Abilify Maintena

Name: Abilify Maintena

Uses For Abilify Maintena

Aripiprazole injection is used to treat agitation caused by schizophrenia or bipolar mania.

Aripiprazole extended-release injection is used to treat schizophrenia (a mental disorder). It works in the brain to change how certain chemicals affect patients. Aripiprazole is an antipsychotic agent.

This medicine is available only with your doctor's prescription.

Precautions While Using Abilify Maintena

It is very important that your doctor check your progress at regular visits to allow for changes in your dose and help reduce any unwanted effects. Blood and urine tests may be needed to check for unwanted effects.

This medicine may increase risk for stroke in elderly patients with dementia. Tell your doctor right away if you have confusion, difficulty in speaking, slow speech, inability to speak, inability to move the arms, legs, or facial muscles, double vision, or headache while using this medicine.

This medicine may affect blood sugar levels. If you are diabetic and notice a change in the results of your blood or urine sugar tests, check with your doctor.

This medicine may add to the effects of alcohol and other medicines that make you drowsy or less alert. Some examples of these medicines are antihistamines or medicines for hay fever, allergies, or colds, sedatives, tranquilizers, or sleeping medicines, prescription pain medicines or narcotics, medicines for seizures or barbiturates, muscle relaxants, or anesthetics (medicines that numb), including some dental anesthetics. If you are taking any of these medicines, make sure you tell your doctor before you receive aripiprazole injection.

Aripiprazole may cause drowsiness, trouble with thinking, or trouble with controlling movements. Make sure you know how you react to this medicine before you drive, use machines, or do other jobs that require you to be alert, well-coordinated, or able to think well.

Check with your doctor right away if you have any of the following symptoms while using this medicine: convulsions (seizures), difficulty with breathing, a fast heartbeat, a high fever, high or low blood pressure, increased sweating, loss of bladder control, severe muscle stiffness, unusually pale skin, or tiredness. These could be symptoms of a serious condition called neuroleptic malignant syndrome (NMS).

This medicine may cause tardive dyskinesia (a movement disorder). Check with your doctor right away if you have any of the following symptoms while using this medicine: lip smacking or puckering, puffing of the cheeks, rapid or worm-like movements of the tongue, uncontrolled chewing movements, or uncontrolled movements of the arms and legs.

Some people who have used this medicine had unusual changes in their behavior. Talk with your doctor right away if you start having unusual urges, such as gambling urges, binge or compulsive eating, compulsive shopping, or sexual urges while using this medicine.

Dizziness, lightheadedness, or fainting may occur, especially when you get up suddenly from a lying or sitting position. Getting up slowly may help. If this problem continues or gets worse, check with your doctor.

This medicine may make it more difficult for your body to cool down. It might reduce how much you sweat. Your body could get too hot if you do not sweat enough. If your body gets too hot, you might feel dizzy, weak, tired, or confused. Avoid places that are very hot. Call your doctor if drinking cool water and moving away from the heat does not cool you down.

This medicine can temporarily lower the number of white blood cells in your blood, increasing the chance of getting an infection. If you can, avoid people with infections. Check with your doctor immediately if you think you are getting an infection or if you get a fever or chills, cough or hoarseness, lower back or side pain, or painful or difficult urination.

This medicine may increase your weight. Your doctor may need to check your weight on a regular basis while you are using this medicine.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines) and herbal or vitamin supplements.

What do I need to tell my doctor BEFORE I take Abilify Maintena?

  • If you have an allergy to aripiprazole or any other part of Abilify Maintena.
  • If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
  • If you are breast-feeding or plan to breast-feed.

This medicine may interact with other drugs or health problems.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take this medicine with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

Contraindications

Abilify Maintena is contraindicated in patients with a known hypersensitivity to aripiprazole. Hypersensitivity reactions ranging from pruritus/urticaria to anaphylaxis have been reported in patients receiving aripiprazole [see ADVERSE REACTIONS (6.1 and 6.2)].

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

Carcinogenesis

Lifetime carcinogenicity studies were conducted in ICR mice, Sprague-Dawley (SD) rats, and F344 rats. Aripiprazole was administered for 2 years in the diet at doses of 1, 3, 10, and 30 mg/kg/day to ICR mice and 1, 3, and 10 mg/kg/day to F344 rats (0.2 to 5 times and 0.3 to 3 times the maximum recommended human dose [MRHD] based on mg/m2, respectively). In addition, SD rats were dosed orally for 2 years at 10, 20, 40, and 60 mg/kg/day (3 to 19 times the MRHD based on mg/m2). Aripiprazole did not induce tumors in male mice or male rats. In female mice, the incidences of pituitary gland adenomas and mammary gland adenocarcinomas and adenoacanthomas were increased at dietary doses of 3 to 30 mg/kg/day (0.1 to 0.9 times human exposure at MRHD based on AUC and 0.5 to 5 times the MRHD based on mg/m2). In female rats, the incidence of mammary gland fibroadenomas was increased at a dietary dose of 10 mg/kg/day (0.1 times human exposure at MRHD based on AUC and 3 times the MRHD based on mg/m2); and the incidences of adrenocortical carcinomas and combined adrenocortical adenomas/carcinomas were increased at an oral dose of 60 mg/kg/day (14 times human exposure at MRHD based on AUC and 19 times the MRHD based on mg/m2).

Proliferative changes in the pituitary and mammary gland of rodents have been observed following chronic administration of other antipsychotic agents and are considered prolactin-mediated. Serum prolactin was not measured in the aripiprazole carcinogenicity studies. However, increases in serum prolactin levels were observed in female mice in a 13-week dietary study at the doses associated with mammary gland and pituitary tumors. Serum prolactin was not increased in female rats in 4-week and 13-week dietary studies at the dose associated with mammary gland tumors. The relevance for human risk of the findings of prolactin-mediated endocrine tumors in rodents is unknown.

Mutagenesis

The mutagenic potential of aripiprazole was tested in the in vitro bacterial reverse-mutation assay, the in vitro bacterial DNA repair assay, the in vitro forward gene mutation assay in mouse lymphoma cells, the in vitro chromosomal aberration assay in Chinese hamster lung (CHL) cells, the in vivo micronucleus assay in mice, and the unscheduled DNA synthesis assay in rats. Aripiprazole and a metabolite (2,3-DCPP) were clastogenic in the in vitro chromosomal aberration assay in CHL cells with and without metabolic activation. The metabolite, 2,3-DCPP, produced increases in numerical aberrations in the in vitro assay in CHL cells in the absence of metabolic activation. A positive response was obtained in the in vivo micronucleus assay in mice; however, the response was due to a mechanism not considered relevant to humans.

Impairment of Fertility

Female rats were treated with oral doses of 2, 6, and 20 mg/kg/day (0.6, 2, and 6 times the maximum recommended human dose [MRHD] on a mg/m2 basis) of aripiprazole from 2 weeks prior to mating through day 7 of gestation. Estrus cycle irregularities and increased corpora lutea were seen at all doses, but no impairment of fertility was seen. Increased pre-implantation loss was seen at 6 and 20 mg/kg/day and decreased fetal weight was seen at 20 mg/kg/day.

Male rats were treated with oral doses of 20, 40, and 60 mg/kg/day (6, 13, and 19 times the MRHD on a mg/m2 basis) of aripiprazole from 9 weeks prior to mating through mating. Disturbances in spermatogenesis were seen at 60 mg/kg and prostate atrophy was seen at 40 and 60 mg/kg, but no impairment of fertility was seen.

Animal Toxicology and/or Pharmacology

Oral Aripiprazole

Aripiprazole produced retinal degeneration in albino rats in a 26-week chronic toxicity study at a dose of 60 mg/kg and in a 2-year carcinogenicity study at doses of 40 and 60 mg/kg. The 40 and 60 mg/kg/day doses are 13 and 19 times the maximum recommended human dose (MRHD) based on mg/m2 and 7 to 14 times human exposure at MRHD based on AUC. Evaluation of the retinas of albino mice and of monkeys did not reveal evidence of retinal degeneration. Additional studies to further evaluate the mechanism have not been performed. The relevance of this finding to human risk is unknown.

Intramuscular Aripiprazole

The toxicological profile for aripiprazole administered to experimental animals by intramuscular injection is generally similar to that seen following oral administration at comparable plasma levels of the drug. With intramuscular injection, however, injection-site tissue reactions are observed that consist of localized inflammation, swelling, scabbing and foreign-body reactions to deposited drug. These effects gradually resolved with discontinuation of dosing.

After 26 weeks of treatment in rats, the no-observed-adverse-effect level (NOAEL) was 50 mg/kg in male rats and 100 mg/kg in female rats, which are approximately 1 and 2 times, respectively, the maximum recommended human 400 mg dose of aripiprazole extended-release injectable suspension on a mg/m2 body surface area. At the NOAEL in rats, the AUC7d values were 14.4 µg∙h/mL in males and 104.1 µg∙h/mL in females. In dogs at 52 weeks of treatment at the NOAEL of 40 mg/kg, which is approximately 3 times the MRHD (400 mg) on a mg/m2 body surface area, the AUC7d values were approximately 59 µg∙h/mL in males and 44 µg∙h/mL in females. In patients at the MRHD of 400 mg, the AUCτ (0-28 days) was 163 µg∙h/mL. For comparison to this human AUC, extrapolating the animal AUC7d values to an AUC28d results in AUC28d values of approximately 58 and 416 µg∙h/mL for male and female rats, respectively, and 236 and 175 µg∙h/mL for male and female dogs, respectively.

PRINCIPAL DISPLAY PANEL - 400 mg Vial Label

NDC 59148-019-70

Rx only

400 mg per vial

Abilify Maintena™ (aripiprazole)
for extended release injectable suspension
Single use only. Sterile. Discard any unused portion.
For deltoid or gluteal intramuscular injection only.
Usual Dosage: See package insert.

Manufactured by: Otsuka Pharmaceutical Co., Ltd.
Distributed and Marketed by: Otsuka America Pharmaceutical, Inc.
Marketed by: Lundbeck

Can aripiprazole long-acting injection cause problems?

Along with their useful effects, most medicines can cause unwanted side-effects although not everyone experiences them. The table below contains some of the most common ones associated with aripiprazole long-acting injection. You will find a full list in the manufacturer's information leaflet supplied with your medicine. The unwanted effects often improve as your body adjusts to the new medicine, but speak with your doctor or pharmacist if any of the following continue or become troublesome.

Common aripiprazole long-acting injection side-effects
(these affect less than 1 in 10 people)
What can I do if I experience this?
Feeling dizzy, tired or sleepyDo not drive or use tools or machines. Do not drink alcohol
HeadacheAsk your pharmacist to recommend a suitable painkiller
Feeling shaky or restless, unusual or uncontrollable movementsSpeak with your doctor. You may be able to take another medicine to help reduce these effects
Difficulties sleeping, feeling anxious, weight increase or weight loss, dry mouth, pain at the injection site, muscular stiffness, erectile dysfunctionDiscuss these with your doctor if any become troublesome
Changes to the results of some blood testsYour doctor will check for these

Important: if you experience symptoms such as muscle stiffness, a very high temperature, feeling confused, a fast heartbeat and sweating, you should contact your doctor immediately. These can be signs of a rare but serious condition known as neuroleptic malignant syndrome.

If you experience any other symptoms which you think may be due to the medicine, please speak with your doctor or pharmacist for further advice.

Abilify Maintena Drug Class

Abilify Maintena is part of the drug class:

  • Other antipsychotics

Abilify Maintena Food Interactions

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

Pharmacology

Mechanism of Action

Atypical antipsychotic; partial agonist at dopamine D2 and serotonin type 1 (5-HT1A) receptors; antagonist at serotonin type 2 (5-HT2A) receptor; also has alpha-blocking activity

Absorption

Bioavailability: 87% (tablet); 100% (IM)

Peak plasma time: 1-3 hr (IR); 5-7 hr (ER); 3-5 hr (tablet)

Distribution

Protein bound: 99%

Vd: 404 L (4.9 L/kg)

Metabolism

Metabolized by CYP2D6 and CYP3A4

Metabolites: Dehydroaripiprazole (40%)

Elimination

Half-life: 75 hr (parent drug); 94 hr (metabolite); 30-47 days (IM); 146 hr (poor metabolizers)

Excretion: Feces (55%), urine (25%)

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