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Brand Name :
rexulti
Synonyms :
Class :
Dopamine Receptor Partial Agonists
Brand Name :
rexulti
Synonyms :
Class :
Dopamine Receptor Partial Agonists
Dosage Forms & StrengthsÂ
TabletÂ
0.25mgÂ
0.5mgÂ
1mgÂ
2mgÂ
3mgÂ
4mgÂ
Day 1-4: 1mg orally every day
Day 5-7: Adjust dosage to 2 mg every day
Day 8: Adjust to 4mg/day
Do not exceed 4mg/day
0.5
mg
Tablet
Orally 
every day
Do not exceed 3mg/day
Dosage Forms & StrengthsÂ
TabletÂ
0.25mgÂ
0.5mgÂ
1mgÂ
2mgÂ
3mgÂ
4mgÂ
<13 years: Safety and efficacy not established
Day 1-4: 0.5 mg orally every day
Day 5-7: Adjust dosage to 1 mg every day
Day 8: Adjust to 2 mg/day
Do not exceed 4 mg/day
Not approvedÂ
may diminish the therapeutic effect of anti-parkinson agents
may diminish the therapeutic effect of anti-parkinson agents
may diminish the therapeutic effect of anti-parkinson agents
may diminish the therapeutic effect of anti-parkinson agents
may diminish the therapeutic effect of anti-parkinson agents
may diminish the serum concentration when combined with brexpiprazole
may diminish the serum concentration when combined with brexpiprazole
may diminish the serum concentration when combined with brexpiprazole
may diminish the serum concentration when combined with brexpiprazole
may diminish the serum concentration when combined with brexpiprazole
brexpiprazole : they may diminish the serum concentration of CYP3A4 Inducers
brexpiprazole : they may diminish the serum concentration of CYP3A4 Inducers
brexpiprazole: they may enhance the serum concentration of CYP2D6 Inhibitors
brexpiprazole: they may enhance the serum concentration of CYP2D6 Inhibitors
brexpiprazole: they may enhance the serum concentration of CYP2D6 Inhibitors
brexpiprazole: they may enhance the serum concentration of CYP2D6 Inhibitors
brexpiprazole: they may enhance the serum concentration of CYP2D6 Inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may increase the level by affecting hepatic enzyme CYP3A4 metabolism
may decrease the level by affecting hepatic enzyme CYP3A4 metabolism
may increase the level by affecting the hepatic enzyme CYP3A4 metabolism
may increase the level by affecting the hepatic enzyme CYP3A4 metabolism
may increase the level by affecting the hepatic enzyme CYP3A4 metabolism
may decrease the level by affecting hepatic enzyme CYP2C9 metabolism
it may increase the effects of each other
may increase the risk of sedation
may increase the level by affecting hepatic enzyme CYP3A4 metabolism
may increase the level by affecting hepatic enzyme CYP3A4 metabolism
It may enhance sedation when combined with oxycodone
CYP3A strong enhancers of the small intestine may reduce the bioavailability of brexpiprazole
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may increase the level by affecting the hepatic enzyme CYP3A4 metabolism
may decrease the level by affecting hepatic enzyme CYP3A4 metabolism
may decrease the effects of the other by pharmacodynamic synergism
may decrease the level by affecting hepatic enzyme CYP3A4 metabolism
may decrease the level by affecting hepatic enzyme CYP3A4 metabolism
may increase the level by affecting the hepatic enzyme CYP3A4 metabolism
may increase the level by affecting the hepatic enzyme CYP3A4 metabolism
may increase the level by affecting the hepatic enzyme CYP3A4 metabolism
may increase the level by affecting the hepatic enzyme CYP3A4 metabolism
may increase the level by affecting the hepatic enzyme CYP3A4 metabolism
may increase the level by affecting the hepatic enzyme CYP3A4 metabolism
may decrease the level by affecting the hepatic enzyme CYP3A4 metabolism
may increase the level by affecting the hepatic enzyme CYP3A4 metabolism
may increase the level by affecting the hepatic enzyme CYP3A4 metabolism
may increase the level by affecting the hepatic enzyme CYP3A4 metabolism
may increase the level by affecting the hepatic enzyme CYP3A4 metabolism
may increase the level by affecting the hepatic enzyme CYP3A4 metabolism
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may enhance the hypotensive effect of beta-blockers
may enhance the hypotensive effect of beta-blockers
may enhance the hypotensive effect of beta-blockers
may enhance the hypotensive effect of beta-blockers
may enhance the hypotensive effect of beta-blockers
may reduce the therapeutic effect of anti-Parkinson drugs
may reduce the therapeutic effect of anti-Parkinson drugs
may reduce the therapeutic effect of anti-Parkinson drugs
may reduce the therapeutic effect of anti-Parkinson drugs
may reduce the therapeutic effect of anti-Parkinson drugs
may increase the effect of beta-blockers
may increase the effect of beta-blockers
may increase the effect of beta-blockers
may increase the effect of beta-blockers
may increase the effect of beta-blockers
may increase the effect of beta-blockers
It may enhance sedation when combined with tramadol
It may increase the hypotensive effect when combined with antihypertensive agents
It may increase the hypotensive effect when combined with antihypertensive agents
It may increase the hypotensive effect when combined with antihypertensive agents
It may increase the hypotensive effect when combined with antihypertensive agents
It may increase the hypotensive effect when combined with antihypertensive agents
may enhance the concentration of serum when combined with brexpiprazole
may enhance the concentration of serum when combined with brexpiprazole
may enhance the concentration of serum when combined with brexpiprazole
may enhance the concentration of serum when combined with brexpiprazole
may enhance the concentration of serum when combined with brexpiprazole
When brexpiprazole is used together with medazepam, the risk or seriousness of CNS depression is enhanced
When brexpiprazole is used together with fluconazole, this leads to reduction in the brexpiprazole metabolism
When chlordiazepoxide is used together with brexpiprazole, this leads to enhanced risk or seriousness of CNS depression
When brexpiprazole is used together with melitracen, this leads to enhanced risk or seriousness of CNS depression
may diminish the therapeutic effect of the drug
When emylcamate is used together with brexpiprazole, this leads to enhanced risk or seriousness of CNS depression
When brexpiprazole is used together with etizolam, this leads to enhanced risk or seriousness of CNS depression
When indisulam is used together with brexpiprazole, this leads to a reduction in brexpiprazole metabolism
When brexpiprazole is used in combination with profenamine, this leads to reduction in therapeutic effectiveness of profenamine
brexpiprazole: it may increase the risk of CNS depression
brexpiprazole: it may increase the risk of CNS depression
brexpiprazole: it may increase the risk of CNS depression
brexpiprazole: it may increase the risk of CNS depression
brexpiprazole: it may increase the risk of CNS depression
brexpiprazole: it may decrease the metabolism of cerivastatin
antipsychotic agents may enhance the adverse/toxic effect of amphetamines
antipsychotic agents may enhance the adverse/toxic effect of amphetamines
antipsychotic agents may enhance the adverse/toxic effect of amphetamines
may enhance the neurotoxic (central) effect of antipsychotic agents
may enhance the neurotoxic (central) effect of antipsychotic agents
may enhance the neurotoxic (central) effect of antipsychotic agents
may enhance the neurotoxic (central) effect of antipsychotic agents
may enhance the neurotoxic (central) effect of antipsychotic agents
may enhance the adverse/toxic effect of antipsychotic agents
may enhance the adverse/toxic effect of antipsychotic agents
may enhance the adverse/toxic effect of antipsychotic agents
may enhance the adverse/toxic effect of antipsychotic agents
may enhance the adverse/toxic effect of antipsychotic agents
antacids may reduce the absorption of antipsychotic agents
antacids may reduce the absorption of antipsychotic agents
antacids may reduce the absorption of antipsychotic agents
antacids may reduce the absorption of antipsychotic agents
antacids may reduce the absorption of antipsychotic agents
may increase the risk of adverse effects of antipsychotic agents
may increase the risk of adverse effects of antipsychotic agents
may increase the risk of adverse effects of antipsychotic agents
may increase the risk of adverse effects of antipsychotic agents
may increase the risk of adverse effects of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may decrease the absorption of antipsychotic agents
may decrease the absorption of antipsychotic agents
may enhance the effect of antipsychotic agents
may enhance the effect of antipsychotic agents
may enhance the effect of antipsychotic agents
may enhance the effect of antipsychotic agents
may enhance the effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may diminish the therapeutic effect of antipsychotic agents
may diminish the therapeutic effect of antipsychotic agents
may diminish the therapeutic effect of antipsychotic agents
may diminish the therapeutic effect of antipsychotic agents
may diminish the therapeutic effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may increase the effect of antipsychotic agents
may increase the effect of antipsychotic agents
may increase the effect of antipsychotic agents
may increase the effect of antipsychotic agents
may increase the effect of antipsychotic agents
may increase the risk of adverse effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may enhance the hypotensive effect
may enhance the hypotensive effect
may enhance the hypotensive effect
may enhance the hypotensive effect
may enhance the hypotensive effect
may enhance the hypotensive effect
may enhance the hypotensive effect
may enhance the serum concentration of CYP3A4 Inhibitors
may increase the risk of adverse effect
may increase the risk of adverse effect
may increase the risk of adverse effect
may increase the risk of adverse effect
may increase the risk of adverse effect
may increase the risk of adverse effect
may increase the risk of adverse effect
may increase the risk of adverse effect
may increase the risk of adverse effect
may increase the risk of adverse effect
the therapeutic effect of brexipiprazole may be reduced
When brexpiprazole is used together in combination with profenamine, this leads to reduction in therapeutic effectiveness of profenamine
Actions and Spectrum:Â
Actions:Â
Brexpiprazole exerts its actions as an antipsychotic medication by modulating neurotransmitter activity in the brain. It interacts with serotonin and dopamine receptors, contributing to its therapeutic effects in managing symptoms of schizophrenia and major depressive disorder. The precise mechanisms through which brexpiprazole produces its effects are complex and involve the regulation of neurotransmitter imbalances associated with these mental health conditions.Â
Spectrum:Â
Brexpiprazole is prescribed for the management of schizophrenia symptoms in adults and adolescents aged 13 and above. Additionally, it is employed in combination with an antidepressant to address depression when the symptoms are not effectively controlled by the antidepressant alone.
The medication is also utilized to alleviate agitation in individuals with dementia caused by Alzheimer’s disease (gradual deterioration of memory, communication skills, cognitive functions, and daily activities). Categorized as an atypical antipsychotic, brexpiprazole operates by modifying the activity of specific natural substances in the brain.
Frequency defined:Â Â
>10%Â
AkathisiaÂ
1-10%Â
MDDÂ
DizzinessÂ
FatigueÂ
HeadacheÂ
AnxietyÂ
NasopharyngitisÂ
Increased appetiteÂ
SomnolenceÂ
RestlessnessÂ
SchizophreniaÂ
DyspepsiaÂ
SedationÂ
AkathisiaÂ
Increased weightÂ
DiarrheaÂ
Frequently not definedÂ
MyalgiaÂ
Blurred visionÂ
NauseaÂ
InsomniaÂ
Salivary hypersecretionÂ
HyperhidrosisÂ
Post-marketing reportsÂ
Malignant syndromeÂ
Black Box Warning:Â
Critical alert for seniors with dementia:Â
Research shows that seniors with dementia face an a higher likelihood of strokes and increased risk of death while undergoing treatment with antipsychotics like brexpiprazole. Brexpiprazole lacks FDA approval for addressing dementia-related psychosis without agitation. If someone with dementia is prescribed brexpiprazole, consult the prescribing doctor.Â
Caution for those dealing with depression:Â
Children, teens, and young adults (up to 24 years old) taking antidepressants like brexpiprazole during clinical studies displayed suicidal tendencies. Those in this age group using antidepressants may have a higher suicide risk. Children under 18 typically shouldn’t use brexpiprazole for depression except when a doctor deems it the most suitable treatment.Â
Be aware that your mental well-being might shift unexpectedly when taking brexpiprazole or other antidepressants, even as an adult over 24. Suicidal thoughts may arise, especially at the treatment’s start or dosage adjustments.
If symptoms like anxiety, worsening depression, suicidal thoughts, agitation, extreme worry, panic attacks, aggressive behavior, sleep disturbances, irritability, severe restlessness, impulsive actions, or manic episodes occur, contact your doctor promptly. Ensure your family or caregiver recognizes these symptoms to seek help if you are unable to do so yourself.Â
Contraindication/Caution:Â
ContraindicationsÂ
CautionsÂ
Pregnancy consideration: Insufficient data availableÂ
Lactation: Excretion of the drug in human breast milk is unknown Â
Pregnancy category:Â
Pharmacology:Â
Brexpiprazole is an antipsychotic medication employed for alleviating symptoms associated with schizophrenia. Additionally, it is utilized in conjunction with other medications for major depressive disorder treatment in adults.Â
Pharmacodynamics:Â
Brexpiprazole interacts with various receptors in the brain, including serotonin, dopamine, noradrenergic, histamine, and muscarinic receptors. It has different levels of affinity for these receptors, acting as a partial agonist at some (5-HT1A, D2, D3) and as an antagonist at others (5-HT2A, 5-HT2B, 5-HT7, α1A, α1B, α1D, α2C). This complex interaction profile contributes to its therapeutic effects in managing mental health conditions.Â
Pharmacokinetics:Â
AbsorptionÂ
The bioavailability is 95%Â
The time to achieve peak effect is 4 hoursÂ
DistributionÂ
Protein-bound is >99%Â
The volume of distribution is 1.56 L/kg Â
MetabolismÂ
Hepatic metabolism by CYP3A4 and CYP2D6 isoenzymes.Â
Elimination and ExcretionÂ
The half-life is 91 hours Â
The drug is excreted 46% in feces and 25% in urine.Â
Administration:Â
Brexpiprazole is administered orally in tablet form, typically once a day with or without food. It is essential to take it at the same time daily. Follow the prescription label instructions diligently, and consult your doctor or pharmacist for clarification. Adhere to the prescribed dosage and frequency, avoiding any deviations.Â
Patient information leafletÂ
Generic Name: brexpiprazoleÂ
Pronounced: brek-SPIP-rÉ™-zohlÂ
Why do we use brexpiprazole?Â
It is used to treat schizophrenia symptoms such as disturbed thinking, intense emotions in adults and childrenÂ
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