施贵宝公司（Bristol-Myers Squibb）和大冢制药公司（Otsuka）于2005年3月7日宣布，FDA批准阿立哌唑（aripiprazole，Abilify）片剂和口服溶液剂用于新近出现躁狂或混合型发作的双相I型情感障碍患者保持疗效。FDA于2004年9月29日批准本品用于治疗急性双相性躁狂症，包括双相障碍相关躁狂和混合性发作。 　　最新的FDA批准是基于一项随机双盲多中心安慰剂对照研究的有效结果，依据复发时间评判以比较本品和安慰剂的疗效保持。在这项研究中，新近出现躁狂或混合性发作的患者先用本品防止病情波动至少6周。在达到病情稳定标准[在最少6周的4次随访期间躁狂量表(Y-MRS)总评￡10Montgomery-Asberg抑郁量表(MADRS)总评分￡13]后，161例患者在双盲随机阶段给予本品或安慰剂。 　　主要终点为躁狂和抑郁症状复发的时间。在出现复发的患者中，本品组患者的复发明显迟于用安慰剂组（P＝0.020）。此外，复发的总次数本品组明显少于用安慰剂者（25%对43%；P＝0.013）。多数复发归为躁狂症状而非抑郁症状。没有足够数据显示本品对延缓双相I型障碍患者的抑郁症状出现是否有效。研究期间报告的不良反应与本品的其他长期安慰剂对照研究中的基本一致。 　　“Abilify获准用于新适应证对于有躁狂和混合性发作的双相I型情感障碍患者是一个重要的消息，因为不幸的是复发很常见。” 治疗研究中心主任、Rush大学医学中心副教授John Zajecka医学博士说，“作为一名医生，得知患者在其治疗的各个阶段都能受益于Abilify非常 令人振奋。” ABILIFY : ARIPEXIA Aripiprazole  20mg PHARMACOLOGICAL ACTION: Aripiprazole functions as a partial agonist at the dopamine D 2 and the serotonin 5-HT 1A receptors, and as an antagonist at serotonin 5-HT 2A receptor.. The mechanism of action of aripiprazole, as with other drugs having efficacy in schizophrenia and bipolar disorder, is unknown. However, it has been proposed that the efficacy of aripiprazole is mediated through a combination of partial agonist activity at D 2 and 5-HT 1A receptors and antagonist activity at 5-HT 2A receptors. Pharmacokinetics: Aripiprazole is well absorbed after administration of the tablet, with peak plasma concentrations occurring within 3 to 5 hours . Aripiprazole is metabolized primarily by three biotransformation pathways: dehydrogenation, hydroxylation, and N-dealkylation. CYP3A4 and CYP2D6 enzymes are responsible for dehydrogenation and hydroxylation of aripiprazole, and N-dealkylation is catalyzed by CYP3A4. INDICATIONS: Aripexia is indicated for the treatment of schizophrenia ,  acute manic and mixed episodes associated with Bipolar Disorder . DOSAGE AND DIRECTIONS FOR USE: Schizophrenia The recommended starting and target dose for Aripexia is 10 or 15 mg/day administered on a once-a-day schedule without regard to meals. ABILIFY has been systematically evaluated and shown to be effective in a dose range of 10 to 30 mg/day .Dosage adjustments are not routinely indicated on the basis of age, gender, race, or renal or hepatic impairment status . Bipolar Disorder The starting dose was 30 mg given once a day. SIDE-EFFECTS:  gastrointestinal disorders such as constipation, dyspepsia, nausea, and vomiting, headache, anxiety, insomnia, lightheadedness, and drowsiness. Weight gain has been reported .Orthostatic hypotension may occur with aripiprazole treatment . WARNINGS  &  Precautions Aripexia should be used with caution in patients with cardiovascular or cerebrovascular disease, or in those with conditions that would predispose to hypotension. CONTRA-INDICATIONS: Aripexia  is contraindicated in patients with a known hypersensitivity to Aripiprazole . Drug Interactions: Agents that induce CYP3A4 (e.g., carbamazepine) could cause an increase in aripiprazole clearance and lower blood levels. Inhibitors of CYP3A4 (e.g., ketoconazole) or CYP2D6 (e.g., quinidine, fluoxetine, or paroxetine) can inhibit aripiprazole elimination and cause increased blood levels. PRESENTATION: Cartoon box contain one or two (Al/Pvc) strip each strip contain 10 tablets With inner leaflet stored In dry state at room temperature (15-30°c) Keep out of reach of children Brand name: Abilify Generic name: Aripiprazole What is Abilify (Aripiprazole)? Abilify is an antipsychotic medication. It works by changing the actions of chemicals in the brain. Abilify is used to treat the symptoms of psychotic conditions such as schizophrenia and bipolar disorder (manic depression). It is also used together with other medications to treat major depressive disorder in adults. Abilify may also be used for other purposes not listed in this medication guide. What is the most important information I should know about aripiprazole? Abilify is not for use in psychotic conditions that are related to dementia. Abilify has caused fatal heart attack and stroke in older adults with dementia-related conditions. Stop using aripiprazole and call your doctor at once if you have the following symptoms: fever with stiff muscles and rapid heart rate; uncontrolled muscle movements; symptoms that come on suddenly such as numbness or weakness, severe headache, and problems with vision, speech, or balance. Abilify can cause side effects that may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be awake and alert. Avoid drinking alcohol, which can increase some of the side effects of aripiprazole. Avoid using other medicines that make you sleepy (such as cold medicine, pain medication, muscle relaxers, and medicine for seizures, depression or anxiety). They can add to sleepiness caused by aripiprazole. Tell your doctor if you regularly use any of these medicines. Avoid becoming overheated or dehydrated. Drink plenty of fluids, especially in hot weather and during exercise. It is easier to become dangerously overheated and dehydrated while you are taking aripiprazole. What should I discuss with my healthcare provider before taking aripiprazole? Abilify is not for use in psychotic conditions that are related to dementia. Abilify has caused fatal heart attack and stroke in older adults with dementia-related conditions. Before taking aripiprazole, tell your doctor if you have: liver or kidney disease; heart disease, high blood pressure, heart rhythm problems; a history of heart attack or stroke; a history of breast cancer; seizures or epilepsy; a personal or family history of diabetes; or trouble swallowing. If you have any of these conditions, you may need a dose adjustment or special tests to safely take this medication. The liquid form (oral solution) of this medication may contain up to 15 grams of sugar per dose. Before taking aripiprazole oral solution, tell your doctor if you have diabetes. The orally disintegrating tablet form of this medication may contain over 3 milligrams of phenylalanine per tablet. Before taking Abilify Discmelt, tell your doctor if you have phenylketonuria. Abilify may cause you to have high blood sugar (hyperglycemia). Talk to your doctor if you have any signs of hyperglycemia such as increased thirst or urination, excessive hunger, or weakness. If you are diabetic, check your blood sugar levels on a regular basis while you are taking aripiprazole. FDA pregnancy category C. This medication may be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. Abilify can pass into breast milk and may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby. How should I take aripiprazole? Take this medication exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Do not take aripiprazole for longer than 6 weeks unless your doctor has told you to. Take each dose with a full glass of water. Abilify can be taken with or without food. Abilify is usually taken once a day. Follow your doctor's instructions. Measure the liquid form of aripiprazole with a special dose-measuring spoon or cup, not a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist where you can get one. To take aripiprazole orally disintegrating tablets (Abilify Discmelt): Keep the tablet in its blister pack until you are ready to take the medicine. Open the package and peel back the foil from the tablet blister. Do not push a tablet through the foil or you may damage the tablet. Using dry hands, remove the tablet and place it in your mouth. It will begin to dissolve right away. Do not swallow the tablet whole. Allow it to dissolve in your mouth without chewing. Swallow several times as the tablet dissolves. If desired, you may drink liquid to help swallow the dissolved tablet. It is important to take aripiprazole regularly to get the most benefit. To be sure this medication is helping your condition, your doctor will need to check your progress on a regular basis. It is important that you not miss any scheduled visits to your doctor. Store aripiprazole tablets at room temperature away from moisture and heat. Abilify oral solution should be stored in the refrigerator and can be used for up to 6 months after opening. What happens if I miss a dose? Take the missed dose as soon as you remember. If it is almost time for your next dose, skip the missed dose and take the medicine at the next regularly scheduled time. Do not take extra medicine to make up the missed dose. What happens if I overdose? Seek emergency medical attention if you think you have used too much of this medicine. Overdose symptoms may include drowsiness, vomiting, agitation, aggression, confusion, tremors, fast or slow heart rate, seizure (convulsions), trouble breathing, feeling light-headed, or fainting. What should I avoid while taking aripiprazole? Abilify can cause side effects that may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be awake and alert. Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Get up slowly and steady yourself to prevent a fall. Avoid drinking alcohol, which can increase some of the side effects of aripiprazole. Avoid using other medicines that make you sleepy (such as cold medicine, pain medication, muscle relaxers, and medicine for seizures, depression or anxiety). They can add to sleepiness caused by aripiprazole. Tell your doctor if you regularly use any of these medicines. Avoid becoming overheated or dehydrated. Drink plenty of fluids, especially in hot weather and during exercise. It is easier to become dangerously overheated and dehydrated while you are taking aripiprazole. Abilify side effects Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop using aripiprazole and call your doctor at once if you have any of these serious side effects: fever, stiff muscles, confusion, sweating, fast or uneven heartbeats; jerky muscle movements you cannot control; sudden numbness or weakness, headache, confusion, or problems with vision, speech, or balance; increased thirst or urination, loss of appetite, fruity breath odor, drowsiness, dry skin, nausea, and vomiting seizure (convulsions); thoughts of hurting yourself; feeling like you might pass out; jaundice (yellowing of your skin or eyes); or urinating less than usual or not at all. Less serious side effects may include: choking or trouble swallowing; dizziness, drowsiness, or weakness; constipation, mild stomach upset; headache, anxiety; sleep problems (insomnia); or weight gain. This is not a complete list of side effects and others may occur. Tell your doctor about any unusual or bothersome side effect. What other drugs will affect aripiprazole? Before taking aripiprazole, tell your doctor if you are taking any of the following medicines: a medication to treat high blood pressure or a heart condition; carbamazepine (Tegretol), phenobarbital (Luminal, Solfoton), or phenytoin (Dilantin); rifabutin (Mycobutin) or rifampin (Rifadin, Rimactane, Rifater); ketoconazole (Nizoral), itraconazole (Sporanox); quinidine (Cardioquin, Quinaglute); or fluoxetine (Prozac), fluvoxamine (Luvox), or paroxetine (Paxil). This list is not complete and there may be other drugs that can interact with aripiprazole. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor.