Clinical Pharmacology Details


ARIPIPAZOLE


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Indications & Dose:

Maintenance in schizophrenia in patients stabilised with oral aripiprazole



Adult: 400 mg every month, to be injected into the gluteal muscle, minimum of 26 days between injections, for dose adjustment due to side effects or concomitant use of interacting drugs, consult product literature and (by mouth) 10–20 mg daily continued for 14 consecutive days after the first injection, for missed depot doses consult product literature


Schizophrenia



Adult: 10–15 mg once daily; usual dose 15 mg once daily (max. per dose 30 mg once daily), for dose adjustments due to concomitant use of interacting drugs—consult product literature


Treatment and recurrence prevention of mania



Adult: 15 mg once daily, increased if necessary up to 30 mg once daily, for dose adjustments due to concomitant use of interacting drugs—consult product literature


Control of agitation and disturbed behaviour in schizophrenia



Adult: Initially 5.25–15 mg for 1 dose, alternatively usual dose 9.75 mg for 1 dose, followed by 5.25– 15 mg after 2 hours if required, maximum 3 injections daily; maximum daily combined oral and parenteral dose 30 mg, for dose adjustments due to concomitant use of interacting drugs— consult product literature

Contraindications:

CNS depression . comatose state . phaeochromocytoma 

Side Effects:

CNS: Extrapyramidal symptoms, depression, nervousness, increased salivation, hostility, suicidal thought, manic reaction, abnormal gait, confusion, cogwheel rigidity


CV: Chest pain, hypertension, tachycardia, hypotension, bradycardia


EENT: Conjunctivitis, ear pain


GI: Anorexia, nausea, vomiting


GU: Urinary incontinence


METAB: Weight gain


MS: Neck pain, neck rigidity, muscle cramp


RESP: Dyspnea, pneumonia


MISC: Flulike syndrome 

Cautions:

Precautions:

Neuroleptic malignant syndrome, tardive dyskinesia, orthostatic hypotension with cardiovascular disease, cerebrovascular disease, dehydration, hypovolemia, antihypertensive medications 

Interaction:

Drugs


Alcohol: Additive CNS depression and psychomotor depression


a-blockers (doxazocin, prazocin, terazocin) Potential for enhanced blood pressure lowering effect


Amiodarone: Hepatic metabolism inhibition; consider decreasing aripiprazole dose


Azole antifungals (fluconazole, itraconazole, ketoconazole, miconazole, variconazole): Increased aripiprazole and metabolite concentrations via CYP3A4 inhibition; reduce dose of aripiprazole


Bosentan: Hepatic metabolism induced; consider doubling aripirazole dose


Carbamazepine,oxcarba zepine: Reductions in aripiprazole and metabolite concentrations via CYP3A4 induction; double dose of aripiprazole


Centrally acting agents (i.e., opiates, antidepressants, antihistamines, sedative/ hypnotics): Additive CNS depression and psychomotor depression


Cimetidine: Hepatic metabolism inhibition; consider reducing aripiprazole dose or use alternate H2 receptor blocker


Cyclosporine: Hepatic metabolism inhibition; consider reducing aripiprazole dose


Danazole: Hepatic metabolism inhibition; consider reducing aripiprazole dose


Delavirdine: Hepatic metabolism inhibition; consider reducing aripiprazole dose


Dexamethasone: Hepatic metabolism induced; consider doubling aripirazole dose


Diltiazem: Hepatic metabolism inhibition; consider reducing aripiprazole dose


Droperidol: Increased risk of extrapyrimidal reactions, CNS depression, QT prolongation with similar drug (ziprasidone)


Efavirenz: Hepatic metabolism induced; consider doubling aripiprazole dose


Estrogen: Hepatic metabolism inhibition; consider reducing aripiprazole dose


ID Grapefruit juice: Increased aripiprazole and metabolite concentrations via CYP3A4 inhibition


Griseofulvin: Hepatic metabolism induced; consider doubling aripiprazole dose


Isoniazid: Hepatic metabolism induced; consider doubling aripiprazole dose


ID Macrolide antibiotics (erythromycin, clairithromycin): Increased aripiprazole and metabolite concentrations via CYP3A4 inhibition


Protease inhibitors (indinivir, saquinivir, ritonavir, neljinavir, amprenivir, lopinavir): Hepatic metabolism inhibition; consider reducing aripiprazole dosage


Quinidine:Increased aripiprazole and metabolite concentrations via CYP2D6 inhibition; reduce dose of aripiprazole by approximately 50%


SSRI’s (Fluoxetine, fluvoxamine, paroxetine):Increased aripiprazole and metabolite concentrations via CYP2D6 inhibition; reduce dose of aripiprazole by approximately 50% 


 

Warnings:

Adverse Effects:

Lactations:

Pregnancy category C; excreted in milk of rats during lactation; no human information 

Special Precautions:

Counselling:

Side Effects Or Adverse Reactions:

Patient And Carer Advice: