cardiac dysrhythmia); additional signs may include elevated creatinine phosphokinase, myoglobinuria (rhabdomyolysis), and acute renal failure If NMS is suspected, immediately discontinue therapy, and provide intensive symptomatic treatment and monitoring Tardive dyskinesia Tardive dyskinesia reported in patients treated with antipsychotic drugs Incidence highest in elderly persons, especially elderly women Increased duration of treatment and cumulative dose increases may increase risk of tardive dyskinesia and the potential for it to be irreversible Use lowest dose and shortest duration of treatment needed to produce a satisfactory clinical response; periodically reassess the need for continued treatment If signs and symptoms of tardive dyskinesia appear, consider discontinuing therapy Reserve chronic antipsychotic treatment for the following patients Who suffer from chronic illness and is responsive to antipsychotics For whom alternative therapies are not available or appropriate Metabolic changes Atypical antipsychotic drugs have been associated with metabolic changes that include hyperglycemia/diabetes mellitus (including extreme cases associated with ketoacidosis or hyperosmolar coma or death), dyslipidemia, and body weight gain Assess fasting plasma glucose, fasting lipid profile, and weight before or soon after initiation of antipsychotic medication, and monitor periodically during long-term treatment Drug interaction overview Strong CYP3A4 inhibitors Reduce brexpiprazole dose Strong CYP3A4 inhibitors may increase exposure of brexpiprazole Strong CYP2D6 inhibitors Reduce brexpiprazole dose Strong CY2D6 inhibitors may increase exposure of brexpiprazole Both CYP3A4 and CYP2D6 inhibitors Reduce brexpiprazole dose Drugs that are strong or moderate CYP3A4 and CYP2D6 inhibitors may increase exposure of brexpiprazole Strong CYP3A4 inducers Increase brexpiprazole dose Strong CYP3A4 inducers may decrease exposure of brexpiprazole Pregnancy Adequate and well-controlled studies have not been conducted with brexpiprazole in pregnant females inform drug-associated risks Pregnancy exposure registry Monitors pregnancy outcomes in women exposed to brexpiprazole during pregnancy; for more information contact the National Pregnancy Registry for Atypical Antipsychotics at 1-866-961-2388 or visit http://womensmentalhealth.org/clinical-and-research-programs/pregnancy Clinical considerations Neonates whose mothers are exposed to antipsychotic drugs, like brexpiprazole, during the third trimester are at risk for extrapyramidal and/or withdrawal symptoms (eg, agitation, hypertonia, hypotonia, tremor, somnolence, respiratory distress, and feeding disorder) Animal studies No teratogenicity was observed with oral administration to pregnant rats and rabbits during organogenesis at doses up to 73x and 146x, respectively, of maximum recommended human dose (MRHD) of 4 mg/day on a mg/m2 basis However, when pregnant rats were administered brexpiprazole during organogenesis through lactation, the number of perinatal deaths of pups was increased at 73x the MRHD Lactation Unknown if distributed in human breast milk Present in rat milk The development and health benefits of breastfeeding should be considered along with the mother’s clinical need for the drug and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal conditionPregnancy Categories A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk. B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available. Mechanism of Action Serotonin-dopamine activity modulator (SDAM) that acts as a partial agonist at 5-HT1A and dopamine D2 receptors at similar potency, and an antagonist at 5-HT2A and noradrenaline alpha1B/2C receptors Absorption Absolute bioavailability: 95% Peak plasma time: 4 hr Steady-state concentration: 1-12 days Distribution Protein bound: >99% to serum albumin and alpha-1-acid glycoprotein; its protein binding is not affected by renal or hepatic impairment Brexpiprazole protein binding is not affected by warfarin, diazepam, or digitoxin Vd: 1.56 L/kg Metabolism Metabolized primarily by CYP2D6 and CYP3A4 isoenzymes Elimination Half-life: 91 hr Clearance: 19.8 mL·hr/kg Excretion: 25% urine; 46% feces Oral Administration Take with or without food Storage Store at 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF) BRAND FORM. UNIT PRICE PILL IMAGE Rexulti oral- 4 mg tabletRexulti oral- 3 mg tabletRexulti oral- 2 mg tabletRexulti oral- 1 mg tabletRexulti oral- 0.5 mg tabletRexulti oral- 0.25 mg tabletCopyright © 2010 First DataBank, Inc.Print Patient Educationbrexpiprazole oral BREXPIPRAZOLE - ORAL (brex-PIP-ra-zole) COMMON BRAND NAME(S): Rexulti WARNING: There may be a slightly increased risk of serious, possibly fatal side effects (such as stroke, 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 without agitation that may occur with dementia due to Alzheimer's disease. 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. See also Uses section.Brexpiprazole is used to treat certain mental/mood disorders (such as schizophrenia, depression). Drugs used to treat depression can help prevent suicidal thoughts/attempts and provide other important benefits. However, studies have shown that a small number of people (especially people younger than 25) who take antidepressants for any condition may experience worsening depression, other mental/mood symptoms, or suicidal thoughts/attempts. It is very important to talk with the doctor about the risks and benefits of drugs used to treat depression (especially for people younger than 25), even if treatment is not for a mental/mood condition.Tell the doctor right away if you notice worsening depression/other psychiatric conditions, unusual behavior changes (including possible suicidal thoughts/attempts), or other mental/mood changes (including new/worsening anxiety, panic attacks, trouble sleeping, irritability, hostile/angry feelings, impulsive actions, severe restlessness, very rapid speech). Be especially watchful for these symptoms when a new drug to treat depression is started or when the dose is changed. USES: This medication is used to treat certain mental/mood disorders (such as schizophrenia, depression). Brexpiprazole is also used to treat agitation that may occur with dementia due to Alzheimer's disease. Brexpiprazole helps you to think more clearly, feel less nervous, and take part in everyday life. It may also help to decrease hallucinations (hearing/seeing things that are not there). In addition, this medication may improve your mood, sleep, appetite, and energy level. Brexpiprazole is a psychiatric medication that belongs to the class of drugs called atypical antipsychotics. It works by helping to restore the balance of certain natural substances in the brain. HOW TO USE: Read the Medication Guide provided by your pharmacist before you start taking brexpiprazole and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with or without food as directed by your doctor, usually once daily. The dosage is based on your medical condition, response to treatment, and other drugs you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).To reduce your risk of side effects, your doctor may direct you to start this medication at a low dose and gradually increase your dose. Follow your doctor's instructions carefully.Take this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.Continue taking this medication exactly as prescribed, even if you are feeling better and thinking more clearly. Do not increase your dose or take this drug more often than prescribed. Your symptoms will not improve any faster, and your risk of side effects will increase. Do not stop taking this medication without consulting your doctor.Tell your doctor if you do not get better or if you get worse. It may take several weeks before you feel the full benefit of this medication. SIDE EFFECTS: See also Warning section.Drowsiness, dizziness, lightheadedness, shaking, increased appetite, weight gain, restlessness, and inability to keep still may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.This medication may cause a serious drop in blood pressure, especially after starting or increasing your dose of this medication. Dizziness and lightheadedness can increase the risk of falling. Get up slowly when rising from a sitting or lying position.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: trouble swallowing, fainting, interrupted breathing during sleep, unusual strong urges (such as increased gambling, increased sexual urges).Brexpiprazole may rarely cause a condition known as tardive dyskinesia. In some cases, this condition may be permanent. Tell your doctor right away if you develop any unusual/uncontrolled movements (especially of the face, lips, mouth, tongue, arms, or legs).This medication may rarely make your blood sugar rise, which can cause or worsen diabetes. Tell your doctor right away if you have symptoms of high blood sugar such as increased thirst/urination. If you already have diabetes, check your blood sugar regularly as directed and share the results with your doctor. Your doctor may need to adjust your diabetes medication, exercise program, or diet.This drug may also cause weight gain and a rise in your blood cholesterol (or triglyceride) levels. These effects, along with diabetes, may increase your risk for developing heart disease. Discuss the risks and benefits of treatment with your doctor.Rarely, this medication may increase your blood level of a certain hormone (prolactin). In females, an increase in prolactin levels may result in unwanted breast milk, missed/stopped periods, or difficulty becoming pregnant. In males, it may result in decreased sexual ability, inability to produce sperm, or enlarged breasts. If you develop any of these symptoms, tell your doctor right away.Get medical help right away if you have any very serious side effects, including: seizure.This medication may rarely cause a very serious condition called neuroleptic malignant syndrome (NMS). Get medical help right away if you have any of the following symptoms: fever, muscle stiffness/pain/tenderness/weakness, severe tiredness, severe confusion, sweating, fast/irregular heartbeat, dark urine, signs of kidney problems (such as change in the amount of urine).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345. PRECAUTIONS: See also Warning section.Before taking brexpiprazole, 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: kidney problems, liver problems, personal or family history of diabetes, high cholesterol/triglyceride levels, heart problems, seizures, stroke, trouble swallowing, low white blood cell count, breathing trouble during sleep (sleep apnea).This drug may make you dizzy or drowsy. Alcohol or marijuana (cannabis) can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Avoid alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).This medication may make you sweat less, making you more likely to get heat stroke. Avoid doing things that may cause you to overheat, such as hard work or exercise in hot weather, or using hot tubs. When the weather is hot, drink a lot of fluids and dress lightly. If you overheat, quickly look for a place to cool down and rest. Get medical help right away if you have a fever that does not go away, mental/mood changes, headache, or dizziness.Older adults may be more sensitive to the side effects of this drug, especially drowsiness, dizziness, and lightheadedness. Drowsiness, dizziness, and lightheadedness can increase the risk of falling.During pregnancy, this medication should be used only when clearly needed. Babies