Aripiprazole is a quinoline derivate and atypical antipsychotic agent. Aripiprazole has partial agonistic activity at dopamine D2 receptors and serotonin 5-HT1A receptors, as well as potent antagonistic activity on serotonin 5-HT2A receptors. This drug stabilizes dopamine and serotonin activity in the limbic and cortical system. Aripiprazole is used in managing symptoms of schizophrenia and of acute manic and mixed episodes associated with bipolar I disorders.
Aripiprazole is an atypical antipsychotic & it is recommended and primarily used in the treatment of schizophrenia and bipolar disorder. It is used to treat the symptoms of psychotic conditions such as schizophrenia and bipolar I disorder(manic depression). It is not known if aripiprazole is safe or effective in children younger than 13 with schizophrenia, or children younger than 10 with bipolar disorder.
Mechanism of Action of Aripiprazole
Aripiprazole’s antipsychotic activity is likely due to a combination of antagonism at D2 receptors in the mesolimbic pathway and 5HT2A receptors in the frontal cortex. Antagonism at D2 receptors relieves positive symptoms while antagonism at 5HT2A receptors relieves negative symptoms of schizophrenia. Aripiprazole is a selective monoaminergic antagonist with high affinity for the serotonin Type 2 (5HT2), dopamine Type 2 (D2), 1 and 2 adrenergic, and H1 histaminergic receptors. Aripiprazole acts as an antagonist at other receptors, but with lower potency. Antagonism at receptors other than dopamine and 5HT2 with similar receptor affinities may explain some of the other therapeutic and side effects of Aripiprazole. Aripiprazole’s antagonism of histamine H1 receptors may explain the somnolence observed with this drug.
Indications of Aripiprazole
- Borderline Personality Disorder
- Bipolar Disorder
- Autism
- Schizoaffective Disorder
- Depression
- Major Depressive Disorder
- Obsessive Compulsive Disorder
- Post Traumatic Stress Disorder
- Schizophrenia
- Acute Agitation, Irritability
- Mixed manic depressive episode
- Psychotic Depression
- Schizophrenic Disorders
- Acute Manic episode
- Also for the treatment of schizophrenia and related psychotic disorders.
Contra-Indications of Aripiprazole
- Diabetes
- Excessive fat in the blood
- Low amount of magnesium in the blood
- Extreme Loss of Body Water
- Low amount of potassium in the blood
- Overweight
- Decreased Function of Bone Marrow
- Deficiency of granulocytes a type of white blood Cell
- Increased eosinophils in the Blood
- Abnormal movements of facial muscles and tongue
- Neuroleptic malignant syndrome
- Lower seizure threshold
- Closed angle glaucoma
- Very Rapid Heartbeat – Torsades de Pointes
- Slow Heartbeat
- Stroke
- Disorder of the Blood Vessels of the Brain
- The blood clot in a deep vein of the extremities
- Blood Pressure Drop Upon Standing
- Abnormally low blood pressure
- Paralysis of the Intestines
- Constipation
- Liver problems
- Acute Inflammation of the Pancreas
- Enlarged Prostate
- Seizures
- Cannot Empty Bladder
- High Blood Sugar
- abnormal liver function tests
- Susceptible to Breathing Fluid Into Lungs
- a mother who is producing milk and breastfeeding
- Metabolic Syndrome X
- Dementia in an Elderly Person
- Decreased Motility Function of Stomach or Intestines
Dosages of Aripiprazole
Strengths: 2 mg; 5 mg; 10 mg; 15 mg; 20 mg; 30 mg;300 mg; 400 mg; 1 mg/mL; 9.75 mg/1.3 mL;
Schizophrenia
Oral
Immediate-Release
- Initial dose: 10 or 15 mg orally once a day
- Target dose: 10 to 15 mg per day; effective dose range 10 to 30 mg per day; however, clinical trials have not found doses exceeding 10 or 15 mg per day to be more effective.
- Maximum dose: 30 mg/day
Parenteral
Aripiprazole Extended-Release IM Suspension
- Initial dose: 400 mg IM once; continue aripiprazole 10 to 20 mg orally once a day for 14 days
- Maintenance dose: 300 to 400 mg IM once a month; should not be given sooner than 26 days after the previous injection.
Aripiprazole Lauroxil Extended-Release IM Suspension
- Patients stable on oral aripiprazole 10 mg/day: Initial dose 441 mg IM once; continue aripiprazole 10 mg orally once a day for 21 days.
- Patients stable on oral aripiprazole 15 mg/day: Initial dose 662 mg IM once; continue aripiprazole 15 mg orally once a day for 21 days.
- Patients stable on oral aripiprazole at least 20 mg/day: Initial dose 882 mg IM; continue oral aripiprazole once a day for 21 days.
- Maintenance doses: 441 mg, 662 mg, or 882 mg IM monthly, 882 mg IM every 6 weeks, or 1064 mg IM every 2 months; this drug should not be given sooner than 14 days after the previous injection.
Bipolar Disorder
Oral
Immediate-Release
- Initial dose: 15 mg orally once a day
- Target dose: 15 mg orally once a day; may increase dose based on clinical response. Dose increases, if needed, should be at 2-week intervals to allow time to achieve steady state.
- Maximum dose: 30 mg/day
Adjunctive Therapy with Lithium or Valproate
- Initial dose: 10 to 15 mg orally once a day
- Target dose: 15 mg orally once a day; may increase dose based on clinical response.
- Maximum dose: 30 mg/day
Parenteral
Aripiprazole Extended-Release IM Suspension
- Initial dose: 400 mg IM once; continue aripiprazole 10 to 20 mg orally once a day for 14 days
- Maintenance dose: 300 to 400 mg IM once a month; should not be given sooner than 26 days after the previous injection
Depression
Oral
Immediate-Release
- Initial dose: 2 to 5 mg orally once a day
- Doses may be adjusted in increments up to 5 mg per day at intervals of no less than 1 week.
- Maintenance dose: 2 to 15 mg once a day
- Maximum dose: 15 mg/day
Agitated State
Parenteral formulation
Immediate-Release
- Initial dose: 9.75 mg IM once
- Maintenance dose: 5.25 to 15 mg IM once
- Maximum dose: 30 mg/day
Side Effects
The most common
- Difficulty with speaking
- loss of balance control
- muscle trembling, jerking, or stiffness
- Aggressive behavior
- agitation
- anxiety
- changes in vision, including blurred vision
- difficulty concentrating
- difficulty speaking or swallowing
- dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
- Chest pain or tightness
- dry mouth
- trembling or shaking of the hands or feet
- stomach pain or cramping
- diarrhea
- a headache
- stomach pain;
- back pain, joint or muscle pain.
- problems with your vision (including color vision);
- sudden chest pain or trouble breathing;
- pain or swelling in one or both legs;
- a migraine headache;
- pale skin, feeling light-headed or short of breath, rapid heart rate, trouble concentrating; or
- feeling like you might pass out.
More common
- Abdominal or stomach pain, discomfort, or tenderness
- chills or fever
- difficulty with moving
- headache, severe and throbbing
- joint or back pain
- muscle aching or cramping
- muscle pains or stiffness
- chest pressure or squeezing pain in chest
- discomfort in arms, shoulders, neck or upper back
- excessive sweating
- feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
- sudden tingling or coldness in an arm or leg
- sudden slow or difficult speech
- sudden drowsiness or need to sleep
- fast breathing
- sharp pain when taking a deep breath
- fast or slow heartbeat
- coughing up blood
- rust colored urine
- decreased amount of urine
Rare
- Anxiety
- change in vision
- chest pain or tightness
- confusion
- cough
- Agitation
- arm, back, or jaw pain
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats
- fainting
- hallucinations
- headache
- irritability
- lightheadedness
- mood or mental changes
- muscle pain or cramps
- muscle spasm or jerking of all extremities
- nervousness
Drug Interactions
Aripiprazole may interact with following drug, ssupplements & may change the efficacy of drug
- antihistamines (e.g,. cetirizine, doxylamine, diphenhydramine, hydroxyzine,loratadine)
- anti-Parkinsons medications (e.g., amantadine, apomorphine, bromocriptine, levodopa,pramipexole, ropinirole)
- antipsychotics (e.g., chlorpromazine, , haloperidol, quetiapine, risperidone)
- antiseizure medications (e.g., clobazam, ethosuximide, felbamate, levetiracetam, phenobarbital, phenytoin, topiramate, valproic acid, zonisamide)
- aripiprazole
- “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- baclofen
- barbiturates (e.g., butalbital, pentobarbital, phenobarbital)
- benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
- beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol)
- bupropion
- calcitriol
- calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
- captopril
- celecoxib
- chloroquine
- cholecalciferol
- cyclosporine
- dantrolene
- domperidone
- “gliptin” diabetes medications (e.g., linagliptin, saxagliptin, sitagliptin)
- gabapentin
- H2 antagonists (e.g., famotidine, ranitidine)
- ipratropium
- macrolide antibiotics (e.g., clarithromycin, erythromycin)
- mirabegron
- mirtazapine
- monoamine oxidase inhibitors (MAOIs; moclobemide, phenelzine, rasagiline, selegiline, tranylcypromine)
- non-steroidal anti-inflammatory medications (NSAIDs; e.g., diclofenac, ibuprofen, naproxen)
- phosphodiesterase 5 inhibitors (e.g., sildenafil, vardenafil)tadalafil,
- proton pump inhibitors (e.g., lansoprazole, omeprazole)
- quinolone antibiotics (e.g., levofloxacin, norfloxacin, moxifloxacin)
- selective serotonin reuptake inhibitors (SSRIs; e.g., paroxetine, fluoxetine,citalopram)
- serotonin antagonists (anti-emetic medications; e.g., granisetron, ondansetron)
- tapentadol
- theophylline
- thiazide diuretics (water pills; e.g., hydrochlorothiazide, indapamide, metolazone)
- tramadol
- tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
- tyrosine kinase inhibitors (e.g., dasatinib, imatinib, nilotinib, sunitinib)
- “triptan” migraine medications (e.g., eletriptan, sumatriptan)
Pregnancy Catagory of Aripiprazole
FDA Pregnancy Category C
Pregnancy
This medication falls into category C. In animal studies, pregnant animals were given this medication and had some babies born with problems. No well-controlled studies have been done in humans. Therefore, this medication may be used if the potential benefits to the mother outweigh the potential risks to the unborn child.
Lactation
Aripiprazole has been detected in human breast milk. Because of the possibility for adverse reactions in nursing infants from aripiprazole, a choice should be made whether to stop nursing or to stop use of this medication. The importance of the drug to the mother should be considered.
References
-
https://ec.europa.eu/health/documents/community-register/html/h1005.htm
Aripiprazolehttps://ec.europa.eu/health/documents/community-register/html/ho25875.htm
https://ec.europa.eu/health/documents/community-register/html/h882.htm
https://ec.europa.eu/health/documents/community-register/html/h1029.htm
https://ec.europa.eu/health/documents/community-register/html/h1009.htm
https://ec.europa.eu/health/documents/community-register/html/h276.htm
https://ec.europa.eu/health/documents/community-register/html/h1045.htm
Explore this medical topic
Continue through verified related conditions, investigations, medicines, and patient guides. These links are educational and do not replace professional medical advice.
