Overview
Agitation and aggression are challenging behaviors that can happen in people with dementia, especially in Alzheimer’s disease. It can cause you or your relative to act out in different ways. You may see differences in verbal aggression, physical aggression, or restlessness. Some people struggle to find the right treatment or combination of treatments to help make this agitation happen less often.
Antipsychotic medicines have been used for many years to treat mental health conditions but have a history of increased side effects, like tremors, rigid muscles, or weight gain. The newer second-generation antipsychotics block chemicals in the brain in a different way to help with symptoms but also reduce the risk of side effects. Rexulti was the first medicine approved by the FDA for reducing symptoms of agitation in dementia due to Alzheimer’s disease.
How Does the Medicine Work?
Rexulti is a third-generation antipsychotic medicine that works by increasing dopamine and serotonin levels in the brain. It may improve mood and behavior by blocking certain receptors in the brain that bind to the neurotransmitters serotonin and dopamine.
How Should I Take This Medicine?
Rexulti is an oral tablet that is taken once daily, with or without food. The starting dose is usually a half-milligram daily and is increased, depending on your response and other things, like drug interactions and liver or kidney function. The maximum dose is 3 milligrams each day.
Your health care provider will give you instructions on how to start and change doses. It is important to take Rexulti as prescribed by your health care provider. Taking the medicine daily will help balance symptoms to improve daily functions. It can take several weeks to start to see any improvement in symptoms. Consistent use is the key to seeing improvements over time.
What Studies Were Completed for Agitation in Alzheimer’s Disease Dementia?
Two 12-week studies were completed to see if Rexulti eased agitation in people who have Alzheimer’s disease dementia (ADD), when compared with placebo. Placebo-controlled studies help researchers see differences in benefit or harm of a medicine when compared to no treatment.
People in the studies had Alzheimer’s disease, moderate to severe decreases in cognition, and severe aggression or agitation that required treatment. A little more than half of the people were females and were living in a care facility. Almost all of the people were white (95%). The average age was 74.
Rexulti or placebo was started at a low dose and increased at specific times, based on the following.
- Study 1: Started at a quarter-milligram and increased up to 1 or 2 milligrams
- Study 2: Stared at a half-milligram and increased up to 2 or 3 milligrams
The effectiveness of Rexulti was measured using a scale that measures how often dementia-related symptoms happen. A higher score on the scale means more severe depression symptoms. A decrease in score over time indicates less frequent symptoms.
What Benefits Were Seen in the Studies?
In study 6, people taking 2 milligrams of Rexulti showed improvement in symptoms. In study 7, people taking either Rexulti dose showed improvement in symptoms. This means that people taking 2 or 3 milligrams of Rexulti had less frequent aggressive or agitated symptoms at the end of 12 weeks.
Scores in Agitation with Acute Dementia Due to Alzheimer’s Disease | ||||||
STUDY 6 |
| STUDY 7 | ||||
Placebo | Rexulti 1 mg | Rexulti 2 mg |
| Placebo | Rexulti 2 or 3 mg | |
| Beginning | 72.2 | 70.5 | 71.0 |
| 79.2 | 80.6 |
| At Week 12 | 54.4 | 52.9 | 49.4 |
| 61.9 | 58 |
| Total Change | -17.8 | -17.6 | -21.6 |
| -17.3 | -22.6 |
Your results may differ from what was seen in clinical studies. You and your provider should determine if the benefits outweigh any potential risks for your diagnosis.
How Will I Know That This Medication Is Working, and How Long Is Treatment?
After a few weeks to months, you should see less frequent signs of aggression or agitation and other improvements listed below.
- Decreased verbal agitation or physical aggression
- More cooperation with care, less pacing
- Improved sleep
- More engagement with activities
- Easier care management
For some people, this may mean that they are able to function better in daily activities. The changes can be gradual and take weeks to show, so it is important to track how your symptoms change over time. The length of treatment is different for each person. Some may see short-term use, while others find benefit in long-term therapy. Your health care provider will assess your symptoms based on the scales or scores used for your diagnosis. Your family or friends may also notice more engagement.
Do not stop taking Rexulti without talking with your health care provider, even if your symptoms have improved. If you stop, your symptoms may worsen or require further treatment.
Tell your health care provider if you do not think your symptoms are improving after a few months.
How Can I Prevent and Manage Side Effects?
The most common side effects of Rexulti are weight gain, sleepiness, dizziness, cold-like symptoms, and restlessness or fidgeting.
Antipsychotics may lead to weight gain, high blood pressure, diabetes, or high cholesterol. Your health care provider will monitor your weight, blood pressure, cholesterol level, hemoglobin A1c (a measure of blood sugar over time), and waist circumference. Healthy lifestyle choices such as exercising; controlling portion sizes; eating more vegetables, fruits and lean meats; and limiting unhealthy fats and salt may prevent weight gain. Short walks every day can be helpful for your weight and mental health. For more information on adopting a healthy lifestyle, visit the American Heart Association website at https://www.heart.org/en/.
Dizziness or sleepiness may cause falls. If you get dizzy, avoid sudden head movements or getting up quickly from a sitting or lying position. If you feel sleepy, try taking your dose in the evening, before bedtime. Avoid driving or doing other tasks or actions that require alertness until you know how Rexulti affects you.
You may have an inner feeling of restlessness (akathisia) that makes it hard to sit still or makes you fidget more. This is usually seen at the beginning of treatment and may decrease over time. Regular exercise, like walking, stretching, or doing light activities around the house, may help reduce this feeling. Find activities that calm your brain, like breathing exercises, meditation, light yoga, or spending time in nature. Caffeine may worsen jitteriness, so limit or avoid soda, tea, coffee, or other stimulants.
Rexulti may cause problems with body temperature, making it difficult for your body to cool down (heat intolerance). Heavy exercise, extreme heat, dehydration, and certain medicines may worsen heat intolerance. Wearing lightweight clothing, staying hydrated, avoiding extreme heat, and exercising in cooler temperatures are some ways to help prevent heat intolerance.
While not common with Rexulti, antipsychotics may lead to belly pain or indigestion, nausea, vomiting, constipation, or dry mouth. Eating smaller or lighter meals or taking Rexulti with food may help reduce these effects. If you have a dry mouth, try sipping water frequently, sucking on ice, chewing sugar-free gum, or sucking on sugar-free candy. If you get constipated, drink plenty of water throughout the day; include high-fiber foods in your diet, like wheat, corn, bran, beans, and prunes; and avoid foods and drinks like tea, cheese, chocolate, unripe bananas, and white rice.
If your side effects get worse or don’t let up, talk with your health care provider.
These are not all of the possible side effects. Talk with your health care provider if you are having symptoms that bother you. In the U.S., you can report side effects to the FDA at www.fda.gov/medwatch or by calling 800-FDA-1088 (800-332-1088). In Canada, you can report side effects to Health Canada at www.health.gc.ca/medeffect or by calling 866-234-2345.
What Monitoring or Blood Tests May I Need Before Starting or During Treatment?
Your health care provider may do lab tests to monitor your health and see how your body responds to the medication. The following are key pieces of this monitoring.
- Weight at the start and changes in your weight during treatment
- Complete blood count (CBC), to monitor your red blood cells (RBCs), white blood count (WBC), and platelets, especially in people with a history of leukopenia, neutropenia, or agranulocytosis
- Fasting blood checks of your cholesterol, including total cholesterol, LDL cholesterol, HDL cholesterol, and triglycerides
- Fasting blood glucose or hemoglobin A1c, especially if you have a history or a risk of diabetes
- Blood pressure
- Magnesium levels
- Abnormal involuntary movement scale (AIMS), which is a tool that detects any changes in your movement or fidgeting, such as tardive dyskinesia
What Types of Interactions Can Happen?
Several medicines can affect the blood levels of Rexulti. This may increase the risk of side effects or can cause Rexulti to not work as well.
Your health care provider may lower the dose of Rexulti if you take the things listed below.
- Strong/moderate CYP3A4 inhibitors, which include ciprofloxacin (Cipro), clarithromycin (Biaxin), diltiazem (Cardizem), fluconazole (Diflucan), itraconazole (Sporanox, Tolsura), ketoconazole (Nizoral), and grapefruit juice
- Strong/moderate CYP2D6 inhibitors, which include bupropion (Wellbutrin, Zyban), cinacalcet (Sensipar), duloxetine (Cymbalta), fluoxetine (Prozac), mirabegron (Myrbetriq), paroxetine (Paxil), quinidine, and terbinafine (Lamisil)
Your health care provider may increase the dose of Rexulti if you take the things listed below.
- Strong CYP3A4 inducers, which include phenytoin (Dilantin, Phenytek, and others), rifampin, barbiturates (such as phenobarbital), or the supplement St. John’s wort
This is not a complete list of interactions. Tell your pharmacist or other health care provider about all the prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, or other supplements you take or have recently taken. This will help them find out if there are any interactions, or if you need a dose adjustment.
Is There Any Cost Assistance Available?
There is a copay program from the drugmaker that may allow you to pay $0 for your prescription. Whether you are eligible depends on whether you have prescription insurance and what type of insurance you have. You can find out more at https://www.rexulti.com/savings-cost, texting “SAVE” to 96747, and by calling 844-415-0674.
