated with autistic disorder.

Major depressive disorder: Adjunctive treatment of major depressive disorder.

Schizophrenia: Treatment of schizophrenia.

Tourette disorder: Treatment of Tourette disorder.

Injection:

Agitation associated with schizophrenia or bipolar mania (immediate-release injection only): Treatment of agitation associated with schizophrenia or bipolar mania.

Bipolar I disorder (extended-release injection only): Maintenance monotherapy treatment of bipolar I disorder.

Schizophrenia (extended-release injection only): Treatment of schizophrenia.

Off Label Uses

Psychosis/agitation associated with dementia

Data from randomized, double-blind, placebo-controlled trials supports the use of aripiprazole in the treatment psychosis and agitation related to Alzheimer dementia [De Deyn 2005], [Mintzer 2007], [Rappaport 2009], [Streim 2008]. Additional trials may be necessary to further define the role of aripiprazole in this condition.

Based on the American Psychiatric Association (APA) practice guideline on the use of antipsychotics to treat agitation or psychosis in patients with dementia, antipsychotics, such as aripiprazole, may be considered for the treatment of agitation and psychosis in certain patients; however, evidence for efficacy is modest and use should be limited to patients whose symptoms are dangerous, severe, or cause significant patient distress due to safety risks associated with antipsychotic use. Based on the World Federation of Societies of Biological Psychiatry guidelines for the treatment of Alzheimer disease and other dementias, drug treatment with aripiprazole for behavioral and psychological aspects (including hyperactivity and psychosis) is recommended at low doses and for short durations, as a last option after addressing causative factors and using psychosocial interventions.

For the Consumer

Applies to aripiprazole: oral solution, oral tablet, oral tablet disintegrating

Other dosage forms:

  • intramuscular powder for suspension extended release, intramuscular solution

Along with its needed effects, aripiprazole may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur while taking aripiprazole:

More common
  • Difficulty with speaking
  • drooling
  • loss of balance control
  • muscle trembling, jerking, or stiffness
  • restlessness
  • shuffling walk
  • stiffness of the limbs
  • twisting movements of the body
  • uncontrolled movements, especially of the face, neck, and back
Less common
  • Blurred vision
  • dizziness
  • headache
  • inability to move the eyes
  • increased blinking or spasms of the eyelid
  • nervousness
  • pounding in the ears
  • slow or fast heartbeat
  • sticking out the tongue
  • trouble with breathing or swallowing
  • unusual facial expressions
Rare
  • Convulsions
  • fast heartbeat
  • high fever
  • high or low blood pressure
  • increased sweating
  • lip smacking or puckering
  • loss of bladder control
  • muscle spasm or jerking of all extremities
  • puffing of the cheeks
  • rapid or worm-like movements of the tongue
  • severe muscle stiffness
  • sudden loss of consciousness
  • tiredness
  • uncontrolled chewing movements
  • uncontrolled movements of the arms and legs
  • unusually pale skin
Incidence not known
  • Hives or welts, itching, or skin rash
  • itching, puffiness, or swelling of the eyelids or around the eyes, face, lips, or tongue
  • large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs
  • redness of the skin
  • tightness in the chest
  • unusual tiredness or weakness

Get emergency help immediately if any of the following symptoms of overdose occur while taking aripiprazole:

Symptoms of overdose
  • Bigger, dilated, or enlarged pupils (black part of the eye)
  • diarrhea
  • fast, pounding, or irregular heartbeat or pulse
  • increased sensitivity of the eyes to light
  • lack or loss of strength
  • nausea
  • sleepiness or unusual drowsiness
  • vomiting

Some side effects of aripiprazole may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common
  • Acid or sour stomach
  • anxiety
  • belching
  • blurred vision
  • difficulty having a bowel movement (stool)
  • dry mouth
  • fear
  • fever
  • headache
  • heartburn
  • hyperventilation
  • inability to sit still
  • indigestion
  • irritability
  • lightheadedness
  • need to keep moving
  • nervousness
  • rash
  • runny nose
  • shaking
  • sore throat
  • stomach discomfort, upset, or pain
  • trouble sleeping
  • weight gain
Less common
  • Accidental injury
  • bloating or swelling of the face, arms, hands, lower legs, or feet
  • body aches or pain
  • congestion
  • coughing
  • difficulty with moving
  • dryness or soreness of the throat
  • hoarseness
  • increased appetite
  • increased salivation
  • joint pain
  • muscle aching or cramping
  • muscle pains or stiffness
  • rapid weight gain
  • sneezing
  • stuffy nose
  • swollen joints
  • tender, swollen glands in the neck
  • tingling of the hands or feet
  • tremor
  • unusual weight gain or loss
  • voice changes

Response and Effectiveness

  • Peak blood levels are reached within three to five hours of taking oral aripiprazole. Effects are long lasting, so aripiprazole is usually taken once daily.
  • May take up to two weeks to achieve stable blood concentrations.
  • Target dosages of 10-15mg per day of aripiprazole are recommended for schizophrenia; dosages above 15 mg/day have not been found to be more effective than 15 mg/day.
  • Dosage reductions may be needed for people known to be poor metabolizers of drugs like aripiprazole, or in people taking other medications known to interfere with the hepatic enzymes CYP2D6 and CYP3A4. Conversely, a dosage increase of aripiprazole may be needed when given with medications that induce CYP3A4.

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