Abilify Side effect. Adverse Effects, Treatment, and Precautions

Index Effects on body-weight. Dose adjustments. Pharmacokinetics

Abilify Aripiprazole

Abilify / Aripiprazole (BAN, USAN, rINN)
Aripiprazol; Aripiprazolum; OPC-31; OPC-14597. 7-{4-[4-(2,3- Dichlorophenyl)-piperazin-1-yl]butoxy}-3,4-dihydroquinolin- 2(1H)-one.

Арипипразол

Preparations. Proprietary

Also know as: Arlemide; Groven; Irazem; Siblix; Abilify; Belg.: Abilify;
Braz.: Abilify; Chile: Abilify; Azymol; Viza; Cz.: Abilify; Denm.: Abilify; Fin.:
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Abilify; India: Real One; Indon.: Abilify; Irl.: Abilify; Ital.: Abilify; Malaysia:
Abilify; Mex.: Abilify; Neth.: Abilify; Norw.: Abilify; NZ: Abilify; Philipp.:
Abilify; Port.: Abilify; S.Afr.: Abilify; Singapore: Abilify; Spain: Abilify;
Swed.: Abilify; Switz.: Abilify; Thai.: Abilify; UK: Abilify; USA: Abilify; Venez.:
Abilify.
abilify-<b>aripiprazole</b>-2-5-10-15-20-30mg-oral-use

C23H27Cl2N3O2 = 448.4.
CAS — 129722-12-9.
ATC — N05AX12.
ATC Vet — QN05AX12.

Adverse Effects, Treatment, and Precautions

Although aripiprazole may share some of the adverse effects seen with the classical antipsychotics (see Chlorpromazine, p.969), the incidence and severity of such effects may vary. Common adverse effects with aripiprazole include gastrointestinal disorders such as constipation, dyspepsia, nausea, and vomiting, headache, anxiety, insomnia, lightheadedness, and drowsiness.

Aripiprazole may affect the performance of skilled tasks including driving. ◊ References. 1. Marder SR, et al. Aripiprazole in the treatment of schizophrenia: safety and tolerability in short-term, placebo-controlled trials. Schizophr Res 2003; 61: 123–36.

Dementia. The FDA1 has issued advice against the use of atypical antipsychotics in the treatment of behavioural problems in elderly patients with dementia after analysis of placebo-controlled studies showed an increased risk of mortality with certain appeared due to cardiovascular events or infection.

See also under Risperidone, p.1024. The manufacturer subsequently also included a warning in the licensed product information for aripiprazole about evidence of a dose-response relationship between cerebrovascular adverse events and the use of aripiprazole in elderly patients with psychosis associated with Alzheimer's disease.

1. FDA. FDA issues public health advisory for antipsychotic drugs used for treatment of behavioral disorders in elderly patients (issued 11th April, 2005). Available at: http://www.fda.gov/bbs/topics/ANSWERS/2005/ANS01350.html (accessed 24/05/05)

Abilify Effects on body-weight

The increased risk of weight gain with some atypical antipsychotics is discussed under Adverse Effects of Clozapine, p.981. Further references.

Effects on body-weight

1. McQuade RD, et al. A comparison of weight change during treatment with olanzapine or aripiprazole: results from a randomized, double-blind study. J Clin Psychiatry 2004; 65 (suppl 18): 47–56.

Effects on carbohydrate metabolism. The increased risk of glucose intolerance and diabetes mellitus with some atypical antipsychotics, and recommendations on monitoring, are discussed under Adverse Effects of Clozapine, p.981.

Effects on lipid metabolism. The increased risk of hyperlipidaemia with some atypical antipsychotics is discussed under Adverse Effects of Chlorpromazine, p.970. See also Effects on Carbohydrate Metabolism under Adverse Effects of Clozapine, p.981

Pregnancy.

For comments on the use of some atypical antipsychotics, including aripiprazole, during pregnancy, see under Precautions of Clozapine, p.983. Licensed product information states that aripiprazole showed possible teratogenic effects in some animals; it was noted that there are no adequate and well-controlled studies in human pregnancy.
Aripiprazole should only be used if the benefits to the mother outweigh the risks to the fetus.

Interactions

The central effects of other CNS depressants including alcohol may be enhanced by aripiprazole.

Aripiprazole may also enhance the effects of antihypertensive drugs. It should be used with caution in patients also receiving drugs that prolong the QT interval or cause electrolyte imbalance. Aripiprazole is metabolised by the cytochrome P450 isoenzymes CYP3A4 and CYP2D6. Ketoconazole, a potent CYP3A4 inhibitor, can increase aripiprazole plasma concentrations by about 60%; licensed product information states that the dose of aripiprazole should be reduced by half when given with ketoconazole.

Similarly, the dose of aripiprazole should be halved when given with quinidine, a potent inhibitor of CYP2D6. Conversely, plasma concentrations of aripiprazole may decrease by about 70% when given with carbamazepine, a potent CYP3A4 inducer; the dose of aripiprazole should be doubled if carbamazepine is added to aripiprazole treatment. Similar effects may occur with other potent inhibitors or inducers of these isoenzymes and a reduced or increased dose of aripiprazole, respectively, in such combinations is recommended.

Antiepileptics. For a report of Stevens-Johnson syndrome occurring on use of aripiprazole with lamotrigine, see p.486.

Pharmacokinetics

Aripiprazole is well absorbed from the gastrointestinal tract after oral doses with peak plasma concentrations reached in about 3 to 5 hours. Following intramuscular injection, peak plasma concentrations are reached between 1 to 3 hours. The absolute bioavailability is reported to be 87% with tablet formulations and 100% with the intramuscular injection; it is widely distributed.

Aripiprazole is metabolised mainly in the liver and pathways involved include dehydrogenation and hydroxylation, via the cytochrome P450 isoenzymes CYP3A4 and CYP2D6, and N-dealkylation, via CYP3A4. The major metabolite, dehydro-aripiprazole, is also active and represents about 40% of the plasma levels of aripiprazole. The mean elimination half-lives of aripiprazole and dehydro-aripiprazole are about 75 and 95 hours, respectively; in a minority of poor metabolisers the half-life of aripiprazole may be extended to about 146 hours. Protein binding of aripiprazole and
its major metabolite is about 99%, mainly to albumin.

Elimination is mostly in the faeces (about 55%), with about 25% of a dose appearing in the urine, mainly in the form of metabolites. On the basis of studies in rats, it is thought to be distributed into breast milk.

References.
1. Mallikaarjun S, et al. Pharmacokinetics, tolerability, and safety of aripiprazole following multiple oral dosing in normal healthy volunteers. J Clin Pharmacol 2004; 44: 179–87.

Uses and Administration

Aripiprazole is an atypical antipsychotic that has serotonin 5-HT1A-receptor partial agonist and 5-HT2A-receptor antagonist properties as well as being a partial agonist at dopamine D2 receptors. It is used in the management of schizophrenia and in acute manic or mixed episodes associated with bipolar disorder.

Aripiprazole is also used as an adjunct in the treatment of depression.

For the treatment of schizophrenia, aripiprazole is given in an initial oral dose of 10 or 15 mg once daily. The usual maintenance dose is 15 mg once daily although the dose may be adjusted at intervals of not less than 2 weeks up to a maximum of 30 mg daily.

Aripiprazole is also used for the treatment of mania associated with bipolar disorder. In the USA, it is given in an initial oral dose of 30 mg once daily, this may subsequently be decreased to 15 mg once daily according to tolerance. Similar doses are licensed in the UK although licensed product information recommends an initial dose of 15 mg once daily.

Aripiprazole may be given by deep intramuscular injection for acute agitation in patients with schizophrenia or bipolar mania. The recommended initial dose is 9.75 mg although some patients may only need 5.25 mg and others up to 15 mg. If necessary, further doses may be given after at least 2 hours, up to a maximum total daily dose of 30 mg. Patients should be switched to oral therapy as soon as possible if ongoing treatment is required.

Aripiprazole is used as adjunctive therapy in depression.

US licensed product information recommends an initial oral dose of 2 to 5 mg once daily, which may be adjusted in increments of up to 5 mg at intervals of not less than 1 week to a maximum of 15 mg daily. The usual recommended dose is 5 to 10 mg once daily. Dose adjustments of aripiprazole may be necessary in patients also taking potent inhibitors or inducers of cytochrome P450 isoenzymes. See Interactions, above for further details.

For details of uses and associated doses in children, see below.

Administration in children. In the USA, aripiprazole may be used for the treatment of schizophrenia in adolescents aged 13 to 17 years and for the treatment of acute manic or mixed episodes associated with bipolar disorder in those aged 10 to 17 years. For both indications, the recommended initial oral dose is 2 mg daily increased to 5 mg daily after 2 days and then to the target dose of 10 mg daily after another 2 days; subsequent dose increases should be made in 5-mg increments up to a total maximum dose of 30 mg daily.

Dose adjustments

Dose adjustments of aripiprazole may be necessary in patients also taking potent inhibitors or inducers of cytochrome P450 isoenzymes. See Interactions, above for further details. Psychiatric disorders. Aripiprazole is used in the management of schizophrenia (p.955) and bipolar disorder (p.372).

1-9 Although data are scanty, systematic reviews8,9 have concluded that aripiprazole does not have significant advantages over other atypical and classical antipsychotics in the treatment of schizophrenia. However, it was found to have a lower risk for hyperprolactinaemia and QT interval prolongation compared with other atypical antipsychotics, and a higher risk for insomnia compared with classical antipsychotics. Aripiprazole is also used as an adjunct in the treatment of depression.10,11

1. McGavin JK, Goa KL. Aripiprazole. CNS Drugs 2002; 16:
779–86.
2. Goodnick PJ, Jerry JM. Aripiprazole: profile on efficacy and
safety. Expert Opin Pharmacother 2002; 3: 1773–81.
3. Taylor DM. Aripiprazole: a review of its pharmacology and
clinical use. Int J Clin Pract 2003; 57: 49–54.
4. Keck PE, McElroy SL. Aripiprazole: a partial dopamine D2 receptor
agonist antipsychotic. Expert Opin Invest Drugs 2003;
12: 655–62.
5. Bowles TM, Levin GM. Aripiprazole: a new atypical antipsychotic
drug. Ann Pharmacother 2003; 37: 687–94.
6. Keck PE, et al. A placebo-controlled, double-blind study of the
efficacy and safety of aripiprazole in patients with acute bipolar
mania. Am J Psychiatry 2003; 160: 1651–8.
7. Harrison TS, Perry CM. Aripiprazole: a review of its use in
schizophrenia and schizoaffective disorder. Drugs 2004; 64:
1715–36.
8. El-Sayeh HG, Morganti C. Aripiprazole for schizophrenia.
Available in The Cochrane Database of Systematic Reviews; Issue 2. Chichester: John Wiley; 2006 (accessed 15/05/06).
9. Bhattacharjee J, El-Sayeh HGG. Aripiprazole versus typicals for schizophrenia. Available in The Cochrane Database of Systematic Reviews; Issue 1. Chichester: John Wiley; 2008 (accessed 07/04/08).
10. Berman RM, et al. The efficacy and safety of aripiprazole as
adjunctive therapy in major depressive disorder: a multicenter,
randomized, double-blind, placebo-controlled study. J Clin Psychiatry
2007; 68: 843–53.
11. Marcus RN, et al. The efficacy and safety of aripiprazole as adjunctive
therapy in major depressive disorder: a second multicenter,
randomized, double-blind, placebo-controlled study. J
Clin Psychopharmacol 2008; 28: 156–65.



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