ABILIFY® aripiprazole
ABILIFY DESCRIPTION

Aripiprazole is a psychotropic drug that is available as ABILIFY® (aripiprazole) Tablets, ABILIFY DISCMELT®
(aripiprazole) Orally Disintegrating Tablets, ABILIFY® (aripiprazole) Oral Solution, and ABILIFY® (aripiprazole)
Injection, a solution for intramuscular injection. Aripiprazole is 7-[4-[4-(2,3-dichlorophenyl)-1piperazinyl]butoxy]
-3,4-dihydrocarbostyril. The empirical formula is C23H27Cl2N3O2. ABILIFY Tablets are available in 2 mg, 5 mg,
10 mg, 15 mg, 20 mg, and 30 mg strengths. Inactive ingredients include cornstarch, hydroxypropyl cellulose,
lactose monohydrate, magnesium stearate, and microcrystalline cellulose. Colorants include ferric oxide (yellow
or red) and FD&C Blue No. 2 Aluminum Lake.

ABILIFY DISCMELT Orally Disintegrating Tablets are available in 10 mg and 15 mg strengths. Inactive
ingredients include acesulfame potassium, aspartame, calcium silicate, croscarmellose sodium, crospovidone,
crème de vanilla (natural and artificial flavors), magnesium stearate, microcrystalline cellulose, silicon dioxide,
tartaric acid, and xylitol. Colorants include ferric oxide (yellow or red) and FD&C Blue No. 2 Aluminum Lake.

ABILIFY Oral Solution is a clear, colorless to light yellow solution available in a concentration of 1 mg/mL. The
inactive ingredients for this solution include disodium edetate, fructose, glycerin, dl-lactic acid, methylparaben,
propylene glycol, propylparaben, sodium hydroxide, sucrose, and purified water. The oral solution is flavored
with natural orange cream and other natural flavors.

ABILIFY Injection is available in single-dose vials as a ready-to-use, 9.75 mg/1.3 mL (7.5 mg/mL) clear,
colorless, sterile, aqueous solution for intramuscular use only. Inactive ingredients for this solution include 150
mg/mL of sulfobutylether β-cyclodextrin (SBECD), tartaric acid, sodium hydroxide, and water for injection.

ABILIFY INDICATIONS

ABILIFY is indicated for the treatment of schizophrenia, manic and mixed episodes associated with bipolar I
disorder. ABILIFY is also indicated as an adjunctive therapy to either lithium or valproate for the acute
treatment of manic and mixed episodes associated with bipolar I disorder. Finally, ABILIFY is also indicated for
use as an adjunctive therapy to antidepressants for the treatment of major depressive disorder (MDD),
irritability associated with autistic disorder, agitation associated with schizophrenia or bipolar disorder, manic or
mixed.

DOSAGE AND ADMINSTRATION

In general, the starting and target dose for ABILIFY is 10 mg/day or 15 mg/day administered on a once-a-day
schedule without regard to meals for adults with schizophrenia and bipolar disorder, 2 mg/day to 5 mg/day for
adults with Major Depressive Disorder, 5 mg/day to 15 mg/day for pediatric patients with irritability associated
with autistic disorder, etc. Discuss with your doctor for details.

SIDE EFFECTS / ADVERSE REACTION

The most common side effects in adult patients in clinical trials ( ≥ 10%) were nausea, vomiting, constipation,
headache, dizziness, akathisia, anxiety, insomnia, and restlessness.

The most common side effects in the pediatric clinical trials ( ≥ 10%) were somnolence, headache, vomiting,
extrapyramidal disorder, fatigue, increased appetite, insomnia, nausea, nasopharyngitis, and weight increased.

In clinical studies, there was little difference in the incidence of discontinuation due to adverse reactions
between aripiprazole-treated (7%) and placebo-treated (9%) patients. The types of adverse reactions that led
to discontinuation were similar for the aripiprazole-treated and placebo-treated patients. The only commonly
observed side effects / adverse reaction associated with the use of aripiprazole in patients with schizophrenia
(incidence of 5% or greater and aripiprazole incidence at least twice that for placebo) was akathisia
(aripiprazole 8%; placebo 4%).

Overall, in patients with bipolar mania, there was little difference in the incidence of discontinuation due to side
effects between aripiprazole-treated (11%) and placebo-treated (10%) patients. The types of side effects that
led to discontinuation were similar between the aripiprazole-treated and placebo-treated patients.

WARNINGS

Patients with major depressive disorder (MDD), both adult and pediatric, may experience worsening of their
depression and/or the emergence of suicidal ideation and behavior (suicidality) or unusual changes in
behavior, whether or not they are taking antidepressant medications, and this risk may persist until significant
remission occurs. Suicide is a known risk of depression and certain other psychiatric disorders, and these
disorders themselves are the strongest predictors of suicide. There has been a long-standing concern,
however, that antidepressants may have a role in inducing worsening of depression and the emergence of
suicidality in certain patients during the early phases of treatment. Pooled analyses of short-term placebo-
controlled trials of antidepressant drugs (SSRIs and others) showed that these drugs increase the risk of
suicidal thinking and behavior (suicidality) in children, adolescents, and young adults (ages 18-24) with MDD
and other psychiatric disorders. Short-term studies did not show an increase in the risk of suicidality with
antidepressants compared to placebo in adults beyond age 24; there was a reduction with antidepressants
compared to placebo in adults aged 65 and older.

A potentially fatal symptom complex sometimes referred to as Neuroleptic Malignant Syndrome (NMS) may
occur with administration of antipsychotic drugs, including aripiprazole. Hyperglycemia, in some cases extreme
and associated with ketoacidosis or hyperosmolar coma or death, has been reported in patients treated with
atypical antipsychotics. There have been few reports of hyperglycemia in patients treated with ABILIFY.

Only popular side effects and potential adverse reactions of Abilify have been discussed. Users MUST discuss
with their health-care provider for detailed information.

A total of 76 cases of deliberate or accidental overdosage with oral aripiprazole have been reported worldwide
(January 2011). The largest known case of acute ingestion with a known outcome involved 1080 mg of oral
aripiprazole (36 times the maximum recommended daily dose) in a patient who fully recovered. Common
adverse reactions (reported in at least 5% of all overdose cases) reported with oral aripiprazole overdosage
(alone or in combination with other substances) include vomiting, somnolence, and tremor. Other clinically
important signs and symptoms observed in one or more patients with aripiprazole overdoses (alone or with
other substances) include acidosis, aggression, aspartate aminotransferase increased, atrialfibrillation,
bradycardia, coma, confusional state, convulsion, blood creatine phosphokinase increased, depressed level of
consciousness, hypertension, hypokalemia, hypotension, lethargy, loss of consciousness, QRS complex
prolonged, QT prolonged, pneumonia aspiration, respiratory arrest, status epilepticus, and tachycardia. So
users should their best not to overdose themselves and users should report to their doctor immediately if they
are overdosed.

PHARMACOLOGY / PHARMADYNAMICS / PHARMCOKINETICS

It is believed that the efficacy of aripiprazole is mediated through a combination of partial agonist activity at D2
and 5-HT1A receptors and antagonist activity at 5-HT2A receptors. Actions at receptors other than D2, 5-
HT1A, and 5-HT2A may explain some of the other clinical effects of aripiprazole (eg, the orthostatic hypotension
observed with aripiprazole may be explained by its antagonist activity at adrenergic alpha1 receptors).

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.

ABILIFY activity is presumably primarily due to the parent drug, aripiprazole, and to a lesser extent, to its major
metabolite, dehydro-aripiprazole, which has been shown to have affinities for D2 receptors similar to the parent
drug and represents 40% of the parent drug exposure in plasma. The mean elimination half-lives are about 75
hours and 94 hours for aripiprazole and dehydro-aripiprazole, respectively. Steady-state concentrations are
attained within 14 days of dosing for both active moieties. Elimination of aripiprazole is mainly through hepatic
metabolism involving two P450 isozymes, CYP2D6 and CYP3A4.

Aripiprazole is well absorbed after administration of the tablet, with peak plasma concentrations occurring within
3 hours to 5 hours; the absolute oral bioavailability of the tablet formulation is 87%. ABILIFY can be
administered with or without food. Administration of a 15 mg ABILIFY Tablet with a standard high-fat meal did
not significantly affect the Cmax or AUC of aripiprazole or its active metabolite, dehydroaripiprazole, but delayed
Tmax by 3 hours for aripiprazole and 12 hours for dehydroaripiprazole. Aripiprazole is also well absorbed when
administered orally as the solution. At equivalent doses, the plasma concentrations of aripiprazole from the
solution were higher than that from the tablet formulation. In a relative bioavailability study comparing the
pharmacokinetics of 30 mg aripiprazole as the oral solution to 30 mg aripiprazole tablets in healthy subjects, the
solution to tablet ratios of geometric mean Cmax and AUC values were 122% and 114%, respectively. The
single-dose pharmacokinetics of aripiprazole were linear and dose-proportional between the doses of 5 mg to
30 mg.

Aripiprazole is metabolized primarily by three biotransformation pathways: dehydrogenation, hydroxylation, and
N-dealkylation. Following a single oral dose of [14C]-labeled aripiprazole, approximately 25% and 55% of the
administered radioactivity was recovered in the urine and feces, respectively. Less than 1% of unchanged
aripiprazole was excreted in the urine and approximately 18% of the oral dose was recovered unchanged in the
feces.

NOTE: This is only a summary article of the product insert. One must consult her/his medical doctor for details
or before taking this medicine.
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