Aripiprazole (Abilify) is an atypical antipsychotic used for the treatment of manic and mixed episodes in bipolar disorder, schizophrenia, irritability in autism and Tourette’s syndrome. It is also used as an adjunct in the treatment of major depressive disorder. [1] It was developed by Otsuka Pharmaceutical and its patent has since expired allowing the approval of generic versions since 2015.[2]
Introduction to Aripiprazole
Aripiprazole is primarily used for the treatment of bipolar and schizophrenia. It differs from other atypical antipsychotics in that instead of antagonising the D2 receptor it acts as a partial agonist. It is also associated with minimal weight gain by comparison to other atypical antipsychotics, it is believed this may be due to its 5-HT2c agonism.[3]
Using Aripiprazole
Ways of Administration
Oral
IM Injection.Dose
Column 1 Column 2 Threshold 0.25 mg Light 2-5mg Medium 10-15mg Strong 15-30mg Effects of Aripiprazole
Aripiprazole combinations
Recreational drug combinations with Aripiprazole
Concurrent use with stimulants (Amphetamines, MDMA, Cocaine) may reduce the efficacy of either or both agents. [4]Dangerous interactions with Aripiprazole
No dangerous combinations with Aripiprazole have been added to this wiki yet.Medication interactions with Aripiprazole
Strong CYP3A4 Inhibitors (e.g. itraconazole, clarithromycin) – Increases exposure of Aripiprazole.
Strong CYP2D6 Inhibitors (e.g. quinidine, fluoxetine, paroxetine) – Increases exposure of Aripiprazole.
Strong CYP3A4 Inducers (e.g. carbamazepine, rifampin) – Decreases exposure of Aripiprazole.
Antihypertensive drugs – May potentiate Antihypertensive drugs.
Benzodiazepines – Increased sedation.Potentiators of Aripiprazole
No Potentiation combinations with Aripiprazole have been added to this wiki yet.Different Uses for Aripiprazole
Aripiprazole is approved in the U.S. as an antipsychotic for schizophrenia and acute manic episodes in bipolar disorder. It is also used as adjunctive therapy in major depressive disorder, and may be of use in autism spectrum disorders and obsessive-compulsive disorder.
Pharmacology of Aripiprazole
General
Aripiprazole has a novel binding profile that differs from other atypical antispychotics in that it is a dopamine D2 partial agonist, rather than an antagonist.[5]
It appears to show predominantly antagonist activity on postsynaptic D2 receptors and partial agonist activity on presynaptic D2 receptors. Aripiprazole is also a partial agonist of the D3 receptor.
Aripiprazole is also a partial agonist of the serotonin 5-HT1A receptor (intrinsic activity = 68%). It is a very weak partial agonist of the 5-HT2A receptor (intrinsic activity = 12.7%), and like other atypical antipsychotics, displays a functional antagonist profile at this receptor. The drug differs from other atypical antipsychotics in having higher affinity for the D2 receptor than for the 5-HT2A receptor. At the 5-HT2B receptor, aripiprazole acts as a potent inverse agonist. Unlike other antipsychotics, aripiprazole is a high-efficacy partial agonist of the 5-HT2C receptor (intrinsic activity = 82%) and with relatively weak affinity; this property may underlie the minimal weight gain seen in the course of therapy.Targets, Enzymes, and Transporters
Targets
D2 partial agonist D3 partial agonist D4 partial agonist 5HT1A partial agonist 5HT2A antagonist 5HT2C partial agonist
Chemistry of Aripiprazole
[6]
Systematic(IUPAC) name: 7-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy]-3,4-dihydro-1H-quinolin-2-one Synonyms: 14597, OPC; 7-(4-(4-(2,3-dichlorophenyl)-1-piperazinyl)butyloxy)-3,4-dihydro-2(1H)-quinolinone; Abilify; Aripiprazol; aripiprazole; OPC 14597; OPC-14597 Molecular Formula: CXHYClNZOM... Molar mass: 448.38538 g/mol. CAS Registry Number: 129722-12-9 Melting Point: No data Boiling Point: 139.0-139.5 ℃+ Flash Point: No data Solubility: <0.3 [ug/mL] Additional data: Notes:
Aripiprazole is a phenylpiperazine and is chemically related to nefazodone, etoperidone, and trazodone.
The Dangers of Aripiprazole
General Warnings
Cerebrovascular adverse reactions in elderly patients with dementia related psychosis.
Neuroleptic malignant syndrome
Tardive Dyskinesia
Metabolic changes – hyperglycaemia/diabetes mellitus, dyslipidemia, weight gain
Orthostatic hypotension
Leukopenia, Neutropenia and Argranulocytosis
Seizures/Convulsions – Use cautiously in patients with history of seizures or with conditions that lower the seizure threshold.
Potential for cognitive and motor impairment.
SuicideSide Effects and Interactions
Potential Side Effects
Akathisia
Extrapyramidal disorder
Somnolence
Tremor
Sedation
Restlessness
Insomnia
Fatigue
Nausea
Blurred vision
Salivary hypersecretion
Dizziness
Constipation
Vomiting
Pyrexia
Drooling
Decreased appetite
Lethargy
Headache
Nasopharyngitis
Increased appetitePotential Drug Interactions
Strong CYP3A4 Inhibitors (e.g. itraconazole, clarithromycin) – Increases exposure of Aripiprazole.
Strong CYP2D6 Inhibitors (e.g. quinidine, fluoxetine, paroxetine) – Increases exposure of Aripiprazole.
Strong CYP3A4 Inducers (e.g. carbamazepine, rifampin) – Decreases exposure of Aripiprazole.
Antihypertensive drugs – May potentiate Antihypertensive drugs.
Benzodiazepines – Increased sedation.Mental Health Risks
Suicide
Risk of suicide is associated with schizophrenia and bipolar disorders. Close supervision of at risk patients should accompany therapy.
Legal Status of Aripiprazole
USA
Unscheduled but prescription only.
History of Aripiprazole
Aripiprazole was developed by Otsuka Pharmaceutical and its patent has since expired allowing the approval of generic versions since 2015.[7].
More Aripiprazole Sections and Information
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