Aripiprazole
Tranquilizer, Sedative/Hypnotic · Dopamine partial agonist
Indications
Schizophrenia.
Dosage
Adults: Schizophrenia: Initial/Target: 10-15 mg daily. Titrate: Should not increase before 2 wk. Maintenance: Periodically reassess need for therapy. Adjust dose with CYP3A4 inducers or inhibitors, or with CYP2D6 inhibitors. Bipolar Disorder: Acute Manic or Mixed Episodes: Initial: 30 mg daily. Titrate: May decrease to 15 mg every day based on tolerability. Adjust dose with CYP450 3A4 inducers or inhibitors, or with CYP450 2D6 inhibitors. Children: Treatment of mania: 13-18 yr, initially 2 mg once daily for 2 days, increased to 5 mg once daily for 2 days, thereafter increased to usual dose of 10 mg once daily; further increased if necessary in steps of 5 mg to max 30 mg daily, max duration of treatment 12 wk. Schizophrenia: 15-18 yr, initially 2 mg once daily for 2 days, increased to 5 mg once daily for 2 days, thereafter increased to 10 mg once daily; further increased if necessary in…
Adverse Effects
Insomnia, restlessness, headache, dizziness, akathisia, somnolence, tremor, blurred vision, GI upset, asthaenia. Stroke, TIA in elderly demented patients, diabetes, anxiety, restlessness, extrapyramidal disorder, sedation, salivary hypersecretion, fatigue. Reports of orthostatic hypotension, cardiac rhythm disorders, wt changes, increased creatine kinase, dysphagia. In adolescents: Wt loss, blood insulin increased, arrhythmia, leucopenia, low serum prolactin.
Risk Factor (Pregnancy/Lactation)
Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Precautions: Severe hepatic impairment. Cardiovascular or cerebrovascular disease, incl history of QT prolongation or predisposing factors for hypo- or hypertension. Monitor high risk patients for suicidal behaviour. Risk factors for VTE. Tardive dyskinesia; reduce dose or discontinue. Signs of neuroleptic malignant syndrome. History of seizures, diabetes. Monitor for impulse control disorders incl pathological gambling, hypersexuality, compulsive spending or eating. Hyperglycaemia. Monitor wt gain in adolescents. Aspiration pneumonia. Elderly.
Interactions
Potent inhibitors of CYP3A4 or 2D6. Potent inducers of CYP3A4. Alpha blockers, alcohol, CNS drugs. Drugs that prolong QT interval, other antihypertensives, serotonergic agents, stimulants.
Advice to Patient
Take with or without meals. Take at the same time each day. Open the blister pack of disintegrating tablets only when you are ready to take the tablet. Peel back the foil and do not push tablet through the foil because doing so could damage the tablet. Place the tablet on tongue without breaking it and let it dissolve. If needed, you may take a drink. Contact prescriber if there is change in vision, constant abdominal discomfort, muscle or skeletal pain, chest pain or palpitations, muscle weakness/cramps/tremors, change in respiration, increased weight gain or loss, change in gait, flu-like symptoms. Avoid alcohol during therapy. Change position slowly from sitting or lying to standing. If you have diabetes, regularly check blood glucose level and inform prescriber about changes. Patient should be watched for suicidal tendencies by caregivers or family.
Pharmacokinetics
Note: In paediatric patients 10-17 yrs of age, the pharmacokinetic parameters of aripiprazole and dehydroaripiprazole have been shown to be similar to adult values when adjusted for weight. Onset of action: Initial: 1-3 wks. Absorption: IM: Extended-release: Slow, prolonged. Oral: Well absorbed. Metabolism: Hepatic. Bioavailability: IM: 100%; Tab: 87%. Half-life elimination: Aripiprazole: 75 hrs; dehydroaripiprazole: 94 hrs; IM, extended release (terminal): Approx. 30-47 days (dose-dependent). CYP2D6 poor metabolizers: Aripiprazole: 146 hrs. Time to peak, plasma: IM: Immediate release: 1-3 hrs. Extended release (after multiple doses): 4 days (deltoid administration); 5-7 days (gluteal administration). Tab: 3-5 hrs. With high-fat meal: Aripiprazole: Delayed by 3 hrs; dehydroaripiprazole: Delayed by 12 hrs. Excretion: Faeces (55%). Urine (25%).
Brands with this active ingredient
Compiled by Healify Pharmacy from published drug references. How we compile it →
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