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Aripiprazole; Indications/Uses, Dosage, Side effects, Drug Interaction, Pregnancy

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

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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

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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)

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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.