aripiprazole


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aripiprazole

Abilify

Pharmacologic class: Quinolone-derived atypical antipsychotic agent

Therapeutic class: Antipsychotic, neuroleptic

Pregnancy risk category C

FDA Box Warning

• Drug increased mortality in elderly patients with dementia-related psychosis. Although causes of death were varied, most appeared to be cardiovascular or infectious. Drug isn't approved to treat dementia-related psychosis.

• Children, adolescents, and young adults taking antidepressants for major depressive disorder and other psychiatric disorders are at increased risk for suicidal thinking and behavior.

• Drug isn't approved for use in children with depression.

Action

Unclear. Thought to exert partial agonist activity at central dopamine D2 and type 1A serotonin (5-HT1A) receptors and antagonistic activity at serotonin 5-HT2A receptors. Also has alpha-adrenergic and histamine1-blocking properties.

Availability

Injection: 9.75 mg/1.3 ml (7.5 mg/ml)

Oral solution: 1 mg/ml

Tablets: 2 mg, 5 mg, 10 mg, 15 mg, 20 mg, 30 mg

Tablets (orally disintegrating): 10 mg, 15 mg

Indications and dosages

Schizophrenia

Adults: 10 to 15 mg P.O. daily. If needed, increase to 30 mg daily after 2 weeks.

Adolescents ages 13 to 17: Initially, 2 mg P.O. daily; increase to 5 mg P.O. after 2 days. Then increase to 10 mg P.O. after 2 additional days. Subsequent dosage intervals should occur in increments no greater than 5 mg, up to a maximum of 30 mg.

To maintain stability in schizophrenic patients

Adults: 15 mg P.O. daily. Therapy may continue for up to 26 weeks with periodic evaluations.

Adolescents ages 13 to 17: General recommendation, continue responding patients beyond the acute response but at the lowest dosage needed to maintain remission.

Acute manic and mixed episodes associated with bipolar disorder

Adults: 30 mg P.O. daily for up to 3 weeks

Agitation associated with schizophrenia or bipolar mania

Adults: Usual dosage, 5.25 to 15 mg I.M. as single dose. Recommended dosage is 9.75 mg I.M. as single dose. No additional benefit was demonstrated for 15 mg compared to 9.75 mg. Lower dosage of 5.25 mg may be considered when clinical factors warrant. If agitation warranting second dose persists following initial dose, cumulative dosages up to total of 30 mg/day may be given. However, efficacy of repeated doses in agitated patients hasn't been systematically evaluated in controlled clinical trials. Also, safety of total daily doses greater than 30 mg or injections given more frequently than every 2 hours hasn't been adequately evaluated in clinical trials. If ongoing aripiprazole therapy is clinically indicated, oral aripiprazole ranging from 10 to 30 mg/day P.O. should replace aripiprazole injection as soon as possible.

Adjunctive treatment of major depressive disorder

Adults: Initially, 2 to 5 mg P.O. daily. May increase up to 15 mg daily at increments of up to 5 mg/day at intervals of no less than 1 week.

Dosage adjustment

• Concurrent use of potent CYP3A4 inhibitors (such as ketoconazole), CYP2D6 inhibitors (such as fluoxetine, paroxetine, quinidine), or CYP3A4 inducers (such as carbamazepine)

Contraindications

• Hypersensitivity to drug

Precautions

Use cautiously in:

• cerebrovascular disease, hypotension, seizure disorder, suicidal ideation

• high risk for aspiration pneumonia

• neuroleptic malignant syndrome, tardive dyskinesia, diabetes mellitus

• leukopenia, neutropenia, agranulocytosis

• pregnant or breastfeeding patients

• elderly patients (with dementia-related psychosis)

• children, adolescents, and young adults with major depressive disorder

Administration

• Give with or without food.

• Don't administer with grapefruit juice.

• Be aware that oral solution may be substituted for tablets on a mg-to-mg basis up to 25-mg dose. Patients receiving 30 mg of tablets should receive 25 mg of oral solution.

Adverse reactions

CNS: dizziness, insomnia, akathisia, agitation, anxiety, headache, light-headedness, drowsiness, tremor, tardive dyskinesia, seizures, neuroleptic malignant syndrome, increased suicide risk

CV: orthostatic hypotension, hypertension, peripheral edema, chest pain, bradycardia, tachycardia

EENT: rhinitis

GI: nausea, vomiting, diarrhea, constipation, jaundice, abdominal pain, esophageal motility disorders, dysphagia

GU: urinary incontinence

Respiratory: cough

Skin: rash

Other: fever, hypersensitivity reactions (including anaphylaxis)

Interactions

Drug-drug. CNS depressants: increased sedation

Drugs that induce CYP3A4: decreased aripiprazole effect

Drugs that inhibit CYP3A4 or CYP2D6: serious toxic effects

Other antipsychotic agents: increased extrapyramidal effects

Drug-diagnostic tests. Granulocytes, leukocytes, neutrophils: decreased values

Serum glucose: increased level

Drug-herbs. Kava: increased CNS depression

Drug-behaviors. Alcohol use: increased sedation

Patient monitoring

Watch for signs and symptoms of depression, and evaluate patient for suicidal ideation.

• Monitor neurologic status closely. Watch for tardive dyskinesia.

Evaluate patient for neuroleptic malignant syndrome (fever, altered mental status, rigid muscles, arrhythmia, tachycardia, sweating). Stop drug and notify prescriber if these signs and symptoms occur.

• Monitor blood pressure, pulse, CBC with differential, and weight.

Monitor blood glucose level closely; be aware that in patients with diabetes mellitus or risk factors for diabetes, serious hyperglycemia possibly associated with coma or death may occur.

Patient teaching

Instruct patient to immediately contact prescriber if he experiences depression or has suicidal thoughts, altered mental status, rigid muscles, irregular heart beat, excessive sweating, rash, itching, difficulty breathing, or excessive thirst or urination.

• Inform patient that symptoms will subside slowly over several weeks.

• Tell patient he may take drug with or without food.

• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.

• Tell patient that drug may cause urinary incontinence.

• Caution patient to avoid strenuous exercise and hot environments whenever possible.

• Instruct patient to move slowly when rising to avoid dizziness from sudden blood pressure decrease.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, herbs, and behaviors mentioned above.

aripiprazole

(ā′rə-pĭp′rə-zōl′)
n.
An antipsychotic drug, C23H27Cl2N3O2, that functions as a partial dopamine receptor agonist and is used to treat schizophrenia, bipolar disorder, and, in combination with other drugs, depression.

aripiprazole

A dopamine partial agonist drug used to treat SCHIZOPHRENIA. Aripiprazole is a member of a new class of antipsychotic drugs with agonist properties in parts of the brain in which the local concentrations of dopamine is abnormally low and antagonist action in parts in which levels of dopamine are abnormally high. Extrapyramidal effects are said to be avoided. A brand name is ABILIFY.
References in periodicals archive ?
conclusion of non-exclusive discount agreements pursuant to section 130a (8) sgb v on medicines containing the active substance aripiprazole depot suspension for injection (atc: N05ax12) within the period from 1.5.2019 to 30.4.2021 with possibility of contract conclusion at any time (open-house model) ,
* Participants were randomly assigned to 1 of 3 groups: switching to bupropion (n = 511), augmenting with bupropion (n = 506), or augmenting with aripiprazole (n = 505).
Aripiprazole is associated with sedation, weight gain, and extrapyramidal symptoms.
The alternative formulation of the long-acting injectable is intended be used with a single 30-mg dose of oral aripiprazole and can be initiated on the first day of treatment, Alkermes stated.
The researchers found that from baseline to week 12, the dual-energy X-ray absorptiometry percentage total body fat increased by 1.18, 4.12, and 1.66 percent for risperidone, olanzapine, and aripiprazole, respectively, and was significantly greater for olanzapine than risperidone or aripiprazole.
Aripiprazole, ziprasidone, and risperidone during pregnancy was not associated with an increased risk of gestational diabetes.
We focus specifically on the uptake of aripiprazole when it was newly available in the Veterans Health Administration and prior to it being approved by the Food and Drug Administration for the treatment of bipolar mania in September of 2004.
Otsuka explains that the Abilify MyCite system includes Abilify MyCite, the MyCite[R] Patch (a wearable sensor, developed by Proteus); the MyCite[R] APP, a smartphone application, used with a compatible smartphone to display information for the patient; and web-based portals for healthcare providers and caregivers that display a summary of aripiprazole ingestion over time.
Aripiprazole is regarded as a second- or third-generation antipsychotic, mainly because it provides a control mechanism for the dopamine "see-saw".
Aripiprazole is an antipsychotic drug with a complex pharmacology.
Similar to the APA, the schizophrenia Patient Outcomes Research Team (PORT) recommends that patients with acute agitation be treated using an oral or intramuscular (IM) atypical antipsychotic such as olanzapine, ziprasidone, or aripiprazole, either as a monotherapy or with an adjunctive fast-acting benzodiazepine [36].
14 -- Ajanta Pharma Limited announces the receipt of final approval for Aripiprazole Tablets (2mg, 5mg, 10mg, 15mg, 20mg, 30mg), the bioequivalent generic to Abilify(R)1 from the US FDA*.