Abilify – Flashcard

Abilify, Abilify Discmelt

aripiprazole (AR i PIP ra zole)

Classifications: Central nervous system (CNS) agent; psychotherapeutic; antipsychotic; atypical Therapeutic Class: Atypical antipsychotic DEA Class: Rx (prescription) Controlled Substance: Abilify is not a controlled substance. Pregnancy Class: C

(PO) Treatment of schizophrenia in adults and adolescents (13-17 yrs of age). Acute treatment of manic and mixed episodes associated with bipolar I disorder, as monotherapy in adults and pediatric patients (10-17 yrs of age) and as an adjunct to lithium or valproate in adults. Maintenance treatment of bipolar I disorder, both as monotherapy and adjunct to either lithium or valproate, in adults. Adjunctive therapy to antidepressants for treatment of MDD in adults. Treatment of irritability associated with autistic disorder in pediatric patients (6-17 yrs of age). (Inj) Acute treatment of agitation associated with schizophrenia or bipolar disorder, manic or mixed, in adults.

What is Abilify? - Abilify (aripiprazole) is an antipsychotic medication. It works by changing the actions of chemicals in the brain. - Abilify is used to treat the symptoms of psychotic conditions such as schizophrenia and bipolar disorder (manic depression). It is also used together with other medications to treat major depressive disorder in adults. - Abilify is also used to treat irritability and symptoms of aggression, mood swings, temper tantrums, and self-injury related to autistic disorder in children who are at least 6 years old. Important information: - Abilify is not approved for use in psychotic conditions that are related to dementia. Abilify may increase the risk of death in older adults with dementia-related conditions. - Some young people have thoughts about suicide when taking medicine for a major depressive disorder and other psychiatric disorders. Your doctor will need to check your progress at regular visits while you are using Abilify. Your family or other caregivers should also be alert to changes in your mood or symptoms. - Stop using Abilify and call your doctor at once if you have the following symptoms: fever with stiff muscles and rapid heart rate; uncontrolled muscle movements; symptoms that come on suddenly such as numbness or weakness, severe headache, and problems with vision, speech, or balance.

- Abilify is not approved for use in psychotic conditions that are related to dementia. Abilify may cause heart failure, sudden death, or pneumonia in older adults with dementia-related conditions. - You should not take Abilify if you are allergic to aripiprazole. To make sure this medicine is safe for you, tell your doctor if you have: - liver or kidney disease - heart disease, high or low blood pressure, heart rhythm problems - high cholesterol or triglycerides (a type of fat in the blood) - a history of low white blood cell (WBC) counts - a history of heart attack or stroke - a history of breast cancer - seizures or epilepsy - a personal or family history of diabetes - trouble swallowing - Some young people have thoughts about suicide when taking medicine for a major depressive disorder and other psychiatric disorders. Your doctor will need to check your progress at regular visits while you are using Abilify. Your family or other caregivers should also be alert to changes in your mood or symptoms. - The liquid form (oral solution) of this medication may contain up to 15 grams of sugar per dose. Before taking the oral solution, tell your doctor if you have diabetes. - Abilify may cause you to have high blood sugar (hyperglycemia). Talk to your doctor if you have any signs of hyperglycemia such as increased thirst or urination, excessive hunger, or weakness. If you are diabetic, check your blood sugar levels on a regular basis while you are taking Abilify. - The orally disintegrating tablet form of this medication may contain over 3 milligrams of phenylalanine per tablet. Before taking Abilify Discmelt, tell your doctor if you have phenylketonuria. - FDA pregnancy category C. Tell your doctor if you are pregnant or plan to become pregnant during treatment. - Taking antipsychotic medication during the last 3 months of pregnancy may cause problems in the newborn, such as withdrawal symptoms, breathing problems, feeding problems, fussiness, tremors, and limp or stiff muscles. However, you may have withdrawal symptoms or other problems if you stop taking your medicine during pregnancy. If you become pregnant while taking Abilify, do not stop taking it without your doctor's advice. - Aripiprazole can pass into breast milk and may harm a nursing baby. You should not breast-feed while using this medicine.

Take Abilify exactly as prescribed by your doctor. Follow all directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results. Do not take this medicine in larger or smaller amounts or for longer than recommended. - Do not take this medicine for longer than 6 weeks unless your doctor has told you to. - Abilify can be taken with or without food. - Measure liquid medicine with a special dose-measuring spoon or medicine cup. If you do not have a dose-measuring device, ask your pharmacist for one. To take the orally disintegrating tablet (Abilify Discmelt): - Keep the tablet in its blister pack until you are ready to take it. Open the package and peel back the foil. Do not push a tablet through the foil or you may damage the tablet. - Use dry hands to remove the tablet and place it in your mouth. - Do not swallow the tablet whole. Allow it to dissolve in your mouth without chewing. If desired, you may drink liquid to help swallow the dissolved tablet. - Use Abilify regularly to get the most benefit. Get your prescription refilled before you run out of medicine completely. - Your doctor will need to check your progress while you are using this medicine. - Store at room temperature away from moisture and heat. Abilify oral solution may be used for up to 6 months after opening, but not after the expiration date on the medicine label.

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222 FREE. Overdose symptoms may include drowsiness, vomiting, aggression, confusion, tremors, fast or slow heart rate, seizure (convulsions), trouble breathing, or fainting.

- This medication may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert. - Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Get up slowly and steady yourself to prevent a fall. - Drinking alcohol can increase certain side effects of Abilify. - Avoid becoming overheated or dehydrated. Drink plenty of fluids, especially in hot weather and during exercise. It is easier to become dangerously overheated and dehydrated while you are taking Abilify.

Adult Dosage: Schizophrenia: - Initial/Target: 10mg or 15mg qd - Titrate: Should not increase dose before 2 weeks - Usual: 10-30mg/day - Reassess periodically to determine the need for maintenance treatment Bipolar I Disorder: Acute Treatment of Manic and Mixed Episodes, Both as Monotherapy and as an Adjunct to Lithium or Valproate: - Initial: 15mg qd (monotherapy), 10-15mg qd (adjunct) - Target: 15mg qd - Titrate: May increase to 30mg/day based on clinical response - Max: 30mg/day - Reassess periodically to determine the need for maintenance treatment Major Depressive Disorder: Adjunctive Therapy to Antidepressants: - Initial: 2-5mg/day - Titrate: Dose adjustments of up to 5mg/day should occur gradually at intervals of no <1 week - Usual: 2-15mg/day - Reassess periodically to determine the need for maintenance treatment Agitation: Acute Agitation Associated w/ Schizophrenia or Bipolar Disorder, Manic or Mixed: - Inj: - Usual: 9.75mg IM - Effective Range: 5.25-15mg A lower dose of 5.25mg may be considered when clinical factors warrant. If agitation warranting a 2nd dose persists following the initial dose, cumulative doses of up to a total of 30mg/day may be given - Max: 30mg/day. Not more frequent than q2h - If ongoing treatment is clinically indicated, replace w/ PO at 10-30mg/day as soon as possible Pediatric Dosage: Schizophrenia: 13-17 Years: - Initial: 2mg/day - Titrate: May increase to 5mg/day after 2 days and to the target dose of 10mg/day after 2 additional days. Subsequent dose increases, if needed, should be administered in 5mg increments - Max: 30mg/day - Reassess periodically to determine the need for maintenance treatment Bipolar I Disorder: Acute Treatment of Manic and Mixed Episodes, Both as Monotherapy and as an Adjunct to Lithium or Valproate: 10-17 Years: - Initial: 2mg/day - Titrate: May increase to 5mg/day after 2 days and to the target dose of 10mg/day after 2 additional days. Subsequent dose increases, if needed, should be administered in 5mg increments - Max: 30mg/day - Reassess periodically to determine the need for maintenance treatment Irritability: Associated w/ Autistic Disorder: 6-17 Years: - Initial: 2mg/day - Titrate: Increase to 5mg/day May increase to 10mg or 15mg/day if needed Dose adjustments of up to 5mg/day should occur gradually at intervals of no <1 week - Usual: 5-15mg/day - Reassess periodically to determine the need for maintenance treatment Dose Modification: - Concomitant Medications Strong CYP3A4 or Potential CYP2D6 Inhibitors: Reduce to 1/2 the usual dose; when CYP3A4 or 2D6 inhibitor is withdrawn from combination therapy, increase the aripiprazole dose - Potential CYP2D6 Inhibitors in Patient w/ Major Depressive Disorder: Administer w/o dose adjustment - Strong CYP3A4 and CYP2D6 Inhibitors: Reduce to 1/4 of the usual dose; when CYP3A4 and CYP2D6 inhibitors are withdrawn from combination therapy, increase the aripiprazole dose - Strong, Moderate or Weak CYP3A4, and CYP2D6 Inhibitors: Initial: Reduce to 1/4 of usual dose Titrate: Adjust to achieve a favorable clinical response - Potential CYP3A4 Inducers: Double aripiprazole dose and base additional dose increases on clinical evaluation; when CYP3A4 inducer is withdrawn from therapy, reduce aripiprazole dose to 10-15mg - Other Important Modifications Poor CYP2D6 Metabolizer Patients: Initial: Reduce to 1/2 or 1/4 (on strong CYP3A4 inhibitor) of usual dose Titrate: Adjust to achieve a favorable clinical response Administration: Oral/IM route - PO: Administer w/o regard to meals Oral sol can be substituted for tabs on a mg-per-mg basis up to 25mg Patients receiving 30mg tabs should receive 25mg of oral sol - Inj: Inject slowly, deep into the muscle mass Availability/How Supplied: Inj: 7.5mg/mL [1.3mL]; Sol: 1mg/mL [150mL] Tab: 2mg, 5mg, 10mg, 15mg, 20mg, 30mg Tab, Disintegrating: (Discmelt) 10mg, 15mg

- History of seizures or conditions that lower seizure threshold (e.g., Alzheimer's dementia); suicidal ideation; brain tumor; dementia; diabetes mellitus; patients with known cardiovascular disease (history of MI or ischemic heart disease, heart failure, or conduction abnormalities), cerebrovascular disease, or conditions that predispose to hypotension (dehydration, hypovolemia, and treatment with antihypertensive medications); dysphagia; ethanol intoxication; hyperglycemia, hypothermia; obesity, elderly, children. - Hypersensitivity to aripiprazole; lactation; pregnancy (category C)

- Body as a Whole: Headache, asthenia, fever, flu-like symptoms, peripheral edema, chest pain, neck pain, neck rigidity. - CNS: Anxiety, insomnia, lightheadedness, somnolence, akathisia, tremor, extrapyramidal symptoms, depression, nervousness, increased salivation, hostility, suicidal thought, manic reaction, abnormal gait, confusion, cogwheel rigidity. - CV: Hypertension, tachycardia, hypotension, bradycardia. Risk of stroke in elderly with dementia-related psychosis. - GI: Nausea, vomiting, constipation, anorexia. - Hematologic: Ecchymosis, anemia. - Metabolic: Weight gain, weight loss, hyperglycemia, diabetes mellitus, increased creatine kinase. - Musculoskeletal: Muscle cramp. - Respiratory: Rhinitis, cough. Skin: Rash. - Special Senses: Blurred vision.

Get emergency medical help if you have any of these signs of an allergic reaction to Abilify: hives; difficult breathing; swelling of your face, lips, tongue, or throat. Stop using Abilify and call your doctor at once if you have: - very stiff (rigid) muscles, high fever, sweating, confusion, fast or uneven heartbeats, tremors, feeling like you might pass out - severe agitation, distress, or restless feeling - twitching or uncontrollable movements of your eyes, lips, tongue, face, arms, or legs - mask-like appearance of the face, trouble swallowing, problems with speech - seizure (convulsions) - thoughts about suicide or hurting yourself - low blood cell counts--sudden weakness or ill feeling, fever, chills, sore throat, swollen gums, painful mouth sores, red or swollen gums, skin sores, cold or flu symptoms, cough, trouble breathing - high blood sugar--increased thirst, increased urination, hunger, dry mouth, fruity breath odor, drowsiness, dry skin, weight loss Common Abilify side effects may include: - weight gain - blurred vision - drooling - dizziness, drowsiness - sleep problems (insomnia) This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 FREE.

- Drug: Carbamazepine will decrease aripiprazole levels (may need to double aripiprazole dose); ketoconazole, quinidine, fluoxetine, paroxetine may increase aripiprazole levels (reduce dose by ½); may enhance effects of antihypertensive agents. - Herbal: St. John's wort may decrease aripiprazole levels. - Food: High fat meals may delay time to peak plasma levels.

Taking this medicine with other drugs that make you sleepy can worsen this effect. Ask your doctor before taking Abilify with a sleeping pill, narcotic pain medicine, muscle relaxer, or medicine for anxiety, depression, or seizures. Many other drugs can interact with aripiprazole. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed here. Tell your doctor about all your medications and any you start or stop using during treatment with this medicine.

Aripiprazole has not been systematically studied in humans for its potential for abuse, tolerance, or physical dependence. In physical dependence studies in monkeys, withdrawal symptoms were observed upon abrupt cessation of dosing. While the clinical trials did not reveal any tendency for any drug-seeking behavior, these observations were not systematic and it is not possible to predict on the basis of this limited experience the extent to which a CNS-active drug will be misused, diverted, and/or abused once marketed. Consequently, patients should be evaluated carefully for a history of drug abuse, and such patients should be observed closely for signs of Abilify misuse or abuse (e.g., development of tolerance, increases in dose, drug-seeking behavior).

Monitor for clinical worsening of depression, suicidality, unusual changes in behavior, NMS, TD, hyperglycemia, orthostatic hypotension, seizures/convulsions, esophageal dysmotility, aspiration, and other adverse effects. Monitor CBC frequently in patients with preexisting low WBC counts or drug-induced leukopenia/neutropenia. Monitor for fever or other signs/symptoms of infection in patients with neutropenia. Monitor weight regularly and FPG in patients with DM or at risk for DM periodically during therapy. Periodically reassess to determine the continued need for maintenance treatment.

Partial D2/5HT1A agonist/5HT2A antagonist; not established.

Aripiprazole is a psychotropic agent belonging to the chemical class of benzisoxazole derivatives and is indicated for the treatment of schizophrenia. Aripiprazole is a selective monoaminergic antagonist with high affinity for the serotonin Type 2 (5HT2), dopamine Type 2 (D2), 1 and 2 adrenergic, and H1 histaminergic receptors. Aripiprazole acts as an antagonist at other receptors, but with lower potency. Antagonism at receptors other than dopamine and 5HT2 with similar receptor affinities may explain some of the other therapeutic and side effects of Aripiprazole. Aripiprazole's antagonism of histamine H1 receptors may explain the somnolence observed with this drug. Aripiprazole's antagonism of adrenergic a1 receptors may explain the orthostatic hypotension observed with this drug.

Aripiprazole exhibits high affinity for dopamine D2 and D3, serotonin 5-HT1A and 5-HT2A receptors (Ki values of 0.34 nM, 0.8 nM, 1.7 nM, and 3.4 nM, respectively), moderate affinity for dopamine D4, serotonin 5-HT2C and 5-HT7, alpha1-adrenergic and histamine H1 receptors (Ki values of 44 nM, 15 nM, 39 nM, 57 nM, and 61 nM, respectively), and moderate affinity for the serotonin reuptake site (Ki=98 nM). Aripiprazole has no appreciable affinity for cholinergic muscarinic receptors (IC50>1000 nM). Aripiprazole functions as a partial agonist at the dopamine D2 and the serotonin 5-HT1A receptors, and as an antagonist at serotonin 5-HT2A receptor.

- Absorption: Well absorbed, 87% bioavailable. - Peak: 3-5 h. - Metabolism: Metabolized in liver by CYP3A4 and 2D6. Major metabolite, dehydroaripiprazole has some activity. - Elimination: 55% excreted in feces, 25% in urine. - Half-Life: 75 h (94 h for metabolite).

25°C (77°F); excursions permitted to 15-30°C (59-86°F). Oral Sol: May be used for ≤6 months after opening. Inj: Store in original container; protect from light.

The most favorable course of action is to use an alternative chemical product with less inherent propensity for occupational exposure or environmental contamination. Recycle any unused portion of the material for its approved use or return it to the manufacturer or supplier. Ultimate disposal of the chemical must consider: the material's impact on air quality; potential migration in soil or water; effects on animal, aquatic, and plant life; and conformance with environmental and public health regulations.

Inform about the risks and benefits of treatment. Instruct patients, families, and caregivers to be alert to the emergence of anxiety, agitation, panic attacks, insomnia, irritability, hostility, aggressiveness, impulsivity, akathisia, hypomania, mania, other unusual changes in behavior, worsening of depression, and suicidal ideation; advise to contact physician if these symptoms occur. Instruct to use caution when operating hazardous machinery and to avoid alcohol use while on therapy. Counsel to avoid overheating and dehydration. Advise to notify physician if patient becomes pregnant or intends to become pregnant during therapy, and if patient is taking or plans to take any prescription or OTC drugs. Instruct to not breastfeed during therapy. (Discmelt) Inform phenylketonurics that product contains phenylalanine. Instruct to not open blister until ready to administer. Instruct that drug is to be taken without liquid. However, if needed, drug can be taken with liquid. Advise not to split the tab. (Sol) Inform that sol contains sucrose and fructose.

Assessment & Drug Effects: - Monitor diabetics for loss of glycemic control. - Monitor cardiovascular status. Assess for and report orthostatic hypotension. Take BP supine then in sitting position. Report systolic drop of >15-20 mm Hg. Patients at increased risk are those who are dehydrated, hypovolemic, or receiving concurrent antihypertensive therapy. - Monitor body temperature in situations likely to elevate core temperature (e.g., exercising strenuously, exposure to extreme heat, receiving drugs with anticholinergic activity, or being subject to dehydration). - Monitor for and report signs of tardive dyskinesia. - Monitor for and immediately report S&S of neuroleptic malignant syndrome (NMS) that include: hyperpyrexia, muscle rigidity, altered mental status, irregular pulse or blood pressure, tachycardia, diaphoresis, and cardiac dysrhythmia. Withhold drug if NMS is suspected. - Lab tests: Monitor periodically Hct & Hgb. Monitor periodically blood glucose. Monitor for elevated CPK and myoglobinuria if NMS is suspected. Additional Assessment: - Assess for dementia-related psychosis - Drug hypersensitivity - Psychiatric disorders or any other conditions where treatment is cautioned - Pregnancy/nursing status, and possible drug interactions - Obtain baseline FPG in patients with DM or at risk for DM - Obtain baseline CBC if at risk for leukopenia/neutropenia Patient & Family Education: - Carefully monitor blood glucose levels if diabetic. - Do not drive or engage in other potentially hazardous activities until reaction to drug is known. - Avoid situations where you are likely to become overheated or dehydrated. - Notify physician if you become pregnant or intend to become pregnant while taking this drug. - Do not breast feed while taking this drug.