Brexpiprazole

Brexpiprazole Brand Name– REXULTI

What is Brexpiprazole

Brexpiprazole is in an atypical antipsychotic drug subclass known as ‘dopamine system stabilizers’ (DSSs).

Similar to aripiprazole, brexpiprazole is a partial dopamine agonist, which is in contrast to other antipsychotic agents that are full dopamine antagonists.

Atypical antipsychotics are the standard of care for schizophrenia and related disorders, and with the exception of clozapine, are first-line treatment options for the management of psychosis.

In clinical trials for schizophrenia, brexpiprazole was superior to placebo in the primary efficacy endpoint of change from baseline to Week 6 in the Positive and Negative Syndrome Scale (PANSS) total score, which measures positive and negative symptoms of schizophrenia, and general psychopathology.

Brexpiprazole was also superior to placebo in a long-term maintenance trial assessing the safety and efficacy of brexpiprazole in delaying the time to relapse in adults with schizophrenia.

During clinical trials evaluating brexpiprazole as adjunctive treatment in major depressive disorder (MDD), brexpiprazole was superior to placebo in change from baseline to Week 6 in the Montgomery-Asberg Depression Rating Scale (MADRS), a 10-item clinician-related scale used to assess the degree of depressive symptomatology.

Patients were eligible for study enrollment if they met the criteria for MDD and had an inadequate response to prior antidepressant therapy (1 to 3 courses) in the current episode and who had also demonstrated an inadequate response throughout the 8 weeks of prospective antidepressant treatment.

Similar to aripiprazole, drugs having clinically important interactions with brexpiprazole include moderate to strong inhibitors of CYP3A4 and CYP2D6, and strong inducers of CYP3A4. In July 2015, the FDA approved brexpiprazole for the monotherapy treatment of schizophrenia in adults and as adjunctive treatment of major depressive disorder (MDD) in adults.

Indications

1. behavioral or psychological symptoms of dementia
2. depression
3. schizophrenia

Side Effects

1. abdominal pain
2. abnormal dreams
3. agranulocytosis
4. akathisia
5. anaphylactoid reactions
6. anxiety
7. appetite stimulation
8. blurred vision
9. constipation
10. depression
11. diabetes mellitus
12. diabetic ketoacidosis
13. diarrhea
14. dizziness
15. drowsiness
16. dyspepsia
17. dysphagia
18. dystonic reaction
19. fatigue
20. flatulence
21. headache
22. hyperglycemia
23. hyperhidrosis
24. hyperlipidemia
25. hyperprolactinemia
26. hypersalivation
27. hyperthermia
28. hypoglycemia
29. hyponatremia
30. hypothermia
31. impulse control symptoms
32. infection
33. insomnia
34. leukopenia
35. myalgia
36. neuroleptic malignant syndrome
37. neutropenia
38. orthostatic hypotension
39. pharyngitis
40. polydipsia
41. pseudoparkinsonism
42. rash
43. restlessness
44. seizures
45. SIADH
46. sinus tachycardia
47. stroke
48. suicidal ideation
49. syncope
50. tardive dyskinesia
51. tremor
52. urticaria
53. water intoxication
54. weight gain
55. weight loss
56. xerostomia

Monitoring Parameters

• AIMS assessment
• blood glucose
• CBC
• glycosylated hemoglobin A1c (HbA1c)
• LFTs
• neurologic function
• pregnancy testing
• serum creatinine
• serum electrolytes
• serum lipid profile
• serum prolactin
• thyroid function tests (TFTs)
• weight

Contraindications

• abrupt discontinuation
• agranulocytosis
• ambient temperature increase
• anticholinergic medications
• breast cancer
• breast-feeding
• cardiac disease
• cerebrovascular disease
• children
• coadministration with other CNS depressants
• coronary artery disease
• dehydration
• dementia
• diabetes mellitus
• diabetic ketoacidosis
• driving or operating machinery
• dysphagia
• ethanol ingestion
• geriatric
• heart failure
• hematological disease
• hepatic disease
• hyperglycemia
• hyperlipidemia
• hyperprolactinemia
• hyperthermia
• hypotension
• hypothermia
• hypovolemia
• impulse control symptoms
• infertility
• leukopenia
• myocardial infarction
• neonates
• neurological disease
• neutropenia
• obesity
• orthostatic hypotension
• Parkinson’s disease
• poor metabolizers
• pregnancy
• pregnancy testing
• renal disease
• renal failure
• renal impairment
• seizure disorder
• seizures
• strenuous exercise
• stroke
• suicidal ideation
• syncope
• tardive dyskinesia

Interactions

• Abiraterone
• Acarbose
• Acebutolol
• Acetaminophen; Butalbital
• Acetaminophen; Butalbital; Caffeine
• Acetaminophen; Butalbital; Caffeine; Codeine
• Acetaminophen; Caffeine; Dihydrocodeine
• Acetaminophen; Codeine
• Acetaminophen; Dichloralphenazone; Isometheptene
• Acetaminophen; Hydrocodone
• Acetaminophen; Oxycodone
• Acetaminophen; Pentazocine
• Acetaminophen; Tramadol
• Albiglutide
• Alfentanil
• Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
• Aliskiren; Hydrochlorothiazide, HCTZ
• Aliskiren; Valsartan
• Alogliptin
• Alogliptin; Metformin
• Alogliptin; Pioglitazone
• Alpha-blockers
• Alpha-glucosidase Inhibitors
• Alprazolam
• Amifampridine
• Amiloride
• Amiloride; Hydrochlorothiazide, HCTZ
• Amiodarone
• Amitriptyline
• Amitriptyline; Chlordiazepoxide
• Amlodipine; Benazepril
• Amlodipine; Celecoxib
• Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
• Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
• Amlodipine; Olmesartan
• Amlodipine; Telmisartan
• Amlodipine; Valsartan
• Amobarbital
• Amoxapine
• Amoxicillin; Clarithromycin; Lansoprazole
• Amoxicillin; Clarithromycin; Omeprazole
• Amprenavir
• Angiotensin II receptor antagonists
• Angiotensin-converting enzyme inhibitors
• Apalutamide
• Aprepitant, Fosaprepitant
• Aripiprazole
• Armodafinil
• Artemether; Lumefantrine
• Asenapine
• Aspirin, ASA; Butalbital; Caffeine
• Aspirin, ASA; Butalbital; Caffeine; Codeine
• Aspirin, ASA; Caffeine; Dihydrocodeine
• Aspirin, ASA; Carisoprodol; Codeine
• Aspirin, ASA; Oxycodone
• Atazanavir
• Atazanavir; Cobicistat
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• Atenolol; Chlorthalidone
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• Brompheniramine; Hydrocodone; Pseudoephedrine
• Bumetanide
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• Butabarbital
• Butorphanol
• Cabergoline
• Canagliflozin
• Canagliflozin; Metformin
• Candesartan
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• Cannabidiol
• Captopril
• Captopril; Hydrochlorothiazide, HCTZ
• Carbamazepine
• Carbetapentane; Chlorpheniramine
• Carbetapentane; Chlorpheniramine; Phenylephrine
• Carbetapentane; Diphenhydramine; Phenylephrine
• Carbetapentane; Guaifenesin
• Carbetapentane; Guaifenesin; Phenylephrine
• Carbetapentane; Phenylephrine
• Carbetapentane; Phenylephrine; Pyrilamine
• Carbetapentane; Pseudoephedrine
• Carbetapentane; Pyrilamine
• Carbidopa; Levodopa
• Carbidopa; Levodopa; Entacapone
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• Carbinoxamine; Hydrocodone; Pseudoephedrine
• Cariprazine
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• Chlorpheniramine; Dihydrocodeine; Phenylephrine
• Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
• Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
• Chlorpheniramine; Hydrocodone
• Chlorpheniramine; Hydrocodone; Phenylephrine
• Chlorpheniramine; Hydrocodone; Pseudoephedrine
• Chlorpromazine
• Chlorthalidone
• Chlorthalidone; Clonidine
• Cinacalcet
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• Clobazam
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• Codeine
• Codeine; Guaifenesin
• Codeine; Phenylephrine; Promethazine
• Codeine; Promethazine
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• Deutetrabenazine
• Dexamethasone
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• Dextromethorphan; Quinidine
• Dihydrocodeine; Guaifenesin; Pseudoephedrine
• Diltiazem
• Dipeptidyl Peptidase-4 Inhibitors
• Diphenhydramine; Hydrocodone; Phenylephrine
• Diuretics
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• Doxazosin
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• Dulaglutide
• Duloxetine
• Efavirenz
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• Elbasvir; Grazoprevir
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• Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
• Empagliflozin
• Empagliflozin; Linagliptin
• Empagliflozin; Linagliptin; Metformin
• Empagliflozin; Metformin
• Enalapril, Enalaprilat
• Enalapril; Felodipine
• Enalapril; Hydrochlorothiazide, HCTZ
• Entacapone
• Enzalutamide
• Eprosartan
• Eprosartan; Hydrochlorothiazide, HCTZ
• Ertugliflozin
• Ertugliflozin; Metformin
• Ertugliflozin; Sitagliptin
• Erythromycin
• Erythromycin; Sulfisoxazole
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• food
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• Gabapentin
• Ganirelix
• Glimepiride; Pioglitazone
• Glimepiride; Rosiglitazone
• Glipizide; Metformin
• Glyburide; Metformin
• Goserelin
• grapefruit juice
• Guaifenesin; Hydrocodone
• Guaifenesin; Hydrocodone; Pseudoephedrine
• Guanabenz
• Guanfacine
• Haloperidol
• Heterocyclic antidepressants
• Histrelin
• Homatropine; Hydrocodone
• Hydantoins
• Hydralazine; Hydrochlorothiazide, HCTZ
• Hydrochlorothiazide, HCTZ
• Hydrochlorothiazide, HCTZ; Irbesartan
• Hydrochlorothiazide, HCTZ; Lisinopril
• Hydrochlorothiazide, HCTZ; Losartan
• Hydrochlorothiazide, HCTZ; Methyldopa
• Hydrochlorothiazide, HCTZ; Metoprolol
• Hydrochlorothiazide, HCTZ; Moexipril
• Hydrochlorothiazide, HCTZ; Olmesartan
• Hydrochlorothiazide, HCTZ; Propranolol
• Hydrochlorothiazide, HCTZ; Quinapril
• Hydrochlorothiazide, HCTZ; Spironolactone
• Hydrochlorothiazide, HCTZ; Telmisartan
• Hydrochlorothiazide, HCTZ; Triamterene
• Hydrochlorothiazide, HCTZ; Valsartan
• Hydrocodone
• Hydrocodone; Ibuprofen
• Hydrocodone; Phenylephrine
• Hydrocodone; Potassium Guaiacolsulfonate
• Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
• Hydrocodone; Pseudoephedrine
• Hydromorphone
• Ibuprofen; Oxycodone
• Idelalisib
• Iloperidone
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• Incretin Mimetics
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• Meperidine; Promethazine
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• Metformin; Pioglitazone
• Metformin; Repaglinide
• Metformin; Rosiglitazone
• Metformin; Saxagliptin
• Metformin; Sitagliptin
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• Perphenazine
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• Phentolamine
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• Phenytoin
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